Pharmacokinetics and pharmacodynamics of the reverse transcriptase inhibitor tenofovir and prophylactic efficacy against HIV-1 infection

PLoS ONE

Volumn 7, Issue 7, 2012, Pages

  Duwal, Sulav ^a   Schütte, Christof ^a   von Kleist, Max ^a  

^a FREIE UNIVERSITÄT BERLIN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

TENOFOVIR DISOPROXIL;

ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DISEASE TRANSMISSION; DRUG EFFICACY; DRUG HALF LIFE; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; IC 50; INFECTION PREVENTION; PERIPHERAL BLOOD MONONUCLEAR CELL; PREDICTION; SINGLE DRUG DOSE; STOCHASTIC MODEL; TREATMENT DURATION; TREATMENT RESPONSE; VIRUS LOAD;

ADENINE; ADMINISTRATION, ORAL; DOSE-RESPONSE RELATIONSHIP, DRUG; HIV INFECTIONS; HIV-1; HUMANS; INTRACELLULAR SPACE; KINETICS; MODELS, BIOLOGICAL; ORGANOPHOSPHONATES; REVERSE TRANSCRIPTASE INHIBITORS; TREATMENT OUTCOME; VIRAL LOAD;

HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 84863856906     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0040382     Document Type: Article

References (76)

1. Chapman T, McGavin J, Noble S, (2003) Tenofovir disoproxil fumarate. Drugs 63: 1597-1608.
2. National Institute of Health (NIH). (2012) Accessed: 27 Feb Current HIV treatment guidelines: Available:http://www.aidsinfo.nih.gov/guidelines/.
3. Anderson PL, Kiser JJ, Gardner EM, Rower JE, Meditz A, et al. (2011) Pharmacological considerations for tenofovir and emtricitabine to prevent HIV infection. J Antimicrob Chemother 66: 240-250.
4. Naesens L, Balzarini J, Bischofberger N, Clercq ED, (1996) Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2- phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2- phosphonylmethoxyethyl)adenine. Antimicrob Agents Chemother 40: 22-28.
5. Kearney BP, Flaherty JF, Shah J, (2004) Tenofovir disoproxil fumarate: clinical pharmacology and pharmacokinetics. Clin Pharmacokinet 43: 595-612.
6. von Kleist M, Metzner P, Marquet R, Scutte C, (2012) Polymerase inhibition by nucleoside analogs: Cellular- and kinetic parameters of efficacy, susceptibility and resistance selection. Plos Comput Biol 8: e1002359.
7. Droste JAH, van Wissen CPWGMV, Kearney BP, Buffels R, Vanhorssen PJ, et al. (2005) Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy volunteers. Antimicrob Agents Chemother 49: 680-684.
8. Blum MR, Chittick GE, Begley JA, Zong J, (2007) Steady-state pharmacokinetics of emtricitabine and tenofovir disoproxil fumarate administered alone and in combination in healthy volunteers. J Clin Pharmacol 47: 751-759.
9. Chittick GE, Zong J, Blum MR, Sorbel JJ, Begley JA, et al. (2006) Pharmacokinetics of tenofovir disoproxil fumarate and ritonavir-boosted saquinavir mesylate administered alone or in combination at steady state. Antimicrob Agents Chemother 50: 1304-1310.
10. Jullien V, Téluyer JM, Rey E, Jaffray P, Krivine A, et al. (2005) Population pharmacokinetics of tenofovir in human immunodeficiency virus-infected patients taking highly active antiretroviral therapy. Antimicrob Agents Chemother 49: 3361-3366.
11. Hawkins T, Veikley W, Claire RLS, Guyer B, Clark N, et al. (2005) Intracellular pharmacokinetics of tenofovir diphosphate, carbovir triphosphate, and lamivudine triphosphate in patients receiving triple-nucleoside regimens. J Acquir Immune Defic Syndr 39: 406-411.
12. Barditch-Crovo P, Deeks SG, Collier A, Safrin S, Coakley DF, et al. (2001) Phase I/II trial of the pharmacokinetics, safety, and antiretroviral activity of tenofovir disoproxil fumarate in human immunodeficiency virus-infected adults. Antimicrob Agents Chemother 45: 2733-2739.
13. Hirt D, Ekouvi DK, Pruvost A, Urien S, Arriv E, et al. (2011) Plasma and intracellular tenofovir pharmacokinetics in the neonate (anrs 12109 trial, step 2). Antimicrob Agents Chemother 55: 2961-2967.
14. Baheti G, Kiser JJ, Havens PL, Fletcher CV, (2011) Plasma and intracellular population pharmacokinetic analysis of tenofovir in HIV-1 infected patients. Antimicrob Agents Chemother.
15. von Kleist M, Huisinga W, (2009) Pharmacokinetic-pharmacodynamic relationship of NRTIs and its connection to viral escape: an example based on zidovudine. Eur J Pharm Sci 36: 532-543.
16. Sharma PL, Nurpeisov V, Hernandez-Santiago B, Beltran T, Schinazi RF, (2004) Nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. Curr Top Med Chem 4: 895-919.
17. Hurwitz SJ, Asif G, Schinazi RF, (2007) Development of a population simulation model for HIV monotherapy virological outcomes using lamivudine. Antivir Chem Chemother 18: 329-341.
18. Garca-Lerma JG, Paxton L, Kilmarx PH, Heneine W, (2010) Oral pre-exposure prophylaxis for HIV prevention. Trends Pharmacol Sci 31: 74-81.
19. [No authors listed], (2011) Early end for FEM-PrEP HIV prevention trial. AIDS Patient Care STDS 25: 383.
20. Grant RM, Lama JR, Anderson PL, McMahan V, Liu AY, et al. (2010) Pre-exposure chemoprophylaxis for HIV prevention in men who have sex with men. N Engl J Med 363: 2587-2599.
21. University of Washington (2011) Pivotal study finds that HIV medications are highly effective as prophylaxis against HIV infection in men and women in africa.
22. Centers for Disease Control and Prevention (CDC) (2011) CDC trial and another major study find PrEP can reduce risk of HIV infection among heterosexuals.
23. Hayden EC, (2011) HIV drug-prevention strategy carries risks. Nature 476: 260-261.
24. Van Damme L, Corneli A, Ahmed K, Agot K, Lombaard J, et al. (2012) The FEMPrEP trial of emtricitabine/tenofovir disoproxil fumarate (truvada) among African women. In: The 19th Conference on Retroviruses and Oportunistic Infections, Abstract 32LB, March 5-8.
25. Chapman EH, Kurec AS, Davey FR, (1981) Cell volumes of normal and malignant mononuclear cells. J Clin Pathol 34: 1083-1090.
26. Bisset LR, Lung TL, Kaelin M, Ludwig E, Dubs RW, (2004) Reference values for peripheral blood lymphocyte phenotypes applicable to the healthy adult population in switzerland. Eur J Haematol 72: 203-212.
27. Bonate PL, (2006) Pharmacokinetic-Pharmacodynamic Modeling and Simulation. Springer.
28. Gagnieu MC, Barkil ME, Livrozet JM, Cotte L, Miailhes P, et al. (2008) Population pharmacokinetics of tenofovir in AIDS patients. J Clin Pharmacol 48: 1282-1288.
29. von Kleist M, Menz S, Huisinga W, (2010) Drug-class specific impact of antivirals on the reproductive capacity of HIV. PLoS Comput Biol 6: e1000720.
30. von Kleist M, Menz S, Stocker H, Arasteh K, Schutte C, et al. (2011) HIV quasispecies dynamics during pro-active treatment switching: impact on multi-drug resistance and resistance archiving in latent reservoirs. PLoS One 6: e18204.
31. Zhou Y, Zhang H, Siliciano JD, Siliciano RF, (2005) Kinetics of human immunodeficiency virus type 1 decay following entry into resting CD4+ T cells. J Virol 79: 2199-2210.
32. Shen L, Peterson S, Sedaghat AR, McMahon MA, Callender M, et al. (2008) Doseresponse curve slope sets class-specific limits on inhibitory potential of anti-HIV drugs. Nat Med 14: 762-766.
33. Baggaley RF, White RG, Boily MC, (2010) Infectiousness of HIV-infected homosexual men in the era of highly active antiretroviral therapy. AIDS 24: 2418-2420.
34. Royce RA, Sea A, Cates W, Cohen MS, (1997) Sexual transmission of HIV. N Engl J Med 336: 1072-1078.
35. Keele BF, Giorgi EE, Salazar-Gonzalez JF, Decker JM, Pham KT, et al. (2008) Identification and characterization of transmitted and early founder virus envelopes in primary HIV-1 infection. Proc Natl Acad Sci U S A 105: 7552-7557.
36. Salazar-Gonzalez JF, Bailes E, Pham KT, Salazar MG, Guffey MB, et al. (2008) Deciphering human immunodeficiency virus type 1 transmission and early envelope diversification by single-genome amplification and sequencing. J Virol 82: 3952-3970.
37. Frank M, von Kleist M, Kunz A, Harms G, Schutte C, et al. (2011) Quantifying the impact of nevirapine-based prophylaxis strategies to prevent mother-to-child transmission of HIV-1: a combined pharmacokinetic, pharmacodynamic, and viral dynamic analysis to predict clinical outcomes. Antimicrob Agents Chemother 55: 5529-5540.
38. Mayer KH, Mimiaga MJ, Gelman M, Grasso C, (2012) Raltegravir, tenofovir df, and emtricitabine for post-exposure prophylaxis to prevent the sexual transmission of HIV: Safety, tolerability and adherence. J Acquir Immune Defic Syndr.
39. Tosini W, Muller P, Prazuck T, Benabdelmoumen G, Peyrouse E, et al. (2010) Tolerability of HIV postexposure prophylaxis with tenofovir/emtricitabine and lopinavir/ritonavir tablet formulation. AIDS 24: 2375-2380.
40. Winston A, McAllister J, Amin J, Cooper DA, Carr A, (2005) The use of a triple nucleoside-nucleotide regimen for nonoccupational HIV post-exposure prophylaxis. HIV Med 6: 191-197.
41. Otten RA, Smith DK, Adams DR, Pullium JK, Jackson E, et al. (2000) Efficacy of postexposure prophylaxis after intravaginal exposure of pig-tailed macaques to a human-derived retrovirus (human immunodeficiency virus type 2). J Virol 74: 9771-9775.
42. Tsai CC, Emau P, Follis KE, Beck TW, Benveniste RE, et al. (1998) Effectiveness of postinoculation (r)-9-(2-phosphonylmethoxypropyl) adenine treatment for prevention of persistent simian immunodeficiency virus sivmne infection depends critically on timing of initiation and duration of treatment. J Virol 72: 4265-4273.
43. Lifson JD, Piatak M, Cline AN, Rossio JL, Purcell J, et al. (2003) Transient early post-inoculation anti-retroviral treatment facilitates controlled infection with sparing of CD4+ T cells in gut-associated lymphoid tissues in SIVmac239-infected rhesus macaques, but not resistance to rechallenge. J Med Primatol 32: 201-210.
44. Benaboud S, Hirt D, Launay O, Pannier E, Firtion G, et al. (2012) Pregnancy-related effects on tenofovir pharmacokinetics: a population study with 186 women. Antimicrob Agents Chemother 56: 857-862.
45. Bouazza N, Urien S, Hirt D, Frange P, Rey E, et al. (2011) Population pharmacokinetics of tenofovir in HIV-1-infected pediatric patients. J Acquir Immune Defic Syndr 58: 283-288.
46. Hurwitz SJ, Asif G, Kivel NM, Schinazi RF, (2008) Development of an optimized dose for coformulation of zidovudine with drugs that select for the K65R mutation using a population pharmacokinetic and enzyme kinetic simulation model. Antimicrob Agents Chemother 52: 4241-4250.
47. Piliero PJ, (2004) Pharmacokinetic properties of nucleoside/nucleotide reverse transcriptase inhibitors. J Acquir Immune Defic Syndr 37: S2-S12.
48. Peter K, Gambertoglio JG, (1998) Intracellular phosphorylation of zidovudine (ZDV) and other nucleoside reverse transcriptase inhibitors (RTI) used for human immunodeficiency virus (HIV) infection. Pharm Res 15: 819-825.
49. Pruvost A, Negredo E, Benech H, Theodoro F, Puig J, et al. (2005) Measurement of intracellular didanosine and tenofovir phosphorylated metabolites and possible interaction of the two drugs in human immunodeficiency virus-infected patients. Antimicrob Agents Chemother 49: 1907-1914.
50. Pruvost A, Negredo E, Théodoro F, Puig J, Levi M, et al. (2009) Pilot pharmacokinetic study of human immunodeficiency virus-infected patients receiving tenofovir disoproxil fumarate (TDF): investigation of systemic and intracellular interactions between TDF and abacavir, lamivudine, or lopinavir-ritonavir. Antimicrob Agents Chemother 53: 1937-1943.
51. Patterson KB, Prince HA, Kraft E, Jenkins AJ, Shaheen NJ, et al. (2011) Penetration of tenofovir and emtricitabine in mucosal tissues: implications for prevention of hiv-1 transmission. Sci Transl Med 3: 112re4.
52. Donnell D, Baeten J, Hendrix C, Bumpus N, Bangsberg D, et al. (2012) Tenofovir disoproxil fumarate drug levels indicate PrEP use is strongly correlated with HIV-1 protective effects: Kenya and uganda. In: The 19th Conference on Retroviruses and Oportunistic Infections, Abstract 30, March 5-8.
53. Cohen J, (2012) Aids research. FDA panel recommends anti-hiv drug for prevention. Science 336: 792.
54. Emau P, Jiang Y, Agy MB, Tian B, Bekele G, et al. (2006) Post-exposure prophylaxis for SIV revisited: animal model for HIV prevention. AIDS Res Ther 3: 29.
55. Haase AT, (2010) Targeting early infection to prevent HIV-1 mucosal transmission. Nature 464: 217-223.
56. Pudney J, Quayle AJ, Anderson DJ, (2005) Immunological microenvironments in the human vagina and cervix: mediators of cellular immunity are concentrated in the cervical transformation zone. Biol Reprod 73: 1253-1263.
57. Bobardt MD, Chatterji U, Selvarajah S, der Schueren BV, David G, et al. (2007) Cell-free human immunodeficiency virus type 1 transcytosis through primary genital epithelial cells. J Virol 81: 395-405.
58. Wu L, (2008) Biology of HIV mucosal transmission. Curr Opin HIV AIDS 3: 534-540.
59. Morrow G, Vachot L, Vagenas P, Robbiani M, (2008) Current concepts of HIV transmission. Curr Infect Dis Rep 10: 133-139.
60. Galvin SR, Cohen MS, (2004) The role of sexually transmitted diseases in HIV transmission. Nat Rev Microbiol 2: 33-42.
61. Hallett TB, Baeten JM, Heffron R, Barnabas R, de Bruyn G, et al. (2011) Optimal uses of antiretrovirals for prevention in HIV-1 serodiscordant heterosexual couples in south africa: a modelling study. PLoS Med 8: e1001123.
62. Cohen MS, Chen YQ, McCauley M, Gamble T, Hosseinipour MC, et al. (2011) Prevention of HIV-1 infection with early antiretroviral therapy. N Engl J Med 365: 493-505.
63. Garca-Lerma JG, Aung W, er Cong M, Zheng Q, Youngpairoj AS, et al. (2011) Natural substrate concentrations can modulate the prophylactic efficacy of nucleotide HIV reverse transcriptase inhibitors. J Virol 85: 6610-6617.
64. Karim QA, Karim SSA, Frohlich JA, Grobler AC, Baxter C, et al. (2010) Effectiveness and safety of tenofovir gel, an antiretroviral microbicide, for the prevention of HIV infection in women. Science 329: 1168-1174.
65. Dobard C, Sharma S, Martin A, Pau CP, Holder A, et al. (2012) Durable protection from vaginal simian-human immunodeficiency virus infection in macaques by tenofovir gel and its relationship to drug levels in tissue. J Virol 86: 718-725.
66. Schwartz JL, Rountree W, Kashuba ADM, Brache V, Creinin MD, et al. (2011) A multi-compartment, single and multiple dose pharmacokinetic study of the vaginal candidate microbicide 1% tenofovir gel. PLoS One 6: e25974.
67. Katz DF, Gao Y, Kang M, (2011) Using modeling to help understand vaginal microbicide functionality and create better products. Drug Deliv Transl Res 1: 256-276.
68. Durand-Gasselin L, Silva DD, Benech H, Pruvost A, Grassi J, (2007) Evidence and possible consequences of the phosphorylation of nucleoside reverse transcriptase inhibitors in human red blood cells. Antimicrob Agents Chemother 51: 2105-2111.
69. Markowitz M, Louie M, Hurley A, Sun E, Mascio MD, et al. (2003) A novel antiviral intervention results in more accurate assessment of human immunodeficiency virus type 1 replication dynamics and T-cell decay in vivo. J Virol 77: 5037-5038.
70. Ramratnam B, Bonhoeffer S, Binley J, Hurley A, Zhang L, et al. (1999) Rapid production and clearance of HIV-1 and hepatitis C virus assessed by large volume plasma apheresis. Lancet 354: 1782-1785.
71. Tan WY, Wu H, (1998) Stochastic modeling of the dynamics of CD4+ T-cell infection by HIV and some monte carlo studies. Math Biosci 147: 173-205.
72. Tuckwell HC, Shipman PD, Perelson AS, (2008) The probability of HIV infection in a new host and its reduction with microbicides. Math Biosci 214: 81-86.
73. Wei X, Ghosh SK, Taylor ME, Johnson VA, Emini EA, et al. (1995) Viral dynamics in human immunodeficiency virus type 1 infection. Nature 373: 117-122.
74. Sedaghat AR, Siliciano RF, Wilke CO, (2009) Constraints on the dominant mechanism for HIV viral dynamics in patients on raltegravir. Antivir Ther 14: 263-271.
75. Koelsch KK, Liu L, Haubrich R, May S, Havlir D, et al. (2008) Dynamics of total, linear nonintegrated, and integrated HIV-1 DNA in vivo and in vitro. J Infect Dis 197: 411-419.
76. Sedaghat AR, Dinoso JB, Shen L, Wilke CO, Siliciano RF, (2008) Decay dynamics of HIV-1 depend on the inhibited stages of the viral life cycle. Proc Natl Acad Sci U S A 105: 4832-4837.