Therapy Detail
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| Therapy Name | Neratinib |
| Synonyms | |
| Therapy Description |
Nerlynx (neratinib) inhibits the ERBB2 (HER2) receptor as well as EGFR, resulting in decreased proliferation of HER2 and EGFR expressing tumor cells (PMID: 15173008). Nerlynx (neratinib) is FDA approved for breast cancer patients with ERBB2 (HER2) overexpression and/or amplification (FDA.gov). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Neratinib | Nerlynx | HKI-272|PB272 | HER2 Inhibitor 23 | Nerlynx (neratinib) inhibits the ERBB2 (HER2) receptor as well as EGFR, resulting in decreased proliferation of HER2 and EGFR expressing tumor cells (PMID: 15173008). Nerlynx (neratinib) is FDA approved for use in patients with early stage ERBB2 (HER2)-positive breast cancer following Herceptin (trastuzumab)-based therapy, and in combination with Xeloda (capecitabine) in patients with advanced/metastatic ERBB2 (HER2)-positive breast cancer who have received two or more anti-ERBB2 (HER2) regimens (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 R678Q | 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) R678Q demonstrated stable disease when treated with Nerlynx (neratinib) (PMID: 32723675; NCT01953926). | 32723675 |
| 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 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 L841V | 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 2.8 months in a patient with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) L841V (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 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 mut PIK3CA mut | breast cancer | predicted - resistant | Neratinib | Case Reports/Case Series | Actionable | In a Phase II trial (SUMMIT), 6 of 7 patients with ERBB2 (HER2)-mutant breast cancer who progressed on Nerlynx (neratinib) harbored either a PIK3CA (n=5) or PIK3R1 (n=1) mutation (PMID: 31978326). | 31978326 |
| ERBB2 mutant | Her2-receptor positive breast cancer | sensitive | Neratinib | Phase II | Actionable | In a Phase II trial, Nerlynx (neratinib) treatment resulted in complete response in 12.5% (3/24) and partial response in 20.8% (5/24) of ERBB2 (HER2) mutant but not amplified breast cancer patients (Cancer Res 2017;77(4 Suppl):Abstract nr PD2-08). | detail... |
| ERBB2 pos PIK3CA E542K | Her2-receptor positive breast cancer | predicted - sensitive | Neratinib | Phase III | Actionable | In a Phase III trial (ExteNET), Nerlynx (neratinib) treatment resulted in improved 5-year invasive disease-free survival (92.4% vs 84.5%, HR=0.41, p=0.028) and clinical benefit (HR=0.40, p=0.041) compared to placebo in patients with ERBB2 (HER2)-positive early breast cancer who completed trastuzumab-based adjuvant therapy, and harbored PIK3CA amplification (n=61) or mutations (n=210), including H1047R (n=110), E542K (n=18), and E545K/D (n=82) (PMID: 30867034; NCT00878709). | 30867034 |
| ERBB2 D769Y | 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 1.4 months in a patient with bladder cancer harboring both ERBB2 (HER2) D769Y (PMID: 29420467; NCT01953926). | 29420467 |
| 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 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 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 mutant | lung cancer | sensitive | Neratinib | Phase I | Actionable | In a Phase I clinical trial, Nerlynx (neratinib) administered with Torisel (temsirolimus) was tolerable and demonstrated antitumor activity in ERBB2 (HER2)-mutant non-small-cell lung cancer (PMID: 24323026). | 24323026 |
| 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 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 L866M | colorectal cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of colorectal cancer cells over expressing ERBB2 (HER2) L866M in culture (PMID: 26243863). | 26243863 |
| ERBB2 V842I | 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 1.8 months in a patient with endometrial cancer harboring ERBB2 (HER2) V842I (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 mutant | Her2-receptor negative breast cancer | sensitive | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in an object response rate of 24% (6/25), a clinical benefit rate of 40% (10/25), and a median progression-free survival of 3.5 months in patients with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) mutations (PMID: 29420467; NCT01953926). | 29420467 |
| 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 P489L | cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of transformed cells expressing ERBB2 (HER2) P489L in culture (PMID: 32366937). | 32366937 |
| 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 V842I | colorectal cancer | conflicting | 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 1 patient with colorectal cancer harboring ERBB2 (HER2) V842I (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 V842I | colorectal cancer | conflicting | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of colorectal cancer cell lines over expressing ERBB2 (HER2) V842I in culture (PMID: 26243863). | 26243863 |
| ERBB2 G292R | 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) G292R (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 | 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 L755_E757delinsS | 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 9.0 months in a patient with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) L755_E757delinsS (PMID: 29420467; NCT01953926). | 29420467 |
| 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 V777L PIK3CA H1047R | breast cancer | resistant | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line harboring ERBB2 (HER2) V777L and PIK3CA H1047R demonstrated resistance to Nerlynx (neratinib) in culture (PMID: 31978326). | 31978326 |
| 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 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 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 |
| BRAF G596R PIK3CA E545K | colorectal cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of colorectal cancer cells harboring both BRAF G596R and PIK3CA E545K in culture (PMID: 26243863). | 26243863 |
| 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... |
| PIK3CA H1047R | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
| 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 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 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 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 V777L | 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 6.9 months in a patient with endometrial cancer harboring ERBB2 (HER2) V777L (PMID: 29420467; NCT01953926). | 29420467 |
| 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 mutant | urinary bladder cancer | no benefit | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in no objective response, a clinical benefit rate of 18.8% (3/16), and a median progression-free survival of 1.8 months in patients with bladder cancer harboring ERBB2 (HER2) mutations (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 mutant | gastroesophageal junction adenocarcinoma | no benefit | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in no objective response, a clinical benefit rate of 20% (1/5), and a median progression-free survival of 1.7 months in patients with gastroesophageal cancer harboring ERBB2 (HER2) mutations (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 | 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 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 pos PIK3CA H1047R | Her2-receptor positive breast cancer | predicted - sensitive | Neratinib | Phase III | Actionable | In a Phase III trial (ExteNET), Nerlynx (neratinib) treatment resulted in improved 5-year invasive disease-free survival (92.4% vs 84.5%, HR=0.41, p=0.028) and clinical benefit (HR=0.40, p=0.041) compared to placebo in patients with ERBB2 (HER2)-positive early breast cancer who completed trastuzumab-based adjuvant therapy, and harbored PIK3CA amplification (n=61) or mutations (n=210), including H1047R (n=110), E542K (n=18), and E545K/D (n=82) (PMID: 30867034; NCT00878709). | 30867034 |
| 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 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 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 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 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 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 | 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 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 R678Q | 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 1.6 months in a patient with colorectal cancer harboring ERBB2 (HER2) R678Q (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 G660R | Advanced Solid Tumor | predicted - sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G660R demonstrated decreased cell proliferation and reduced survival when treated with Nerlynx (neratinib) in culture (PMID: 30449325). | 30449325 |
| ERBB2 L869R | 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 patient harboring ERBB2 (HER2) L869R achievd stable disease for 24 weeks or more (PMID: 28679771; NCT01670877). | 28679771 |
| ERBB2 L869R | breast cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited ERBB2 (HER2) phosphorylation and growth of transformed breast epithelial cells expressing ERBB2 (HER2) L869R in culture (PMID: 28274957). | 28274957 |
| ERBB2 R678Q | 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 5.5 months in a patient with endometrial cancer harboring ERBB2 (HER2) R678Q (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 mutant | cervical cancer | predicted - sensitive | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in an objective response rate of 20% (1/5), a clinical benefit rate of 60% (3/5), and a median progression-free survival of 20.1 months in patients with cervical cancer harboring ERBB2 (HER2) mutations (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 L866M | 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) L866M 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 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 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 R678Q | 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 1.7 months in a patient with gastroesophageal cancer harboring ERBB2 (HER2) R678Q (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 R678Q | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, transformed human breast cell lines expressing ERBB2 (HER2) R678Q demonstrated growth inhibition when treated with Nerlynx (neratinib) (PMID: 23220880). | 23220880 |
| 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 | 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 |
| PIK3CA E542K | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
| 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 |
| PIK3CA N345K | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
| 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 V777L | urinary bladder 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 6.9 months in a patients with bladder cancer harboring ERBB2 (HER2) V777L (PMID: 29420467; NCT01953926). | 29420467 |
| PIK3CA Q546K | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
| 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 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 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 |
| 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 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 |
| PIK3CA H1047L | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
| ERBB2 V842I | 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) V842I in culture (PMID: 26243863). | 26243863 |
| ERBB2 L755_T759del | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, breast cancer cells expressing ERBB2 (HER2) L755_T759del were sensitive to treatment with Nerlynx (neratinib) (PMID: 23220880). | 23220880 |
| ERBB2 mutant | breast cancer | predicted - sensitive | Neratinib | Phase II | Actionable | In a Phase II trial, Nerlynx (neratinib) demonstrated activity in metastatic breast cancer patients harboring ERBB2 (HER2) mutations, with treatment resulting in a clinical benefit rate of 31% (5/16; 1 complete response, 1 partial response, and 3 patients achieving stable disease for 24 weeks or more) and a median progression-free survival of 16 weeks (PMID: 28679771). | 28679771 |
| 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 V777L ERBB2 V842I | 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 1.8 months in a patient with colorectal cancer harboring ERBB2 (HER2) V777L and V842I (PMID: 29420467; NCT01953926). | 29420467 |
| 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 | 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 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 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 L663P | Advanced Solid Tumor | predicted - sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) L663P demonstrated decreased cell proliferation and reduced survival when treated with Nerlynx (neratinib) in culture (PMID: 30449325). | 30449325 |
| ERBB2 mutant | lung non-small cell carcinoma | sensitive | Neratinib | Phase I | Actionable | In a Phase I study, Nerlynx (neratinib) administered with temsirolimus was tolerable and demonstrated antitumor activity in ERBB2-mutant non-small-cell lung cancer (PMID: 24323026). | 24323026 |
| ERBB2 mutant | lung non-small cell carcinoma | sensitive | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in an objective response rate of 3.8% (1/26), a clinical benefit rate of 42.3% (11/26), and a median progression-free survival of 5.5 months in patients with non-small cell lung cancer harboring ERBB2 (HER2) mutations (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 |
| PIK3CA G1049R | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
| PIK3CA E545K | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
| ERBB2 L869R | 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 3.6 months in a patient with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) L869R (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 mutant | endometrial cancer | no benefit | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in no objective response, a clinical benefit rate of 28.6% (2/7), and a median progression-free survival of 2.6 months in patients with endometrial cancer harboring ERBB2 (HER2) mutations (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 V777L | 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 1.1 months in a patient with gastroesophageal cancer harboring ERBB2 (HER2) V777L (PMID: 29420467; NCT01953926). | 29420467 |
| 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 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 V777L | 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 1.4 months in a patient with colorectal cancer harboring ERBB2 (HER2) V777L (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 V777L | colorectal cancer | conflicting | Neratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of colorectal cancer cells over expressing ERBB2 (HER2) V777L in culture and suppressed tumor growth in cell line xenograft models (PMID: 26243863). | 26243863 |
| ERBB2 pos PIK3CA amp | Her2-receptor positive breast cancer | predicted - sensitive | Neratinib | Phase III | Actionable | In a Phase III trial (ExteNET), Nerlynx (neratinib) treatment resulted in improved 5-year invasive disease-free survival (92.4% vs 84.5%, HR=0.41, p=0.028) and clinical benefit (HR=0.40, p=0.041) compared to placebo in patients with ERBB2 (HER2)-positive early breast cancer who completed trastuzumab-based adjuvant therapy, and harbored PIK3CA amplification (n=61) or mutations (n=210), including H1047R (n=110), E542K (n=18), and E545K/D (n=82) (PMID: 30867034; NCT00878709). | 30867034 |
| ERBB2 L1157R | cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of transformed cells expressing ERBB2 (HER2) L1157R in culture (PMID: 32366937). | 32366937 |
| ERBB2 pos PIK3CA mut | Her2-receptor positive breast cancer | predicted - sensitive | Neratinib | Phase III | Actionable | In a Phase III trial (ExteNET), Nerlynx (neratinib) treatment resulted in improved 5-year invasive disease-free survival (92.4% vs 84.5%, HR=0.41, p=0.028) and clinical benefit (HR=0.40, p=0.041) compared to placebo in patients with ERBB2 (HER2)-positive early breast cancer who completed trastuzumab-based adjuvant therapy, and harbored PIK3CA amplification (n=61) or mutations (n=210), including H1047R (n=110), E542K (n=18), and E545K/D (n=82) (PMID: 30867034; NCT00878709). | 30867034 |
| ERBB2 G309A | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, transformed human breast cell lines expressing ERBB2 (HER2) G309A demonstrated growth inhibition when treated with Nerlynx (neratinib) (PMID: 23220880). | 23220880 |
| ERBB2 mutant | colorectal cancer | no benefit | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in no objective response, a clinical benefit rate of 8.3% (1/12), and a median progression-free survival of 1.8 months in patients with colorectal cancer harboring ERBB2 (HER2) mutations (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 L786V | 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 3.7 months in a patient with non-small cell lung cancer harboring ERBB2 (HER2) L786V (PMID: 29420467; NCT01953926). | 29420467 |
| 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 pos PIK3CA E545D | Her2-receptor positive breast cancer | predicted - sensitive | Neratinib | Phase III | Actionable | In a Phase III trial (ExteNET), Nerlynx (neratinib) treatment resulted in improved 5-year invasive disease-free survival (92.4% vs 84.5%, HR=0.41, p=0.028) and clinical benefit (HR=0.40, p=0.041) compared to placebo in patients with ERBB2 (HER2)-positive early breast cancer who completed trastuzumab-based adjuvant therapy, and harbored PIK3CA amplification (n=61) or mutations (n=210), including H1047R (n=110), E542K (n=18), and E545K/D (n=82) (PMID: 30867034; NCT00878709). | 30867034 |
| ERBB2 D769Y | 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 1.9 months in a patient with gastroesophageal cancer harboring ERBB2 (HER2) D769Y (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB2 L841V | 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 1.8 months in a patient with colorectal cancer harboring ERBB2 (HER2) L841V (PMID: 29420467; NCT01953926). | 29420467 |
| 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 G660D | Advanced Solid Tumor | predicted - sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G660D demonstrated decreased cell proliferation and reduced survival when treated with Nerlynx (neratinib) in culture (PMID: 30449325). | 30449325 |
| ERBB2 V777L | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, transformed human breast cell lines expressing ERBB2 (HER2) V777L demonstrated growth inhibition when treated with Nerlynx (neratinib) (PMID: 23220880). | 23220880 |
| 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 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 V777L | biliary tract cancer | conflicting | 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 3.6 months in one patient, and progressive disease with a progression-free survival of 0.8 months in another patient with biliary tract cancer harboring ERBB2 (HER2) V777L (PMID: 29420467; NCT01953926). | 29420467 |
| 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 G778A | 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) G778A (PMID: 29420467; NCT01953926). | 29420467 |
| 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 V777L | 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) V777L in culture (PMID: 26243863). | 26243863 |
| 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 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 mutant | biliary tract cancer | predicted - sensitive | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in an objective response rate at 8 weeks of 22.2% (2/9), a clinical benefit rate of 33.3% (3/9), and a median progression-free survival of 2.8 months in patients with biliary tract cancer harboring ERBB2 (HER2) mutations (PMID: 29420467; NCT01953926). | 29420467 |
| 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 | 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 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 R678Q | Advanced Solid Tumor | predicted - sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) R678Q demonstrated decreased cell proliferation and reduced survival when treated with Nerlynx (neratinib) in culture (PMID: 30449325). | 30449325 |
| ERBB2 D769N | cervical 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 cervical cancer harboring ERBB2 (HER2) D769N (PMID: 29420467; NCT01953926). | 29420467 |
| 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 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 | 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, Nerlynx (neratinib) inhibited growth of transformed cells expressing ERBB2 (HER2) G778_P780dup (also referred to as P780_Y781insGSP) in culture (PMID: 28363995). | 28363995 |
| 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 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 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 mutant | ovarian cancer | no benefit | Neratinib | Phase II | Actionable | In a Phase II trial (SUMMIT), Nerlynx (neratinib) treatment resulted in no objective response, no clinical benefit, and a median progression-free survival of 2.1 months in patients with ovarian cancer harboring ERBB2 (HER2) mutations (PMID: 29420467; NCT01953926). | 29420467 |
| 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 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 V842I | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, transformed human breast cell lines expressing ERBB2 (HER2) V842I demonstrated growth inhibition when treated with Nerlynx (neratinib) (PMID: 23220880). | 23220880 |
| 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 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 pos PIK3CA E545K | Her2-receptor positive breast cancer | predicted - sensitive | Neratinib | Phase III | Actionable | In a Phase III trial (ExteNET), Nerlynx (neratinib) treatment resulted in improved 5-year invasive disease-free survival (92.4% vs 84.5%, HR=0.41, p=0.028) and clinical benefit (HR=0.40, p=0.041) compared to placebo in patients with ERBB2 (HER2)-positive early breast cancer who completed trastuzumab-based adjuvant therapy, and harbored PIK3CA amplification (n=61) or mutations (n=210), including H1047R (n=110), E542K (n=18), and E545K/D (n=82) (PMID: 30867034; NCT00878709). | 30867034 |
| ERBB2 V777L | 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 in one patient, and progressive disease in 4 patient with Erbb2 (Her2) receptor negative (non-amplified) breast cancer harboring ERBB2 (HER2) V777L (PMID: 29420467; NCT01953926). | 29420467 |
| 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 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 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 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 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 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 D769Y | breast cancer | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, transformed human breast cell lines expressing ERBB2 (HER2) D769Y reverted to normal morphology in culture upon Nerlynx (neratinib) treatment (PMID: 23220880). | 23220880 |
| 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 | 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 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 | 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 | 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 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status |
|---|---|---|---|---|
| NCT03094052 | Phase II | Neratinib Loperamide Crofelemer Neratinib + Trastuzumab | Diarrhea Prophylaxis in Patients With HER2+ Breast Cancer Treated With Neratinib, With or Without Trastuzumab | Recruiting |
| NCT03289039 | Phase II | Neratinib Fulvestrant + Neratinib | Neratinib +/- Fulvestrant in HER2+, ER+ Metastatic Breast Cancer | Active, not recruiting |
| NCT01953926 | Phase II | Neratinib + Trastuzumab Fulvestrant + Neratinib + Trastuzumab Neratinib Neratinib + Paclitaxel | Neratinib HER Mutation Basket Study (SUMMIT) | Recruiting |
| NCT02932280 | Phase Ib/II | Neratinib | Safety and Dose Finding Study of Neratinib in Children and Young Adults With Cancer That Has Returned or Not Responded to Treatment | Recruiting |
| NCT03812393 | Phase II | Carboplatin + Neratinib + Paclitaxel Neratinib | Evaluating the Efficacy of Neratinib on Live Cell HER2 Signaling Transduction Analysis Positive Triple Negative Breast (FACT-2) | Recruiting |
| NCT01670877 | Phase II | Neratinib Neratinib + Trastuzumab Fulvestrant + Neratinib + Trastuzumab Fulvestrant + Neratinib | Neratinib +/- Fulvestrant in Metastatic HER2 Non-amplified But HER2 Mutant Breast Cancer | Recruiting |
| NCT01494662 | Phase II | Capecitabine + Neratinib Neratinib | HKI-272 for HER2-Positive Breast Cancer and Brain Metastases | Recruiting |
| NCT02673398 | Phase II | Neratinib | Neratinib in Treating Older Patients With Stage IV HER2-Positive Breast Cancer | Active, not recruiting |
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