Futibatinib

Futibatinib, also known as TAS-120 is an orally bioavailable, highly selective, and irreversible FGFR1-4 inhibitor, currently being used in the treatment of intrahepatic cholangiocarcinoma, a bile duct cancer in the liver. Fibroblast growth factor 21 (FGF-21) is a member of the FGF family that lacks the heparin-binding ability and can be released into circulation to act as an endocrine factor. It is found in the liver, adipose tissue, central nervous system and other tissues, with circulating FGF-21 being expressed in the liver. It is a stress-inducible hormone that plays a key role in regulating energy balance, as well as glucose and lipid homeostasis, through a heterodimeric receptor complex composed of FGF receptor 1 (FGFR1), which is a tyrosine kinase, and co-receptor beta-Klotho. In the liver, the effects of transcription factor PPARalpha (Peroxisome proliferator-activated receptor alpha) are mediated by increased production of FGF-21. FGF-21 regulates sugar intake and insulin sensitivity. Mutations in FGF-21 have been linked to obesity and type-2 diabetes (T2D) risk, therefore FGF-21 has attracted attention as a therapeutic target for those disorders. Further studies are required to elucidate the detailed mechanisms of action of FGF-21 and the benefits of drugs targeting this hepatokine. Futibatinib, also known as TAS-120 is an orally bioavailable, highly selective, and irreversible FGFR1-4 inhibitor, currently being used in the treatment of intrahepatic cholangiocarcinoma, a bile duct cancer in the liver.