Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand.
Division of Diabetes, Nutrition and Metabolic Disorders, Department of Medicine, CHU Liège, University of Liège, Liège, Belgium.
Drugs. 2017 Sep;77(14):1577-1592. doi: 10.1007/s40265-017-0801-6.
Canagliflozin (Invokana) is a sodium-glucose co-transporter-2 (SGLT2) inhibitor indicated in various countries worldwide for the once-daily oral treatment of type 2 diabetes (T2D). Canagliflozin lowers blood glucose levels independently of insulin, with the inhibition of SGLT2 reducing renal reabsorption of glucose and increasing excretion of glucose in the urine. In well-designed clinical trials, canagliflozin (as first-line monotherapy or add-on therapy to other antihyperglycaemic agents) improved glycaemic control in adults with T2D, including those of older age and/or at high cardiovascular (CV) risk, and also had beneficial effects on their bodyweight and blood pressure (BP). CV risk reduction, as well as possible renal benefits, were also seen with canagliflozin in T2D patients at high CV risk in the CANVAS Program, an integrated analysis of two large CV outcomes studies. Canagliflozin was generally well tolerated, had a low risk of hypoglycaemia and was most commonly associated with adverse events such as genital and urinary tract infections and increased urination, consistent with its mechanism of action. Although the amputation and fracture risk observed among recipients of the drug require further investigation, canagliflozin is an important option for T2D management in adults.
卡格列净(Invokana)是一种钠-葡萄糖共转运蛋白 2(SGLT2)抑制剂,在世界范围内的多个国家被批准用于每日口服治疗 2 型糖尿病(T2D)。卡格列净可独立于胰岛素降低血糖水平,通过抑制 SGLT2 减少肾脏对葡萄糖的重吸收,并增加尿液中葡萄糖的排泄。在精心设计的临床试验中,卡格列净(作为一线单药治疗或与其他抗高血糖药物联合治疗)改善了 T2D 成人的血糖控制,包括年龄较大和/或心血管(CV)风险较高的患者,同时对其体重和血压(BP)也有有益影响。在 CANVAS 计划中,对两项大型 CV 结局研究的综合分析显示,卡格列净还可降低 T2D 高 CV 风险患者的 CV 风险,并可能带来肾脏获益。卡格列净通常具有良好的耐受性,低血糖风险低,最常与不良事件相关,如生殖器和尿路感染以及排尿增多,与其作用机制一致。尽管该药物使用者的截肢和骨折风险需要进一步研究,但卡格列净是成人 T2D 管理的重要选择。