GTA182

GTA182 is a proprietary, brain-penetrant, second-generation small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5). It is designed to be MTA-cooperative, meaning its inhibitory activity is enhanced in the presence of methylthioadenosine (MTA), which accumulates in cells with deletions of the MTAP gene. This confers high selectivity for MTAP-deleted cancer cells—found in up to 10% of solid tumors including glioblastoma, lung, pancreatic, and bladder cancers—while sparing normal cells. Preclinical studies have shown that GTA182 achieves over 100-fold selectivity for MTAP-deleted tumor cell lines and induces tumor regression in both central nervous system (CNS) and non-CNS models. The drug was discovered using Apeiron’s AI-guided drug discovery platform and is currently being evaluated in Phase 1 clinical trials for patients with advanced solid tumors harboring MTAP deletions[2][3][4][5][6][7].