Crepaldi G, Carruba M, Comaschi M, Del Prato S, Frajese G, Paolisso G
Department of Medical and Surgical Sciences, University of Padua, 35128 Padua, Italy.
J Endocrinol Invest. 2007 Jul-Aug;30(7):610-4. doi: 10.1007/BF03346357.
Dipeptidyl peptidase 4 (DPP-4) inhibitors are a new pharmacological class of drugs for treating Type 2 diabetes. They improve the capacity of the organism to control glycemia by increasing the levels of active incretins. Their mechanism of action is thus radically different from those of other anti-diabetic drugs currently available. DDP-4 inhibitors use a physiological mechanism to control hyperglycemia, by stimulating the secretion of insulin from beta-cells, decreasing the secretion of glucagon from pancreatic alpha-cells, and at the same time reducing the production of glucose by the liver. DDP-4 inhibitors have shown significant efficacy in maintaining reduced levels of glycosylated hemoglobin for up to 1 year. In vitro and animal studies have shown that they can inhibit apoptosis of beta-cells and favor their regeneration and differentiation. The oral DPP-4 inhibitors vildagliptin, sitagliptin, and saxagliptin are efficacious both alone and in association with other oral anti-diabetic agents and may be administered in a single daily dose. Lastly, they have substantial advantages with respect to other anti-diabetic drugs, since they involve a low risk of hypoglycemia and do not affect body weight.
二肽基肽酶4（DPP-4）抑制剂是一类用于治疗2型糖尿病的新型药物。它们通过提高活性肠促胰岛素水平来增强机体控制血糖的能力。因此，其作用机制与目前可用的其他抗糖尿病药物截然不同。DPP-4抑制剂利用一种生理机制来控制高血糖，即刺激β细胞分泌胰岛素，减少胰腺α细胞分泌胰高血糖素，同时减少肝脏葡萄糖生成。DPP-4抑制剂在长达1年的时间里维持糖化血红蛋白水平降低方面显示出显著疗效。体外和动物研究表明，它们可以抑制β细胞凋亡并促进其再生和分化。口服DPP-4抑制剂维格列汀、西他列汀和沙格列汀单独使用或与其他口服抗糖尿病药物联合使用均有效，且可每日单次给药。最后，与其他抗糖尿病药物相比，它们具有显著优势，因为它们导致低血糖的风险较低且不影响体重。
