Development of Petrelintide: a Potent, Stable, Long-Acting Human Amylin Analogue
The past few years have seen the approval of several medications for weight management, but there is an increasing need for new therapies that target different pathways of energy balance. Owing to its role as a physiological satiety signal released after nutrient intake, amylin is an attractive pharmacological target for weight management in individuals living with obesity. Furthermore, combinations of peptide drugs for weight management may be more effective than individual peptide drugs. Thus, there is a need for peptide drugs that potentially also can be used as combination therapies, to enable coformulation with currently marketed drugs. Herein, we report the development of petrelintide, a potent, stable, long-acting analogue of human amylin that can be formulated at about neutral pH. This was enabled through optimization of chemical stability while retaining <i>in vitro</i> and <i>in vivo</i> potency. Petrelintide is in clinical development as a potential treatment for weight management.
Authors
- Lise Giehm (ORCID: https://orcid.org/0000-0002-7068-452X)
- Henrik K. Munch (ORCID: https://orcid.org/0000-0002-3464-677X)
- Tamara Baader-Pagler
- Jolanta Skarbaliene (ORCID: https://orcid.org/0000-0003-3965-7504)
- Jesper Mosolff Mathiesen (ORCID: https://orcid.org/0000-0003-4251-4416)
- Dieter Hamprecht (ORCID: https://orcid.org/0000-0002-8858-3153)
- Jesper Skodborg Villadsen
- Rasmus Just
- Alexander Heim‐Riether (ORCID: https://orcid.org/0000-0001-8052-1559)
- Wolfgang Rist (ORCID: https://orcid.org/0000-0002-0626-3544)
- Achim Grube
- Maria A. Deryabina
- Oliver Demmer
- Bill Vestergaard
- Per‐Olof Eriksson (ORCID: https://orcid.org/0000-0002-7411-7872)
Institutions
- Boehringer Ingelheim (Germany) (DE)
- Boehringer Ingelheim (Italy) (IT)
- Zealand Pharma (Denmark) (DK)
- Boehringer Ingelheim (Australia) (AU)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2025-11-11
- DOI
- https://doi.org/10.1021/acs.jmedchem.5c01185
- Citations
- 5
- Primary Topic
- Regulation of Appetite and Obesity
- Type
- article
- Field-Weighted Citation Impact
- 4.57