Irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) are highly
prevalent gastrointestinal disorders. Traditional symptoms based therapies had somewhat limited success and efficacy in
addressing the disorders. Recently, linaclotide emerged as novel peptide capable of improving abdominal symptoms in
patients suffering from IBS-C and CIC. Guanylate cyclase C (GC-C) receptor a multi domain protein, found to be
molecular target for linaclotide which acts by activating GC-C receptor on the apical surface of intestinal epithelial cells.
Binding of linaclotide to GC-C receptor triggers the elevation of second messenger cGMP that elicits fluid secretion into
intestinal cells which play a critical role in maintaining homeostasis through cystic fibrosis transmembrane conductance
regulator (CFTR). Data from Phase and clinical trials demonstrated that linaclotide seems to produce a statistically
significant increase in stool frequency, improved straining, decreased abdominal pain and discomfort.
Keywords: CIC, cGMP, guanylate cyclase C, homeostasis, IBS-C, Linaclotide.
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Published on: 26 August, 2013
Page: [1685 - 1690]