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Study · Non-randomized trial · 2010

7 results

Metabolism and excretion of the once-daily human glucagon-like peptide-1 analog liraglutide in healthy male subjects and its in vitro degradation by dipeptidyl peptidase IV and neutral endopeptidase.

Malm-Erjefält M, Bjørnsdottir I, Vanggaard J, Helleberg H, Larsen U, Oosterhuis B, van Lier JJ, Zdravkovic M, Olsen AK

Drug metabolism and disposition: the biological fate of chemicals13 Aug 2010Cited by 146 (Europe PMC)

PMID20709939 (opens in a new tab)DOI10.1124/dmd.110.034066 (opens in a new tab)PepBankPUB-20709939
Publisher pagePubMedAsk about this study
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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study7

7 results from studies that gave the peptide. 3 results from people.

  1. 01HumanNon-randomized trialPharmacokinetics

    In healthy males after one subcutaneous dose of radiolabelled liraglutide, plasma radioactivity exposure was at least 89% intact liraglutide and at most 11% two minor metabolites.

    In plain wordsIn healthy men, most of the radioactivity in blood after one injection was intact liraglutide, with little from two minor breakdown products.

    Peptide
    Liraglutide
    Outcome
    Not applicablePlasma radioactivity composition
    Study

    n: not reported in source

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    0.75 mg · subcutaneous · single doseAs given in this study (human).

    Measurements

    Share of plasma AUC as liraglutide
    ≥ 89%
    AUC 2-24 h
    Share of plasma AUC as two minor metabolites
    ≤ 11%
    AUC 2-24 h

    Source sentences

    Summary
    The exposure of radioactivity in plasma (area under the concentration-time curve from 2 to 24 h) was represented by liraglutide (≥89%) and two minor metabolites (totaling ≤11%).
    1 context sentence
    Summary · context
    To study metabolism and excretion of [(3)H]liraglutide, a single subcutaneous dose of 0.75 mg/14.2 MBq was given to healthy males. The recovered radioactivity in blood, urine, and feces was measured, and metabolites were profiled.
  2. 02HumanNon-randomized trialPharmacokinetics

    In healthy males, three minor metabolites totalling 6% and 5% of the administered radioactivity were excreted in urine and feces.

    In plain wordsIn healthy men, only small amounts of liraglutide breakdown products, 6% in urine and 5% in feces, were excreted.

    Peptide
    Liraglutide
    Outcome
    Not applicableExcretion of metabolites in urine and feces
    Study

    n: not reported in source

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    0.75 mg · subcutaneous · single doseAs given in this study (human).

    Measurements

    Metabolites excreted in urine
    6 % of dose
    urine
    Metabolites excreted in feces
    5 % of dose
    feces

    Source sentences

    Summary
    Three minor metabolites totaling 6 and 5% of the administered radioactivity were excreted in urine and feces, respectively
    1 context sentence
    Summary · context
    To study metabolism and excretion of [(3)H]liraglutide, a single subcutaneous dose of 0.75 mg/14.2 MBq was given to healthy males. The recovered radioactivity in blood, urine, and feces was measured, and metabolites were profiled.
  3. 03HumanNon-randomized trialPharmacokinetics

    In healthy males, no intact liraglutide was detected in urine or feces.

    In plain wordsIn healthy men, no unchanged liraglutide was found in urine or feces.

    Peptide
    Liraglutide
    Outcome
    No significant changeIntact liraglutide in urine and feces
    Study

    n: not reported in source

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    0.75 mg · subcutaneous · single doseAs given in this study (human).

    Source sentences

    Summary
    but no liraglutide was detected.
    1 context sentence
    Summary · context
    To study metabolism and excretion of [(3)H]liraglutide, a single subcutaneous dose of 0.75 mg/14.2 MBq was given to healthy males. The recovered radioactivity in blood, urine, and feces was measured, and metabolites were profiled.
  4. 04LabIn vitro (cell-free)Mechanism

    In vitro, DPP-IV cleaved liraglutide in the Ala8-Glu9 position of the N terminus, as it does with GLP-1.

    In plain wordsIn lab tests, the DPP-IV enzyme cut liraglutide at the same place as natural GLP-1.

    Peptide
    Liraglutide
    Outcome
    Not applicableDPP-IV cleavage site
    Study

    n: not reported in source

    In vitro incubation with DPP-IV
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Similarly to GLP-1, liraglutide was cleaved in vitro by DPP-IV in the Ala8-Glu9 position of the N terminus
  5. 05LabIn vitro (cell-free)Mechanism

    In vitro, neutral endopeptidase degraded liraglutide into several metabolites.

    In plain wordsIn lab tests, the NEP enzyme broke liraglutide down into several smaller products.

    Peptide
    Liraglutide
    Outcome
    Not applicableNEP degradation
    Study

    n: not reported in source

    In vitro incubation with NEP
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    degraded by NEP into several metabolites.
  6. 06LabIn vitro (cell-free)Mechanism

    In vitro, the chromatographic retention time of DPP-IV-truncated liraglutide correlated well with the primary human plasma metabolite GLP-1(9-37).

    In plain wordsIn lab tests, the main liraglutide breakdown product matched the main breakdown product seen in human blood.

    Peptide
    Liraglutide
    Outcome
    Not applicableMatch of DPP-IV-truncated liraglutide to plasma metabolite
    Study

    n: not reported in source

    In vitro incubation with DPP-IV
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    The chromatographic retention time of DPP-IV-truncated liraglutide correlated well with the primary human plasma metabolite [GLP-1(9-37)]
  7. 07LabIn vitro (cell-free)Mechanism

    In vitro, DPP-IV and neutral endopeptidase metabolized liraglutide in a manner similar to native GLP-1, but at a much slower rate.

    In plain wordsIn lab tests, the enzymes DPP-IV and NEP broke down liraglutide in the same way as natural GLP-1, but much more slowly.

    Peptide
    Liraglutide
    Outcome
    DecreaseIn vitro degradation rate by DPP-IV and NEP versus GLP-1
    Study

    n: not reported in source

    In vitro incubation with DPP-IV and NEP
    Comparator
    GLP-1
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    In conclusion, liraglutide is metabolized in vitro by DPP-IV and NEP in a manner similar to that of native GLP-1, although at a much slower rate.

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

Registered trials1

Trials this study reports on, or that list this study as a reference. Registry data from ClinicalTrials.gov.

1 trial · 1 completed · source ClinicalTrials.gov (opens in a new tab)

CompletedPhase 1NCT01517568

Metabolism and Excretion of Liraglutide in Healthy Male Volunteers

Novo Nordisk A/Sn = 7Nov 2006 to Dec 2006

Diabetes · Healthy

Trial pageClinicalTrials.govUpdated 26 Jan 2017

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

    12 Oct 2026, 12:10 UTC

    Study results updated

  2. Version 1

    9 Oct 2026, 03:05 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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