Division of Endocrinology, Metabolism & Lipid Research, Washington University in St Louis School of Medicine, 660 South Euclid, Campus Box 8127, St Louis, MO 63110, USA.
Ther Adv Endocrinol Metab. 2012 Aug;3(4):113-24. doi: 10.1177/2042018812449406.
Patients with type 2 diabetes mellitus (T2DM) frequently require multiple therapies to effectively control hyperglycemia, and many new agents for glucose control have been developed over the past few decades. Linagliptin is a recently approved oral antidiabetic drug that acts by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4). Unlike other DPP-4 inhibitors, linagliptin is excreted chiefly via the enterohepatic system, and can be used without dose adjustment in patients with renal or hepatic impairment. Linagliptin was approved by the US Food and Drug Administration based on a large development program, including four pivotal trials in patients with T2DM, assessing the efficacy and safety of linagliptin when used as monotherapy or in combination with other oral antidiabetes drugs. Linagliptin was associated with significant improvements in glycosylated hemoglobin, fasting plasma glucose and postprandial glucose, and more patients receiving linagliptin showed meaningful improvements and achieved targets for glycosylated hemoglobin. Linagliptin was well tolerated, with an adverse event profile similar to that of placebo, and low rates of hypoglycemic events. Taken together, the pivotal trials confirm linagliptin is effective and safe in patients with T2DM: the convenience of oral dosing with no requirement for dose adjustment in patients with renal or hepatic impairment make linagliptin a valuable option when considering therapies for patients with T2DM.
2 型糖尿病（T2DM）患者常需采用多种疗法来有效控制高血糖，过去几十年中已开发出许多新的降糖药物。利拉利汀是一种最近获批的口服降糖药，通过抑制二肽基肽酶-4（DPP-4）发挥作用。与其他 DPP-4 抑制剂不同，利拉利汀主要通过肠肝系统排泄，因此在有肾或肝功能损害的患者中无需调整剂量。利拉利汀的获批基于一项大型研发项目，该项目包括四项在 T2DM 患者中开展的关键性试验，评估了利拉利汀作为单药或与其他口服降糖药联合使用时的疗效和安全性。研究结果显示，利拉利汀可显著改善糖化血红蛋白、空腹血糖和餐后血糖，更多接受利拉利汀治疗的患者血糖水平得到显著改善并达到了糖化血红蛋白目标。利拉利汀具有良好的耐受性，不良事件谱与安慰剂相似，且低血糖事件发生率较低。综上所述，关键性试验证实利拉利汀在 T2DM 患者中安全有效：该药口服给药方便，且在有肾或肝功能损害的患者中无需调整剂量，因此在考虑 T2DM 患者治疗方案时，利拉利汀是一种颇具价值的选择。
