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ADX10059 (raseglurant) is a potent and selective negative allosteric modulator (NAM) of the metabotropic glutamate receptor 5 (mGluR5). It is an orally available small molecule developed by Addex for the treatment of gastroesophageal reflux disease (GERD), migraine, and anxiety. The drug works by binding to an allosteric site on mGluR5, reducing its activation and thereby modulating physiological responses associated with glutamate signaling. This mechanism offers potential advantages over traditional antagonists due to its non-competitive inhibition. ADX10059 reached Phase IIb clinical trials for GERD and migraine prevention but was discontinued in development due to liver enzyme changes observed during studies. It also showed potential in preclinical models for Parkinson’s disease levodopa-induced dyskinesia[1][2][4][5][6][7][8].
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