Presentation at 2nd Annual RAS-Targeted Drug Development Conference Highlights First Publicly Reported Data for Inhibitors of Notorious Cancer Protein KRASG12D(ON)
REDWOOD CITY, CA, USA I September 16, 2020 I Revolution Medicines, Inc. (Nasdaq: RVMD), a clinical-stage precision oncology company focused on developing targeted therapies to inhibit frontier targets in RAS-addicted cancers, today reported data demonstrating that its first-in-class KRASG12D(ON) inhibitors induced tumor regressions in a preclinical model of human pancreatic cancer carrying an oncogenic KRASG12D mutation. This first public disclosure of results showing anti-tumor activity for potent inhibitors of the notorious KRASG12D(ON) cancer protein was made by Steve Kelsey, M.D., president of research and development, in a presentation entitled “Approaches to Inhibiting RAS Driven Tumors Beyond KRASG12C” at the 2nd Annual RAS-Targeted Drug Development Conference.
Revolution Medicines uses its proprietary tri-complex technology platform to create innovative compounds designed to inhibit the active, GTP-bound form of RAS, or RAS(ON), proteins. The company previously reported representative preclinical profiles of its potent inhibitors of another common cancer driver, KRASG12C(ON). The newly presented data demonstrated that its KRASG12D(ON) inhibitors induced significant decreases in tumor volume in a xenograft model of human pancreatic cancer driven by a KRASG12D mutation. This anti-tumor activity was observed across multiple dose levels, and all dose levels were well tolerated. The KRASG12D(ON) program is currently in lead optimization.
The KRASG12D genotype is of particularly high clinical interest as there are currently no approved targeted therapies for the treatment of cancers driven by this mutation, which is found in approximately 35 percent of pancreatic cancer cases and 15 percent of colorectal cancers in the U.S. The company continues its efforts to discover and develop inhibitors of multiple oncogenic mutants of RAS proteins, which in aggregate are believed to drive approximately 30% of all human cancers in the U.S. Earlier in 2020 the company named KRASG12C, KRASG12D, KRASG13C and NRASG12C as its four initial priority RAS(ON) targets.
“It is gratifying for our R&D organization to present this exciting demonstration of preclinical anti-cancer activity of compounds targeting the oncogenic KRASG12D(ON) protein. Advancement of our KRASG12D(ON) inhibitor program into the lead optimization stage represents an important corporate milestone, and highlights the substantial progress that we continue to make across our broad-based mutant RAS(ON) inhibitor effort,” said Mark A. Goldsmith, M.D., Ph.D., chief executive officer and chairman of Revolution Medicines. “We believe that targeted inhibitors directed to mutant forms of RAS that drive various cancers, and in particular the RAS(ON) form of these proteins, represent a potential therapeutic strategy for serving important unmet needs on behalf of patients battling RAS-driven cancers.”
About Revolution Medicines, Inc.
Revolution Medicines is a clinical-stage precision oncology company focused on developing novel targeted therapies to inhibit high-value frontier targets in RAS-addicted cancers. The company possesses sophisticated structure-based drug discovery capabilities built upon deep chemical biology and cancer pharmacology know-how and innovative, proprietary technologies that enable the creation of small molecules tailored to unconventional binding sites.
The company’s R&D pipeline includes RMC-4630, a clinical-stage investigational drug that is designed to selectively inhibit the activity of SHP2, an upstream node in RAS signaling. Preclinical programs include inhibitors of multiple mutant RAS proteins and SOS1. RMC-5552, currently in IND-enabling development, is designed for use against tumors featuring mTORC1 activation, including certain RAS-addicted cancers.
SOURCE: Revoluation Medicines
Post Views: 66
Presentation at 2nd Annual RAS-Targeted Drug Development Conference Highlights First Publicly Reported Data for Inhibitors of Notorious Cancer Protein KRASG12D(ON)
REDWOOD CITY, CA, USA I September 16, 2020 I Revolution Medicines, Inc. (Nasdaq: RVMD), a clinical-stage precision oncology company focused on developing targeted therapies to inhibit frontier targets in RAS-addicted cancers, today reported data demonstrating that its first-in-class KRASG12D(ON) inhibitors induced tumor regressions in a preclinical model of human pancreatic cancer carrying an oncogenic KRASG12D mutation. This first public disclosure of results showing anti-tumor activity for potent inhibitors of the notorious KRASG12D(ON) cancer protein was made by Steve Kelsey, M.D., president of research and development, in a presentation entitled “Approaches to Inhibiting RAS Driven Tumors Beyond KRASG12C” at the 2nd Annual RAS-Targeted Drug Development Conference.
Revolution Medicines uses its proprietary tri-complex technology platform to create innovative compounds designed to inhibit the active, GTP-bound form of RAS, or RAS(ON), proteins. The company previously reported representative preclinical profiles of its potent inhibitors of another common cancer driver, KRASG12C(ON). The newly presented data demonstrated that its KRASG12D(ON) inhibitors induced significant decreases in tumor volume in a xenograft model of human pancreatic cancer driven by a KRASG12D mutation. This anti-tumor activity was observed across multiple dose levels, and all dose levels were well tolerated. The KRASG12D(ON) program is currently in lead optimization.
The KRASG12D genotype is of particularly high clinical interest as there are currently no approved targeted therapies for the treatment of cancers driven by this mutation, which is found in approximately 35 percent of pancreatic cancer cases and 15 percent of colorectal cancers in the U.S. The company continues its efforts to discover and develop inhibitors of multiple oncogenic mutants of RAS proteins, which in aggregate are believed to drive approximately 30% of all human cancers in the U.S. Earlier in 2020 the company named KRASG12C, KRASG12D, KRASG13C and NRASG12C as its four initial priority RAS(ON) targets.
“It is gratifying for our R&D organization to present this exciting demonstration of preclinical anti-cancer activity of compounds targeting the oncogenic KRASG12D(ON) protein. Advancement of our KRASG12D(ON) inhibitor program into the lead optimization stage represents an important corporate milestone, and highlights the substantial progress that we continue to make across our broad-based mutant RAS(ON) inhibitor effort,” said Mark A. Goldsmith, M.D., Ph.D., chief executive officer and chairman of Revolution Medicines. “We believe that targeted inhibitors directed to mutant forms of RAS that drive various cancers, and in particular the RAS(ON) form of these proteins, represent a potential therapeutic strategy for serving important unmet needs on behalf of patients battling RAS-driven cancers.”
About Revolution Medicines, Inc.
Revolution Medicines is a clinical-stage precision oncology company focused on developing novel targeted therapies to inhibit high-value frontier targets in RAS-addicted cancers. The company possesses sophisticated structure-based drug discovery capabilities built upon deep chemical biology and cancer pharmacology know-how and innovative, proprietary technologies that enable the creation of small molecules tailored to unconventional binding sites.
The company’s R&D pipeline includes RMC-4630, a clinical-stage investigational drug that is designed to selectively inhibit the activity of SHP2, an upstream node in RAS signaling. Preclinical programs include inhibitors of multiple mutant RAS proteins and SOS1. RMC-5552, currently in IND-enabling development, is designed for use against tumors featuring mTORC1 activation, including certain RAS-addicted cancers.
SOURCE: Revoluation Medicines
Post Views: 66
