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Pumosetrag is an orally available small molecule drug developed as a selective partial agonist of the serotonin 5-HT3 receptor. It was investigated primarily for the treatment of irritable bowel syndrome with constipation (IBS-C) and gastroesophageal reflux disease (GERD), including nocturnal GERD. Pumosetrag acts as a prokinetic agent by modulating gastrointestinal motility—delaying liquid gastric emptying through proximal stomach relaxation and enhancing fasting antroduodenal migrating motor complex activity, while also speeding up small intestinal transit. Its mechanism is mediated by partial agonism at the 5-HT3 receptor, with species-specific differences in efficacy observed in preclinical studies. Clinical trials reached up to phase III for IBS and phase II for GERD; however, development has been discontinued[2][3][4][6].
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