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Tenofovir Alafenamid  (GS 7340)
 
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Elvitegravir/Cobicistat/ Emtricitabine/Tenofovir Alafenamide (Genvoya«)
Emtricitabine/Tenofovir Alafenamide  (Descovy)

 


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Last Update:  March 11, 2017
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New and Noteworthy
 

March 2017
 
 

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Journal Abstracts , Papers, and Commentaries
 

  Effect of Tenofovir Disoproxil Fumarate on Incidence of Chronic Kidney Disease and Rate of Estimated Glomerular Filtration Rate Decrement in HIV-1-Infected Treatment-Na´ve 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. 2
016 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

FULL-TEXT ARTICLE
Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue.
Lee WA, He GX, Eisenberg E,  et al
Antimicrob Agents Chemother. 2005 May;49(5):
Paper


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Tenofovir Alafenamid (GS 7340)