encenicline (EVP-6124) - Forum Pharmaceuticals, Mitsubishi Tanabe
EnVivo confirms EVP-6124 mechanism of action (Drug Discovery & Development) - Jan 10, 2012 - EnVivo has demonstrated that EVP-6124 is a potent & highly selective agonist of alpha-7 neuronal nicotinic acetylcholine receptors in brain & treatment with EVP-6124, both alone& in combination with donepezil, restored memory loss & improved memory function in preclinical models; The company expects to report data from a multicenter, multinational, double-blind, placebo-controlled P2b study of EVP-6124 in Alzheimer's disease in H1 2012 
Anticipated P2b data • MOA Alzheimer's Disease • Schizophrenia
http://www.dddmag.com/EnVivo-Confirms-EVP-6124-Mechanism-of-Action-1-10-12.aspx
 
Jan 10, 2012
 
EnVivo Pharmaceuticals announced data confirming the novel mechanism of action of its lead program EVP-6124.  EVP-6124 is a partial agonist and 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 shows 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. 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. The findings 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,” says Gerhard Koenig, PhD, 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.” EnVivo announced topline Phase 2b clinical data and a comprehensive data analysis of EVP-6124 in schizophrenia. 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.