Neratinib is a protein kinase inhibitor used to treat breast cancer that over expresses the HER2 receptor. Neratinib was approved in July 2017 for use as an extended adjuvant therapy in Human Epidermal Growth Factor Receptor 2 (HER2) positive breast cancer.
- Mechanism
- Curator reviewed
Neratinib binds to and irreversibly inhibits EGFR, HER2, and HER4. This prevents auotphoshorylation of tyrosine residues on the receptor and reduces oncogenic signalling through the mitogen-activated protein kinase and Akt pathways.
- Primary indication
- For use as an extended adjuvant treatment in adult patients with early stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab-based therapy.Curator reviewed · 1 structured indication
- Formula / weight
- C30H29ClN6O3 · 557.05 g/mol (avg)
- First approval
- Canada, 2019 · United States, 2017 · European Union, 2020
- Code names
- HKI-272 · PB-272
- Brand names
Resolves to
Clinical / RWD
Structure
InChIKey
JWNPDZNEKVCWMY-VQHVLOKHSA-NSMILESCCOC1=C(NC(=O)\C=C\CN(C)C)C=C2C(NC3=CC=C(OCC4=CC=CC=N4)C(Cl)=C3)=C(C=NC2=C1)C#NTransporters
What you can answer from here — as of September 23, 2026
4Protein targetsEach mapped to UniProt, with action and pharmacological actionListed above
1TransporterSubstrate / inhibitor direction, not just membershipListed above
Which drugs share a target with Neratinib, and which of those have an active Phase 3 trial?
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