Diabetes is a ubiquitous chronic disease worldwide. The prevalence is expected to increase further to 9.9% by the year 2045. Dipeptidyl peptidase-4 (DPP-4) inhibitors, also called as gliptins, act as incretin enhancers. They inhibit glucagon secretion and arouse postprandial insulin secretion, both in a glucose-dependent mode. In 2006, sitagliptin was approved as a first DPP-4 inhibitor in the treatment of diabetes concurrently with lifestyle modification. Sitagliptin has a high bioavailability, while linagliptin has a safety and tolerability profile similar to that of placebo, with a very low risk for hypoglycemia. DPP-4 inhibitors have a weight neutrality effect. One major benefit of gliptins is their excellent tolerability/safety profile compared with other glucose-lowering medications, including other new glucose-lowering agents such as sodium/glucose cotransporter 2 inhibitors. Compared with sulfonylureas, they have a smaller decline in HbA1c. The three gliptins showed excellent effect on glycemic control as an add-on therapy in treating type 2 diabetes. The major adverse cardiovascular events, malignancy and pancreatitis, were not associated with the treatment with sitagliptin, a DPP-4 inhibitor. The objective of establishing cardiovascular safety trials such as SAVOR-TIMI 53, EXAMINE, TECOS, CAROLINA, and CARMELINA. DPP-4 inhibitors have higher rates of adherence and persistence compared with sulfonylureas and thiazolidinediones.

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二肽基肽酶 4 抑制剂对血糖控制和心血管安全的影响与依从性：概述

糖尿病是世界范围内普遍存在的慢性病。预计到 2045 年，流行率将进一步增加到 9.9%。二肽基肽酶-4 (DPP-4) 抑制剂，也称为格列汀，充当肠促胰岛素增强剂。它们以葡萄糖依赖性方式抑制胰高血糖素分泌并引起餐后胰岛素分泌。2006 年，西格列汀被批准作为第一个 DPP-4 抑制剂，用于治疗糖尿病并改变生活方式。西格列汀的生物利用度高，而利格列汀的安全性和耐受性与安慰剂相似，发生低血糖的风险非常低。DPP-4 抑制剂具有重量中和作用。与其他降糖药物相比，格列汀的一个主要好处是其优异的耐受性/安全性，包括其他新的降糖剂，如钠/葡萄糖协同转运蛋白 2 抑制剂。与磺脲类相比，它们的 HbA1c 下降幅度较小。这三种格列汀作为治疗 2 型糖尿病的附加疗法对血糖控制显示出极好的效果。主要的心血管不良事件、恶性肿瘤和胰腺炎与 DPP-4 抑制剂西格列汀的治疗无关。建立心血管安全性试验的目标，如 SAVOR-TIMI 53、EXAMINE、TECOS、CAROLINA 和 CARMELINA。与磺酰脲类和噻唑烷二酮类药物相比，DPP-4 抑制剂具有更高的依从性和持久性。这三种格列汀作为治疗 2 型糖尿病的附加疗法对血糖控制显示出极好的效果。主要的心血管不良事件、恶性肿瘤和胰腺炎与 DPP-4 抑制剂西格列汀的治疗无关。建立心血管安全性试验的目标，如 SAVOR-TIMI 53、EXAMINE、TECOS、CAROLINA 和 CARMELINA。与磺酰脲类和噻唑烷二酮类药物相比，DPP-4 抑制剂具有更高的依从性和持久性。这三种格列汀作为治疗 2 型糖尿病的附加疗法对血糖控制显示出极好的效果。主要的心血管不良事件、恶性肿瘤和胰腺炎与 DPP-4 抑制剂西格列汀的治疗无关。建立心血管安全性试验的目标，如 SAVOR-TIMI 53、EXAMINE、TECOS、CAROLINA 和 CARMELINA。与磺酰脲类和噻唑烷二酮类药物相比，DPP-4 抑制剂具有更高的依从性和持久性。