文献标题：Tenofovir disoproxil fumarate: in chronic hepatitis B.
文献出处：Drugs. 2009 Nov 12;69(16):2245-56
文献类型：Review
期刊影响因子：4.732
PMID：19852527
富马酸替诺福韦酯（替诺福韦DF）为替诺福韦的前体酯类口服药物，属于核苷酸逆转录酶抑制剂，在体内表现出强大的抗乙型肝炎病毒（HBV）与抗HIV-1的活性。作为联合抗逆转录病毒疗法中的药物之一，替诺福韦DF对感染HIV-1的成年患者具有良好疗效。
替诺福韦DF每日1次口服，可用于治疗成年慢性乙型肝炎（CHB）。2项大型III期随机临床研究纳入了伴有肝功能代偿的、乙型肝炎e抗原（HBe-Ag）阴性或阳性成年患者，这些试验评估了在CHB治疗中替诺福韦抗HBV的有效性。
这2项试验（计划时间为8年）在前48周以双盲方式进行，此后以开放标签形式向患者们提供替诺福韦DF。通过试验获得了48及96周治疗结果。在研究的第48周，与每日1次口服10 mg阿德福韦酯者相比，在每日1次口服300 mg替诺福韦DF患者中，获得完全反应（主要终点）者比例显著增高。完全反应的定义为血清乙型肝炎病毒DNA由基线水平降至<400 copies/mL、以及组织学改善（Knodell坏死性炎症积分降低2分及以上，且不伴纤维化加重）。在这2项研究当中，96周的治疗结果也阐明了替诺福韦DF在CHB治疗中的有效性。在2项III期研究当中，患有CHB的成年患者对替诺福韦具有普遍良好的耐受性。
医脉通推荐英文摘要：
Drugs. 2009 Nov 12;69(16):2245-56
Tenofovir disoproxil fumarate: in chronic hepatitis B
Perry CM, Simpson D.
（Adis, North Shore, Auckland, New Zealand. ）
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 endpoint). A complete response was defined as a reduction from baseline in plasma HBV DNA level to <400 copies/mL and histological improvement (reduction of 2 or more points in Knodell necroinflammatory score without worsening of fibrosis). The efficacy of tenofovir DF in the treatment of CHB was also demonstrated over a 96-week treatment period in both studies. Tenofovir DF was generally well tolerated by adults with CHB in the two phase III trials.
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