Drug intelligence / Profile preview

fasiglifam + glimepiride

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

Overview

**Fasiglifam + glimepiride** is a combination of two oral antidiabetic drugs: **fasiglifam (TAK-875)**, a selective **free fatty acid receptor 1 (FFAR1/GPR40) agonist**, and **glimepiride**, a sulfonylurea. Fasiglifam acts as an ago-allosteric modulator, activating FFAR1 primarily on pancreatic β-cells, resulting in *glucose-dependent potentiation of insulin secretion*. Glimepiride increases insulin release by binding to **ATP-sensitive potassium channels (KATP)** on β-cells, leading to cell depolarization and insulin exocytosis, but this mechanism is *not glucose-dependent* and can cause hypoglycemia. Studies show the combination provides additive glucose lowering with a low risk of severe hypoglycemia, as fasiglifam maintains normoglycemia even when glimepiride alone can induce hypoglycemia[1][3].

Other names
fasiglifamglimepiride
02

Targets

FFAR1 (Free fatty acid receptor 1)KATP channel (ATP-sensitive potassium channel)

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