{"entity":{"id":"gilteritinib","kind":"drug","name":"Gilteritinib","aka":[],"tldr":"A single pill that beats salvage chemotherapy for relapsed FLT3-mutated AML, and the backbone of the triplets now being tested in frontline disease.","summary":"ADMIRAL (n=371): gilteritinib vs salvage chemotherapy in relapsed/refractory FLT3-mutated AML, OS 9.3 vs 5.6 months (HR 0.64), CR/CRh 34%. Approved 2018. Post-transplant maintenance (MORPHO) reduced relapse in MRD-positive patients. Frontline triplets (gilteritinib + azacitidine + venetoclax) show high CR rates in unfit patients; the phase 3 vs midostaurin (HOVON 156 AML) reported non-superiority for EFS in 2025-26 data, keeping midostaurin/quizartinib as intensive standards.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Gilteritinib","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Gilteritinib"}],"tags":[],"related":["flt3-itd","flt3-tkd"],"cancers":["aml","aml-flt3"],"sections":[],"technologies":["kinase-inhibitors"],"targets":["flt3"],"drugs":[],"companies":["astellas"],"institutions":[],"pathways":[],"terms":["differentiation-syndrome"],"trials":["admiral","nct04988555","nct05520567","nct03182244"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Xospata","modality":"Small-molecule kinase inhibitor (FLT3, type I)","mechanism":"Type I FLT3/AXL inhibitor active against ITD and TKD (D835) mutations.","approvals":[{"region":"US","year":2018,"indication":"Relapsed or refractory FLT3-mutated AML"}],"mechanismSteps":["Gilteritinib binds active FLT3 regardless of ITD or TKD mutation","AXL, a bypass kinase, is co-inhibited","STAT5/MAPK/PI3K signalling collapses in blasts","Oral daily dosing continues until progression or as post-transplant maintenance"],"dosing":{"route":"Oral","schedule":"120 mg once daily until progression or unacceptable toxicity (minimum 6 months to allow response)","monitoring":"Differentiation syndrome (boxed warning), QT, LFTs, PRES, pancreatitis","source":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Xospata"},"toxicity":[{"event":"Differentiation syndrome","anyGradePct":3,"source":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Xospata","note":"Boxed warning"},{"event":"Transaminase elevation","anyGradePct":44},{"event":"Myalgia/arthralgia","anyGradePct":42},{"event":"Febrile neutropenia","grade3PlusPct":46}],"access":[],"regulatoryEvents":[{"date":"2018-11-28","type":"approval","region":"US","note":"ADMIRAL interim; full OS data 2019"}]},"route":"/drugs/gilteritinib/","neighbours":{"biomarker":[{"id":"flt3-itd","kind":"biomarker","name":"FLT3-ITD (internal tandem duplication)","route":"/biomarkers/flt3-itd/"},{"id":"flt3-tkd","kind":"biomarker","name":"FLT3-TKD (D835 and I836 tyrosine kinase domain mutations)","route":"/biomarkers/flt3-tkd/"}],"cancer":[{"id":"aml","kind":"cancer","name":"Acute myeloid leukaemia","route":"/cancers/aml/"},{"id":"aml-paediatric","kind":"cancer","name":"Acute myeloid leukaemia in children","route":"/cancers/aml-paediatric/"},{"id":"aml-older-unfit","kind":"cancer","name":"Acute myeloid leukaemia in older or unfit patients","route":"/cancers/aml-older-unfit/"},{"id":"aml-flt3","kind":"cancer","name":"FLT3-mutated acute myeloid leukaemia","route":"/cancers/aml-flt3/"},{"id":"aml-secondary","kind":"cancer","name":"Secondary and therapy-related acute myeloid leukaemia","route":"/cancers/aml-secondary/"}],"technology":[{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"target":[{"id":"flt3","kind":"target","name":"FLT3","route":"/targets/flt3/"},{"id":"stat5","kind":"target","name":"STAT5 (STAT5A, STAT5B)","route":"/targets/stat5/"}],"company":[{"id":"astellas","kind":"company","name":"Astellas","route":"/companies/astellas/"}],"term":[{"id":"seven-plus-three","kind":"term","name":"7+3 induction chemotherapy","route":"/terms/seven-plus-three/"},{"id":"differentiation-syndrome","kind":"term","name":"Differentiation syndrome","route":"/terms/differentiation-syndrome/"}],"trial":[{"id":"nct04988555","kind":"trial","name":"A Phase 1/2 Study of Enzomenib (DSP-5336) in Patients With Acute Leukemia (Horizen-1)","route":"/trials/nct04988555/"},{"id":"nct03182244","kind":"trial","name":"A Study of ASP2215 Versus Salvage Chemotherapy In Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) With FMS-like Tyrosine Kinase 3 (FLT3) Mutation","route":"/trials/nct03182244/"},{"id":"nct05520567","kind":"trial","name":"A Study of Gilteritinib, Venetoclax and Azacitidine as a Combined Treatment for People Newly Diagnosed With Acute Myeloid Leukemia","route":"/trials/nct05520567/"},{"id":"nct04293562","kind":"trial","name":"A Study to Compare Standard Chemotherapy to Therapy With CPX-351 and/or Gilteritinib for Patients With Newly Diagnosed AML With or Without FLT3 Mutations","route":"/trials/nct04293562/"},{"id":"admiral","kind":"trial","name":"ADMIRAL","route":"/trials/admiral/"},{"id":"beat-aml-master-trial","kind":"trial","name":"Beat AML Master Trial","route":"/trials/beat-aml-master-trial/"},{"id":"morpho","kind":"trial","name":"MORPHO","route":"/trials/morpho/"}],"pairing":[{"id":"flt3i-plus-7-3","kind":"pairing","name":"FLT3 inhibitor + intensive chemotherapy","route":"/pairings/flt3i-plus-7-3/"}],"person":[{"id":"eunice-wang","kind":"person","name":"Eunice S. Wang","route":"/people/eunice-wang/"}],"paper":[{"id":"paper-admiral-gilteritinib-flt3-nejm-2019","kind":"paper","name":"ADMIRAL: gilteritinib pills versus chemotherapy for relapsed FLT3-mutated acute myeloid leukaemia","route":"/key-papers/paper-admiral-gilteritinib-flt3-nejm-2019/"},{"id":"paper-morpho-gilteritinib-levis-jco-2024","kind":"paper","name":"MORPHO: gilteritinib as post-transplant maintenance for FLT3-ITD acute myeloid leukaemia","route":"/key-papers/paper-morpho-gilteritinib-levis-jco-2024/"},{"id":"paper-quantum-first-quizartinib-lancet-2023","kind":"paper","name":"QuANTUM-First: quizartinib added to intensive chemotherapy and continued as maintenance in newly diagnosed FLT3-ITD AML","route":"/key-papers/paper-quantum-first-quizartinib-lancet-2023/"}],"pathway":[{"id":"aml-signalling","kind":"pathway","name":"Acute myeloid leukaemia (KEGG map)","route":"/pathways/aml-signalling/"}]}}