PSTA-6208

PSTA-6208 is a highly potent, selective, and orally bioavailable small molecule inhibitor of the KRAS G12V mutant protein. Developed by Prospect Therapeutics, it is designed to target the constitutive activation of the MAPK pathway in KRAS G12V-driven cancers, such as pancreatic, colorectal, and lung malignancies. In preclinical studies, PSTA-6208 demonstrated sub-nanomolar cellular potency (IC50 ~0.1 nM) and over 500-fold selectivity for the G12V mutant over wild-type KRAS. The compound exhibits favorable pharmacokinetic properties, including a half-life of approximately 10 hours and high plasma exposure, supporting once-daily oral dosing. In vivo xenograft models have shown that PSTA-6208 induces significant tumor growth inhibition and regression at low doses, positioning it as a promising clinical candidate for KRAS G12V-positive solid tumors.