Abstract
After the problems associated with the non-selective 5-HT4 receptor agonists cisapride and tegaserod, the 5-HT4 receptor is now beginning to come in from the cold. Thus, prucalopride is now the first of a new class of drug defined by selectivity and high intrinsic activity at the 5-HT4 receptor. Prucalopride has been developed for treatment of chronic constipation rather than constipation-predominant irritable bowel syndrome (IBS). This follows the trend of first evaluating new gastrointestinal (GI) prokinetic drugs in disorders where disrupted GI motility is known to exist, rather than in a functional bowel disorder where changes in motility are uncertain. If prucalopride is not progressed towards the IBS indication, it has at least shown the way for other selective 5-HT4 receptor agonists. Most notable among these is TD-5108 (velusetrag), also characterized by good selectivity at the 5-HT4 receptor, high intrinsic activity and efficacy in patients with chronic constipation.
Original language | English |
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Title of host publication | Clinical Medicine Insights: Gastroenterology |
Pages | 21-33 |
Number of pages | 13 |
Volume | 3 |
DOIs | |
State | Published - Dec 1 2010 |
Keywords
- 5-HT
- Constipation
- IBS
- Prucalopride
ASJC Scopus subject areas
- Gastroenterology