ISM6166

ISM6166 is a preclinical, orally bioavailable small molecule pan-KRAS inhibitor developed by Insilico Medicine using its proprietary Chemistry42 generative AI platform. It is designed as a dual-state inhibitor, meaning it binds to KRAS in both its active (GTP-bound 'ON') and inactive (GDP-bound 'OFF') states. The compound demonstrates broad-spectrum activity against multiple KRAS mutations and alterations while maintaining selectivity by sparing related proteins HRAS and NRAS. Preclinical studies have shown significant tumor growth inhibition and regression in various KRAS-driven solid tumor models, including lung adenocarcinoma, pancreatic, colorectal, and gastric cancers. As of early 2026, the program is in IND-enabling stages with the goal of entering clinical trials either independently or through partnerships.

Other names

ISM6166ISM-6166ISM 6166