Date: 2015-09-08
Type of information: Licensing agreement
Compound: mGlu3 receptor program
Company: Pierre Fabre (France) Addex Therapeutics (Switzerland)
Therapeutic area: CNS diseases
Type agreement: licensing
Action mechanism: mGlu3 receptor is part of the metabotropic glutamate receptor family, a group of eight G protein-coupled receptors involved in modulation of glutamatergic neurotransmission. Expression of mGlu3 receptors is high in pyramidal cells in the prefrontal cortex and neocortical regions, as well as in astrocytes and oligodendrocytes. So far, industry was able to find only orthosteric compounds acting as mGlu3 receptor agonists or antagonists, but all of these compounds suffer from poor selectivity versus other mGlu receptors, and in particular versus mGlu2 receptor. Targeting the allosteric site of mGlu3 receptor provides a unique approach to find subtype selective compounds, and will allow a focused strategy to modulate specifically those pathways involving the mGlu3 receptor. In particular, scientific evidence suggests astroglial mGlu3 receptor activation leads to neuroprotection, through modulation of glutamate excitotoxicity and glutamate transport, neurotrophin production and reduction of oxidative damage, pointing to the potential utility of mGlu3 PAMs for neurodegenerative disease such as Alzheimer\'s or Parkinson\'s diseases. Blocking the receptor on the other hand appears to offer the potential to treat schizophrenia, depression or pain afflictions such as migraine. Both modes of action appear to represent novel avenues for developing therapies for central nervous system disorders.
Disease: CNS diseases
Details: * On September 8, 2015, Addex Therapeutics announced that it has granted an option to license its metabotropic glutamate receptor subtype 3 (\"mGlu3 receptor\") program to Pierre Fabre Pharmaceuticals. Using its proprietary allosteric modulator discovery platform, Addex has been able to identify unique mGlu3 receptor positive and negative allosteric modulators. These compounds, although still at an early stage, represent excellent starting points for chemical optimisation, and have a great potential to become first-in-class molecules useful for the treatment of CNS disorders involving an imbalance in mGlu3 receptor signalling. Under the terms of the agreement, Pierre Fabre will conduct chemistry, pharmacology and ADME*, while Addex will support the project with its proprietary in vitro pharmacological assay platform. Financial terms of the agreement have not been disclosed.
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