Novel Nicotinic Alpha-7 Agonist Shown to be Selective and Potent;
Demonstrates Ability to Improve and Restore Memory in Preclinical Models
WATERTOWN, Mass.--(BUSINESS WIRE)-- EnVivo Pharmaceuticals, a company dedicated to developing a broad range of novel central nervous system (CNS) therapies, today announced data published in the peer-reviewed journal Neuropharmacology confirming the novel mechanism of action of its lead program EVP-6124. EnVivo has demonstrated that EVP-6124 is a potent and highly selective agonist of alpha-7 neuronal nicotinic acetylcholine receptors (nAChRs) in the brain and that treatment with EVP-6124, both alone and in combination with donepezil, restored memory loss and improved memory function in preclinical models. These findings further support the company’s clinical development strategy for EVP-6124 as a long-term treatment to restore and improve cognitive function with sustained effect in schizophrenia and Alzheimer’s disease.
“This research increases our understanding of how EVP-6124 enhances synaptic transmission in the brain and acts as a co-agonist in combination with the body’s own natural acetylcholine response to enhance cognition,” said Gerhard Koenig, Ph.D., senior vice president, research and chief scientific officer of EnVivo Pharmaceuticals. “These preclinical data also underscore the recent progress we have made with EVP-6124, including positive Phase 2b data in schizophrenia, and we look forward to reporting our Phase 2b Alzheimer’s data in the first half of 2012.”
The publication details EVP-6124 as a partial agonist and outlines how its co-agonism mechanism at much lower doses may lead to a more desirable side effect profile than classical approaches, which dictate that a drug be dosed to full agonist concentrations. The data outlined in the publication show that when used in combination, sub-efficacious doses of EVP-6124 and the currently approved acetylcholinesterase inhibitor (AChE-I) donepezil reversed memory loss or deficit in a preclinical model. This approach could not only improve the safety profile of current treatments, but also could minimize undesired interactions with other receptors and identify new combination therapies that utilize lower than typically prescribed doses of AChE-Is.
The paper, titled “EVP-6124, a novel and selective a7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of a7 nicotinic acetylcholine receptors,” is available online at http://www.sciencedirect.com/science/article/pii/S0028390811004795 and will appear in the February 2012 issue of Neuropharmacology (DOI: 10.1016/j.neuropharm.2011.10.024).
EnVivo recently announced topline Phase 2b clinical data and a comprehensive data analysis of EVP-6124 in schizophrenia, which were presented at the American College of Neuropsychopharmacology (ACNP) annual meeting. The results demonstrated EVP-6124’s statistically significant and clinically meaningful effects on both cognition and functional symptoms, including global cognitive function. The company expects to report data from a multicenter, multinational, double-blind, placebo-controlled Phase 2b study of EVP-6124 in Alzheimer’s disease in the first half of 2012.
About EnVivo Pharmaceuticals
EnVivo Pharmaceuticals, Inc. and its subsidiaries (“EnVivo Pharmaceuticals” or “EnVivo”) are dedicated to discovering and developing small molecule therapeutics for disorders of the central nervous system (CNS). EnVivo Pharmaceuticals, Inc. is a biotech company located in Watertown, Mass. The company’s focus is on building an integrated company and it is working to convert its broad pipeline into a range of CNS therapies that leverage novel mechanisms of action by altering the progression of disease and providing improvement in cognitive and overall function. EnVivo’s lead product is an alpha-7 nicotinic acetylcholine receptor agonist that has successfully completed a Phase 2b clinical trial in schizophrenia and is currently in an ongoing Phase 2b clinical trial for the treatment of cognitive impairment in Alzheimer’s disease. EnVivo’s other programs include an epigenetics program based on Histone Deacetylase inhibition (HDACi) in preparation for Phase 2 studies, a Gamma Secretase Modulator program in Phase 1 and several preclinical programs, including a potent and selective PDE10 inhibitor program expected to enter the clinic in early 2012. For more information about EnVivo, visit www.envivopharma.com.
Sheryl Seapy, 949-608-0841
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