Addex Dipraglurant Demonstrates Anxiolytic- and Antidepressant-like Activity in Multiple Preclinical Models Relevant for Non-Motor Symptoms in Parkinson's Disease

Aug.14, 2015

Addex Therapeutics a leading company pioneering allosteric modulation-based drug discovery and development announced today that its lead compound dipraglurant, a metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator (NAM) demonstrated robust efficacy in multiple preclinical models of anxiety and depression. 

The studies were conducted in collaboration with the laboratory of Professor Andrzej Pilc of the department of Neurobiology, Institute of Pharmacology at the Polish Academy of Sciences in Krakow, Poland. 

Dipraglurant is a novel small molecule inhibitor of the metabotropic glutamate receptor 5 (mGluR5) that has successfully completed Phase II proof-of-concept testing in Parkinson's disease (PD) patients suffering from debilitating levodopa-induced dyskinesia (LID). Dipraglurant given orally showed anxiolytic effects in the elevated plus maze test (EPM) and the stress-induced hyperthermia test (SIH) in mice at the dose of 50 mg/kg, and antidepressant effects in the forced swim test (FST) in rats (at doses of 10 and 30 mg/kg) and mice (at doses of 30 and 50 mg/kg) . 

These data will be presented at the XIX International Congress of the Polish Pharmacological Society, 17-19 September 2015 being held in Swinoujscie, Poland. "The consistent effects across a battery of different preclinical models provides further evidence that excessive glutamate activity mediated through mGluR5 can contribute to the development of anxiety and depression symptoms" commented Professor Andrzej Pilc of the department of Neurobiology, Institute of Pharmacology, Polish Academy of Sciences, Krakow, Poland. "There remains a significant unmet medical need for medications to treat the full range of motor and non-motor complications of PD" said Sonia Poli, CSO at Addex, "dipraglurant may represent an attractive approach to treat not only levodopa induced dyskinesia, but also the concomitant non-motor symptoms which are present in almost all PD patients and can have a greater negative impact on the quality of life than motor complications. "The collaboration with Prof. Pilc, a world leader in fundamental research on mGlu receptors is a further demonstration of our strategy to drive forward our research in collaboration with leading academic institutions." said Tim Dyer, CEO at Addex. "While we continue to prioritize the development of dipraglurant for Parkinson's disease levodopa induced dyskinesia and dystonia, these data provide evidence of additional utility for dipraglurant in PD patients." 

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