KMT2A-rearranged acute myeloid leukemia (AML) is a highly aggressive leukemia subtype characterized by poor prognosis and high relapse rates. Because the menin-MLL interaction is essential for the stability and transcriptional activity of MLL fusion complexes, targeting this protein-protein interaction represents a promising therapeutic strategy for this aggressive form of AML. Researchers from Zhejiang University reported the discovery and preclinical characterization of [I], a novel menin inhibitor, designed for the treatment of AML.