ERAS-601 + gilteritinib

**ERAS-601 + gilteritinib** is a combination of two investigational/approved small molecule drugs for the treatment of FLT3-mutated acute myeloid leukemia (AML). ERAS-601 is a potent, selective allosteric inhibitor of SHP2, a protein tyrosine phosphatase encoded by PTPN11, which mediates receptor tyrosine kinase (RTK) signaling and is involved in the regulation of the RAS/MAPK pathway. Gilteritinib is an oral small molecule inhibitor of fms-like tyrosine kinase 3 (FLT3), approved for relapsed or refractory FLT3-mutated AML. Preclinical studies demonstrated that the combination synergistically inhibits oncogenic RAS/MAPK signaling, cellular viability, and tumor growth in FLT3-ITD mutant AML cell models better than either agent alone. This combination is being developed in clinical trials, including the HERKULES-4 Phase 1b/2 study, for patients with FLT3-mutated AML[1][5]. ERAS-601 is being developed by Erasca. Gilteritinib (Xospata) is developed and manufactured by Astellas.

Other names

ERAS-601 + Xospata