Abstract
Irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) are highly prevalent gastrointestinal disorders associated with health, economical and social problems. Recently, after a long journey of preclinical studies and clinical trials, linaclotide, a first-in-class GC-C receptor peptide agonist, has received the approval in the USA and Europe for the treatment of IBS-C and CIC. This article provides an overview of clinical, economic and biological aspects of IBS-C and CIC and covers the current and emerging therapeutic agents for treating these conditions. Particularly, the pharmacodynamic and pharmacokinetic properties of linaclotide, a small, disulfide-rich peptide, and its implications in the future of peptide drug discovery and development are discussed.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Amino Acid Sequence
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Animals
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Chronic Disease
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Colon / pathology
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Constipation / complications*
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Constipation / drug therapy*
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Constipation / economics
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Constipation / pathology
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Humans
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Irritable Bowel Syndrome / complications*
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Irritable Bowel Syndrome / drug therapy*
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Irritable Bowel Syndrome / economics
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Irritable Bowel Syndrome / pathology
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Models, Molecular
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Molecular Sequence Data
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Peptides / chemistry
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Peptides / pharmacokinetics
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Peptides / pharmacology
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Peptides / therapeutic use*
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Receptors, Enterotoxin
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Receptors, Guanylate Cyclase-Coupled / agonists*
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Receptors, Guanylate Cyclase-Coupled / metabolism
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Receptors, Peptide / agonists*
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Receptors, Peptide / metabolism
Substances
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Peptides
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Receptors, Peptide
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Receptors, Enterotoxin
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Receptors, Guanylate Cyclase-Coupled
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linaclotide