5-HT4 receptor agonist treatment of chronic constipation

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Abstract

Chronic constipation and irritable bowel syndrome (IBS) with constipation affect patient quality of life and are associated with a high healthcare expenditure. Conventional therapies for chronic constipation have limited effectiveness. New-generation, selective 5-HT4 receptor agonists are effective for chronic constipation, but none are currently approved in the U.S.; prucalopride is approved for the treatment of chronic constipation in Europe. The 5-HT4 receptor agonist velusetrag is being developed for chronic constipation and IBS with constipation; it has high selectivity and affinity for the 5-HT4 receptor. Velusetrag accelerates colonic transit in a dose-related manner, with a dose of 30 mg daily being the most effective over 9 days of treatment in healthy controls. In patients with chronic constipation, velusetrag increased spontaneous bowel movements after 4 weeks of therapy, with no serious cardiac events reported. Velusetrag has shown great promise, and further studies in chronic constipation and IBS with constipation are warranted.

Original languageEnglish (US)
Pages (from-to)447-454
Number of pages8
JournalDrugs of the Future
Volume36
Issue number6
DOIs
StatePublished - 2011

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ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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