Definition

An orally bioavailable, small molecule pan-inhibitor of fibroblast growth factor receptor (FGFR) family proteins, with potential antineoplastic activity. Upon oral administration, pan-FGFR inhibitor ABSK-121 binds to and inhibits FGFR family proteins, including FGFR2 and FGFR3 gatekeeper, molecular brake, and activation loop mutations. This prevents FGFR-mediated signaling, and inhibits both tumor angiogenesis and proliferation of FGFR-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases upregulated in many tumor cell types, plays a key role in cellular proliferation, cell survival and angiogenesis.