RGT-018

RGT-018 is a potent, selective, and orally bioavailable small molecule inhibitor of Son of Sevenless 1 (SOS1), developed by Regor Therapeutics. SOS1 is a guanine nucleotide exchange factor (GEF) that facilitates the transition of KRAS from its inactive GDP-bound state to its active GTP-bound state. By binding to the catalytic domain of SOS1, RGT-018 prevents KRAS activation and suppresses the proliferation of a broad spectrum of mutant KRAS-driven cancers, including non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and pancreatic cancer. Preclinical data demonstrate that RGT-018 exhibits robust anti-tumor activity both as a monotherapy and in combination with other targeted agents such as MEK, KRAS G12C, EGFR, or CDK4/6 inhibitors. The compound was identified using Regor's Computer Accelerated Rational Design (CARD) technology platform.