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Revolution Medicines Begins Phase I Trial of KRAS G12C Inhibitor

NEW YORK – Revolution Medicines on Thursday said the first patient with a KRAS-mutated tumor has received its KRAS G12C(ON) inhibitor RMC-6291 in a Phase I/Ib trial. 

Revolution is developing a pipeline of RAS(ON) inhibitors, and RMC-6291 is a drug that specifically targets KRAS G12C-mutant cancers. The Phase I study will enroll 117 participants with advanced colorectal, pancreatic, non-small cell lung, or other solid cancers harboring such mutations. The study will assess safety and tolerability of RMC-6291 and determine the recommended Phase II dose and schedule.

Earlier this year, Revolution began evaluating RMC-6236, an inhibitor of multiple RAS variants, in a Phase I study. That trial is enrolling patients with solid tumors harboring KRAS G12A, G12D, G12R, G12S, or G12V mutations.

Revolution CEO Mark Goldsmith said in a statement that the next candidate the company expects to enter the clinic from the RAS(ON) pipeline is the KRAS G12D inhibitor RMC-9805.

"The mutant-selective approach exemplified by RMC-6291, RMC-9805, and other assets in our pipeline differs from the profile of RMC-6236, which entered clinical evaluation recently and is designed to inhibit many RAS variants rather than a single RAS mutation," Goldsmith said. "We believe that these complementary approaches, used in monotherapy or combination treatment regimens, will provide a powerful set of tools for countering the complex processes that cause and sustain a wide range of RAS-addicted cancers."

Revolution, based in Redwood City, California, has one other RAS(ON) inhibitor targeting KRAS G13C in preclinical development. The firm is also developing a pipeline of RAS companion inhibitors, including a SHP2 inhibitor in a Phase II trial, an mTORC1/4EBP1 inhibitor, and a preclinical SOS1 inhibitor.