ETX-880 / Ensem Therap - LARVOL DELTA

ETX-880, a potential best-in-class, oral, highly potent and selective covalent inhibitor of Werner helicase for the treatment of microsatellite instability-high (MSI-H) cancers (AACR 2026) - "The preclinical activity of ETX-880 was characterized and compared to clinical stage WRN inhibitors, including RO7589831, HRO761, and GSK4418959 (non-covalent). Importantly, human PK predictions reveal low clearance, high oral bioavailability and long half-life, supporting a low once daily oral efficacious dose. Overall, ETX-880 is a potent, selective, covalent WRN inhibitor with excellent ADMET properties leading to deep and sustained target coverage, highlighting its best-in-class potential in MSI-H cancers."

IO biomarker • MSI-H • Colorectal Cancer • Microsatellite Instability • Oncology • Solid Tumor • MSI • WRN

Ensem Therapeutics Highlights Novel, Potent, and Selective Oral pan-KRAS and WRN Inhibitors with Best-in-Class Potential (Businesswire) - "The data support the differentiated preclinical profiles of ETX-929, a pan-KRAS inhibitor for the treatment of KRAS-altered solid tumors, and ETX-880, a covalent WRN inhibitor for the treatment of microsatellite instability-high (MSI-H) solid tumors."

MSI-H • Preclinical • Microsatellite Instability • Solid Tumor