First-in-class, oral, RAS(ON) Inhibitor being evaluated initially in patients with cancers driven by KRASG12 mutations

Sushil Patel, Ph.D., industry veteran with commercial oncology expertise, elected to board of directors

REDWOOD CITY, CA, USA I June 28, 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-6236, the company’s oral, potent, tri-complex RAS(ON) Inhibitor designed to treat patients with cancers driven by a variety of RAS mutations. RMC-6236, which the company refers to as a RASMULTI (ON) Inhibitor, is the first development candidate from Revolution Medicines’ portfolio of novel RAS(ON) Inhibitors to enter clinical development.

The Phase 1/1b trial (NCT05379985) is a multicenter, open-label, dose-escalation and dose-expansion study of RMC-6236 in patients with advanced solid tumors harboring selected KRASG12 mutations, including KRASG12D, KRASG12V and KRASG12R. 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. The study’s first patient has pancreatic cancer with a KRASG12D mutation, the most common genetic variant of RAS proteins causing cancer.  

“Beginning clinical evaluation of the first compound from our broad portfolio of RAS(ON) Inhibitors marks a significant milestone in our efforts to serve unmet needs of patients with RAS-addicted cancers,” said Mark A. Goldsmith, M.D., Ph.D., chief executive officer and chairman of Revolution Medicines. “To our knowledge, RMC-6236 is the first oral, direct RAS inhibitor to be deployed against a tumor harboring the KRASG12D variant, and it ushers in a wave of groundbreaking RAS(ON) Inhibitors we expect to advance.”

Steve Kelsey, M.D., president, research and development at Revolution Medicines said, “RMC-6236 is a compelling drug candidate with the potential to demonstrate broad utility across many RAS cancer variants, particularly those harboring KRASG12 mutations. We are enthusiastic about its potential both to display first-in-class single agent activity as an inhibitor of mutant RAS and to be deployed as a RAS Companion Inhibitor in combination with mutant-selective RAS(ON) Inhibitors we have in development.”

The company also highlights the election of Sushil Patel, Ph.D., to its board of directors at its recent annual meeting of stockholders. Dr. Patel has more than twenty years of experience in the biotech industry, focused on commercialization strategy and execution in U.S. and global oncology markets. He currently serves as chief commercial officer of Replimune Group, a clinical-stage biotechnology company developing novel tumor-directed oncolytic immunotherapies. Previously, Dr. Patel held various positions at Genentech, Inc., where he served as franchise head for lung, skin, and rare cancers that included several blockbuster products in both targeted therapies and immuno-oncology. Notably, he led lifecycle management of Tecentriq® (atezolizumab) in lung cancer and helped lead more than eight product launches across more than twenty different indications. Dr. Patel holds a Ph.D. in molecular biology from the University of London and a Master’s degree in biotechnology from the Imperial College London.

Dr. Goldsmith added, “We are very fortunate to have Sushil join our board of directors. His commercial expertise in bringing innovative cancer drugs to patients will provide a valuable perspective as we advance our deep product pipeline.”

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) Inhibitor RMC-6236 (RASMULTI) is in clinical development. Additional RAS(ON) Inhibitors in development include RMC-6291(KRASG12C), 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