title: Safety and clinical effects of EVP-6124 in subjects with Alzheimer's disease currently or previously receiving an acetylcholinesterase inhibitor medication.
abstract: Alzheimer's disease (AD) is a prevalent and currently incurable brain disease whose impact will continue to rise as the population ages. With limited treatment options, a variety of experimental therapies are currently in clinical trials. EVP-6124 (encenicline) is an α7 nicotinic acetylcholine receptor partial agonist under investigation for the symptomatic treatment of AD. EVP-6124 activates the α7 nicotinic acetylcholine receptor at low nanomolar brain concentrations and improves memory performance in rats. Treatment with EVP-6124 in Phase I and II trials involving patients with mild-to-moderate AD was well tolerated and showed statistically significant improvements compared with placebo on cognitive and functional measures. Two Phase III trials under the title COGNITIV AD will assess the efficacy and tolerability of EVP-6124 in patients with mild-to-moderate AD. Based on the completed clinical trials and proposed mechanism of action, EVP-6124 would appear to be a good candidate for therapy in combination with cholinesterase inhibitors.
authors.affiliation: St. Louis University School of Medicine, 1438 South Grand St Louis, MO 63104, USA.
authors.forename: William James
authors.initials: WJ
authors.lastname: Deardorff
authors.forename: Ahmad
authors.initials: A
authors.lastname: Shobassy
authors.forename: George T
authors.initials: GT
authors.lastname: Grossberg
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy*; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000627:therapeutic use*; D017326:Clinical Trials, Phase III as Topic; D006801:Humans; D018722:Nicotinic Agonists / Q000627:therapeutic use*; D011812:Quinuclidines / Q000737:chemistry / Q000627:therapeutic use*; D013876:Thiophenes / Q000737:chemistry / Q000627:therapeutic use*
chemical_list: C573817:7-chloro-N-quinuclidin-3-yl-benzo(b)thiophene-2-carboxamide; D002800:Cholinesterase Inhibitors; D018722:Nicotinic Agonists; D011812:Quinuclidines; D013876:Thiophenes
keywords: Alzheimer’s disease; EVP-6124; cholinergic; encenicline; α-7 nicotinic acetylcholine receptor partial agonist