Disease relevance of Lubiprostone

• Significantly greater improvements occurred with lubiprostone than placebo in the degree of straining, stool consistency and constipation severity (where reported) in both pivotal studies (p < 0.05 for all comparisons at all timepoints) [1].

High impact information on Lubiprostone

• Lubiprostone (Amitiza) is an oral bicyclic fatty acid that selectively activates type 2 chloride channels in the apical membrane of the gastrointestinal epithelium, resulting in increased fluid secretion [1].
• Effect of a selective chloride channel activator, lubiprostone, on gastrointestinal transit, gastric sensory, and motor functions in healthy volunteers [2].
• Thus the ClC-2 activator lubiprostone accelerates small intestinal and colonic transit, which confers potential in the treatment of constipation [2].
• Lubiprostone accelerated small bowel and colonic transit, increased fasting gastric volume, and retarded gastric emptying [2].
• If empirical treatment of patients with chronic constipation fails, osmotic laxatives (e.g. lactulose and polyethylene glycol), a serotonin (5-HT4) receptor agonist (e.g. tegaserod) or a chloride channel activator (e.g. lubiprostone) can be considered [3].

Chemical compound and disease context of Lubiprostone

• Use of tegaserod and the recently approved lubiprostone is supported by high-quality evidence, and these agents have acceptable safety profiles in patients with chronic constipation [3].

Anatomical context of Lubiprostone

• Lubiprostone, a selective type 2 chloride channel (ClC-2) activator, induces intestinal secretion and has been shown to relieve constipation in clinical trials; however, the effects of lubiprostone on gastric function and whole gut transit in humans are unclear [2].
• Lubiprostone is a bicyclic fatty acid that acts locally on ClC-2 channels located in the apical membrane of intestinal epithelial cells [4].

Gene context of Lubiprostone

• Our aim was to compare the effects of the selective ClC-2 activator lubiprostone on maximum tolerated volume (MTV) of a meal, postprandial symptoms, gastric volumes, and gastrointestinal and colonic transit in humans [2].

Analytical, diagnostic and therapeutic context of Lubiprostone

• Lubiprostone was generally well tolerated in clinical trials with no reports of treatment-related serious adverse events in pivotal trials [1].

References