EPICS Therapeutics announces the publication of its peer-reviewed article, “Discovery, Optimization, and Preclinical Pharmacology of EP652, a METTL3 Inhibitor with Efficacy in Liquid and Solid Tumor Models” in the highly-cited Journal of Medicinal Chemistry.
This article describes the lead optimization of a chemical series of novel METTL3 inhibitors culminating in compound “EP652”. EP652 is a potent and selective inhibitor of METTL3 with a favorable pharmacokinetic profile commensurate with its clear, dose-dependent demonstration of in vivo target engagement (m6A depletion). EP652 elicited significant tumor growth inhibition in preclinical models of liquid and solid tumors. The efficacy of EP652 provides additional evidence for the applicability of mRNA epigenetic mechanisms to the treatment of cancer and specifically advances the validation of METTL3 as a cancer target.