Revolution Medicines announced publication of a manuscript in the Journal of Medicinal Chemistry that details the discovery efforts leading to RMC-5552, the company’s first-in-class, bi-steric mTORC1-selective inhibitor. The manuscript describes the unprecedented compound profile that includes 40-fold selectivity for mTORC1 over mTORC2 and greater than 53-fold selectivity over other lipid kinases. The paper also shows that selective mTORC1 inhibition using the company’s related preclinical tool compound in combination with a covalent KRASG12C inhibitor induced tumor regressions in a preclinical model of KRASG12C mutant non-small cell lung cancer that exhibits resistance to KRASG12C inhibitor monotherapy. "The Journal of Medicinal Chemistry manuscript details the sophisticated structure-based chemical design and synthesis employed by our drug discovery team that produced RMC-5552," said Steve Kelsey, M.D., president, research and development at Revolution Medicines. "The differentiated antitumor and tolerability profile of RMC-5552 in the preclinical setting compared to earlier mTORC inhibitors provides a strong rationale for evaluating it in patients with tumors that have abnormally high mTORC1 growth signaling, including in combination with our RAS Inhibitors in patients with tumors that have both RAS and mTORC1 pathway co-mutations."
Published first on TheFly
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