2. Academic Validation
  3. Development of Cagrilintide, a Long-Acting Amylin Analogue

Development of Cagrilintide, a Long-Acting Amylin Analogue

  • J Med Chem. 2021 Aug 12;64(15):11183-11194. doi: 10.1021/acs.jmedchem.1c00565.
Thomas Kruse 1,  Jakob Lerche Hansen 1,  Kirsten Dahl 1,  Lauge Schäffer 1,  Ulrich Sensfuss 1,  Christian Poulsen 1,  Morten Schlein 1,  Ann Maria Kruse Hansen 1,  Claus Bekker Jeppesen 1,  Charlotta Dornonville de la Cour 1,  Trine Ryberg Clausen 1,  Eva Johansson 1,  Simone Fulle 1,  Rikke Bjerring Skyggebjerg 1,  Kirsten Raun 1
Affiliations

Affiliation

  • 1 Novo Nordisk, Novo Nordisk Park, DK-2760 Maaloev, Denmark.
PMID: 34288673 DOI: 10.1021/acs.jmedchem.1c00565
Abstract

A hallmark of the pancreatic hormone amylin is its high propensity toward the formation of amyloid fibrils, which makes it a challenging drug design effort. The amylin analogue pramlintide is commercially available for diabetes treatment as an adjunct to Insulin therapy but requires three daily injections due to its short half-life. We report here the development of the stable, lipidated long-acting amylin analogue cagrilintide (23) and some of the structure-activity efforts that led to the selection of this analogue for clinical development with obesity as an indication. Cagrilintide is currently in clinical trial and has induced significant weight loss when dosed alone or in combination with the GLP-1 analogue semaglutide.

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