The 2010 Meeting of the American Society of Clinical Oncology

Discovery of a Novel Mode of Protein Kinase Inhibition Characterized by the Mechanism of Inhibition of Human Mesenchymal-epithelial Transition Factor (c-Met) Protein Autophosphorylation by ARQ 197

“…ARQ 197 inhibits c-Met activation across a range of human tumor cell lines and shows anti-tumor activity in several human tumor xenografts (7). In clinical studies to date, ARQ 197 has been well tolerated and has yielded encouraging clinical responses including prolonged stable disease across a range of human tumors either alone or in combination with other agents (9,10). In a subset of patients with non-small cell lung cancer, met gene amplification is associated with both de novo and acquired resistance to pharmacologic EGFR inhibition (11).…”