FGFR2/3 inhibitor CGT4859

An orally bioavailable reversible inhibitor of fibroblast growth factor receptor (FGFR) types 2 and 3 (FGFR2/3), with potential antineoplastic activity. Upon oral administration, FGFR2/3 inhibitor CGT4859 targets, reversibly binds to and inhibits FGFR2/3, and is specifically active against FGFR2 molecular brake and gatekeeper resistance mutations. This blocks FGFR2/3-mediated signaling and leads to an inhibition of tumor cell proliferation in FGFR2/3-overexpressing 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.