OST08267 / Open Source Therapeutics - LARVOL DELTA

Discovery of OST08267, an orally available PDE3A-SLFN12 molecular glue for the treatment of gastrointestinal stromal tumors with tyrosine kinase inhibitors (TKIs) resistance (AACR 2025) - "In vivo, OST08267 causes dose-dependent regression of tumor volume in the GIST patient-derived xenograft (PDX) model with imatinib resistance, with 4 mg/kg/day dose resulting in deeper and durable tumor regressions that were maintained for at least a month even after the dosing had discontinued.Moreover, OST08267 exhibited favorable pharmacokinetic and toxicity properties. These promising preclinical results strongly support the potential of OST08267 to address unmet needs in GIST treatment, justifying its further clinical development."

Stroma • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Oncology • Sarcoma • KIT • PDE3A • SLFN