Maulana Azad Medical College, New Delhi, India.
J Clin Pharmacol. 2012 Apr;52(4):457-63. doi: 10.1177/0091270011400604. Epub 2011 May 4.
The incidence of type 2 diabetes mellitus is increasing worldwide. The existing therapeutic classes of antidiabetic drugs are not adequately effective in maintaining long-term glycemic control in most patients, even when used in combination. One emerging novel therapeutic class of antidiabetic drugs is sodium glucose cotransporter 2 (SGLT2) inhibitors. SGLT2 accounts for 90% of the glucose reabsorption in the kidney. The SGLT2 inhibitors increase urinary excretion of glucose and lower plasma glucose levels in an insulin-independent manner. Dapagliflozin, the most prominent molecule in this class, is currently in a phase III clinical trial. Other members of this class (eg, sergliflozin, remogliflozin) are also in different phases of clinical trials. This class of novel agents can effectively control blood sugar level without producing weight gain or hypoglycemia. Results of ongoing phase III clinical trials are crucial to determine whether the risk-benefit ratio will allow approval of this new class of drugs for the management of type 2 diabetes mellitus.
2 型糖尿病的发病率在全球范围内呈上升趋势。现有的抗糖尿病药物治疗类别在大多数患者中不能有效地维持长期血糖控制，即使联合使用也是如此。一类新兴的抗糖尿病药物治疗类别是钠-葡萄糖共转运蛋白 2（SGLT2）抑制剂。SGLT2 占肾脏葡萄糖重吸收的 90%。SGLT2 抑制剂以不依赖胰岛素的方式增加尿葡萄糖排泄并降低血浆葡萄糖水平。达格列净是该类药物中最突出的分子，目前正在进行 III 期临床试验。该类药物的其他成员（如，恩格列净、瑞格列净）也处于不同的临床试验阶段。这类新型药物可有效控制血糖水平，而不会导致体重增加或低血糖。正在进行的 III 期临床试验的结果对于确定该新药类的风险效益比是否允许批准用于 2 型糖尿病的管理至关重要。
