Increasing extracellular protein concentration reduces intracellular antiretroviral drug concentration and antiviral effect

AIDS Research and Human Retroviruses

Volumn 29, Issue 11, 2013, Pages 1434-1442

  Avery, Lindsay B ^a   Zarr, Melissa A ^a   Bakshi, Rahul P ^a   Siliciano, Robert F ^a   Hendrix, Craig W ^a  

^a JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EFAVIRENZ; ENFUVIRTIDE; ETRAVIRINE; GREEN FLUORESCENT PROTEIN; HUMAN SERUM ALBUMIN; RALTEGRAVIR;

ADULT; ANTIVIRAL ACTIVITY; ARTICLE; CD4+ T LYMPHOCYTE; CELLULAR DISTRIBUTION; CONCENTRATION RESPONSE; CONTROLLED STUDY; FEMALE; FLOW CYTOMETRY; HUMAN; HUMAN CELL; HUMAN EXPERIMENT; HUMAN IMMUNODEFICIENCY VIRUS 1; IC 50; IN VITRO STUDY; MALE; NORMAL HUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN EXPRESSION; REPORTER GENE; TANDEM MASS SPECTROMETRY; ULTRA PERFORMANCE LIQUID CHROMATOGRAPHY; VIRUS INFECTIVITY;

ADOLESCENT; ADULT; AGED; ANTI-RETROVIRAL AGENTS; CD4-POSITIVE T-LYMPHOCYTES; CHROMATOGRAPHY, LIQUID; CYTOSOL; FEMALE; HIV-1; HUMANS; INHIBITORY CONCENTRATION 50; MALE; MIDDLE AGED; PROTEIN BINDING; SERUM ALBUMIN; TANDEM MASS SPECTROMETRY; VIRUS INTERNALIZATION; VIRUS REPLICATION; YOUNG ADULT;

EID: 84886707973     PISSN: 08892229     EISSN: 19318405     Source Type: Journal    
DOI: 10.1089/aid.2013.0031     Document Type: Article

References (34)

1. Hammer SM, Eron JJ, Reiss P, et al.: Antiretroviral treatment of adult HIV infection: 2008 recommendations of the international aids society-USA panel. JAMA 2008; 300(5): 555-570.
2. Grant RM, Lama JR, Anderson PL, et al.: Preexposure chemoprophylaxis for HIV prevention in men who have sex with men. N Engl J Med 2010; 363(27): 2587-2599.
3. Cohen MS, Chen YQ, McCauley M, et al.: Prevention of HIV-1 infection with early antiretroviral therapy. N Engl J Med 2011; 365(6): 493-505.
4. Mujugira A, Baeten JM, Donnell D, et al.: Characteristics of HIV-1 serodiscordant couples enrolled in a clinical trial of antiretroviral pre-exposure prophylaxis for HIV-1 prevention. PLoS ONE 2011; 6(10): e25828.
5. Abdool Karim Q, Abdool Karim SS, Frohlich JA, et al.: Effectiveness and safety of tenofovir gel, an antiretroviral microbicide, for the prevention of HIV infection in women. Science 2010; 329(5996): 1168-1174.
6. Smith DA, Di L, and Kerns EH: The effect of plasma protein binding on in vivo efficacy: Misconceptions in drug discovery. Nat Rev 2010; 9(12): 929-939.
7. Avery LB, Bakshi RP, Cao YJ, and Hendrix CW: The male genital tract is not a pharmacological sanctuary from efavirenz. Clin Pharmacol Ther 2011; 90(1): 151-156.
8. Fischl MA, Richman DD, Flexner C, et al.: Phase I/II study of the toxicity, pharmacokinetics, and activity of the HIV protease inhibitor SC-52151. JAIDS J Acquir Immune Defic Syndr 1997; 15(1): 28-34.
9. Benet LZ and Hoener BA: Changes in plasma protein binding have little clinical relevance. Clin Pharmacol Ther 2002; 71(3): 115-121.
10. Craig WA and Kunin CM: Significance of serum protein and tissue binding of antimicrobial agents. Annu Rev Med 1976; 27(1): 287-300.
11. Avery LB, Sacktor N, McArthur JC, and Hendrix CW: Protein- free efavirenz concentrations in cerebrospinal fluid and blood plasma are equivalent: Applying the law of mass action to predict protein-free drug concentration. Antimicrob Agents Chemother 2013; 57(3): 1409-1414.
12. Boffito M, Back DJ, Blaschke TF, et al.: Protein binding in antiretroviral therapies. AIDS Res Hum Retroviruses 2003; 19(9): 825-835.
13. Ganrot K and Laurell C-B: Measurement of IgG and albumin content of cerebrospinal fluid, and its interpretation. Clin Chem 1974; 20(5): 571-573.
14. Zeitlinger MA, Derendorf H, Mouton JW, et al.: Protein binding: Do we ever learn? Antimicrob Agents Chemother 2011; 55(7): 3067-3074.
15. Company. BMS. Sustiva Package Insert. Princeton, NJ, 2012.
16. Pharmaceuticals. T. Intelence Package Insert. Titusville, NJ, 2012.
17. Merck & Co. I. Isentress Package Insert. 2011.
18. Genentech I and Trimeris, Inc. Fuzeon Package Insert. 2012.
19. Jilek BL, Zarr M, Sampah ME, et al.: A quantitative basis for antiretroviral therapy for HIV-1 infection. Nat Med 2012; 18(3): 446-451.
20. Shen L, Peterson S, Sedaghat AR, et al.: Dose-response curve slope sets class-specific limits on inhibitory potential of anti- HIV drugs. Nat Med 2008; 14(7): 762-766.
21. Sampah MES, Shen L, Jilek BL, and Siliciano RF: Dose- response curve slope is a missing dimension in the analysis of HIV-1 drug resistance. Proc Natl Acad Sci USA 2011; 108(18): 7613-7618.
22. Zhang H, Zhou Y, Alcock C, et al.: Novel single-cell-level phenotypic assay for residual drug susceptibility and reduced replication capacity of drug-resistant human immunodeficiency virus type 1. J Virol 2004; 78(4): 1718-1729.
23. Pierson TC, Zhou Y, Kieffer TL, Ruff CT, Buck C, and Siliciano RF: Molecular characterization of preintegration latency in human immunodeficiency virus type 1 infection. J Virol 2002; 76(17): 8518-8531.
24. Simiele M, D'Avolio A, Baietto L, et al.: Evaluation of the mean corpuscular volume of peripheral blood mononuclear cells of HIV patients by a Coulter counter to determine intracellular drug concentrations. Antimicrob Agents Chemother 2011; 55(6): 2976-2978.
25. Avery LB, Parsons TL, Meyers DJ, and Hubbard WC: A highly sensitive ultra performance liquid chromatography- tandem mass spectrometric (UPLC-MS/MS) technique for quantitation of protein free and bound efavirenz (EFV) in human seminal and blood plasma. J Chromatogr B 2010; 878(31): 3217-3224.
26. Garrison M, Vance-Bryan K, Larson T, Toscano J, and Rotschafer J: Assessment of effects of protein binding on daptomycin and vancomycin killing of Staphylococcus aureus by using an in vitro pharmacodynamic model. Antimicrob Agents Chemother 1990; 34(10): 1925-1931.
27. Cha R and Rybak MJ: Influence of protein binding under controlled conditions on the bactericidal activity of daptomycin in an in vitro pharmacodynamic model. J Antimicrob Chemother 2004; 54(1): 259-262.
28. Zeitlinger M, Sauermann R, Fille M, Hausdorfer J, Leitner I, and Müller M: Plasma protein binding of fluoroquinolones affects antimicrobial activity. J Antimicrob Chemother 2008; 61(3): 561-567.
29. Bojko B, Su1kowska A, Maciazek-Jurczyk M, Równicka J, Pentak D, and Su1kowski W: Alterations of furosemide binding to serum albumin induced by increased level of fatty acid. J Pharm Biomed Anal 2010; 51(1): 273-277.
30. Dockal M, Carter DC, and Rüker F: Conformational transitions of the three recombinant domains of human serum albumin depending on pH. J Biol Chem 2000; 275(5): 3042-3050.
31. Matsuyama K, Sen AC, and Perrin JH: The effects of pH, calcium and chloride ions on the binding of tolmetin to human serum albumin: Circular dichroic, dialysis and fluorometric measurements. J Pharm Pharmacol 1987; 39(3): 190-195.
32. Bazzoli C, Jullien V, Le Tiec C, Rey E, Mentré F, and Taburet AM: Intracellular pharmacokinetics of antiretroviral drugs in HIV-infected patients, and their correlation with drug action. Clin Pharmacokinet 2010; 49(1): 17-45.
33. Goutelle S, Maurin M, Rougier F, et al.: The Hill equation: A review of its capabilities in pharmacological modelling. Fund Clin Pharmacol 2008; 22(6): 633-648.
34. Shen L, Rabi SA, Sedaghat AR, et al.: A critical subset model provides a conceptual basis for the high antiviral activity of major HIV drugs. Sci Transl Med 2011; 3: 91ra63.