AMI-408

AMI-408 is an early-phase, small molecule inhibitor of protein arginine methyltransferase 1 (PRMT1). PRMT1 is an enzyme responsible for the majority of asymmetric arginine dimethylation, an epigenetic modification implicated in the regulation of gene expression and oncogenesis. AMI-408 has demonstrated the ability to reduce levels of histone H4R3 asymmetric dimethylation (H4R3me2a), inhibit leukemic colony formation, suppress tumor burden, and prolong survival in preclinical mouse models of acute myeloid leukemia (AML) driven by MLL fusion oncogenes. Although not optimized for clinical use, AMI-408 is considered a proof-of-concept compound for PRMT1 targeting in hematological malignancies.