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Addex Partner Starts First-Ever Clinical Trial of an mGluR Positive Allosteric Modulator

Novel Approach Has Potential for Treatment of Multiple CNS Disorders

25 Jun 2009 - Addex Pharmaceuticals announced that its partner Ortho-McNeil-Janssen Pharmaceuticals Inc. (OMP) has started Phase I testing of ADX71149, a metabotropic glutamate receptor 2 (mGluR2) positive allosteric modulator (PAM). This product, which has potential to treat schizophrenia, anxiety, depression and other CNS disorders, is the first PAM of any mGluR subtype to enter clinical trials. Targeting mGluR2 with a PAM is a novel approach that may offer advantages over classical drug approaches. In reaching this milestone, Addex received a €1 million payment from OMP and remains eligible for additional development milestones and royalties.
 
Allosteric modulators are a novel class drugs that exert their effects on a specific receptor by interacting with a different site than the traditional binding site used by traditional "orthosteric" drugs and the body's natural activators (i.e. endogenous ligands), glutamate in this case. Allosteric molecules afford modulation of receptors that is different than orthosteric drugs. Furthermore, Addex believes it can find specific drug-like allosteric modulators with more success than others have had with orthosteric drug discovery.
 
"We are proud to have been able, together with our partner, to discover and develop the first mGluR2 PAM to reach human beings," said Vincent Mutel, CEO of Addex. "Because activating mGluR2 has been recognized as one of the most promising strategies for treating anxiety and more recently, schizophrenia, developing an allosteric modulator, like ADX71149, specifically targeting this brain receptor has been an exciting scientific endeavor and we are looking forward to seeing how differentiated this modulatory approach will be in humans."