Navigation Links
EnVivo Pharmaceuticals Research Shows EVP-6124 Acts as Acetylcholine Co-Agonist

WATERTOWN, Mass., Nov. 5, 2010 /PRNewswire/ -- EnVivo Pharmaceuticals today announced it has discovered that EVP-6124, its alpha-7 nicotinic acetylcholine receptor agonist, possesses a novel mechanism not previously seen in the scientific community: it acts as a co-agonist with Acetylcholine (ACh) to enhance cognition.

By acting as a co-agonist and sensitizing the alpha-7 receptor, EVP-6124 makes it possible for smaller amounts of naturally occurring ACh, typically found in individuals with memory disorders such as Alzheimer's, to be required to activate the receptor.  In this scenario, EnVivo's research demonstrated that memory deficits can be minimized or entirely reversed by controlling the neuronal channel with EVP-6124 alone or in combination with other Alzheimer's drugs.

"This is groundbreaking research in terms of understanding how the alpha-7 receptor operates in conjunction with EVP-6124," said Kees Been, president and CEO of EnVivo.  "The potential, as evidenced in our studies, is significant for how we look at and approach the treatment of Alzheimer's disease."

EnVivo simulated physiologically relevant brain conditions in vitro and alpha-7 receptor action was measured in response to ACh in the presence of low EVP-6124 concentrations.  At drug concentrations resulting in pro-cognitive effects in in vivo studies, EVP-6124 appeared to significantly increase the alpha-7 receptor response to ACh.  This suggests that at low concentrations, EVP-6124 acts as a co-agonist and sensitizes the alpha-7 receptor to its natural response to ACh, but does not desensitize the receptor.  This co-agonist mechanism of action was supported by testing the combined effect of sub-threshold doses of both EVP-6124 and donepezil (Aricept) on the memory deficit in a rat model.  While each drug alone at these very low doses had no effect on reversing the deficit, dosing the two agents together completely restored the memory function in these animals.

"Low doses of EVP-6124 could enhance current cholinergic treatments and when combined with available agents could provide a pro-cognitive effect for as long as acetylcholine is present in the brain," said Dr. Jeff Cummings, director of the Cleveland Clinic Lou Ruvo Center for Brain Health (Las Vegas, Nevada and Cleveland, Ohio).  "EnVivo's experimental results suggest that pro-cognitive drugs could be taken in earlier stages of Alzheimer's disease and that EVP-6124 could continue to boost the pro-cognitive effect of cholinesterase inhibitors throughout the disease course.  The effectiveness of reduced doses of cholinesterase inhibitors when given with EVP-6124 in experimental models suggests that EVP-6124 might allow use of lower doses with fewer side effects in humans."

The results of EnVivo's ongoing Phase IIb trial, expected in the second half of 2011, will hopefully further corroborate EnVivo's most recent findings.

About EnVivo Pharmaceuticals

EnVivo Pharmaceuticals, located in Watertown, Mass., is a biopharmaceutical company dedicated to discovering and developing small molecule therapeutics for disorders of the central nervous system, with a current focus on Alzheimer's disease, cognitive disorders and schizophrenia.  The company's lead product is an alpha-7 nicotinic acetylcholine receptor agonist and is currently in Phase IIb clinical trials for cognition disorders in Alzheimer's disease and schizophrenia.  The company's other programs include an epigenetics program based on Histone Deacetylase inhibition (HDACi) with EVP-0334 as the lead molecule which is in preparation for Phase II studies, and several preclinical programs such as a Gamma Secretase Modulator (for Alzheimer's disease) and a PDE10 inhibitor program (for schizophrenia), expected to enter the clinic in 2011.  For more information about EnVivo, visit

SOURCE EnVivo Pharmaceuticals
Copyright©2010 PR Newswire.
All rights reserved

Related medicine technology :

1. EnVivo Pharmaceuticals Announces Significant Results from GSM Transgenic Mouse Model for Alzheimers Disease
2. EnVivo Pharmaceuticals Announces Initiation of Clinical Safety and Biomarker Study of Alpha-7 Nicotinic Agonist, EVP-6124, in Patients with Schizophrenia
3. EnVivo Pharmaceuticals Announces Progress on Major Drug Programs Focusing on Alzheimers, Schizophrenia and Huntingtons Diseases
4. Cadence Pharmaceuticals Reports Third Quarter 2010 Financial Results
5. Neuraltus Pharmaceuticals Awarded $733,437 Under the Qualifying Therapeutic Discovery Projects Grant Program (QTDP)
6. Inspiration Biopharmaceuticals Awarded Two Grants Under the Qualifying Therapeutic Discovery Projects Grant Program (QTDP)
7. Savient Pharmaceuticals Announces Expected Availability of KRYSTEXXA™ for Prescription and Reports Third Quarter 2010 Financial Results
8. Penwest Pharmaceuticals Shareholders Approve Merger With Subsidiary of Endo Pharmaceuticals
9. Arena Pharmaceuticals Provides Update on GPR119 Portfolio for Type 2 Diabetes
10. Keryx Biopharmaceuticals, Inc. Announces Third Quarter 2010 Financial Results
11. Onyx Pharmaceuticals to Present at the Credit Suisse 2010 Healthcare Conference
Post Your Comments:
(Date:11/30/2015)... REHOVOT, Israel , Nov. 30, 2015 ... focused on acquiring and developing innovative therapies for ear, ... of Keith A. Katkin as chairman of ... Flesher , chief executive officer for OticPharma, Ltd.  "Keith ... As chairman, he will be able to share this ...
(Date:11/29/2015)...  Strengthening its leadership in connected healthcare informatics, ... IntelliSpace Portal 8.0 , the latest edition of ... helps radiologists detect, diagnose and follow-up on treatment of ... North America Annual Meeting (RSNA) in ... the changing demands in radiology that result from an ...
(Date:11/29/2015)... GE Health Cloud 1 was unveiled today at the ... America (RSNA) meeting in Chicago ... ecosystem and its applications will connect radiologists and clinicians to ... – both inside and outside the hospital setting. ... the digital industrial leader, we are betting big on the ...
Breaking Medicine Technology:
(Date:11/30/2015)... ... November 30, 2015 , ... Newly reviewed and approved “NJ ... graduated from Tufts School of Dental Medicine in 1935. His father graduated from ... family being in dentistry as well as their commitment and passion to the Practice ...
(Date:11/30/2015)... ... November 30, 2015 , ... The ... National Poison Data System (NPDS) reveals that in 2014, someone called a poison ... over two million of which were human exposure cases. , The American Association ...
(Date:11/30/2015)... ... , ... Two years ago, Debbie Gregory, the CEO of, found herself ... Meditation (TM). After encouraging a number of veterans to go through the program, ... the talk. , TM is becoming one of the best alternative treatments for Post-Traumatic ...
(Date:11/30/2015)... ... ... The American Society for Clinical Pathology (ASCP) announced today that it has launched ... ASCP shared its “Give a minute. Get tested. Find a cure.” icon and infographic ... tested for HIV. , ASCP has asked members to replace their Facebook, Twitter, or ...
(Date:11/30/2015)... Beach, FL (PRWEB) , ... November 30, 2015 ... ... of Consumer Reports magazine, quoted Michael Hansen, Ph.D., a senior scientist at Consumer ... and even more so for a child’s exposure limits. , The original Nov ...
Breaking Medicine News(10 mins):