Definition

An orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, ICP-105 specifically targets, binds to and blocks the binding of the ligand FGF19 to FGFR4. This prevents the activation of FGFR4, inhibits FGFR4-mediated signaling and leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4, a receptor tyrosine kinase overexpressed on a variety of cancer cell types, is involved in tumor cell proliferation, differentiation, angiogenesis, and survival. FGF19 is overexpressed by certain tumor cell types.