Abstract
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.
Mini-Reviews in Medicinal Chemistry
Title:Linaclotide-a Novel Secretagogue in the Treatment of Irritable Bowel Syndrome with Constipation and Chronic Idiopathic Constipation
Volume: 13 Issue: 11
Author(s): Shivani Sharma, Tina Sharma, Richa Dhingra, Prince Tomar, Sukhminder Singh, Manav Malhotra and T. R. Bhardwaj
Affiliation:
Keywords: CIC, cGMP, guanylate cyclase C, homeostasis, IBS-C, Linaclotide.
Abstract: 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.
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Cite this article as:
Sharma Shivani, Sharma Tina, Dhingra Richa, Tomar Prince, Singh Sukhminder, Malhotra Manav and Bhardwaj R. T., Linaclotide-a Novel Secretagogue in the Treatment of Irritable Bowel Syndrome with Constipation and Chronic Idiopathic Constipation, Mini-Reviews in Medicinal Chemistry 2013; 13 (11) . https://dx.doi.org/10.2174/1389557511313110011
DOI https://dx.doi.org/10.2174/1389557511313110011 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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