PE-0260

PE-0260 is a potent, selective, and oral brain-penetrant methylthioadenosine (MTA)-cooperative protein arginine methyltransferase 5 (PRMT5) inhibitor. Developed by PharmaEngine, it leverages the synthetic lethal relationship between PRMT5 and methylthioadenosine phosphorylase (MTAP) gene deletion, which occurs in approximately 10-15% of all cancers. PE-0260 demonstrates high selectivity for MTAP-deleted cells over wild-type cells across various solid tumors, including non-small cell lung cancer (NSCLC), glioblastoma (GBM), pancreatic, and breast cancers. Its ability to penetrate the blood-brain barrier makes it a promising candidate for treating primary brain tumors and brain metastases.