cetuximab + gefitinib

Cetuximab + gefitinib is an experimental combination therapy that targets the epidermal growth factor receptor (EGFR) pathway in cancer. Cetuximab is a chimeric monoclonal antibody that binds to the extracellular domain of EGFR, blocking ligand binding and receptor activation, leading to inhibition of downstream signaling pathways involved in cell proliferation, survival, angiogenesis, and metastasis. Gefitinib is a small molecule tyrosine kinase inhibitor that blocks the intracellular ATP-binding site of EGFR, preventing autophosphorylation and subsequent activation of downstream signaling cascades. The combination exploits complementary mechanisms—cetuximab inhibits ligand-induced activation at the cell surface while gefitinib blocks intracellular kinase activity—resulting in synergistic inhibition of tumor growth and enhanced induction of apoptosis compared to either agent alone. This dual blockade has shown superior antitumor effects in preclinical models and has been explored for overcoming resistance to single-agent EGFR inhibitors[6][7][9].

Other names

cetuximab + gefitinib