Role of tenofovir alafenamide (TAF) in the treatment and prophylaxis of HIV and HBV infections

被引:37
作者
De Clercq, Erik [1 ]
机构
[1] Katholieke Univ Leuven, Rega Inst Med Res, Dept Microbiol & Immunol, Herestr 49, B-3000 Leuven, Belgium
关键词
Tenofovir; TDF; TAF; INSTIs; HIV; HBV; PrEP; HEPATITIS-B-VIRUS; VIROLOGICALLY SUPPRESSED ADULTS; SINGLE-TABLET REGIMEN; TRANSCRIPTASE INHIBITOR TENOFOVIR; DISOPROXIL FUMARATE; DOUBLE-BLIND; ANTIVIRAL ACTIVITY; OPEN-LABEL; ELVITEGRAVIR/COBICISTAT/EMTRICITABINE/TENOFOVIR ALAFENAMIDE; REVERSE-TRANSCRIPTASE;
D O I
10.1016/j.bcp.2017.11.023
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Tenofovir (TFV) is the cornerstone of the treatment and prophylaxis of HIV infections. It has been routinely used in its prodrug form TDF (tenofovir disoproxil fumarate) combined with emtricitabine ((-)FTC) and other antiretroviral agents. TDF has now been replaced by TAF (tenofovir alafenamide) which allows better uptake by the lymphoid tissue. In combination with elvitegravir (E), cobicistat (C), emtricitabine (F), TAF can be advocated as an STR (single tablet regimen, Genvoya (R)) for the treatment of HIV infections. In this combination, E and C may in the future be replaced by bictegravir. The prophylaxis of HIV infection is momentarily based upon Truvada (R), the combination of F with TDF, which in the future may also be replaced by TAF. TAF (Vemlidy (R)) has also replaced TDF (Viread (R)) for the treatment of hepatitis B virus (HBV) infections. Both TDF and TAF offer little or no risk for virus-drug resistance. As compared to TDF, TAF limits the risk for nephrotoxicity and loss of bone mineral density. What remains to be settled, however, before the universal use of TAF could be recommended, is its safety during pregnancy and its applicability in the treatment of tuberculosis, in combination with rifampicin. (C) 2017 Elsevier Inc. All rights reserved.
引用
收藏
页码:2 / 11
页数:10
相关论文
共 108 条
[1]   Twenty-eight day safety, antiviral activity, and pharmacokinetics of tenofovir alafenamide for treatment of chronic hepatitis B infection [J].
Agarwal, Kosh ;
Fung, Scott K. ;
Nguyen, Tuan T. ;
Cheng, Wendy ;
Sicard, Eric ;
Ryder, Stephen D. ;
Flaherty, John F. ;
Lawson, Eileen ;
Zhao, Sally ;
Subramanian, G. Mani ;
McHutchison, John G. ;
Gane, Edward J. ;
Foster, Graham R. .
JOURNAL OF HEPATOLOGY, 2015, 62 (03) :533-540
[2]  
Aloy B, 2016, AIDS REV, V18, P184
[3]  
Angione S. A., J PHARM PRACT
[4]   The role of tenofovir alafenamide in future HIV management [J].
Antela, A. ;
Aguiar, C. ;
Compston, J. ;
Hendry, B. M. ;
Boffito, M. ;
Mallon, P. ;
Pourcher-Martinez, V. ;
Di Perri, G. .
HIV MEDICINE, 2016, 17 :4-16
[5]   Synthesis and evaluation of novel amidate prodrugs of PMEA and PMPA [J].
Ballatore, C ;
McGuigan, C ;
De Clercq, E ;
Balzarini, J .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (08) :1053-1056
[6]   Tenofovir alafenamide is not a substrate for renal organic anion transporters (OATs) and does not exhibit OAT-dependent cytotoxicity [J].
Bam, Rujuta A. ;
Yant, Stephen R. ;
Cihlar, Tomas .
ANTIVIRAL THERAPY, 2014, 19 (07) :687-692
[7]   Metabolism and antiretroviral activity of tenofovir alafenamide in CD4+ T-cells and macrophages from demographically diverse donors [J].
Bam, Rujuta A. ;
Birkus, Gabriel ;
Babusis, Darius ;
Cihlar, Tomas ;
Yant, Stephen R. .
ANTIVIRAL THERAPY, 2014, 19 (07) :669-677
[8]   Tenofovir alafenamide for the treatment of chronic hepatitis B virus infection [J].
Basit, Syed Abdul ;
Dawood, Altaf ;
Ryan, John ;
Gish, Robert .
EXPERT REVIEW OF CLINICAL PHARMACOLOGY, 2017, 10 (07) :707-716
[9]   Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors [J].
Birkus, Gabriel ;
Bam, Rujuta A. ;
Willkom, Madeleine ;
Frey, Christian R. ;
Tsai, Luong ;
Stray, Kirsten M. ;
Yant, Stephen R. ;
Cihlar, Tomas .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2016, 60 (01) :316-322
[10]   Chronic hepatitis B: A wave of new therapies on the horizon [J].
Block, Timothy M. ;
Rawat, Siddhartha ;
Brosgart, Carol L. .
ANTIVIRAL RESEARCH, 2015, 121 :69-81