mGluR2 NAM

Preclinical data suggest that mGluR2 inhibition may have potential for the treatment of Alzheimer's disease and depression. Addex is optimizing multiple series of mGluR2 NAM. This program is available for partnering.

Data from Addex and others show that mGluR2 inhibition can reverse cognitive deficit. Preclinical research from other groups suggest not only that mGluR2 NAM might slow the progression* of Alzheimer’s, an effect not seen with any marketed drug, but also that it may have a synergistic effect on cognition** when combined with donepezil. Alzheimer’s disease represents a large and growing market with unmet medical need. None of the currently marketed drugs for Alzheimer’s disease offers patients sustained life-changing benefits.

Most recently, an Addex mGluR2 NAM was tested in a model that mimics aspects of the pathophysiology and cognitive impairment, including the progressive memory impairment, observed in human Alzheimer’s disease. In the preclinical study, the mGluR2 NAM dose-dependently reversed memory deficit exhibited after beta-amyloid protein administration. Working memory impairment was measured using the novel object recognition (NOR) test. The statistically significant effect of the mGluR2 NAM was similar to the active comparator used in the same experiment, donepezil (Aricept), the benchmark marketed drug currently used to treat symptoms of Alzheimer’s disease. Furthermore, the mGluR2 NAM did not change locomotor activity compared to vehicle.

* The Journal of Neuroscience, March 17, 2010; 30(11):3870-3875
** Bioorganic & Medicinal Chemistry Letters, Dec 1, 2010; 20(23):6969-6974