crizotinib + gefitinib

Crizotinib + gefitinib is a combination of two small molecule tyrosine kinase inhibitors used in the treatment of non-small cell lung cancer (NSCLC), particularly in cases with acquired resistance to EGFR tyrosine kinase inhibitors due to MET amplification. Crizotinib targets and inhibits multiple kinases, including anaplastic lymphoma kinase (ALK), hepatocyte growth factor receptor (HGFR/c-MET), ROS1, and Recepteur d'Origine Nantais (RON). Gefitinib selectively inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase by binding to its ATP-binding site, thereby blocking downstream signaling pathways involved in cell proliferation and survival. The combination is primarily investigated for overcoming resistance mechanisms—specifically HGF/MET-driven resistance—in EGFR-mutant NSCLC patients who have progressed on prior EGFR-TKI monotherapy[1][3][6]. Preclinical and clinical data suggest that this dual inhibition can induce apoptosis, inhibit tumor growth, and delay or prevent the emergence of drug-resistant cancer cells[6].

Other names

crizotinib + gefitinib