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fasiglifam + sitagliptin
- Development stage
- Discontinued
- Lead developer
- Takeda
- Modality
- Small Molecules
- Administration
- Oral
01
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].
- Other names
- fasiglifam + sitagliptin
02
Targets
DPP-4 (Dipeptidyl Peptidase-IV)FFAR1 (Free fatty acid receptor 1)
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