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Study · In vitro (cell-free) · 2021

1 result

Improving the Gastrointestinal Stability of Linaclotide.

Braga Emidio N, Tran HNT, Andersson A, Dawson PE, Albericio F, Vetter I, Muttenthaler M

Journal of medicinal chemistry12 May 2021Cited by 31 (Europe PMC)

PMID33979161 (opens in a new tab)PMCIDPMC8237258 (opens in a new tab)DOI10.1021/acs.jmedchem.1c00380 (opens in a new tab)PepBankPUB-33979161
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Summary

High susceptibility to proteolytic degradation in the gastrointestinal tract limits the therapeutic application of peptide drugs in gastrointestinal disorders. Linaclotide is an orally administered peptide drug for the treatment of irritable bowel syndrome with constipation (IBS-C) and abdominal pain. Linaclotide is however degraded in the intestinal environment within 1 h, and improvements in gastrointestinal stability might enhance its therapeutic application. We therefore designed and synthesized a series of linaclotide analogues employing a variety of strategic modifications and evaluated their gastrointestinal stability and pharmacological activity at its target receptor guanylate cyclase-C. All analogues had substantial improvements in gastrointestinal half-lives (>8 h vs linaclotide 48 min), and most remained active at low nanomolar concentrations. This work highlights strategic approaches for the development of gut-stable peptides toward the next generation of orally administered peptide drugs for the treatment of gastrointestinal disorders.
CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study1

1 result from studies that gave the peptide. No result from this study comes from people.

  1. 01LabIn vitro (cell-free)Pharmacokinetics

    In gastrointestinal stability tests, native linaclotide had a half-life of 48 min.

    In plain wordsIn lab tests, native linaclotide had a gastrointestinal half-life of 48 minutes.

    Peptide
    Linaclotide
    Outcome
    Not applicableGastrointestinal half-life
    Study

    n: not reported in source

    Gastrointestinal stability assay
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Measurements

    Gastrointestinal half-life
    48 min
    native linaclotide

    Source sentences

    Summary
    All analogues had substantial improvements in gastrointestinal half-lives (>8 h vs linaclotide 48 min), and most remained active at low nanomolar concentrations.

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

  1. Version 2Current

    28 Oct 2026, 02:03 UTC

    Study results updated

  2. Version 1

    27 Oct 2026, 16:34 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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