二肽基肽酶-4(DPP-4)抑制剂是一类口服抗糖尿病药物,可改善2型糖尿病(T2DM)患者的血糖控制,而不会引起体重增加或增加低血糖风险。八种可用的DPP-4抑制剂,包括阿格列汀,安格列汀,吉格列汀,利拉列汀,沙格列汀,西格列汀,teneligliptin,还有维格列汀,是口服使用的小分子,在T2DM患者中具有相同的作用机制和相似的安全性。DPP-4抑制剂可作为单一疗法或与其他口服降糖药如二甲双胍、噻唑烷二酮,或磺酰脲类。尽管DPP-4抑制剂具有相同的作用模式,它们在一些重要的药代动力学和药效学特性上不同,这些特性在某些患者中可能与临床相关.八种gliptins之间的主要区别包括:效力,目标选择性,口服生物利用度,消除半衰期,结合血浆蛋白,代谢途径,活性代谢物的形成,主要排泄途径,肾和肝功能不全的剂量调整,和潜在的药物-药物相互作用。选择性DPP-4抑制剂的脱靶抑制是多器官毒性的原因,如免疫功能障碍,受损的愈合,和皮肤反应。作为一个药物类别,DPP-4抑制剂由于其优异的耐受性而在临床实践中被接受,低血糖的风险很低,对体重的中性影响,和每日一次给药。目前尚不清楚DPP-4抑制剂是否可以预防疾病进展。当密切监测DPP-4抑制剂的潜在毒性时,需要更多的临床研究来验证DPP-4抑制剂治疗T2DM的最佳方案。
Dipeptidyl peptidase-4 (DPP-4) inhibitors are a class of oral antidiabetic drugs that improve glycaemic control without causing weight gain or increasing hypoglycaemic risk in patients with type 2 diabetes mellitus (T2DM). The eight available DPP-4 inhibitors, including alogliptin, anagliptin,
gemigliptin, linagliptin, saxagliptin, sitagliptin, teneligliptin, and vildagliptin, are small molecules used orally with identical mechanism of action and similar safety profiles in patients with T2DM. DPP-4 inhibitors may be used as monotherapy or in double or triple combination with other oral glucose-lowering agents such as metformin, thiazolidinediones, or sulfonylureas. Although DPP-4 inhibitors have the same mode of action, they differ by some important pharmacokinetic and pharmacodynamic properties that may be clinically relevant in some patients. The main differences between the eight gliptins include: potency, target selectivity, oral bioavailability, elimination half-life, binding to plasma proteins, metabolic pathways, formation of active metabolite(s), main excretion routes, dosage adjustment for renal and liver insufficiency, and potential drug-drug interactions. The off-target inhibition of selective DPP-4 inhibitors is responsible for multiorgan toxicities such as immune dysfunction, impaired healing, and skin reactions. As a drug class, the DPP-4 inhibitors have become accepted in clinical practice due to their excellent tolerability profile, with a low risk of hypoglycaemia, a neutral effect on body weight, and once-daily dosing. It is unknown if DPP-4 inhibitors can prevent disease progression. More clinical studies are needed to validate the optimal regimens of DPP-4 inhibitors for the management of T2DM when their potential toxicities are closely monitored.