Ligand id: 5017

Name: linaclotide

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Summary of Clinical Use
Used to treat chronic constipation and irritable bowel syndrome (IBS) where constipation is the main symptom (IBS-C).
Mechanism Of Action and Pharmacodynamic Effects
Linaclotide mimics the action of heat-stable enterotoxins in the gut which would cause diarrhea via activation of the enzyme guanylate cyclase 2C (GUCY2C) [1]. Linaclotide activation of guanylate cyclase 2C in the luminal aspect of intestinal epithelium causes increased cGMP levels and this causes activation of the cystic fibrosis transmembrane conductance regulator (CFTR), which controls chloride ion efflux from enterocytes lining the GI tract. The result is a net efflux of water into the intestinal lumen which softens stools and stimulates bowel movements [2,4].
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