gefitinib + tepotinib

Gefitinib + tepotinib is a combination of two small molecule tyrosine kinase inhibitors used in the treatment of advanced or metastatic non–small cell lung cancer (NSCLC) with EGFR mutations and acquired resistance to first- or second-generation EGFR inhibitors, particularly in patients with MET gene amplification or overexpression. Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, while tepotinib is a selective MET inhibitor. The combination targets both the EGFR and MET pathways to overcome resistance mechanisms that arise after initial EGFR TKI therapy. Clinical trials have shown that this combination improves progression-free survival and overall survival compared to chemotherapy in patients with MET-amplified, EGFR-mutant NSCLC who have progressed on prior EGFR TKI therapy[1][2][3][4][7].