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Pharmacokinetics of a weekly transdermal delivery system of tenofovir alafenamide in hairless rats.替诺福韦艾拉酚胺经皮给药每周系统在无毛大鼠中的药代动力学。
Int J Pharm. 2020 May 30;582:119342. doi: 10.1016/j.ijpharm.2020.119342. Epub 2020 Apr 18.
2
An LC-MS/MS method for determination of tenofovir (TFV) in human plasma following tenofovir alafenamide (TAF) administration: Development, validation, cross-validation, and use of formic acid as plasma TFV stabilizer.一种 LC-MS/MS 法测定人血浆中替诺福韦（TFV）在替诺福韦艾拉酚胺（TAF）给药后的浓度：开发、验证、交叉验证和使用甲酸作为血浆 TFV 稳定剂。
Anal Biochem. 2020 Mar 15;593:113611. doi: 10.1016/j.ab.2020.113611. Epub 2020 Feb 5.
3
A Subcutaneous Implant of Tenofovir Alafenamide Fumarate Causes Local Inflammation and Tissue Necrosis in Rabbits and Macaques.富马酸替诺福韦艾拉酚胺的皮下植入物可引起兔和猕猴的局部炎症和组织坏死。
Antimicrob Agents Chemother. 2020 Feb 21;64(3). doi: 10.1128/AAC.01893-19.
4
Changes in Body Mass Index and Atherosclerotic Disease Risk Score After Switching From Tenofovir Disoproxil Fumarate to Tenofovir Alafenamide.从富马酸替诺福韦二吡呋酯转换为替诺福韦艾拉酚胺后体重指数和动脉粥样硬化疾病风险评分的变化
Open Forum Infect Dis. 2019 Oct 4;6(10):ofz414. doi: 10.1093/ofid/ofz414. eCollection 2019 Oct.
5
Characterization of a Reservoir-Style Implant for Sustained Release of Tenofovir Alafenamide (TAF) for HIV Pre-Exposure Prophylaxis (PrEP).用于替诺福韦艾拉酚胺（TAF）持续释放的储库型植入物用于HIV暴露前预防（PrEP）的特性研究。
Pharmaceutics. 2019 Jul 4;11(7):315. doi: 10.3390/pharmaceutics11070315.
6
Simultaneous determination of tenofovir alafenamide and tenofovir in human plasma by LC-MS/MS and its application to pharmacokinetics study in clinic.采用 LC-MS/MS 法同时测定人血浆中替诺福韦艾拉酚胺和替诺福韦的浓度及其在临床药代动力学研究中的应用。
J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Jun 1;1117:148-157. doi: 10.1016/j.jchromb.2019.04.011. Epub 2019 Apr 5.
7
Renal safety of tenofovir alafenamide vs. tenofovir disoproxil fumarate: a pooled analysis of 26 clinical trials.替诺福韦艾拉酚胺与富马酸替诺福韦二吡呋酯的肾脏安全性：26 项临床试验的汇总分析。
AIDS. 2019 Jul 15;33(9):1455-1465. doi: 10.1097/QAD.0000000000002223.
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J Control Release. 2018 Sep 28;286:315-325. doi: 10.1016/j.jconrel.2018.08.010. Epub 2018 Aug 6.
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Validation and implementation of liquid chromatographic-mass spectrometric (LC-MS) methods for the quantification of tenofovir prodrugs.验证和实施液相色谱-质谱（LC-MS）方法，用于定量测定替诺福韦前药。
J Pharm Biomed Anal. 2018 Apr 15;152:248-256. doi: 10.1016/j.jpba.2018.02.011. Epub 2018 Feb 8.
10
Superior Efficacy and Improved Renal and Bone Safety After Switching from a Tenofovir Disoproxil Fumarate- to a Tenofovir Alafenamide-Based Regimen Through 96 Weeks of Treatment.在长达96周的治疗期间，从基于富马酸替诺福韦二吡呋酯转换为基于替诺福韦艾拉酚胺的治疗方案后，疗效更佳，肾脏和骨骼安全性得到改善。
AIDS Res Hum Retroviruses. 2018 Apr;34(4):337-342. doi: 10.1089/AID.2017.0203. Epub 2018 Mar 20.

富马酸替诺福韦艾拉酚胺在血浆中的种间稳定性差异。

Interspecies Differences in Tenofovir Alafenamide Fumarate Stability in Plasma.

作者信息

Parsons Teresa L, Gwenden Kevin N, Marzinke Mark A

机构信息

Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA.

Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA

出版信息

Antimicrob Agents Chemother. 2020 Aug 20;64(9). doi: 10.1128/AAC.00930-20.

DOI:10.1128/AAC.00930-20
PMID:32540983
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7449208/
Abstract

Tenofovir (TFV) alafenamide fumarate (TAF) is an antiretroviral that has been evaluated in alternative drug delivery systems in several species. The stability of TAF was evaluated, and TAF was stable in dog-, sheep-, and macaque-spiked plasma. A negative bias was observed in TAF recovery in rabbit-spiked plasma; there was complete loss of TAF and corresponding overestimation of TFV in rodent-spiked plasma. These data highlight considerations when evaluating TAF and TFV concentrations in preclinical studies.

摘要

替诺福韦艾拉酚胺富马酸盐（TAF）是一种抗逆转录病毒药物，已在多个物种的替代给药系统中进行了评估。对TAF的稳定性进行了评估，结果显示TAF在添加了犬、羊和猕猴血浆的样本中稳定。在添加了兔血浆的样本中，TAF回收率出现负偏差；在添加了啮齿动物血浆的样本中，TAF完全损失，同时相应地高估了替诺福韦（TFV）。这些数据突出了在临床前研究中评估TAF和TFV浓度时需要考虑的因素。