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Study · Animal study (in vivo) · mouse · 2026

2 results

Discovery of Small-Molecule GLP‑1 Receptor Agonists with Improved Oral Pharmacokinetics Based on Orforglipron.

Li M, Fang J, Qi G, Guo S, Xu T, Lu Y, Yuan Q, Wang J, Zhu S, Shen J, Yang H, Xie X, Wang K

ACS medicinal chemistry letters6 May 2026Cited by 1 (Europe PMC)

PMID42305200 (opens in a new tab)PMCIDPMC13266644 (opens in a new tab)DOI10.1021/acsmedchemlett.6c00077 (opens in a new tab)PepBankPUB-42305200
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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 study2

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

  1. 01AnimalAnimal study (in vivo)Pharmacokinetics

    In mice, orforglipron oral bioavailability was 6.4%, lower than that of the two new analogues.

    In plain wordsIn mice, orforglipron oral bioavailability was lower than that of the two new analogues.

    Peptide
    Orforglipron
    Outcome
    DecreaseOral bioavailability
    Study

    mousen: not reported in source

    mice
    Comparator
    17-P1 and 24-P1
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated · oralAs given in this study (mouse).

    Measurements

    Oral bioavailability
    6.4%
    orforglipron

    Source sentences

    Summary
    Compared with orforglipron, both compounds exhibited markedly improved permeability (Caco-2 P app = 2.83 and 4.75 nm/s vs 0.14 nm/s) and enhanced oral bioavailability in mice (54.0% and 72.4% vs 6.4%).
  2. 02LabIn vitro (cells)Pharmacokinetics

    In Caco-2 assays, orforglipron permeability was 0.14 nm/s, lower than that of the two new analogues.

    In plain wordsIn lab tests, orforglipron permeability was lower than that of the two new analogues.

    Peptide
    Orforglipron
    Outcome
    DecreaseCaco-2 permeability
    Study

    humann: not reported in source

    Caco-2 cells
    Comparator
    17-P1 and 24-P1
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Measurements

    Caco-2 Papp
    0.14 nm/s
    orforglipron

    Source sentences

    Summary
    Compared with orforglipron, both compounds exhibited markedly improved permeability (Caco-2 P app = 2.83 and 4.75 nm/s vs 0.14 nm/s) and enhanced oral bioavailability in mice (54.0% and 72.4% vs 6.4%).

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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