Tenofovir Disoproxil Fumarate In Chronic Hepatitis B
Tenofovir Disoproxil Fumarate In Chronic Hepatitis B
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DOI：
10.2165/10482940-000000000-00000
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发表时间：
2009-01-01
期刊：
影响因子：
11.5
通讯作者：
Simpson, Dene
中科院分区：
文献类型：
--
作者：
Perry, Caroline M.;Simpson, Dene
替诺福韦酯（Tenofovir disoprotanil fumarate，tenofovir DF）是一种核苷类逆转录酶抑制剂替诺福韦酯的前体药物，体外抗B肝炎病毒（HepatitisB virus，HBV）和HIV-1的活性均较强。替诺福韦DF，每日一次给药，也用于治疗慢性B型肝炎（CH B）成人[本资料的主要焦点]。在CH B中，替诺福韦DF对HBV的疗效已在两项大型随机、III期临床研究中进行了评估，研究对象为具有代偿肝功能的B e抗原（HBeAg）阴性或HBeAg阳性成人。这些试验（计划持续8年）在前48周是双盲的;此后，患者接受开放标签的替诺福韦DF。在这些研究中，在第48周，替诺福韦DF 300 mg每日一次的接受者比口服阿德福韦酯10 mg每日一次的接受者获得完全应答的比例显著更高（主要终点）。完全缓解定义为血浆HBV DNA水平从基线降低至
Tenofovir disoproxil fumarate (tenofovir DF) is an orally administered ester prodrug of tenofovir, a nucleotide reverse transcriptase inhibitor that shows potent in vitro activity against both hepatitis B virus (HBV) and HIV-1.As a component of antiretroviral combination therapy regimens, tenofovir DF is well established in the treatment of adults with HIV-1 infection. Tenofovir DF, administered once daily, is also used in the treatment of adults with chronic hepatitis B (CHB) [the main focus of this profile].In CHB, the efficacy of tenofovir DF against HBV has been evaluated in two large randomized, phase III clinical studies in hepatitis B e antigen (HBeAg)-negative or HBeAg-positive adults, with compensated liver function. The trials (planned duration 8 years) were double-blind for the first 48 weeks; thereafter, patients received open-label tenofovir DF. Results at 48 and 96 weeks are available.In these studies, at week 48, a significantly greater proportion of recipients of tenofovir DF 300 mg once daily than oral adefovir dipivoxil 10 mg once daily achieved a complete response (primary end-point). A complete response was defined as a reduction from baseline in plasma HBV DNA level to