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Profile Name ERBB2 P761del
Gene Variant Detail

ERBB2 P761del (unknown)

Relevant Treatment Approaches

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
ERBB2 G776C lung non-small cell carcinoma predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 G776C demonstrated a partial response when treated with Pyrotinib (PMID: 30596880; NCT02535507). 30596880
ERBB2 P780_Y781insGSP lung non-small cell carcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, Kadcyla (ado-trastuzumab emtansine) treatment demonstrated limited efficacy in patients with relapsed non-small cell lung cancer harboring ERBB2 (Her2) mutations, resulting in stable disease in a patient harboring ERBB2 (HER2) P780_Y781insGSP (PMID: 29313813). 29313813
ERBB2 P780_Y781insGSP lung non-small cell carcinoma predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 P780_Y781insGSP demonstrated stable disease and progression-free survival for more than one year when treated with Pyrotinib (PMID: 30596880; NCT02535507). 30596880
ERBB2 G776_V777insVC ERBB2 over exp lung non-small cell carcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, a non-small cell lung cancer patient with ERBB2 overexpression (IHC 3+) and harboring ERBB2 G776_V777insVC demonstrated a partial response when treated with Kadcyla (ado-trastuzumab emtansine), with a duration of response of 7.3 months, a progression-free survival of 8.5 months, and an overall survival of 20.2 months (PMID: 30206164; NCT02289833). 30206164
ERBB2 G778_S779insCPG Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited growth of transformed cells expressing ERBB2 (HER2) G778_S779insCPG in culture (PMID: 28363995). 28363995
ERBB2 G778_S779insCPG lung adenocarcinoma no benefit Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, treatment with Kadcyla (trastuzumab emtansine) resulted in best overall responses of partial response in 44% (8/18) and stable disease in 39% (7/18), and median progression-free survival of 5 months in patients with lung adenocarcinoma harboring ERBB2 (HER2) activating mutations, but one patient specifically harboring a G778_S779insCPG mutation did not have a partial response (PMID: 29989854; NCT02675829). 29989854
ERBB2 H878Y Advanced Solid Tumor sensitive AEE788 Preclinical Actionable In a preclinical study, transformed cell lines expressing ERBB2 (HER2) H878Y demonstrated growth inhibition when treated with AEE788 in culture (PMID: 22046346). 22046346
ERBB2 H878Y Advanced Solid Tumor sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited proliferation of transformed cell lines expressing ERBB2 (HER2) H878Y in culture (PMID: 22046346). 22046346
ERBB2 E719G Advanced Solid Tumor sensitive Tesevatinib Preclinical Actionable In a preclinical study, XL647 inhibited survival of transformed cells over expressing ERBB2 (HER2) E719G in culture (PMID: 18413839). 18413839
ERBB2 E719G Advanced Solid Tumor decreased response Lapatinib Preclinical Actionable In a preclinical study, transformed cells over expressing ERBB2 (HER2) E719G demonstrated reduced sensitivity to Tykerb (lapatinib) in culture (PMID: 18413839). 18413839
ERBB2 G776_V777insYVMA Advanced Solid Tumor sensitive Canertinib Preclinical Actionable In a preclinical study, Canertinib inhibited Erbb2 (Her2) phosphorylation and cell growth in transformed human cell lines expressing ERBB2 (HER2) G776_V777insYVMA (PMID: 16843263). 16843263
ERBB2 exon 20 ins lung non-small cell carcinoma predicted - sensitive Docetaxel + Trastuzumab Case Reports/Case Series Actionable In a clinical study, treatment with the combination of Herceptin (trastuzumab) and Taxotere (docetaxel) in a non-small cell lung cancer patient harboring an ERBB2 exon 20 insertion resulted in a partial response (PMID: 23610105). 23610105
ERBB2 exon 20 ins lung non-small cell carcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a clinical study, targeted therapy with Gilotrif (afatinib) or Herceptin (trastuzumab) resulted in an objective response rate of 44% (4/9) in non-small cell lung carcinoma patients harboring ERBB2 (HER2) mutations that progressed during previous therapies, all four responders harbored ERBB2 (HER2) exon 20 insertions (PMID: 28167203). 28167203
ERBB2 exon 20 ins lung adenocarcinoma predicted - sensitive Dacomitinib Phase II Actionable In a Phase II trial, Vizimpro (dacomitinib) treatment resulted in an overall response rate of 25% (3/26) in patients with lung adenocarcinoma harboring ERBB2 (HER2) exon 20 mutations, including exon 20 insertions, indels, and missense mutations (23, 2, 1, respectively) (PMID: 25899785; NCT00818441). 25899785
ERBB2 exon 20 ins Her2-receptor negative breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in complete response in 1, partial response in 1, and stable disease in 3 of the 5 patients with Erbb2 (Her2)-receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) exon 20 insertion mutations (PMID: 29420467; NCT01953926). 29420467
ERBB2 exon 20 ins Advanced Solid Tumor sensitive AP32788 Preclinical - Pdx & cell culture Actionable In a preclinical study, AP32788 inhibited growth of transformed cell lines over expressing ERBB2 (HER2) exon 20 insertions in culture, and induced tumor regression in PDX models (AACR, Cancer Res: April 2016; Volume 57, Abstract #2644). detail...
ERBB2 exon 20 ins lung non-small cell carcinoma no benefit Neratinib Phase II Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease in 10 and progressive disease in 5 of the 15 patients with non-small cell lung cancer harboring ERBB2 (HER2) exon 20 insertion mutations (PMID: 29420467; NCT01953926). 29420467
ERBB2 exon 20 ins lung non-small cell carcinoma predicted - sensitive Carboplatin + Paclitaxel + Trastuzumab Case Reports/Case Series Actionable In a clinical study, treatment with the combination of Herceptin (trastuzumab), Paraplatin (carboplatin), and Taxol (paclitaxel) in non-small cell lung cancer patients harboring an ERBB2 exon 20 insertion (n=2) resulted in a partial response in one patient and stable disease in the other patient (PMID: 23610105). 23610105
ERBB2 exon 20 ins lung adenocarcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a clinical study, treatment with pulse Gilotrif (afatinib) resulted in an objective response rate of 33.3% (1/3) in lung adenocarcinoma patients with ERBB2 (HER2) exon 20 insertion mutations (PMID: 26964772). 26964772
ERBB2 exon 20 ins lung non-small cell carcinoma predicted - sensitive Trastuzumab Case Reports/Case Series Actionable In a clinical study, Herceptin (trastuzumab) treatment in a non-small cell lung cancer patient harboring an ERBB2 exon 20 insertion resulted in a partial response (PMID: 23610105). 23610105
ERBB2 exon 20 ins lung non-small cell carcinoma predicted - sensitive Trastuzumab Case Reports/Case Series Actionable In a clinical study, targeted therapy with Gilotrif (afatinib) or Herceptin (trastuzumab) resulted in an objective response rate of 44% (4/9) in non-small cell lung carcinoma patients harboring ERBB2 (HER2) mutations that progressed during previous therapies, all four responders harbored ERBB2 (HER2) exon 20 insertions (PMID: 28167203). 28167203
ERBB2 exon 20 ins lung non-small cell carcinoma predicted - sensitive Trastuzumab + Vinorelbine Case Reports/Case Series Actionable In a clinical study, treatment with the combination of Herceptin (trastuzumab) and Navelbine (vinorelbine) in non-small cell lung cancer patients harboring an ERBB2 exon 20 insertion (n=8) resulted in a partial response in 5 patients and stable disease in 2 patients (PMID: 23610105). 23610105
ERBB2 N813D lung adenocarcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a Phase II trial, Gilotrif (afatinib) treatment resulted in partial response in a patient with lung adenocarcinoma harboring ERBB2 (HER2) N813D (PMID: 30149884; NCT02979821). 30149884
ERBB2 T862A Advanced Solid Tumor sensitive AEE788 Preclinical Actionable In a preclinical study, AEE788 inhibited proliferation of transformed cell lines expressing ERBB2 (HER2) T862A in culture (PMID: 22046346). 22046346
ERBB2 T862A Advanced Solid Tumor decreased response Lapatinib Preclinical Actionable In a preclinical study, higher dose of Tykerb (lapatinib) inhibited proliferation of transformed cell lines expressing ERBB2 (HER2) N862A in culture (PMID: 22046346). 22046346
ERBB2 T798I lung cancer resistant Lapatinib Preclinical Actionable In a preclinical study, transformed lung cancer cells over expressing ERBB2 (HER2) T798I were resistant to Tykerb (lapatinib) in culture (PMID: 25238247). 25238247
ERBB2 T798I Advanced Solid Tumor sensitive Tesevatinib Preclinical Actionable In a preclinical study, XL647 inhibited survival of transformed cells over expressing ERBB2 (HER2) T798I in culture (PMID: 18413839). 18413839
ERBB2 T798I Advanced Solid Tumor resistant Lapatinib Preclinical Actionable In a preclinical study, transformed cells over expressing ERBB2 (HER2) T798I were resistant to Tykerb (lapatinib) in culture (PMID: 25238247). 25238247
ERBB2 K753E breast cancer resistant Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) K753E were resistant to Herceptin (trastuzumab) in culture (PMID: 27697991). 27697991
ERBB2 K753E breast cancer sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) K753 were sensitive to Nerlynx (neratinib) in culture, resulting in decreased colony formation (PMID: 27697991). 27697991
ERBB2 K753E breast cancer resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) K753E were resistant to Tykerb (lapatinib) in culture (PMID: 27697991). 27697991
ERBB2 over exp stomach cancer predicted - sensitive Trastuzumab deruxtecan Phase II Actionable In a Phase II trial (DESTINY-Gastric01), Enhertu (fam-trastuzumab deruxtecan-nxki) treatment improved objective response rate (51%, 61/119 vs 14%, 8/56, p<0.0001) and overall survival (12.5 vs 8.4 mo, HR=0.59, p=0.01) compared to chemotherapy in patients with advanced gastric cancer or gastroesophageal junction adenocarcinoma with high Erbb2 (Her2) expression (IHC 3+ or IHC 2+ plus ISH +), whose disease progressed after 2 or more prior therapies (PMID: 32469182; NCT03329690). 32469182
ERBB2 over exp Her2-receptor positive breast cancer sensitive Capecitabine + Trastuzumab + Tucatinib FDA approved Actionable In a Phase II trial (HER2CLIMB) that supported FDA approval, addition of Tukysa (tucatinib) to Herceptin (trastuzumab) and Xeloda (capecitabine) significantly improved progression-free survival at 1 year (PFS1) compared to placebo (33.1% vs 12.3%, HR=0.54, p<0.001) in patients with metastatic ERBB2 (HER2)-positive breast cancer who received prior HER2-targeted therapy, PFS1 was significantly improved (24.9% vs 0%, HR=0.48, p<0.001) in patients with brain metastasis (PMID: 31825569; NCT02614794). detail... 31825569
ERBB2 over exp Her2-receptor positive breast cancer sensitive Capecitabine + Trastuzumab + Tucatinib Guideline Actionable Tukysa (tucatinib), Herceptin (trastuzumab), and Xeloda (capecitabine) combination therapy is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive trastuzumab and hyaluronidase-oysk injection FDA approved - On Companion Diagnostic Actionable In a Phase III trial (HannaH) that supported FDA approval, Herceptin Hylecta (trastuzumab and hyaluronidase-oysk injection) treatment demonstrated safety and efficacy profile comparable to intravenous trastuzumab treatment, resulted in pathologic complete response in 45.4% (118/260) of patients with ERBB2 (HER2)-positive (IHC 3+ or ISH positive) breast cancer (PMID: 22884505; NCT00950300). detail... detail... 22884505
ERBB2 over exp stomach cancer sensitive MM-302 + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, combination of MM-302 and Herceptin (trastuzumab) resulted in improved tumor growth inhibition in cell line xenograft models of Erbb2 (Her2)-over expressing gastric cancer (PMID: 26759238). 26759238
ERBB2 over exp cholangiocarcinoma predicted - sensitive HER2 CAR-T cells Phase I Actionable In a Phase I trial, a patient with perihilar cholangiocarcinoma over expressing ERBB2 achieved a partial response and progression-free survival for 4.5 months following treatment with ERBB2 (HER2)-specific CAR-T cells (PMID: 28710747, NCT01935843). 28710747
ERBB2 over exp colorectal cancer decreased response Panitumumab Clinical Study - Cohort Actionable In a retrospective analysis, patients with metastatic KRAS exon 2 wild-type colorectal cancer harboring ERBB2 (HER2) amplification or overexpression (n=79) demonstrated poorer objective response rate (31.2 vs 46.9, p=0.031) and progression-free survival (5.7 vs 7 months, p=0.087) to anti-EGFR treatment (Vectibix (panitumumab) or Erbitux (cetuximab), as monotherapy or combined with chemotherapy) when compared to ERBB2 (HER2)-negative patients (n=113) (PMID: 30952821). 30952821
ERBB2 over exp breast cancer sensitive MM-302 + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, combination of MM-302 and Herceptin (trastuzumab) synergistically inhibited tumor growth in cell line xenograft models of Erbb2 (Her2)-over expressing breast cancer (PMID: 26759238). 26759238
ERBB2 over exp Her2-receptor positive breast cancer sensitive Trastuzumab Guideline Actionable Herceptin (trastuzumab) combined with a taxane, such as Taxotere (docetaxel) or Taxol (paclitaxel), is included in guidelines as neoadjuvant therapy for patients with ERBB2 (HER2)-positive early breast cancer or as first-line therapy for patients with ERBB2 (HER2)-positive advanced breast cancer (PMID: 31236598, PMID: 30032243; ESMO.org). detail... 31236598 30032243
ERBB2 over exp Her2-receptor positive breast cancer sensitive Trastuzumab FDA approved - On Companion Diagnostic Actionable Herceptin (trastuzumab) is FDA approved as an adjuvant treatment for ERBB2 (HER2)-overexpressing (or amplification) breast cancer patients and for metastatic ERBB2 (HER2)-overexpressing (or amplification) breast cancer patients as indicated by an FDA approved companion diagnostic (FDA.gov). detail... detail...
ERBB2 over exp stomach cancer sensitive MM-111 + Paclitaxel + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, MM-111, in combination with Herceptin (trastuzumab) and Taxol (paclitaxel), resulted in a synergistic effect thereby inhibiting ErbB2 in ERBB2 (HER2) over expressing gastric cancer cell line xenograft models (J Clin Oncol 31, 2013 (suppl 4; abstr 48)). detail...
ERBB2 over exp stomach cancer sensitive Dacomitinib Phase II Actionable In a Phase II trial, Vizimpro (dacomitinib) resulted in a 7.4% (2/27) response rate and 40.7% (11/27) disease control rate when treating advanced gastric cancer patients with ERBB2 (HER2) over expression (J Clin Oncol 30, 2012 (suppl 4; abstr 54)). detail...
ERBB2 over exp stomach cancer sensitive Dacomitinib Preclinical Actionable In a preclinical study, ERBB2 (HER2) over expressing gastric cancer cells were sensitive to Vizimpro (dacomitinib), resulting in inhibition of ERBB2 (HER2)/ERBB3 (HER3) heterodimers (PMID: 22135232). 22135232
ERBB2 over exp stomach cancer sensitive M802 Preclinical - Cell culture Actionable In a preclinical study, M802 inhibited growth of a gastric cancer cell line expressing high levels of ERBB2 (HER2) in culture, and inhibited tumor growth in xenograft models (PMID: 31412896). 31412896
ERBB2 over exp Her2-receptor positive breast cancer sensitive TAK-285 Preclinical - Cell line xenograft Actionable In a preclinical study, TAK-285 inhibited growth of breast cancer cell line harboring ERBB2 (HER2) over expression in culture and in cell line xenograft models (PMID: 23983820). 23983820
ERBB2 over exp Her2-receptor positive breast cancer sensitive Neratinib FDA approved Actionable In a Phase III trial that supported FDA approval, ERBB2 (HER2)-positive (overexpressing and/or amplification) breast cancer patients previously treated with Herceptin (trastuzumab) demonstrated a significantly greater two year invasive disease-free survival rate (93.9%) when treated with Nerlynx (neratinib) compared to the rate (91.6%) in those patients treated with placebo (PMID: 26874901; NCT00878709). 26874901 detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Neratinib Guideline Actionable Nerlynx (neratinib) is included in guidelines for patients with high-risk ERBB2 (HER2)-positive early breast cancer (PMID: 31236598; ESMO.org). 31236598 detail...
ERBB2 over exp salivary gland cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 80% (4/5, all partial response) of patients with salivary gland cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp Her2-receptor positive breast cancer sensitive Pertuzumab + Trastuzumab Guideline Actionable The combination of Herceptin (trastuzumab) and Perjeta (pertuzumab) with a taxane, such as Taxotere (docetaxel) or Taxol (palictaxel), is included in guidelines for patients with ERBB2 (HER2)-positive early breast cancer patients or advanced breast cancer (PMID: 31236598, PMID: 30032243; ESMO.org). 31236598 detail... 30032243
ERBB2 over exp stomach cancer sensitive Epertinib Phase I Actionable In a Phase I trial, S-222611 resulted in a complete response in a gastric-esophageal junction cancer patient overexpressing ERBB2 (HER2) and a partial response in a gastric cancer patient also overexpressing ERBB2 (HER2) (J Clin Oncol 33, 2015 (suppl; abstr 2511)). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Docetaxel + Pertuzumab + Trastuzumab FDA approved - On Companion Diagnostic Actionable In a Phase III trial (CLEOPATRA) that supported FDA approval, treatment with Perjeta (pertuzumab), combined with Herceptin (trastuzumab) and Taxotere (docetaxel), improved median progression free survival to 18.5 months compared to 12.4 months with placebo plus Herceptin (trastuzumab) and Taxotere (docetaxel) in patients with ERBB2 (HER2)-positive (overexpression and amplification) metastatic breast cancer (PMID: 23602601; NCT00567190). detail... 23602601 detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Docetaxel + Pertuzumab + Trastuzumab Guideline Actionable Perjeta (pertuzumab), Herceptin (trastuzumab), and Taxotere (docetaxel) therapy is included in the guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp pancreatic carcinoma predicted - sensitive HER2 CAR-T cells Phase I Actionable In a Phase I trial, treatment with ERBB2 (HER2)-specific CAR-T cells demonstrated safety and preliminary activity in patients with biliary tract or pancreatic carcinoma with ERBB2 (HER2) over expression, resulting in partial response in one of 11 patients and stable disease in 5, and a median progression free survival of 4.8 months (PMID: 28710747; NCT01935843). 28710747
ERBB2 over exp stomach cancer sensitive HER2 CAR-T cells Preclinical - Cell line xenograft Actionable In a preclinical study, ERBB2 (HER2)-specific CAR-T cells induced cell death in ERBB2 (HER2)-over expressing gastric cancer cell lines in culture, and inhibited tumor growth and improved survival in a ERBB2 (HER2)-over expressing gastric cancer cell line xenograft model (PMID: 28284008). 28284008
ERBB2 over exp estrogen-receptor positive breast cancer predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a clinical case study, Pyrotinib treatment resulted in stable disease for 4 months in a patient with advanced metastatic ER-positive, ERBB2 (HER2)-overexpressing breast cancer (PMID: 32547945). 32547945
ERBB2 over exp stomach cancer sensitive KU004 Preclinical Actionable In a preclinical study, KU004 inhibited growth and induced apoptosis in gastric cancer cell lines over expressing ERBB2 in culture and suppressed growth in a dose dependent manner in xenograft models (PMID: 26437915). 26437915
ERBB2 over exp stomach cancer sensitive Varlitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Varlitinib (ARRY-334543) resulted in a 74% tumor growth inhibition and tumor regression in 88% (7/8) of human cell line xenograft models of gastric cancer overexpressing ERBB2 (HER2) (Cancer Res January 15, 2009 69; 2150). detail...
ERBB2 over exp pancreatic cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 22% (2/9, all partial response) and stable disease lasting over 120 days in 11% (1/9) of patients with pancreatic cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp colorectal cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 38% (14/37, all partial response) and stable disease lasting over 120 days in 11% (4/37) of patients with colorectal cancer harboring ERBB2 (HER2) amplification or overexpression, with a median duration of response of 11 months (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp gastric adenocarcinoma predicted - sensitive Capecitabine + Lapatinib + Oxaliplatin Phase II Actionable In a Phase II trial, Tykerb (lapatinib), Xeloda (capecitabine), and Eloxatin (oxaliplatin) combination treatment resulted in a disease control rate of 81.3% (26/32, 7 complete response, 15 partial response, 4 stable disease) in patients with Erbb2 (Her2)-positive (defined as IHC3+ or IHC 2+ with ERBB2 amplification) gastric adenocarcinoma (PMID: 29409051; NCT02015169). 29409051
ERBB2 over exp Her2-receptor positive breast cancer sensitive Trazimera Preclinical Actionable In a preclinical study, PF-05280014 inhibited growth of ERBB2 (HER2)-over expressing breast cancer cells with activity comparable to Herceptin (trastuzumab) in culture (PMID: 25001079). 25001079
ERBB2 over exp stomach cancer sensitive MBS301 Preclinical - Cell line xenograft Actionable In a preclinical study, MBS301 inhibited proliferation of a gastric cancer cell line expressing high levels of ERBB2 (HER2) in culture, and inhibited tumor growth in xenograft models (PMID: 30081724). 30081724
ERBB2 over exp Her2-receptor positive breast cancer sensitive Trastuzumab + Vinorelbine Guideline Actionable Herceptin (trastuzumab) combined with Navelbine (vinorelbine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Trastuzumab + Vinorelbine Guideline Actionable The combination of Herceptin (trastuzumab) and Navelbine (vinorelbine) is included in guidelines as first-line therapy for patients with ERBB2 (HER2)-positive advanced breast cancer (PMID: 30032243; ESMO.org). 30032243 detail...
ERBB2 over exp biliary tract cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 29% (2/7, all partial response) and stable disease lasting over 120 days in 38% (3/7) of patients with biliary cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp Her2-receptor positive breast cancer sensitive Capecitabine + Lapatinib Guideline Actionable Tykerb (lapatinib) combined with Xeloda (capecitabine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp esophagus adenocarcinoma sensitive Trastuzumab Guideline Actionable Herceptin (trastuzumab), in combination with first-line chemotherapy with fluoropyrimidine and cisplatin or other chemotherapy agents, but not anthracyclines, is included in guidelines for Erbb2 (Her2)-overexpressing metastatic esophageal adenocarcinoma patients (NCCN.org) detail...
ERBB2 over exp ovarian cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 13% (1/8, all partial response) of patients with ovarian cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp breast cancer sensitive Trastuzumab-anns FDA approved - On Companion Diagnostic Actionable In a Phase I trial that supported FDA approval, the Herceptin (trastuzumab) biosimilar Kanjinti (Trastuzumab-anns) demonstrated structure, function, and pharmacokinetic profile comparable to Herceptin (trastuzumab) (PMID: 28341959), thus supporting the extrapolation of data from the Phase III trial that supported the approval of Herceptin (trastuzumab) in Erbb2 (Her2) overexpressing breast cancer (PMID: 23602601; NCT00567190) for approval of Kanjinti (Trastuzumab-anns) (FDA.gov). 23602601 detail... 28341959 detail... detail...
ERBB2 over exp pancreatic carcinoma sensitive ADC ST8176AA1 Preclinical - Pdx Actionable In a preclinical study, ADC ST8176AA1 treatment inhibited tumor growth in patient-derived xenograft (PDX) models of pancreatic carcinoma overexpressing ERBB2 (HER2) (PMID: 32039017). 32039017
ERBB2 over exp stomach cancer sensitive Ado-trastuzumab emtansine Preclinical - Cell line xenograft Actionable In a preclinical study, Kadcyla (trastuzumab emtansine) inhibited tumor growth in human cell line xenograft models of gastric cancer with ERBB2 (HER2) amplification and over expression (PMID: 21458915). 21458915
ERBB2 over exp Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine FDA approved - On Companion Diagnostic Actionable In a Phase III trial (EMILIA) that supported FDA approval, treatment with Kadclya (trastuzumab emtansine) improved median progression free survival (9.6 mo vs 6.4 mo) and overall survival (30.9 mo vs 25.1 mo) compared to Tykerb (lapatinib) combined with Xeloda (capecitabine) in patients with metastatic ERBB2 (HER2)-positive breast cancer (PMID: 24879797, PMID: 23020162; NCT00829166). 24879797 detail... detail... 23020162
ERBB2 over exp Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine FDA approved - On Companion Diagnostic Actionable In a Phase III trial (KATHERINE) that supported FDA approval, treatment with Kadclya (trastuzumab emtansine) resulted in improved invasive disease-free survival (HR=0.50, p<0.001) compared to Herceptin (trastuzumab) in patients with ERBB2 (HER2)-positive early breast cancer who had residual invasive disease after taxane and trastuzumab-based neoadjuvant therapy (PMID: 30516102; NCT01772472). detail... detail... 30516102
ERBB2 over exp Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine Guideline Actionable Kadcyla (ado-trastuzumab emtansine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine Guideline Actionable Kadcyla (ado-trastuzumab emtansine) is included in the guidelines for patients with ERBB2 (HER2)-positive advanced breast cancer who progressed through one line of Herceptin (trastuzumab)-based therapy or ERBB2 (HER2)-positive patients with early breast cancer (PMID: 31236598, PMID: 30032243; ESMO.org). 31236598 detail... 30032243
ERBB2 over exp Her2-receptor positive breast cancer sensitive Docetaxel + Trastuzumab Guideline Actionable Herceptin (trastuzumab) combined with Taxotere (docetaxel) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp breast cancer sensitive AV-412 Preclinical - Cell line xenograft Actionable In a preclinical study, AV-412 inhibited growth of ERBB2 (HER2)-over expressing breast cancer cell lines in culture, and inhibited tumor growth in a ERBB2 (HER2)-over expressing breast cancer cell line xenograft model (PMID: 17888033). 17888033
ERBB2 over exp uterine cancer no benefit Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in no objective response (0/7) in patients with uterine cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp Her2-receptor positive breast cancer sensitive Lapatinib Preclinical - Cell culture Actionable In a preclinical study, Tykerb (lapatinib) inhibited growth of HER2-over expressing breast carcinoma cell lines in culture (PMID: 27450453). 27450453
ERBB2 over exp Her2-receptor positive breast cancer sensitive Pertuzumab/trastuzumab/hyaluronidase-zzxf FDA approved Actionable In a Phase III trial (FeDeriCa) that supported FDA approval, Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) treatment in combination with chemotherapy in the neoadjuvant-adjuvant setting demonstrated safety and total pathological complete response rate (59.7% vs 59.5%) comparable to intravenous Perjeta (pertuzumab) and Herceptin (trastuzumab) plus chemotherapy in patients with ERBB2 (HER2)-positive early breast cancer (Cancer Res 2020;80(4 Suppl):Abstract nr PD4-07; NCT03493854). detail... detail...
ERBB2 over exp breast cancer sensitive ZW49 Preclinical - Pdx Actionable In a preclinical study, ZW49 treatment induced tumor regression in a patient-derived xenograft (PDX) model of breast cancer overexpressing ERBB2 (HER2) (Cancer Res 2019;79(4 Suppl):Abstract nr P6-17-13). detail...
ERBB2 over exp gastric adenocarcinoma sensitive VS-5584 Preclinical - Cell line xenograft Actionable In a preclinical study, VS-5584 inhibited tumor growth in human gastric cancer cell line xenograft models overexpressing ERBB2 (HER2) (PMID: 23270925). 23270925
ERBB2 over exp Her2-receptor positive breast cancer sensitive Carboplatin + Paclitaxel + Trastuzumab Guideline Actionable Herceptin combined with Paraplatin (carboplatin) and Taxol (paclitaxel) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive ADXS31-164 Preclinical Actionable In a preclinical study, ADXS31-164 prevented development of spontaneous mammary tumors in Erbb2 (Her2)-over expressing transgenic animal models (PMID: 20725099). 20725099
ERBB2 over exp breast cancer sensitive M802 Preclinical - Cell culture Actionable In a preclinical study, treatment with M802 increased apoptosis and inhibited growth of breast cancer cell lines expressing high levels of ERBB2 (HER2) in culture (PMID: 31412896). 31412896
ERBB2 over exp stomach cancer predicted - sensitive MM-302 Preclinical Actionable In a preclinical study, ERBB2 (HER2) over expressing gastric cancer xenograft models demonstrated anti-tumor activity when treated with MM-302 (Cancer Res December 15, 2010 70; P3-14-09). detail...
ERBB2 over exp gastroesophageal adenocarcinoma sensitive Trastuzumab-anns FDA approved - On Companion Diagnostic Actionable In a Phase I trial that supported FDA approval, the Herceptin (trastuzumab) biosimilar Kanjinti (Trastuzumab-anns) demonstrated structure, function, and pharmacokinetic profile comparable to Herceptin (trastuzumab) (PMID: 28341959), thus supporting the extrapolation of data from the Phase III trial that supported the approval of Herceptin (trastuzumab) in Erbb2 (Her2) overexpressing gastrioesophageal adenocarcinoma (PMID: 20728210; NCT01041404) for approval of Kanjinti (Trastuzumab-anns) (FDA.gov). 20728210 detail... 28341959 detail... detail...
ERBB2 over exp colorectal cancer resistant Cetuximab Preclinical - Cell line xenograft Actionable In a preclinical study, ERBB2 (HER2) over expression was associated with resistance to Erbitux (cetuximab) treatment in a human cell line xenograft model of colorectal cancer (PMID: 26296355). 26296355
ERBB2 over exp colorectal cancer resistant Cetuximab Clinical Study - Cohort Actionable In a retrospective analysis, patients with metastatic KRAS exon 2 wild-type colorectal cancer harboring ERBB2 (HER2) amplification or overexpression (n=79) demonstrated poorer objective response rate (31.2 vs 46.9, p=0.031) and progression-free survival (5.7 vs 7 months, p=0.087) to anti-EGFR treatment (Vectibix (panitumumab) or Erbitux (cetuximab), as monotherapy or combined with chemotherapy) when compared to ERBB2 (HER2)-negative patients (n=113) (PMID: 30952821). 30952821
ERBB2 over exp stomach cancer sensitive TAK-285 Preclinical Actionable In a preclinical study, the N87 gastric cancer cell line, which has been demonstrated to have ERBB2 (HER2) amplification and over expression, was sensitive to TAK-285, inhibiting phosphorylation of ERBB2 (HER2) and ERBB3 (HER3) (PMID: 25594012, PMID: 18441328). 18441328 25594012
ERBB2 over exp stomach cancer sensitive TAK-285 Preclinical - Cell line xenograft Actionable In a preclinical study, TAK-285 inhibited tumor growth in gastric cancer cell line xenograft models over expressing ERBB2 (HER2) (PMID: 23983820). 23983820
ERBB2 over exp Her2-receptor positive breast cancer sensitive CUDC-101 Phase I Actionable In a Phase I clinical trial, a breast cancer patient with ERBB2 (HER2) over expression that had progressed on Herceptin (trastuzumab) demonstrated stable disease for more than 12 weeks following treatment with CUDC-101 (PMID: 25107918). 25107918
ERBB2 over exp lung non-small cell carcinoma predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 13% (2/16, all partial response) and stable disease lasting over 120 days in 13% (2/16) of patients with non-small cell lung cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp biliary tract cancer predicted - sensitive HER2 CAR-T cells Phase I Actionable In a Phase I trial, treatment with ERBB2 (HER2)-specific CAR-T cells demonstrated safety and preliminary activity in patients with biliary tract or pancreatic carcinoma with ERBB2 (HER2) over expression, resulting in partial response in one of 11 patients and stable disease in 5, and a median progression free survival of 4.8 months (PMID: 28710747; NCT01935843). 28710747
ERBB2 over exp stomach cancer sensitive Trastuzumab + Varlitinib Preclinical - Cell line xenograft Actionable In a preclinical study, Varlitinib (ARRY-334543), in combination with Herceptin (trastuzumab), resulted in a 91% tumor growth inhibition and tumor regression in human cell line xenograft models of gastric cancer overexpressing ERBB2 (HER2) (Cancer Res January 15, 2009 69; 2150). detail...
ERBB2 over exp breast cancer sensitive KU004 Preclinical Actionable In a preclinical study, KU004 inhibited growth and induced apoptosis in breast cancer cell lines over expressing ERBB2 in culture (PMID: 26437915). 26437915
ERBB2 over exp stomach cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited growth of HER2-amplified and HER2-over expressing gastric cancer cell lines in culture (PMID: 18774637). 18774637
ERBB2 over exp urinary bladder cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 33% (3/9, 1 complete response, 1 partial response) and stable disease lasting over 120 days in 22% (2/9) of patients with bladder cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp gastric adenocarcinoma sensitive Trastuzumab Guideline Actionable Herceptin (trastuzumab) in combination with fluoropyrimidine and cisplatin (category 1) or other platinum agents (category 2A), but not anthracyclines, is included in guidelines as first-line therapy for Erbb2 (Her2)-overexpressing metastatic gastric adenocarcinoma patients (NCCN.org) detail...
ERBB2 over exp gastric adenocarcinoma sensitive Trastuzumab FDA approved - On Companion Diagnostic Actionable In a Phase III trial (ToGA) that supported FDA approval, patients with either gastric or gastroesophageal junction adenocarcinoma with ERBB2 (HER2) overexpression or ERBB2 (HER2) amplification had increased overall survival (13.8 mo vs 11.1 mo) when treated with Herceptin (trastuzumab) in combination with chemotherapy compared to chemotherapy alone (PMID: 20728210; NCT01041404). 20728210 detail... detail...
ERBB2 over exp gastroesophageal junction adenocarcinoma sensitive Epertinib Phase I Actionable In a Phase I trial, S-222611 resulted in a complete response in a gastric-esophageal junction cancer patient over expressing ERBB2 (HER2) and a partial response in a gastric cancer patient also over expressing ERBB2 (HER2) (J Clin Oncol 33, 2015 (suppl; abstr 2511)). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Capecitabine + Trastuzumab Guideline Actionable Herceptin (trastuzumab) combined with Xeloda (capecitabine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Trastuzumab deruxtecan Guideline Actionable Enhertu (fam-trastuzumab deruxtecan-nxki) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Trastuzumab-anns Phase III Actionable In a Phase III (LILAC) trial, Kanjinti (Trastuzumab-anns) treatment demonstrated safety and efficacy similar to Herceptin (trastuzumab) in neoadjuvant and adjuvant settings, resulted in a complete response in 48% (172/358) of patients with Erbb2 (Her2)-positive breast cancer, compared to 41% (137/338) in Herceptin (trastuzumab)-treated patients (PMID: 29880292; NCT01901146). 29880292
ERBB2 over exp Her2-receptor positive breast cancer predicted - sensitive Entinostat + Lapatinib Phase I Actionable In a Phase Ib trial, Entinostat and Tykerb (lapatinib) combination therapy resulted in complete response in 7.1% (1/14) and stable disease in 28.6% (4/14) of patients with ERBB2 (HER2)-positive breast cancer that progressed through Herceptin (trastuzumab) treatment (PMID: 31097774; NCT01434303). 31097774
ERBB2 over exp Her2-receptor positive breast cancer predicted - sensitive Entinostat + Lapatinib + Trastuzumab Phase I Actionable In a Phase Ib trial, combination treatment consisted of Entinostat, Tykerb (lapatinib) and Herceptin (trastuzumab) resulted in complete response in 9.5% (2/21), partial response in 14.3% (3/21), and stable disease in 38.1% (8/21) of patients with ERBB2 (HER2)-positive breast cancer that progressed through Herceptin (trastuzumab) treatment (PMID: 31097774; NCT01434303). 31097774
ERBB2 over exp Her2-receptor positive breast cancer sensitive NAX014 Preclinical Actionable In a preclinical study, NAX014 induced cellular senescence, prevented tumor growth, and decreased tumor volume in a Her2 positive breast cancer mouse model (PMID: 26168818). 26168818
ERBB2 over exp gastric adenocarcinoma sensitive Trastuzumab-anns FDA approved - On Companion Diagnostic Actionable In a Phase I trial that supported FDA approval, the Herceptin (trastuzumab) biosimilar Kanjinti (Trastuzumab-anns) demonstrated structure, function, and pharmacokinetic profile comparable to Herceptin (trastuzumab) (PMID: 28341959), thus supporting the extrapolation of data from the Phase III trial that supported the approval of Herceptin (trastuzumab) in Erbb2 (Her2) overexpressing gastric adenocarcinoma (PMID: 20728210; NCT01041404) for approval of Kanjinti (Trastuzumab-anns) (FDA.gov). 20728210 28341959 detail... detail... detail...
ERBB2 over exp Advanced Solid Tumor predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 26% (30/114, 2 complete response, 28 partial response) and stable disease lasting over 120 days in 14% (16/114) of patients with advanced solid tumors harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 over exp Her2-receptor positive breast cancer sensitive Lapatinib + Trastuzumab Guideline Actionable Herceptin (trastuzumab) combined with Tykerb (lapatinib) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Lapatinib + Trastuzumab Guideline Actionable The combination of Herceptin (trastuzumab) and Tykerb (lapatinib) is included in guidelines for patients with ERBB2 (HER2)-positive advanced breast cancer who progressed on Herceptin (trastuzumab)-based therapy, however, the combination therapy is not recommended as neoadjuvant therapy for ERBB2 (HER2)-positive patients with early breast cancer (PMID: 31236598, PMID: 30032243; ESMO.org). detail... 30032243 31236598
ERBB2 over exp stomach cancer sensitive BMS-690514 Preclinical Actionable In a preclinical study, BMS-690514 inhibited tumor growth in a gastric cancer xenograft model with ERBB2 (HER2) amplification and overexpression (PMID: 21531814). 21531814
ERBB2 over exp Her2-receptor positive breast cancer sensitive Capecitabine + Neratinib FDA approved Actionable In a Phase III (NALA) trial that supported FDA approval, combination of Nerlynx (neratinib) and Xeloda (capecitabine) reduced risk of disease progression or death (HR=0.76, p=0.006), improved 12-month PFS (28.8%, 88/307 vs 14.8%, 46/314) compared to lapatinib and capecitabine combination in patients with metastatic ERBB2 (HER2)-positive (amp/over exp) breast cancer who had 2 or more prior ERBB2 (HER2)-targeted therapies (J Clin Oncol 37, no. 15_suppl (May 20, 2019) 1002-1002; NCT01808573). detail...
ERBB2 over exp stomach cancer sensitive Tucatinib Preclinical - Cell culture Actionable In a preclinical study, Tukysa (tucatinib) inhibited proliferation of an ERBB2 (HER2) over expressing gastric cancer cell line in culture (Cancer Res April 15, 2010 70:3610). detail...
ERBB2 over exp Her2-receptor positive breast cancer predicted - sensitive Margetuximab Phase Ib/II Actionable In Phase I clinical trial, Margetuximab (MGAH22) displayed safety and had initial efficacy in patients with ERBB2 (HER2) positive breast cancer (J Clin Oncol 31, 2013 (suppl; abstr 3004)). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Paclitaxel + Pertuzumab + Trastuzumab Guideline Actionable Perjeta (pertuzumab), Herceptin (trastuzumab), and Taxol (paclitaxel) therapy is included in the guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2) receptor-positive breast cancer (NCCN.org). detail...
ERBB2 over exp Her2-receptor positive breast cancer sensitive Docetaxel + Pertuzumab/trastuzumab/hyaluronidase-zzxf FDA approved Actionable In a Phase III trial (FeDeriCa) that supported FDA approval, Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) demonstrated pharmacokinetics, safety, and efficacy comparable to i.v. pertuzumab and trastuzumab (H+P) (Cancer Res 2020;80(4 Suppl):Abstract nr PD4-07; NCT03493854), warranted the extrapolation of data from a Phase III trial supporting the approval of H+P plus docetaxel in Erbb2 (Her2)-positive metastatic breast cancer (PMID: 23602601; NCT00567190) for approval of Phesgo (FDA.gov). detail... detail... 23602601 detail...
ERBB2 over exp salivary gland carcinoma predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II (MyPathway) trial, Perjeta (pertuzumab) and Herceptin (trastuzumab) combination therapy resulted in an objective response rate of 60% (9/15, 1 complete response, 8 partial responses) and a clinical benefit rate of 67% (10/15) in patients with advanced salivary gland carcinoma harboring ERBB2 (HER2) amplification or overexpression, with a median progression- free survival of 8.6 months, and a median overall survival of 20.4 months (PMID: 32067683; NCT02091141). 32067683
ERBB2 over exp gastroesophageal junction adenocarcinoma sensitive Trastuzumab Guideline Actionable Herceptin (trastuzumab), in combination with fluoropyrimidine and cisplatin, or other chemotherapy agents, but not anthracyclines, is included in guidelines for Erbb2 (Her2)-overexpressing metastatic esophagogastric junction adenocarcinoma patients (NCCN.org) detail...
ERBB2 over exp gastroesophageal junction adenocarcinoma sensitive Trastuzumab FDA approved - On Companion Diagnostic Actionable In a Phase III trial (ToGA) that supported FDA approval, patients with either gastric cancer or gastroesophageal junction adenocarcinoma with ERBB2 (HER2) overexpression or ERBB2 (HER2) amplification had increased overall survival (13.8 mo vs 11.1 mo) when treated with Herceptin (trastuzumab) in combination with chemotherapy compared to chemotherapy alone (PMID: 20728210; NCT01041404). 20728210 detail... detail...
ERBB2 over exp gastroesophageal junction adenocarcinoma predicted - sensitive Trastuzumab deruxtecan Phase II Actionable In a Phase II trial (DESTINY-Gastric01), Enhertu (fam-trastuzumab deruxtecan-nxki) treatment improved objective response rate (51%, 61/119 vs 14%, 8/56, p<0.0001) and overall survival (12.5 vs 8.4 mo, HR=0.59, p=0.01) compared to chemotherapy in patients with advanced gastric cancer or gastroesophageal junction adenocarcinoma with high Erbb2 (Her2) expression (IHC 3+ or IHC 2+ plus ISH +), whose disease progressed after 2 or more prior therapies (PMID: 32469182; NCT03329690). 32469182
ERBB2 over exp lung non-small cell carcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, Kadcyla (ado-trastuzumab emtansine) treatment demonstrated limited efficacy in patients with relapsed non-small cell lung cancer harboring ERBB2 (Her2) overexpression (n=5) or amplification (n=3), resulting in stable disease as best response in 37.5% (3/8) of the patients (PMID: 29313813). 29313813
ERBB2 over exp lung non-small cell carcinoma predicted - sensitive Ado-trastuzumab emtansine Phase II Actionable In a Phase II trial, Kadcyla (ado-trastuzumab emtansine) treatment in non-small cell lung cancer patients who were ERBB2 positive (defined as IHC 2+ or IHC 3+) resulted in an objective response rate of 20% (4/20), with 4 partial responses, a median progression-free survival (PFS) of 2.7 mo, and a median overall survival (OS) of 15.3 mo in patients who were IHC 3+ (n=20) while patients who were IHC 2+ (n=29) had a median PFS of 2.6 mo, a median OS of 12.2 mo, and no responses (PMID: 30206164; NCT02289833). 30206164
ERBB2 over exp carcinoma predicted - sensitive Margetuximab Phase I Actionable In a Phase I trial, Margetuximab (MGAH22) treatment resulted in partial responses in 12% (7/60) and stable disease in 50% (30/60) of patients with ERBB2 (HER2)-positive breast or gastric cancer, or other carcinomas that overexpress Erbb2 (Her2) (PMID: 28119295). 28119295
ERBB2 over exp stomach cancer sensitive CDX-3379 Preclinical Actionable In a preclinical study, CDX-3379 (KTN3379) inhibited tumor growth by 43% in N87 gastric cancer xenograft model, which has been demonstrated to have ERBB2 (HER2) amplification and overexpression (AACR; 2015. Abstract nr 1558, PMID: 18441328). detail... 18441328
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer sensitive Buparlisib + Trastuzumab Preclinical Actionable In a preclinical study, the combination of Herceptin (trastuzumab) and Buparlisib (BKM120) inhibited tumor growth in mouse ERBB2 (HER2)-over expressing breast cancer models expressing PIK3CA H1047R, with moderate efficacy over Buparlisib (BKM120) alone (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R stomach cancer predicted - resistant Trastuzumab Clinical Study - Cohort Actionable In a clinical study (AMNESIA-1), assessment of pre-treatment tumor samples from ERBB2 (HER2)-positive gastric or gastroesophageal cancer patients (defined as HER2 IHC 3+ or HER2 IHC 2+/ISH+) identified PIK3CA mutations in 15% (3/20) of patients demonstrating primary resistance to Herceptin (trastuzumab), including 1 patient harboring PIK3CA H1047R (PMID: 29208673). 29208673
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer sensitive Bevacizumab + Buparlisib Preclinical Actionable In a preclinical study, treatment with Buparlisib (BKM120) resulted in decreased tumor growth, but not tumor regression, in mouse models of ERBB2 (HER2)-over expressing breast cancer expressing PIK3CA H1047R (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer sensitive Buparlisib + Pertuzumab + Trastuzumab Preclinical Actionable In a preclinical study, the combination of Buparlisib (BKM120), Herceptin (trastuzumab), and Perjeta (pertuzumab) inhibited tumor growth in mouse models of ERBB2 (HER2)-over expressing breast cancer expressing PIK3CA H1047R, with improved efficacy over Buparlisib (BKM120) alone (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer no benefit Buparlisib + Lapatinib + Trastuzumab Preclinical Actionable In a preclinical study, the combination of Buparlisib (BKM120), Herceptin (trastuzumab), and Tykerb (lapatinib) inhibited tumor growth in mouse models of ERBB2 (HER2)-over expressing breast cancer expressing PIK3CA H1047R, but efficacy was not significantly improved over Buparlisib (BKM120) alone (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer resistant Lapatinib + Trastuzumab Preclinical Actionable In a preclinical study, a mouse breast cancer model with mammary ERBB2 (HER2) over-expression that also expressed the PIK3CA H1047R mutation showed resistance to the combination of Herceptin (trastuzumab) and Tykerb (lapatinib) (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer resistant Pertuzumab + Trastuzumab Preclinical Actionable In a preclinical study, a mouse breast cancer model with ERBB2 (HER2) over-expression that also expressed the PIK3CA H1047R mutation showed resistance to the combination of Heceptin (trastuzumab) and Perjeta (pertuzumab) (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer resistant Trastuzumab Preclinical Actionable In a preclinical study, mouse breast cancer models over expressing ERBB2 (HER2) and expressing PIK3CA H1047R were resistant to Herceptin (trastuzumab) (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R SRC over exp urinary bladder cancer no benefit Lapatinib Preclinical - Pdx Actionable In a preclinical study, treatment with Tykerb (lapatinib) was not effective in inhibiting tumor growth in a patient-derived xenograft (PDX) model of bladder cancer with ERBB2 (HER2) over expression, which also over expressed SRC and harbored PIK3CA H1047R (PMID: 26270481). 26270481
ERBB2 over exp PIK3CA H1047R SRC over exp urinary bladder cancer no benefit Ponatinib Preclinical - Pdx Actionable In a preclinical study, treatment with Iclusig (ponatinib) was not effective in inhibiting tumor growth in a patient-derived xenograft (PDX) model of bladder cancer with SRC over expression, which also over expressed ERBB2 (HER2) and harbored PIK3CA H1047R (PMID: 26270481). 26270481
ERBB2 amp ERBB2 over exp stomach cancer sensitive Afatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Gilotrif (afatinib) induced tumor regression in a gastric cancer cell line xenograft model with HER2 (ERBB2) amplification and over expression (PMID: 23578997). 23578997
ERBB2 amp ERBB2 over exp lung non-small cell carcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, a non-small cell lung cancer patient with ERBB2 overexpression (IHC 3+) and ERBB2 amplification demonstrated a partial response when treated with Kadcyla (ado-trastuzumab emtansine), with a duration of response of 8.3 months, a progression-free survival of 9.6 months, and an overall survival of 21.6 months (PMID: 30206164; NCT02289833). 30206164
ERBB2 amp ERBB2 over exp stomach cancer sensitive Ado-trastuzumab emtansine Preclinical - Cell line xenograft Actionable In a preclinical study, Kadcyla (trastuzumab emtansine) inhibited tumor growth in human cell line xenograft models of gastric cancer with ERBB2 (HER2) amplification and over expression (PMID: 21458915). 21458915
ERBB2 over exp PIK3CA mut breast cancer sensitive Miransertib + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer xenograft model with ERBB2 (HER2) over expression and harboring a PIK3CA mutation was sensitive to the combination treatment of Miransertib (ARQ092) and Herceptin (trastuzumab), demonstrating greater inhibition of tumor growth when compared to treatment with either agent alone (PMID: 26469692). 26469692
ERBB2 over exp PIK3CA mut breast cancer sensitive Miransertib + Paclitaxel Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer xenograft model with ERBB2 (HER2) over expression and harboring a PIK3CA mutation was sensitive to the combination treatment of Miransertib (ARQ092) and Taxol (paclitaxel), demonstrating greater inhibition of tumor growth when compared to treatment with either agent alone (PMID: 26469692). 26469692
ERBB2 over exp PIK3CA mut Her2-receptor positive breast cancer sensitive PKI-179 Preclinical - Cell line xenograft Actionable In a preclinical study, PKI-179 inhibited growth of breast cancer cells harboring PIK3CA mutations and ERBB2 (HER2) over expression in culture and cell line xenograft models (PMID: 20797855). 20797855
ERBB2 over exp PIK3CA N345T stomach cancer predicted - resistant Trastuzumab Clinical Study - Cohort Actionable In a clinical study (AMNESIA-1), assessment of pre-treatment tumor samples from ERBB2 (HER2)-positive gastric or gastroesophageal cancer patients (defined as HER2 IHC 3+ or HER2 IHC 2+/ISH+) identified PIK3CA mutations in 15% (3/20) of patients demonstrating primary resistance to Herceptin (trastuzumab), including 1 patient harboring PIK3CA N345T (PMID: 29208673). 29208673
ERBB2 over exp PIK3CA H1047L stomach cancer predicted - resistant Trastuzumab Clinical Study - Cohort Actionable In a clinical study (AMNESIA-1), assessment of pre-treatment tumor samples from ERBB2 (HER2)-positive gastric or gastroesophageal cancer patients (defined as HER2 IHC 3+ or HER2 IHC 2+/ISH+) identified PIK3CA mutations in 15% (3/20) of patients demonstrating primary resistance to Herceptin (trastuzumab), including 1 patient harboring PIK3CA H1047L (PMID: 29208673). 29208673
ERBB2 over exp PIK3CA act mut Her2-receptor positive breast cancer decreased response Poziotinib Phase II Actionable In a Phase II trial, the presence of PIK3CA activating mutations including E542X, E545X, and H1047X correlated with shorter progression-free survival (2.66 months) compared to PIK3CA wild-type or other mutations (4.24 month, HR=1.68, p=0.033) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
ERBB2 over exp PIK3CA E542X Her2-receptor positive breast cancer decreased response Poziotinib Phase II Actionable In a Phase II trial, the presence of PIK3CA activating mutations including E542X, E545X, and H1047X correlated with shorter progression-free survival (2.66 months) compared to PIK3CA wild-type or other mutations (4.24 month, HR=1.68, p=0.033) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
ERBB2 over exp PIK3CA E545X Her2-receptor positive breast cancer decreased response Poziotinib Phase II Actionable In a Phase II trial, the presence of PIK3CA activating mutations including E542X, E545X, and H1047X correlated with shorter progression-free survival (2.66 months) compared to PIK3CA wild-type or other mutations (4.24 month, HR=1.68, p=0.033) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
ERBB2 over exp PIK3CA H1047X Her2-receptor positive breast cancer decreased response Poziotinib Phase II Actionable In a Phase II trial, the presence of PIK3CA activating mutations including E542X, E545X, and H1047X correlated with shorter progression-free survival (2.66 months) compared to PIK3CA wild-type or other mutations (4.24 month, HR=1.68, p=0.033) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
ERBB2 amp ERBB2 over exp ERBB2 rearrange lung non-small cell carcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, a non-small cell lung cancer patient with ERBB2 overexpression (IHC 3+), ERBB2 amplification, and an ERBB2 rearrangement demonstrated a partial response when treated with Kadcyla (ado-trastuzumab emtansine), with a duration of response of 10.8 months, a progression-free survival of 12.2 months, and an overall survival of 12.9 months (PMID: 30206164; NCT02289833). 30206164
ERBB2 wild-type Advanced Solid Tumor sensitive Osimertinib Preclinical Actionable In a preclinical study, Tagrisso (osimertinib) treatment resulted in antitumor efficacy in cells overexpressing wild-type ERBB2 (HER2), demonstrating inhibition of ERBB2 (HER2) phosphorylation and cell growth in culture and tumor regression in mouse models overexpressing wild-type ERBB2, with an 80% reduction in tumor volume (PMID: 29298799). 29298799
ERBB2 wild-type Advanced Solid Tumor sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited proliferation of transformed cell lines expressing wild-type ERBB2 (HER2) in culture (PMID: 22046346). 22046346
ERBB2 wild-type Advanced Solid Tumor sensitive AEE788 Preclinical Actionable In a preclinical study, AEE788 inhibited proliferation of transformed cell lines expressing wild-type ERBB2 (HER2) in culture (PMID: 22046346). 22046346
ERBB2 negative Her2-receptor negative breast cancer predicted - sensitive Exemestane + Seribantumab Phase II Actionable In a Phase II trial, Seribantumab (MM-12) and Aromasin (exemestane) combination treatment resulted in a 74% decrease in risk of progression (HR 0.26) and a a 59% decrease in risk of death (HR 0.436) compared to exemestane alone in ERBB2-negative, hormone receptor positive breast cancer patients (AACR Precision Medicine Series: Targeting the Vulnerabilities of Cancer, May 2016, Abstract # A14). detail...
ERBB2 negative Her2-receptor negative breast cancer predicted - sensitive Sorafenib + Vinorelbine Phase Ib/II Actionable In a Phase I/II trial, combination of Navelbine (vinorelbine) and Nexavar (sorafenib) resulted in a response rate of 30% (8/27), median progression free survival of 5.7 months, and a clinical benefit rate (absence of disease progression at 6 months) of 48% (13/27) in patients with ERBB2 (HER2)-negative metastatic breast cancer (PMID: 27992451). 27992451
ERBB2 negative Her2-receptor negative breast cancer no benefit Docetaxel + Ramucirumab Phase III Actionable In a Phase III trial, Cyramze (ramucirumab) in combination with Taxotere (docetaxel) did not improve clinical outcomes in ERBB2 (HER2)-negative breast cancer patients (PMID: 25185099). 25185099
ERBB2 neg ERBB2 pos Her2-receptor negative breast cancer sensitive Paclitaxel + RO4929097 Preclinical Actionable In a preclinical study, circulating tumor cells (CTC) from patients with ERBB2 (HER2)-negative breast cancer were demonstrated to contain both ERBB2 (HER2)-positive and ERBB2 (HER2)-negative subpopulations, and the combination of RO4929097 and Taxol (paclitaxel) resulted in increased tumor growth inhibition in CTC-derived xenograft models compared to either agent alone (PMID: 27556950). 27556950
ERBB2 neg ERBB2 pos Her2-receptor negative breast cancer sensitive LY411575 + Paclitaxel Preclinical Actionable In a preclinical study, circulating tumor cells (CTC) from patients with ERBB2 (HER2)-negative breast cancer were demonstrated to contain both ERBB2 (HER2)-positive and ERBB2 (HER2)-negative subpopulations, and the combination of LY411575 and Taxol (paclitaxel) resulted in increased tumor growth inhibition in CTC-derived xenograft models compared to either agent alone (PMID: 27556950). 27556950
ERBB2 V697L endometrial cancer predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.6 months in a patient with endometrial cancer harboring ERBB2 (HER2) V697L (PMID: 29420467; NCT01953926). 29420467
ERBB2 V697L Advanced Solid Tumor predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial, a patient with cancer of unknown primary involving the head and neck that harbored ERBB2 (HER2) V697L demonstrated a response to treatment with Nerlynx (neratinib) that lasted 13 months (PMID: 29247016). 29247016
ERBB2 V697L triple-receptor negative breast cancer sensitive Neratinib Phase II Actionable In a Phase II trial, a triple-negative breast cancer patient harboring ERBB2 V697L demonstrated a response to treatment with Nerlynx (neratinib) (PMID: 29247016). 29247016
ERBB2 E812K Advanced Solid Tumor sensitive Tesevatinib Preclinical Actionable In a preclinical study, XL647 inhibited survival of transformed cells over expressing ERBB2 (HER2) E812K in culture (PMID: 18413839). 18413839
ERBB2 E812K lung adenocarcinoma predicted - sensitive Poziotinib Case Reports/Case Series Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in stable disease in a patient with lung adenocarcinoma harboring ERBB2 (HER2) E812K (PMID: 30149884; NCT02979821). 30149884
ERBB2 E812K Advanced Solid Tumor decreased response Lapatinib Preclinical Actionable In a preclinical study, transformed cells over expressing ERBB2 (HER2) E812K demonstrated reduced sensitivity to Tykerb (lapatinib) in culture (PMID: 18413839). 18413839
ERBB2 L755S ERBB2 V777L ERBB2 R1153* urinary bladder cancer no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.7 months in a patient with bladder cancer harboring ERBB2 (HER2) L755S, R1153*, and V777L (PMID: 29420467; NCT01953926). 29420467
ERBB2 amp Her2-receptor positive breast cancer sensitive Capecitabine + Neratinib FDA approved Actionable In a Phase III (NALA) trial that supported FDA approval, combination of Nerlynx (neratinib) and Xeloda (capecitabine) reduced risk of disease progression or death (HR=0.76, p=0.006), improved 12-month PFS (28.8%, 88/307 vs 14.8%, 46/314) compared to lapatinib and capecitabine combination in patients with metastatic ERBB2 (HER2)-positive (amp/over exp) breast cancer who had 2 or more prior ERBB2 (HER2)-targeted therapies (J Clin Oncol 37, no. 15_suppl (May 20, 2019) 1002-1002; NCT01808573). detail... detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive Capecitabine + Neratinib Guideline Actionable Nerlynx (neratinib) combined with Xeloda (capecitabine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp gastric adenocarcinoma no benefit Lapatinib Phase III Actionable In a Phase III clinical trial, the addition of Tykerb (lapatinib) to Xeloda (capecitabine) and Eloxatin (oxaliplatin) combination treatment did not significantly prolong overall survival compared to placebo, but did improve progression-free survival and response rate in gastric adenocarcinoma patients harboring ERBB2 amplification (PMID: 26628478). 26628478
ERBB2 amp colorectal cancer resistant Trastuzumab Preclinical Actionable In a preclinical study, colorectal cancer tumorgrafts with ERBB2 (HER2) amplification demonstrated resistance to Herceptin (trastuzumab) treatment in animal models (PMID: 26296355). 26296355
ERBB2 amp stomach cancer sensitive Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, Herceptin (trastuzumab) inhibited tumor growth in human cell line xenograft models of gastric cancer with ERBB2 (HER2) amplification (PMID: 26296355). 26296355
ERBB2 amp colorectal cancer sensitive Cetuximab + Lapatinib Preclinical - Pdx Actionable In a preclinical study, the combination of Erbitux (cetuximab) and Tykerb (lapatinib) induced tumor regression in patient-derived xenograft (PDX) models of colorectal cancer with ERBB2 (HER2) amplification (PMID: 22586653). 22586653
ERBB2 amp stomach cancer sensitive Lapatinib Preclinical Actionable In preclinical studies, Tykerb (lapatinib) demonstrated antiproliferative activity in HER2-amplified gastric cancer in cell assays and in xenograft models (PMID: 20179222). 20179222
ERBB2 amp breast cancer sensitive Neratinib + Pertuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, breast cancer cell line xenograft models harboring ERBB2 (HER2) amplification were sensitive to the combination of Perjeta (pertuzumab) and Nerlynx (neratinib), resulting in a delay of brain lesion growth and improved survival (PMID: 28539475). 28539475
ERBB2 amp gastroesophageal junction adenocarcinoma sensitive Trastuzumab FDA approved - On Companion Diagnostic Actionable In a Phase III trial (ToGA) that supported FDA approval, patients with either gastric cancer or gastroesophageal junction adenocarcinoma with ERBB2 (HER2) overexpression or ERBB2 (HER2) amplification had increased overall survival (13.8 mo vs 11.1 mo) when treated with Herceptin (trastuzumab) in combination with chemotherapy compared to chemotherapy alone (PMID: 20728210; NCT01041404). 20728210 detail... detail...
ERBB2 amp urinary bladder cancer sensitive Afatinib Phase II Actionable In a Phase II clinical trial, patients with ERBB2 (HER2) amplified urothelial carcinoma had improved progression free survival when treated with Gilotrif (afatinib), and median PFS was 6.6 months for patients with ERBB2 or ERBB3 alterations relative to 1.4 months for patients lacking alterations (PMID: 27044931). 27044931
ERBB2 amp ovarian cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 13% (1/8, all partial response) of patients with ovarian cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp uterine corpus serous adenocarcinoma sensitive Trastuzumab Duocarmazine Preclinical Actionable In a preclinical study, Trastuzumab Duocarmazine (SYD895) induced cell death in ERBB2 (HER2)-amplified primary uterine serous carcinoma (USC) cell lines in culture and inhibited tumor growth and improved survival in ERBB2 (HER2)-amplified USC primary cell line xenografts (PMID: 27256376). 27256376
ERBB2 amp uterine corpus serous adenocarcinoma sensitive Neratinib + Taselisib Preclinical - Cell culture Actionable In a preclinical study, the combination of Taselisib (GDC-0032) and Nerlynx (neratinib) resulted in a synergistic effect, demonstrating greater cell growth inhibitory activity in uterine serous carcinoma cells harboring ERBB2 (HER2) amplification compared to either agent alone (PMID: 26333383). 26333383
ERBB2 amp Her2-receptor positive breast cancer sensitive CDX-3379 + Trastuzumab Preclinical Actionable In a preclinical study, the combination of Herceptin (trastuzumab) and CDX-3379 (KTN3379) inhibited tumor growth in xenograft models of ERBB2 (HER2)-amplified breast cancer, with increased efficacy compared to KTN3379 alone (PMID: 26880266). 26880266
ERBB2 amp Her2-receptor negative breast cancer sensitive Capecitabine + Lapatinib Guideline Actionable Tykerb (lapatinib) combined with Xeloda (capecitabine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp lung non-small cell carcinoma predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 13% (2/16, all partial response) and stable disease lasting over 120 days in 13% (2/16) of patients with non-small cell lung cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp Her2-receptor positive breast cancer sensitive Docetaxel + Trastuzumab Guideline Actionable Herceptin (trastuzumab) combined with Taxotere (docetaxel) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp biliary tract cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 29% (2/7, all partial response) and stable disease lasting over 120 days in 38% (3/7) of patients with biliary cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp salivary gland carcinoma predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II (MyPathway) trial, Perjeta (pertuzumab) and Herceptin (trastuzumab) combination therapy resulted in an objective response rate of 60% (9/15, 1 complete response, 8 partial responses) and a clinical benefit rate of 67% (10/15) in patients with advanced salivary gland carcinoma harboring ERBB2 (HER2) amplification or overexpression, with a median progression- free survival of 8.6 months, and a median overall survival of 20.4 months (PMID: 32067683; NCT02091141). 32067683
ERBB2 amp breast cancer sensitive Dacomitinib Preclinical Actionable In a preclinical study, Vizimpro (dacomitinib) was more effective in preventing proliferation in ERBB2 (HER2) amplified breast cancer cells than in wild-type ERBB2 (HER2) breast cancer cells (PMID: 22761403). 22761403
ERBB2 amp colorectal cancer decreased response Panitumumab Clinical Study - Cohort Actionable In a retrospective analysis, patients with metastatic KRAS exon 2 wild-type colorectal cancer harboring ERBB2 (HER2) amplification or overexpression (n=79) demonstrated poorer objective response rate (31.2 vs 46.9, p=0.031) and progression-free survival (5.7 vs 7 months, p=0.087) to anti-EGFR treatment (Vectibix (panitumumab) or Erbitux (cetuximab), as monotherapy or combined with chemotherapy) when compared to ERBB2 (HER2)-negative patients (n=113) (PMID: 30952821). 30952821
ERBB2 amp Her2-receptor positive breast cancer sensitive Lapatinib + Trastuzumab Guideline Actionable Herceptin (trastuzumab) combined with Tykerb (lapatinib) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp colorectal cancer sensitive Lapatinib + Pertuzumab Preclinical - Pdx Actionable In a preclinical study, the combination of Perjeta (pertuzumab) and Tykerb (lapatinib) induced tumor regression in patient-derived xenograft (PDX) models of colorectal cancer with ERBB2 (HER2) amplification (PMID: 22586653). 22586653
ERBB2 amp gastric adenocarcinoma sensitive Trastuzumab FDA approved - On Companion Diagnostic Actionable In a Phase III trial (ToGA) that supported FDA approval, patients with either gastric or gastroesophageal junction adenocarcinoma with ERBB2 (HER2) overexpression or ERBB2 (HER2) amplification had increased overall survival (13.8 mo vs 11.1 mo) when treated with Herceptin (trastuzumab) in combination with chemotherapy compared to chemotherapy alone (PMID: 20728210; NCT01041404). detail... 20728210 detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive CDX-3379 Preclinical Actionable In a preclinical study, CDX-3379 (KTN3379) inhibited tumor growth in xenograft models of ERBB2 (HER2)-amplified breast cancer (PMID: 26880266). 26880266
ERBB2 amp Her2-receptor positive breast cancer sensitive S63845 + Trastuzumab Preclinical - Pdx & cell culture Actionable In a preclinical study, S63845 and Herceptin (trastuzumab) demonstrated synergy in ERBB2 (HER2)-amplified breast cancer cells in culture and in ERBB2 (HER2)-amplified breast cancer patient-derived xenograft (PDX) models, resulting in enhanced tumor growth inhibition and overall survival compared to either agent alone (PMID: 28768804). 28768804
ERBB2 amp stomach cancer predicted - sensitive Afatinib + Trastuzumab Case Reports/Case Series Actionable In a Phase II clinical trial, a gastric cancer patient with ERBB2 (HER2) amplification who progressed on previous therapy demonstrated a 22% regression in a metastatic site when treated with a combination of Gilotrif (afatinib) and Herceptin (trastuzumab) (PMID: 30463996; NCT01522768). 30463996
ERBB2 amp pancreatic cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 22% (2/9, all partial response) and stable disease lasting over 120 days in 11% (1/9) of patients with pancreatic cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp breast cancer sensitive eFT226 Preclinical - Cell line xenograft Actionable In a preclinical study, eFT226 inhibited cell growth and induced apoptosis in a ERBB2 (HER2)-amplified breast cancer cell line in culture, and induced tumor regression in a cell line xenograft model (Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133). detail...
ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive BGB-283 Preclinical - Cell culture Actionable In a preclinical study, BGB-283 inhibited proliferation of ERBB2 (HER2) amplified breast cancer cells in culture (PMID: 26208524). 26208524
ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive Entinostat + Lapatinib + Trastuzumab Phase I Actionable In a Phase Ib trial, combination treatment consisted of Entinostat, Tykerb (lapatinib) and Herceptin (trastuzumab) resulted in complete response in 9.5% (2/21), partial response in 14.3% (3/21), and stable disease in 38.1% (8/21) of patients with ERBB2 (HER2)-positive breast cancer that progressed through Herceptin (trastuzumab) treatment (PMID: 31097774; NCT01434303). 31097774
ERBB2 amp uterine cancer no benefit Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in no objective response (0/7) in patients with uterine cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp Her2-receptor positive breast cancer sensitive Capecitabine + Trastuzumab Guideline Actionable Herceptin (trastuzumab) combined with Xeloda (capecitabine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive KRIBB11 + MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK-2206 and KRIBB11 synergistically inhibited growth of ERBB2 (HER2)-amplified breast cancer cell lines in culture (PMID: 28598816). 28598816
ERBB2 amp Her2-receptor positive breast cancer sensitive Neratinib Guideline Actionable Nerlynx (neratinib) is included in guidelines for ERBB2 (HER2)-positive patients with high-risk early breast cancer (PMID: 31236598; ESMO.org). detail... 31236598
ERBB2 amp Her2-receptor positive breast cancer sensitive Neratinib FDA approved Actionable In a Phase III trial that supported FDA approval, ERBB2 (HER2)-positive (overexpressing and/or amplification) breast cancer patients previously treated with Herceptin (trastuzumab) demonstrated a significantly greater two year invasive disease-free survival rate (93.9%) when treated with Nerlynx (neratinib) compared to the rate (91.6%) in those patients treated with placebo (PMID: 26874901; NCT00878709). 26874901 detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive Pertuzumab/trastuzumab/hyaluronidase-zzxf FDA approved Actionable In a Phase III trial (FeDeriCa) that supported FDA approval, Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) treatment in combination with chemotherapy in the neoadjuvant-adjuvant setting demonstrated safety and total pathological complete response rate (59.7% vs 59.5%) comparable to intravenous Perjeta (pertuzumab) and Herceptin (trastuzumab) plus chemotherapy in patients with ERBB2 (HER2)-positive early breast cancer (Cancer Res 2020;80(4 Suppl):Abstract nr PD4-07; NCT03493854). detail... detail...
ERBB2 amp colorectal cancer resistant Cetuximab Clinical Study - Cohort Actionable In a clinical study, ERBB2 (HER2) amplification was associated with resistance to Erbitux (cetuximab) in colorectal cancer patients (PMID: 21900593). 21900593
ERBB2 amp colorectal cancer resistant Cetuximab Clinical Study - Cohort Actionable In a retrospective analysis, patients with metastatic KRAS exon 2 wild-type colorectal cancer harboring ERBB2 (HER2) amplification or overexpression (n=79) demonstrated poorer objective response rate (31.2 vs 46.9, p=0.031) and progression-free survival (5.7 vs 7 months, p=0.087) to anti-EGFR treatment (Vectibix (panitumumab) or Erbitux (cetuximab), as monotherapy or combined with chemotherapy) when compared to ERBB2 (HER2)-negative patients (n=113) (PMID: 30952821). 30952821
ERBB2 amp Her2-receptor positive breast cancer sensitive Trastuzumab-anns Phase III Actionable In a Phase III (LILAC) trial, Kanjinti (Trastuzumab-anns) treatment demonstrated safety and efficacy similar to Herceptin (trastuzumab) in neoadjuvant and adjuvant settings, resulted in a complete response in 48% (172/358) of patients with Erbb2 (Her2)-positive breast cancer, compared to 41% (137/338) in Herceptin (trastuzumab)-treated patients (PMID: 29880292; NCT01901146). 29880292
ERBB2 amp stomach cancer predicted - sensitive Fluorouracil + Oxaliplatin + Trastuzumab Case Reports/Case Series Actionable In a Phase II clinical trial, a gastric cancer patient with ERBB2 (HER2) amplification demonstrated a response for 24 months when treated with the combination of Adrucil (fluorouracil), Eloxatin (oxaliplatin), and Herceptin (trastuzumab) (PMID: 30463996; NCT01522768). 30463996
ERBB2 amp Her2-receptor positive breast cancer sensitive Trastuzumab deruxtecan Guideline Actionable Enhertu (fam-trastuzumab deruxtecan-nxki) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp lung non-small cell carcinoma sensitive Afatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Gilotrif (afatinib) inhibited proliferation and induced cell-cycle arrest and apoptosis of non-small cell lung cancer (NSCLC) cell lines with ERBB2 (HER2) amplification in culture, and inhibited tumor growth in ERBB2 (HER2)-amplified NSCLC cell line xenograft models (PMID: 26545934). 26545934
ERBB2 amp scrotum Paget's disease predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II (MATCH) trial, Kadcyla (trastuzumab emtansine) treatment resulted in partial response in a patient with ERBB2 (HER2) amplified Paget’s disease of the scrotum (J Clin Oncol 36, 2018 (suppl; abstr 100); NCT02465060). detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine Guideline Actionable Kadcyla (ado-trastuzumab emtansine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine FDA approved - On Companion Diagnostic Actionable In a Phase III trial (EMILIA) that supported FDA approval, treatment with Kadclya (trastuzumab emtansine) improved median progression free survival (9.6 mo vs 6.4 mo) and overall survival (30.9 mo vs 25.1 mo) compared to Tykerb (lapatinib) combined with Xeloda (capecitabine) in patients with metastatic ERBB2 (HER2)-positive breast cancer (PMID: 24879797, PMID: 23020162; NCT00829166). 24879797 23020162 detail... detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine FDA approved - On Companion Diagnostic Actionable In a Phase III trial (KATHERINE) that supported FDA approval, treatment with Kadclya (trastuzumab emtansine) resulted in improved invasive disease-free survival (HR=0.50, p<0.001) compared to Herceptin (trastuzumab) in patients with ERBB2 (HER2)-positive early breast cancer who had residual invasive disease after taxane and trastuzumab-based neoadjuvant therapy (PMID: 30516102; NCT01772472). detail... detail... 30516102
ERBB2 amp Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine Guideline Actionable Kadcyla (ado-trastuzumab emtansine) is included in the guidelines for ERBB2 (HER2)-positive patients with advanced breast cancer who progressed through one line of Herceptin (trastuzumab)-based therapy or ERBB2 (HER2)-positive patients with early breast cancer (PMID: 31236598, PMID: 30032243; ESMO.org). detail... 31236598 30032243
ERBB2 amp Her2-receptor positive breast cancer sensitive Carboplatin + Paclitaxel + Trastuzumab Guideline Actionable Herceptin combined with Paraplatin (carboplatin) and Taxol (paclitaxel) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp colorectal cancer decreased response Lapatinib Preclinical - Pdx Actionable In a preclinical study, treatment with Tykerb (lapatinib) resulted in initial disease stabilization with subsequent progression, in patient-derived colorectal cancer tumorgraft models with ERBB2 (HER2) amplification (PMID: 26296355). 26296355
ERBB2 amp Her2-receptor positive breast cancer sensitive Docetaxel + Pertuzumab/trastuzumab/hyaluronidase-zzxf FDA approved Actionable In a Phase III trial (FeDeriCa) that supported FDA approval, Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) demonstrated pharmacokinetics, safety, and efficacy comparable to i.v. pertuzumab and trastuzumab (H+P) (Cancer Res 2020;80(4 Suppl):Abstract nr PD4-07; NCT03493854), warranted the extrapolation of data from a Phase III trial supporting the approval of H+P plus docetaxel in Erbb2 (Her2)-positive metastatic breast cancer (PMID: 23602601; NCT00567190) for approval of Phesgo (FDA.gov). detail... 23602601 detail... detail...
ERBB2 amp breast cancer sensitive Elgemtumab + Neratinib Preclinical - Cell line xenograft Actionable In a preclinical study, breast cancer cell line xenograft models harboring ERBB2 (HER2) amplification were sensitive to the combination of LJM716 and Nerlynx (neratinib), resulting in a delay of brain lesion growth and improved survival (PMID: 28539475). 28539475
ERBB2 amp lung adenocarcinoma no benefit Dacomitinib Case Reports/Case Series Actionable In a Phase II trial, Vizimpro (dacomitinib) treatment resulted in an overall response rate of 0% (0/4) in patients with lung adenocarcinoma harboring ERBB2 (HER2) amplification (PMID: 25899785; NCT00818441). 25899785
ERBB2 amp duodenum adenocarcinoma predicted - sensitive Fluorouracil + Leucovorin + Oxaliplatin + Trastuzumab Case Reports/Case Series Actionable In a clinical case study, a patient with duodenal adenocarcinoma harboring ERBB2 (HER2) amplification demonstrated a complete pathologic response after treatment with a combination of Herceptin (trastuzumab), Adrucil (fluorouracil), Wellcovorin (leucovorin), and Eloxatin (oxaliplatin) (PMID: 28784859). 28784859
ERBB2 amp Her2-receptor positive breast cancer sensitive trastuzumab and hyaluronidase-oysk injection FDA approved - On Companion Diagnostic Actionable In a Phase III trial (HannaH) that supported FDA approval, Herceptin Hylecta (trastuzumab and hyaluronidase-oysk injection) treatment demonstrated safety and efficacy profile comparable to intravenous trastuzumab treatment, resulted in pathologic complete response in 45.4% (118/260) of patients with ERBB2 (HER2)-positive (IHC 3+ or ISH positive) breast cancer (PMID: 22884505; NCT00950300). detail... detail... 22884505
ERBB2 amp breast cancer sensitive Lapatinib + Torkinib Preclinical - Cell culture Actionable In a preclinical study, the combination therapy of Tykerb (lapatinib) and Torkinib (PP242) in ERBB2 (HER2) amplified breast cancer cells in culture blocked cell growth, inhibited phosphorylation of Akt and S6, and led to greater caspase activity when compared to each agent alone (PMID: 27197158). 27197158
ERBB2 amp Her2-receptor positive breast cancer sensitive Trastuzumab FDA approved - On Companion Diagnostic Actionable Herceptin (trastuzumab) is FDA approved as an adjuvant treatment for ERBB2 (HER2)-overexpressing (or amplification) breast cancer patients and for metastatic ERBB2 (HER2)-overexpressing (or amplification) breast cancer patients as indicated by an FDA approved companion diagnostic (FDA.gov). detail... detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive Trastuzumab Clinical Study - Meta-analysis Actionable In a meta-analysis, breast cancer patients with >12 copies of ERBB2 (HER2) had a better response to Herceptin (trastuzumab) than patients with 6-12 copies of ERBB2 (HER2) (PMID: 24691421). 24691421
ERBB2 amp Her2-receptor positive breast cancer sensitive Trastuzumab Guideline Actionable Herceptin (trastuzumab) combined with a taxane, such as Taxotere (docetaxel) or Taxol (paclitaxel), is included in guidelines as neoadjuvant therapy for ERBB2 (HER2)-positive patients with early breast cancer or as first-line therapy for ERBB2 (HER2)-positive patients with advanced breast cancer (PMID: 31236598, PMID: 30032243; ESMO.org). 31236598 detail... 30032243
ERBB2 amp urinary bladder cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 33% (3/9, 1 complete response, 1 partial response) and stable disease lasting over 120 days in 22% (2/9) of patients with bladder cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp lung non-small cell carcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, Kadcyla (ado-trastuzumab emtansine) treatment demonstrated limited efficacy in patients with relapsed non-small cell lung cancer harboring ERBB2 (Her2) overexpression (n=5) or amplification (n=3), resulting in stable disease as best response in 37.5% (3/8) of the patients (PMID: 29313813). 29313813
ERBB2 amp Advanced Solid Tumor predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 26% (30/114, 2 complete response, 28 partial response) and stable disease lasting over 120 days in 14% (16/114) of patients with advanced solid tumors harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp breast cancer sensitive CYH33 Preclinical - Cell culture Actionable In a preclinical study, breast cancer cell lines harboring ERBB2 (HER2) amplification demonstrated increased sensitivity to CYH33 compared to cells with normal ERBB2 (HER2) expression in culture (p<0.05) (PMID: 30003928). 30003928
ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive Entinostat + Lapatinib Phase I Actionable In a Phase Ib trial, Entinostat and Tykerb (lapatinib) combination therapy resulted in complete response in 7.1% (1/14) and stable disease in 28.6% (4/14) of patients with ERBB2 (HER2)-positive breast cancer that progressed through Herceptin (trastuzumab) treatment (PMID: 31097774; NCT01434303). 31097774
ERBB2 amp gastrointestinal system cancer sensitive Dacomitinib Preclinical Actionable In a preclinical study, Vizimpro (dacomitinib) demonstrated significant growth-inhibitory effects in HER2- amplified gastric cancer cells (PMID: 18606718). 18606718
ERBB2 amp Her2-receptor positive breast cancer sensitive Docetaxel + Pertuzumab + Trastuzumab FDA approved - On Companion Diagnostic Actionable In a Phase III trial (CLEOPATRA) that supported FDA approval, treatment with Perjeta (pertuzumab), combined with Herceptin (trastuzumab) and Taxotere (docetaxel), improved median progression free survival to 18.5 months compared to 12.4 months with placebo plus Herceptin (trastuzumab) and Taxotere (docetaxel) in patients with ERBB2 (HER2)-positive (overexpression and amplification) metastatic breast cancer (PMID: 23602601; NCT00567190). 23602601 detail... detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive Docetaxel + Pertuzumab + Trastuzumab Guideline Actionable Perjeta (pertuzumab), Herceptin (trastuzumab), and Taxotere (docetaxel) therapy is included in the guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp breast cancer predicted - sensitive Neratinib + Temsirolimus Phase I Actionable In a Phase I clinical trial, Nerlynx (neratinib) administered with Torisel (temsirolimus) was tolerable and demonstrated antitumor activity in ERBB2 (HER2)-amplified breast cancer resistant to (Herceptin) trastuzumab (PMID: 24323026). 24323026
ERBB2 amp stomach cancer sensitive BMS-690514 Preclinical Actionable In a preclinical study, BMS-690514 inhibited tumor growth in a gastric cancer xenograft model with ERBB2 (HER2) amplification and overexpression (PMID: 21531814). 21531814
ERBB2 amp colorectal cancer sensitive Lapatinib + Trastuzumab Preclinical - Pdx Actionable In a preclinical study, the combination of Herceptin (trastuzumab) and Tykerb (lapatinib) treatment induced tumor regression in patient-derived colorectal cancer tumorgraft models harboring ERBB2 (HER2) amplification (PMID: 26296355). 26296355
ERBB2 amp colorectal cancer no benefit Pertuzumab Preclinical - Pdx Actionable In a preclinical study, Perjeta (pertuzumab) did not inhibit tumor growth in patient-derived xenograft (PDX) models of ERBB2 (HER2)-amplified colorectal cancer (PMID: 22586653). 22586653
ERBB2 amp breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of breast cancer cells with ERBB2 (HER2) amplification in culture (PMID: 21558396). 21558396
ERBB2 amp acral lentiginous melanoma sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a clinical case study, Kadcyla (trastuzumab emtansine) treatment resulted in complete radiographic response that lasted over 28 months in a patient with acral melanoma harboring ERBB2 (HER2) amplification (26-fold) that was resistant to check-point inhibition (PMID: 30093446). 30093446
ERBB2 amp Her2-receptor positive breast cancer sensitive TAS0728 Preclinical - Cell line xenograft Actionable In a preclinical study, TAS0728 inhibited Erbb2 downstream signaling and proliferation of ERBB2 (HER2) amplified breast cancer cell lines in culture, and induced tumor regression in cell line xenograft models (PMID: 30787176). 30787176
ERBB2 amp Advanced Solid Tumor sensitive Afatinib Phase II Actionable In a Phase II trial, Gilotrif (afatinib), demonstrated safety and efficacy in various advanced solid tumor patients with ERBB2 (HER2) amplification (PMID: 23775486). 23775486
ERBB2 amp uterine corpus serous adenocarcinoma sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, a uterine serous carcinoma cell line harboring ERBB2 (HER2) amplification demonstrated sensitivity to treatment with Nerlynx (neratinib) in culture, resulting in inhibition of cell growth (PMID: 26333383). 26333383
ERBB2 amp breast cancer sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line xenograft model harboring ERBB2 (HER2) amplification demonstrated tumor regression within the mammary fat pad when treated with Buparlisib (BKM120) (PMID: 28539475). 28539475
ERBB2 amp lung cancer sensitive Lapatinib Preclinical - Cell culture Actionable In a preclinical study, Tykerb (lapatinib) treatment reduced viability of a lung cancer cell line harboring an ERBB2 (HER2) amplification in culture (PMID: 30674502). 30674502
ERBB2 amp colorectal cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 38% (14/37, all partial response) and stable disease lasting over 120 days in 11% (4/37) of patients with colorectal cancer harboring ERBB2 (HER2) amplification or overexpression, with a median duration of response of 11 months (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp breast cancer sensitive Elgemtumab + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, breast cancer cell line xenograft models harboring ERBB2 (HER2) amplification were sensitive to the combination of Herceptin (trastuzumab) and LJM716, resulting in a delay of brain lesion growth and improved survival (PMID: 28539475). 28539475
ERBB2 amp stomach carcinoma no benefit Debio 1347 Preclinical - Cell line xenograft Actionable In a preclinical study, Debio 1347 did not inhibit tumor growth in cell line xenograft models of ERBB2 (HER2) amplified gastric carcinoma (PMID: 26438159). 26438159
ERBB2 amp Her2-receptor positive breast cancer sensitive Trastuzumab + Vinorelbine Guideline Actionable Herceptin (trastuzumab) combined with Navelbine (vinorelbine) is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp Her2-receptor positive breast cancer sensitive Trastuzumab + Vinorelbine Guideline Actionable The combination of Herceptin (trastuzumab) and Navelbine (vinorelbine) is included in guidelines as first-line therapy for ERBB2 (HER2)-positive patients with advanced breast cancer (PMID: 30032243; ESMO.org). 30032243 detail...
ERBB2 amp stomach cancer sensitive Poziotinib Preclinical Actionable In a preclinical study, Poziotinib suppressed cell growth, decreased phosphorylation of downstream signaling molecules, and induced apoptosis of human gastric cancer cells harboring ERBB2 (HER2) amplification (PMID: 21306821). 21306821
ERBB2 amp lung cancer predicted - sensitive TAS0728 Preclinical - Cell culture Actionable In a preclinical study, TAS0728 inhibited Erbb2 downstream signaling and proliferation of ERBB2 (HER2) amplified lung cancer cells in culture (PMID: 30787176). 30787176
ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive Poziotinib Phase II Actionable In a Phase II trial, increased copy number (CN) of ERBB2 (HER2) was associated with improved response to Poziotinib (HM781-36B) treatment in patients with Erbb2 (Her2)-positive breast cancer, with a median progression-free survival of 4.86 months in patients with CN over 8 and 2.99 months in patients with CN equal to or less than 8 (HR=0.61, p=0.037) (PMID: 30720867, NCT02418689). 30720867
ERBB2 amp Her2-receptor positive breast cancer sensitive Pertuzumab + Trastuzumab Guideline Actionable The combination of Herceptin (trastuzumab) and Perjeta (pertuzumab) with a taxane, such as Taxotere (docetaxel) or Taxol (palictaxel), is included in guidelines for ERBB2 (HER2)-positive patients with early breast cancer patients or advanced breast cancer (PMID: 31236598, PMID: 30032243; ESMO.org). detail... 31236598 30032243
ERBB2 amp stomach cancer sensitive TAS0728 Preclinical - Cell line xenograft Actionable In a preclinical study, TAS0728 inhibited Erbb2 downstream signaling and proliferation of ERBB2 (HER2) amplified gastric cancer cells in culture, and induced tumor regression in cell line xenograft models (PMID: 30787176). 30787176
ERBB2 amp breast cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited proliferation of breast cancer cell lines with ERBB2 (HER2) amplification in culture (PMID: 26545934). 26545934
ERBB2 amp vulva squamous cell carcinoma sensitive Depatuxizumab mafodotin Preclinical - Cell line xenograft Actionable In a preclinical study, ABT-414 demonstrated cytoxicity against a EGFR-amplified vulvar epidermoid carcinoma cell line in culture and induced tumor regression in EGFR-amplified vulvar epidermoid carcinoma cell line xenograft models (PMID: 26846818). 26846818
ERBB2 amp colorectal adenocarcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a clinical case study, a patient with metastatic colorectal adenocarcinoma harboring ERBB2 (HER2) amplification demonstrated clinical benefit with stable disease in the primary tumor for 7 months following treatment with Kadcyla (trastuzumab emtansine) (PMID: 28040715). 28040715
ERBB2 amp Her2-receptor positive breast cancer sensitive Capecitabine + Trastuzumab + Tucatinib FDA approved Actionable In a Phase II trial (HER2CLIMB) that supported FDA approval, addition of Tukysa (tucatinib) to Herceptin (trastuzumab) and Xeloda (capecitabine) significantly improved progression-free survival at 1 year (PFS1) compared to placebo (33.1% vs 12.3%, HR=0.54, p<0.001) in patients with metastatic ERBB2 (HER2)-positive breast cancer who received prior HER2-targeted therapy, PFS1 was significantly improved (24.9% vs 0%, HR=0.48, p<0.001) in patients with brain metastasis (PMID: 31825569; NCT02614794). detail... 31825569
ERBB2 amp Her2-receptor positive breast cancer sensitive Capecitabine + Trastuzumab + Tucatinib Guideline Actionable Tukysa (tucatinib), Herceptin (trastuzumab), and Xeloda (capecitabine) combination therapy is included in guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp gastroesophageal junction adenocarcinoma no benefit Lapatinib Phase III Actionable In a Phase III clinical trial, the addition of Tykerb (lapatinib) to Xeloda (capecitabine) and Eloxatin (oxaliplatin) combination treatment did not significantly prolong overall survival compared to placebo, but did improve progression-free survival and response rate in gastroesophageal junction adenocarcinoma patients harboring ERBB2 amplification (PMID: 26628478). 26628478
ERBB2 amp Her2-receptor positive breast cancer sensitive Lapatinib + S63845 Preclinical - Cell culture Actionable In a preclinical study, the combination of Tykerb (lapatinib) and S63845 demonstrated synergy in an ERBB2 (HER2)-amplified breast cancer cell line in culture, resulting in decreased cell viability (PMID: 28768804). 28768804
ERBB2 amp Her2-receptor positive breast cancer sensitive Paclitaxel + Pertuzumab + Trastuzumab Guideline Actionable Perjeta (pertuzumab), Herceptin (trastuzumab), and Taxol (paclitaxel) therapy is included in the guidelines as systemic therapy for patients with recurrent or metastatic hormone receptor-positive (ER and/or PR) or negative, ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 amp parotid gland cancer predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II (MATCH) trial, Kadcyla (trastuzumab emtansine) treatment resulted in partial response in a patient with ERBB2 (HER2) amplified salivary duct carcinoma of the parotid gland and a patient with ERBB2 (HER2) amplified squamous cell carcinoma of the parotid gland (J Clin Oncol 36, 2018 (suppl; abstr 100); NCT02465060). detail...
ERBB2 amp breast cancer sensitive Torkinib Preclinical - Cell culture Actionable In a preclinical study, ERBB2 (HER2) amplified breast cancer cells treated with Torkinib (PP242) demonstrated some efficacy in culture including reduced phosphorylation of S6 and Akt, apoptosis, and decreased cell growth (PMID: 27197158). 27197158
ERBB2 amp uterine corpus serous adenocarcinoma sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, a uterine serous carcinoma cell line harboring ERBB2 (HER2) amplification demonstrated sensitivity to treatment with Taselisib (GDC-0032) in culture, resulting in inhibition of cell growth (PMID: 26333383). 26333383
ERBB2 amp gastric adenocarcinoma predicted - sensitive Capecitabine + Lapatinib + Oxaliplatin Phase II Actionable In a Phase II trial, Tykerb (lapatinib), Xeloda (capecitabine), and Eloxatin (oxaliplatin) combination treatment resulted in a disease control rate of 81.3% (26/32, 7 complete response, 15 partial response, 4 stable disease) in patients with Erbb2 (Her2)-positive (defined as IHC3+ or IHC 2+ with ERBB2 amplification) gastric adenocarcinoma (PMID: 29409051; NCT02015169). 29409051
ERBB2 amp lung squamous cell carcinoma resistant Gefitinib Preclinical Actionable In a preclinical study, a lung squamous cell carcinoma cell line with ERBB2 (HER2) amplification demonstrated resistance to treatment with Iressa (gefitinib) in culture (PMID: 26545934). 26545934
ERBB2 amp breast cancer sensitive Pertuzumab + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, breast cancer cell line xenograft models harboring ERBB2 (HER2) amplification were sensitive to the combination of Herceptin (trastuzumab) and Perjeta (pertuzumab), resulting in a delay of brain lesion growth and improved survival (PMID: 28539475). 28539475
ERBB2 amp salivary gland cancer predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 80% (4/5, all partial response) of patients with salivary gland cancer harboring ERBB2 (HER2) amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 amp stomach cancer sensitive Lapatinib + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Herceptin (trastuzumab) and Tykerb (lapatinib) treatment induced tumor regression in ERBB2 (HER2)-amplified cell line xenograft models of gastric cancer (PMID: 26296355). 26296355
ERBB2 amp esophagus adenocarcinoma no benefit Lapatinib Phase III Actionable In a Phase III clinical trial, the addition of Tykerb (lapatinib) to Xeloda (capecitabine) and Eloxatin (oxaliplatin) combination treatment did not significantly prolong overall survival compared to placebo, but did improve progression-free survival and response rate in esophagus adenocarcinoma patients harboring ERBB2 amplification (PMID: 26628478). 26628478
ERBB2 amp Her2-receptor positive breast cancer sensitive Palbociclib + Trastuzumab Preclinical Actionable In a preclinical study, the combination of Ibrance (palbociclib) and Herceptin (trastuzumab) worked synergistically to inhibit growth of ERBB2 (HER2)-amplified breast cancer cells in culture (PMID: 19874578). 19874578
ERBB2 amp breast cancer decreased response Lapatinib Preclinical - Cell culture Actionable In a preclinical study, ERBB2 (HER2) amplified breast cancer cells treated with Tykerb (lapatinib) demonstrated decreased phosphorylation of Erbb2 (her2) and Akt, however, after 4-8 hours, Akt-driven Rictor showed upregulation, thereby resulting in a decreased treatment response (PMID: 27197158). 27197158
ERBB2 amp esophageal cancer sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, esophageal cancer cells with ERBB2 (HER2) amplification demonstrated sensitivity to Imbruvica (ibrutinib), resulting in decreased survival in culture (PMID: 28830912). 28830912
ERBB2 amp breast cancer sensitive Lapatinib + S63845 Preclinical - Cell culture Actionable In a preclinical study, the combination of S63845 and Tykerb (lapatinib) resulted in potent cytotoxic effects in ERBB2 (HER2)-amplified breast cancer cells in culture compared to the cytostatic effect of Tykerb (lapatinib) alone (PMID: 27760111). 27760111
ERBB2 amp Advanced Solid Tumor predicted - sensitive Ado-trastuzumab emtansine Phase II Actionable In a Phase II (MATCH) trial, Kadcyla (trastuzumab emtansine) treatment resulted in partial response in 8.1% (3/37) and stable disease in 43% (16/37) of patients with ERBB2 (HER2) amplified non-breast, non-gastric advanced solid tumors, with a 6-month progression-free survival rate of 24.8% (J Clin Oncol 36, 2018 (suppl; abstr 100); NCT02465060). detail...
ERBB2 amp FGFR2 wild-type stomach cancer resistant AZD4547 Preclinical Actionable In a preclinical study, gastric cancer cells with wild-type FGFR2 and ERBB2 (HER2) amplification were resistant to treatment with AZD4547 in culture (PMID: 22869148). 22869148
ERBB2 amp PIK3CA C420R breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R and ERBB2 (HER2) amplification (PMID: 21558396). 21558396
ERBB2 amp PIK3CA C420R breast cancer sensitive CYH33 Preclinical - Cell culture Actionable In a preclinical study, CYH33 inhibited proliferation of breast cancer cell lines harboring PIK3CA C420R and ERBB2 (HER2) amplification in culture (PMID: 30003928). 30003928
ERBB2 amp PIK3CA N345K breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA N345K and ERBB2 (HER2) amplification in culture (PMID: 21558396). 21558396
ERBB2 amp PIK3CA H1047R breast cancer sensitive CYH33 Preclinical - Cell culture Actionable In a preclinical study, CYH33 inhibited proliferation of breast cancer cell lines harboring PIK3CA H1047R and ERBB2 (HER2) amplification in culture (PMID: 30003928). 30003928
ERBB2 amp PIK3CA H1047R breast cancer sensitive Gedatolisib Preclinical Actionable In a preclinical study, Gedatolisib (PKI-587) inhibited growth of human breast cancer cells harboring ERBB2 (HER2) amplification and PIK3CA H1047R in culture (PMID: 21325073, PMID: 17314276). 17314276 21325073
ERBB2 amp PIK3CA H1047R breast cancer sensitive CH5132799 + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of CH5132799 and Herceptin (trastuzumab) inhibited tumor growth and overcame Herceptin (trastuzumab) insensitivity in xenograft models of a human breast cancer cell line harboring PIK3CA H1047R and ERBB2 (HER2) amplification (PMID: 21558396). 21558396
ERBB2 amp PIK3CA H1047R ovarian cancer sensitive CH5132799 Preclinical - Cell line xenograft Actionable In a preclinical study, CH5132799 inhibited cell growth in a human ovarian cancer cell line harboring PIK3CA H1047R and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). 21558396
ERBB2 amp PIK3CA H1047R breast cancer sensitive CH5132799 Preclinical - Cell line xenograft Actionable In a preclinical study, CH5132799 inhibited cell growth and Akt phosphorylation, and promoted apoptosis in a human breast cancer cell line harboring PIK3CA H1047R and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). 21558396
ERBB2 amp PIK3CA K111N breast cancer predicted - sensitive CYH33 Preclinical - Cell culture Actionable In a preclinical study, CYH33 inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N and ERBB2 (HER2) amplification in culture (PMID: 30003928). 30003928
ERBB2 amp PIK3CA K111N breast cancer sensitive CH5132799 Preclinical - Cell line xenograft Actionable In a preclinical study, CH5132799 inhibited cell growth and Akt phosphorylation, and promoted apoptosis in a human breast cancer cell line harboring PIK3CA K111N and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). 21558396
ERBB2 amp PIK3CA E545K breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA E545K and ERBB2 (HER2) amplification in culture (PMID: 21558396). 21558396
ERBB2 amp PIK3CA E545K breast cancer predicted - sensitive CYH33 Preclinical - Cell culture Actionable In a preclinical study, CYH33 inhibited proliferation of a breast cancer cell line harboring PIK3CA E545K and ERBB2 (HER2) amplification in culture (PMID: 30003928). 30003928
ERBB2 amp PIK3CA E545K breast cancer sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line xenograft model co-harboring ERBB2 (HER2) amplification and PIK3CA E545K demonstrated tumor regression within the mammary fat pad when treated with Buparlisib (BKM120) (PMID: 28539475). 28539475
ERBB2 amp PIK3CA E545K PIK3CA K567R Her2-receptor positive breast cancer sensitive Gedatolisib Preclinical - Cell line xenograft Actionable In a preclinical study, Gedatolisib (PKI-587) inhibited PI3K signaling, cell growth and induced apoptosis in human breast cancer cells harboring ERBB2 (HER2) amplification, PIK3CA E545K, and PIK3CA K567R in culture and in cell line xenografts (PMID: 21325073, PMID: 17314276). 17314276 21325073
ERBB2 amp PIK3CA mut uterine corpus serous adenocarcinoma sensitive Neratinib + Taselisib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Nerlynx (neratinib) and Taselisib (GDC-0032), compared to either agent alone, resulted in greater inhibition of cell cycle activity in a uterine serous carcinoma cell line harboring ERBB2 (HER2) amplification and a PIK3CA mutation in culture, and in xenograft models, showed increased tumor growth inhibition and tumor regression (PMID: 26333383). 26333383
ERBB2 amp PIK3CA mut Her2-receptor positive breast cancer sensitive Copanlisib Preclinical - Cell line xenograft Actionable In a preclinical study, Aliqopa (copanlisib) promoted tumor regression in xenograft models of a human ERBB2 (HER2)-amplified breast cancer cell line harboring a PIK3CA activating mutation (PMID: 24170767). 24170767
ERBB2 amp PIK3CA mut breast cancer sensitive CUDC-907 Preclinical Actionable In a preclinical study, CUDC-907 inhibited downstream signaling and growth of PIK3CA-mutant breast cancer cells with ERBB2 amplification in culture (PMID: 22693356). 22693356
ERBB2 amp PIK3CA mut Her2-receptor positive breast cancer sensitive Ipatasertib Preclinical - Cell line xenograft Actionable In a preclinical study, ERBB2 (HER2)-receptor positive breast cancer cell line xenograft models harboring amplification of ERBB2 (HER2) and a PIK3CA mutation demonstrated sensitivity to treatment with Ipatasertib (GDC-0068), resulting in inhibition of tumor growth (PMID: 24141624). 24141624
ERBB2 T798M ERBB2 amp breast cancer resistant Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, a human ERBB2-amplified breast cancer cell line expressing ERBB2 (HER2) T798M was resistant to Herceptin (trastuzumab) in culture and in xenograft models (PMID: 23948973). 23948973
ERBB2 L866M ERBB2 amp colorectal cancer resistant Cetuximab Preclinical Actionable In a preclinical study, xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) L866M and ERBB2 (HER2) amplification were resistant to Erbitux (cetuximab) (PMID: 26243863). 26243863
ERBB2 L866M ERBB2 amp colorectal cancer resistant Trastuzumab Preclinical Actionable In a preclinical study, Herceptin (trastuzumab) had no effect on tumor growth in xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) L866M and ERBB2 (HER2) amplification (PMID: 26243863). 26243863
ERBB2 L866M ERBB2 amp colorectal cancer sensitive Neratinib + Trastuzumab Preclinical Actionable In a preclinical study, Herceptin (trastuzumab) and Nerlynx (neratinib) combination treatment resulted in sustained tumor regression in xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) L866M and ERBB2 (HER2) amplification (PMID: 26243863). 26243863
ERBB2 L866M ERBB2 amp colorectal cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) treatment resulted in stable tumor size in xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) L866M and ERBB2 (HER2) amplification (PMID: 26243863). 26243863
ERBB2 amp PIK3CA wild-type uterine corpus serous adenocarcinoma sensitive Neratinib + Taselisib Preclinical - Cell culture Actionable In a preclinical study, the combination of Taselisib (GDC-0032) and Nerlynx (neratinib) delayed cell cycle activity in a uterine serous carcinoma cell line harboring PIK3CA wild-type and ERBB2 (HER2) amplification in culture (PMID: 26333383). 26333383
ERBB2 amp PIK3CA wild-type uterine corpus serous adenocarcinoma sensitive Taselisib Preclinical - Cell line xenograft Actionable In a preclinical study, Taselisib (GDC-0032) did not result in delay of cell cycle activity during treatment of a uterine serous carcinoma cell line harboring PIK3CA wild-type and ERBB2 (HER2) amplification in culture, however, did result in tumor growth inhibition in xenograft models (PMID: 26333383). 26333383
ERBB2 amp PIK3CA wild-type Her2-receptor positive breast cancer predicted - sensitive Poziotinib Phase II Actionable In a Phase II trial, the presence of high ERBB2 (HER2) copy number and wild-type PIK3CA correlated with improved progression-free survival (HR=0.45, p=0.024) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
ERBB2 amp PIK3CA wild-type uterine corpus serous adenocarcinoma sensitive Neratinib Preclinical - Cell line xenograft Actionable In a preclinical study, Nerlynx (neratinib) delayed cell cycle activity during treatment of a uterine serous carcinoma cell line harboring PIK3CA wild-type and ERBB2 (HER2) amplification in culture, and inhibited tumor growth in xenograft models (PMID: 26333383). 26333383
ARID1A loss ERBB2 amp breast cancer sensitive MK2206 + Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line with ARID1A loss and harboring ERBB2 (HER2) amplification demonstrated restored sensitivity to Herceptin (trastuzumab) when additionally treated with MK2206 in culture (PMID: 27172896). 27172896
ERBB2 amp FGFR2 amp esophagus adenocarcinoma sensitive AZD4547 + Lapatinib Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD-4547 and Tykerb (lapatinib) worked synergistically to inhibit growth of an esophageal adenocarcinoma cell line with ERBB2 (HER2) and FGFR2 amplification in culture (PMID: 27595477). 27595477
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer decreased response Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, breast cancer cell lines with ERBB2 (HER2) amplification and expressing ERBB2 L755S demonstrated decreased inhibition proliferation compared to cells expressing wild-type ERBB2 (HER2) following treatment with Herceptin (trastuzumab) (PMID: 30301790). 30301790
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of ESR1-positive/ERBB2 (HER2)-positive breast cancer cell lines with ERBB2 amplification and harboring ERBB2 L755S in culture (PMID: 28487443). 28487443
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer sensitive Neratinib Case Reports/Case Series Actionable In a clinical study, Nerlynx (neratinib) treatment resulted in partial response in 2 of 6 and disease stabilization in 4 of 6 breast cancer patients with ERBB2 (HER2) amplification and an ERBB2 (HER2) mutation, including stable disease in a patient harboring ERBB2 (HER2) L755S, and breast cancer cell lines with ERBB2 (HER2) amplification and expressing ERBB2 (HER2) L755S demonstrated sensitivity to Nerlynx (neratinib) in culture (PMID: 30301790). 30301790
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer resistant Lapatinib + Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, expression of ERBB2 (HER2) L755S conferred resistance to Tykerb (lapatinib) plus Herceptin (trastuzumab) combination therapy in ESR1-positive/ERBB2 (HER2)-positive breast cancer cells with ERBB2 amplification in culture (PMID: 28487443). 28487443
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer resistant Lapatinib + Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, breast cancer cell lines with ERBB2 (HER2) amplification and expressing ERBB2 L755S demonstrated decreased inhibition proliferation compared to cells expressing wild-type ERBB2 (HER2) following treatment with Herceptin (trastuzumab) and Tykerb (lapatinib) (PMID: 30301790). 30301790
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer sensitive Afatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Gilotrif (afatinib) inhibited growth of ESR1-positive/ERBB2 (HER2)-positive breast cancer cell lines with ERBB2 amplification and harboring ERBB2 L755S in culture, and inhibited tumor growth in xenograft models (PMID: 28487443). 28487443
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer decreased response Ado-trastuzumab emtansine Preclinical - Cell culture Actionable In a preclinical study, expression of ERBB2 (HER2) L755S resulted in decreased sensitivity to treatment with Kadcyla (trastuzumab emtansine) in ESR1-positive/ERBB2 (HER2)-positive breast cancer cells with ERBB2 amplification in culture (PMID: 28487443). 28487443
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer resistant Pertuzumab + Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, expression of ERBB2 (HER2) L755S conferred resistance to Perjeta (pertuzumab) plus Herceptin (trastuzumab) combination therapy in ESR1-positive/ERBB2 (HER2)-positive breast cancer cells with ERBB2 amplification in culture (PMID: 28487443). 28487443
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cell lines with ERBB2 (HER2) amplification and expressing ERBB2 L755S demonstrated decreased inhibition of ERBB2 (HER2) signaling and proliferation compared to cells expressing wild-type ERBB2 (HER2) following treatment with Tykerb (lapatinib) (PMID: 30301790). 30301790
ERBB2 L755S ERBB2 amp Her2-receptor positive breast cancer resistant Lapatinib Preclinical - Cell line xenograft Actionable In a preclinical study, ERBB2 (HER2) L755S was associated with reactivation of ERBB2 (HER2) signaling and acquired resistance to Tykerb (lapatinib) in ESR1-positive/ERBB2 (HER2)-positive breast cancer cell lines with ERBB2 amplification in culture and in xenograft models (PMID: 28487443). 28487443
ERBB2 amp SRC E527K gastroesophageal junction adenocarcinoma sensitive Lapatinib + Saracatinib Preclinical - Cell culture Actionable In a preclinical study, the combination of Tykerb (lapatinib) and Saracatinib (AZD0530) inhibited growth of ERBB2 (HER2)-amplified gastroesophageal adenocarcinoma cells harboring SRC E527K in culture (PMID: 25350844). 25350844
ERBB2 amp SRC E527K gastroesophageal junction adenocarcinoma resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, an ERBB2 (HER2)-amplified gastroesophageal cancer cell line initially sensitive to treatment with Tykerb (lapatinib) in culture developed resistance and was subsequently found to have acquired a secondary drug resistant mutation, SRC E527K (PMID: 25350844). 25350844
ROS1 fusion ERBB2 amp NOTCH1 amp SRC amp STK11 amp lung non-small cell carcinoma predicted - resistant Crizotinib Case Reports/Case Series Actionable In a clinical study, a non-small cell lung carcinoma patient harboring a ROS1 fusion treated with Xalkori (crizotinib) responded, but eventually progressed, and was subsequently found to harbor presumed resistance alterations, including amplification of SRC, ERBB2 (HER2), STK11, and NOTCH1 (PMID: 29636358). 29636358
ROS1 fusion ERBB2 amp FGFR3 amp RET amp lung non-small cell carcinoma predicted - resistant Crizotinib Case Reports/Case Series Actionable In a clinical study, a non-small cell lung carcinoma patient harboring a ROS1 fusion treated with Xalkori (crizotinib) responded, but eventually progressed, and was subsequently found to harbor presumed resistance alterations, including amplification of ERBB2 (HER2), FGFR3, and RET (PMID: 29636358). 29636358
ERBB2 S310F ERBB2 amp lung adenocarcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, treatment with Kadcyla (trastuzumab emtansine) resulted in best overall responses of partial response in 44% (8/18) and stable disease in 39% (7/18), and median progression-free survival of 5 months in patients with lung adenocarcinoma harboring ERBB2 (HER2) activating mutations; a patient harboring ERBB2 (HER2) S310F and ERBB2 (HER2) amplification had a partial response (PMID: 29989854; NCT02675829). 29989854
ERBB2 Y772_A775dup ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a clinical study, Nerlynx (neratinib) treatment resulted in partial response in 2 of 6 and disease stabilization in 4 of 6 breast cancer patients with ERBB2 (HER2) amplification and an ERBB2 (HER2) mutation, including stable disease in a patient harboring ERBB2 (HER2) Y772_A775dup (PMID: 30301790). 30301790
ERBB2 D769Y ERBB2 amp Her2-receptor positive breast cancer sensitive Neratinib Case Reports/Case Series Actionable In a clinical study, Nerlynx (neratinib) treatment resulted in partial response in 2 of 6 and disease stabilization in 4 of 6 breast cancer patients with ERBB2 (HER2) amplification and an ERBB2 (HER2) mutation, including stable disease in a patient harboring ERBB2 (HER2) D769Y, and Nerlynx (neratinib) inhibited tumor growth in a breast cancer patient-derived xenograft (PDX) model with ERBB2 (HER2) amplification and ERBB2 (HER2) D769Y (PMID: 30301790). 30301790
ERBB2 D769Y ERBB2 amp Her2-receptor positive breast cancer resistant Trastuzumab Preclinical - Pdx Actionable In a preclinical study, a breast cancer patient-derived xenograft (PDX) model with ERBB2 (HER2) amplification and ERBB2 D769Y was refractory to treatment with Herceptin (trastuzumab) (PMID: 30301790). 30301790
ERBB2 D769Y ERBB2 amp Her2-receptor positive breast cancer resistant Lapatinib Preclinical - Pdx Actionable In a preclinical study, a breast cancer patient-derived xenograft (PDX) model with ERBB2 (HER2) amplification and ERBB2 D769Y was refractory to treatment with Tykerb (lapatinib) (PMID: 30301790). 30301790
ERBB2 V777L ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a clinical study, Nerlynx (neratinib) treatment resulted in partial response in 2 of 6 and disease stabilization in 4 of 6 breast cancer patients with ERBB2 (HER2) amplification and an ERBB2 (HER2) mutation, including partial response in a patient harboring ERBB2 (HER2) V777L (PMID: 30301790). 30301790
ERBB2 L313I ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a clinical study, Nerlynx (neratinib) treatment resulted in partial response in 2 of 6 and disease stabilization in 4 of 6 breast cancer patients with ERBB2 (HER2) amplification and an ERBB2 (HER2) mutation, including partial response in a patient harboring ERBB2 (HER2) L313I (PMID: 30301790). 30301790
ERBB2 R456C ERBB2 amp Her2-receptor positive breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a clinical study, Nerlynx (neratinib) treatment resulted in partial response in 2 of 6 and disease stabilization in 4 of 6 breast cancer patients with ERBB2 (HER2) amplification and an ERBB2 (HER2) mutation, including stable disease in a patient harboring ERBB2 (HER2) R456C (PMID: 30301790). 30301790
ERBB2 amp PIK3CA act mut Her2-receptor positive breast cancer decreased response Poziotinib Phase II Actionable In a Phase II trial, the presence of PIK3CA activating mutations including E542X, E545X, and H1047X correlated with shorter progression-free survival (2.66 months) compared to PIK3CA wild-type or other mutations (4.24 month, HR=1.68, p=0.033) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
ERBB2 amp PIK3CA E542X Her2-receptor positive breast cancer decreased response Poziotinib Phase II Actionable In a Phase II trial, the presence of PIK3CA activating mutations including E542X, E545X, and H1047X correlated with shorter progression-free survival (2.66 months) compared to PIK3CA wild-type or other mutations (4.24 month, HR=1.68, p=0.033) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
ERBB2 amp PIK3CA H1047X Her2-receptor positive breast cancer decreased response Poziotinib Phase II Actionable In a Phase II trial, the presence of PIK3CA activating mutations including E542X, E545X, and H1047X correlated with shorter progression-free survival (2.66 months) compared to PIK3CA wild-type or other mutations (4.24 month, HR=1.68, p=0.033) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
ERBB2 amp PIK3CA E545X Her2-receptor positive breast cancer decreased response Poziotinib Phase II Actionable In a Phase II trial, the presence of PIK3CA activating mutations including E542X, E545X, and H1047X correlated with shorter progression-free survival (2.66 months) compared to PIK3CA wild-type or other mutations (4.24 month, HR=1.68, p=0.033) in patients with metastatic Erbb2 (Her2)-positive (amplification or overexpression) breast cancer treated with Poziotinib (HM781-36B) (PMID: 30720867, NCT02418689). 30720867
BRAF wild-type ERBB2 amp NRAS wild-type colon cancer sensitive Pertuzumab + Trastuzumab Guideline Actionable Herceptin (trastuzumab) in combination with Perjeta (pertuzumab) is included in guidelines as second-line therapy for advanced or metastatic colon cancer patients with ERBB2 amplification and NRAS, BRAF wild-type (NCCN.org). detail...
BRAF wild-type ERBB2 amp NRAS wild-type rectum cancer sensitive Lapatinib + Trastuzumab Guideline Actionable Herceptin (trastuzumab) in combination with Tykerb (lapatinib) is included in guidelines as second-line therapy for advanced or metastatic rectum cancer patients with ERBB2 amplification and wild-type NRAS and BRAF (NCCN.org). detail...
BRAF wild-type ERBB2 amp NRAS wild-type colon cancer sensitive Lapatinib + Trastuzumab Guideline Actionable Herceptin (trastuzumab) in combination with Tykerb (lapatinib) is included in guidelines as second-line therapy for advanced or metastatic colon cancer patients with ERBB2 amplification and NRAS, BBRAF wild-type (NCCN.org). detail...
BRAF wild-type ERBB2 amp NRAS wild-type rectum cancer sensitive Pertuzumab + Trastuzumab Guideline Actionable Herceptin (trastuzumab) in combination with Perjeta (pertuzumab) is included in guidelines as second-line therapy for advanced or metastatic rectum cancer patients with ERBB2 amplification and wild-type NRAS and BRAF (NCCN.org). detail...
ERBB2 G778_P780dup ERBB2 amp lung adenocarcinoma predicted - sensitive Dacomitinib Case Reports/Case Series Actionable In a clinical case study, a patient with metastatic lung adenocarcinoma harboring ERBB2 (HER2) G778_P780dup (also reported as P780_Y781insGSP) demonstrated an ongoing partial response following four months of Vizimpro (dacomitinib) treatment (PMID: 32036069). 32036069
ERBB2 G778_P780dup ERBB2 amp lung adenocarcinoma predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a clinical case study, Pyrotinib treatment resulted in 11 months of stable disease in a lung adenocarcinoma patient harboring ERBB2 (HER2) G778_P780dup (also reported as V777_G778insGSP) and ERBB2 (HER2) amplification (PMID: 32036069). 32036069
ERBB2 P761del endometrial cancer predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.9 months in a patient with endometrial cancer harboring ERBB2 (HER2) P761del (PMID: 29420467; NCT01953926). 29420467
ERBB2 V773L breast cancer sensitive Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) V773L were sensitive to Tykerb (lapatinib) in culture, resulting in decreased colony formation (PMID: 27697991). 27697991
ERBB2 V773L breast cancer sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) V773L were sensitive to Nerlynx (nerlatinib) in culture, resulting in decreased colony formation (PMID: 27697991). 27697991
ERBB2 V773L breast cancer sensitive Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) V773L were sensitive to Herceptin (trastuzumab) in culture, resulting in decreased colony formation (PMID: 27697991). 27697991
ERBB2 V604_E619del breast cancer sensitive Lapatinib Preclinical - Cell culture Actionable In a preclinical study, Tykerb (lapatinib) inhibited Erbb2 signaling and viability of transformed breast epithelial cells expressing ERBB2 (HER2) V604_E619del in culture (PMID: 31135266). 31135266
ERBB2 V604_E619del breast cancer sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) inhibited Erbb2 signaling and viability of transformed breast epithelial cells expressing ERBB2 (HER2) V604_E619del in culture (PMID: 31135266). 31135266
ERBB2 G778_P780dup lung adenocarcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a clinical study, five lung adenocarcinoma patients each harboring ERBB2 (HER2) G778_P780dup (also reported as P780_Y781insGSP) demonstrated a clinical benefit from treatment with Gilotrif (afatinib), including one patient with a partial response lasting nine months, a second patient demonstrating a 51% reduction in primary tumor size after one month with a partial response lasting eight months, and three patients with stable disease ranging from 6 to 9 months (PMID: 32036069). 32036069
ERBB2 G778_P780dup lung adenocarcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a clinical case study, a patient with metastatic lung adenocarcinoma harboring ERBB2 (HER2) G778_P780dup (also referred to as V777_G778insGSP) demonstrated tumor shrinkage and clinical response for 7 months following treatment with Gilotrif (afatinib) (PMID: 28363995). 28363995
ERBB2 G778_P780dup lung adenocarcinoma predicted - sensitive Afatinib Clinical Study - Cohort Actionable In a retrospective study, Gilotrif (afatinib) treatment resulted in an objective response rate (ORR) of 15.6% (5/32) and a disease control rate of 68.8% (22/32) in patients with lung adenocarcinoma harboring ERBB2 (HER2) mutations, patients harboring G776delinsVC (n=5) or G778_P780dup (n=5) achieved longer median progression-free survival (7.6 mo) than those with Y772_A775dup (n=14, 1.2 mo) or missense mutations (n=8, 3.6 mo), with an ORR of 40% (4/10) and a DCR of 100% (10/10) (PMID: 32162827). 32162827
ERBB2 G778_P780dup lung adenocarcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a clinical study, a lung adenocarcinoma patient harboring ERBB2 (HER2) G778_P780dup (also referred to as V747_G748insGSP and G748_P750dup), demonstrated a 13% regression of target lesions and stable disease for 11 months following treatment with pulse Gilotrif (afatinib) (PMID: 26964772). 26964772
ERBB2 G778_P780dup breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 (HER2) P780_Y781insGSP reverted to normal morphology in culture upon Nerlynx (neratinib) treatment (PMID: 23220880). 23220880
ERBB2 G778_P780dup breast cancer sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial, Nerlynx (neratinib) treatment resulted in a clinical benefit rate of 31% (5/16) in metastatic breast cancer patients harboring ERBB2 (HER2) mutations, with 1 complete response (referred to as V777_G778insGSP) and 1 stable disease for more than 24 weeks (referred to as P780_Y781insGSP) in 3 patients harboring ERBB2 G778_P780dup (PMID: 28679771; NCT01670877). 28679771
ERBB2 G778_P780dup Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor resistant AZ5104 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) were resistant to AZ5104 in culture (PMID: 30527195). 30527195
ERBB2 G778_P780dup lung adenocarcinoma predicted - sensitive Poziotinib Case Reports/Case Series Actionable In a clinical case study, Poziotinib (HM781-36B) treatment resulted in stable disease lasting nine months in a metastatic lung adenocarcinoma patient harboring ERBB2 (HER2) G778_P780dup (also reported as P780_Y781insGSP) with prior disease progression following an initial partial response to Gilotrif (afatinib) (PMID: 32036069). 32036069
ERBB2 G778_P780dup Her2-receptor negative breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in partial response with a progression-free survival of 3.5 months in one patient, and stable disease with a progression-free survival of 20.0 months in another patient with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) G778_P780dup (PMID: 29420467; NCT01953926). 29420467
ERBB2 G778_P780dup breast cancer predicted - sensitive Lapatinib + Perifosine Preclinical - Cell culture Actionable In a preclinical study, addition of Perifosine restored sensitivity to Tykerb (lapatinib) in breast epithelial cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP in culture (PMID: 31980423). 31980423
ERBB2 G778_P780dup lung non-small cell carcinoma predicted - sensitive Afatinib Clinical Study Actionable In a retrospective analysis, Gilotrif (afatinib) treatment resulted in an objective response rate of 25% (1/4) in non-small cell lung cancer patients harboring ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) (PMID: 30527195). 30527195
ERBB2 G778_P780dup Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) demonstrated decreased response to Gilotrif (afatinib) compared to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 G778_P780dup Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung adenocarcinoma sensitive Dacomitinib Case Reports/Case Series Actionable In a Phase II trial, two lung adenocarcinoma patients harboring ERBB2 (HER2) G778_780dup (reported as P780_Y781insGSP) demonstrated partial response to treatment with Vizimpro (dacomitinib) (PMID: 25899785; NCT00818441). 25899785
ERBB2 G778_P780dup Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung cancer no benefit Gefitinib Preclinical Actionable In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) G778_P780dup (also referred to as P780_Y781insGSP) did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). 26545934
ERBB2 G778_P780dup Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor decreased response Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) demonstrated decreased response to Tagrisso (osimertinib) compared to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 G778_P780dup Advanced Solid Tumor decreased response Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) P780_Y781insGSP were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung non-small cell carcinoma predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a Phase II trial, Pyrotinib treatment resulted in an objective response rate of 60% (3/5) in non-small cell lung cancer patients harboring ERBB2 (HER2) G778_P780dup (also reported as P780_Y781insGSP) who had received prior platinum-based chemotherapy (PMID: 32614698; NCT02834936). 32614698
ERBB2 G778_P780dup Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of transformed cells expressing ERBB2 (HER2) G778_P780dup (also referred to as P780_Y781insGSP) in culture (PMID: 28363995). 28363995
ERBB2 G778_P780dup Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) P780_Y781insGSP demonstrated decreased response to Nerlynx (neratinib) compared to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 G778_P780dup Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Her2-receptor positive breast cancer predicted - resistant Lapatinib Case Reports/Case Series Actionable In a clinical case study, ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) was identified in a patient with ERBB2 (HER2)-positive breast cancer at the time of disease progression while on Tykerb (lapatinib) treatment (PMID: 31980423). 31980423
ERBB2 G778_P780dup Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited growth of a transformed cell line expressing ERBB2 (HER2) G778_P780dup (reported P780insGSP) in culture (PMID: 29686424). 29686424
ERBB2 G778_P780dup Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) P780_Y781insGSP in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited Erbb2 (Her2) phosphorylation and downstream signaling in bronchial epithelial cells expressing ERBB2 (HER2) G778_P780dup (also referred to as P780_Y781insGSP) in culture (PMID: 26545934). 26545934
ERBB2 G778_P780dup Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) were resistant to Tykerb (lapatinib) in culture (PMID: 30527195). 30527195
ERBB2 G778_P780dup Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P80dup were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung non-small cell carcinoma predicted - sensitive Poziotinib Phase II Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in a confirmed objective response rate of 42% (5/12) in patients with non-small cell lung cancer harboring ERBB2 (HER2) Y772_A775dup (n=9) or ERBB2 (HER2) G778_P780dup (n=3), with a median progression-free survival of 5.6 months (PMID: 31588020; NCT03066206). 31588020
ERBB2 G778_P780dup breast cancer resistant Lapatinib Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 P780_Y781insGSP demonstrated resistance when treated with Tykerb (lapatinib) (PMID: 23220880). 23220880
ERBB2 G778_P780dup breast cancer resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, breast epithelial cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) were resistant to Tykerb (lapatinib) treatment in cell culture (PMID: 31980423). 31980423
ERBB2 G778_P780dup lung non-small cell carcinoma no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival over 17 months in 2 patients with non-small cell lung cancer harboring ERBB2 (HER2) G778_P780dup (PMID: 29420467; NCT01953926). 29420467
ERBB2 G778_P780dup breast cancer sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited viability of breast cancer cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung adenocarcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, treatment with Kadcyla (trastuzumab emtansine) resulted in best overall responses of partial response in 44% (8/18) and stable disease in 39% (7/18), and median progression-free survival of 5 months in patients with lung adenocarcinoma harboring ERBB2 (HER2) activating mutations, and a subset of patients specifically harboring ERBB2 (HER2) G778_P780dup (also referred to as P780_Y781insGSP) had a 33% (1/3) partial response rate (PMID: 29989854; NCT02675829). 29989854
ERBB2 G778_P780dup Advanced Solid Tumor decreased response Tucatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) demonstrated decreased response to Tukysa (tucatinib) compared to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 G778_P780dup breast cancer sensitive Ado-trastuzumab emtansine + Poziotinib Preclinical - Cell culture Actionable In a preclinical study, addition of Poziotinib (HM781-36B) enhanced growth inhibition by Kadcyla (ado-trastuzumab emtansine) treatment in breast cancer cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung adenocarcinoma predicted - sensitive Afatinib + Cisplatin + Pemetrexed Disodium Case Reports/Case Series Actionable In a clinical case study, the combination of Gilotrif (afatinib), Platinol (cisplatin), and Alimta (Pemetrexed Disodium) followed by the combination of Gilotrif (afatinib) and Alimta (Pemetrexed Disodium) resulted in an ongoing partial response over 19 months in a patient with lung adenocarcinoma harboring ERBB2 (HER2) G778_P780dup (also reported as P780_Y781insGSP) (PMID: 32036069). 32036069
ERBB2 G778_P780dup Advanced Solid Tumor resistant Erlotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) were resistant to Tarceva (erlotinib) in culture (PMID: 30527195). 30527195
ERBB2 G778_P780dup breast cancer resistant Trastuzumab Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 P780_Y781insGSP demonstrated resistance when treated with Herceptin (trastuzumab) (PMID: 23220880). 23220880
ERBB2 G778_P780dup Advanced Solid Tumor conflicting Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited growth of transformed cells expressing ERBB2 (HER2) G778_P780dup (also referred to as P780_Y781insGSP) in culture (PMID: 28363995). 28363995
ERBB2 G778_P780dup Advanced Solid Tumor conflicting Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung adenocarcinoma predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a clinical study, three lung adenocarcinoma patients harboring ERBB2 (HER2) G778_P780dup (also reported as V777_G778insGSP) demonstrated a clinical benefit when treated with Pyrotinib, including a patient with three months of stable disease who had progressed on several prior lines of therapy, a patient with an ongoing partial response of six months, and a patient with an ongoing partial response of eight months who had prior disease progression with Gilotrif (afatinib) (PMID: 32036069). 32036069
ERBB2 G778_P780dup Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup PIK3CA H1047R breast cancer decreased response Neratinib Preclinical - Pdx Actionable In a preclinical study, Nerlynx (neratinib) resulted in a moderate delay of tumor growth in a breast cancer patient-derived xenograft model harboring ERBB2 (HER2) G778_P780dup and PIK3CA H1074R (PMID: 31978326). 31978326
ERBB2 T733I biliary tract cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 3.7 months in a patient with biliary tract cancer harboring ERBB2 (HER2) T733I (PMID: 29420467; NCT01953926). 29420467
ERBB2 T733I Advanced Solid Tumor resistant Lapatinib Preclinical Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) T733I demonstrated resistance to treatment with Tykerb (lapatinib) (PMID: 18413839). 18413839
ERBB2 T733I Advanced Solid Tumor sensitive Tesevatinib Preclinical Actionable In a preclinical study, XL647 inhibited survival of transformed cells over expressing ERBB2 (HER2) T733I in culture (PMID: 18413839). 18413839
ERBB2 K831N colorectal cancer predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.7 months in a patient with colorectal cancer harboring ERBB2 (HER2) K831N (PMID: 29420467; NCT01953926). 29420467
ERBB2 L755A lung non-small cell carcinoma no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 3.6 months in a patient with non-small cell lung cancer harboring ERBB2 (HER2) L755A (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F lung non-small cell carcinoma predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.9 months in a patient with non-small cell lung cancer harboring ERBB2 (HER2) S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F colorectal cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited growth of colorectal cancer cells over expressing ERBB2 (HER2) S310F in culture (PMID: 26243863). 26243863
ERBB2 S310F cervical cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in partial response in 1 patient, stable disease in 1 patient, and progressive disease in 1 patient with cervical cancer harboring ERBB2 (HER2) S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F colorectal cancer resistant Panitumumab Preclinical Actionable In a preclinical study, colorectal cancer cells over expressing ERBB2 (HER2) S310F were resistant to Vectibix (panitumumab) in culture (PMID: 26243863). 26243863
ERBB2 S310F salivary gland carcinoma predicted - sensitive Pertuzumab + Trastuzumab Case Reports/Case Series Actionable In a Phase II (MyPathway) trial, Perjeta (pertuzumab) and Herceptin (trastuzumab) combination therapy resulted in stable disease in a patient with advanced salivary gland carcinoma harboring ERBB2 (HER2) S310F, with a progression-free survival of 11 months (PMID: 32067683; NCT02091141). 32067683
ERBB2 S310F urinary bladder cancer decreased response Selumetinib Preclinical Actionable In a preclinical study, bladder cancer cells over expressing ERBB2 (HER2) S310F demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture (PMID: 24971884). 24971884
ERBB2 S310F Advanced Solid Tumor sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited proliferation of transformed cells expressing ERBB2 S310F in culture (PMID: 22908275). 22908275
ERBB2 S310F endometrial cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 2.6 months in a patient with endometrial cancer harboring ERBB2 (HER2) S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F breast cancer resistant Pertuzumab Preclinical - Cell culture Actionable In a preclinical study, ligand-activated breast cancer cells expressing ERBB2 (HER2) S310F demonstrated resistance to treatment with Perjeta (pertuzumab) in culture compared to cells expressing wild-type ERBB2 (HER2) (PMID: 31920346). 31920346
ERBB2 S310F colon cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited colony formation in transformed mouse colon epithelial cells over expressing ERBB2 (HER2) S310F in culture (PMID: 26243863). 26243863
ERBB2 S310F colon cancer sensitive Trastuzumab Preclinical Actionable In a preclinical study, Herceptin (trastuzumab) inhibited colony formation in transformed mouse colon epithelial cells over expressing ERBB2 (HER2) S310F in culture (PMID: 26243863). 26243863
ERBB2 S310F gastroesophageal junction adenocarcinoma predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 3.9 months in a patient with gastroesophageal cancer harboring ERBB2 (HER2) S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F colorectal cancer conflicting Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.7 months in a patient with colorectal cancer harboring ERBB2 (HER2) S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F colorectal cancer conflicting Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of colorectal cancer cells over expressing ERBB2 (HER2) S310F in culture (PMID: 26243863). 26243863
ERBB2 S310F urinary bladder cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited foci formation of bladder cancer cells over expressing ERBB2 (HER2) S310F in culture (PMID: 24971884). 24971884
ERBB2 S310F urinary bladder cancer sensitive Gefitinib Preclinical - Cell culture Actionable In a preclinical study, a bladder cancer cell line harboring ERBB2 S310F demonstrated decreased viability when treated with Iressa (gefitinib) in culture (PMID: 31635022). 31635022
ERBB2 S310F urinary bladder cancer sensitive Lapatinib Preclinical - Cell culture Actionable In a preclinical study, Tykerb (lapatinib) inhibited foci formation of bladder cancer cells over expressing ERBB2 (HER2) S310F in culture (PMID: 24971884). 24971884
ERBB2 S310F urinary bladder cancer no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease in 4 patients and progressive disease in 1 patient with bladder cancer harboring ERBB2 (HER2) S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F colorectal cancer resistant Cetuximab Preclinical Actionable In a preclinical study, colorectal cancer cells over expressing ERBB2 (HER2) S310F were resistant to Erbitux (cetuximab) in culture (PMID: 26243863). 26243863
ERBB2 S310F urinary bladder cancer no benefit Pertuzumab Preclinical - Cell culture Actionable In a preclinical study, a bladder cancer cell line harboring ERBB2 S310F did not demonstrate decreased viability when treated with Perjeta (pertuzumab) in culture (PMID: 31635022). 31635022
ERBB2 S310F urinary bladder cancer sensitive Cetuximab Preclinical - Cell culture Actionable In a preclinical study, a bladder cancer cell line harboring ERBB2 S310F demonstrated decreased viability when treated with Erbitux (cetuximab) in culture (PMID: 31635022). 31635022
ERBB2 S310F gallbladder cancer predicted - sensitive Capecitabine + Lapatinib Case Reports/Case Series Actionable In a clinical case study, Tykerb (lapatinib) in combination with Xeloda (capecitabine) resulted in rapid clinical improvement and decrease of tumor size after 2 cycles of treatment in a patient with metastatic gallbladder cancer harboring ERBB2 (HER2) S310F (PMID: 31558980). 31558980
ERBB2 S310F Advanced Solid Tumor sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) decreased cell survival of transformed human cells expressing ERBB2 (HER2) S310F (PMID: 22908275). 22908275
ERBB2 S310F biliary tract cancer conflicting Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in partial response in one and progressive disease in another patient with biliary tract cancer harboring ERBB2 (HER2) S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F urinary bladder cancer no benefit Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, a bladder cancer cell line harboring ERBB2 S310F did not demonstrate decreased viability when treated with Herception (trastuzumab) in culture (PMID: 31635022). 31635022
ERBB2 S310F breast cancer resistant Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, ligand-activated breast cancer cells expressing ERBB2 (HER2) S310F demonstrated resistance to treatment with Herceptin (trastuzumab) in culture (PMID: 31920346). 31920346
ERBB2 S310F Her2-receptor negative breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in complete response with a progression-free survival of 14.6 months in one patient, and stable disease with a progression-free survival of 3.7 months in another patient with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 D277H ERBB2 S310F urinary bladder cancer decreased response Selumetinib Preclinical Actionable In a preclinical study, bladder cancer cells over expressing both ERBB2 (HER2) D277H and S310F demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture (PMID: 24971884). 24971884
ERBB2 D277H ERBB2 S310F urinary bladder cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited foci formation of bladder cancer cells over expressing both ERBB2 (HER2) D277H and S310F in culture (PMID: 24971884). 24971884
ERBB2 D277H ERBB2 S310F urinary bladder cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited foci formation of bladder cancer cells over expressing both ERBB2 (HER2) D277H and S310F in culture (PMID: 24971884). 24971884
ERBB2 S310F ERBB2 V842I breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial, Nerlynx (neratinib) treatment resulted in a clinical benefit rate of 31% (5/16) in metastatic breast cancer patients harboring ERBB2 (HER2) mutations, with 1 patient harboring ERBB2 (HER2) S310F and V842R achieved stable disease over 6 months (PMID: 28679771; NCT01670877). 28679771
ERBB2 S310F ERBB2 V842I cervical cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), a heavily pretreated cervical cancer patient co-harboring ERBB2 (HER2) S310F and ERBB2 (HER2) V842I demonstrated a partial response when treated with Nerlynx (neratinib) (PMID: 32723675; NCT01953926). 32723675
ERBB2 D277G ERBB2 S310F urinary bladder cancer predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.7 months in a patient with bladder cancer harboring both ERBB2 (HER2) D277G and S310F (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310F ERBB2 G660D ampulla of Vater carcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a clinical case study, Gilotrif (afatinib) treatment resulted in stable disease with slight lymph node metastasis reduction in a patient with ampulla of Vater carcinoma harboring ERBB2 S310F and G660D, but the disease eventually progressed after 4 months (PMID: 29146616). 29146616
ERBB2 G776_V777insVGC lung non-small cell carcinoma predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease in 1 patient and progressive disease in 2 patients with non-small cell lung cancer harboring ERBB2 (HER2) G776_V777insVGC (PMID: 29420467; NCT01953926). 29420467
ERBB2 V659E Advanced Solid Tumor no benefit Erlotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V659E did not benefit from treatment with Tarceva (erlotinib) in culture when compared to Erbb2 (Her2) inhibitors (PMID: 30449325). 30449325
ERBB2 V659E Advanced Solid Tumor predicted - resistant Gefitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V659E did not benefit from treatment with Iressa (gefitinib) in culture when compared to Erbb2 (Her2) inhibitors (PMID: 30449325). 30449325
ERBB2 V659E Advanced Solid Tumor predicted - sensitive Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V659E demonstrated decreased cell proliferation and reduced survival when treated with Tykerb (lapatinib) in culture (PMID: 30449325). 30449325
ERBB2 V659E lung non-small cell carcinoma predicted - sensitive Icotinib Case Reports/Case Series Actionable In a clinical case study, a patient with non-small cell lung cancer harboring ERBB2 (HER2) V659E achieved six months of progression-free survival with Icotinib treatment, prior to disease progression (PMID: 32478891). 32478891
ERBB2 V659E Advanced Solid Tumor predicted - sensitive Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V659E demonstrated decreased cell proliferation and reduced survival when treated with Herceptin (trastuzumab) in culture (PMID: 30449325). 30449325
ERBB2 V659E lung non-small cell carcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a clinical case study, Gilotrif (afatinib) treatment resulted in eight months of progression-free survival followed by disease progression in a non-small cell lung cancer patient harboring ERBB2 (HER2) V659E previously treated with the combination of Tykerb (lapatinib) and Xeloda (capecitabine) (PMID: 32478891). 32478891
ERBB2 V659E lung adenocarcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, treatment with Kadcyla (trastuzumab emtansine) resulted in best overall responses of partial response in 44% (8/18) and stable disease in 39% (7/18), and median progression-free survival of 5 months in patients with lung adenocarcinoma harboring ERBB2 (HER2) activating mutations, and a subset of patients specifically harboring ERBB2 (HER2) V659E had a 50% (1/2) partial response rate (PMID: 29989854; NCT02675829). 29989854
ERBB2 V659E lung cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited Erbb2 (Her2) phosphorylation and downstream signaling in bronchial epithelial cells expressing ERBB2 (HER2) V659E in culture (PMID: 26545934). 26545934
ERBB2 V659E lung cancer no benefit Gefitinib Preclinical Actionable In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) V659E did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). 26545934
ERBB2 V659E Advanced Solid Tumor predicted - sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V659E demonstrated decreased cell proliferation and reduced survival when treated with Gilotrif (afatinib) in culture (PMID: 30449325). 30449325
ERBB2 V659E Advanced Solid Tumor predicted - resistant Pertuzumab Preclinical - Cell culture Actionable In a preclinical study, treatment with Perjeta (pertuzumab) led to induced growth of cells expressing ERBB2 (HER2) V659E in culture (PMID: 30449325). 30449325
ERBB2 V659E lung non-small cell carcinoma no benefit Anlotinib Case Reports/Case Series Actionable In a clinical case study, Anlotinib (AL-3818) treatment resulted in disease progression after seven months in a non-small cell lung cancer patient harboring ERBB2 (HER2) V659E that progressed in response to multiple prior therapies (PMID: 32478891). 32478891
ERBB2 V659E Advanced Solid Tumor predicted - resistant Cetuximab Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V659E demonstrated resistance to treatment with Erbitux (cetuximab) in culture (PMID: 30449325). 30449325
ERBB2 V659E breast cancer sensitive 23814 + Tivozanib Preclinical Actionable In a preclinical study, the combination of 23814 and Tivozanib (AV-951) inhibited tumor growth in several transgenic mouse models of breast cancer expressing ERBB2 (HER2) V659E, including those with resistance to VEGFR inhibitors (PMID: 25995436). 25995436
ERBB2 V659E lung non-small cell carcinoma no benefit Afatinib + Rivoceranib Case Reports/Case Series Actionable In a clinical case study, Gilotrif (afatinib) and Apatinib (YN968D1) combination treatment resulted in disease progression within one month in a non-small cell lung cancer patient harboring ERBB2 (HER2) V659E that progressed in response to prior therapies (PMID: 32478891). 32478891
ERBB2 V659E biliary tract cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 11.1 months in a patient with biliary tract cancer harboring ERBB2 (HER2) V659E (PMID: 29420467; NCT01953926). 29420467
ERBB2 V659E lung non-small cell carcinoma predicted - sensitive Capecitabine + Lapatinib Case Reports/Case Series Actionable In a clinical case study, treatment with the combination of Tykerb (lapatinib) and Xeloda (capecitabine) resulted in eight months of progression-free survival followed by disease progression in a non-small cell lung cancer patient harboring ERBB2 (HER2) V659E (PMID: 32478891). 32478891
ERBB2 V659E lung non-small cell carcinoma predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease in two patients with non-small cell lung cancer harboring ERBB2 (HER2) V659E (PMID: 29420467; NCT01953926). 29420467
ERBB2 V659E Advanced Solid Tumor predicted - sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V659E demonstrated decreased cell proliferation and reduced survival when treated with Nerlynx (neratinib) in culture (PMID: 30449325). 30449325
ERBB2 G776V cervical cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), a heavily pretreated cervical cancer patient harboring ERBB2 (HER2) G776V demonstrated stable disease when treated with Nerlynx (neratinib) (PMID: 32723675; NCT01953926). 32723675
ERBB2 G776V Advanced Solid Tumor sensitive AP32788 Preclinical - Cell culture Actionable In a preclinical study, AP32788 inhibited growth of transformed cell lines over expressing ERBB2 (HER2) G776V in culture (AACR, Cancer Res: April 2016; Volume 57, Abstract #2644). detail...
ERBB2 G776V PIK3CA H1047R ovarian cancer resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, expression of PIK3CA H1047R conferred resistance to Nerlynx (neratinib) in an ovarian cancer cell line harboring ERBB2 (HER2) G776V in culture (PMID: 31978326). 31978326
ERBB2 G776V PIK3CA H1047R ovarian cancer sensitive Everolimus + Neratinib Preclinical - Cell culture Actionable In a preclinical study, the addition of Afinitor (everolimus) to treatment with Nerlynx (neratinib) inhibited viability of an ovarian cancer cell line harboring ERBB2 (HER2) G776V and expressing PIK3CA H1047R in culture (PMID: 31978326). 31978326
ERBB2 G776delinsLC Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC lung cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited Erbb2 (Her2) phosphorylation and downstream signaling in bronchial epithelial cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 26545934). 26545934
ERBB2 G776delinsLC Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC lung cancer no benefit Gefitinib Preclinical Actionable In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) G776delinsLC did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). 26545934
ERBB2 G776delinsLC Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 L768S breast cancer sensitive Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) L768S were sensitive to Tykerb (lapatinib) in culture, resulting in decreased colony formation (PMID: 27697991). 27697991
ERBB2 L768S breast cancer sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) L768S were sensitive to Nerlynx (neratinib) in culture, resulting in decreased colony formation (PMID: 27697991). 27697991
ERBB2 L768S breast cancer sensitive Trastuzumab Preclinical - Cell culture Actionable In a preclinical study, transformed human breast cells expressing ERBB2 (HER2) L768S were sensitive to Herceptin (trastuzumab) in culture, resulting in decreased colony formation (PMID: 27697991). 27697991
ERBB2 A775_G776insYVMA Advanced Solid Tumor sensitive JQ1 + Osimertinib Preclinical Actionable In a preclinical study, transgenic mouse models expressing ERBB2 (HER2) A775_G776insYVMA demonstrated greater tumor regression when treated with the combination of JQ1 and Tagrisso (osimertinib) compared to treatment with either agent alone, which resulted in little to no regression (PMID: 29298799). 29298799
ERBB2 A775_G776insYVMA lung non-small cell carcinoma sensitive Afatinib Preclinical - Pdx & cell culture Actionable In a preclinical study, treatment with Gilotrif (afatinib) resulted in decreased cell viability of patient-derived non-small cell lung cancer organoids harboring ERBB2 A775_G776insYVMA and tumor growth inhibition and tumor regression in patient derived xenograft (PDX) models, but to a lesser degree than treatment with Pyrotinib (PMID: 30596880; NCT02535507). 30596880
ERBB2 A775_G776insYVMA lung non-small cell carcinoma sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, Kadcyla (ado-trastuzumab emtansine) treatment demonstrated limited efficacy in patients with relapsed non-small cell lung cancer harboring ERBB2 (Her2) mutations, resulting in a partial response in 20% (1/5) and stable disease in 60% (3/5) of patients harboring ERBB2 (HER2) A775_G776insYVMA (PMID: 29313813). 29313813
ERBB2 A775_G776insYVMA lung non-small cell carcinoma sensitive Ado-trastuzumab emtansine Preclinical - Pdx Actionable In a preclinical study, treatment with Kadcyla (ado-trastuzumab emtansine) resulted in tumor growth inhibition and tumor regression of patient derived xenograft (PDX) models harboring ERBB2 A775_G776insYVMA, but to a lesser degree than treatment with Pyrotinib (PMID: 30596880; NCT02535507). 30596880
ERBB2 A775_G776insYVMA lung adenocarcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, treatment with Kadcyla (trastuzumab emtansine) resulted in best overall responses of partial response in 44% (8/18) and stable disease in 39% (7/18), and median progression-free survival of 5 months in patients with lung adenocarcinoma harboring ERBB2 (HER2) activating mutations, and a subset of patients specifically harboring ERBB2 (HER2) A775_G776insYVMA mutation had a 60% (3/5) partial response rate (PMID: 29989854; NCT02675829). 29989854
ERBB2 A775_G776insYVMA lung non-small cell carcinoma sensitive Pyrotinib Case Reports/Case Series Actionable In a Phase II trial, ten patients with non-small cell lung cancer harboring ERBB2 A775_G776insYVMA demonstrated an objective response rate of 50% (5/10) and a progression-free survival of 4.1 months when treated with Pyrotinib, and preclinical analysis showed Pyrotinib treatment led to reduced cell viability in patient-derived organoids and tumor growth inhibition and regression in patient derived xenograft (PDX) models (PMID: 30596880; NCT02535507). 30596880
ERBB2 A775_G776insYVMA PIK3CA R425L lung non-small cell carcinoma predicted - resistant Trastuzumab Case Reports/Case Series Actionable In a clinical study, the PIK3CA R425L mutation was identified as a potential resistance mechanism in a non-small cell lung carcinoma patient harboring ERBB2 (HER2) A775_G776insYVMA, that progressed during Herceptin (trastuzumab) treatment (PMID: 28167203). 28167203
ERBB2 D769H breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 (HER2) D769H demonstrated growth inhibition when treated with Nerlynx (neratinib) (PMID: 23220880). 23220880
ERBB2 D769H breast cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 D769H demonstrated growth inhibition when treated with Tykerb (lapatinib) (PMID: 23220880). 23220880
ERBB2 D769H Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 D769H colorectal cancer predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.9 months in a patient with colorectal cancer harboring ERBB2 (HER2) D769H (PMID: 29420467; NCT01953926). 29420467
ERBB2 D769H Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 D769H Her2-receptor negative breast cancer no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 3.5 months in a patient with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) D769H (PMID: 29420467; NCT01953926). 29420467
ERBB2 D769H Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) D769H were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) D769H were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 D769H breast cancer sensitive Trastuzumab Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 D769H reverted to normal morphology in culture upon Herceptin (trastuzumab) treatment (PMID: 23220880). 23220880
ERBB2 D769H Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 act mut lung non-small cell carcinoma predicted - resistant Osimertinib Case Reports/Case Series Actionable In a retrospective analysis, activating ERBB2 (HER2) mutations were identified in 3 of 100 patients with non-small cell lung cancer at treatment discontinuation of Tagrisso (osimertinib) (PMID: 31839416). 31839416
ERBB2 act mut lung adenocarcinoma sensitive Trastuzumab deruxtecan Phase II Actionable In a Phase II trial (DESTINY-Lung01), Enhertu (trastuzumab deruxtecan) treatment resulted in an objective response rate of 61.9% (26/42) and a median progression free survival of 14 months in patients with metastatic non-small cell lung carcinoma harboring ERBB2 activating mutations (J Clin Oncol 38: 2020 (suppl; abstr 9504); NCT03505710). detail...
ERBB2 act mut Advanced Solid Tumor sensitive AEE788 Preclinical Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) activation loop mutations demonstrated sensitivity to AEE788 in culture (PMID: 22046346). 22046346
ERBB2 act mut lung adenocarcinoma predicted - sensitive Ado-trastuzumab emtansine Phase II Actionable In a Phase II trial, treatment with Kadcyla (trastuzumab emtansine) resulted in best overall response rates of 44% (8/18) and 39% (7/18) partial response and stable disease, respectively, and median progression-free survival of 5 months in patients with lung adenocarcinoma harboring ERBB2 (HER2) activating mutations (PMID: 29989854; NCT02675829). 29989854
ERBB2 act mut estrogen-receptor positive breast cancer predicted - sensitive Vistusertib Phase I Actionable In a Phase I trial, Vistusertib (AZD2014) demonstrated safety and preliminary efficacy in patients with advanced solid tumors, including a patient with ER-positive breast cancer harboring an ERBB2 activating mutation (PMID: 25805799). 25805799
ERBB2 act mut lung non-small cell carcinoma predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in partial response in 21% (3/14) and stable disease lasting over 120 days in 21% (3/14) of patients with non-small cell lung cancer harboring ERBB2 (HER2) activating mutations but not amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 act mut Advanced Solid Tumor predicted - sensitive Pertuzumab + Trastuzumab Phase II Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in objective response in 11% (4/36) of patients with advanced solid tumors harboring ERBB2 (HER2) activating mutations but not amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 act mut lung non-small cell carcinoma decreased response Atezolizumab Clinical Study - Cohort Actionable In a clinical study, immunotherapies including Tecentriq (atezolizumab) (n=5), Opdivo (nivolumab) (n=17), Keytruda (pembrolizumab) (n=36), and Camrelizumab (SHR-1210) (n=20) resulted in significantly shorter median progression-free survival (51.0 vs 70.5 days, HR=2.47, p=0.0037) in non-small cell lung cancer patients harboring EGFR (n=7) or ERBB2 (HER2) (n=7) activating mutations compared to wild-type patients (PMID: 31085721). 31085721
ERBB2 act mut lung non-small cell carcinoma decreased response Pembrolizumab Clinical Study - Cohort Actionable In a clinical study, immunotherapies including Tecentriq (atezolizumab) (n=5), Opdivo (nivolumab) (n=17), Keytruda (pembrolizumab) (n=36), and Camrelizumab (SHR-1210) (n=20) resulted in significantly shorter median progression-free survival (51.0 vs 70.5 days, HR=2.47, p=0.0037) in non-small cell lung cancer patients harboring EGFR (n=7) or ERBB2 (HER2) (n=7) activating mutations compared to wild-type patients (PMID: 31085721). 31085721
ERBB2 act mut lung non-small cell carcinoma decreased response Camrelizumab Clinical Study - Cohort Actionable In a clinical study, immunotherapies including Tecentriq (atezolizumab) (n=5), Opdivo (nivolumab) (n=17), Keytruda (pembrolizumab) (n=36), and Camrelizumab (SHR-1210) (n=20) resulted in significantly shorter median progression-free survival (51.0 vs 70.5 days, HR=2.47, p=0.0037) in non-small cell lung cancer patients harboring EGFR (n=7) or ERBB2 (HER2) (n=7) activating mutations compared to wild-type patients (PMID: 31085721). 31085721
ERBB2 act mut cervical cancer predicted - sensitive Neratinib Phase II Actionable In a Phase II trial (SUMMIT), heavily pretreated cervical cancer patients harboring an ERBB2 (HER2) mutation demonstrated an objective response rate of 25% (4/16), including 1 complete response and 3 partial responses, a median progression-free survival of 7.0 months, a median overall survival of 16.8 months, and a clinical benefit rate of 43.8% (7/16) when treated with Nerlynx (neratinib) (PMID: 32723675; NCT01953926). 32723675
ERBB2 act mut breast cancer sensitive Neratinib Phase II Actionable In a Phase II clinical trial, Nerlynx (neratinib) treatment resulted in clinical benefit in 36% (5/14) of metastatic breast cancer patients harboring ERBB2 (HER2) activating mutations, with 1 complete response, 1 partial response, and 2 patients achieving stable disease for greater than 6 months, and a median progression-free survival of 5 months (J Clin Oncol 34, 2016 (suppl; abstr 516)). detail...
ERBB2 act mut lung non-small cell carcinoma decreased response Nivolumab Clinical Study - Cohort Actionable In a clinical study, immunotherapies including Tecentriq (atezolizumab) (n=5), Opdivo (nivolumab) (n=17), Keytruda (pembrolizumab) (n=36), and Camrelizumab (SHR-1210) (n=20) resulted in significantly shorter median progression-free survival (51.0 vs 70.5 days, HR=2.47, p=0.0037) in non-small cell lung cancer patients harboring EGFR (n=7) or ERBB2 (HER2) (n=7) activating mutations compared to wild-type patients (PMID: 31085721). 31085721
ERBB2 act mut biliary tract cancer predicted - sensitive Pertuzumab + Trastuzumab Case Reports/Case Series Actionable In a Phase II trial (MyPathway), Herceptin (trastuzumab) and Perjeta (pertuzumab) combination treatment resulted in an objective response in a patient with biliary cancer harboring an ERBB2 (HER2) activating mutation, but no amplification or overexpression (PMID: 29320312; NCT02091141). 29320312
ERBB2 act mut lung non-small cell carcinoma predicted - sensitive Pyrotinib Phase II Actionable In a Phase II trial, Pyrotinib treatment resulted in an objective response rate of 30% (18/60), with 55% (33/60) demonstrating stable disease, median duration of response of 6.9 mo, and median progression-free survival of 6.9 mo, and median overall survival of 14.4 mo in non-small cell lung cancer patients harboring ERBB2 (HER2) activating mutations, including exon 20 insertions and mutations occurring at L755, G776, and V777, who had received prior platinum-based chemotherapy (PMID: 32614698; NCT02834936). 32614698
ERBB2 act mut PIK3CA act mut breast cancer sensitive VS-5584 Preclinical Actionable In a preclinical study, breast cancer cells with mutations in both ERBB2 (HER2) and PIK3CA were more sensitive to VS-5584 (PMID: 23270925). 23270925
ERBB2 act mut STK11 loss breast cancer sensitive AZD8055 Preclinical Actionable In a preclinical study, AZD8055 inhibited tumor growth in a mouse model of spontaneous breast cancer harboring an ERBB2 (HER2) activating mutation and loss of STK11 (LKB1), which was enhanced by the addition of 2-DG (2-deoxyglucose) (PMID: 25436981). 25436981
ERBB2 R896C breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 (HER2) R896C reverted to normal morphology in culture upon Nerlynx (neratinib) treatment (PMID: 23220880). 23220880
ERBB2 R896C breast cancer sensitive Trastuzumab Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 R896C reverted to normal morphology in culture upon Herceptin (trastuzumab) treatment (PMID: 23220880). 23220880
ERBB2 R896C breast cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, transformed human breast cell lines expressing ERBB2 R896C reverted to normal morphology in culture upon Tykerb (lapatinib) treatment (PMID: 23220880). 23220880
ERBB2 L755S Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive Tesevatinib Preclinical Actionable In a preclinical study, XL647 inhibited survival of transformed cells over expressing ERBB2 (HER2) L755S in culture (PMID: 18413839). 18413839
ERBB2 L755S Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor resistant Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 L755S colorectal cancer conflicting Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of colorectal cancer cells over expressing ERBB2 (HER2) L755S in culture (PMID: 26243863). 26243863
ERBB2 L755S colorectal cancer conflicting Neratinib Preclinical - Cell line xenograft Actionable In a preclinical study, Nerlynx (neratinib) treatment resulted in increased tumor growth compared to vehicle control in cell line xenograft models of colorectal cancer harboring ERBB2 (HER2) L755S (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive EKI-785 Preclinical Actionable In a preclinical study, EKI-285 (CL-387785) inhibited proliferation of transformed cell lines expressing ERBB2 (HER2) L755S in culture (PMID: 22046346). 22046346
ERBB2 L755S Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 L755S biliary tract cancer no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease in one and stable disease in another patient with biliary tract cancer harboring ERBB2 (HER2) L755S (PMID: 29420467; NCT01953926). 29420467
ERBB2 L755S breast cancer sensitive Lapatinib + Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Tykerb (lapatinib) and Selumetinib (AZD6244) synergistically inhibited viability of transformed breast epithelial cells expressing ERBB2 L755S in culture (PMID: 31135266). 31135266
ERBB2 L755S colon cancer sensitive Trastuzumab Preclinical Actionable In a preclinical study, Herceptin (trastuzumab) inhibited colony formation in transformed mouse colon epithelial cells over expressing ERBB2 (HER2) L755S in culture (PMID: 26243863). 26243863
ERBB2 L755S Her2-receptor negative breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in complete response in 1 patient, partial response in 1 patient, stable disease in 2 patients, and progressive disease in 4 patients with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) L755S (PMID: 29420467; NCT01953926). 29420467
ERBB2 L755S colon cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited colony formation in transformed mouse colon epithelial cells over expressing ERBB2 (HER2) L755S in culture (PMID: 26243863). 26243863
ERBB2 L755S Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 L755S breast cancer resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed breast epithelial cells expressing ERBB2 (HER2) L755S were resistant to Tykerb (lapatinib) in culture (PMID: 31135266). 31135266
ERBB2 L755S breast cancer conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, treatment with Nerlynx (neratinib) resulted in growth inhibition in transformed human breast cell lines expressing ERBB2 (HER2) L755S in culture (PMID: 23220880). 23220880
ERBB2 L755S breast cancer conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed breast epithelial cells expressing ERBB2 (HER2) L755S were resistant to Nerlynx (neratinib) in culture (PMID: 31135266). 31135266
ERBB2 L755S breast cancer conflicting Neratinib Case Reports/Case Series Actionable In a Phase II trial, Nerlynx (neratinib) treatment resulted in a clinical benefit rate of 31% (5/16) in metastatic breast cancer patients harboring ERBB2 (HER2) mutations, with 1 partial response and 1 stable disease in 6 patients harboring ERBB2 (HER2) L755S (PMID: 28679771; NCT01670877). 28679771
ERBB2 L755S colorectal cancer sensitive Poziotinib Preclinical - Cell line xenograft Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited viability of colorectal cancer cells harboring ERBB2 (HER2) L755S in culture, and reduced tumor size by 58% in a cell line xenograft model (PMID: 31588020). 31588020
ERBB2 L755S breast cancer sensitive Lapatinib + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Tykerb (lapatinib) and Pictilisib (GDC-0941) synergistically inhibited viability of transformed breast epithelial cells expressing ERBB2 L755S in culture (PMID: 31135266). 31135266
ERBB2 L755S Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor resistant AEE788 Preclinical Actionable In a preclinical study, transformed cell lines expressing ERBB2 (HER2) L755S demonstrated resistance to AEE788 in culture, except at very high doses (PMID: 22046346). 22046346
ERBB2 L755S Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 L755S colorectal cancer resistant Panitumumab Preclinical Actionable In a preclinical study, colorectal cancer cells over expressing ERBB2 (HER2) L755S were resistant to Vectibix (panitumumab) in culture (PMID: 26243863). 26243863
ERBB2 L755S Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 L755S breast cancer sensitive Neratinib + Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) and Selumetinib (AZD6244) synergistically inhibited viability of transformed breast epithelial cells expressing ERBB2 L755S in culture (PMID: 31135266). 31135266
ERBB2 L755S Her2-receptor positive breast cancer resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, expression of ERBB2 (HER2) L755S conferred resistance to Tykerb (lapatinib) in ERBB2 (HER2)-positive breast cancer cell lines in culture (PMID: 28487443). 28487443
ERBB2 L755S colorectal cancer conflicting Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited growth of colorectal cancer cells over expressing ERBB2 (HER2) L755S in culture (PMID: 26243863). 26243863
ERBB2 L755S colorectal cancer conflicting Afatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Gilotrif (afatinib) did not significantly inhibit tumor growth compared to vehicle control in cell line xenograft models of colorectal cancer harboring ERBB2 (HER2) L755S (PMID: 31588020). 31588020
ERBB2 L755S lung non-small cell carcinoma predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in partial response with a progression-free survival of 12.7 months in a patient with non-small cell lung cancer harboring ERBB2 (HER2) L755S (PMID: 29420467; NCT01953926). 29420467
ERBB2 L755S colorectal cancer resistant Cetuximab Preclinical Actionable In a preclinical study, colorectal cancer cells over expressing ERBB2 (HER2) L755S were resistant to Erbitux (cetuximab) in culture (PMID: 26243863). 26243863
ERBB2 L755S Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S demonstrated resistance when treated with Tykerb (lapatinib) in culture (PMID: 22046346). 22046346
ERBB2 L755S Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive WZ4002 Preclinical Actionable In a preclinical study, WZ4002 inhibited proliferation of transformed cell lines expressing ERBB2 (HER2) L755S in culture (PMID: 22046346). 22046346
ERBB2 L755S breast cancer sensitive Neratinib + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) and Pictilisib (GDC-0941) synergistically inhibited viability of transformed breast epithelial cells expressing ERBB2 L755S in culture (PMID: 31135266). 31135266
APC Q1429fs BRAF N581S ERBB2 L755S rectum adenocarcinoma no benefit Fluorouracil + Leucovorin + Trastuzumab Case Reports/Case Series Actionable In a clinical case study, a rectal adenocarcinoma patient harboring APC Q1429fs, BRAF N581S, and ERBB2 L755S did not respond to Herceptin (trastuzumab) treatment in combination with Fluorouracil and Wellcovorin (leucovorin) (PMID: 27626067). 27626067
ERBB2 L755S PIK3CA H1047R breast cancer resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring ERBB2 (HER2) L755S and PIK3CA H1047R demonstrated resistance to Nerlynx (neratinib) in culture (PMID: 31978326). 31978326
ERBB2 L755S PIK3CA H1047R breast cancer sensitive Everolimus + Neratinib Preclinical - Cell culture Actionable In a preclinical study, Afinitor (everolimus) and Nerlynx (neratinib) worked synergistically to inhibit viability of a breast cancer cell line harboring ERBB2 (HER2) L755S and PIK3CA H1047R in culture (PMID: 31978326). 31978326
ERBB2 N857S Advanced Solid Tumor decreased response Lapatinib Preclinical Actionable In a preclinical study, higher dose of Tykerb (lapatinib) inhibited proliferation of transformed cell lines expressing ERBB2 (HER2) N857S in culture (PMID: 22046346). 22046346
ERBB2 N857S Advanced Solid Tumor sensitive AEE788 Preclinical Actionable In a preclinical study, AEE788 inhibited proliferation of transformed cell lines expressing ERBB2(HER2) N857S in culture (PMID: 22046346). 22046346
ERBB2 L755P lung adenocarcinoma no benefit Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, treatment with Kadcyla (trastuzumab emtansine) resulted in best overall responses of partial response in 44% (8/18) and stable disease in 39% (7/18), and median progression-free survival of 5 months in patients with lung adenocarcinoma harboring ERBB2 (HER2) activating mutations, but a subset of patients specifically harboring ERBB2 L755P (2/2) did not demonstrate a partial response (PMID: 29989854; NCT02675829). 29989854
ERBB2 L755P lung non-small cell carcinoma predicted - sensitive Poziotinib Case Reports/Case Series Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in stable disease lasted more than 7 months in a patient with non-small cell lung cancer harboring ERBB2 (HER2) L755P (PMID: 31588020; NCT03066206). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor sensitive WZ4002 Preclinical Actionable In a preclinical study, WZ4002 inhibited proliferation of transformed cell lines expressing ERBB2 (HER2) L755P in culture (PMID: 22046346). 22046346
ERBB2 L755P Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cell lines expressing ERBB2 (HER2) L755P demonstrated resistance when treated with Tykerb (lapatinib) in culture (PMID: 22046346). 22046346
ERBB2 L755P Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor sensitive EKI-785 Preclinical Actionable In a preclinical study, EKI-285 (CL-387785) inhibited proliferation of transformed cell lines expressing ERBB2 (HER2) L755P in culture (PMID: 22046346). 22046346
ERBB2 L755P Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) L755P in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) L755P in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P lung non-small cell carcinoma no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 14.8 months in a patient with non-small cell lung cancer harboring ERBB2 (HER2) L755P (PMID: 29420467; NCT01953926). 29420467
ERBB2 L755P lung non-small cell carcinoma predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 L755P demonstrated a partial response when treated with Pyrotinib (PMID: 30596880; NCT02535507). 30596880
ERBB2 L755P lung non-small cell carcinoma predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a Phase II trial, Pyrotinib treatment resulted in an objective response rate of 25% (1/4) in non-small cell lung cancer patients harboring ERBB2 (HER2) L755P who had received prior platinum-based chemotherapy (PMID: 32614698; NCT02834936). 32614698
ERBB2 L755P Advanced Solid Tumor resistant Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant AEE788 Preclinical Actionable In a preclinical study, transformed cell lines expressing ERBB2 (HER2) L755P demonstrated resistance when treated with AEE788 in culture (PMID: 22046346). 22046346
ERBB2 G776delinsVV Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsVV in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited growth of a transformed cell line expressing ERBB2 (HER2) G776delinsVV in culture (PMID: 29686424). 29686424
ERBB2 G776delinsVV Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsVV in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 P780L Advanced Solid Tumor resistant Lapatinib Preclinical Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) P780L demonstrated resistance to treatment with Tykerb (lapatinib) (PMID: 18413839). 18413839
ERBB2 P780L Advanced Solid Tumor sensitive Tesevatinib Preclinical Actionable In a preclinical study, XL647 inhibited survival of transformed cells over expressing ERBB2 (HER2) P780L in culture (PMID: 18413839). 18413839
ERBB2 R188C cancer sensitive Pelitinib Preclinical - Cell culture Actionable In a preclinical study, Pelitinib inhibited growth of transformed cells expressing ERBB2 (HER2) R188C in culture (PMID: 32366937). 32366937
ERBB2 R188C cancer sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited growth of transformed cells expressing ERBB2 (HER2) R188C in culture (PMID: 32366937). 32366937
ERBB2 R188C cancer sensitive Canertinib Preclinical - Cell culture Actionable In a preclinical study, Canertinib (CI-1033) inhibited growth of transformed cells expressing ERBB2 (HER2) R188C in culture (PMID: 32366937). 32366937
ERBB2 R188C cancer sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited growth of transformed cells expressing ERBB2 (HER2) R188C in culture (PMID: 32366937). 32366937
ERBB2 R188C cancer no benefit Erlotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) R188C did not demonstrate sensitivity to growth inhibition by Tarceva (erlotinib) in culture (PMID: 32366937). 32366937
ERBB2 R188C cancer no benefit Gefitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) R188C did not demonstrate sensitivity to growth inhibition by Iressa (gefitinib) in culture (PMID: 32366937). 32366937
ERBB2 R188C cancer sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of transformed cells expressing ERBB2 (HER2) R188C in culture (PMID: 32366937). 32366937
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells co-expressing ERBB2 (HER2) C805S and ERBB2 (HER2) Y772_A775dup (also referred to as A775_G776insYVMA) demonstrated resistance to Vizimpro (dacomitinib) in culture (PMID: 28363995). 28363995
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S were resistant to Tykerb (lapatinib) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells co-expressing ERBB2 (HER2) Y772_A775dup (also referred to as A775_G776insYVMA) and ERBB2 (HER2) C805S demonstrated resistance to Nerlynx (neratinib) in culture (PMID: 28363995). 28363995
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S were resistant to Tagrisso (osimertinib) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor predicted - sensitive Luminespib Preclinical - Cell culture Actionable In a preclinical study, Luminespib (AUY922) inhibited growth of transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S were resistant to Pyrotinib in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Erlotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S were resistant to Tarceva (erlotinib) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells co-expressing ERBB2 (HER2) Y772_A775dup (also referred to as A775_G776insYVMA) and ERBB2 (HER2) C805S demonstrated resistance to Gilotrif (afatinib) in culture (PMID: 28363995). 28363995
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor predicted - sensitive Ganetespib Preclinical - Cell culture Actionable In a preclinical study, Ganetespib inhibited growth of transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Tucatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S were resistant to Tukysa (tucatinib) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant Poziotinib Preclinical - Cell culture Actionable In a preclinical study, ERBB2 (HER2) C805S was identified as a secondary mutation in transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) that acquired resistance to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup ERBB2 C805S Advanced Solid Tumor resistant AZ5104 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S were resistant to AZ5104 in culture (PMID: 30527195). 30527195
ERBB2 M774delinsWLV ERBB2 C805S Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, acquisition of ERBB2 (HER2) C805S in transformed cells expressing ERBB2 (HER2) M774delinsWLV conferred resistance to Vizimpro (dacomitinib) in culture (PMID: 28363995). 28363995
ERBB2 M774delinsWLV ERBB2 C805S Advanced Solid Tumor resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells co-expressing ERBB2 (HER2) M774delinsWLV and ERBB2 (HER2) C805S demonstrated resistance to Nerlynx (neratinib) in culture (PMID: 28363995). 28363995
ERBB2 M774delinsWLV ERBB2 C805S Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells co-expressing ERBB2 (HER2) M774delinsWLV and ERBB2 (HER2) C805S demonstrated resistance to Gilotrif (afatinib) in culture (PMID: 28363995). 28363995
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Gilotrif (afatinib) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Vizimpro (dacomitinib) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Tykerb (lapatinib) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Pyrotinib in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Erlotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Tarceva (erlotinib) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant AZ5104 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to AZ5104 in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Nerlynx (neratinib) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Poziotinib Preclinical - Cell culture Actionable In a preclinical study, ERBB2 (HER2) C805S was identified as a secondary mutation in transformed cells expressing ERBB2 (HER2) G776delinsVC that acquired resistance to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor predicted - sensitive Luminespib Preclinical - Cell culture Actionable In a preclinical study, Luminespib (AUY922) inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Tagrisso (osimertinib) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor predicted - sensitive Ganetespib Preclinical - Cell culture Actionable In a preclinical study, Ganetespib inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC ERBB2 C805S Advanced Solid Tumor resistant Tucatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Tucatinib (ARRY-380) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC lung non-small cell carcinoma no benefit Dacomitinib Clinical Study Actionable In a retrospective analysis, Vizimpro (dacomitinib) treatment resulted in an objective response rate of 0% (0/2) in non-small cell lung cancer patients harboring ERBB2 (HER2) G776delinsVC (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor decreased response Erlotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC demonstrated decreased response to Tarceva (erlotinib) compared to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC lung non-small cell carcinoma no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 8.5 months in a patient with non-small cell lung cancer harboring ERBB2 (HER2) G776delinsVC (PMID: 29420467; NCT01953926). 29420467
ERBB2 G776delinsVC Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor resistant Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tarloxotinib (TRLX) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor predicted - sensitive Luminespib Preclinical - Cell culture Actionable In a preclinical study, Luminespib (AUY922) inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC lung non-small cell carcinoma no benefit Lapatinib Clinical Study Actionable In a retrospective analysis, Tykerb (lapatinib) treatment resulted in an objective response rate of 0% (0/1) in non-small cell lung cancer patients harboring ERBB2 (HER2) G776delinsVC (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor predicted - sensitive Ganetespib Preclinical - Cell culture Actionable In a preclinical study, Ganetespib inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC lung non-small cell carcinoma resistant Gefitinib Preclinical Actionable In a preclinical study, non-small cell lung cancer cells harboring ERBB2 (HER2) G776delinsVC demonstrated resistance to treatment with Iressa (gefitinib) in culture (PMID: 26545934). 26545934
ERBB2 G776delinsVC Advanced Solid Tumor resistant Tucatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tukysa (tucatinib) in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor sensitive AZ5104 Preclinical - Cell culture Actionable In a preclinical study, AZ5104 inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC lung adenocarcinoma predicted - sensitive Afatinib Clinical Study - Cohort Actionable In a retrospective study, Gilotrif (afatinib) treatment resulted in an objective response rate (ORR) of 15.6% (5/32) and a disease control rate of 68.8% (22/32) in patients with lung adenocarcinoma harboring ERBB2 (HER2) mutations, patients harboring G776delinsVC (n=5) or G778_P780dup (n=5) achieved longer median progression-free survival (7.6 mo) than those with Y772_A775dup (n=14, 1.2 mo) or missense mutations (n=8, 3.6 mo), with an ORR of 40% (4/10) and a DCR of 100% (10/10) (PMID: 32162827). 32162827
ERBB2 G776delinsVC lung adenocarcinoma predicted - sensitive Poziotinib Case Reports/Case Series Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in a partial response in one patient and stable disease in another patient with lung adenocarcinoma harboring ERBB2 (HER2) G776delinsVC (PMID: 30149884; NCT02979821). 30149884
ERBB2 G776delinsVC Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited growth of a transformed cell line expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 29686424). 29686424
ERBB2 G776delinsVC Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC lung adenocarcinoma predicted - sensitive Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, treatment with Kadcyla (trastuzumab emtansine) resulted in best overall responses of partial response in 44% (8/18) and stable disease in 39% (7/18), and median progression-free survival of 5 months in patients with lung adenocarcinoma harboring ERBB2 (HER2) activating mutations, and a subset of patients specifically harboring ERBB2 (HER2) G776delinsVC had a 100% (2/2) partial response rate (PMID: 29989854; NCT02675829). 29989854
ERBB2 G776delinsVC lung cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited Erbb2 (Her2) phosphorylation and downstream signaling in bronchial epithelial cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 26545934). 26545934
ERBB2 G776delinsVC breast cancer sensitive Ado-trastuzumab emtansine + Poziotinib Preclinical - Cell culture Actionable In a preclinical study, addition of Poziotinib (HM781-36B) enhanced growth inhibition by Kadcyla (ado-trastuzumab emtansine) treatment in breast cancer cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC lung non-small cell carcinoma no benefit Erlotinib Clinical Study Actionable In a retrospective analysis, Tarceva (erlotinib) treatment resulted in an objective response rate of 0% (0/1) in non-small cell lung cancer patients harboring ERBB2 (HER2) G776delinsVC (PMID: 30527195). 30527195
ERBB2 G776delinsVC lung non-small cell carcinoma conflicting Afatinib Clinical Study Actionable In a retrospective analysis, Gilotrif (afatinib) treatment resulted in an objective response rate of 0% (0/3) in non-small cell lung cancer patients harboring ERBB2 (HER2) G776delinsVC (PMID: 30527195). 30527195
ERBB2 G776delinsVC lung non-small cell carcinoma conflicting Afatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Gilotrif (afatinib) inhibited proliferation and induced cell-cycle arrest and apoptosis of a non-small cell lung cancer (NSCLC) cell line harboring ERBB2 (HER2) G776delinsVC in culture and inhibited tumor growth in NSCLC cell line xenografts carrying ERBB2 (HER2) G776delinsVC (PMID: 26545934). 26545934
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC lung non-small cell carcinoma predicted - sensitive Poziotinib Clinical Study Actionable In a retrospective analysis, Poziotinib (HM781-36B) treatment resulted in an objective response rate of 50% (1/2) in non-small cell lung cancer patients harboring ERBB2 (HER2) G776delinsVC (PMID: 30527195). 30527195
ERBB2 G776delinsVC lung cancer no benefit Gefitinib Preclinical Actionable In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) G776delinsVC did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). 26545934
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). 30527195
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC breast cancer sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited Erbb2 (Her2) phosphorylation and viability of breast cancer cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC lung non-small cell carcinoma no benefit Ado-trastuzumab emtansine Case Reports/Case Series Actionable In a Phase II trial, Kadcyla (ado-trastuzumab emtansine) treatment demonstrated limited efficacy in patients with relapsed non-small cell lung cancer harboring ERBB2 (Her2) mutations, resulting in progressive disease in a patient harboring ERBB2 (HER2) G776delinsVC (PMID: 29313813). 29313813
ERBB2 G776delinsVC lung non-small cell carcinoma predicted - sensitive Pyrotinib Case Reports/Case Series Actionable In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 G776delinsVC demonstrated a partial response and an ongoing progression-free survival when treated with Pyrotinib (PMID: 30596880; NCT02535507). 30596880
ERBB2 G776delinsVC Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tykerb (lapatinib) in culture (PMID: 30527195). 30527195
ERBB2 S310Y urinary bladder cancer no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease in 2 patients and progressive disease in 2 patients with bladder cancer harboring ERBB2 (HER2) S310Y (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310Y lung squamous cell carcinoma predicted - sensitive Afatinib Case Reports/Case Series Actionable In a clinical case study, Gilotrif (afatinib) treatment resulted in stable disease over 8-months in a patient with advanced squamous cell lung carcinoma harboring ERBB2 (HER2) S310Y (PMID: 30584328). 30584328
ERBB2 S310Y gastroesophageal junction adenocarcinoma predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 0.8 month in a patient with gastroesophageal cancer harboring ERBB2 (HER2) S310Y (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310Y colorectal cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) delayed tumor growth in xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) S310Y (PMID: 26243863). 26243863
ERBB2 S310Y cervical cancer predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 0.5 month in a patient with cervical cancer harboring ERBB2 (HER2) S310Y (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310Y colorectal cancer sensitive Lapatinib + Trastuzumab Preclinical Actionable In a preclinical study, Herceptin (trastuzumab) and Tykerb (lapatinib) combination treatment resulted in tumor regression in xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) S310Y (PMID: 26243863). 26243863
ERBB2 S310Y colorectal cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) delayed tumor growth in xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) S310Y (PMID: 26243863). 26243863
ERBB2 S310Y colorectal cancer resistant Cetuximab Preclinical Actionable In a preclinical study, xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) S310Y were resistant to Erbitux (cetuximab) (PMID: 26243863). 26243863
ERBB2 S310Y endometrial cancer no benefit Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease with a progression-free survival of 9.6 months in a patient with endometrial cancer harboring ERBB2 (HER2) S310Y (PMID: 29420467; NCT01953926). 29420467
ERBB2 S310Y colorectal cancer sensitive Trastuzumab Preclinical Actionable In a preclinical study, Herceptin (trastuzumab) delayed tumor growth in xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) S310Y (PMID: 26243863). 26243863
ERBB2 S310Y colorectal cancer sensitive Neratinib + Trastuzumab Preclinical Actionable In a preclinical study, Herceptin (trastuzumab) and Nerlynx (neratinib) combination treatment resulted in tumor regression in xenograft models of patient derived colorectal cancer cells harboring ERBB2 (HER2) S310Y (PMID: 26243863). 26243863
ERBB2 Y772_A775dup lung adenocarcinoma predicted - sensitive Poziotinib Case Reports/Case Series Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in one partial response, stable disease in one patient, and progressive disease in three patients with lung adenocarcinoma harboring ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) (PMID: 30149884; NCT02979821). 30149884
ERBB2 Y772_A775dup Advanced Solid Tumor resistant AZ5104 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) were resistant to AZ5104 in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup breast cancer sensitive Ado-trastuzumab emtansine + Poziotinib Preclinical - Cell culture Actionable In a preclinical study, addition of Poziotinib (HM781-36B) enhanced growth inhibition by Kadcyla (ado-trastuzumab emtansine) treatment in breast cancer cells expressing ERBB2 (HER2) Y772_A775dup in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung non-small cell carcinoma predicted - sensitive Afatinib Clinical Study Actionable In a retrospective analysis, Gilotrif (afatinib) treatment resulted in an objective response rate of 16% (5/31) in non-small cell lung cancer patients harboring ERBB2 (HER2) Y772_A775dup (reported as (A775_G776insYVMA) (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Her2-receptor negative breast cancer predicted - sensitive Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in complete response in one patient, and stable disease in 2 patient with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) Y772_A775dup (PMID: 29420467; NCT01953926). 29420467
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) were resistant to Tagrisso (osimertinib) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup lung cancer no benefit Gefitinib Preclinical Actionable In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) Y772_A775dup (also referred to as A775_G776insYVMA) did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). 26545934
ERBB2 Y772_A775dup urinary bladder cancer predicted - resistant Neratinib Case Reports/Case Series Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in progressive disease with a progression-free survival of 1.7 months in a patients with bladder cancer harboring ERBB2 (HER2) Y722_A775dup (PMID: 29420467; NCT01953926). 29420467
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) demonstrated decreased response to Gilotrif (afatinib) compared to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of transformed cells expressing ERBB2 (HER2) Y772_A775dup (also referred to as ERBB2 A775_G776insYVMA) in culture (PMID: 28363995). 28363995
ERBB2 Y772_A775dup lung non-small cell carcinoma predicted - sensitive Poziotinib Phase II Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in a confirmed objective response rate of 42% (5/12) in patients with non-small cell lung cancer harboring ERBB2 (HER2) Y772_A775dup (n=9) or ERBB2 (HER2) G778_P780dup (n=3), with a median progression-free survival of 5.6 months (PMID: 31588020; NCT03066206). 31588020
ERBB2 Y772_A775dup lung non-small cell carcinoma predicted - sensitive Poziotinib Clinical Study Actionable In a retrospective analysis, Poziotinib (HM781-36B) treatment resulted in an objective response rate of 33% (1/3) in non-small cell lung cancer patients harboring ERBB2 (HER2) Y772_A775dup (reported as (A775_G776insYVMA) (PMID: 30527195). 30527195
ERBB2 Y772_A775dup lung non-small cell carcinoma no benefit Dacomitinib Clinical Study Actionable In a retrospective analysis, Vizimpro (dacomitinib) treatment resulted in an objective response rate of 0% (0/13) in non-small cell lung cancer patients harboring ERBB2 (HER2) Y772_A775dup (reported as (A775_G776insYVMA) (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Erlotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) were resistant to Tarceva (erlotinib) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) demonstrated decreased response to Vizimpro (dacomitinib) compared to Poziotinib (HM781-36B) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung adenocarcinoma no benefit Afatinib Case Reports/Case Series Actionable In a clinical study, a lung adenocarcinoma patient harboring ERBB2 Y772_A775dup (also referred to as A775_G776insYVMA and E740_A741insAYVM) achieved a partial response for 5 months following treatment with pulse Gilotrif (afatinib), however, a second patient harboring ERBB2 Y772_A775dup treated with pulse Gilotrif (afatinib) demonstrated progressive disease (PMID: 26964772). 26964772
ERBB2 Y772_A775dup lung adenocarcinoma no benefit Afatinib Clinical Study - Cohort Actionable In a retrospective study, Gilotrif (afatinib) treatment resulted in an objective response rate (ORR) of 15.6% (5/32) and a disease control rate of 68.8% (22/32) in patients with lung adenocarcinoma harboring ERBB2 (HER2) mutations, ORR (0%, 0/14), DCR (35.7%, 5/14), and median progression-free survival (1.2 mo) were significantly lower in patients with Y772_A775dup than those with other exon 20 insertions (40%, 4/10; 100%, 10/10; 7.6 mo) or missense mutations (13%, 1/8; 75%, 6/8; 3.6 mo) (PMID: 32162827). 32162827
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) were resistant to Tykerb (lapatinib) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Advanced Solid Tumor conflicting Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y722_A755dup were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor conflicting Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited growth of transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Advanced Solid Tumor predicted - sensitive Ganetespib Preclinical - Cell culture Actionable In a preclinical study, Ganetespib inhibited growth of transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as reported as A775_G776insYVMA) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup lung non-small cell carcinoma predicted - sensitive Pyrotinib Phase II Actionable In a Phase II trial, Pyrotinib treatment resulted in an objective response rate of 27.3% (12/44) in non-small cell lung cancer patients harboring ERBB2 (HER2) Y772_A775dup (also reported as A775_G776insYVMA or M774_A775insAYVM) who had received prior platinum-based chemotherapy (PMID: 32614698; NCT02834936). 32614698
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Tucatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) were resistant to Tukysa (tucatinib) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Advanced Solid Tumor predicted - sensitive Luminespib Preclinical - Cell culture Actionable In a preclinical study, Luminespib (AUY922) inhibited growth of transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as reported as A775_G776insYVMA) in culture (PMID: 30527195). 30527195
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung cancer sensitive Afatinib Preclinical Actionable In a preclinical study, Gilotrif (afatinib) inhibited Erbb2 (Her2) phosphorylation and downstream signaling in bronchial epithelial cells expressing ERBB2 (HER2) Y772_A775dup (also referred to as A775_G776insYVMA) in culture (PMID: 26545934). 26545934
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Tarloxotinib (TRLX) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung non-small cell carcinoma sensitive Ado-trastuzumab emtansine + Poziotinib Preclinical - Pdx Actionable In a preclinical study, Poziotinib (HM781-36B) and Kadcyla (ado-trastuzumab emtansine) combination treatment resulted in sustained tumor regression in patient-derived xenograft models of non-small cell lung cancer harboring ERBB2 (HER2) Y772_A775dup (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung cancer sensitive Poziotinib Preclinical Actionable In a preclinical study, Poziotinib (HM781-36B) induced regression of lung tumors in mouse models harboring ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA), with no signs of progression at 12 weeks (PMID: 29686424). 29686424
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung non-small cell carcinoma no benefit Neratinib Phase II Actionable In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in stable disease in 5 patients and progressive disease in 4 patients with non-small cell lung cancer harboring ERBB2 (HER2) Y772_A775dup (PMID: 29420467; NCT01953926). 29420467
ERBB2 Y772_A775dup Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited ERBB2 (HER2) phosphorylation and growth of a transformed cell line expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) in culture (PMID: 29686424). 29686424
ERBB2 Y772_A775dup Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) Y772_A775dup in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup breast cancer sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited viability of breast cancer cells expressing ERBB2 (HER2) Y772_A775dup in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung non-small cell carcinoma no benefit Erlotinib Clinical Study Actionable In a retrospective analysis, Tarceva (erlotinib) treatment resulted in an objective response rate of 0% (0/1) in non-small cell lung cancer patients harboring ERBB2 (HER2) Y772_A775dup (reported as (A775_G776insYVMA) (PMID: 30527195). 30527195
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Abemaciclib + Fulvestrant + Trastuzumab Phase II Actionable In a Phase II trial, the combination therapy of Verzenio (abemaciclib), Herceptin (trastuzumab), and Faslodex (fulvestrant) in patients with ERBB2 (HER2)-receptor positive breast cancer (n=79) resulted in safety and a greater progression-free survival (PFS) compared to patients treated with standard of care chemotherapy plus Herceptin (trastuzumab) (n=79), demonstrating a PFS of 8.3 months versus 5.7 months (p=0.051), respectively (PMID: 32353342; NCT02675231). 32353342
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Trastuzumab + Tucatinib Phase Ib/II Actionable In a Phase Ib clinical trial, the combination of Tukysa (tucatinib) and Herceptin (trastuzumab) demonstrated clinical activity in central nervous system (CNS) metastases in patients with ERBB2 (HER2)-positive metastatic breast cancer, with 100% (3/3) patients achieving CNS stable disease as best response (San Antonio Breast Cancer Symposium 2015, Abstract P4-14-19). detail...
ERBB2 positive ovarian carcinoma sensitive Trastuzumab Duocarmazine Preclinical - Cell culture Actionable In a preclinical study, Trastuzumab Duocarmazine (SYD985) decreased survival of a ERBB2 (HER2)-positive ovarian carcinoma cell line in culture (PMID: 25589493). 25589493
ERBB2 positive Her2-receptor positive breast cancer sensitive Capecitabine + Trastuzumab Phase Ib/II Actionable In a Phase Ib/II trial, the combination therapy of Herceptin (trastuzumab) and Xeloda (capecitabine) resulted in an objective response rate of 56% (5/9) in pretreated ERBB2 (HER2)-receptor positive breast cancer patients, including 5 patients with a partial response (PMID: 31892325). 31892325
ERBB2 positive Her2-receptor positive breast cancer sensitive Capecitabine + Trastuzumab Phase II Actionable In Phase II clinical trials, the combination of Xeloda (capecitabine) and Herceptin (trastuzumab) demonstrated efficacy with a manageable toxicity profile in heavily pretreated patients with ERBB2 (HER2)-positive advanced breast cancer and earlier Herceptin (trastuzumab) exposure (PMID: 17679724). 17679724
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Poziotinib Phase II Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in a median progression-free survival of 4.04 months, and a disease control rate of 75.49% (77/102; 20 partial responses) in heavily-treated Erbb2 (Her2)-positive breast cancer patients (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 237O; NCT02418689). detail...
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive MEDI4276 Phase I Actionable In a Phase I trial, MEDI4276 treatment resulted in complete response in 1 patient with breast cancer, partial response in 1 patient with breast cancer, and stable disease in 12 patients with Erbb2 (Her2)-positive breast or gastric cancer (Annals of Oncology, Volume 29, Issue suppl_3, 1 March 2018, abstract 470; NCT02576548). detail...
ERBB2 positive breast cancer predicted - sensitive MP0274 Preclinical - Cell line xenograft Actionable In a preclinical study, MP0274 inhibited proliferation of Erbb2 (Her2)-positive breast cancer cells in culture and induced tumor regression in cell line xenograft models (Cancer Res 2013;73(24 Suppl): Abstract nr P4-12-30). detail...
ERBB2 positive colon carcinoma sensitive ADC ST8176AA1 Preclinical - Cell line xenograft Actionable In a preclinical study, ADC ST8176AA1 treatment reversed epithelial to mesenchymal (EMT) transition, induced DNA damage, increased apoptosis, and inhibited Erbb2 (Her2) signaling and proliferation of ERBB2 (HER2) expressing colon carcinoma cells in culture, and increased median survival in a cell line xenograft model (PMID: 32039017). 32039017
ERBB2 positive Her2-receptor positive breast cancer sensitive Lapatinib + MK2206 Phase I Actionable In a Phase I trial, Tykerb (lapatinib) and MK2206 combination treatment resulted in stable disease for more than 6 months in 40% (2/5) of patients with ERBB2 (HER2)-positive breast cancer (PMID: 27026198). 27026198
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive HER2 Vaccine Phase II Actionable In Phase II clinical trials, ERBB2 (HER2) vaccines demonstrated safety and some efficacy in the adjuvant setting in ERBB2 (HER2)-positive breast cancer patients (PMID: 23585514). 23585514
ERBB2 positive Her2-receptor positive breast cancer sensitive MYL-1401O + Paclitaxel Phase III Actionable In a Phase III trial, MYL-1401O demonstrated safety and efficacy comparable to Herceptin (trastuzumab) when given in combination with Taxol (paclitaxel), resulted in an objective response rate of 69.6% in ERBB2 (HER2)-positive breast cancer patients (J Clin Oncol 34, 2016 (suppl; abstr LBA503)). detail...
ERBB2 positive Advanced Solid Tumor predicted - sensitive Trastuzumab deruxtecan Phase I Actionable In a Phase I trial, treatment with Enhertu (fam-trastuzumab deruxtecan-nxki) was well-tolerated and resulted in an overall response rate (ORR) of 38% (19/50) and disease control rate (DCR) of 90% (45/50) in patients with ERBB2 (HER2)-expressing solid tumors, and an ORR of 29% (4/14) and DCR of 93% (13/14) in patients with low ERBB2 (HER2) expression (J Clin Oncol 35, 2017 (suppl; abstr 108)). detail...
ERBB2 positive gastroesophageal junction adenocarcinoma predicted - sensitive Trastuzumab deruxtecan Phase II Actionable In a Phase II trial (DESTINY-Gastric01), Enhertu (fam-trastuzumab deruxtecan-nxki) treatment improved objective response rate (51.3%, 61/119 vs 14.3%, 8/56, p<0.0001), median progression-free survival (5.6 vs 3.5 mo, HR=0.47, p=0.0003), and overall survival (12.5 vs 8.4 mo, HR=0.59, p=0.0097) compared to chemotherapy in patients with advanced ERBB2 (HER2)-positive gastric or gastroesophageal junction adenocarcinoma (J Clin Oncol 38: 2020 (suppl; abstr 4513); NCT03329690). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Trastuzumab deruxtecan FDA approved Actionable In a Phase II trial (DESTINY-Breast01) that supported FDA approval, Enhertu (fam-trastuzumab deruxtecan-nxki) treatment resulted in an objective response rate of 60.9% (112/184) in patients with unresectable or metastatic ERBB2 (HER2)-positive breast cancer who have received two or more prior anti-HER2 therapies, with a median response duration of 14.8 months and a median progression-free survival of 16.4 months (PMID: 31825192; NCT03248492). 31825192
ERBB2 positive Her2-receptor positive breast cancer sensitive Trastuzumab deruxtecan Preclinical - Pdx & cell culture Actionable In a preclinical study, Enhertu (fam-trastuzumab deruxtecan-nxki) inhibited growth of ERBB2 (HER2)-positive breast cancer cell lines in culture and xenograft models, and demonstrated antitumor activity in patient-derived xenograft (PDX) models of ERBB2 (HER2)-positive breast cancer, including models with low ERBB2 (HER2) expression (PMID: 27026201). 27026201
ERBB2 positive Advanced Solid Tumor predicted - sensitive MT-5111 Preclinical - Cell culture Actionable In a preclinical study, MT-5111 demonstrated toxicity against Erbb2 (Her2) positive tumor cell lines in culture regardless of their sensitivity to Kadcyla (ado-trastuzumab emtansine) (Cancer Res 2018;78(13 Suppl):Abstract nr 5769). detail...
ERBB2 positive Advanced Solid Tumor predicted - sensitive AC480 Phase I Actionable In a Phase I clinical trial, AC480 (BMS-599626) treatment demonstrated preliminary clinical activity, resulting in stable disease as best response in 25% (11/44) of patients with advanced solid tumors, including patients expressing EGFR and/or ERBB2, with 2 patients achieving stable disease for greater than 6 months (PMID: 21576284). 21576284
ERBB2 positive stomach cancer sensitive Lapatinib + Paclitaxel Phase III Actionable In a Phase III trial, second-line treatment using Tykerb (lapatinib) with paclitaxel demonstrated some efficacy in patients with HER2-positive advanced gastric cancer (PMID: 24868024). 24868024
ERBB2 positive Advanced Solid Tumor predicted - sensitive ZW25 Phase I Actionable In a Phase I trial, ZW25 treatment resulted in partial response in 14% (2/14) and stable disease in 21% (3/14) of patients with ERBB2 (HER2)-positive tumors, including breast, gastric, esophageal, colorectal, and adnexal cancers (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 255P; NCT02892123). detail...
ERBB2 positive salivary gland cancer predicted - sensitive Timigutuzumab Case Reports/Case Series Actionable In a Phase I trial, Timigutuzumab eliminated a tumor lesion 178 days following treatment in an ERBB2 (HER2)-positive salivary duct carcinoma patient, and led to a complete remission that was ongoing for 53 months (PMID: 30018811; NCT01409343). 30018811
ERBB2 positive uterine corpus serous adenocarcinoma sensitive Carboplatin + Paclitaxel + Trastuzumab Guideline Actionable Combination Paraplatin (carboplatin), Taxol (paclitaxel), and Herceptin (trastuzumab) is in guidelines for ERBB2 (HER2)-positive patients with advanced and recurrent uterine serous carcinoma (NCCN.org). detail...
ERBB2 positive gastroesophageal cancer predicted - sensitive Margetuximab + Pembrolizumab Phase Ib/II Actionable In a Phase Ib/II trial, the combination of Margetuximab (MGAH22) and Keytruda (pembrolizumab) demonstrated safety and tolerability with an objective response rate of 18.5% (17/92), median progression-free survival of 2.73 months, and median overall survival of 12.48 months in patients with ERBB2 (HER2)-positive gastroesophogeal adenocarcinoma (PMID: 32653053; NCT02689284). 32653053
ERBB2 positive salivary gland cancer sensitive Trastuzumab Guideline Actionable ERBB2 (HER2)-targeted therapy, including Herceptin (trastuzumab) is included in guidelines for patients with ERBB2 (HER2)-positive salivary gland tumors with distant metastases (NCCN.org). detail...
ERBB2 positive gastric adenocarcinoma predicted - sensitive Afatinib + Trastuzumab Phase II Actionable In a Phase II clinical trial, the combination therapy of Gilotrif (afatinib) and Herceptin (trastuzumab) in ERBB2 (HER2)-positive patients with either gastroesophageal junction adenocarcinoma, metastatic esophageal cancer, or gastric adenocarcinoma resulted in a partial response in 8% (1/12) and disease control for 4 months or more in 17% (2/12) (PMID: 30463996; NCT01522768). 30463996
ERBB2 positive stomach carcinoma sensitive Trastuzumab Duocarmazine Preclinical - Cell culture Actionable In a preclinical study, Trastuzumab Duocarmazine (SYD985) decreased survival of a ERBB2 (HER2)-positive gastric carcinoma cell line in culture (PMID: 25589493). 25589493
ERBB2 positive Her2-receptor positive breast cancer sensitive Neratinib + Paclitaxel Phase II Actionable In a Phase II trial, Nerlynx (neratinib) plus Taxol (paclitaxel) demonstrated similar efficacy to Herceptin (trastuzumab) plus Taxol (paclitaxel), with an median progression-free survival of 12.9 months, however, potentially decreased CNS metastasis risk, with an incidence of 8.3% (20/242) compared to 17.3% (41/237) in the Herceptin (trastuzumab) plus Taxol (paclitaxel) group (PMID: 27078022). 27078022
ERBB2 positive stomach cancer predicted - sensitive MEDI4276 Phase I Actionable In a Phase I trial, MEDI4276 treatment resulted in complete response in 1 patient with breast cancer, partial response in 1 patient with breast cancer, and stable disease in 12 patients with Erbb2 (Her2)-positive breast or gastric cancer (Annals of Oncology, Volume 29, Issue suppl_3, 1 March 2018, abstract 470; NCT02576548). detail...
ERBB2 positive breast adenocarcinoma sensitive Trastuzumab deruxtecan Preclinical - Cell culture Actionable In a preclinical study, Enhertu (fam-trastuzumab deruxtecan-nxki) inhibited growth of an ERBB2 (HER2)-positive breast adenocarcinoma cell line in culture (PMID: 27026201). 27026201
ERBB2 positive breast cancer sensitive XMT-1522 Preclinical - Cell line xenograft Actionable In a preclinical study, XMT-1522 demonstrated improved efficacy compared to Kadcyla (ado-trastuzumab emtansine), inhibited growth of Erbb2 (Her2)-positive breast cancer cells in culture, resulted in tumor regression and prolonged survival in cell line xenograft models (PMID: 31292166). 31292166
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Margetuximab + MGD013 Case Reports/Case Series Actionable In a Phase I trial, MGD013 and Margetuximab (MGAH22) combination treatment resulted in a partial response in 2 patients with ERBB2 (HER2)-positive breast cancer (J Clin Oncol 38: 2020 (suppl; abstr 3004); NCT03219268). detail...
ERBB2 positive Advanced Solid Tumor predicted - sensitive Margetuximab + MGD013 Phase I Actionable In a Phase I trial, MGD013 and Margetuximab (MGAH22) combination treatment resulted in a partial response in 50% (3/6) and stable disease in 33.3% (2/6) of patients with ERBB2 (HER2)-positive advanced solid tumors (J Clin Oncol 38: 2020 (suppl; abstr 3004); NCT03219268). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Everolimus + Trastuzumab + Vinorelbine Phase III Actionable In a Phase III trial (BOLERO-3), the combination of Afinitor (everolimus), Herceptin (trastuzumab), and Navelbine (vinorelbine) increased progression-free survival in patients with Herceptin (trastuzumab)-resistant, ERBB2 (HER2)-positive, advanced breast cancer who had prior taxane treatment (PMID: 24742739; NCT01007942). 24742739
ERBB2 positive stomach cancer predicted - sensitive Margetuximab Phase I Actionable In a Phase I trial, Margetuximab (MGAH22) treatment resulted in partial responses in 12% (7/60) and stable disease in 50% (30/60) of patients with ERBB2 (HER2)-positive breast or gastric cancer, or other carcinomas that overexpress Erbb2 (Her2) (PMID: 28119295). 28119295
ERBB2 positive Her2-receptor positive breast cancer sensitive MBS301 Preclinical - Cell line xenograft Actionable In a preclinical study, MBS301 inhibited proliferation of ERBB2 (HER2)-positive breast cancer cell lines expressing high or low levels of ERBB2 (HER2) in culture, and inhibited tumor growth in xenograft models (PMID: 30081724). 30081724
ERBB2 positive esophageal cancer predicted - sensitive Afatinib Phase II Actionable In a Phase II clinical trial, monotherapy with Gilotrif (afatinib) resulted in a moderate clinical benefit in ERBB2 (HER2)-positive patients with either gastroesophageal junction adenocarcinoma, metastatic esophageal cancer, or gastric adenocarcinoma, demonstrating a tumor reduction in 25% (5/20) according to RECIST, an objective partial response in 10% (2/20), a median progression-free survival of 2 months, and a median overall survival of 7 months (PMID: 30463996; NCT01522768). 30463996
ERBB2 positive Her2-receptor positive breast cancer sensitive Carboplatin + Docetaxel + Pertuzumab + Trastuzumab Guideline Actionable Taxotere (docetaxel), Paraplatin (carboplatin), and Herceptin (trastuzumab) plus Perjeta (pertuzumab) therapy, is included in the guidelines as adjuvant therapy for patients with hormone receptor-negative (ER and PR), ERBB2 (HER2)-positive breast cancer who are node positive (NCCN.org). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Tucatinib Phase I Actionable In a Phase I trial, treatment with Tukysa (tucatinib) resulted in a response rate of 14% (3/22; all partial responses (PR)) and a clinical benefit rate (PR plus stable disease for greater than or equal to 24 weeks) of 27% (6/22) in Erbb2 (Her2)-positive breast cancer patients (PMID: 28053022). 28053022
ERBB2 positive glioblastoma multiforme sensitive HER2 CAR-T cells Phase I Actionable In a Phase I trial, glioblastoma patients positive for ERBB2 (HER2) demonstrated antitumor activity when treated with ERBB2 (HER2)-CAR-T cell therapy including one patient with a partial response and seven patients with stable disease ranging from 8 weeks to 29 months (PMID: 28426845). 28426845
ERBB2 positive breast cancer sensitive ARX-788 Preclinical - Cell line xenograft Actionable In a preclinical study, an ERBB2 (HER2)-positive breast cancer xenograft model was sensitive to treatment with ARX-788, resulting in tumor regression (Cancer Res 2015;75(15 Suppl):Abstract nr 639). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Disitamab vedotin Preclinical - Cell culture Actionable In a preclinical study, Hertuzumab-vc-MMAE decreased viability of ERBB2 (HER2)-positive breast cancer cell lines in culture (PMID: 27509865). 27509865
ERBB2 positive salivary gland cancer predicted - sensitive Trastuzumab deruxtecan Phase I Actionable In a Phase I trial, treatment with Enhertu (fam-trastuzumab deruxtecan-nxki) resulted in a partial response in 50% (2/4) of evaluable patients with salivary gland cancer and ERBB2 (HER2) expression (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 409P; NCT02564900). detail...
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Epertinib + Trastuzumab Phase Ib/II Actionable In a Phase Ib/II trial, the combination therapy of Epertinib (S-222611) and Herceptin (trastuzumab) resulted in an objective response rate of 67% (6/9) in pretreated ERBB2 (HER2)-receptor positive breast cancer patients, including 6 patients with a partial response (PMID: 31892325). 31892325
ERBB2 positive Her2-receptor positive breast cancer sensitive Varlitinib Phase I Actionable In a Phase I expansion trial, 36% (5/14) of metastatic breast cancer patients positive for ERBB2 (HER2) demonstrated stable disease for up to 16 weeks when treated with Varlitinib (ARRY-334543) (Cancer Res May 1, 2009 69; 3603). detail...
ERBB2 positive ovarian cancer sensitive Disitamab vedotin Preclinical - Cell line xenograft Actionable In a preclinical study, treatment with Hertuzumab-vc-MMAE decreased viability of ERBB2 (HER2)-positive ovarian cancer cell lines in culture and inhibited tumor growth in ERBB2 (HER2)-positive ovarian cancer cell line xenograft models (PMID: 27509865). 27509865
ERBB2 positive ovarian cancer sensitive PRS-343 Preclinical - Cell line xenograft Actionable In a preclinical study, PRS-343 induced localized immune activation in cell line xenograft models of Erbb2 (Her2)-positive ovarian cancer, resulted in significant tumor growth inhibition (Eur J Cancer, Dec 2016, 69 (Suppl. 1): S99, abstract 301). detail...
ERBB2 positive gastric adenocarcinoma predicted - sensitive Afatinib Phase II Actionable In a Phase II clinical trial, monotherapy with Gilotrif (afatinib) resulted in a moderate clinical benefit in ERBB2 (HER2)-positive patients with either gastroesophageal junction adenocarcinoma, metastatic esophageal cancer, or gastric adenocarcinoma, demonstrating a tumor reduction in 25% (5/20) according to RECIST, an objective partial response in 10% (2/20), a median progression-free survival of 2 months, and a median overall survival of 7 months (PMID: 30463996; NCT01522768). 30463996
ERBB2 positive colorectal cancer predicted - sensitive Timigutuzumab Case Reports/Case Series Actionable In a Phase I trial, Timigutuzumab treatment resulted in a partial response in an ERBB2 (HER2)-positive colorectal cancer patient with a 56% reduction in tumor size following 56 days of treatment (PMID: 30018811; NCT01409343). 30018811
ERBB2 positive Her2-receptor positive breast cancer sensitive Sunitinib + Trastuzumab Phase II Actionable In a Phase II trial, Sutent (sunitinib), in combination with Herceptin (trastuzumab), demonstrated safety and efficacy in ERBB2 (HER2) positive advanced breast cancer patients (PMID: 24606768). 24606768
ERBB2 positive stomach cancer sensitive Oxaliplatin + Trastuzumab Preclinical Actionable In a preclinical study, the combination of Herceptin (trastuzumab) and Eloxatin (oxaliplatin) resulted in growth inhibition of ERBB2 (HER2)-positive gastric cancer cells in culture (PMID: 24300914). 24300914
ERBB2 positive Advanced Solid Tumor predicted - sensitive GBR1302 Phase I Actionable In a Phase I trial, GBR 1302 treatment resulted in no radiological response, only prolonged (more than 4 months) stable disease in 10.5% (2/19) of patients with ERBB2 (HER2) positive advanced solid tumors (Annals of Oncology, Volume 29, Issue suppl_8, October 2018, mdy288.020; NCT02829372). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Oxaliplatin + Trastuzumab Preclinical Actionable In a preclinical study, the combination of Herceptin (trastuzumab) and Eloxatin (oxaliplatin) resulted in growth inhibition of ERBB2 (HER2)-positive breast cancer cells in culture (PMID: 24300914). 24300914
ERBB2 positive Her2-receptor positive breast cancer sensitive Oxaliplatin + Tegafur-gimeracil-oteracil Potassium + Trastuzumab Phase II Actionable In a Phase II clinical trial, the combination of TS-1 (S-1) and Herceptin (trastuzumab) demonstrated safety and efficacy in patients with ERBB2 (HER2)-positive metastatic breast cancer, with an overall response rate of 53.6% (15/28), and a clinical benefit rate of 75.0% (21/28) (PMID: 24982373). 24982373
ERBB2 positive transitional cell carcinoma no benefit lapuleucel-T Phase II Actionable In a Phase II trial, Neuvenge (lapuleucel-T) treatment did not result in statistically significant improvement of overall survival (37.0 vs 22.2 months, HR = 0.96) or disease recurrence-free survival (11.9 vs 10.1 months, HR = 0.99) compared to standard of care in ERBB2 (HER2) positive urothelial cancer patients (J Clin Oncol 34, 2016 (suppl; abstr 4513)). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Cyclophosphamide + Doxorubicin + Paclitaxel + Pertuzumab + Trastuzumab Guideline Actionable Sequential therapy, Adriamycin (doxorubicin) and Cytoxan (cyclophosphamide), followed by Taxol (paclitaxel) plus Herceptin (trastuzumab) and Perjeta (pertuzumab), is included in the guidelines as adjuvant therapy for patients with hormone receptor-negative (ER and PR), ERBB2 (HER2)-positive breast cancer who are node positive (NCCN.org). detail...
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Capecitabine + Pyrotinib Phase I Actionable In a Phase I trial, Pyrotinib and Xeloda (capecitabine) combination treatment was well-tolerated, and resulted in an overall response rate of 78.6% (22/28) in patients with Erbb2 (Her2)-positive metastatic breast cancer, with a median progression-free survival of 22.1 months (PMID: 31138588; NCT02361112). 31138588
ERBB2 positive Her2-receptor positive breast cancer sensitive Lapatinib + Trastuzumab Phase II Actionable In a Phase II trial, Tykerb (lapatinib) and Herceptin (trastuzumab) combination treatment resulted in complete response in the breast in 10.6% (7/66) and minimal residual disease in 16.7% (11/66) of ERBB2-positive breast cancer patients 11 days after receiving the treatment (European Breast Cancer Conference; Mar 2016; Abstract #6LBA). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Lapatinib + Trastuzumab Clinical Study - Meta-analysis Actionable In a meta-analysis of six randomized clinical trials, Tykerb (lapatinib) and Herceptin (trastuzumab) combination treatment resulted in 13% absolute improvement in pathologic complete response rate in ERBB2 (HER2)-positive breast cancer patients compared to Herceptin (trastuzumab) single treatment (PMID: 27140927). 27140927
ERBB2 positive stomach cancer sensitive HER2 Vaccine Preclinical - Patient cell culture Actionable In a preclinical study, ERBB2 (HER2)-specific cytotoxic T-cell lines generated from gastric cancer patients demonstrated activity against autologous ERBB2 (HER2)-expressing gastric cancer cells in culture (PMID: 9754653). 9754653
ERBB2 positive ovarian cancer sensitive ARX-788 Preclinical - Cell line xenograft Actionable In a preclinical study, an ERBB2 (HER2)-positive ovarian cancer xenograft model was sensitive to treatment with ARX-788, resulting in tumor regression (Cancer Res 2015;75(15 Suppl):Abstract nr 639). detail...
ERBB2 positive Advanced Solid Tumor predicted - sensitive Epertinib Phase I Actionable In a Phase I clinical trial, S-222611 demonstrated safety and some efficacy in patients with advanced solid tumors expressing EGFR or ERBB2 (HER2), with an overall clinical benefit rate of 27% (7/33) (PMID: 25434923). detail... 25434923
ERBB2 positive esophageal cancer predicted - sensitive Afatinib + Trastuzumab Phase II Actionable In a Phase II clinical trial, the combination therapy of Gilotrif (afatinib) and Herceptin (trastuzumab) in ERBB2 (HER2)-positive patients with either gastroesophageal junction adenocarcinoma, metastatic esophageal cancer, or gastric adenocarcinoma resulted in a partial response in 8% (1/12) and disease control for 4 months or more in 17% (2/12) (PMID: 30463996; NCT01522768). 30463996
ERBB2 positive carcinoma sensitive Timigutuzumab Phase I Actionable In a Phase I study, Timigutuzumab treatment was well-tolerated and demonstrated safety, and resulted in a clinical benefit in 50% (1 complete response, 2 partial response, and 12 stable disease), a disease control rate of 50%, and an objective response rate of 10% in ERBB2 (HER2)-positive advanced carcinoma patients (n=30) (PMID: 30018811; NCT01409343). 30018811
ERBB2 positive breast cancer sensitive ZW49 Preclinical - Pdx Actionable In a preclinical study, ZW49 treatment induced tumor regression in patient-derived xenograft (PDX) models of breast cancer expressing low and high levels of ERBB2 (HER2) (Cancer Res 2019;79(4 Suppl):Abstract nr P6-17-13). detail...
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Ado-trastuzumab emtansine + Tucatinib Phase Ib/II Actionable In a Phase Ib trial, the combination of Tukysa (tucatinib) and Trastuzumab emtansine (T-DM1) demonstrated clinical activity in CNS metastases in patients with ERBB2 (HER2)-positive metastatic breast cancer, with 12.5% (1/8) evaluable patients achieving CNS complete response, 25% (2/8) partial CNS response, and 62.5% (5/8) CNS stable disease (San Antonio Breast Cancer Symposium 2015, Abstract P4-14-19). detail...
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Ado-trastuzumab emtansine + Tucatinib Phase Ib/II Actionable In a Phase Ib clinical trial, treatment with the combination of Tucatinib (ARRY-380) and Trastuzumab emtansine (T-DM1) resulted in an overall response rate of 47% (15/52) and median progression-free survival of 6.5 months in patients with ERBB2 (HER2)-positive metastatic breast cancer, including patients with CNS metastasis (J Clin Oncol 34, 2016 (suppl; abstr 513)). detail...
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Ado-trastuzumab emtansine + Tucatinib Phase Ib/II Actionable In a Phase Ib clinical trial, treatment with the combination of Tukysa (tucatinib) and Trastuzumab emtansine (T-DM1) resulted in partial response in 33% (11/33) and stable disease in 48% (16/33) and a clinical benefit rate of 58% (19/33) in patients with ERBB2 (HER2)-positive metastatic breast cancer (San Antonio Breast Cancer Symposium 2015, Abstract P4-14-20). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive MM-302 Phase I Actionable In a Phase I study, MM-302 demonstrated safety in patients with ERBB2 (HER2) positive breast cancer (Cancer Res 2012;72(24 Suppl):Abstract nr P5-18-09) detail...
ERBB2 positive breast carcinoma sensitive Trastuzumab Duocarmazine Preclinical - Pdx & cell culture Actionable In a preclinical study, Trastuzumab Duocarmazine (SYD985) decreased survival of ERBB2 (HER2)-positive breast carcinoma cell lines in culture, and inhibited tumor growth and induced tumor remission in cell line and patient-derived xenograft models of ERBB2 (HER2)-positive breast carcinoma, including models with low ERBB2 (HER2) expression (PMID: 25589493). 25589493
ERBB2 positive Her2-receptor positive breast cancer sensitive Copanlisib Preclinical Actionable In a preclinical study, breast cancer cell lines with a PIK3CA activating mutation and/or ERBB2 (HER2)-over expression demonstrated increased sensitivity to inhibition of proliferation by Aliqopa (copanlisib) in culture, compared to ERBB2 (HER2)-negative and wild-type PIK3CA cell lines (PMID: 24170767). 24170767
ERBB2 positive gastroesophageal junction adenocarcinoma no benefit MM-111 + Paclitaxel + Trastuzumab Phase II Actionable In a Phase II trial, Taxol (paclitaxel) and Herceptin (trastuzumab) treatment in combination with MM-111 did not improve progression free survival (9.6 weeks) and median overall survival (32.1 weeks) compared to without MM-111 (23.3 weeks, 56.1 weeks) in ERBB2 positive gastroesophageal junction cancer patients (J Clin Oncol 34, 2016 (suppl; abstr 4043)). detail...
ERBB2 positive breast cancer sensitive ADCT-502 Preclinical - Pdx Actionable In a preclinical study, ADCT-502 demonstrated anti-tumor activity in ERBB2 (HER2)-expressing breast cancer cell line and patient-derived xenograft (PDX) models, including PDX models expressing low levels of ERBB2 (HER2) (Eur J Cancer, 2016, Vol. 69, Supp1, S28). detail...
ERBB2 positive gastroesophageal adenocarcinoma predicted - sensitive GBR1302 Case Reports/Case Series Actionable In a Phase I trial, GBR 1302 treatment resulted in prolonged (more than 4 months) stable disease in a patient with ERBB2 (HER2) positive (IHC 3+) gastroesophageal adenocarcinoma (Annals of Oncology, Volume 29, Issue suppl_8, October 2018, mdy288.020; NCT02829372). detail...
ERBB2 positive breast cancer sensitive MI130004 Preclinical - Cell line xenograft Actionable In a preclinical study, MI130004 inhibited proliferation of ERBB2 (HER2)-receptor positive breast cancer cells in culture, and led to decreased tumor volume and improved survival in cell line xenograft models (PMID: 29440297). 29440297
ERBB2 positive gastroesophageal junction adenocarcinoma no benefit Ado-trastuzumab emtansine Phase III Actionable In a Phase III trial (GATSBY), Kadcyla (trastuzumab emtansine) did not demonstrate efficacy benefit over Taxol (paclitaxel) in median overall survival (7.9 vs 8.6 months) in patients with previously treated ERBB2 (HER2)-positive locally advanced or metastatic gastric/gastroesophageal junction adenocarcinoma (PMID: 28343975; NCT01641939). detail... 28343975
ERBB2 positive colorectal cancer predicted - sensitive Trastuzumab deruxtecan Phase I Actionable In a Phase I trial, treatment with Enhertu (fam-trastuzumab deruxtecan-nxki) resulted in an objective response rate of 25% (3/12) and disease control rate of 83.3% (10/12) in evaluable patients with Erbbe (Her2)-expressing colorectal cancer (Annals of Oncology (2018) 29 (suppl_8): viii150-viii204; NCT02564900). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive CT-P6 Phase III Actionable In a Phase III trial, CT-P6 demonstrated equivalence to reference Herceptin (trastuzumab) in patients with ERBB2 (HER2)-positive breast cancer, with 46.8% (116/248) of patients treated with CT-P6 achieving pathologic complete response compared to 50.4% (129/256) with Herceptin (trastuzumab) treatment (PMID: 28592386). 28592386
ERBB2 positive pancreatic cancer sensitive Trastuzumab deruxtecan Preclinical - Cell line xenograft Actionable In a preclinical study, Enhertu (fam-trastuzumab deruxtecan-nxki) inhibited tumor growth in a pancreatic cancer cell line xenograft model with low ERBB2 (HER2) expression (PMID: 27026201). 27026201
ERBB2 positive gastroesophageal junction adenocarcinoma predicted - sensitive Afatinib + Trastuzumab Phase II Actionable In a Phase II clinical trial, the combination therapy of Gilotrif (afatinib) and Herceptin (trastuzumab) in ERBB2 (HER2)-positive patients with either gastroesophageal junction adenocarcinoma, metastatic esophageal cancer, or gastric adenocarcinoma resulted in a partial response in 8% (1/12) and disease control for 4 months or more in 17% (2/12) (PMID: 30463996; NCT01522768). 30463996
ERBB2 positive Her2-receptor positive breast cancer sensitive Neratinib Phase II Actionable In a Phase II clinical trial, Nerlynx (neratinib) demonstrated safety and efficacy as a monotherapy in patients with ERBB2 (HER2)-positive breast cancer (PMID: 23953056). 23953056
ERBB2 positive uterine corpus serous adenocarcinoma sensitive Trastuzumab Duocarmazine Preclinical - Cell line xenograft Actionable In a preclinical study, Trastuzumab Duocarmazine (SYD895) induced cell death in ERBB2 (HER2)-expressing primary uterine serous carcinoma (USC) cell lines in culture, including cell lines with both high and low levels of ERBB2 (HER2) expression, and inhibited tumor growth and improved survival in ERBB2 (HER2)-expressing USC primary cell line xenografts (PMID: 27256376). 27256376
ERBB2 positive stomach carcinoma sensitive Tucatinib Preclinical - Cell culture Actionable In a preclinical study, Tukysa (tucatinib) inhibited tumor growth in a ERBB2 (HER2)-positive gastric carcinoma cell line xenograft model (Cancer Res April 15, 2012 72:852). detail...
ERBB2 positive stomach cancer sensitive MI130004 Preclinical - Cell line xenograft Actionable In a preclinical study, MI130004 inhibited proliferation of ERBB2 (HER2)-positive gastric cancer cells in culture, and led to decreased tumor volume and improved survival in cell line xenograft models (PMID: 29440297). 29440297
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive ZW25 Phase I Actionable In a Phase I trial, ZW25 treatment resulted in partial response in 28.6% (2/7) and stable disease in 28.6% (2/7) of patients with ERBB2 (HER2)-positive breast cancers (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 255P; NCT02892123). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive CDX-3379 Preclinical Actionable In a preclinical study, CDX-3379 (KTN3379) inhibited tumor growth in xenograft models of ERBB2 (HER2)-positive breast cancer (PMID: 26880266). 26880266
ERBB2 positive Her2-receptor positive breast cancer predicted - sensitive Ibrutinib Preclinical - Cell line xenograft Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited Her family receptor signaling, resulted in apoptosis and growth inhibition in ERBB2 (HER2)-positive breast cancer cell lines in culture and in cell line xenograft models (PMID: 27256378). 27256378
ERBB2 positive Her2-receptor positive breast cancer sensitive Buparlisib + Trastuzumab Phase I Actionable In a Phase I clinical trial, the combination of Buparlisib (BKM120) and Herceptin (trastuzumab) was well tolerated in patients with ERBB2 (HER2)-positive advanced or metastatic breast cancer that had progressed on Herceptin (trastuzumab) (PMID: 24470511). 24470511
ERBB2 positive Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine + Docetaxel Phase Ib/II Actionable In a Phase Ib/II trial, Kadcyla (trastuzumab emtansine) and Taxotere (docetaxel) combination treatment resulted in median progression-free survival of 13.8 months and objective response in 80.0% (20/25) of patients with ERBB2 (HER2)-positive metastatic breast cancer (PMID: 27052654). 27052654
ERBB2 positive sarcoma predicted - sensitive HER2 CAR-T cells Phase Ib/II Actionable In a Phase I/II trial, treatment with ERBB2 (HER2)-specific CAR-T cells resulted in stable disease for 12 weeks to 14 months in 4/17 evaluable patients with ERBB2 (HER2)-positive sarcomas and a median overall survival of 10.3 months (PMID: 25800760; NCT00902044). 25800760
ERBB2 positive Her2-receptor positive breast cancer sensitive Capecitabine + Neratinib Phase II Actionable In a Phase II trial, Nerlynx (neratinib) and Xeloda (capecitabine) combination therapy resulted in an overall 12-month survival rate of 63% (23/37) in patients with Erbb2 (Her2)-positive breast cancer brain metastases (J Clin Oncol 35, 2017 (suppl; abstr 1005)). detail... detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Carboplatin + Docetaxel + Trastuzumab Guideline Actionable Taxotere (docetaxel), Paraplatin (carboplatin), and Herceptin (trastuzumab) therapy is included in the guidelines as adjuvant therapy for patients with hormone receptor-negative (ER and PR), ERBB2 (HER2)-positive breast cancer (NCCN.org). detail...
ERBB2 positive Her2-receptor positive breast cancer sensitive Ado-trastuzumab emtansine + Docetaxel + Pertuzumab Phase Ib/II Actionable In a Phase Ib/II trial, Kadcyla (trastuzumab emtan