gilteritinib-hemifumarate

Description: Gilteritinib hemifumarate (formerly known as ASP2215 hemifumarate; Trade name: Xospata), the hemifumarate salt ofGilteritinib (ASP2215), is a potent small-molecule inhibitor of FLT3/AXL with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL respectively. It potently inhibits FLT3 with an IC50 that is about 800-fold higher than the concentration required to inhibit c-KIT (230 nM). Gilteritinib has the potential to treat leukemia such as AML with either or both FLT3-ITD and FLT3-D835 mutations. In vitro, among the 78 tyrosine kinases tested, Gilteritinib at 1 nM concentration inhibits FLT3, leukocyte tyrosine kinase (LTK), anaplastic lymphoma kinase (ALK), and AXL kinases by over 50% with an IC50 value of 0.29 nM for FLT3, and is approximately 800-fold more potent than for c-KIT. As of November 2018, Gilteritinib was approved by US FDA to treat patients who have relapsed or refractory acute myeloid leukemia (AML).

References: Invest New Drugs. 2017 Oct; 35(5):556-565; Blood. 2016, 128:2830

Related CAS#:1254053-43-4 (free base)