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Biomea Fusion Announces IND Candidate Selection: BMF-500, a Potential Best-in-Class Oral Covalent Inhibitor of FLT3
BMF-500, an investigational third-generation covalent inhibitor of FLT3, demonstrated picomolar IC50 values across key FLT3 isoforms, potentially making it
About this update from Biomea Fusion, Inc.
[{"type":"text","content":"BMF-500, an investigational third-generation covalent inhibitor of FLT3, demonstrated picomolar IC50 values across key FLT3 isoforms, potentially making it the most potent inhibitor of its classHighly selective for FLT3, BMF-500 was observed to avoid other type III receptor tyrosine kinase (RTK) family members, including cKIT, which drives myelosuppression and limits utility of some first and second-generation FLT3 inhibitorsInitial in vivo studies demonstrated that BMF-500 elicited complete tumor regression of FLT3-ITD in mouse tumor models and maintained its effect without continued exposureBMF-500 is potentially synergistic with BMF-219, Biomea’s investigational covalent menin inhibitor currently in a Phase I clinical trial, COVALENT-101, for acute myeloid leukemia (AML)Together, BMF-500 and BMF-219 could potentially treat the majority of AML patients as single agents or in combinationBMF-500 was designed and developed in-house, from target to IND candidate, utilizing Biomea’s proprietary FUSION™ System REDWOOD CITY, Calif., May 19, 2022 (GLOBE NEWSWIRE) -- Biomea Fusion, Inc. (Nasdaq: BMEA), a clinical-stage biopharmaceutical company dedicated to discovering and developing novel covalent small molecules to treat and improve the lives of patients with genetically defined cancers and metabolic diseases, announced the nomination of its second product candidate, BMF-500, a highly selective and potent covalent investigational third-generation FLT3 inhibitor. Approximately 30% of AML patients present with a FLT3 mutation and remain poorly controlled with currently available therapies. First and second-generation FLT3 inhibitors frequently have a narrow therapeutic window and patients often acquire rapid resistance to treatment, limiting the clinical efficacy of these agents. As a third-generation FLT3 inhibitor, BMF-500 is designed to overcome some of the characteristics that are believed to limit the duration of response and utility of these earlier generation FLT3 inhibitors. BMF-500 was discovered and developed in-house at Biomea using the company’s proprietary FUSION™ System. BMF-500, like BMF-219, was designed to be clinically effective at relatively low drug concentrations in order to deliver an optimal therapeutic profile. Specifically, BMF-500 was observed in preclinical studies to be a highly active inhibitor of FLT3 with...