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gilteritinib fumarate

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The fumarate salt form of gilteritinib, an orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-like tyrosine kinase 3 (FLT3; STK1; FLK2), AXL (UFO; JTK11), anaplastic lymphoma kinase (ALK; CD246), and leukocyte receptor tyrosine kinase (LTK), with potential antineoplastic activity. Upon administration, gilteritinib binds to and inhibits both the wild-type and mutated forms of FLT3, AXL, ALK and LTK. This may result in an inhibition of FLT3-, AXL-, ALK-, and LTK-mediated signal transduction pathways and reduced proliferation in cancer cells that overexpress these RTKs. FLT3, AXL, ALK, and LTK, which are overexpressed or mutated in a variety of cancer cell types, play key roles in tumor cell growth and survival.
Synonym:gilteritinib hemifumarate
US brand name:Xospata
Code name:ASP-2215 hemifumarate
ASP2215 hemifumarate
Chemical structure:2-pyrazinecarboxamide, 6-ethyl-3-((3-methoxy-4-(4-(4-methyl-1-piperazinyl)-1-piperidinyl)phenyl)amino)-5-((tetrahydro-2H-pyran-4-yl)amino)-, (2E)-2-butenedioate (2:1)
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