E-52862

E-52862 is a potent and highly selective small molecule antagonist of the sigma-1 receptor (S1R), developed by Esteve for the treatment of neuropathic pain and as an adjunct to enhance opioid analgesia. It demonstrates high selectivity for sigma-1 over sigma-2 receptors and other targets (Ki = 17 nM). Preclinical studies show efficacy in relieving neuropathic pain and improving negative emotional states associated with pain. In animal models, it crosses the blood–brain barrier and binds to central nervous system S1R sites. Phase I clinical trials established favorable safety, tolerability, pharmacokinetics compatible with once-daily oral dosing; Phase II trials have evaluated its efficacy in chronic postsurgical pain and painful diabetic neuropathy. The drug is considered first-in-class as a selective sigma-1 receptor antagonist evaluated in humans for these indications[1][4][5][6].

Other names

E-52862.HClE52862.HClE 52862.HCl