565
Views
8
CrossRef citations to date
0
Altmetric
Drug Evaluations

Emtricitabine/tenofovir in the treatment of HIV infection: current PK/PD evaluation

, MD, , MD, , MD & , MD
Pages 1305-1314 | Published online: 04 Sep 2012

Bibliography

  • Fielden SJ, Rusch ML, Yip B, Nonadherence increases the risk of hospitalization among HIV-infected antiretroviral naive patients started on HAART. J Int Assoc Physicians AIDS Care 2008;7:238-44
  • Kitahata MM, Reed SD, Dillingham PW, Pharmacy-based assessment of adherence to HAART predicts virologic and immunologic treatment response and clinical progression to AIDS and death. Int J STD AIDS 2004;15:803-10
  • Lima VD, Harrigan R, Bangsberg DR, The combined effect of modern highly active antiretroviral therapy regimens and adherence on mortality over time. J Acquir Immune Defic Syndr 2009;50:529-36
  • EACS Guidelines Version 6 –October 2011. Available from: http://www.europeanaidsclinicalsociety.org/images/stories/EACS-Pdf/eacsguidelines-v6_english.pdf [Last accessed 20 May 2012]
  • Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services. 1–239. 2012. Available from: http://www.aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf [Last accessed 20 May 2012]
  • Arribas JR, Pozniak AL, Gallant JE, Tenofovir disoproxil fumarate, emtricitabine, and efavirenz compared with zidovudine/lamivudine and efavirenz in treatment-naive patients: 144-week analysis. J Acquir Immune Defic Syndr 2008;47:74-8
  • Fisher M, Moyle GJ, Shahmanesh M, for SWEET (Simplification With Easier EmtricitabineTenofovir) group UK. A randomized comparative trial of continued zidovudine/lamivudine or replacement with tenofovirdisoproxilfumarate/emtricitabine in efavirenz-treated HIV-1-infected individuals. J Acquir Immune Defic Syndr 2009;51:562-8
  • Sax PE, Tierney C, Collier AC, for AIDS Clinical Trials Group Study A5202 Team. Abacavir-lamivudine versus tenofovir-emtricitabine for initial HIV-1 therapy. N Engl J Med 2009;361:2230-40
  • Post FA, Moyle GJ, Stellbrink HJ, Randomized comparison of renal effects, efficacy, and safety with once-daily abacavir/lamivudine versus tenofovir/emtricitabine, administered with efavirenz, in antiretroviral-naive, HIV-1-infected adults: 48-week results from the ASSERT study. J Acquir Immune Defic Syndr 2010;55:49-57
  • Smith KY, Patel P, Fine D, for HEAT Study Team. Randomized, double-blind, placebo-matched, multicenter trial of abacavir/lamivudine or tenofovir/emtricitabine with lopinavir/ritonavir for initial HIV treatment. AIDS 2009;23:1547-56
  • Martin A, Amin J, Emery S, STEAL Study Group. Predictors of limb fat gain in HIV positive patients following a change to tenofovir-emtricitabine or abacavir-lamivudine. PLoS One 2011;6:e26885
  • Behrens G, Maserati R, Rieger A, Switching from Kivexa [ABC/3TC]+Kaletra [LPV/r] to Truvada [TDF/FTC]+Kaletra [LPV/r] Reduces High Cholesterol: results of a 12 Week Randomized, Controlled Study (ROCKET II) [Poster WEPE0110]. 18th Internatonal AIDS Conference; Wien, Austria; 2010
  • Cooper RD, Wiebe N, Smith N, Systematic review and meta-analysis: renal safety of tenofovir disoproxil fumarate in HIV-infected patients. Clin Infect Dis 2010;51:496-505
  • Gazzard BG. Use of tenofovir disoproxil fumarate and emtricitabine combination in HIV-infected patients. Expert Opin Pharmacother 2006;7:793-802
  • Somboonwit C, Kurtyka D, Velez AP. Abacavir and lamivudine combination. Expert Opin Drug Metab Toxicol 2009;5:1599-606
  • Costagliola D, Lang S, Mary-Krause M, Abacavir and cardiovascular risk: reviewing the evidence. Curr HIV/AIDS Rep 2010;7:127-33
  • Blum MR, Chittick GE, Begley JA, Steady-state pharmacokinetics of emtricitabine and tenofovir disoproxil fumarate administered alone and in combination in healthy volunteers. J Clin Pharmacol 2007;47:751-9
  • Truvada® capsules. Product Monograph. March 13, 2012
  • Bang LM, Scott LJ. Emtricitabine: an antiretroviral agent for HIV infection. Drugs 2003;63:2413-24
  • Shaw J-P, Sueoka CM, Oliyai R, Metabolism and pharmacokinetics of novel oral prodrugs of 9-[(R)-2-(phosphonomethoxy)propyl]adenine (PMPA) in dogs. Pharm Res 1997;14:1824-9
  • Suo Z, Johnson KA. Selective inhibition of HIV-1 reverse transcriptase by an antiviral inhibitor, (R)-9-(2- phosphonylmethoxypropyl)adenine. J Biol Chem 1998;273:27250-8
  • Schinazi RF, McMillan A, Cannon D, Selective inhibition of human immunodeficiency viruses by racemates and enantiomers of cis-5-fluoro-1-[2-(hydromethyl)-1, 3-oxathiolan-5-yl]cytosine. Antimicrob Agents Chemother 1992;36:2423-31
  • Hazen R, Lanier ER. Relative anti-HIV-1 efficacy of lamivudine and emtricitabine in vitro is dependent on cell type. J Acquir Immune Defic Syndr 2003;32:255-8
  • Rousseau FS, Kahn JO, Thompson M, Prototype trial design for rapid dose selection of antiretroviral drugs: an example using emtricitabine (Coviracil). J Antimicrob Chemother 2001;48:507-13
  • Rousseau FS, Wakeford C, Mommeja-Marin H, Prospective randomized trial of emtricitabine versus lamivudine short-term monotherapy in human immunodeficiency virus-infected patients. J Infect Dis 2003;188:1652-8
  • Schinazi RF, Lloyd RM Jr, Nguyen M-H, Characterization of human immunodeficiency viruses resistant to oxathiolane-cytosine nucleosides. Antimicrob Agents Chemother 1993;37:875-81
  • Borroto-Esoda K, Quinn J, Harris J, Lower incidence if the M184V mutation in ART naïve patients receiving combination therapy with emtricitabine (FTC) compared to lamivudine (3TC), results of a double blind equivalence trial [abstract LB-P21]. 1st IAS Conference on HIV Pathogenesis and Treatment; Buenos Aires, Argentina; 2001
  • Sanne I, Anderson J, Kargl D, for the MKC-401 Study Team. Evaluation of emtricitabine within a triple NRTI HAART Regimen [abstract H-868]. 43rd Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC); Chicago, USA; 2003
  • Maserati R, De Silvestri A, Uglietti A, for ARCA Collaborative Group. Emerging mutations at virological failure of HAART combinations containing tenofovir and lamivudine or emtricitabine. AIDS 2010;24:1013-18
  • Svicher V, Alteri C, Artese A, Different evolution of genotypic resistance profiles to emtricitabine versus lamivudine in tenofovir-containing regimens. J Acquir Immune Defic Syndr 2010;55:336-44
  • Marcelin AG, Charpentier C, Wirden M, Resistance profiles of emtricitabine and lamivudine in tenofovir-containing regimens. J Antimicrob Chemother 2012;67:1475-8
  • McColl DJ, Margot N, Chen SS, Reduced emergence of the M184V/I resistance mutation when antiretroviral-naïve subjects use emtricitabine versus lamivudine in regimens composed of two NRTIs plus the NNRTI efavirenz. HIV Clin Trials 2011;12:61-70
  • Robbins BL, Srinivas RV, Kim C, Anti-human immunodeficiency virus activity and cellular metabolism of a potential prodrug of the acyclic nucleoside phosphonate 9-R-(2-phosphonomethoxypropyl)adenine (PMPA), Bis(isopropylox-ymethylcarbonyl) PMPA. Antimicrob Agents Chemother 1998;42:612-17
  • Barditch-Crovo P, Deeks SG, Collier A, Phase i/ii trial of the pharmacokinetics, safety, and antiretroviral activity of tenofovir disoproxil fumarate in human immunodeficiency virus-infected adults. Antimicrob Agents Chemother 2001;45:2733-9
  • Louie M, Hogan C, Hurley A, Determining the antiviral activity oftenofovirdisoproxilfumaratein treatment-naïve chronically HIV-1-infected individuals. AIDS 2003;17:1151-6
  • Borroto-Esoda K, Vela JE, Myrick F, In vitro evaluation of the anti-HIV activity and metabolic interactions of tenofovir and emtricitabine. Antivir Ther 2006;11:377-84
  • Miller MD. K65R, TAMs and tenofovir. AIDS Rev 2004;6:22-33
  • Wainberg MA, Miller MD, Quan Y, In vitro selection and characterization of HIV-1 with reduced susceptibility to PMPA. Antivir Ther 1999;4:87-94
  • Chapman T, McGavin J, Noble S. Tenofovir disoproxil fumarate. Drugs 2003;63:1597-608
  • Margot NA, Waters JM, Miller MD. In vitro human immunodeficiency virus type 1 resistance selections with combinations of tenofovir and emtricitabine or abacavir and lamivudine. Antimicrob Agents Chemother 2006;50:4087-95
  • Brenner BG, Coutsinos D. The K65R mutation in HIV-1 reverse transcriptase: genetic barriers, resistance profile and clinical implications. HIV Ther 2009;3:583-94
  • Emtriva® capsules. Product Monograph. July 27, 2011
  • Wang LH, Begley J, St Claire RL III, Pharmacokinetic and pharmacodynamic characteristics of emtricitabine support its once daily dosing for the treatment of HIV infection. AIDS Res Hum Retrovir 2004;20:1173-82
  • Frampton JE, Perry CM. Emtricitabine. A review of its use in the management of HIV infection. Drugs 2005;65:1427-48
  • Viread® capsules. Product Monograph. February 6, 2012
  • Kohler JJ, Hosseini SH, Green E, Tenofovir renal proximal tubular toxicity is regulated by OAT1 and MRP4 transporters. Lab Invest 2011;91:852-8
  • Lebrecht D, Venhoff AC, Kirschner J, Mitochondrial tubulopathy in tenofovir disoproxil fumarate-treated rats. J Acquir Immune Defic Syndr 2009;51:258-63
  • Vidal F, Domingo JC, Guallar J, In vitro cytotoxicity and mitochondrial toxicity of tenofovir alone and in combination with other antiretrovirals in human renal proximal tubule cells. Antimicrob Agents Chemother 2006;50:3824-32
  • Agarwala S, Eley T, Villegas C, Pharmacokinetic interaction between tenofovir and atazanavir coadministered with ritonavir in healthy subjects [abstract 16]. 6th International Workshop on Clinical Pharmacology of HIV Therapy; Quebec City, Canada; 2005
  • Kiser JJ, Fletcher CV, Flynn PM, for Adolescent Trials Network for HIV/AIDS Interventions. Pharmacokinetics of antiretroviral regimens containing tenofovir disoproxil fumarate and atazanavir-ritonavir in adolescents and young adults with human immunodeficiency virus infection. Antimicrob Agents Chemother 2008;52:631-7
  • Kiser JJ, Carten ML, Aquilante CL, The effect of lopinavir/ritonavir on the renal clearance of tenofovir in HIV-infected patients. Clin Pharmacol Ther 2008;83:265-72
  • Anderson PL. Recent developments in the clinical pharmacology of anti-HIV nucleoside analogs. Curr Opin HIV AIDS 2008;3:258-65
  • http://www.hiv-druginteractions.org; http://hivinsite.ucsf.edu/insite?page=ar-00-02; both accessed online on July 13, 2012)
  • Hawkins T, Veikley W, St Claire RL III, Intracellular pharmacokinetics of tenofovir diphosphate, carbovir triphosphate, and lamivudine triphosphate in patients receiving triple-nucleoside regimens. J Acquir Immune Defic Syndr 2005;39:406-11
  • Pruvost A, Negredo E, Benech H, Measurement of intracellular di- danosine and tenofovir phosphorylated metabolites and possible interaction of the two drugs in human immunodeficiency virus-infected patients. Antimicrob Agents Chemother 2005;49:1907-14
  • Margot NA, Enejosa J, Cheng AK, for Study 934 Team. Development of HIV-1 drug resistance through 144 weeks in antiretroviral-naïve subjects on emtricitabine, tenofovir disoproxil fumarate, and efavirenz compared with lamivudine/zidovudine and efavirenz in study GS-01-934. J Acquir Immune Defic Syndr 2009;52:209-21
  • Sax PE, Tierney C, Collier AC, for the AIDS Clinical Trials Group Study A5202 Team. Avir/lamivudine versus tenofovir DF/emtricitabine as part of combination regimens for initial treatment of HIV: final results. J Infect Dis 2011;204:1191-201
  • Moyle GJ, Stellbrink HJ, Compston J, Comparison of Bone and Renal Toxicities in the ASSERT Study: Final 96-Week Results From a Prospective Randomised Safety Trial (oral presentation O23). 12th International Workshop on Adverse Drug Reactions and Co-morbidities in HIV; London, United Kingdom; 2010
  • Molina JM, Andrade-Villanueva J, Echevarria J, for CASTLE Study Team. Once-daily atazanavir/ritonavir versus twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 48 week efficacy and safety results of the CASTLE study. Lancet 2008;372:646-55
  • Orkin C, DeJesus E, Khanlou H, ARTEMIS: 192-week efficacy and safety of once-daily darunavir/ritonavir (DRV/r) vs lopinavir/r (LPV/r) in treatment-naïve HIV-1-infected adults. J Int AIDS Soc 2010;13:P3
  • Rockstroh JK, Lazzarin A, Zhao J, Long-term Efficacy of Raltegravir (RAL) or Efavirenz (EFV) Combined with Tenofovir (TDF) and Emtricitabine (FTC) in Treatment-naive HIV-1-infected Patients: Wk-192 Subgroup Analysis from the STARTMRK trial [abstract PS1/1]. 13th European AIDS Conference; Belgrade, Serbia; 2011
  • Nelson M, Behrens G, Cohen C, Sustained efficacy with low and similar rates of virologic failures in second year observed with rilpivirine versus efavirenz plus emtricitabine/tenofovir DF in treatment-naive, HIV-1 infected adults–pooled 96-week ECHO and THRIVE analysis [abstract LBPE7.3/7]. 13th European AIDS Conference; Belgrade, Serbia; 2011
  • DeJesus E, Rockstroh JK, Henry H, Efficacy and safety of elvitegravir/cobicistat/emtricitabine/tenofovir DF “Quad” compared to ritonavir-boosted atazanavir plus emtricitabine/tenofovir DF in treatment naïve HIV-1 infected subjects [Poster #627]. 19th Conference on Retroviruses and Opportunistic Infections; Seattle, USA; 2012
  • Dando TM, Wagstaff AJ. Emtricitabine/tenofovir disoproxil fumarate. Drugs 2004;64:2075-82
  • Munoz de Benito RM, Arribad Lopez JR. Tenofovir disoproxil fumarate- emtricitabine coformulation for once-daily dual NRTI backbone. Expert Rev Anti Infect Ther 2006;4:523-35
  • Izzedine H, Isnard-Bagnis C, Hulot JS, Renal safety of tenofovir in HIV treatment-experienced patients. AIDS 2004;18:1074-6
  • Kohler JJ, Hosseini SH, Hoying-Brandt A, Tenofovir renal toxicity targets mitochondria of renal proximal tubules. Lab Invest 2009;89:513-19
  • Tong L, Phan TK, Robinson KL, Effects of Human Immunodeficiency Virus Protease Inhibitors on the Intestinal Absorption of Tenofovir Disoproxil Fumarate In Vitro. Antimicrob Agents Chemother 2007;51:3498-504
  • Louiseau-Peres S, Delaunay C, Lespessailles E, Osteopenia in patients infected by the human im- munodeficiency virus. A case control study. Clin Infect Dis 2002;69:482-5
  • Amiel C, Ostertag A, Slama L, BMD is reduced in HIV-infected men irrespective of treatment. J Bone Miner Res 2004;19:402-9
  • Ofotokun I, McIntosh E, Weitzmann MN. HIV: inflammation and bone. Curr HIV/AIDS Rep 2012;9:16-25
  • Tebas P, Powderly WG, Claxton S, Accelerated bone mineral loss in HIV- infected patients receiving potent antiretroviral therapy. AIDS 2000;14:F63-7
  • Bedimo R, Maalouf NM, Zhang S, Osteoporotic fracture risk associated with cumulative exposure to tenofovir and other antiretroviral agents. AIDS 2012;26:825-31
  • McComsey GA, Kitch D, Daar ES, Bone mineral density and fractures in antiretroviral-naive persons randomized to receive abacavir-lamivudine or tenofovirdisoproxilfumarate-emtricitabine along with efavirenz or atazanavir-ritonavir: Aids Clinical Trials Group A5224s, a substudy of ACTG A5202. J Infect Dis 2011;203:1791-801
  • Womack JA, Goulet JL, Gibert C, for Veterans Aging Cohort Study Project Team. Increased risk of fragility fractures among HIV infected compared to uninfected male veterans. PLoS ONE 2011;6:e17217
  • Hansen AB, Gerstoft J, Kronborg G, Incidence of low and high-energy fractures in persons with and without HIV infection: a Danish population-based cohort study. AIDS 2012;26:285-93
  • Jones R, Stebbing J, Nelson M, Renal dysfunction with tenofovirdisoproxilfumarate-containing highly active antiretroviral therapy regimens is not observed more frequently: a cohort and case-control study. J Acquir Immune Defic Syndr 2004;37:1489-95
  • Kalyesubula R, Perazella MA. Nephrotoxicity of HAART. AIDS Res Treat 2011;2011:562790
  • Campbell LJ, Ibrahim F, Fisher M, Spectrum of chronic kidney disease in HIV-infected patients. HIV Med 2009;10:329-36
  • Gallant JE, Parish MA, Keruly JC, Changes in renal function associated with tenofovir disoproxil fumarate treatment, compared with nucleoside reverse-transcriptase inhibitor treatment. Clin Infect Dis 2005;40:1194-8
  • Wever K, van Agtmael MA, Carr A. Incomplete reversibility of tenofovir-related renal toxicity in HIV-infected men. J Acquir Immune Defic Syndr 2010;55:78-81
  • Tungsiripat M, Kitch D, Glesby MJ, A pilot study to determine the impact on dyslipidemia of adding tenofovir to stable background antiretroviral therapy: ACTG 5206. AIDS 2010;24:1781-4
  • Hill A, Sawyer W. Effects of nucleoside reverse transcriptase inhibitor backbone on the efficacy of first-line boosted highly active antiretroviral therapy based on protease inhibitors: meta-regression analysis of 12 clinical trials in 5168 patients. HIV Med 2009;10:527-35
  • Feng JY, Ly JK, Myrick F, The triple combination of tenofovir, emtricitabine and efavirenz shows synergistic anti-HIV-1 activity in vitro: a mechanism of action study. Retrovirology 2009;6:44
  • Gallant JE, DeJesus E, Arribas JR, Tenofovir DF, emtricitabine, and efavirenz vs. zidovudine, lamivudine, and efavirenz for HIV. N Engl J Med 2006;354:251-60
  • Pozniak AL, Gallant JE, DeJesus E, Tenofovir disoproxil fumarate, emtricitabine, and efavirenz versus fixed-dose zidovudine/lamivudine and efavirenz in antiretroviral-naive patients: virologic, immunologic, and morphologic changes–a 96-week analysis. J Acquir Immune Defic Syndr 2006;43:535-40
  • Lazzarin A, Johnson M, Ribera E, 5-year safety and efficacy of the once-daily antiretroviral regimen of efavirenz (EFV)/emtricitabine (FTC)/tenofovir disoproxil fumarate (TDF). 10th International Congress on Drug Therapy in HIV Infection; Glasgow, UK; 2010. p. P006
  • Molina JM, Andrade-Villanueva J, Echevarria J, Once-daily atazanavir/ritonavir compared with twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine, for management of antiretroviral-naive HIV-1-infected patients: 96-week efficacy and safety results of the CASTLE study. J Acquir Immune Defic Syndr 2010;53:33-2
  • Ortiz R, Dejesus E, Khanlou H, Efficacy and safety of once-daily darunavir/ritonavir versus lopinavir/ritonavir in treatment-naive HIV-1-infected patients at week 48. AIDS 2008;22:1389-97
  • Mills AM, Nelson M, Jayaweera D, Once-daily darunavir/ritonavir vs. lopinavir/ritonavir in treatment-naive, HIV-1-infected patients: 96-week analysis. AIDS 2009;23:1679-88
  • Lennox JL, DeJesus E, Lazzarin A, Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial. Lancet 2009;374:796-806
  • Lennox JL, Dejesus E, Berger DS, Raltegravir versus efavirenz regimens in treatment-naive HIV-1-infected patients: 96-week efficacy, durability, subgroup, safety, and metabolic analyses. J Acquir Immune Defic Syndr 2010;55:39-48
  • Rockstroh JK, Lennox JL, Dejesus E, Long-term treatment with raltegravir or efavirenz combined with tenofovir/emtricitabine for treatment-naive human immunodeficiency virus-1-infected patients: 156-week results from STARTMRK. Clin Infect Dis 2011;53:807-16
  • Cohen CJ, Molina JM, Cahn P, Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naive HIV-1-infected patients: pooled results from the phase 3 double-blind randomized ECHO and THRIVE Trials. J Acquir Immune Defic Syndr 2012;60:33-42

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.