Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus

Bioorg Med Chem Lett. 2014 Jul 15;24(14):2991-3000. doi: 10.1016/j.bmcl.2014.05.019. Epub 2014 May 16.


Despite the availability of established medication for treatment of type 2 diabetes mellitus (T2DM) there still remains a significant unmet need for new effective, oral antidiabetic agents that improve glycemic control while maintaining an excellent safety profile. In this regard the FFA1 receptor has emerged as an attractive target in recent years. Activation of the FFA1 receptor has been shown to not only amplify glucose induced insulin secretion from pancreatic beta cells but also to stimulate incretin secretion from intestinal endocrine cells. The current review highlights on the latest developments and clinical data from evolving research on the potential of FFA1 agonists as effective treatment for T2DM.

Keywords: FFA1; GPCRs; GPR40; Oral antidiabetics; Type 2 diabetes.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Drug Discovery*
  • Humans
  • Hypoglycemic Agents / administration & dosage*
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology*
  • Molecular Structure
  • Receptors, G-Protein-Coupled / agonists*


  • FFAR1 protein, human
  • Hypoglycemic Agents
  • Receptors, G-Protein-Coupled