[摘要] 二肽基肽酶-4(DPP-4)抑制剂是一类新型口服降糖药，自上市以来，其降糖疗效得到广泛认可，同时具有低血糖风险小、不增加体重、服用方便等优势。此外，DPP-4抑制剂具有独立于降糖之外的心血管保护作用——降压、降脂、抗炎、抗动脉粥样硬化及改善心功能等。既往回顾性研究证实，DPP-4抑制剂可降低心血管风险，但因其研究设计的局限性，证据级别尚显不足。自2008年美国FDA公布新上市降糖药物心血管安全性的要求后，大量前瞻性的以心血管事件为终点的DPP-4抑制剂临床试验逐渐开展起来，其中，沙格列汀的SAVOR及阿格列汀的EXAMINE研究最早公布结果，结果提示均不增加心血管风险。但这两个试验也发现了一个特殊信号，即因心力衰竭导致的住院率增加。未来，还会有更多的试验公布，如西格列汀的TECOS研究，利格列汀的CAROLINA研究，期待这些结果能为T2DM伴心血管疾病及高危患者治疗药物的选择提供更多强有力的循证医学证据。

　　[关键词]二肽基肽酶-4抑制剂;糖尿病，2型;心血管疾病;药物评价

　　[Abstract] Dipeptidyl peptidase-4(DPP-4)inhibitors is a new kind oral anti-diabetic medicine, with good glucose lowering effect, as well as low risk of hypoglycemia, no weight gain, easy to use. In addition, it is with cardiovascular protection which beyond glucose lowering, such as: anti-hypertension, lipids lowering, anti-inflammation, anti-atherosclerosis, improving cardiac function etc. Previous retrospective studies demonstrated that DPP-4 inhibitors can reduce cardiovascular risks, but with the limitations of the study design, the evidence is not powerful enough. Since the FDA released new requirement for new anti-diabetic drug in 2008, many prospective clinical trials which using cardiovascular events as primary endpoint has been launched. SAVOR study and EXAMINE study are first to release the results, bothdemonstrated that saxagliptin and alogliptin do not increase CV risks.But an unexpected signal came out, that is increasing hospitalization for heart failure which needs continuous attention. More study results will be release later in future, including TECOS of sitagliptin and CAROLINA of linagliptin, hope they can be robust clinical evidence for the treatment choice of T2DM with CVD and high CV risk patients.

　　[Key words]Dipeptidyl peptidase-4(DPP-4)inhibitors; Diabetes mellitus, type 2;Cardiovascular diseases;Drug evaluation