BILN2061、telaprevir和boceprevir治疗慢性丙型肝炎临床疗效比较

摘要

HCV感染易导致慢性肝炎、肝硬化及肝癌等相关性疾病,病死率较高.HCV在体内的翻译是经宿主信号肽和非结构蛋白(non-structural protein,NS)3病毒蛋白酶水解成熟.此外,NS3还可直接破坏宿主细胞,抑制其对干扰素的应答,因此研究HCV NS3具有重要的临床意义.本文通过对3种NS3/4A蛋白酶抑制剂(BILN 2061、telaprevir和boceprevir)的药理作用、药动学与代谢、安全性和临床研究进行分析,总结其作用特性和临床疗效.同时,对boceprevir和telaprevir(VX-950)分别联合聚乙二醇干扰素和利巴韦林的疗效进行评价,为临床医生治疗慢性丙型肝炎提供指导.%HCV infection can easily cause chronic hepatitis, liver cirrhosis, liver cancer and other related diseases, with high mortality. HCV RNA translation is stimulated in the body by both host signal peptidase and HCV-encoded proteases non-structural protein (NS)3 to generate mature protein products. In addition, NS3 can damage host cells directly and inhibit the response to interferon. Therefore, it is of clinical significance in the study of HCV NS3. This paper aims to summarize characteristics and clinical efficacy of 3 kinds of NS3/4A protease inhibitors (BILN 2061, telaprevir and boceprevir) by analyzing the pharmacological functions, pharmacokinetics and metabolism, safety and clinical research of the 3 kinds of inhibitors. Meanwhile, the therapeutic efficacy of boceprevir or telaprevir (VX-950) combined with pegylated interferon and ribavirin is evaluated and the recent progress in the treat ment of chronic hepatitis C (CHC) is introduced, so as to provide guidance for clinicians in the treatment of CHC.