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Expert Opin Investig Drugs. 2016 Aug;25(8):871-90. doi: 10.1080/13543784.2016.1189530. Epub 2016 May 27.

Free fatty acid receptor agonists for the treatment of type 2 diabetes: drugs in preclinical to phase II clinical development.

Author information

1
a Center of Drug Discovery, State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
2
b Department of Endocrinology and Metabolism , Shanghai Jiao Tong University Affiliated Sixth People's Hospital, Shanghai Diabetes Institute, Shanghai Key Laboratory of Diabetes Mellitus, Shanghai Clinical Center for Diabetes , Shanghai , PR China.
3
c Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease , China Pharmaceutical University , Nanjing , PR China.

Abstract

INTRODUCTION:

The alarming prevalence of type 2 diabetes mellitus (T2DM) stimulated the exploitation of new antidiabetic drugs with extended durability and enhanced safety. In this regard, the free fatty acid receptor 1 (FFA1) and FFA4 have emerged as attractive targets in the last decade. FFA1 has prominent advantages in promoting insulin and incretin secretion while FFA4 shows great potential in incretin secretion, insulin sensitization and anti-inflammatory effects.

AREA COVERED:

Herein, the authors focus specifically on FFA1 and FFA4 agonists in clinical trials and preclinical development. LY2922470, P11187 and SHR0534 are currently active in clinical trials while the CNX-011-67, SAR1, DS-1558 and BMS-986118 are in preclinical phase. The information for this review is retrieved from Integrity, Scifinder, Espacenet and clinicaltrials.gov databases.

EXPERT OPINION:

Current proof-of-concept in clinical trials suggests that FFA1 agonists have a significant improvement for T2DM without the risk of hypoglycemia. However, there are still several challenging problems including the mechanism of the receptor and the efficacy and safety of the ligands.

KEYWORDS:

FFA1; Free fatty acid; GLP-1; GPR120; GPR40; type 2 diabetes

PMID:
27171154
DOI:
10.1080/13543784.2016.1189530
[Indexed for MEDLINE]

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