Università di Napoli Federico II, Dipartimento di Medicina Pubblica e Sicurezza Sociale, Sezione di Malattie Infettive (Ed. 18), 80131 Naples, Italy.
Expert Opin Investig Drugs. 2010 Jan;19(1):151-9. doi: 10.1517/13543780903501505.
Hepatitis C virus (HCV) is the main agent of chronic hepatitis, liver cirrhosis and hepatocellular carcinoma in the western world. It affects more than 170 million people worldwide. HCV treatment, based on the combination of Peg-interferon and ribavirin, is effective in about 50% of treated patients. Therefore, there is a need to develop new drugs active against HCV.
Data were obtained by searching for all full articles on Medline and abstracts presented at major international congresses on viral hepatitis.
A review of clinical data about the efficacy and safety of telaprevir (VX-950), the HCV protease inhibitor that is in the most advanced phase of clinical development.
Telaprevir has an acceptable pharmacokinetic profile and seems to be a potent antiviral drug against HCV, although, owing to a low genetic barrier, resistant variants emerge within a few days when used in monotherapy, thereby decreasing its efficacy. Consequently, telaprevir has been combined with pegylated-interferon and ribavirin in clinical trials. This triple combination is more effective but has a higher rate of adverse events (notably rash) than the standard of care, despite the shorter duration of therapy.
丙型肝炎病毒（HCV）是在西方国家慢性肝炎、肝硬化和肝细胞癌的主要病原体。它影响全球超过 1.7 亿人。基于聚乙二醇干扰素和利巴韦林联合治疗 HCV，在约 50%的治疗患者中是有效的。因此，有必要开发针对 HCV 的新药。
通过在 Medline 上搜索所有关于 HCV 的全文文章，并对主要国际病毒性肝炎大会上的摘要进行检索，获得了数据。
telaprevir（VX-950）的临床疗效和安全性的综述，telaprevir 是处于临床开发最先进阶段的 HCV 蛋白酶抑制剂。
telaprevir 具有可接受的药代动力学特征，似乎是一种针对 HCV 的有效抗病毒药物，但由于遗传屏障低，当单独使用时，在几天内就会出现耐药变异体，从而降低其疗效。因此，telaprevir 已在临床试验中与聚乙二醇干扰素和利巴韦林联合使用。这种三联疗法比标准护理更有效，但不良反应（尤其是皮疹）的发生率更高，尽管治疗时间更短。
