Scott Lesley J, Keating Gillian M
Wolters Kluwer Health/Adis, 41 Centorian Drive, Mairangi Bay, North Shore 0754, Auckland, New Zealand.
Drugs. 2009 May 29;69(8):1003-33. doi: 10.2165/00003495-200969080-00005.
Entecavir (Baraclude), a nucleoside analogue, is rapidly phosphorylated to the active intracellular 5'-triphosphate form that inhibits replication of hepatitis B virus (HBV). Oral entecavir is approved in the US, EU and several countries worldwide for the treatment of chronic HBV infection in adults (> or =16 years of age) with evidence of active viral replication and persistently elevated serum ALT and/or AST levels, and/or histological evidence of active disease. In several randomized, double-blind, multicentre trials, oral entecavir was an effective and generally well tolerated treatment in nucleoside-naive and lamivudine-refractory adult patients with chronic HBV infection, irrespective of whether patients were hepatitis B e antigen (HBeAg)-positive or -negative. Furthermore, it was more efficacious, associated with a lower risk of resistance, and more cost effective than lamivudine in these patient populations, with both drugs having a similar tolerability profile. In the EARLY trial, entecavir was significantly more effective than and as well tolerated as adefovir dipivoxil therapy in nucleoside-naive patients. In addition, in a double-blind, multicentre trial, entecavir plus lamivudine-based highly active antiretroviral therapy (HAART) was more effective than placebo plus lamivudine-based HAART in patients co-infected with HBV and HIV. Although the exact position of entecavir relative to other agents, such as tenofovir disoproxil fumarate and adefovir dipivoxil, for the treatment of chronic HBV infection remains to be fully determined, an important aspect in this positioning is the emergence of drug resistance. Hence, entecavir therapy provides a valuable first-line option in nucleoside-naive patients with chronic HBV infection and is a useful alternative in lamivudine-refractory patients.
恩替卡韦（博路定）是一种核苷类似物，可迅速磷酸化为具有活性的细胞内5'-三磷酸形式，抑制乙型肝炎病毒（HBV）复制。在美国、欧盟及全球多个国家，口服恩替卡韦被批准用于治疗16岁及以上、有病毒活跃复制证据、血清ALT和/或AST持续升高以及/或者有活动性疾病组织学证据的慢性HBV感染成人患者。在多项随机、双盲、多中心试验中，口服恩替卡韦对于初治和拉米夫定耐药的慢性HBV感染成人患者是一种有效且耐受性良好的治疗方法，无论患者乙肝e抗原（HBeAg）是阳性还是阴性。此外，在这些患者群体中，恩替卡韦比拉米夫定更有效、耐药风险更低且更具成本效益，两种药物的耐受性相似。在EARLY试验中，恩替卡韦在初治患者中显著比阿德福韦酯治疗更有效且耐受性相当。此外，在一项双盲、多中心试验中，恩替卡韦联合基于拉米夫定的高效抗逆转录病毒疗法（HAART）在合并HBV和HIV感染的患者中比安慰剂联合基于拉米夫定的HAART更有效。尽管恩替卡韦相对于其他药物（如替诺福韦酯和阿德福韦酯）在治疗慢性HBV感染的确切地位仍有待充分确定，但这种地位的一个重要方面是耐药性的出现。因此，恩替卡韦治疗为初治慢性HBV感染患者提供了一种有价值的一线选择，并且是拉米夫定耐药患者的一种有用替代方案。
