FGFR4 inhibitor BLU-554

An orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, BLU-554 specifically 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 is a receptor tyrosine kinase and is involved in tumor cell proliferation, differentiation, angiogenesis, and survival. FGF19 is overexpressed by certain tumor cell types. Check for active clinical trials using this agent. (NCI Thesaurus)

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