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GPR40 agonists for the treatment of type 2 diabetes: life after ‘TAKing’ a hit
Author(s) -
Mancini A. D.,
Poitout V.
Publication year - 2015
Publication title -
diabetes, obesity and metabolism
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.445
H-Index - 128
eISSN - 1463-1326
pISSN - 1462-8902
DOI - 10.1111/dom.12442
Subject(s) - free fatty acid receptor 1 , type 2 diabetes , agonist , receptor , clinical trial , diabetes mellitus , medicine , pharmacology , endocrinology
The free fatty acid receptor GPR40 has been proposed as a potential target for type 2 diabetes ( T2D ) pharmacotherapy. This idea has been validated in both preclinical and clinical studies, in which activation of GPR40 was shown to improve glycaemic control by stimulating glucose‐dependent insulin secretion; however, the recent termination of phase III clinical trials using the GPR40 agonist TAK ‐875 (fasiglifam) has raised important questions regarding the long‐term safety and viability of targeting GPR40 and, more specifically, about our understanding of this receptor's basic biology. In the present review, we provide a summary of established and novel concepts related to GPR40 's pharmacobiology and discuss the current status and future outlook for GPR40 ‐based drug development for the treatment of T2D .