The Medical Letter on Drugs and Therapeutics
Linaclotide (Linzess) for Constipation
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Linaclotide (lin´´ a kloe´ tide; Linzess – Ironwood/Forest), a guanylate cyclase-C receptor agonist, was recently approved by the FDA for oral treatment of chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C) in adults. It is the second drug approved for this indication; lubiprostone (Amitiza), a metabolite of prostaglandin E1, was the first.1,2

MECHANISM OF ACTION — Linaclotide is a 14-amino acid synthetic peptide that activates guanylate cyclase-C receptors on the luminal surface of the intestinal epithelium, increasing cGMP within the intestinal epithelial cells. This results in activation of the CFTR ion channel, increasing the secretion of chloride and bicarbonate ions into the intestinal lumen, increasing intraluminal fluid and accelerating intestinal transit.

CLINICAL STUDIES — Chronic ... more      

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Title: Linaclotide (Linzess) for Constipation
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