新型葡萄糖激酶激活剂HMS5552研究进展

Recent progress in the novel glucokinase activator HMS5552

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.