title: Constella™(EU)-Linzess™(USA): the last milestone in the long journey of the peptide linaclotide and its implications for the future of peptide drugs.
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.
authors: Institute for Research in Biomedicine, Barcelona Science Park, 08028-Barcelona, Spain.
authors: Miriam
authors: M
authors: Góngora-Benítez
authors: Judit
authors: J
authors: Tulla-Puche
authors: Fernando
authors: F
authors: Albericio
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D002908:Chronic Disease; D003106:Colon / Q000473:pathology; D003248:Constipation / Q000150:complications* / Q000188:drug therapy* / Q000191:economics / Q000473:pathology; D006801:Humans; D043183:Irritable Bowel Syndrome / Q000150:complications* / Q000188:drug therapy* / Q000191:economics / Q000473:pathology; D008958:Models, Molecular; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D000074261:Receptors, Enterotoxin; D050705:Receptors, Guanylate Cyclase-Coupled / Q000819:agonists* / Q000378:metabolism; D018000:Receptors, Peptide / Q000819:agonists* / Q000378:metabolism
chemical_list: D010455:Peptides; D018000:Receptors, Peptide; D000074261:Receptors, Enterotoxin; D050705:Receptors, Guanylate Cyclase-Coupled; C523483:linaclotide