Caviglia G P, Abate M L, Pellicano R, Smedile A
Department of Medical Sciences, University of Turin, Turin, Italy -
Minerva Gastroenterol Dietol. 2015 Jun;61(2):61-70. Epub 2014 Oct 17.
There are currently several drugs approved for the treatment of chronic hepatitis B including recombinant interferons, such as interferon-α and its pegylated formulation, and the nucleos(t)ide analogues, such as lamivudine, adefovir, telbivudine, entecavir and tenofovir. Pegylated-interferon is an immune-modulatory agent that works mainly by enhancing the innate immune response while nucleos(t)ide analogues are oral drugs with direct inhibition of viral replication. Each agent has its own advantages and drawbacks. Pegylated-Interferon treatment has a finite duration without induction of drug resistance but only a limited number of patients achieve a sustained virological response to therapy. On the other hand, the care with nucleos(t)ide analogues requires a long-term treatment with a potential risk of induction of drug resistance, but higher rates of viral replication suppression are achieved. Nevertheless, second generation nucleos(t)ide analogues, such as Entecavir and Tenofovir, have both high genetic barrier to resistance and potent antiviral action. This review describes the mechanisms of antiviral activity and the efficacy of viral suppression of the different available drugs for chronic hepatitis B treatment, considering the recent clinical guidelines for an optimal management of chronic HBV infection.
目前有几种药物被批准用于治疗慢性乙型肝炎,包括重组干扰素,如α干扰素及其聚乙二醇化制剂,以及核苷(酸)类似物,如拉米夫定、阿德福韦、替比夫定、恩替卡韦和替诺福韦。聚乙二醇化干扰素是一种免疫调节剂,主要通过增强先天免疫反应起作用,而核苷(酸)类似物是口服药物,可直接抑制病毒复制。每种药物都有其自身的优缺点。聚乙二醇化干扰素治疗疗程有限,不会诱导耐药性,但只有少数患者能实现持续病毒学应答。另一方面,核苷(酸)类似物治疗需要长期用药,存在诱导耐药性的潜在风险,但能实现更高的病毒复制抑制率。然而,第二代核苷(酸)类似物,如恩替卡韦和替诺福韦,具有高耐药基因屏障和强效抗病毒作用。本综述根据慢性HBV感染最佳管理的最新临床指南,描述了用于慢性乙型肝炎治疗的不同现有药物的抗病毒活性机制和病毒抑制疗效。