Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]

FGFR3:1.6 nM (IC50), FGFR2 (E566G):2.4 nM (IC50), FGFR2:1.3 nM (IC50), FGFR2 (WT):0.3 nM (IC50), FGFR4:8.3 nM (IC50), FGFR2 (N550H):3.6 nM (IC50), FGFR2 (V5651):1-3 nM (IC50), FGFR1:3.9 nM (IC50)

TAS-120 (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. TAS-120 shows anti-tumor effect by administering at moderate intervals, such as intermittent administration of every other day dosing and 2 times/week, and reducing the sustained elevation and weight suppression blood phosphorus level, and take a antitumor effective as daily administration.

METHODS: Patient-derived ICC xenograft (PDX) model mice were treated with 25 mg/kg Futibatinib（TAS-120） orally daily for 3 and 14 days prior to harvest. Tumor samples were collected for biochemical analysis and histological processing.
RESULTS Treatment of MG69 PDX tumors with TAS-120 (beginning when they reached ~500 mm in volume 3) resulted in tumor regression and complete proliferation arrest, with effects evident within three days and sustained over the 14-day treatment course. [1]