Revolution Medicines announced the first patient was dosed in its first-in-human clinical trial evaluating RMC-5127, a RAS(ON) G12V-selective inhibitor. The first-in-human trial, RMC-5127-001 [NCT07349537], is an open-label trial evaluating the safety, tolerability, pharmacokinetics, and preliminary antitumor activity of RMC-5127 as both a monotherapy and in combination settings. The trial will enroll patients with RAS G12V-mutated solid tumors, including pancreatic ductal adenocarcinoma (PDAC), colorectal cancer (CRC), and non-small cell lung cancer (NSCLC), who have progressed on or are intolerant to prior standard therapies, including targeted treatments.
RMC-5127 is an innovative inhibitor that binds to cyclophilin A, creating a complex that selectively recognizes and inhibits the oncogenic RAS(ON) form of the RAS G12V variant. RAS G12V is the second most common driver of RAS-addicted human cancers with approximately 48,000 patients diagnosed in the U.S.1 each year, predominantly among patients with PDAC, CRC, or NSCLC.
