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Renzapride is an orally bioavailable, substituted benzamide small molecule that acts as a gastrointestinal prokinetic and antiemetic agent. Its mechanism of action involves full agonism at the serotonin 5-HT4 receptor and partial antagonism at the serotonin 5-HT3 receptor, with additional antagonistic activity at the 5-HT2B receptor and some affinity for the 5-HT2A and 5-HT2C receptors. Renzapride accelerates gastrointestinal transit and motility, making it a candidate for treating constipation-predominant irritable bowel syndrome (IBS-C) as well as other GI motility disorders. Originally developed by GlaxoSmithKline, it has since been further developed by Alizyme, Atlantic Healthcare, and Ambrose Healthcare. As of early 2025, its primary focus is on management of gastrointestinal motility in patients with cystic fibrosis[1][3][4][6][7].
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