It is a full agonist at 5-HT4 receptors and stimulates gut motility. It is also a partial antagonist at 5-HT3 receptors, which has the effect of reducing nausea and vomiting, symptoms experienced by many patients with impaired gut motility. This dual mode of action means renzapride has the potential to treat a variety of gastrointestinal disorders.

In clinical trials involving over 1,000 patients, renzapride has demonstrated efficacy in the upper and lower gastrointestinal tract.  These trials have shown that it can enhance gastric emptying, reduce small bowel transit time and increase colonic motility.

In development, renzapride has been found to be well tolerated. It does not demonstrate the cardiac toxicity and prolonged QT interval (the time it takes for the ventricles of the heart to contract and relax) that is exhibited by some other products with the same pharmacology.