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DOI: 10.1055/s-0045-1809991
Gilteritinib
Funding None.

Abstract
Introduction
Acute myeloid leukemia (AML) is a heterogeneous and aggressive form of blood cancer that affects the myeloid lineage of the cells. Among various genetic mutations associated with AML, the FLT-3 mutation is one of the most common and associated with poor prognosis. Gilteritinib (previously known as ASP2215) is the first tyrosine kinase inhibitor approved as monotherapy for treatment of relapsed/refractory AML.
Areas Covered
We review gilteritinib in detail, including its mechanism of action, pharmacology, efficacy, toxicity profile, and key clinical trials.
Patient Consent
Patient consent is not required.
Publikationsverlauf
Artikel online veröffentlicht:
10. Juli 2025
© 2025. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting unrestricted use, distribution, and reproduction so long as the original work is properly cited. (https://creativecommons.org/licenses/by/4.0/)
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References
- 1 Perl AE, Martinelli G, Cortes JE. et al. Gilteritinib or chemotherapy for relapsed or refractory FLT3-mutated AML. N Engl J Med 2019; 381 (18) 1728-1740
- 2 Levis M, Perl AE. Gilteritinib: potent targeting of FLT3 mutations in AML. Blood Adv 2020; 4 (06) 1178-1191
- 3 Pratz KW, Cherry M, Altman JK. et al. Gilteritinib in combination with induction and consolidation chemotherapy and as maintenance therapy: a phase IB study in patients with newly diagnosed AML. J Clin Oncol 2023; 41 (26) 4236-4246
- 4 Astellas Pharma US, Inc. Highlights of prescribing information [Internet]. Northbrook, IL: Astellas Pharma US, Inc.; 2018 . Accessed April 4, 2025 at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211349s000lbl.pdf
- 5 McMahon CM, Canaani J, Rea B. et al. Gilteritinib induces differentiation in relapsed and refractory FLT3-mutated acute myeloid leukemia. Blood Adv 2019; 3 (10) 1581-1585
- 6 Levis MJ, Hamadani M, Logan B. et al; BMT-CTN 1506/MORPHO Study Investigators. Gilteritinib as post-transplant maintenance for AML with internal tandem duplication mutation of FLT3 . J Clin Oncol 2024; 42 (15) 1766-1775
- 7 Daver N, Perl AE, Maly J. et al. Venetoclax plus gilteritinib for FLT3-mutated relapsed/refractory acute myeloid leukemia. J Clin Oncol 2022; 40 (35) 4048-4059
- 8 Janssen M, Schmidt C, Bruch PM. et al. Venetoclax synergizes with gilteritinib in FLT3 wild-type high-risk acute myeloid leukemia by suppressing MCL-1. Blood 2022; 140 (24) 2594-2610
- 9 Wang ES, Montesinos P, Minden MD. et al. Phase 3 trial of gilteritinib plus azacitidine vs azacitidine for newly diagnosed FLT3mut+ AML ineligible for intensive chemotherapy. Blood 2022; 140 (17) 1845-1857
- 10 Maiti A, DiNardo CD, Daver NG. et al. Triplet therapy with venetoclax, FLT3 inhibitor and decitabine for FLT3-mutated acute myeloid leukemia. Blood Cancer J 2021; 11 (02) 25
- 11 Abuasab T, Kantarjian H, Garcia-Manero G. et al. Phase II study of cladribine, idarubicin, cytarabine (CLIA) plus gilteritinib in patients with FLT3 mutated acute myeloid leukemia (AML). Blood 2021; 138 (Supplement 1): 2330
- 12 Numan Y, Abdel Rahman Z, Grenet J. et al. Gilteritinib clinical activity in relapsed/refractory FLT3 mutated acute myeloid leukemia previously treated with FLT3 inhibitors. Am J Hematol 2022; 97 (03) 322-328
- 13 Gyan E, Minden MD, Kubo K. et al. Maintenance therapy with the FMS-like tyrosine kinase 3 inhibitor gilteritinib in patients with FMS-like tyrosine kinase 3-internal tandem duplication acute myeloid leukemia: a phase 2 study. Cancer 2025; 131 (04) e35746
- 14 Shatilova A, Budaeva I, Matvienko Y. et al. Myeloid sarcoma or extramedullary acute myeloid leukemia: experience in managing single-centre patients cohort. Blood 2024; 144 (Supplement 1): 5987
- 15 HOVON Foundation. . Gilteritinib versus midostaurin in FLT3 mutated acute myeloid leukemia. ClinicalTrials.gov Identifier: NCT04027309. Amsterdam: HOVON; 2018 [updated June 13, 2023]. Accessed April 08, 2025 at: https://clinicaltrials.gov/study/NCT04027309
- 16 Smith CC, Levis MJ, Perl AE, Hill JE, Rosales M, Bahceci E. Molecular profile of FLT3-mutated relapsed/refractory patients with AML in the phase 3 ADMIRAL study of gilteritinib. Blood Adv 2022; 6 (07) 2144-2155