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 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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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Neratinib | Nerlynx | HKI-272|PB272 | HER2 Inhibitor 41 | 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 |
|---|---|---|---|---|---|---|---|
| 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 |
| 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 |
| ERBB3 mutant | Advanced Solid Tumor | 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 12.5% (2/16), and a median progression-free survival of 1.7 months in patients with advanced solid tumors harboring ERBB3 (HER3) mutations (PMID: 29420467; NCT01953926). | 29420467 |
| ERBB4 G936R | Advanced Solid Tumor | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB4 G936R demonstrated sensitivity to Nerlynx (neratinib) similar to wild-type Erbb4 in culture, resulting in decreased cell viability (PMID: 33323455). | 33323455 |
| PIK3CA H1047R | breast cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of breast cancer organoids harboring PIK3CA H1047R in culture (PMID: 37272756). | 37272756 |
| 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 |
| ERBB3 D297H | head and neck squamous cell carcinoma | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) treatment inhibited viability of a hypopharyngeal squamous cell carcinoma cell line harboring ERBB3 (HER3) D297H in culture (PMID: 33473169). | 33473169 |
| 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 |
| ERBB4 R687K | Advanced Solid Tumor | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of a transformed cell line expressing ERBB4 R687K in culture (PMID: 36860695). | 36860695 |
| ERBB3 V104M | colon cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) treatment inhibited Erbb2 (Her2) phosphorylation and downstream signaling, and inhibited viability and proliferation in a colon cancer cell line harboring ERBB3 (HER3) V104M in culture (PMID: 38751013). | 38751013 |
| ERBB3 M91I | bladder carcinoma | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) treatment inhibited viability of a bladder carcinoma cell line harboring ERBB3 (HER3) M91I in culture (PMID: 33473169). | 33473169 |
| 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 |
| ERBB4 E715K | Advanced Solid Tumor | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of a transformed cell line expressing ERBB4 E715K in culture (PMID: 36860695). | 36860695 |
| ERBB3 E332K | extrahepatic bile duct carcinoma | predicted - sensitive | Neratinib | Case Reports/Case Series | Actionable | In a clinical case study, erlynx (neratinib) treatment resulted in improvement in performance status lasting 4 months in a patient with extrahepatic cholangiocarcinoma harboring ERBB3 E332K (PMID: 33279901). | 33279901 |
| 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 |
| ERBB4 G741R | Advanced Solid Tumor | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) inhibited growth of a transformed cell line expressing ERBB4 G741R in culture (PMID: 36860695). | 36860695 |
| BRAF V600E CBL dec exp | high grade glioma | predicted - resistant | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, glioma cell lines harboring BRAF V600E and siRNA mediated knockdown of CBL were resistant to treatment with Nerlynx (neratinib) in culture (PMID: 34433654). | 34433654 |
| ERBB3 V104M | lung cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) treatment inhibited Erbb2 (Her2) phosphorylation and downstream signaling, and inhibited viability and colony formation in a lung cancer cell line harboring ERBB3 (HER3) V104M in culture (PMID: 38751013). | 38751013 |
| 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 |
| ERBB3 V104M | urinary bladder cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) treatment inhibited Erbb2 (Her2) phosphorylation and downstream signaling, and inhibited viability and proliferation in a bladder cancer cell line harboring ERBB3 (HER3) V104M in culture (PMID: 38751013). | 38751013 |
| ERBB3 V104L | Her2-receptor positive breast cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Nerlynx (neratinib) treatment inhibited activation of Erbb2 (Her2) and decreased viability and proliferation in an ERBB2 (HER2)-positive breast cancer cell line expressing ERBB3 (HER3) V104L in culture (PMID: 38751013). | 38751013 |
| ERBB4 A17V | hematologic cancer | sensitive | Neratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB4 A17V demonstrated sensitivity to Nerlynx (neratinib) similar to wild-type Erbb4 in culture, resulting in decreased cell viability (PMID: 33323455). | 33323455 |
| 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 |
| ERBB3 act mut | Advanced Solid Tumor | sensitive | Neratinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing ERBB3 (HER3) activating mutations demonstrated sensitivity to Nerlynx (neratinib), resulting in inhibition of Erbb3 (Her3) phosphorylation, downstream signaling, and cell growth (Cancer Res October 1, 2014 74; 3419). | detail... |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT05564377 | Phase II | Selumetinib Binimetinib + Fulvestrant Binimetinib + Palbociclib Nilotinib + Paclitaxel Binimetinib + Fluorouracil + Leucovorin + Oxaliplatin Panitumumab + Sotorasib Binimetinib Fulvestrant Olaparib Olaparib + Selumetinib Alpelisib + Olaparib Neratinib Neratinib + Palbociclib Fluorouracil + Leucovorin + Oxaliplatin Ipatasertib + Paclitaxel | Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial | Recruiting | USA | 1 |
| NCT04781374 | Phase II | Neratinib | Neratinib in Patients With Metastatic Castration-Resistant Prostate Cancer | Withdrawn | USA | 0 |
| 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) | Active, not recruiting | USA | 0 |
| NCT01494662 | Phase II | Capecitabine + Neratinib Neratinib | HKI-272 for HER2-Positive Breast Cancer and Brain Metastases | Active, not recruiting | USA | 0 |
| NCT03289039 | Phase II | Neratinib Fulvestrant + Neratinib | Neratinib +/- Fulvestrant in HER2+, ER+ Metastatic Breast Cancer | Terminated | USA | 0 |
| NCT05388149 | Phase II | Neratinib | Kadcyla And Neratinib for Interception of HER2+ Breast Cancer With Molecular Residual Disease | Recruiting | CAN | 0 |
| NCT01670877 | Phase II | Neratinib Neratinib + Trastuzumab Fulvestrant + Neratinib + Trastuzumab Fulvestrant + Neratinib | Neratinib +/- Fulvestrant in Metastatic HER2 Non-amplified But HER2 Mutant Breast Cancer | Completed | USA | CAN | 0 |
| NCT06126276 | Phase II | Neratinib Neratinib + Palbociclib | Testing the Use of Neratinib or the Combination of Neratinib and Palbociclib Targeted Treatment for HER2+ Solid Tumors (A ComboMATCH Treatment Trial) | Recruiting | USA | 0 |
| NCT04886531 | Phase II | Anastrozole + Neratinib + Trastuzumab Letrozole + Neratinib + Trastuzumab Neratinib Anastrozole + Neratinib Letrozole + Neratinib Letrozole Anastrozole Anastrozole + Trastuzumab | Trial of Pre-operative Neratinib and Endocrine Therapy With Trastuzumab in ER-Positive, HER-2 Positive Breast Cancers | Recruiting | USA | 0 |
| NCT03094052 | Phase II | Neratinib Loperamide Crofelemer Neratinib + Trastuzumab | Incidence and Severity of Diarrhea in Patients With Stage II-IIIC HER2 Positive Breast Cancer Treated With Trastuzumab and Neratinib | Completed | USA | 0 |
| 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 | Active, not recruiting | USA | CAN | 0 |
| NCT05919108 | Phase II | Neratinib | Neoadjuvant Neratinib in Stage I-III HER2-Mutated Lobular Breast Cancers | Recruiting | USA | 0 |
| NCT02673398 | Phase II | Neratinib | Neratinib in Treating Older Patients With Stage IV HER2-Positive Breast Cancer | Completed | USA | 0 |
| NCT01953926 | Phase II | Neratinib + Trastuzumab Fulvestrant + Neratinib + Trastuzumab Neratinib Neratinib + Paclitaxel | Basket Study of Neratinib in Participants With Solid Tumors Harboring Somatic HER2 or EGFR Exon 18 Mutations | Terminated | USA | ITA | GBR | FRA | ESP | CAN | BEL | AUS | 5 |
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