Drug intelligence / Profile preview

gilteritinib

Development stage
Approved
Lead developer
Astellas Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Gilteritinib is an oral small molecule tyrosine kinase inhibitor that selectively inhibits FMS-like tyrosine kinase 3 (FLT3) and AXL receptor tyrosine kinases. It is primarily used for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) harboring FLT3 mutations. Gilteritinib blocks FLT3 receptor signaling and inhibits the proliferation of leukemia cells with FLT3-ITD and TKD mutations, inducing apoptosis in these cells. The drug was developed by Astellas Pharma and was first approved by the US FDA in November 2018 for this indication. In China, it is marketed as Xospata/适加坦 and received conditional approval in January 2021 for treating relapsed or refractory AML with FLT3 mutations[1][4][5][6].

Brand names
Xospata适加坦
Other names
吉瑞替尼富马酸吉瑞替尼片gilteritinib fumarate tablets
02

Targets

AXL (AXL receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)

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