Drug intelligence / Profile preview

gilteritinib + azacitidine

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

**Gilteritinib + azacitidine** is a combination therapy being evaluated for the treatment of acute myeloid leukemia (AML), particularly in patients with FLT3-mutated AML who are unfit for intensive chemotherapy. **Gilteritinib** is an oral, second-generation small molecule inhibitor of fms-like tyrosine kinase 3 (FLT3), with additional activity against kinases such as AXL, ALK, and c-kit, and is approved for relapsed/refractory FLT3-mutant AML. **Azacitidine** is a DNA methyltransferase inhibitor and hypomethylating agent approved for the treatment of myelodysplastic syndromes and AML. The combination is investigated for synergistic efficacy, aiming to induce higher rates of complete remission (CR), molecular responses, and improved survival in FLT3-mutated AML. This regimen has been studied primarily for newly diagnosed or relapsed/refractory FLT3-mutated AML patients ineligible for intensive induction therapy[1][3][4][6].

02

Targets

AXL (AXL receptor tyrosine kinase)DNMT (DNA methyltransferase)FLT3 (Fms related receptor tyrosine kinase 3)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)DNAKIT (c-KIT proto-oncogene receptor tyrosine kinase)

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