{"entity":{"id":"futibatinib","kind":"drug","name":"Futibatinib","aka":[],"tldr":"Futibatinib is a covalent FGFR inhibitor for FGFR2-fusion bile duct cancer, with the highest response rate of the first-generation drugs.","summary":"Futibatinib is an irreversible inhibitor of FGFR1-4 that binds covalently to a cysteine in the kinase P-loop, a mechanism that retains activity against some resistance mutations that defeat reversible FGFR inhibitors. It is used in previously treated intrahepatic cholangiocarcinoma with an FGFR2 fusion or rearrangement. FOENIX-CCA2 (NEJM 2023) showed an ORR of 42%, median PFS of 9.0 months and median OS of 21.7 months, the highest response rate of the first-generation FGFR drugs. Accelerated approval followed in September 2022 (EMA 2023) at 20 mg daily continuously; hyperphosphataemia is near universal (85%, 30% grade 3 or higher). Whether it should be preferred over pemigatinib, and how to treat acquired FGFR2 kinase-domain mutations, are open questions now addressed by agents such as tinengotinib. For a newcomer, futibatinib is the covalent FGFR pill for bile duct cancer.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Futibatinib","links":[{"label":"NEJM 2023","url":"https://www.nejm.org/doi/full/10.1056/NEJMoa2206834"},{"label":"NICE TA1005: futibatinib for previously treated FGFR2 fusion or rearrangement cholangiocarcinoma (11 September 2024)","url":"https://www.nice.org.uk/guidance/ta1005"}],"tags":[],"related":["fgfr2-fusion-rearrangement"],"cancers":["cholangiocarcinoma","intrahepatic-cholangiocarcinoma"],"sections":[],"technologies":["kinase-inhibitors"],"targets":["fgfr2"],"drugs":[],"companies":["taiho"],"institutions":[],"pathways":[],"terms":["fgfr2-fusion"],"trials":["foenix-cca2","nct06506955","nct07710885","nct05945823"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["Gallbladder cancer: the FDA indication is intrahepatic cholangiocarcinoma with an FGFR2 fusion or rearrangement (Lytgobi label), so futibatinib has no licensed or trial role in gallbladder cancer."],"brand":"Lytgobi","modality":"Small-molecule irreversible kinase inhibitor (FGFR1-4)","mechanism":"Irreversible covalent binder of the FGFR kinase P-loop cysteine.","approvals":[{"region":"US","year":2022,"indication":"Previously treated FGFR2-fusion/rearranged intrahepatic cholangiocarcinoma (accelerated)"},{"region":"EU","year":2023,"indication":"Same"},{"region":"UK","year":2024,"indication":"Locally advanced or metastatic cholangiocarcinoma with FGFR2 fusion or rearrangement after at least one systemic treatment; NICE TA1005 recommended 11 September 2024 as an alternative to pemigatinib","note":"https://www.nice.org.uk/guidance/ta1005"}],"mechanismSteps":[],"dosing":{"route":"Oral","schedule":"20 mg daily continuously","monitoring":"Phosphate, eyes"},"toxicity":[{"event":"Hyperphosphataemia","anyGradePct":85,"grade3PlusPct":30,"note":"FOENIX-CCA2"},{"event":"Alopecia","anyGradePct":33},{"event":"Dry mouth","anyGradePct":30}],"access":[],"regulatoryEvents":[{"date":"2022-09-30","type":"accelerated-approval","region":"US","note":"Accelerated approval on a surrogate endpoint; the confirmatory requirement was still open 4.0 years later, when the FDA's table was read.","indication":"Adult patients with previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma harboring fibroblast growth factor receptor 2 (FGFR2) gene fusions or other rearrangements"}]},"route":"/drugs/futibatinib/","neighbours":{"biomarker":[{"id":"fgfr2-fusion-rearrangement","kind":"biomarker","name":"FGFR2 fusion or rearrangement","route":"/biomarkers/fgfr2-fusion-rearrangement/"}],"cancer":[{"id":"biliary-tract-cancer","kind":"cancer","name":"Biliary tract cancer (all types)","route":"/cancers/biliary-tract-cancer/"},{"id":"cholangiocarcinoma","kind":"cancer","name":"Biliary tract cancer (cholangiocarcinoma)","route":"/cancers/cholangiocarcinoma/"},{"id":"gallbladder","kind":"cancer","name":"Gallbladder cancer","route":"/cancers/gallbladder/"},{"id":"intrahepatic-cholangiocarcinoma","kind":"cancer","name":"Intrahepatic cholangiocarcinoma","route":"/cancers/intrahepatic-cholangiocarcinoma/"}],"technology":[{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"target":[{"id":"fgfr1","kind":"target","name":"FGFR1","route":"/targets/fgfr1/"},{"id":"fgfr2","kind":"target","name":"FGFR2","route":"/targets/fgfr2/"}],"company":[{"id":"taiho","kind":"company","name":"Taiho Pharmaceutical (Otsuka)","route":"/companies/taiho/"}],"term":[{"id":"fgfr2-fusion","kind":"term","name":"FGFR2 fusions and rearrangements","route":"/terms/fgfr2-fusion/"}],"trial":[{"id":"foenix-cca2","kind":"trial","name":"FOENIX-CCA2","route":"/trials/foenix-cca2/"},{"id":"nct07710885","kind":"trial","name":"Futibatinib (TAS-120) in Patients With Advanced Biliary Tract Cancer","route":"/trials/nct07710885/"},{"id":"nct06506955","kind":"trial","name":"Futibatinib in Patients Previously Enrolled in an Antecedent Futibatinib as Monotherapy or Combination Therapy.","route":"/trials/nct06506955/"},{"id":"nct07745296","kind":"trial","name":"Investigating Precision Medicine in the Adjuvant Setting in Biliary Tract Cancer","route":"/trials/nct07745296/"},{"id":"nct05945823","kind":"trial","name":"Phase 2 Futibatinib in Combination With PD-1 Antibody Based Standard of Care in Solid Tumors","route":"/trials/nct05945823/"},{"id":"safir-abc10","kind":"trial","name":"SAFIR-ABC10","route":"/trials/safir-abc10/"}],"idea":[{"id":"idea-btc-ctdna-fgfr-resistance","kind":"idea","name":"ctDNA-guided switching among FGFR inhibitors","route":"/ideas/idea-btc-ctdna-fgfr-resistance/"}],"pathway":[{"id":"fgfr-signalling","kind":"pathway","name":"FGF / FGFR signalling","route":"/pathways/fgfr-signalling/"},{"id":"proteoglycans-in-cancer","kind":"pathway","name":"Proteoglycans in cancer","route":"/pathways/proteoglycans-in-cancer/"}],"drug":[{"id":"infigratinib","kind":"drug","name":"Infigratinib","route":"/drugs/infigratinib/"}]}}