Amarapurkar Deepak N
Department of Gastroenterology and Hepatology, Bombay Hospital & Medical Research Centre, Mumbai 400025, India.
World J Gastroenterol. 2007 Dec 14;13(46):6150-5. doi: 10.3748/wjg.v13.i46.6150.
Three hundred and fifty million people worldwide are estimated to be chronically infected with hepatitis B virus. 15%-40% of these subjects will develop cirrhosis, liver failure or hepatocellular carcinoma during their life. The treatment of chronic hepatitis B has improved dramatically over the last decade merits to the advent of nucleoside/nucleotide analogues and the use of pegylated interferons. Approved drugs for chronic hepatitis B treatment include: standard interferon-alpha 2b, pegylated interferon-alpha 2a, lamivudine, adefovir dipivoxil, and entecavir. Unfortunately, these agents are not effective in all patients and are associated with distinct side effects. Interferons have numerous side effects and nucleoside or nucleotide analogues, which are well tolerated, need to be used for prolonged periods, even indefinitely. However, prolonged treatment with nucleoside or nucleotide analogues is associated with a high rate of resistance. Telbivudine is a novel, orally administered nucleoside analogue for use in the treatment of chronic hepatitis B. In contrast to other nucleoside analogues, Telbivudine has not been associated with inhibition of mammalian DNA polymerase with mitochondrial toxicity. Telbivudine has demonstrated potent activity against hepatitis B with a significantly higher rate of response and superior viral suppression compared with lamivudine, the standard treatment. Telbivudine has been generally well tolerated, with a low adverse effect profile, and at its effective dose, no dose-limiting toxicity has been observed. Telbivudine is one of the most potent antiviral agents for chronic hepatitis B virus and was approved by the FDA in late 2006.
据估计，全球有3.5亿人长期感染乙肝病毒。其中15% - 40%的患者在其一生中会发展为肝硬化、肝衰竭或肝细胞癌。在过去十年中，由于核苷/核苷酸类似物的出现以及聚乙二醇化干扰素的使用，慢性乙型肝炎的治疗有了显著改善。批准用于慢性乙型肝炎治疗的药物包括：标准干扰素α - 2b、聚乙二醇化干扰素α - 2a、拉米夫定、阿德福韦酯和恩替卡韦。不幸的是，这些药物并非对所有患者都有效，而且还伴有明显的副作用。干扰素副作用众多，而核苷或核苷酸类似物虽然耐受性良好，但需要长期使用，甚至可能需无限期使用。然而，长期使用核苷或核苷酸类似物会导致高耐药率。替比夫定是一种新型的口服核苷类似物，用于治疗慢性乙型肝炎。与其他核苷类似物不同，替比夫定不会抑制具有线粒体毒性的哺乳动物DNA聚合酶。与标准治疗药物拉米夫定相比，替比夫定已显示出对乙肝病毒有强大的活性，应答率显著更高，病毒抑制效果更佳。替比夫定总体耐受性良好，不良反应较少，在有效剂量下未观察到剂量限制性毒性。替比夫定是治疗慢性乙肝病毒最有效的抗病毒药物之一，并于2006年末获得美国食品药品监督管理局（FDA）批准。
