Phase I, first-in-human study of futibatinib, a highly selective, irreversible FGFR1–4 inhibitor in patients with advanced solid tumors

Abstract

Background: Futibatinib is an oral, irreversible, highly selective fibroblast growth factor receptor (FGFR)1–4 inhibitor with potent preclinical activity against tumors harboring FGFR aberrations. This first-in-human, phase I dose-escalation trial (NCT02052778) evaluates the safety and pharmacokinetics/pharmacodynamics of futibatinib in advanced solid tumors. Patients and methods: Following a standard 3+3 dose-escalation design, eligible patients with advanced solid tumors refractory to standard therapies received 8–200 mg futibatinib three times a week (t.i.w.) or 4–24 mg once daily (q.d.). Results: A total of 86 patients were enrolled in the nine t.i.w. (n = 42) and five q.d. cohorts (n = ..