IDE251

IDE251 is an equipotent, highly selective, small molecule dual inhibitor of lysine acetyltransferase 6 (KAT6) and lysine acetyltransferase 7 (KAT7). It is being developed as a potential first-in-class therapy for cancers characterized by 8p11 amplification, particularly in breast cancer and squamous non-small cell lung cancer (NSCLC). KAT6 and KAT7 are epigenetic modulators involved in cell identity and lineage commitment; their dysregulation supports oncogenic transformation. Preclinical studies have shown that IDE251 delivers robust and durable anti-tumor activity superior to KAT6 inhibition alone in models with 8p11 amplifications. The drug is designed to spare other structurally similar KAT family members, potentially reducing off-target effects. IND-enabling studies are ongoing with a targeted Investigational New Drug submission planned for 2025[1][2][3][4][5][8].