2-Pyridineacetamide, N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[(3R)-3-[(1-oxo-2-butyn-1-yl)amino]-1-piperidinyl]-

BMF-219 is the first and only covalent menin inhibitor in clinical development and is being evaluated in multiple hematologic malignancies, solid tumours, and diabetes mellitus. COVALENT-101 (NCT05153330) is a Phase I dose-escalation and -expansion study of BMF-219 in R/R AL, DLBCL, MM, and CLL.

BMF-219 is a covalently binding inhibitor of menin, a protein that plays an essential role in oncogenic signaling in genetically defined leukemias and diabetes. Preclinically, BMF-219 has demonstrated in well-established acute leukemia cell lines robust downregulation of essential leukemogenic genes in addition to menin itself. Additionally, BMF-219 has shown anticancer activity in multiple in vitro, in vivo, and ex vivo models of acute leukemia, multiple myeloma, diffuse large B-cell lymphoma and chronic lymphocytic leukemia. BMF-219 is currently being evaluated in first-in-human clinical trials enrolling patients with specific menin-dependent mutations in liquid and solid tumours and patients with diabetes.