Rosenwasser R F, Rosenwasser J N, Sutton D, Choksi R, Epstein B
East Coast Institute for Research, Jacksonville, Florida, USA.
American University of Antigua College of Medicine, New York, New York, USA.
Drugs Today (Barc). 2014 Nov;50(11):739-45. doi: 10.1358/dot.2014.50.11.2232267.
Diabetes mellitus impacts a substantial number of people worldwide and despite numerous antidiabetic medications available, approximately half of the drugs do not attain their recommended target, glycated hemoglobin (HbA1c). Recently, the kidney and its role in glucose reabsorption through the sodium/glucose cotransporter 2 (SGLT2) has been the target for novel antidiabetic treatments. Pharmacologic inhibition of SGLT2 in patients with diabetes results in increased urinary glucose excretion and decreased blood glucose levels, decreasing HbA1c levels. Tofogliflozin is the most selective SGLT2 inhibitor, with HbA1c reductions ranging from -0.44% to -0.99% throughout clinical studies, and it is well tolerated with a low rate of drug-related adverse events. Tofogliflozin has demonstrated efficacy and safety as monotherapy or as add-on to various antidiabetic agents, and it is currently undergoing phase IV clinical studies in Japanese patients with diabetes on background insulin therapy. Tofogliflozin is currently approved in Japan for use in patients with type 2 diabetes at a dose of 20 mg orally once daily in the morning, either before or after breakfast.
糖尿病影响着全球大量人口，尽管有多种抗糖尿病药物可供使用，但仍有约一半的药物无法达到推荐的糖化血红蛋白（HbA1c）目标。最近，肾脏及其通过钠/葡萄糖协同转运蛋白2（SGLT2）在葡萄糖重吸收中的作用已成为新型抗糖尿病治疗的靶点。对糖尿病患者的SGLT2进行药理抑制会导致尿糖排泄增加和血糖水平降低，从而降低HbA1c水平。托格列净是最具选择性的SGLT2抑制剂，在整个临床研究中HbA1c降低幅度为-0.44%至-0.99%，并且耐受性良好，药物相关不良事件发生率较低。托格列净已证明作为单药治疗或作为各种抗糖尿病药物的附加治疗具有疗效和安全性，目前正在日本接受胰岛素治疗的糖尿病患者中进行IV期临床研究。托格列净目前在日本被批准用于2型糖尿病患者，剂量为每日早晨口服20毫克，可在早餐前或早餐后服用。
