The aberrant signaling of fibroblast growth factor 19 (FGF19) through the fibroblast growth factor receptor 4 (FGFR4) in combination with the co-receptor β–klotho (KLB) has been shown to be essential for the initiation and maintenance of a subset of hepatocellular carcinomas (HCC). This presentation will describe the discovery of FGF401 as a highly potent and selective, first-in-class, reversible-covalent inhibitor of the kinase activity of the FGFR4. FGF401 exhibits: a good oral pharmacokinetic profile; high in vivo potency, leading to activity in preclinical FGF19/FGFR4 dependent xenograft models; and a favorable safety profile. A PhI/II study with FGF401 is currently ongoing in patients with solid tumors positive for FGFR4 and KLB.<br/>

FGF401: A reversible-covalent inhibitor of FGFR4 for the treatment of hepatocellular carcinoma

253rd National Meeting (2017)

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