balamenib

Balamenib (ZE63-0302) is an oral small molecule inhibitor that selectively targets the menin-KMT2A (also known as MLL1) interaction. By disrupting this protein-protein interaction, balamenib inhibits the formation of oncogenic fusion complexes on chromatin, leading to downregulation of leukemogenic transcriptional programs such as HOX and MEIS1 gene expression. This mechanism is particularly relevant in acute myeloid leukemia (AML), especially in cases with KMT2A rearrangements or NPM1 mutations. Balamenib has demonstrated a differentiated preclinical safety profile compared to other menin inhibitors, notably lacking QTc prolongation and not being a substrate or inducer of CYP3A4 metabolism. The drug is being developed by Eilean Therapeutics for hematologic malignancies including AML[1][3][5][6].

Other names

balamenib