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Revexepride (SSP-002358, SPD-557) is a potent and highly selective 5-HT4 (5-hydroxytryptamine receptor 4) receptor agonist developed by Shire (now Takeda). It was investigated as an add-on therapy to standard proton pump inhibitor (PPI) treatment for patients with gastroesophageal reflux disease (GERD) who continued to experience persistent symptoms, particularly regurgitation, despite acid suppression therapy. The combination aimed to address underlying motility dysfunction by stimulating gastrointestinal motility via the 5-HT4 receptor. While evaluated in Phase 2b clinical trials, revexepride failed to demonstrate superior efficacy over placebo in reducing persistent GERD symptoms and development was subsequently halted.
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