Medical Advocates

Tenofovir Disoproxil Fumarate
(Viread)
   
Journal Citations
 
General Reports           
Animal Studies             

Safety   
Pharmacokinetics
Drug Interactions
Resistance
Viral Dynamics
Efficacy
Adverse Events
Diagnostics/Monitoring
Therapeutic Strategies
Discontinuation
Prophylaxis
Vaginal Microbicide Studies






 

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Last Update:  August 19, 2008
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General Reports
 

 
Tenofovir: what have over 1 million years of patient experience taught us
Pozniak A.
Int J Clin Pract. 2008 Aug;62(8):1285-93
Abstract
 
A WEEK IN REVIEW FEATURED REPORT
Clinical and genetic determinants of intracellular tenofovir diphosphate concentrations in
HIV-infected patients.
Kiser JJ, Aquilante CL, Anderson PL ,et al

J Acquir Immune Defic Syndr. 2008 Mar 1;47(3):298-303.
Abstract
 
Inhibition of HIV-1 Replication in Macrophages by Red Blood Cell-Mediated Delivery of a
Heterodinucleotide of Lamivudine and Tenofovir.

Franchetti P, Cappellacci L, Petrelli R, et al 
Nucleosides Nucleotides Nucleic Acids. 2007;26(8-9):953-7.
Abstract
 
The Microbicide Tenofovir Does Not Inhibit Nucleic Acid Amplification Tests for Chlamydia
trachomatis and Neisseria gonorrhoeae in Urine Samples.

Wood BJ, Rizzo-Price P, Holden J,  et al  

J Clin Microbiol.
2007 Dec 5
Abstract
 
Inhibition of HIV-1 Replication in Macrophages by Red Blood Cell-Mediated Delivery of a
Heterodinucleotide of Lamivudine and Tenofovir.

Franchetti P, Cappellacci L, Petrelli R, et al
Nucleosides Nucleotides Nucleic Acids. 2007;26(8-9):953-7.
Abstract
 
Acceptability of tenofovir gel as a vaginal microbicide by US male participants in a Phase I
clinical trial (HPTN 050).

Carballo-Diéguez A, Balán IC 
AIDS Care. 2007 Sep;19(8):1026-31.
Abstract
 
Effects of HIV Protease Inhibitors on the Intestinal Absorption of Tenofovir Disoproxil
Fumarate in vitro.

Tong L, Phan TK, Robinson KL, et al  

Antimicrob Agents Chemother.
2007 Jul 30;
Abstract
 
Effects of the Translocation Status of HIV-1 Reverse Transcriptase on the Efficiency of
Excision of Tenofovir

Marchand B, White KL, Ly JK, et al 
Antimicrob Agents Chemother. 2007 May 21;
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
CD4+ T cell evolution and predictors of its trend before and after tenofovir/didanosine
backbone in the presence of sustained undetectable HIV plasma viral load.

Torti C, Lapadula G, Barreiro P, et al   
J Antimicrob Chemother. 2007 Apr 13;
Abstract
 
No change in calculated creatinine clearance after tenofovir initiation among Thai patients.
Gayet-Ageron A, Ananworanich J, Jupimai T, et al 
J Antimicrob Chemother. 2007 Mar 21
Abstract
 
Inhibition of human liver microsomal cytochrome P450 activities by adefovir and tenofovir.
Nekvindova J, Masek V, Veinlichova A, et al 
Xenobiotica. 2006 Dec;36(12):1165-77.
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Tenofovir disoproxil fumarate for the treatment of HIV infection.
Pham PA, Gallant JE.
Expert Opin Drug Metab Toxicol. 2006 Jun;2(3):459-469.
Abstract
 
Cost-effectiveness analysis of tenofovir versus zidovudine in combination therapy with efavirenz
and lamivudine for the treatment of HIV in naive patients.

Fernandez Lison L, Pujol de la Llave E, Hevia Alonso A, et al 
Farm Hosp. 2005;29(1):11-17
Abstract
 
Serum Hypophosphatemia in Tenofovir Disoproxil Fumarate Recipients Is Multifactorial in
Origin, Questioning the Utility of Its Monitoring in Clinical Practice.
Day SL, Leake Date HA, Bannister A, et al 
J Acquir Immune Defic Syndr. 2005 Mar 1;38(3):301-304.
Abstract
 
Tenofovir Disoproxil Fumarate: A Review of its Use in the Management of HIV infection.
Lyseng-Williamson KA, Reynolds NA, Plosker GL.

Drugs. 2005;65(3):413-32.
Abstract

Tenofovir: new indication. For first-line antiretroviral therapy: wait and see.
[No authors listed] 

Prescrire Int. 2004 Oct;13(73):180-2.
Abstract
 
Genotypic and phenotypic predictors of the magnitude of response to tenofovir
disoproxil fumarate treatment in antiretroviral-experienced patients.
Miller MD, Margot N, Lu B, et al
J Infect Dis. 2004 Mar 1;189(5):837-46.
Abstract
 
Clinical potential of the acyclic nucleoside phosphonates cidofovir, adefovir, and
tenofovir in treatment of DNA virus and retrovirus infections.
De Clercq E

Clin Microbiol Rev. 2003 Oct;16(4):569-96.
Abstract

Tenofovir disoproxil fumarate.
Gallant JE, Deresinski S.
 
Clin Infect Dis.
2003 Oct 1;37(7):944-50
Abstract

Tenofovir disoproxil fumarate.
Grim SA, Romanelli F .

Ann Pharmacother 2003 Jun;37(6):849-59
Abstract


Animal Studies
 

 
FULL-TEXT ARTICLE
Prevention of SIV Rectal Transmission and Priming of T Cell Responses in Macaques after Local Pre-exposure Application of
Tenofovir Gel.

Cranage M, Sharpe S, Herrera C, et al

PLoS Med. 2008 Aug 5;5(8)
Paper

Safety
 

 
A WEEK-IN-REVIEW FEATURED REPORT
The safety of tenofovir disoproxil fumarate for the treatment of HIV infection in adults:
the first 4 years.

Nelson MR, Katlama C, Montaner JS, et al

AIDS.
2007 Jun;21(10):1273-1281
Abstract

Long-term renal safety of tenofovir disoproxil fumarate in antiretroviral-naive
HIV-1-infected patients. Data from a double-blind randomized active-controlled
multicentre study.
Izzedine H, Hulot JS, Vittecoq D, et al 

Nephrol Dial Transplant. 2005 Mar
Abstract


Pharmacokinetics
 

 
The Pharmacokinetics and Viral Activity of Tenofovir in the Male Genital Tract.
Vourvahis M, Tappouni HL, Patterson KB, et al 
J Acquir Immune Defic Syndr. 2008 Jan 11
Abstract
 
Pharmacokinetics of Antiretroviral Regimens Containing Tenofovir Disoproxil Fumarate and
Atazanavir/Ritonavir in Adolescents and Young Adults with HIV Infection - Study ATN056.

Kiser JJ, Fletcher CV, Flynn PM, et al 
Antimicrob Agents Chemothe
r. 2007 Nov 19;
Abstract
 
Pharmacokinetics of once-daily tenofovir, emtricitabine, ritonavir and fosamprenavir
in HIV-infected subjects.

Parks DA, Jennings HC, Taylor CW, Acosta EP.

AIDS
. 2007 Jun;21(10):1373-5.
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
FULL-TEXT ARTICLE

The distribution of the anti-HIV drug, tenofovir (PMPA), into the brain, CSF and choroid plexuses.
Anthonypillai C, Gibbs JE, Thomas SA.
Cerebrospinal Fluid Res. 2006 Jan 3;3(1):1
Paper
 
Population pharmacokinetics of tenofovir in human immunodeficiency virus-infected patients taking
highly active antiretroviral therapy.

Jullien V, Treluyer JM, Rey E, et al
Antimicrob Agents Chemother.
2005 Aug;49(8):3361-6.
Abstract
 
Intracellular Pharmacokinetics of Tenofovir Diphosphate, Carbovir Triphosphate, and
Lamivudine Triphosphate in Patients Receiving Triple-Nucleoside Regimens.
Hawkins T, Veikley W, St Claire RL 3rd , et al
J Acquir Immune Defic Syndr. 2005 Aug 1;39(4):406-
Abstract
 
Effect of tenofovir disoproxil fumarate on the pharmacokinetics and pharmacodynamics
of total, R-, and S-methadone.

Smith PF, Kearney BP, Liaw S, et al 

Pharmacotherapy. 2004 Aug;24(8):970-7.
Abstract
 
Studies of molecular mechanism of Tenofovir against 3TC- and AZT-resistance
mutant HIV-1 reverse transcriptase.
Chong Y, Akula N, Chu CK. et al.
Bioorg Med Chem Lett. 2003 Nov 17;13(22):4019-22
Abstract
 
FULL-TEXT ARTICLE
Phase i/ii trial of the pharmacokinetics, safety, and antiretroviral activity of tenofovir
disoproxil fumarate in human immunodeficiency virus-infected adults.
Barditch-Crovo P, Deeks SG, Collier A, et al.
Antimicrob Agents Chemother 2001 Oct;45(10):2733-2739
Paper

Drug/Drug Interactions
 

 
Pharmacokinetics and safety of tenofovir disoproxil fumarate on coadministration with
lopinavir/ritonavir.

Kearney BP, Mathias A, Mittan A, et al 
J Acquir Immune Defic Syndr. 2006 Nov 1;43(3):278-83.
Abstract
 
Absence of clinically relevant pharmacokinetic interaction between ribavirin and tenofovir in healthy
subjects.
Ramanathan S, Cheng A, Mittan A, et al  

J Clin Pharmacol.
2006 May;46(5):559-66.
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Assessment of Drug-Drug Interactions Between Tenofovir Disoproxil Fumarate and the
Nonnucleoside Reverse Transcriptase Inhibitors Nevirapine and Efavirenz in HIV-Infected Patients.

Droste JA, Kearney BP, Hekster YA, Burger DM.

J Acquir Immune Defic Syndr.
2006 Jan 1;41(1):37-43.
 
Lack of pharmacokinetic drug interaction between tenofovir disoproxil fumarate and nelfinavir
mesylate.
Boffito M, Pozniak A, Kearney BP, et al 
Antimicrob Agents Chemother. 2005 Oct;49(10):4386-9.
Abstract
 
Measurement of Intracellular Didanosine and Tenofovir Phosphorylated Metabolites and Possible
Interaction of the Two Drugs in Human Immunodeficiency Virus-Infected Patients.

Pruvost A, Negredo E, Benech H, et al 
Antimicrob Agents Chemother.
2005 May;49(5):1907-1914
Abstract
 
Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy
volunteers.
Droste JA, Verweij-van Wissen CP, et al 
Antimicrob Agents Chemother.2005 Feb;49(2):680-4.
Abstract
 
Pancreatitis treated with didanosine and tenofovir disoproxil fumarate.
Blanchard JN, Wohlfeiler M, Canas A, et al 
Clin Infect Dis. 2003 Sep 1;37(5):e57-62.
Abstract
 
Effect of Tenofovir on Didanosine Absorption in Patients with HIV.
Pecora Fulco P, Kirian MA.

Ann Pharmacother. 2003 Sep;37(9):1325-1328

Abstract

Viral Dynamics
 

  Virological response to HIV-1 nucleoside/nucleotide reverse transcriptase inhibitors-based,
tenofovir DF-including regimens in the ANRS Aquitaine Cohort.
Balestre E, Dupon M, Capdepont S, et al  
 
J Clin Virol.
2006 Mar 21;
Abstract

Resistance
 

 
A WEEK IN REVIEW FEATURED REPORT
Changing patterns in HIV reverse transcriptase resistance mutations after availability of tenofovir.
de Mendoza C, Jiménez-Nacher I, Garrido C,
Clin Infect Dis. 2008 Jun 1;46(11):1782-5
Abstract
 
A WEEK IN REVIEW FEATURED REPORT
Factors Associated with the Emergence of K65R in Patients with HIV-1 Infection Treated with
Combination Antiretroviral Therapy Containing Tenofovir.

von Wyl V, Yerly S, Böni J, et al
 
Clin Infect Dis.
2008 Apr 15;46(8):1299-1309.
Abstract
 
Changing Patterns in HIV Reverse Transcriptase Resistance Mutations after Availability of
Tenofovir.

Mendoza CD, Jiménez-Nacher I, Garrido C, et al
Clin Infect Dis. 2008 Apr 21
Abstract
 
Molecular basis of antagonism between K70E and K65R tenofovir-associated mutations in HIV-1
reverse transcriptase.

Kagan RM, Lee TS, Ross L, et al

Antiviral Res
. 2007 Apr 4
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Long-term follow-up of patients taking tenofovir DF with low-level HIV-1 viremia and the
K65R substitution in HIV-1 RT.

Chappell BJ, Margot NA, Miller MD.

AIDS
. 2007 Mar 30;21(6):761-3
Abstract
 
Functional involvement of multidrug resistance associated protein 4 (MRP4/ABCC4)
in the renal elimination of the anti-viral drugs, adefovir and tenofovir.

Imaoka T, Kusuhara H, Adachi M, et al 

Mol Pharmacol.
2006 Nov 16;
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Resistance development over 144 weeks in treatment-naive patients receiving tenofovir disoproxil
fumarate or stavudine with lamivudine and efavirenz in Study 903.
Margot NA, Lu B, Cheng A, Miller MD;

HIV Med. 2006 Oct;7(7):442-50

Abstract
 

Resistance mutations before and after tenofovir regimen failure in HIV-1 infected patients.
Wirden M, Marcelin AG, Simon A,   
J Med Virol. 2005 May 18;76(3):297-301
Abstract
 

Patterns of Resistance Emerging in HIV-1 From Antiretroviral-Experienced Patients
Undergoing Intensification Therapy With Tenofovir Disoproxil Fumarate.
McColl DJ, Margot NA, Wulfsohn M, et al.
J Acquir Immune Defic Syndr. 2004 Nov 1;37(3):1340-50
Abstract
 
Human Immunodeficiency Virus Type 1 Reverse Transcriptase Mutation Selection during
In Vitro Exposure to Tenofovir Alone or Combined with Abacavir or Lamivudine.
Stone C, Ait-Khaled M, Craig C, et al    
Antimicrob Agents Chemother. 2004 Apr;48(4):1413-5.
Abstract

Tenofovir Resistance and Resensitization.
Wolf K, Walter H, Beerenwinkel N, et al

Antimicrob Agents Chemother
. 2003 Nov;47(11):3478-3484
.
Abstract
  Phenotypic susceptibilities to tenofovir in a large panel of clinically derived human
immunodeficiency virus type 1 isolates.

Harrigan PR, Miller MD, McKenna P, et al.
Antimicrob Agents Chemother 2002Apr;46(4):1067-72
Abstract
  Tenofovir, Adefovir, and Zidovudine Susceptibilities of Primary Human Immunodeficiency
Virus Type 1 Isolates with Non-B Subtypes or Nucleoside Resistance.
Palmer S, Margot N, Gilbert H, et al.
AIDS Res Hum Retroviruses 2001 Aug 10;17(12):1167-1173
Abstract

Diagnostic/Monitoring
       

 
A new assay based on solid-phase extraction procedure with LC-MS to measure plasmatic concentrations
of tenofovir and emtricitabine in HIV infected patients.
D'Avolio A, Sciandra M, Siccardi M, et al
  
J Chromatogr Sci.
2008 Jul;46(6):524-8.
Abstract
 
FULL TEXT PDF ARTICLE
Determination of plasma tenofovir concentrations using a conventional LC-MS method.
Takahashi M, Kudaka Y, Okumura N,  et al
 
Biol Pharm Bull.
2007 Sep;30(9):1784-6.

Paper
 
Relevance of a combined UV and single mass spectrometry detection for the determination of
tenofovir in human plasma by HPLC in therapeutic drug monitoring.

Barkil ME, Gagnieu MC, Guitton J.
J Chromatogr B Analyt Technol Biomed Life Sci. 2007 Apr 19;
Abstract
 
Renal tubular toxicity associated with tenofovir assessed using urine-beta 2 microglobulin,
percentage of tubular reabsorption of phosphate and alkaline phosphatase levels.
Kinai E, Hanabusa H.

AIDS.
2005 Nov 18;19(17):2031-2033.
Abstract
 

Simultaneous quantification of emtricitabine and tenofovir in human plasma using high-
performance liquid chromatography after solid phase extraction.
Rezk NL, Crutchley RD, Kashuba AD.  
J Chromatogr B Analyt Technol Biomed Life Sc
i. 2005 Jul 5;

Abstract


Therapeutic Strategies
       

 
Cost and Cost-Effectiveness of Switching From Stavudine to Tenofovir in First-Line Antiretroviral Regimens
in South Africa.
Rosen S, Long L, Fox M, Sanne I.
  
J Acquir Immune Defic Syndr.
2008 Jul 1;48(3):334-344.
Abstract
 

A WEEK-IN-REVIEW FEATURED REPORT
Intensification of a triple-nucleoside regimen with tenofovir or efavirenz in HIV-1-infected
patients with virological suppression.

Gulick RM, Lalama CM, Ribaudo HJ, et al
AIDS. 2007 Apr 23;21(7):813-823.
Abstract
 

Sustained improvement of dyslipidaemia in HAART-treated patients replacing stavudine with
tenofovir.
Llibre JM, Domingo P, Palacios R, et al  

AIDS.
2006 Jun 26;20(10):1407-14.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
Improvement of Dyslipidemia during Different HAART Regimens: Tenofovir- versus Stavudine-
Containing Antiretroviral Combinations.

Manfredi R.
 
Clin Infect Dis.
2006 May 1;42(9):1345-7.

Abstract
 
FULL-TEXT ARTICLE
Media reporting of tenofovir trials in Cambodia and Cameroon.
Mills E, Rachlis B, Wu P, et al
BMC Int Health Hum Rights.  2005 Aug 24;5:6.
Paper


Vaginal Gel
       

  Safety and tolerability of tenofovir vaginal gel in abstinent and sexually active
HIV-infected and uninfected women.
Mayer KH, Maslankowski LA, Gai F, et al

AIDS. 2006 Feb 28;20(4):543-551.
Abstract

Discontinuation
       

  A WEEK IN REVIEW FEATURED REPORT
FULL-TEXT PDF DOCUMENT

Analysis of the causes and predictive factors for discontinuing treatment with tenofovir in
pretreated HIV patients.

Morillo Verdugo R, Gil Navarro MV, Abdel-Kader Martín L, et al

Farm Hosp.
2007 Aug;31(4):200-205.
Paper

Prophylaxis
       

 
Changes in Sexual Risk Behavior Among Participants in a PrEP HIV Prevention Trial.   
Guest G, Shattuck D, Johnson L, et al
Sex Transm Dis. 2008 Jul 25.
Abstract

A WEEK-IN-REVIEW FEATURED REPORT
FULL TEXT ARTICLE

Tenofovir Disoproxil Fumarate for Prevention of HIV Infection in Women: A Phase 2, Double-Blind,
Randomized, Placebo-Controlled Trial.

Peterson L, Taylor D, Roddy R, et al
PLoS Clin Trials. 2007 May 25;2(5):e27.

Paper

Tenofovir trials raise ethical issues.
Mills E.

HIV AIDS Policy Law Rev. 2
005 Aug;10(2):31-2.
Abstract

Vaginal Microbicide Studies
       

  Acceptability of Tenofovir Gel as a Vaginal Microbicide Among Women in a Phase I Trial:
A Mixed-Methods Study.
Rosen RK, Morrow KM, Carballo-Diéguez A, et al   
J Womens Health (Larchmt). 2008 Mar 8
Abstract


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