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Candidates for inclusion in a universal antiretroviral regimen: tenofovir
alafenamide.
Gotham
D, Hill A, Pozniak AL.
Curr
Opin HIV AIDS. 2017
Apr 11.
Abstract
Resolution of Tenofovir Disoproxil Fumarate Induced Fanconi
Syndrome with Switch to Tenofovir Alafenamide Fumarate in a HIV-1 and Hepatitis
B co-infected Patient.
Karris M.
AIDS Res Hum Retroviruses. 2017 Apr 13.
Abstract
Effect of Tenofovir Disoproxil Fumarate on Incidence of Chronic Kidney Disease
and Rate of Estimated Glomerular Filtration Rate Decrement in HIV-1-Infected
Treatment-Naïve Asian Patients: Results from 12-Year Observational Cohort.
Suzuki S, Nishijima T, Kawasaki Y, et al
AIDS Patient Care STDS.
2017 Mar;31(3):105
Abstract
Switching from tenofovir disoproxil fumarate to tenofovir
alafenamide coformulated with rilpivirine and emtricitabine in
virally suppressed adults with HIV-1 infection: a randomised,
double-blind, multicentre, phase 3b, non-inferiority study.
Orkin C, DeJesus E, Ramgopal M,et
al
Lancet HIV. 2017 Mar 1.
Abstract
Switching from efavirenz, emtricitabine, and tenofovir disoproxil fumarate
to tenofovir alafenamide coformulated with rilpivirine and emtricitabine in
virally suppressed adults with HIV-1 infection: a randomised, double-blind,
multicentre, phase 3b, non-inferiority study.
DeJesus E, Ramgopal M, Crofoot G, et al
Lancet HIV. 2017 Mar 1.
Abstract
Emtricitabine + tenofovir alafenamide for the treatment of
HIV.
Corado KC, Daar ES.
Expert Opin Pharmacother. 2017 Feb
2.
Abstract
Tenofovir alafenamide and elvitegravir loaded nanoparticles for long-acting
prevention of HIV-1 vaginal transmission.
Mandal S, Prathipati PK, Kang G,
et al
AIDS. 2017 Feb
20;31(4):469-476.
Abstract
Tenofovir alafenamide (TAF) does not deplete mitochondrial DNA in human
T-cell lines at intracellular concentrations exceeding clinically relevant
drug exposures.
Stray KM, Park Y, Babusis D,
Antiviral Res. 2017 Jan 25. pii: S0166-3542(16)30571-X.
Abstract
Safety, efficacy, and pharmacokinetics of a single-tablet regimen containing
elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide in
treatment-naive, HIV-infected adolescents: a single-arm, open-label trial.
Gaur AH, Kizito H, Prasitsueubsai W, et al
Lancet HIV. 2016 Oct 17.
Abstract
FULL-TEXT ARTICLE
The efficacy
and safety of tenofovir alafenamide versus tenofovir disoproxil fumarate in
antiretroviral regimens for HIV-1 therapy: Meta-analysis.
Wang H, Lu X, Yang X,et al.
Medicine (Baltimore). 2016
Oct;95(41):e5146.
Paper
FULL-TEXT ARTICLE
Equivalent Decline in Inflammation Markers with Tenofovir Disoproxil
Fumarate vs. Tenofovir Alafenamide.
Funderburg NT, McComsey GA, Kulkarni M, et al"
EBioMedicine. 2016 Oct 11.
Paper
Tenofovir Alafenamide: A Review of Its Use in the Treatment of HIV-1
Infection.
Gibson AK, Shah BM, Nambiar PH, Schafer J
J.Ann Pharmacother.
2016 Jul 26.
Abstract
Tenofovir: Is Tenofovir Alafenamide Safer than Tenofovir
Disoproxil Fumarate for the Kidneys?
Aloy B, Tazi I, Bagnis CI, Gauthier M, et al
AIDS Rev.
2016 Jul 19;18(4).
Abstract
A Tunable, Biodegradable, Thin-Film Polymer Device as a Long-Acting Implant
Delivering Tenofovir Alafenamide Fumarate for HIV Pre-exposure Prophylaxis.
Schlesinger E, Johengen D, Luecke E, et al
Pharm Res. 2016 Mar 14
Abstract
A Randomized, Double-Blind comparison of Tenofovir Alafenamide (TAF) vs.
Tenofovir Disoproxil fumarate (TDF), each coformulated with Elvitegravir,
Cobicistat, and Emtricitabine (E/C/F) for initial HIV-1 Treatment: Week 96
results.
Wohl D, Oka S,
Clumeck N, Clarke A,
et al
J Acquir Immune Defic Syndr. 2016 Jan 29.
Abstract
FULL-TEXT ARTICLE
Tenofovir alafenamide: A novel prodrug of tenofovir
for the treatment of Human Immunodeficiency Virus..
Ray AS, Fordyce MW,
Hitchcock MJ.
Antiviral Res.
2015 Nov 27.
Paper
Switching from tenofovir disoproxil fumarate to tenofovir alafenamide in
antiretroviral regimens for virologically suppressed adults with HIV-1
infection: a randomised, active-controlled, multicentre, open-label, phase 3,
non-inferiority study.
Mills A, Arribas JR, Andrade-Villanueva J,
et al
Lancet Infect Dis.
2015 Oct 30.
Abstract
Tenofovir alafenamide for HIV: time to switch?
Dhanireddy S, Baeten JM.
Lancet Infect Dis. 2015 Oct 30
Abstract
Intracellular Activation of Tenofovir Alafenamide (TAF) and the Effect of Viral
and Host Protease Inhibitors.
Birkus G, Bam RA, Willkom M, et al
Antimicrob Agents Chemother.
2015 Oct 26.
Abstract
Characterization of HIV-1 Resistance to Tenofovir Alafenamide (TAF) In
Vitro.
Margot NA, Johnson A,
Miller MD, Callebaut C.
Antimicrob Agents Chemother. 2015 Jul
Abstract
In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of
Tenofovir with Improved Antiviral Activity Compared to Tenofovir Disoproxil
Fumarate.
Callebaut C, Stepan G, Tian Y, Miller MD.
Antimicrob Agents Chemother. 2015 Jul 6.
Abstract
Pharmacokinetics of Long-acting Tenofovir Alafenamide (GS-7340) Subdermal
Implant for HIV Prophylaxis.
Gunawardana M, Remedios-Chan
M, Miller CS, et al
Antimicrob Agents Chemother.
2015 Apr 20.
Abstract
Concentrations of TFV-DP/FTC-TP in dried blood spots and TFV/FTC in hair are
strongly correlated in iPrEx OLE: Implications for PrEP adherence monitoring.
Gandhi M, Glidden DV, Liu A, et al
J Infect Dis. 2015 Apr 20.
Abstract
Population Pharmacokinetics of Tenofovir and Tenofovir-diphosphate
in healthy women.
Burns RN, Hendrix CW,
Chaturvedula A.
J
Clin Pharmacol. 2015 Jan 8
Abstract
Tenofovir Alafenamide vs. Tenofovir Disoproxil Fumarate in Single Tablet
Regimens for Initial HIV-1 Therapy: A Randomized Phase 2 Study.
Sax PE, Zolopa A, Brar I,
et al
J Acquir Immune Defic Syndr.
2014 May 27.
Abstract
Phase I/II study of the pharmacokinetics, safety and antiretroviral activity of
tenofovir alafenamide, a new prodrug of the HIV reverse transcriptase
inhibitor tenofovir, in HIV-infected adults.
Markowitz M, Zolopa A, Squires K, et a
J Antimicrob Chemother. 2014 May;69(5):1362-9.
Abstract
Tenofovir alafenamide is not a substrate for renal organic anion transporters (OATs)
and does not exhibit OAT-dependent cytotoxicity.
Bam RA, Yant SR, Cihlar T.
Antivir Ther. 2014 Apr 4.
Abstract
Metabolism and antiretroviral activity of tenofovir alafenamide in
CD4<sup>+</sup> T-cells and macrophages from demographically diverse donors.
Bam RA, Birkus G, Babusis D,
et al
Antivir Ther.
2014 Mar 13.
Abstract
Antiviral Activity, Safety, and Pharmacokinetics/Pharmacodynamics of
Tenofovir Alafenamide as 10-Day Monotherapy in HIV-1-Positive Adults.
Ruane PJ, Dejesus E, Berger D,
et al
J Acquir Immune Defic Syndr.
2013 Aug 1;63(4):449-455
Abstract
Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir
alafenamide (TAF) as 10-day monotherapy in HIV-1-positive adults.
Ruane P, Dejesus E, Berger D, et al
J Acquir Immune Defic Syndr.
2013 Apr 17.
Abstract
Mechanism for effective lymphoid cell and tissue loading
following oral administration of nucleotide prodrug GS-7340.
Babusis D, Phan TK, Lee WA, et al
Mol Pharm. 2013 Feb
4;10(2):459-66.
Abstract
FULL-TEXT ARTICLE
Activation of
9-[(R)-2-[[(S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]
phenoxyphosphinyl]-methoxy]propyl]adenine (GS-7340) and other tenofovir
phosphonoamidate prodrugs by human proteases.
Birkus G, Kutty N, He GX, et al
Mol Pharmacol.
2008 Jul;74(1):92-100
Paper
FULL-TEXT ARTICLE
Cathepsin A is
the major hydrolase catalyzing the intracellular hydrolysis of the
antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and
GS-9131.
Birkus G, Wang R, Liu X, Kutty N, et
a
Antimicrob Agents Chemother.
2007 Feb;51(2):543-50
Paper
Evaluation of oral tenofovir disoproxil fumarate and topical tenofovir GS-7340
to protect infant macaques against repeated oral challenges with
virulent simian immunodeficiency virus.
Van Rompay KK, Kearney BP, Sexton JJ, et al
J Acquir Immune Defic Syndr.
2006 Sep;43(1):6-14.
Abstract
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New
and Noteworthy
Elvitegravir/Cobicistat/
Emtricitabine/Tenofovir Alafenamide
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