治疗2型糖尿病新药canagliflozin

Canagliflozin,a new drug for treating type 2 diabetes mellitus

Canagliflozin是一种钠-葡萄糖协同转运蛋白2抑制剂,能够阻断肾近曲小管对葡萄糖的重吸收,进而降低肾糖阈,增加尿糖排泄,降低血糖水平,是一种具有全新作用机制的降糖药物,临床上用于治疗2型糖尿病。多个临床前及临床研究证实其对2型糖尿病有明显疗效,可以显著改善患者的血糖水平,对体重、血脂等也有良性改善。不良反应主要有泌尿生殖道感染,发生率达10%,较少出现低血糖反应,不良反应总体较轻,患者耐受性良好。文中对canagliflozin的作用机制、药效学、药动学、药物相互作用、临床评价和安全性等进行综述。

Canagliflozin is an inhibitor of sodium-glucose co-transporter-2. Canagliflozin lowers renal threshold for glucose reabsorption and increases urinary glucose excretion, resulting in decreased plasma glucose in patients with hyperglycaemia. Also, it has effects of mild osmotic diuresis and net caloric loss （by loss of glucose） , promoting weight loss. Canagliflozin is a new antidiabetic drug for symptomatic treatment of type 2 diabetes mellitus in adult patients with a novel mechanism of action. In patients receiving insulin and oral antihyperglycaemic therapy, canagliflozin is well tolerated without evidence for glucose malabsorption, and its pharmacokinetic characteristics are consistent with once-daily dosing. Adverse effects of canagliflozin reported in clinical trials include urinary tract and genital infections, occurring in about 10% of patients. The mechanism, pharmacodynamics, pharmacokinetics, drug interaction, clinical evaluation, and safety of canagliflozin were reviewed.