KST-6051

KST-6051 is an investigational oral small-molecule pan-KRAS inhibitor developed by Kestrel Therapeutics for the treatment of KRAS-mutant solid tumors, including non-small cell lung cancer (NSCLC), pancreatic ductal adenocarcinoma (PDAC), and colorectal cancer (CRC). Utilizing proprietary Switch-II pocket chemistry, KST-6051 is designed to inhibit KRAS in both its active (GTP-bound, ON state) and inactive (GDP-bound, OFF state) forms. This broad-spectrum approach aims to provide more comprehensive pathway inhibition compared to first-generation allele-specific inhibitors. As of March 2026, the drug has received FDA Investigational New Drug (IND) clearance to begin the FALCON trial, a first-in-human Phase 1 study evaluating safety, pharmacokinetics, and preliminary anti-tumor activity.

Other names

Kestrel pan-KRAS inhibitor