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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
ACS chemical neuroscience molecule spotlight on Saredutant
1Vanderbilt University Medical Center, Department of Pharmacology and Vanderbilt Program in Drug Discovery, Vanderbilt University, Nashville, Tennessee 37232-6600.
Abstract:
Saredutant (SR48968), a potentially novel treatment option for major depressive disorders (MDD) and generalized anxiety disorder (GAD), is a drug from Sanofi-Aventis currently in phase III clinical trials. MDD is a common mental disorder that affects 121 million people worldwide, nearly 4% of the adult population (www.who.int/mental_health/management/depression/definition/en/). MDD continues to be one of the leading causes of disability with more than three quarters of the diagnosed cases having effective treatments available (www.who.int/mental_health/management/depression/definition/en/). However, even though MDD affects a large portion of the population, effective treatment options with low incidence of adverse events remain a major concern for the pharmaceutical industry. Adverse events (GI side effects1, weight gain, somnolence/insomnia, etc. (Demyttenaere K. (2003) Risk factors and predictors of compliance in depressionEur. Neuropshychopharm.13S69-S75)) from the typical treatments remain the major reason for premature stopping or poor compliance of treatment. New treatments to the market must bear in mind these adverse events, and the pharmaceutical industry is currently looking for drugs with new mechanisms of action and those that are better tolerated.
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