Renzapride

Renzapride

Renzapride is a gastroprokinetic agent and antiemetic which was developed by Alizyme plc but is no longer being actively pursued. It acts as a 5-HT4 receptor agonist and 5-HT3 receptor antagonist. The compound was under investigation for the treatment of gastrointestinal disorders such as gastroesophageal reflux disease (GERD) and irritable bowel syndrome (IBS).

Pharmacology

Renzapride is a serotonin receptor modulator, with a high affinity for the 5-HT4 and 5-HT3 receptors. It acts as an agonist at the 5-HT4 receptor, which stimulates the peristalsis that moves content through the gastrointestinal tract. It also acts as an antagonist at the 5-HT3 receptor, which reduces the sensation of nausea and vomiting.

Clinical Trials

Renzapride was in Phase III clinical trials for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) in women. However, the trials did not meet their primary efficacy endpoint and development was discontinued.

Side Effects

The most common side effects reported in clinical trials were headache, nausea, and diarrhea. Serious side effects were rare, but included cardiac arrhythmia and hypersensitivity reactions.

History

Renzapride was developed by the British biopharmaceutical company Alizyme plc. The compound entered clinical trials in the early 2000s, but development was halted after Phase III trials failed to meet their primary endpoint.

See Also

• 5-HT4 receptor
• 5-HT3 receptor
• Gastroprokinetic agent
• Antiemetic
• Gastroesophageal reflux disease
• Irritable bowel syndrome

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