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Ref Type
Authors C. Morizane, T. Kojima, Y. Kuboki, H. Bando, N. Matsubara, K. Shitara, K. Yoh, H. Hirai, T. Kato, T. Doi
Title Phase I study of the irreversible FGFR inhibitor (i) futibatinib (FBN; TAS-120) in Japanese patients (pts) with advanced (adv) solid tumours
Abstract Text Background: The FGFRi FBN showed tolerability and preliminary efficacy in a phase I dose-escalation (DE)/expansion (EX) study conducted in primarily Caucasian pts with adv solid tumours (NCT02052778), and 20 mg once-daily (QD) FBN was established as the recommended phase II dose (RP2D). Here, we report results from a Japanese phase I DE/EX study of FBN in adv solid tumours. Methods: In DE, pts received 8–160 mg FBN thrice weekly (TIW; accelerated titration or standard 3+3 design), or 16 and 20 mg QD. The primary objective was safety and maximum tolerated dose (MTD) evaluation; secondary were pharmacokinetics (PK) and preliminary efficacy. The EX phase included pts with FGF/FGFR abnormalities receiving FBN at doses < MTD. Results: Sixty-three pts were enrolled in 8 TIW (DE; 29 pts, EX; 11 pts) and 2 QD cohorts (DE; 10 pts, EX; 13 pts). Pts had colorectal (16%), esophageal (13%), gastric (13%), or biliary tract cancer (11%), and 52% had tumors with FGF/FGFR aberrations. No DLTs were observed in the study; MTD was not reached with TIW dosing. QD enrollment was based on prior phase I data and 20 mg QD was determined as the RP2D. Overall, 5% of pts experienced grade (gr) ≥3 treatment-related adverse events (TRAEs). Most common TRAEs (all gr; gr ≥3) were hyperphosphatemia (89%; 0), decreased appetite (22%; 0), nausea (19%; 0), stomatitis (14%; 2%), retinal detachment (13%; 0), and elevated AST (11%; 3%). TRAEs led to dose reductions, interruptions, and discontinuation in 24%, 48%, and 0% of pts, respectively. The PK profile of 20 mg QD FBN (mean Cmax, 253 ng/mL; AUC0-last, 977ng·h/mL; median Tmax, 2.00 h; apparent T1/2, 2.18 h) was similar to that observed in Caucasian pts. Efficacy assessment is ongoing; at data cutoff (July 4, 2019), partial responses were observed in pts with gastric (n=2; tumor shrinkages of 59% and 70%) and breast cancer (n=1; tumor shrinkage, 37%) harboring FGFR2 amplifications. Conclusions: FBN showed manageable safety and preliminary efficacy in Japanese pts with adv solid tumors; RP2D (20 mg QD) in this study was consistent with prior results. Phase 2/3 studies in cholangiocarcinoma (NCT02052778; NCT04093362), gastric (NCT04189445) and breast tumours (NCT04024436) are ongoing. Clinical trial identification: JapicCTI-142552.


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 amp stomach cancer predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Lytgobi (futibatinib) treatment resulted in a partial response in 2 patients with gastric cancer harboring FGFR2 amplification, with 59% and 90% tumor shrinkage, respectively (Annals of Oncology (2020) 31 (suppl_4): S475). detail...
FGFR2 amp breast cancer sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Lytgobi (futibatinib) treatment resulted in a partial response in a patient with breast cancer harboring FGFR2 amplification, with 37% tumor shrinkage (Annals of Oncology (2020) 31 (suppl_4): S475). detail...