molecules of the month

TAS-120 (futibatinib)

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

Structure of futibatinib (Tas-120)
1 min read

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.

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