Futibatinib (TAS-120, TAS120) is a highly potent, selective, irreversible pan-FGFR inhibitor with IC50 of 0.9 nM for wt FGFR2.
TAS-120 inhibits cancer cell growth in vitro and shows promising activity in human xenografts of FGFR mutation-bearing tumours.
TAS-120 inhibits mutant and wild-type FGFR2 with similar IC50 (wild-type FGFR2, 0.9 nM; V565I 1.3 nM; N550H, 3.6 nM; E566G, 2.4 nM) and has shown efficacy in FGFR inhibitor-resistant cell lines.
1. Hiroaki Ochiiwa, et al. Abstract A270: TAS-120, a highly potent and selective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities. AACR 2013.
2. Kalyukina M, et al. ChemMedChem. 2019 Jan 2. doi: 10.1002/cmdc.201800719.
