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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

Excerpt from the Press Release:

REDWOOD CITY, Calif., Sept. 22, 2022 (GLOBE NEWSWIRE) — 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.

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