Tegaserod for the Treatment of Irritable Bowel Syndrome

Madia VN1, Messore A1, Saccoliti F1, Tudino V1, De Leo A1, De Vita D2, Bortolami M1, Scipione L1, Pindinello I1, Costi R1, Di Santo R1. Antiinflamm Antiallergy Agents Med Chem. 2019 Sep 11. doi: 10.2174/1871523018666190911121306. [Epub ahead of print]


Author information

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur - Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome. Italy.

Dipartimento di Biologia Ambientale, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome. Italy.


BACKGROUND: Tegaserod (Zelnorm®) is a 5-hydroxytryptamine (serotonin) type 4 receptor agonist for the treatment of hypomotility disorders of the lower gastrointestinal tract associated with the irritable bowel syndrome with constipation (IBS-C).

OBJECTIVE: The authors provide the reader with a better understanding on tegaserod mechanism of action, on its pharmacodynamics and pharmacokinetic properties, on safety and tolerability, with a summary of the key published clinical trials conducted in patients with IBS. Its effects on colon inflammation have also been described.

RESULTS: Tegaserod was withdrawn in 2007 due to increased risks of cardiovascular adverse effects. The manufacturer denied this, because pre-existing cardiovascular disease or risk factors were attributed to all affected patients. Thus, no causal relationship between tegaserod use and cardiovascular events was clearly shown. A matched case-control study of tegaserod-treated with untreated patients found no association between tegaserod and adverse cardiovascular outcomes. Despite its adverse effects, tegaserod resulted to be effective in treating chronic constipation in adult women aged < 65 years with IBS-C, while the safety and effectiveness of tegaserod in men with IBS-C have not been established. Tegaserod was resubmitted to the Food and Drug Administration in 2018 for use in a low-risk population. Moreover, tegaserod has also been shown to improve symptoms, enhance gastric accommodation and significantly attenuate visceral pain arising from the colon in functional dyspepsia patients. Treatment with tegaserod seems also to exert a protective effect in inflamed colons, reducing the severity of colitis in animal models.

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