5种DPP-4抑制剂分子结构差异及药代动力学特性

Molecular Structure Differences and Pharmacokinetic Characteristics of Five DPP-4 inhibitors

二肽基肽酶-4 (Dipeptidyl peptidase-4,DPP-4)抑制剂是近年上市的治疗2型糖尿病的新型口服降糖药,其作用机制独特,以葡萄糖依赖性促进胰岛B细胞分泌胰岛素,同时抑制胰岛α细胞分泌胰高血糖素,可有效降低血糖,减少低血糖发作,同时不增加体重,被临床广泛应用。本文将对常见的5种DPP-4抑制剂的化学结构、亲和力、选择性差异、药代动力学特性及特殊人群用药逐项进行分析,因为尽管都是口服小分子化合物,但其化学结构、对DPP-4的亲和力、选择性、吸收、分布、代谢和排泄等药代动力学特性各异,以便为临床合理用药提供参考。

The dipeptidyl peptidase(DPP)-4 inhibitors are a new class of antihyperglycaemic agents which were developed for the treatment of type 2 diabetes.Glucose-dependent insulin secretion byβislet cells was promoted,meanwhile,glucagon secretion byαislet cells was inhibited,with unique mechanism.It can effectively reduce blood sugar,the risk of hypoglycemia and does not increase weight,therefore,it is widely used in clinical.Although they are all small molecules which are orally available,they differ in terms of their chemistry,affinity and selectivity of DPP-4,absorption,distribution,metabolism and elimination of pharmacokinetic characteristics.Thus,in order to provide reference for clinical rational drug use,the chemical structure,affinity,selectivity,pharmacokinetic characteristics and pharmacokinetic in special population of five DPP-4 inhibitors were analyzed.