Literature DB >> 25495510

Safety and clinical effects of EVP-6124 in subjects with Alzheimer's disease currently or previously receiving an acetylcholinesterase inhibitor medication.

William James Deardorff1, Ahmad Shobassy, George T Grossberg.   

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.

Entities:  

Keywords:  Alzheimer’s disease; EVP-6124; cholinergic; encenicline; α-7 nicotinic acetylcholine receptor partial agonist

Mesh:

Substances:

Year:  2014        PMID: 25495510     DOI: 10.1586/14737175.2015.995639

Source DB:  PubMed          Journal:  Expert Rev Neurother        ISSN: 1473-7175            Impact factor:   4.618


  24 in total

Review 1.  The therapeutic potential of α7 nicotinic acetylcholine receptor (α7 nAChR) agonists for the treatment of the cognitive deficits associated with schizophrenia.

Authors:  Corinne Beinat; Samuel D Banister; Marco Herrera; Vivian Law; Michael Kassiou
Journal:  CNS Drugs       Date:  2015-07       Impact factor: 5.749

2.  Allosteric Modulators of the M4 Muscarinic Acetylcholine Receptor.

Authors:  Robert B Kargbo
Journal:  ACS Med Chem Lett       Date:  2017-08-29       Impact factor: 4.345

3.  Phase IIb Trial of an α7 Nicotinic Receptor Partial Agonist With and Without Nicotine Patch for Withdrawal-Associated Cognitive Deficits and Tobacco Abstinence.

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Journal:  J Clin Psychopharmacol       Date:  2018-08       Impact factor: 3.153

4.  Quantitative assessment of oligomeric amyloid β peptide binding to α7 nicotinic receptor.

Authors:  Erika Cecon; Julie Dam; Marine Luka; Clément Gautier; Anne-Marie Chollet; Philippe Delagrange; Laurence Danober; Ralf Jockers
Journal:  Br J Pharmacol       Date:  2019-05-20       Impact factor: 8.739

Review 5.  Nicotinic ligands as multifunctional agents for the treatment of neuropsychiatric disorders.

Authors:  Alvin V Terry; Patrick M Callahan; Caterina M Hernandez
Journal:  Biochem Pharmacol       Date:  2015-07-29       Impact factor: 5.858

6.  Aged rhesus monkeys: Cognitive performance categorizations and preclinical drug testing.

Authors:  Marc R Plagenhoef; Patrick M Callahan; Wayne D Beck; David T Blake; Alvin V Terry
Journal:  Neuropharmacology       Date:  2021-02-06       Impact factor: 5.250

Review 7.  Recent advances on drug development and emerging therapeutic agents for Alzheimer's disease.

Authors:  Teeba Athar; K Al Balushi; Shah Alam Khan
Journal:  Mol Biol Rep       Date:  2021-06-28       Impact factor: 2.316

Review 8.  Drug Development in Alzheimer's Disease: The Contribution of PET and SPECT.

Authors:  Lieven D Declercq; Rik Vandenberghe; Koen Van Laere; Alfons Verbruggen; Guy Bormans
Journal:  Front Pharmacol       Date:  2016-03-31       Impact factor: 5.810

9.  The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia.

Authors:  Linda J Bristow; Amy E Easton; Yu-Wen Li; Digavalli V Sivarao; Regina Lidge; Kelli M Jones; Debra Post-Munson; Christopher Daly; Nicholas J Lodge; Lizbeth Gallagher; Thaddeus Molski; Richard Pieschl; Ping Chen; Adam Hendricson; Ryan Westphal; James Cook; Christiana Iwuagwu; Daniel Morgan; Yulia Benitex; Dalton King; John E Macor; Robert Zaczek; Richard Olson
Journal:  PLoS One       Date:  2016-07-28       Impact factor: 3.240

10.  ABT-126 monotherapy in mild-to-moderate Alzheimer's dementia: randomized double-blind, placebo and active controlled adaptive trial and open-label extension.

Authors:  Laura M Gault; Robert A Lenz; Craig W Ritchie; Andreas Meier; Ahmed A Othman; Qi Tang; Scott Berry; Yili Pritchett; Weining Z Robieson
Journal:  Alzheimers Res Ther       Date:  2016-10-18       Impact factor: 6.982

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