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Drugs. 2017 Feb;77(2):209-224. doi: 10.1007/s40265-016-0686-9.
The dipeptidyl peptidase-4 inhibitor sitagliptin (Januvia; Glactiv; Tesavel; Xelevia™) is approved in more than 130 countries worldwide as monotherapy and in combination with other antihyperglycaemic drugs for the treatment of adult patients with type 2 diabetes (T2D). Extensive clinical experience has firmly established the glycaemic efficacy of oral sitagliptin (±other antihyperglycaemic drugs) in a broad spectrum of patients with T2D, including obese, elderly and renally impaired patients and those with established cardiovascular (CV) disease (CVD). Sitagliptin is generally well tolerated, with most adverse events being of mild to moderate intensity and relatively few patients discontinuing treatment because of these events. Sitagliptin treatment was not associated with an increased risk for the known CVD risk factors of hypoglycaemia and bodyweight gain. Of note, in the TECOS CV safety trial in patients with T2D and established CVD, sitagliptin was noninferior to placebo in terms of the risk of the 4-point major adverse cardiac event (MACE) outcome, with no increased risk in hospitalization for heart failure. Albeit discussion is equivocal regarding the potential increased risk of pancreatitis and pancreatic cancer with incretin-based therapies (including sitagliptin), no causal link between incretin-based drugs and these events has been established to date. With its convenient once-daily oral regimen, low potential for pharmacokinetic drug-drug interactions and good efficacy and safety profiles, including CV safety, sitagliptin remains an important option in the management of patients with T2D.
二肽基肽酶-4 抑制剂西格列汀（捷诺维；加立维；泰格列净；百达扬）已在全球 130 多个国家被批准作为单药治疗以及与其他抗高血糖药物联合用于治疗 2 型糖尿病（T2D）成人患者。广泛的临床经验已明确确立了口服西格列汀（±其他抗高血糖药物）在 T2D 广泛患者中的血糖疗效，包括肥胖、老年和肾功能受损患者以及已患有心血管疾病（CVD）的患者。西格列汀通常具有良好的耐受性，大多数不良反应为轻度至中度，且由于这些不良反应而停止治疗的患者相对较少。西格列汀治疗与已知的 CVD 危险因素低血糖和体重增加无关。值得注意的是，在 T2D 和已患有 CVD 的患者中进行的 TECOS CV 安全性试验中，西格列汀在 4 点主要不良心脏事件（MACE）结局方面与安慰剂相比非劣效，且心力衰竭住院风险无增加。尽管关于基于肠促胰岛素的治疗（包括西格列汀）可能增加胰腺炎和胰腺癌风险的讨论尚无定论，但迄今为止尚未确定肠促胰岛素类药物与这些事件之间存在因果关系。西格列汀具有方便的每日一次口服给药方案、潜在的药代动力学药物相互作用风险低以及良好的疗效和安全性特征，包括 CV 安全性，因此仍然是 T2D 患者管理的重要选择。
