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NERATINIB
Neratinib irreversibly binds to EGFR, HER2, and HER4, reducing their autophosphorylation and downstream signaling, leading to antitumor activity.
At a glance
| Generic name | NERATINIB |
|---|---|
| Target | EGFR, HER2, HER4 |
| Modality | Small molecule |
| Phase | FDA-approved |
| First approval | 2017 |
Mechanism of action
Neratinib works by binding to specific receptors on cancer cells, namely EGFR, HER2, and HER4. This binding prevents these receptors from working properly, which stops the cancer cells from growing and spreading. It also inhibits key signaling pathways that are important for the survival and proliferation of cancer cells.
Approved indications
Common side effects
- Diarrhea
- Nausea
- Abdominal pain
- Vomiting
- Stomatitis
- Dyspepsia
- Abdominal distension
- Dry mouth
- Fatigue
- Alanine aminotransferase increased
- Aspartate aminotransferase increased
- Urinary tract infection
Drug interactions
- proton pump inhibitors
- H2-receptor antagonists
- antacids
- strong CYP3A4 inhibitors
- P-gp and moderate CYP3A4 dual inhibitors
- strong or moderate CYP3A4 inducers
- certain P-gp substrates
Key clinical trials
- Testing the Use of Neratinib or the Combination of Neratinib and Palbociclib Targeted Treatment for HER2+ Solid Tumors (A ComboMATCH Treatment Trial) (PHASE2)
- Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial (PHASE2)
- Testing the Safety and Tolerability of the Anti-cancer Drugs Trastuzumab Deruxtecan and Neratinib for Cancers With Changes in the HER2 Gene (PHASE1)
- I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer (PHASE2)
- Trial of Pre-operative Neratinib and Endocrine Therapy With Trastuzumab in ER-Positive, HER-2 Positive Breast Cancers (PHASE2)
- Neratinib and Paclitaxel With or Without Pertuzumab and Trastuzumab Before Combination Chemotherapy in Treating Patients With Metastatic or Locally Advanced Breast Cancer (PHASE1, PHASE2)
- Neratinib In Combination With Chemotherapy/Trastuzumab/Pembrolizumab In HER2 Gastroesophageal Cancer (PHASE2)
- Pilot Study of [68Ga]Ga-ABY-025 Imaging in Patients Undergoing Treatment With HER2-targeted Therapy (EARLY_PHASE1)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- NERATINIB CI brief — competitive landscape report
- NERATINIB updates RSS · CI watch RSS