roblitinib

Roblitinib is a highly selective, oral, reversible-covalent small molecule inhibitor of fibroblast growth factor receptor 4 (FGFR4), developed as an antineoplastic agent. It targets the FGFR4/β-klotho signaling axis, which is implicated in the growth and survival of certain cancers—particularly hepatocellular carcinoma (HCC) with aberrant FGFR4 or KLB expression. By binding to a unique cysteine residue in the ATP-binding site of FGFR4, roblitinib inhibits its kinase activity and downstream signaling pathways involved in tumor cell proliferation, differentiation, angiogenesis, and survival. Roblitinib has reached phase I/II clinical trials for liver cancer and solid tumors[1][3][4][5][6][7].

Other names

roblitinib