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gefitinib + ramucirumab
- Development stage
- Phase 3
- Lead developer
- Eli Lilly
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A combination therapy consisting of gefitinib, an EGFR tyrosine kinase inhibitor, and ramucirumab, a human monoclonal antibody targeting VEGFR2. This combination works by simultaneously inhibiting EGFR signaling and angiogenesis. Gefitinib blocks the ATP-binding site of EGFR tyrosine kinase, preventing downstream signaling cascades that promote cancer cell proliferation. Ramucirumab binds to VEGFR2, preventing VEGF ligands from binding and inhibiting angiogenesis necessary for tumor growth. This combination has been studied in the RELAY+ trial for first-line treatment of EGFR-mutated metastatic non-small cell lung cancer (NSCLC) in East Asian patients.
02
Targets
EGFR (Epidermal growth factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)
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