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Study · Non-randomized trial · 2026

10 results

Clinical Characterization of Enzyme and Transporter Precipitants to Evaluate Drug-Drug Interactions for Orforglipron, a Small Molecule Glucagon-Like Peptide-1 Receptor Agonist.

Morse BL, Coutant DE, Ma X, Raha S, Aithal K, Nicoll C, Rougée LRA, Bhattachar S

Clinical pharmacology and therapeutics3 Jul 2026Cited by 1 (Europe PMC)

PMID42399716 (opens in a new tab)PMCIDPMC13337131 (opens in a new tab)DOI10.1002/cpt.70377 (opens in a new tab)PepBankPUB-42399716
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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: CC BY-NC. Results still quote short attributed sentences.

Results from this study10

10 results from studies that gave the peptide. 10 results from people.

  1. 01HumanNon-randomized trialPharmacokinetics

    In healthy participants, orforglipron exposure increased in the presence of clarithromycin.

    In plain wordsIn healthy participants, clarithromycin increased orforglipron exposure compared with exposure without clarithromycin.

    Peptide
    Orforglipron
    Outcome
    IncreaseOrforglipron exposure with clarithromycin
    Study

    n: not reported in source

    Comparator
    Without clarithromycin
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated · oralAs given in this study (human).

    Source sentences

    Summary
    Orforglipron exposure increased in the presence of clarithromycin and cyclosporine and decreased with carbamazepine, demonstrating orforglipron exposure is affected by precipitants of CYP3A4 and OATP1B.
    2 context sentences
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
    Summary · context
    Orforglipron is an orally administered, small-molecule glucagon-like peptide-1 receptor agonist in clinical development for the treatment of type 2 diabetes and obesity.
  2. 02HumanNon-randomized trialPharmacokinetics

    In healthy participants, orforglipron exposure increased in the presence of cyclosporine.

    In plain wordsIn healthy participants, cyclosporine increased orforglipron exposure compared with exposure without cyclosporine.

    Peptide
    Orforglipron
    Outcome
    IncreaseOrforglipron exposure with cyclosporine
    Study

    n: not reported in source

    Comparator
    Without cyclosporine
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated · oralAs given in this study (human).

    Source sentences

    Summary
    Orforglipron exposure increased in the presence of clarithromycin and cyclosporine and decreased with carbamazepine, demonstrating orforglipron exposure is affected by precipitants of CYP3A4 and OATP1B.
    2 context sentences
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
    Summary · context
    Orforglipron is an orally administered, small-molecule glucagon-like peptide-1 receptor agonist in clinical development for the treatment of type 2 diabetes and obesity.
  3. 03HumanNon-randomized trialPharmacokinetics

    In healthy participants, orforglipron exposure decreased with carbamazepine.

    In plain wordsIn healthy participants, carbamazepine decreased orforglipron exposure compared with exposure without carbamazepine.

    Peptide
    Orforglipron
    Outcome
    DecreaseOrforglipron exposure with carbamazepine
    Study

    n: not reported in source

    Comparator
    Without carbamazepine
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Orforglipron exposure increased in the presence of clarithromycin and cyclosporine and decreased with carbamazepine, demonstrating orforglipron exposure is affected by precipitants of CYP3A4 and OATP1B.
    1 context sentence
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
  4. 04HumanNon-randomized trialPharmacokinetics

    In healthy participants, quinidine did not meaningfully change orforglipron exposure.

    In plain wordsIn healthy participants, orforglipron exposure did not meaningfully differ with versus without quinidine.

    Peptide
    Orforglipron
    Outcome
    No significant changeOrforglipron exposure with quinidine
    Study

    n: not reported in source

    Comparator
    Without quinidine
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Quinidine did not meaningfully change orforglipron exposure.
    1 context sentence
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
  5. 05HumanNon-randomized trialPharmacokinetics

    In healthy participants, orforglipron had no clinically meaningful effect on midazolam exposure.

    In plain wordsIn healthy participants, midazolam exposure did not meaningfully differ with versus without orforglipron.

    Peptide
    Orforglipron
    Outcome
    No significant changeMidazolam exposure
    Study

    n: not reported in source

    Comparator
    Without orforglipron
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Orforglipron had no clinically meaningful effect on the exposure of midazolam, digoxin, or atorvastatin.
    1 context sentence
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
  6. 06HumanNon-randomized trialPharmacokinetics

    In healthy participants, orforglipron had no clinically meaningful effect on digoxin exposure.

    In plain wordsIn healthy participants, digoxin exposure did not meaningfully differ with versus without orforglipron.

    Peptide
    Orforglipron
    Outcome
    No significant changeDigoxin exposure
    Study

    n: not reported in source

    Comparator
    Without orforglipron
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Orforglipron had no clinically meaningful effect on the exposure of midazolam, digoxin, or atorvastatin.
    1 context sentence
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
  7. 07HumanNon-randomized trialPharmacokinetics

    In healthy participants, orforglipron had no clinically meaningful effect on atorvastatin exposure.

    In plain wordsIn healthy participants, atorvastatin exposure did not meaningfully differ with versus without orforglipron.

    Peptide
    Orforglipron
    Outcome
    No significant changeAtorvastatin exposure
    Study

    n: not reported in source

    Comparator
    Without orforglipron
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Orforglipron had no clinically meaningful effect on the exposure of midazolam, digoxin, or atorvastatin.
    1 context sentence
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
  8. 08HumanNon-randomized trialPharmacokinetics

    In healthy participants, orforglipron weakly increased rosuvastatin exposure, consistent with BCRP inhibition.

    In plain wordsIn healthy participants, rosuvastatin exposure increased slightly with orforglipron compared with exposure without it.

    Peptide
    Orforglipron
    Outcome
    IncreaseRosuvastatin exposure
    Study

    n: not reported in source

    Comparator
    Without orforglipron
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    A weak increase in rosuvastatin exposure was consistent with BCRP inhibition, as CP-I data confirmed orforglipron does not affect OATP1B.
    1 context sentence
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
  9. 09HumanNon-randomized trialMechanism

    In healthy participants, CP-I data confirmed that orforglipron did not affect OATP1B.

    In plain wordsIn healthy participants, marker data showed that orforglipron did not affect OATP1B activity.

    Peptide
    Orforglipron
    Outcome
    No significant changeOATP1B activity
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    A weak increase in rosuvastatin exposure was consistent with BCRP inhibition, as CP-I data confirmed orforglipron does not affect OATP1B.
    1 context sentence
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.
  10. 10HumanNon-randomized trialPharmacokinetics

    In healthy participants, increased simvastatin acid exposure with orforglipron was attributed to simvastatin disposition rather than enzyme or transporter inhibition.

    In plain wordsIn healthy participants, orforglipron increased simvastatin acid exposure versus no orforglipron. The authors attributed this to how the body handles simvastatin.

    Peptide
    Orforglipron
    Outcome
    IncreaseSimvastatin acid exposure
    Study

    n: not reported in source

    Comparator
    Without orforglipron
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Increase in simvastatin acid exposure was attributed to the unique disposition of simvastatin rather than enzyme or transporter inhibition.
    2 context sentences
    Summary · context
    Mechanistic interrogation of the simvastatin interaction was also conducted.
    Summary · context
    The enzyme- and transporter-mediated DDI profile of orforglipron and that of CYP3A4/OATP1B/P-gp precipitants were characterized in six phase 1 clinical studies in healthy participants.

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.

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