XOSPATA Is the First FDA-Approved Targeted Therapy for Relapsed or Refractory FLT3m+ AML That Inhibits ITD and TKD Mutations1

XOSPATA targets FLT3 mutations, a key driver
of disease in relapsed or refractory AML1,2

  • XOSPATA is a small molecule that inhibits multiple receptor tyrosine kinases, including FLT31
  • XOSPATA demonstrated the ability to inhibit FLT3 receptor signaling and proliferation in cells exogenously expressing FLT3 mutations, including1:
    • FLT3-ITD
    • FLT3-TKD (FLT3-D835Y)
    • FLT3-ITD and FLT3-TKD (FLT3-ITD-D835Y)
  • Additionally, XOSPATA induced apoptosis in leukemic cells expressing FLT3-ITD1

AML=acute myeloid leukemia; FLT3=FMS-like tyrosine kinase 3; ITD=internal tandem duplication; m+=mutation-positive; TKD=tyrosine kinase domain.

References: 1. XOSPATA [package insert]. Northbrook, IL: Astellas Pharma US, Inc. 2. Smith CC, Wang Q, Chin CS, et al. Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia. Nature 2012;485(7397):260-3. 3. Annesley CE, Brown P. The biology and targeting of FLT3 in pediatric leukemia. Front Oncol 2014;4:263. 4. Mori M, Kaneko N, Ueno Y, et al. Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia. Invest New Drugs 2017;35(5):556-65.