REDWOOD CITY, Calif., Jan. 29, 2026 (GLOBE NEWSWIRE) -- Revolution Medicines, a late-stage clinical oncology company developing targeted therapies for patients with RAS-addicted cancers, today 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.
"By bringing RMC-5127 to the clinic, we are building on our well-validated RAS(ON) inhibitor approach and extending it to RAS G12V, the second most common RAS mutation driving human cancers, where there are no approved targeted treatment options," said Alan Sandler, M.D., chief development officer of Revolution Medicines. "As our fifth disclosed mutant-selective RAS(ON) inhibitor and fourth clinical-stage program, RMC-5127 broadens the RAS variant coverage of our growing portfolio and opens a suite of development opportunities aimed at improving outcomes for patients with RAS-driven cancers."
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.
About Revolution Medicines, Inc.
Revolution Medicines is a late-stage clinical oncology company developing novel targeted therapies for patients with RAS-addicted cancers. The company's R&D pipeline comprises RAS(ON) inhibitors designed to suppress diverse oncogenic variants of RAS proteins. The company's RAS(ON) inhibitors daraxonrasib (RMC-6236), a RAS(ON) multi-selective inhibitor; elironrasib (RMC-6291), a RAS(ON) G12C-selective inhibitor; zoldonrasib (RMC-9805), a RAS(ON) G12D-selective inhibitor; and RMC-5127, a RAS(ON) G12V-selective inhibitor, are currently in clinical development. Additional development opportunities in the company's pipeline focus on RAS(ON) mutant-selective inhibitors, including RMC-0708 (Q61H) and RMC-8839 (G13C). For more information, please visit www.revmed.com and follow us on LinkedIn.
Forward Looking Statements
This press release contains forward-looking statements within the meaning of the U.S. Private Securities Litigation Reform Act of 1995. Any statements in this press release that are not historical facts may be considered "forward-looking statements," including without limitation statements regarding progression of clinical studies and findings from these studies, including the safety, tolerability and antitumor activity of the company's candidates being studied and the durability of these results; dosing and enrollment in the company's clinical trials; the potential impact of RMC-5127 for patients with KRAS G12V mutations; and the ability of the company to transform outcomes for patients with RAS-driven cancers. Forward-looking statements are typically, but not always, identified by the use of words such as "may," "will," "would," "believe," "intend," "plan," "anticipate," "estimate," "expect," and other similar terminology indicating future results. Such forward-looking statements are subject to substantial risks and uncertainties that could cause the company's development programs, future results, performance or achievements to differ materially from those anticipated in the forward-looking statements. Such risks and uncertainties include without limitation risks and uncertainties inherent in the drug development process, including the company's programs' current stage of development, the process of designing and conducting preclinical and clinical trials, risks that the results of prior clinical trials may not be predictive of future clinical trials, clinical efficacy, or other future results, the regulatory approval processes, the timing of regulatory filings, the challenges associated with manufacturing drug products, the company's ability to successfully establish, protect and defend its intellectual property, other matters that could affect the sufficiency of the company's capital resources to fund operations, reliance on third parties for manufacturing and development efforts, changes in the competitive landscape, and the effects on the company's business of the global events, such as international conflicts or global pandemics. For a further description of the risks and uncertainties that could cause actual results to differ from those anticipated in these forward-looking statements, as well as risks relating to the business of Revolution Medicines in general, see Revolution Medicines' Quarterly Report on Form 10-Q filed with the Securities and Exchange Commission (the "SEC") on November 5, 2025, and its future periodic reports to be filed with the SEC. Except as required by law, Revolution Medicines undertakes no obligation to update any forward-looking statements to reflect new information, events or circumstances, or to reflect the occurrence of unanticipated events.
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1 Estimated using tumor mutation frequencies from Foundation Medicine Insights March 2022 and scaled to estimated patient numbers using cancer incidence from ACS Cancer Facts and Figures 2023
