Biomea Fusion highlights 2023 corporate milestones

ONCOLOGY: COVALENT-101: Presented robust anti-tumor activity of covalent menin small molecule inhibitor, BMF-219, as a single agent and mechanistic evidence for novel inhibition of the menin protein in preclinical models of diffuse large B-cell lymphoma, multiple myeloma, and chronic lymphocytic leukemia. BMF-219 displayed single agent potency, surpassing greater than 90% cell killing at clinically relevant exposures in DLBCL, MM and CLL cell lines and patient-derived samples. BMF-219 is the first investigational menin inhibitor in clinical development to show potential as a therapeutic agent in hematologic malignancies outside of MLLr and NPM1 mutated acute myeloid leukemia/acute lymphoblastic leukemia patients, specifically in subsets of DLBCL, MM and CLL patients. Biomea continued site activation and patient enrollment for the dosing of BMF-219 across four liquid tumor cohorts in the COVALENT-101 study, including patients with AML/ALL, DLBCL, MM and CLL. Next Anticipated Milestone: On track to present initial clinical data of AML/ALL patients dosed in the COVALENT-101 study in the first half of 2023. COVALENT-102: Presented strong and highly specific pan-KRAS anti-cancer activity of BMF-219 as a single agent across KRAS G12C, G12D, G12V and G13D mutant cell lines including in non-small cell lung cancer, colorectal cancer and the most prevalent type of pancreatic cancer, PDAC. BMF-219 is the first investigational menin inhibitor in development to enter clinical trials for the treatment of solid tumors. A targeted pan-KRAS inhibitor could have the potential to treat 25-35% of NSCLC, 35-45% of CRC, and approximately 90% of PDAC patients. Biomea received FDA clearance of its IND in the fourth quarter of 2022 and has since initiated a Phase I/Ib clinical trial of BMF-219 as a monotherapy in patients who have unresectable, locally advanced, or metastatic NSCLC, CRC or PDAC with an activating KRAS mutation. Next Anticipated Milestone: On track to dose first patient in COVALENT-102 study in January 2023. COVALENT-103: Presented data showing multi-fold higher potency and increased cytotoxicity of Biomea’s covalent FLT3 small-molecule inhibitor BMF-500 compared to the commercially available reversible, non-covalent FLT3 inhibitor gilteritinib, and complete, sustained tumor regression in mouse models of FLT3-ITD AML with maintenance of effect after cessation of therapy. Next Anticipated Milestone:On track to file IND for BMF-500 in the first half of 2023 to initiate COVALENT-103 study of the covalent FLT3 inhibitor in patients with acute leukemia. DIABETES; COVALENT-111: Presented preclinical data highlighting the ability of BMF-219 in a Type 2 diabetes rat model to restore normal HOMA-B, a measure of pancreatic beta cell function, following only 4-weeks of treatment and to significantly lower HbA1c compared to active control, liraglutide, -3.5% vs -1.7%, respectively. BMF-219 is the first investigational menin inhibitor in development to enter clinical trials for the improvement of glycemic control and insulin sensitivity in Type 2 diabetes patients. Biomea completed the healthy volunteer portion of the Phase I/II COVALENT-111 study of BMF-219 in Canada. BMF-219 was well tolerated with an encouraging pharmacokinetic and pharmacodynamic profile in healthy volunteers and with no safety signals detected.Biomea received FDA clearance in December 2022 to expand the Phase II portion of COVALENT-111 to sites in the U.S. and in January 2023 announced dosing of the first U.S. patient with Type 2 diabetes. The company continues to enroll Type 2 diabetes patients in the Phase II portion of the study in Canada as well. Next Anticipated Milestones: On track to present initial clinical data from the first two cohorts of the Phase II portion of the study by the end of Q1 2023, and to present details of the healthy volunteer portion of the study at a scientific medical meeting in 2023. FUSION SYSTEM DISCOVERY PLATFORM: Developed two covalently binding small molecules, each within 18 months from target identification to IND candidate, leveraging the proprietary FUSION System Discovery Platform and showing excellent preclinical profiles. Next Anticipated Milestone: On track to announce a third development candidate from the FUSION platform in the first half of 2023.