摘要
大量基础研究已证明,葡萄糖激酶激活剂(GKA)可不同程度提高葡萄糖激酶(GK)活性,有效降低血糖,但在临床试验中多数却因降糖效应不佳或不良反应明显而停滞不前。HMS5552作为第4代新型GKA,具备较好的药代动力学及酶动力学特征,在健康受试者及2型糖尿病患者身上均显示出良好的安全性及耐受性。HMS5552单药治疗可显著降低HbA1c,对胰岛β细胞具有持续保护作用。HMS5552已率先进入Ⅲ期确证性临床研究阶段,目前Ⅲ期试验正在进行中。
Mounting basic studies have proved that glucokinase activator(GKA)can improve glucokinase(GK)activation to varying degrees and effectively reduce blood glucose.In clinical trials,however,most of them stagnated due to quite limited efficacy of glucose reduction or noteworthy side effects.As the fourth generation of GKA,HMS5552 has excellent pharmacokinetic properties and enzyme kinetics.It is safe and well tolerated both in healthy volunteers and type 2 diabetes patients.HMS5552 monotherapy could significantly reduce HbA1c and demonstrate a lasting effect on improving and protectingβcell function in the meanwhile.Dorzagliatin(HMS5552)has taken the lead in entering phaseⅢconfirmatory clinical trial that is under way at the moment.
作者
常明星
顾天伟
朱大龙
Chang Mingxing;Gu Tianwei;Zhu Dalong(Nanjing Drum Tower Hospital,Graduate School of Peking Union Medical College and Chinese Academy of Medical Science,Nanjing 210008,China;Department of Endocrinology,Drum Tower Hospital Affiliated to Nanjing University Medical School,Nanjing 210008,China)
出处
《国际内分泌代谢杂志》
2020年第4期258-261,共4页
International Journal of Endocrinology and Metabolism
基金
江苏省重点研发计划(社会发展)重点病种规范化诊疗项目(BE2015604)
江苏省卫生计生委医学科研课题(Q2017006)。