Treatment of patient derived MLL-rearranged AML cells with EPZ004777 resulted in a concentration-dependent, selective reduction in global H3K79me1 and H3K79me2 levels.129 It also reduced the expression of key MLL fusion target genes (IC50 (scintillation proximity assay (SPA)) = 700 nM), and induced apoptosis-mediated cell death in MLL-rearranged cells. This evidence concerns the gene KMT2A and acute myeloid leukemia.