Glepaglutide, a novel glucagon-like peptide-2 agonist, has anti-inflammatory and mucosal regenerative effects in an experimental model of inflammatory bowel disease in rats

BMC Gastroenterol. 2023 Mar 21;23(1):79. doi: 10.1186/s12876-023-02716-4.

Abstract

Background: Glucagon-like peptide-2 (GLP-2) enhances intestinal repair and attenuates inflammation in preclinical inflammatory bowel disease (IBD) models, making GLP-2 analogues attractive candidates for IBD therapy. Glepaglutide is a long-acting GLP-2 receptor agonist in clinical development for treatment of short bowel syndrome. Here, we investigated if glepaglutide is therapeutically beneficial in rats with small intestinal inflammation.

Methods: Small intestinal inflammation was induced with indomethacin in naive Wistar rats, followed by glepaglutide administration at different disease stages. Glepaglutide was administered in co-treatment and post-treatment regimens. Small intestinal length and concentrations of inflammatory markers α-1-acid glycoprotein and myeloperoxidase were used to assess anti-inflammatory effects. Small intestinal mass was evaluated to determine intestinotrophic effects.

Results: Glepaglutide co- and post-treatment significantly reduced severity of small intestinal inflammation, evidenced by reversed small intestinal shortening and decreased α-1-acid glycoprotein and/or myeloperoxidase concentration(s). Co- and post-treatment with glepaglutide also significantly increased small intestinal mass, indicating intestinal regenerative effects. Similar effects were observed in naive rats after glepaglutide treatment.

Conclusion: Glepaglutide has anti-inflammatory and intestinotrophic effects without the need for pre-treatment in a rat model of small intestinal inflammation. Thus, glepaglutide is of potential clinical interest for patients with IBD.

Keywords: Anti-inflammatory; GLP-2; Glepaglutide; Inflammatory bowel disease; Mucosal healing.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use
  • Glucagon-Like Peptide 2* / agonists
  • Glycoproteins / metabolism
  • Inflammation / drug therapy
  • Inflammatory Bowel Diseases* / drug therapy
  • Intestinal Mucosa
  • Models, Theoretical
  • Peroxidase / metabolism
  • Rats
  • Rats, Wistar

Substances

  • Anti-Inflammatory Agents
  • Glucagon-Like Peptide 2
  • Glycoproteins
  • Peroxidase