Development of Cagrilintide, a Long-Acting Amylin Analogue

J Med Chem. 2021 Aug 12;64(15):11183-11194. doi: 10.1021/acs.jmedchem.1c00565. Epub 2021 Jul 21.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Dose-Response Relationship, Drug
  • Drug Development*
  • Humans
  • Hypoglycemic Agents / chemical synthesis
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology*
  • Islet Amyloid Polypeptide / antagonists & inhibitors*
  • Islet Amyloid Polypeptide / chemical synthesis
  • Islet Amyloid Polypeptide / chemistry
  • Islet Amyloid Polypeptide / metabolism
  • Islet Amyloid Polypeptide / pharmacology
  • Models, Molecular
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Hypoglycemic Agents
  • Islet Amyloid Polypeptide
  • cagrilintide