BMF-500

BMF-500 is a novel, orally bioavailable, highly potent and selective covalent small molecule inhibitor of fms-like tyrosine kinase 3 (FLT3), including wild-type FLT3 as well as activating and resistance-conferring mutations such as ITD, TKD, and gatekeeper F691. It was discovered and developed in-house by Biomea Fusion using their proprietary FUSION System. As a third-generation FLT3 inhibitor, BMF-500 is designed to overcome limitations of earlier generation inhibitors by providing high target selectivity with minimal off-target effects (notably avoiding cKIT inhibition), sustained cell-killing even after drug washout, and strong activity against all known FLT3 mutations. Preclinical studies have demonstrated that BMF-500 has multi-fold higher potency than commercially available non-covalent FLT3 inhibitors like gilteritinib in acute myeloid leukemia (AML) models. The drug is currently being evaluated in Phase 1 clinical trials for relapsed or refractory acute leukemias including AML, acute lymphoblastic leukemia (ALL), and mixed phenotype acute leukemia[1][2][4][5][6][7].