Incretin mimetics and dipeptidyl peptidase-4 inhibitors: innovative treatment therapies for type 2 diabetes
Incretin mimetics and dipeptidyl peptidase-4 inhibitors: innovative treatment therapies for type 2 diabetes
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DOI：
10.1590/s0004-27302008000600016
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发表时间：
2008-08-01
期刊：
影响因子：
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通讯作者：
Gross, Jorge L.
中科院分区：
文献类型：
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作者：
Davidson, Jaime A.;Parente, Erika B.;Gross, Jorge L.
糖尿病和葡萄糖耐量受损的患病率预计将在未来二十年内急剧增加。2型糖尿病（T2 DM）的临床治疗传统上包括生活方式改变、口服降糖药和最终开始胰岛素治疗。在这份报告中，我们回顾了两种创新的T2 DM治疗方法的临床试验结果，这些方法基于肠促胰岛素激素的血糖调节作用。肠促胰岛素模拟物是模拟胰高血糖素样肽-1（GLP-1）的几种作用的肽类药物，已显示可降低T2 DM患者的糖化血红蛋白（A1 C）水平。此外，肠促胰岛素模拟物降低餐后和空腹血糖，抑制胰高血糖素释放升高，并与进行性体重减轻相关。二肽基肽酶-4（DPP-4）抑制剂通过抑制GLP-1的酶降解来增加内源性GLP-1水平。在T2 DM患者中进行的临床研究表明，DPP-4抑制剂可降低A1 C升高，降低餐后和空腹血糖，抑制胰高血糖素释放，并且体重中性。总体而言，这些新药与其他降糖药物（如二甲双胍、磺脲类和/或噻唑烷二酮类）联合给药，可帮助血糖控制不佳的T2 DM患者恢复血糖稳态。
The prevalence of diabetes and impaired glucose tolerance is predicted to dramatically increase over the next two decades. Clinical therapies for type 2 diabetes mellitus (T2DM) have traditionally included lifestyle modification, oral anti-diabetic agents, and ultimately insulin initiation. In this report, we review the clinical trial results of two innovative T2DM treatment therapies that are based on the glucoregulatory effects of incretin hormones. Incretin mimetics are peptide drugs that mimic several of the actions of glucagon-like peptide-1 (GLP-1) and have been shown to lower glycated hemoglobin (A1C) levels in patients with T2DM. Additionally, incretin mimetics lower postprandial and fasting glucose, suppress elevated glucagon release, and are associated with progressive weight reduction. Dipeptidyl peptidase-4 (DPP-4) inhibitors increase endogenous GLP-1 levels by inhibiting the enzymatic degradation of GLP-1. Clinical studies in patients with T2DM have shown that DPP-4 inhibitors reduce elevated A1C, lower postprandial and fasting glucose, suppress glucagon release, and are weight neutral. Collectively, these new drugs, given in combination with other antidiabetic agents, such as metformin, sulfonylureas, and/or thiazolidinediones, can help restore glucose homeostasis in poorly controlled patients, with T2DM.