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Table 9b. Trough Concentrations of Antiretroviral Drugs for Treatment-Experienced Patients with
Virologic Failure

Drug Concentration (ng/mL)
Suggested minimum target trough concentrations for ART-experienced patients who have resistant HIV-1 strains
Maraviroc (MVC) >50

Tipranavir (TPV) 20,500
Median (Range) Trough Concentrations from Clinical Trials 12-14
Darunavir (DRV) (600 mg twice daily) 3300 (1255–7368)

Etravirine (ETR) 275 (81–2980)
Raltegravir (RAL) 72 (29–118)

References

1. Spector R, Park GD, Johnson GF, et al. Therapeutic drug monitoring. Clin Pharmacol Ther. 1988;43(4):345-353.
2. Fletcher CV, Anderson PL, Kakuda TN, et al. Concentration-controlled compared with conventional antiretroviral
therapy for HIV infection. AIDS. 2002;16(4):551-560.
3. Fabbiani M, Di Giambenedetto S, Bracciale L, et al. Pharmacokinetic variability of antiretroviral drugs and correlation with
virological outcome: 2 years of experience in routine clinical practice. J Antimicrob Chemother. 2009;64(1):109-117.
4. Acosta EP, Gerber JG. Position paper on therapeutic drug monitoring of antiretroviral agents. AIDS Res Hum
Retroviruses. 2002;18(12):825-834.
5. van Luin M, Kuks PF, Burger DM. Use of therapeutic drug monitoring in HIV disease. Curr Opin HIV AIDS.
2008;3(3):266-271.
6. Boffito M, Acosta E, Burger D, et al. Current status and future prospects of therapeutic drug monitoring and applied
clinical pharmacology in antiretroviral therapy. Antivir Ther. 2005;10(3):375-392.
7. LaPorte CJL, Back BJ, Blaschke T, et al. Updated guidelines to perform therapeutic drug monitoring for antiretroviral
agents. Rev Antivir Ther. 2006;3:4-14.
8. Pfizer Inc. Selzentry (maraviroc) tablets prescribing information NY. 2007.
9. McFayden L, Jacqmin P, Wade J, et al. Maraviroc exposure response analysis: phase 3 antiviral efficacy in treatment-
experienced HIV+ patients. Paper presented at: 16th Population Approach Group in Europe Meeting; June 2007, 2007;
Kobenhavn, Denmark. Abstract P4-13.
10. Molto J, Santos JR, Perez-Alvarez N, et al. Darunavir inhibitory quotient predicts the 48-week virological response to
darunavir-based salvage therapy in human immunodeficiency virus-infected protease inhibitor-experienced patients.
Antimicrob Agents Chemother. 2008;52(11):3928-3932.

11. Sekar V, DeMeyer S, Vangeneugden T, et al. Pharmacokinetic/pharmacodynamic (PK/PD) analysies of TMC114 in the
POWER 1 and POWER 2 trials in treatment-experienced HIV-infected patients. Paper presented at: 13th Conference on
Retroviruses and Opportunistic Infections; February 5, 2006, 2006; Denver, CO. Abstract J-121.
12. Markowitz M, Morales-Ramirez JO, Nguyen BY, et al. Antiretroviral activity, pharmacokinetics, and tolerability of MK-
0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected
individuals. J Acquir Immune Defic Syndr. 2006;43(5):509-515.
13. Kakuda TN, Wade JR, Snoeck E, et al. Pharmacokinetics and pharmacodynamics of the non-nucleoside reverse-transcriptase
inhibitor etravirine in treatment-experienced HIV-1-infected patients. Clin Pharmacol Ther. 2010;88(5):695-703.
14. Food and Drug Administration (FDA). Prezista (package insert). 2010.
http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021976s016lbl.pdf.

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