ARTS-051 / Allorion Therap - LARVOL DELTA

Characterization of ARTS-051, a potent and selective Werner helicase inhibitor effective against a broad range of MSI-H colorectal cancer models (AACR 2026) - "In contrast, ARTS-051 is effective in WRN C727S and C727A mutant HCT116 cells, outperforming the clinical stage WRN inhibitor HRO761 by nearly 10-fold. Additionally, ARTS-051 displays good drug-like properties including solubility, permeability, and liver microsome stability, as well as a positive PK profile with low clearance and good oral exposure across species, supporting favorable clinical dose projections. Taken together, these data show that ARTS-051 is a promising WRN inhibitor with best-in-class potential to treat MSI-H colorectal cancers."

Late-breaking abstract • MSI-H • Preclinical • Colorectal Cancer • Microsatellite Instability • Oncology • Solid Tumor • MSI • WRN