替诺福韦艾拉酚胺（TAF）用于治疗慢性乙型肝炎单一感染。

StephenW

Pharmacotherapy. 2018 Aug 18. doi: 10.1002/phar.2174. [Epub ahead of print]
Tenofovir alafenamide (TAF) for the treatment of chronic hepatitis B mono-infection.
Childs-Kean LM1, Egelund E2, Jourjy J3.
Author information

1
    University of Florida College of Pharmacy, Gainesville, FL, PO Box 100483, 32610, USA.
2
    University of Florida College of Pharmacy, Jacksonville, FL, USA.
3
    University of Florida College of Pharmacy, Orlando, FL, USA.

Abstract

Tenofovir alafenamide (TAF) is indicated for adult patients with chronic HBV infection with compensated liver disease at a dose of 25mg orally daily. TAF is a more stable prodrug in the plasma than tenofovir disoproxil fumarate (TDF), leading to decreased plasma exposure of tenofovir. Decreased exposure is thought to reduce the risk of long-term TDF toxicities, such as nephrotoxicity and decreased bone mineral density. TAF has the same mechanism of action as TDF: a nucleotide reverse transcriptase inhibitor. The results of Phase III primary trials and extensions showed that TAF is non-inferior to TDF at suppressing the HBV viral load in treatment naïve and treatment-experienced HBeAg-negative and HBeAg-positive patients at 48 weeks, 96 weeks, and 144 weeks of therapy. The most commonly reported adverse events were headache, abdominal pain, fatigue, cough, nausea, and back pain. At all evaluated time points (out to 144 weeks of treatment), patients who received TAF had less risk of nephrotoxicity and less of a decline in bone mineral density than the patients who received TDF. TAF appears to be safe in patients with a creatinine clearance above 15mL/min; however, TAF is not currently recommended in patients with an estimated creatinine clearance below this threshold. TAF is safe in patients with mild hepatic impairment, but is not currently recommended in patients with moderate or severe hepatic impairment (Child-Pugh Class B or C). This article is protected by copyright. All rights reserved.
KEYWORDS:

Antivirals; Hepatitis; Reverse Transcriptase Inhibitors; Tenofovir Alafenamide

PMID:
    30120841
DOI:
    10.1002/phar.217

StephenW

药物治疗。 2018年8月18日doi：10.1002 / phar.2174。 [提前打印]
替诺福韦艾拉酚胺（TAF）用于治疗慢性乙型肝炎单一感染。
Childs-Kean LM1，Egelund E2，Jourjy J3。
作者信息

1
    佛罗里达大学药学院，佛罗里达州盖恩斯维尔，邮政信箱100483,32610，美国。
2
    佛罗里达大学药学院，美国佛罗里达州杰克逊维尔。
3
    佛罗里达大学药学院，美国佛罗里达州奥兰多市。

抽象

替诺福韦艾拉酚胺（TAF）适用于患有慢性HBV感染且患有代偿性肝病的成年患者，每日口服25mg。 TAF是血浆中比替诺福韦地索普西富马酸盐（TDF）更稳定的前药，导致替诺福韦的血浆暴露减少。减少暴露被认为可降低长期TDF毒性的风险，例如肾毒性和骨矿物质密度降低。 TAF具有与TDF相同的作用机制：核苷酸逆转录酶抑制剂。 III期初步试验和扩展的结果显示，在48周，96周和144周时，TAF在治疗初治和治疗经历的HBeAg阴性和HBeAg阳性患者中抑制HBV病毒载量并非劣于TDF。治疗。最常报告的不良事件是头痛，腹痛，疲劳，咳嗽，恶心和背痛。在所有评估的时间点（治疗时间为144周），接受TAF的患者肾脏毒性风险较低，骨密度下降的程度低于接受TDF治疗的患者。对于肌酐清除率高于15mL / min的患者，TAF似乎是安全的;但是，目前建议肌酐清除率低于此阈值的患者不要使用TAF。 TAF对轻度肝功能损害患者是安全的，但目前不推荐用于中度或重度肝功能损害的患者（Child-Pugh B级或C级）。本文受版权保护。版权所有。
关键词：

抗病毒药物;肝炎;逆转录酶抑制剂;替诺福韦Alafenamide

结论：
    30120841
DOI：
    10.1002 / phar.217