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In Silico Exploration of Therapeutics for GLP-1 Receptor Agonist-Induced Nausea and Their in Vivo Validation in Mice

Norihiro Shibui1, Takahide Suzuki1, Hiroki Yamamoto1

  • 1Department of Molecular Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.

Biological & Pharmaceutical Bulletin
|August 27, 2025
PubMed

Insights

Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) can cause nausea. This study found gabapentin effectively reduced nausea in patients and animal models, offering a potential treatment for this common side effect.

Area of Science:

  • Pharmacology
  • Gastroenterology
  • Clinical Research

Background:

  • Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) are vital for managing type 2 diabetes and obesity.
  • Nausea and vomiting are common, dose-limiting side effects of GLP-1 RAs, impacting patient adherence.
  • Novel strategies are needed to mitigate GLP-1 RA-induced gastrointestinal distress.

Purpose of the Study:

  • To identify effective drug combinations for mitigating GLP-1 RA-induced nausea and vomiting.
  • To investigate the efficacy of identified therapeutics in preclinical models of GLP-1 RA-induced nausea.

Main Methods:

  • Analysis of the U.S. Food and Drug Administration Adverse Event Reporting System database for real-world data.
  • Utilizing mouse models to assess GLP-1 RA-induced pica behavior as a surrogate for nausea.
  • Evaluating the impact of co-administered gabapentin on GLP-1 RA-induced pica behavior.

Main Results:

  • Gabapentin and acetaminophen were associated with reduced nausea-related events in patients treated with GLP-1 RAs.
  • Exenatide, a GLP-1 RA, dose-dependently increased pica behavior in mice without affecting food intake.
  • Co-treatment with gabapentin significantly attenuated exenatide-induced pica behavior.

Conclusions:

  • Gabapentin demonstrates therapeutic efficacy in reducing GLP-1 RA-induced nausea and vomiting.
  • These findings support gabapentin as a potential prophylactic or treatment option for managing GLP-1 RA-associated nausea.
Keywords:
gabapentinglucagon-like peptide 1 (GLP-1) receptor agonistnauseapica behaviorvomiting

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