Drug intelligence / Profile preview

cisapride

Development stage
Phase 4
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Oral
01

Overview

Cisapride is a gastroprokinetic agent that enhances motility in the upper gastrointestinal tract. It acts primarily as a serotonin 5-HT4 receptor agonist, stimulating the release of acetylcholine in the enteric nervous system. This leads to increased tone and amplitude of gastric contractions (especially antral), relaxation of the pyloric sphincter and duodenal bulb, and enhanced peristalsis in the duodenum and jejunum—resulting in accelerated gastric emptying and intestinal transit. Cisapride does not stimulate muscarinic or nicotinic receptors nor inhibit acetylcholinesterase activity. It was developed by Janssen Pharmaceuticals for treating symptoms such as nocturnal heartburn due to gastroesophageal reflux disease (GERD) when other treatments have failed[1][2][4][9]. Its use has been limited or withdrawn in many countries due to risks of serious cardiac side effects such as long QT syndrome[4].

Brand names
PrepulsidPropulsid
Other names
西沙必利CisapridaCisapridum
02

Targets

HTR4 (5-Hydroxytryptamine receptor 4)

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