PSTA-2413 / Prospect Therap - LARVOL DELTA

Discovery of PSTA-2413, an oral pan-RAS inhibitor with wild type selectivity and potent in vitro and in vivo efficacy (AACR-NCI-EORTC 2025) - "PSTA-2413 retained nanomolar activity in AMG510-resistant cells, suggesting potential to overcome G12C inhibitor resistance. In contrast, PSTA-2413 showed relatively reduced activity in KRAS wild-type cells compared to RMC-6236 and ERAS-0015...A preliminary rat toxicity study indicated a 10-fold safety margin. Conclusions PSTA-2413 shows distinct advantages over existing pan-RAS inhibitors, including enhanced in vitro potency, selectivity over wild-type KRAS, robust in vivo antitumor activity with tumor regression, favorable pharmacokinetics, and a promising safety profile—supporting its potential for clinical advancement."

Preclinical • Colorectal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • KRAS