LY2801653 + cetuximab

LY2801653 + cetuximab is a combination therapy composed of **merestinib** (LY2801653), an investigational orally bioavailable small molecule multi-kinase inhibitor targeting receptor tyrosine kinases (notably MET, MST1R, FLT3, AXL, MERTK, TEK, ROS1, NTRK1/2/3, DDR1/2), and **cetuximab**, a well-established monoclonal antibody targeting the epidermal growth factor receptor (EGFR). Merestinib disrupts oncogenic signaling by competitively inhibiting the ATP binding site of MET and other kinases involved in tumorigenesis, cell proliferation, motility, invasion, and angiogenesis[1][2][3][4]. Cetuximab binds EGFR, preventing activation by endogenous ligands, resulting in inhibition of cell growth and induction of apoptosis in EGFR-expressing tumors. The combination is under investigation to enhance anti-tumor efficacy via dual blockade of MET-driven and EGFR-driven oncogenic pathways, particularly in cancers demonstrating resistance to single-agent therapies or exhibiting co-activation of MET and EGFR signaling.

Brand names

merestinib

Other names

merestinib + cetuximab