TASI-120 is a highly selective, irreversible FGFR1-4 tyrosine kinase inhibitor. It exhibited similar IC50 for wild type FGFR1-4 and FGFR2 key mutants (including V565I, N550H, E566G, and K660M). In a phase I results presented at the 2018 World Congress on GI Cancer, 45 patients with cholangiocarcinoma were enrolled, with 28 cases (62.2%) with FGFR2 fusion. Among these 28 patients, 20 (71.4%) had tumor shrinkage after treatment with TAS-120, even in those who have been treated with other FGFR inhibitors. The objective response rate was 7/28 (25%) and the disease control rate was 22/28 (78.6%). These results demonstrated that TAS-120 had meaningful clinical benefit in cholangiocarcinoma patients with FGFR2 gene fusions. A global Phase 2 study has been initiated in CCA patients with FGFR2 gene fusions.
Source : Meric-Bernstam F, et al. Ann Oncol. 2018;29 (suppl 5; abstr O-001)