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Clin Exp Pharmacol Physiol. 2018 Jul;45(7):628-635. doi: 10.1111/1440-1681.12953. Epub 2018 May 20.

Cardiovascular effects of sitagliptin - An anti-diabetes medicine.

Zhou Y1, Guo Z2,3, Yan W1, Wang W1,3.

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Department of Physiology and Pathophysiology, School of Basic Medical Sciences, Capital Medical University, Beijing, China.
Department of Pathophysiology, School of Basic Medicine, Jining Medical University, Shandong, China.
Beijing Key Laboratory of Metabolic Disorders Related Cardiovascular Diseases, Beijing, China.


Dipeptidyl-peptidase-4 (DPP-4) inhibitors, as the most recent available anti-diabetic agents, were generally used in clinical treatment of type 2 diabetes (T2DM). In addition to anti-diabetic effects, the five most widely used DPP-4 inhibitors (sitagliptin, vildagliptin, saxagliptin, linagliptin and alogliptin) also exert cardiovascular protective effects. In recent years, increasing studies suggest that sitagliptin shows pleiotropic impacts towards the cardiovascular system either with or without diabetes. In this review, we summarized the recent reports to provide an update discussion about cardiovascular protective effects of sitagliptin and the corresponding mechanisms. Sitagliptin has positive effects towards ischaemic cardiovascular diseases, atherosclerosis and hypertension. These effects are mainly conducted through DPP-4 inhibitions. In addition, sitagliptin exerts anti-inflammation, anti-oxidative stress, anti-apoptosis, mediation on lipid accumulation and so on, which also contribute to its cardiovascular effects.


cardiovascular effects; diabetes; dipeptidyl-peptidase-4 inhibitor; sitagliptin


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