University of New Mexico Health Sciences Center, College of Pharmacy, MSC 09 5360, 1 University of New Mexico, Albuquerque, NM 87131-0001, USA.
Expert Opin Investig Drugs. 2011 Oct;20(10):1435-43. doi: 10.1517/13543784.2011.606214. Epub 2011 Aug 20.
Treatment of chronic hepatitis C virus (HCV) is limited by substantial side effects including ribavirin-induced hemolytic anemia. Taribavirin, a ribavirin prodrug, was designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the subsequent development of hemolytic anemia.
The objective of the review is to evaluate the efficacy and safety of taribavirin as compared with ribavirin in the treatment of chronic HCV infections. A PubMed search was performed using the following key words: viramidine, taribavirin and ribavirin analog. Additional sources included press releases on preliminary results of clinical trials of taribavirin and abstracts presented at international meetings. The literature suggests that weight-based dosing of taribavirin at 25 mg/kg demonstrates lower rates of hemolytic anemia with comparable rates of sustained virologic response (SVR) and is the optimum dose for further studies comparing the efficacy of taribavirin with weight-based dosing of ribavirin.
Failure to eradicate HCV may be associated with extrahepatic viral replication. The dosing strategy of taribavirin favors concentration within the liver to reduce treatment-limiting rates of anemia but may be insufficient to prevent virologic relapse.
慢性丙型肝炎病毒（HCV）的治疗受到严重副作用的限制，包括利巴韦林引起的溶血性贫血。利巴韦林前体药物替拉瑞韦旨在集中在肝脏内以靶向感染 HCV 的肝细胞，同时最大限度地减少在红细胞（RBC）中的分布，从而减少随后发生的溶血性贫血。
本综述的目的是评估替拉瑞韦与利巴韦林相比在治疗慢性 HCV 感染方面的疗效和安全性。使用以下关键词在 PubMed 上进行了搜索：viramidine、替拉瑞韦和利巴韦林类似物。其他来源包括替拉瑞韦临床试验初步结果的新闻稿和国际会议上的摘要。文献表明，替拉瑞韦的剂量为 25mg/kg，根据体重计算，溶血性贫血的发生率较低，持续病毒学应答（SVR）的发生率相当，是进一步比较替拉瑞韦与利巴韦林根据体重计算的疗效的最佳剂量。
未能清除 HCV 可能与肝外病毒复制有关。替拉瑞韦的给药策略有利于在肝脏内集中，以降低治疗相关贫血的发生率，但可能不足以防止病毒学复发。
