核苷类抗乙肝病毒药物研究近况

Current status of anti-hepatitis B virus nucleoside analogues

主要根据 2 0 0 1年 11月 9～ 13日在美国德州达拉斯市召开的第 5 2届美国肝病学年会的内容对新一代核苷类抗乙肝病毒的药物作一介绍。在这次会议上报告了 7种新的核苷类抗乙肝药 ,已分别进入Ⅰ期 ,Ⅱ期和Ⅲ期临床试验阶段 ,其中阿德福韦、恩替卡韦和依曲西他平已在作Ⅲ期临床。但是阿得福韦的肾毒性 ,恩替卡韦的长期安全性和依曲西他平与拉米夫定的交叉耐药性在正式批准临床应用阶段需作进一步的观察。本文还阐述了核苷类药物结构与抗病毒活性的关系 。

This review is based upon the reports of 52 th American Association for the Study of Liver Disease (AASLD) which was held in Dallas, Texas, USA from 9-13, November, 2001. There were seven new anti-HBV nucleoside analogues presented in that meeting. Among those drugs, adefovir dipivoxil, entecavir and emtricitabine have undergone phase Ⅲ clinical trials. But the renal toxicity of adefovir, long-term safety of entecavir and cross-resistance between emtricitabine and lamivudine should do further observation before licensed and marketing.