Fasiglifam as a new potential treatment option for patients with type 2 diabetes.

INTRODUCTION: Fasiglifam , a novel G protein-coupled receptor 40 (GPR40) agonist, has demonstrated glucose-lowering effects in type 2 diabetes mellitus (T2DM) through stimulation of glucose-dependent insulin secretion. AREAS COVERED: This review is based on a PubMed search for all articles on fasiglifam and TAK-875. The pharmacology of fasiglifam is reviewed, focusing on studies in human volunteers and patients with T2DM. All published clinical trials with fasiglifam in T2DM are summarized, including two 12-week dose-ranging studies (one from Japan and the other from Central and North America), both of which employed glimepiride as an active comparator. EXPERT OPINION: Fasiglifam, a novel glucose-dependent insulin secretagogue, is the first GPR40 agonist to enter Phase III clinical evaluation. It has been shown to produce statistically significant and clinically relevant improvements in glycemic control in patients with early-stage T2DM. Furthermore, its tolerability and safety profile was comparable to placebo and no dose-related adverse effects were observed. Importantly, fasiglifam was comparable to placebo with regards to the incidence of hypoglycemia and it produced significantly fewer episodes compared with glimepiride. Fasiglifam is an interesting and novel oral anti-diabetic agent which may offer new avenues for treating T2DM, but clearly more thorough clinical evaluation is still needed.