Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used for the management of type 2 diabetes mellitus. The effect of this medication leads to glucose dependent increases in insulin and decreases in glucagon to improve control of blood sugar.
- Mechanism
- Curator reviewed
Inhibition of DPP-4 by sitagliptin slows DPP-4 mediated inactivation of incretins like GLP-1 and GIP. Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasis. Reduced inhibition of incretins increase insulin synthesis and decrease glucagon release in a manner dependant on glucose concentrations. These effects lead to an overall increase in blood glucose control which is demonstrated by reduced glycosylated hemoglobin (HbA1c).
- Primary indication
- Sitagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.Curator reviewed · 3 structured indications
- Formula / weight
- C16H15F6N5O · 407.3136 g/mol (avg)
- First approval
- Canada, 2007 · United States, 2006 · European Union, 2016
- Code names
- LEZ-763
- Brand names
Resolves to
MFFMDFFZMYYVKS-SECBINFHSA-NSMILESN[C@@H](CC(=O)N1CCN2C(C1)=NN=C2C(F)(F)F)CC1=CC(F)=C(F)C=C1FWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Sitagliptin, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account