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fasiglifam + sitagliptin

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

Overview

**Fasiglifam + sitagliptin** is a combination of the G-protein-coupled receptor 40 agonist fasiglifam (TAK-875) and the dipeptidyl peptidase-4 inhibitor sitagliptin. Designed for the treatment of type 2 diabetes, this combination acts synergistically: fasiglifam enhances glucose-dependent insulin secretion by activating free fatty acid receptor 1 (FFAR1/GPR40), while sitagliptin inhibits DPP-4, prolonging the activity of incretin hormones (GLP-1 and GIP) to increase insulin and reduce glucagon release. Clinical trials demonstrated improved glycemic control without increased hypoglycemia risk. Fasiglifam development was terminated due to liver toxicity concerns, hence this combination is not marketed[1][3][6][7].

Brand names: Januvia
Other names: fasiglifam + sitagliptin

Targets

DPP-4 (Dipeptidyl Peptidase-IV)FFAR1 (Free fatty acid receptor 1)

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