Gilteritinib (Astellas) is an oral multi-tyrosine kinase inhibitor of anaplastic lymphoma kinase (ALK), Axl receptor tyrosine kinase, and FMS-like tyrosine kinase 3 (FLT3). Mutations in the FLT3 gene are found in more than 30% of patients with acute myeloid leukemia (AML) and result in disruption of the secondary structure of the tyrosine kinase, which often leads to constitutive receptor activation and unregulated cell signaling. Gilteritinib exerts its anti-tumor activity by binding to and inhibiting signaling mediated through mutated versions of the FLT3 receptor often found in AML patients.
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