BH-501284

BH-501284 is a potent, selective, orally available non-covalent pan-KRAS inhibitor developed by BlossomHill Therapeutics. It is designed to address the limitations of contemporary KRAS therapies by featuring picomolar binding affinity and a prolonged off-rate, leading to durable target engagement. Unlike many first-generation inhibitors that are mutation-specific, BH-501284 acts as a pan-KRAS inhibitor with broad activity across multiple KRAS mutations. It preferentially targets the inactive state of KRAS and maintains efficacy even under growth factor-driven resistance conditions. Preclinical studies have demonstrated robust and durable tumor regression in models of non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and pancreatic ductal adenocarcinoma (PDAC).