Drug intelligence / Profile preview

fasiglifam + metformin

Development stage
Discontinued
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

**Fasiglifam + metformin** is an investigational oral combination therapy evaluated for treatment of type 2 diabetes mellitus. Fasiglifam (TAK-875) is a small molecule agonist of G-protein-coupled receptor 40 (GPR40, also known as free fatty acid receptor 1, FFAR1), designed to enhance glucose-dependent insulin secretion without causing significant hypoglycemia or weight gain. Metformin is a well-established oral antihyperglycemic agent that primarily reduces hepatic glucose production and improves insulin sensitivity. The combination was studied to provide additive or synergistic effects for glycemic control. However, clinical development was terminated due to liver safety concerns with fasiglifam. The main developer was Takeda.

Other names
fasiglifam + metforminTAK-875 + metformin
02

Targets

FFAR1 (Free fatty acid receptor 1)AMPK (Adenosine monophosphate–activated protein kinase)GPD2 (Glycerol-3-phosphate dehydrogenase 2)

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