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Creating Glepaglutide, the First Long-Acting GLP-2 Analogue to Enable a Ready-to-Use Injection.

Bjarne Due Larsen¹, Jesper Skodborg Villadsen¹, Jolanta Skarbaliene²

¹Zealand Pharma A/S, Sydmarken 11, 2860 Søborg, Denmark.

Journal of Medicinal Chemistry

|January 24, 2025

Summary

Novel human glucagon-like peptide-2 (hGLP-2) analogues were developed with enhanced stability and potency for treating short bowel syndrome (SBS). Glepaglutide, a leading analogue, shows promise for liquid formulation and autoinjector delivery in Phase 3 trials.

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Area of Science:

Gastroenterology and Peptide Therapeutics

Background:

Native human glucagon-like peptide-2 (hGLP-2) is unstable and has a short half-life, limiting its clinical use.
Short bowel syndrome (SBS) and inflammatory bowel disease (IBD) are conditions potentially treatable with hGLP-2 receptor agonists.

Purpose of the Study:

To design novel hGLP-2 peptide analogues with improved physicochemical properties, receptor potency, and half-life.
To develop a stable, long-acting hGLP-2 analogue suitable for clinical application.

Main Methods:

Design and synthesis of hGLP-2 analogues incorporating a C-terminal (lysine)6 tail (Structure Inducing Probe technology).
Evaluation of in vitro receptor potency and physicochemical stability.
Characterization of glepaglutide, a specific hGLP-2 analogue.

Main Results:

Novel hGLP-2 analogues demonstrated significantly improved chemical and physical properties.
High in vitro hGLP-2 receptor potencies and extended half-lives were achieved.
Glepaglutide exhibited excellent physicochemical stability, enabling liquid formulation and autoinjector delivery.

Conclusions:

The developed hGLP-2 analogues, particularly glepaglutide, offer a promising therapeutic approach for SBS.
Glepaglutide's stability and formulation characteristics make it suitable for subcutaneous administration in Phase 3 clinical trials.