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Constella™(EU)–Linzess™(USA): the last milestone in the long journey of the peptide linaclotide and its implications for the future of peptide drugs

    Miriam Góngora-Benítez

    Institute for Research in Biomedicine, Barcelona Science Park, 08028-Barcelona, Spain

    CIBER-BBN, Barcelona Science Park, 08028-Barcelona, Spain

    ,
    Judit Tulla-Puche

    Institute for Research in Biomedicine, Barcelona Science Park, 08028-Barcelona, Spain

    CIBER-BBN, Barcelona Science Park, 08028-Barcelona, Spain

    &
    Fernando Albericio

    * Author for correspondence

    Department of Organic Chemistry, University of Barcelona, 08028-Barcelona, Spain.

    School of Chemistry, University of KwaZulu Natal, 4001-Durban, South Africa

    Published Online:https://doi.org/10.4155/fmc.13.5

    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.

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