E2082-0047

E2082-0047 is a potent, small molecule tyrosine kinase inhibitor specifically targeting the Fms-like tyrosine kinase 3 (FLT3) receptor. It is being developed for the treatment of acute myeloid leukemia (AML), with a particular focus on FLT3-mutant AML that has developed resistance via gatekeeper mutations (e.g., F691L). Originally discovered through a collaboration between ChemDiv, Molsoft, and Expert Systems, the compound is currently being advanced by Eilean Therapeutics. Preclinical studies have demonstrated that E2082-0047 possesses superior potency and selectivity against gatekeeper-resistant FLT3 mutants compared to existing inhibitors like gilteritinib, achieving high selectivity through a multi-property optimization approach. As of late 2023, the drug was described as a clinical candidate supporting ongoing development.