Revolution Medicines Doses First Patient in Phase 1/1b Clinical Trial of RMC-6291, Company’s First Mutant-Selective RAS(ON) Inhibitor

KRASG12C(ON) Inhibitor with highly differentiated mechanism of action being evaluated in patients with cancers harboring KRASG12C mutation

RMC-6291 is first mutant-selective RAS(ON) Inhibitor to enter clinic, following closely behind company’s RASMULTI(ON) Inhibitor, RMC-6236

REDWOOD CITY, CA, USA I September 22, 2022 I Revolution Medicines, Inc. (Nasdaq: RVMD), a clinical-stage oncology company developing targeted therapies for RAS-addicted cancers, today announced the first patient was dosed in its Phase 1/1b monotherapy clinical trial of RMC-6291, an oral, selective, covalent KRASG12C(ON) Inhibitor designed to treat patients with cancers driven by the KRASG12C mutation. RMC-6291, which exhibits a potential best-in-class preclinical profile, is the first drug candidate from the company’s pipeline of mutant-selective RAS(ON) Inhibitors to enter the clinic. Last quarter, Revolution Medicines initiated clinical development of RMC-6236, its oral RASMULTI(ON) Inhibitor designed to treat patients with cancers driven by a variety of RAS mutations.

The Phase 1/1b trial (NCT05462717) sponsored by Revolution Medicines is a multicenter, open-label, dose-escalation and dose-expansion study of RMC-6291 in patients with advanced solid tumors harboring the KRASG12C mutation. The primary objectives of the study are to evaluate safety and tolerability and to inform the recommended Phase 2 dose and schedule (RP2DS) for the compound.

“RMC-6291 is an exciting first drug candidate from our collection of oral, mutant-selective RAS(ON) Inhibitors to advance into clinical development, and we expect learnings from this trial will also inform advancement of our pipeline of innovative compounds. The next mutant-selective RAS(ON) inhibitor we plan to advance into the clinic is RMC-9805, an oral and covalent inhibitor of KRASG12D, the most common mutant RAS driver of human cancers,” said Mark A. Goldsmith, M.D., Ph.D., chief executive officer and chairman of Revolution Medicines. “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. We believe that these complementary approaches, used in monotherapy and/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.”

About Revolution Medicines, Inc.
Revolution Medicines is a clinical-stage oncology company developing novel targeted therapies for RAS-addicted cancers. The company’s R&D pipeline comprises RAS(ON) Inhibitors designed to suppress diverse oncogenic variants of RAS proteins, and RAS Companion Inhibitors for use in combination treatment strategies. The company’s RAS(ON) Inhibitors RMC-6236 (RASMULTI) and RMC-6291(KRASG12C) are in clinical development. Additional RAS(ON) Inhibitors in development include RMC-9805 (KRASG12D) and RMC-8839 (KRASG13C), and a pipeline of research compounds targeting additional RAS variants. RAS Companion Inhibitors in clinical development include RMC-4630 (SHP2) and RMC-5552 (mTORC1/4EBP1).

SOURCE: Revolution Medicines

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