oral irreversible FGFR1-4 inhibitor
in Ph. I-III trials for FGFR+ advanced tumors
from structure-based design
Cancer Res., Sep. 24, 2020
Taiho Pharmaceutical, Tokyo, JP
TAS-120 (futibatinib) is an orally available, irreversible FGFR1-4 inhibitor with a unique binding mode, targeting a unique cysteine in the P-loop of the FGFRs, rather than the Cys in the hinge region of FGFR4 as for roblitinib (above) or BLU9931 and fisogatinib. It is currently the most advanced irreversible FGFR inhibitor in clinical development with a Ph. III trial on-going.