Skip to content

Study · Non-randomized trial · n = 10 · 2026

8 results

Disposition and Absolute Bioavailability of Orally Administered Orforglipron in Healthy Participants.

Morse BL, Bhattachar S, Ma X, Coutant DE, Czeskis B, Nicoll C, Cassidy KC

Clinical pharmacology in drug development1 Sept 2025Cited by 5 (Europe PMC)

PMID40888509 (opens in a new tab)DOI10.1002/cpdd.1594 (opens in a new tab)PepBankPUB-40888509
Publisher pagePubMedAsk about this study
Jump to 8 results

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 study8

8 results from studies that gave the peptide. 8 results from people.

  1. 01HumanNon-randomized trialPharmacokinetics

    In healthy adults, mean absolute oral bioavailability of orforglipron was 79.1% ± 16.8%.

    In plain wordsIn healthy adults, average oral orforglipron bioavailability was 79.1%.

    Peptide
    Orforglipron
    Outcome
    Not applicableAbsolute oral bioavailability
    Study

    n = 10

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    1 mg oral and ∼21 µg intravenous [14C]-orforglipron · oral and intravenousAs given in this study (human).

    Measurements

    Absolute oral bioavailability
    79.1%
    mean
    Bioavailability variability
    16.8%
    ±

    Source sentences

    Summary
    The mean absolute oral bioavailability of orforglipron was 79.1% ± 16.8%.
    1 context sentence
    Summary · context
    Study A participants (N = 10) received a 1-mg orforglipron oral capsule while fasting and an intravenous dose of ∼21 µg of [14C]-orforglipron.
  2. 02HumanNon-randomized trialPharmacokinetics

    In healthy adults, fecal excretion accounted for 87% ± 2.8% of orforglipron-related radioactivity.

    In plain wordsIn healthy adults, most orforglipron-related radioactivity left the body through feces.

    Peptide
    Orforglipron
    Outcome
    Not applicableFecal excretion of radioactivity
    Study

    n = 6

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    3 mg with ∼200 µCi [14C]-orforglipron · oralAs given in this study (human).

    Measurements

    Fecal radioactivity excretion
    87%
    mean
    Fecal excretion variability
    2.8%
    ±

    Source sentences

    Summary
    The primary route of elimination for [14C]-orforglipron-related radioactivity was via the feces (87% ± 2.8%) with minimal urinary excretion (0.2% ± 0.02%).
    1 context sentence
    Summary · context
    Study B participants (N = 6) received an oral solution of 3 mg of orforglipron with ∼200 µCi of [14C]-orforglipron while fasting.
  3. 03HumanNon-randomized trialPharmacokinetics

    In healthy adults, urinary excretion accounted for 0.2% ± 0.02% of orforglipron-related radioactivity.

    In plain wordsIn healthy adults, little orforglipron-related radioactivity left the body through urine.

    Peptide
    Orforglipron
    Outcome
    Not applicableUrinary excretion of radioactivity
    Study

    n = 6

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    3 mg with ∼200 µCi [14C]-orforglipron · oralAs given in this study (human).

    Measurements

    Urinary radioactivity excretion
    0.2%
    mean
    Urinary excretion variability
    0.02%
    ±

    Source sentences

    Summary
    The primary route of elimination for [14C]-orforglipron-related radioactivity was via the feces (87% ± 2.8%) with minimal urinary excretion (0.2% ± 0.02%).
    1 context sentence
    Summary · context
    Study B participants (N = 6) received an oral solution of 3 mg of orforglipron with ∼200 µCi of [14C]-orforglipron while fasting.
  4. 04HumanNon-randomized trialPharmacokinetics

    In healthy adults, total recovery of administered orforglipron-related radioactivity was 88% over 384 hours.

    In plain wordsIn healthy adults, researchers recovered 88% of administered orforglipron-related radioactivity over 384 hours.

    Peptide
    Orforglipron
    Outcome
    Not applicableTotal radioactivity recovery
    Study

    n = 6

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    3 mg with ∼200 µCi [14C]-orforglipron · oralAs given in this study (human).

    Measurements

    Total recovery
    88%
    over 384 hours

    Source sentences

    Summary
    Total recovery of administered radioactivity was 88% over 384 hours after the dose.
    1 context sentence
    Summary · context
    Study B participants (N = 6) received an oral solution of 3 mg of orforglipron with ∼200 µCi of [14C]-orforglipron while fasting.
  5. 05HumanNon-randomized trialPharmacokinetics

    In healthy adults, orforglipron underwent extensive oxidative metabolism followed by microbial metabolism of its oxadiazolone ring.

    In plain wordsIn healthy adults, orforglipron underwent oxidative metabolism followed by microbial metabolism.

    Peptide
    Orforglipron
    Outcome
    Not applicableOxidative and microbial metabolism
    Study

    n: not reported in source

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    3 mg with ∼200 µCi [14C]-orforglipron · oralAs given in this study (human).

    Source sentences

    Summary
    Metabolite profiling from study B showed that orforglipron underwent extensive oxidative metabolism, followed by microbial metabolism of the oxadiazolone ring.
    1 context sentence
    Summary · context
    Study B participants (N = 6) received an oral solution of 3 mg of orforglipron with ∼200 µCi of [14C]-orforglipron while fasting.
  6. 06HumanNon-randomized trialPharmacokinetics

    In healthy adults, orforglipron represented 93.3% of plasma drug-related components in metabolite profiling.

    In plain wordsIn healthy adults, orforglipron was the main drug-related component in plasma.

    Peptide
    Orforglipron
    Outcome
    Not applicableParent drug proportion in plasma
    Study

    n: not reported in source

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    3 mg with ∼200 µCi [14C]-orforglipron · oralAs given in this study (human).

    Measurements

    Parent drug proportion
    93.3%
    plasma

    Source sentences

    Summary
    Orforglipron was the most abundant plasma component (93.3%) with minor oxidative metabolites M7 (3.3%) and M23 (1.6%).
    1 context sentence
    Summary · context
    Study B participants (N = 6) received an oral solution of 3 mg of orforglipron with ∼200 µCi of [14C]-orforglipron while fasting.
  7. 07HumanNon-randomized trialPharmacokinetics

    In healthy adults, oxidative metabolite M7 represented 3.3% of plasma drug-related components after orforglipron administration.

    In plain wordsIn healthy adults, M7 was a minor orforglipron metabolite in plasma.

    Peptide
    Orforglipron
    Outcome
    Not applicableM7 metabolite proportion in plasma
    Study

    n: not reported in source

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    3 mg with ∼200 µCi [14C]-orforglipron · oralAs given in this study (human).

    Measurements

    M7 proportion
    3.3%
    plasma

    Source sentences

    Summary
    Orforglipron was the most abundant plasma component (93.3%) with minor oxidative metabolites M7 (3.3%) and M23 (1.6%).
    1 context sentence
    Summary · context
    Study B participants (N = 6) received an oral solution of 3 mg of orforglipron with ∼200 µCi of [14C]-orforglipron while fasting.
  8. 08HumanNon-randomized trialPharmacokinetics

    In healthy adults, oxidative metabolite M23 represented 1.6% of plasma drug-related components after orforglipron administration.

    In plain wordsIn healthy adults, M23 was a minor orforglipron metabolite in plasma.

    Peptide
    Orforglipron
    Outcome
    Not applicableM23 metabolite proportion in plasma
    Study

    n: not reported in source

    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    3 mg with ∼200 µCi [14C]-orforglipron · oralAs given in this study (human).

    Measurements

    M23 proportion
    1.6%
    plasma

    Source sentences

    Summary
    Orforglipron was the most abundant plasma component (93.3%) with minor oxidative metabolites M7 (3.3%) and M23 (1.6%).
    1 context sentence
    Summary · context
    Study B participants (N = 6) received an oral solution of 3 mg of orforglipron with ∼200 µCi of [14C]-orforglipron while fasting.

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

    14 Oct 2026, 05:02 UTC

    Study results updated

  2. Version 1

    14 Oct 2026, 01:46 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

PepBank is a research reference. Talk to a doctor before you use any peptide.