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Drug intelligence / Profile preview
neratinib + trastuzumab
- Development stage
- Phase 3
- Lead developer
- Puma Biotechnology
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Neratinib + trastuzumab is a combination therapy targeting HER2-positive breast cancer. Neratinib is an irreversible pan-HER tyrosine kinase inhibitor that binds to cysteine residues in the ATP pocket of EGFR, HER2, and HER4, preventing autophosphorylation and downstream signaling. Trastuzumab is a humanized monoclonal antibody that binds to the extracellular domain IV of HER2. The combination prevents reactivation of HER3 and Akt phosphorylation that can occur with neratinib monotherapy, providing more complete HER2 pathway inhibition. Clinical studies have shown encouraging antitumor activity in patients with advanced HER2-positive breast cancer who have previously been treated with trastuzumab-based regimens.
- Brand names
- Nerlynx + Herceptin
- Other names
- SAFIR-ABC10 trastuzumab combinationSAFIR-ABC-10 trastuzumab combinationSAFIR-ABC 10 trastuzumab combination
02
Targets
EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)
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