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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 43 | 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 |
|---|---|---|---|---|---|---|---|
| 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 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 |
| 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 |
| 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 |
| 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 |
| 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 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 |
| 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT05919108 | Phase II | Neratinib | Neoadjuvant Neratinib in Stage I-III HER2-Mutated Lobular Breast Cancers | Recruiting | 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 | ISR | IRL | GBR | FRA | ESP | DNK | CAN | BEL | AUS | 2 |
| 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 |
| NCT01494662 | Phase II | Capecitabine + Neratinib Neratinib | HKI-272 for HER2-Positive Breast Cancer and Brain Metastases | Active, not recruiting | 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 |
| 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 |
| 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 |
| 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 |
| NCT06813079 | Phase II | Abemaciclib Ceritinib Selinexor Doxorubicin Etoposide Brigatinib Ponatinib Neratinib Cobimetinib | Using Tumor Models to Determine Treatments | Not yet recruiting | CAN | 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 |
| NCT04781374 | Phase II | Neratinib | Neratinib in Patients With Metastatic Castration-Resistant Prostate Cancer | Withdrawn | USA | 0 |
| NCT02673398 | Phase II | Neratinib | Neratinib in Treating Older Patients With Stage IV HER2-Positive Breast Cancer | Completed | USA | 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 |
| 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 |
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