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 36 | 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 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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... |
| 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 |
| 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 |
| 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 |
| 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 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 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 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| 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 | Active, not recruiting | USA | ITA | FRA | ESP | CAN | BEL | 7 |
| 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 |
| 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 | Active, not recruiting | USA | 0 |
| NCT04781374 | Phase II | Neratinib | Neratinib in Patients With Metastatic Castration-Resistant Prostate Cancer | Terminated | 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) | Recruiting | 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 | Recruiting | USA | CAN | 0 |
| NCT02673398 | Phase II | Neratinib | Neratinib in Treating Older Patients With Stage IV HER2-Positive Breast Cancer | Active, not 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 | Active, not recruiting | USA | 0 |
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