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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