Recent progress and future options in the development of GLP-1 receptor agonists for the treatment of diabesity

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4011-8. doi: 10.1016/j.bmcl.2013.05.022. Epub 2013 May 16.


The dramatic rise of the twin epidemics, type 2 diabetes and obesity is associated with increased mortality and morbidity worldwide. Based on this global development there is clinical need for anti-diabetic therapies with accompanied weight reduction. From the approved therapies, the injectable glucagon-like peptide-1 receptor agonists (GLP-1 RAs) are the only class of agents which are associated with a modest weight reduction. Physiological effects of the gastro-intestinal hormone GLP-1 are improvement of glycemic control as well as a reduction in appetite and food intake. Different approaches are currently under clinical evaluation to optimize the therapeutic potential of GLP-1 RAs directed to once-weekly up to once-monthly administration. The next generation of peptidic co-agonists comprises the activity of GLP-1 plus additional gastro-intestinal hormones with the potential for increased therapeutic benefits compared to GLP-1 RAs.

Publication types

  • Review

MeSH terms

  • Clinical Trials as Topic
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Dipeptidyl-Peptidase IV Inhibitors / therapeutic use
  • Glucagon-Like Peptide 1 / agonists*
  • Glucagon-Like Peptide 1 / analogs & derivatives
  • Glucagon-Like Peptide 1 / chemistry
  • Glucagon-Like Peptide 1 / metabolism
  • Glucagon-Like Peptide 1 / therapeutic use
  • Glucagon-Like Peptides / analogs & derivatives
  • Humans
  • Hypoglycemic Agents / therapeutic use*
  • Immunoglobulin Fc Fragments / therapeutic use
  • Liraglutide
  • Peptides / therapeutic use
  • Recombinant Fusion Proteins / therapeutic use


  • Dipeptidyl-Peptidase IV Inhibitors
  • Hypoglycemic Agents
  • Immunoglobulin Fc Fragments
  • Peptides
  • Recombinant Fusion Proteins
  • taspoglutide
  • rGLP-1 protein
  • Glucagon-Like Peptides
  • lixisenatide
  • Liraglutide
  • Glucagon-Like Peptide 1
  • dulaglutide