Intracellular and plasma steady-state pharmacokinetics of raltegravir, darunavir, etravirine and ritonavir in heavily pre-treated HIV-infected patients

British Journal of Clinical Pharmacology

Volumn 69, Issue 5, 2010, Pages 475-483

  Ter Heine, Rob ^a   Mulder, Jan Willem ^a   Van Gorp, Eric C M ^a   Wagenaar, Jiri F P ^a   Beijnen, Jos H ^a   Huitema, Alwin D R ^a  

^a SLOTERVAART HOSPITAL   (Netherlands)

Author keywords

Darunavir; Etravirine; Intracellular; Pharmacokinetics; Raltegravir; Ritonavir

Indexed keywords

DARUNAVIR PLUS RITONAVIR; EFAVIRENZ; ETRAVIRINE; LAMIVUDINE; PROTEINASE INHIBITOR; RALTEGRAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; TENOFOVIR;

ADULT; ARTICLE; CELL LYSATE; CLINICAL ARTICLE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; ENTEROHEPATIC CIRCULATION; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; HUMAN IMMUNODEFICIENCY VIRUS 2 INFECTION; HUMAN IMMUNODEFICIENCY VIRUS INFECTED PATIENT; INTRACELLULAR SPACE; LIQUID CHROMATOGRAPHY; MALE; MASS SPECTROMETRY; PERIPHERAL BLOOD MONONUCLEAR CELL; PRIORITY JOURNAL; SALVAGE THERAPY; STEADY STATE; VIRUS REPLICATION;

ANTI-HIV AGENTS; DRUG INTERACTIONS; DRUG THERAPY, COMBINATION; HIV INFECTIONS; HUMANS; INTESTINAL ABSORPTION; MALE; MIDDLE AGED; PYRIDAZINES; RITONAVIR; SALVAGE THERAPY; SULFONAMIDES;

EID: 77950641037     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2010.03634.x     Document Type: Article

References (30)

1. Summa V, Petrocchi A, Bonelli F, Crescenzi B, Donghi M, Ferrara M, Fiore F, Gardelli C, Gonzalez PO, Hazuda DJ, Jones P, Kinzel O, Laufer R, Monteagudo E, Muraglia E, Nizi E, Orvieto F, Pace P, Pescatore G, Scarpelli R, Stillmock K, Witmer MV, Rowley M. Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem 2008 51 : 5843 5855.
2. Dierynck I, De WM, Gustin E, Keuleers I, Vandersmissen J, Hallenberger S, Hertogs K. Binding kinetics of darunavir to human immunodeficiency virus type 1 protease explain the potent antiviral activity and high genetic barrier. J Virol 2007 81 : 13845 13851.
3. Rittweger M, Arasteh K. Clinical pharmacokinetics of darunavir. Clin Pharmacokinet 2007 46 : 739 756.
4. Anderson MS, Kakuda TN, Hanley W, Miller J, Kost JT, Stoltz R, Wenning LA, Stone JA, Hoetelmans RM, Wagner JA, Iwamoto M. Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects. Antimicrob Agents Chemother 2008 52 : 4228 4232.
5. Iwamoto M, Wenning LA, Petry AS, Laethem M, De SM, Kost JT, Breidinger SA, Mangin EC, Azrolan N, Greenberg HE, Haazen W, Stone JA, Gottesdiener KM, Wagner JA. Minimal effects of ritonavir and efavirenz on the pharmacokinetics of raltegravir. Antimicrob Agents Chemother 2008 52 : 4338 4343.
6. Scholler-Gyure M, Kakuda TN, Sekar V, Woodfall B, De SG, Lefebvre E, Peeters M, Hoetelmans RM. Pharmacokinetics of darunavir/ritonavir and TMC125 alone and co-administered in HIV-negative volunteers. Antivir Ther 2007 12 : 789 796.
7. Menard A, Solas C, Mokthari S, Bregigeon S, Drogoul MP, Tamalet C, Lacarelle B, Martin IP. Etravirine-raltegravir, a marked interaction in HIV-1-infected patients: about four cases. AIDS 2009 23 : 869 871.
8. Ter Heine R, Alderden-Los CG, Rosing H, Hillebrand MJ, van Gorp EC, Huitema AD, Beijnen JH. Fast and simultaneous determination of darunavir and eleven other antiretroviral drugs for therapeutic drug monitoring: method development and validation for the determination of all currently approved HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors in human plasma by liquid chromatography coupled with electrospray ionization tandem mass spectrometry. Rapid Commun Mass Spectrom 2007 21 : 2505 2514.
9. Ter Heine R, Rosing H, van Gorp EC, Mulder JW, van der Steeg WA, Beijnen JH, Huitema AD. Quantification of protease inhibitors and non-nucleoside reverse transcriptase inhibitors in dried blood spots by liquid chromatography-triple quadrupole mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 2008 867 : 205 212.
10. Ter Heine R, Hillebrand MJ, Rosing H, van Gorp EC, Mulder JW, Beijnen JH, Huitema AD. Quantification of the HIV-integrase inhibitor raltegravir and detection of its main metabolite in human plasma, dried blood spots and peripheral blood mononuclear cell lysate by means of high-performance liquid chromatography tandem mass spectrometry. J Pharm Biomed Anal 2009 49 : 451 458.
11. Ter Heine R, Rosing H, van Gorp EC, Mulder JW, Beijnen JH, Huitema AD. Quantification of etravirine (TMC125) in plasma, dried blood spots and peripheral blood mononuclear cell lysate by liquid chromatography tandem mass spectrometry. J Pharm Biomed Anal 2009 49 : 393 400.
12. Ter Heine R, Davids M, Rosing H, van Gorp EC, Mulder JW, van der Heide YT, Beijnen JH, Huitema AD. Quantification of HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors in peripheral blood mononuclear cell lysate using liquid chromatography coupled with tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 2009 877 : 575 580.
13. Jonsson EN, Karlsson MO. Xpose - an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for NONMEM. Comput Methods Programs Biomed 1999 58 : 51 64.
14. Lindbom L, Ribbing J, Jonsson EN. Perl-speaks-NONMEM (PsN) - a Perl module for NONMEM related programming. Comput Methods Programs Biomed 2004 75 : 85 94.
15. Keizer RJ, Zandvliet AS, Huitema AD. A simple infrastructure and graphical user interface (GUI) for distributed NONMEM analysis on standard network environments - abstract 1237. Population Approach Group in Europe (PAGE) meeting 17. 29-1-2008.
16. Kappelhoff BS, Huitema AD, Yalvac Z, Prins JM, Mulder JW, Meenhorst PL, Beijnen JH. Population pharmacokinetics of efavirenz in an unselected cohort of HIV-1-infected individuals. Clin Pharmacokinet 2005 44 : 849 861.
17. Kappelhoff BS, Huitema AD, Crommentuyn KM, Mulder JW, Meenhorst PL, van Gorp EC, Mairuhu AT, Beijnen JH. Development and validation of a population pharmacokinetic model for ritonavir used as a booster or as an antiviral agent in HIV-1-infected patients. Br J Clin Pharmacol 2005 59 : 174 182.
18. Khoo SH, Hoggard PG, Williams I, Meaden ER, Newton P, Wilkins EG, Smith A, Tjia JF, Lloyd J, Jones K, Beeching N, Carey P, Peters B, Back DJ. Intracellular accumulation of human immunodeficiency virus protease inhibitors. Antimicrob Agents Chemother 2002 46 : 3228 3235.
19. Miller M, Danovich R, Fransen S, Gupta S, Huang W, Nguyen B, Parkin N, Petropoulos C, Teppler H, Witmer M, Zhao J, Hazuda D. Analysis of resistance to the HIV-1 integrase inhibitor raltegravir: results from BENCHMRK-1 and -2. 48th Annual ICAAC/IDSA. 28-10-0008.
20. Kassahun K, McIntosh I, Cui D, Hreniuk D, Merschman S, Lasseter K, Azrolan N, Iwamoto M, Wagner JA, Wenning LA. Metabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the human immunodeficiency virus 1 integrase enzyme. Drug Metab Dispos 2007 35 : 1657 1663.
21. Monteagudo E, Pesci S, Taliani M, Fiore F, Petrocchi A, Nizi E, Rowley M, Laufer R, Summa V. Studies of metabolism and disposition of potent human immunodeficiency virus (HIV) integrase inhibitors using 19F-NMR spectroscopy. Xenobiotica 2007 37 : 1000 1012.
22. Almond LM, Edirisinghe D, Dalton M, Bonington A, Back DJ, Khoo SH. Intracellular and plasma pharmacokinetics of nevirapine in human immunodeficiency virus-infected individuals. Clin Pharmacol Ther 2005 78 : 132 142. (Pubitemid 41112281)
23. Almond LM, Hoggard PG, Edirisinghe D, Khoo SH, Back DJ. Intracellular and plasma pharmacokinetics of efavirenz in HIV-infected individuals. J Antimicrob Chemother 2005 56 : 738 744.
24. Crommentuyn KM, Mulder JW, Mairuhu AT, van Gorp EC, Meenhorst PL, Huitema AD, Beijnen JH. The plasma and intracellular steady-state pharmacokinetics of lopinavir/ritonavir in HIV-1-infected patients. Antivir Ther 2004 9 : 779 785.
25. Ford J, Cornforth D, Hoggard PG, Cuthbertson Z, Meaden ER, Williams I, Johnson M, Daniels E, Hsyu P, Back DJ, Khoo SH. Intracellular and plasma pharmacokinetics of nelfinavir and M8 in HIV-infected patients: relationship with P-glycoprotein expression. Antivir Ther 2004 9 : 77 84.
26. Ford J, Boffito M, Wildfire A, Hill A, Back D, Khoo S, Nelson M, Moyle G, Gazzard B, Pozniak A. Intracellular and plasma pharmacokinetics of saquinavir-ritonavir, administered at 1,600/100 milligrams once daily in human immunodeficiency virus-infected patients. Antimicrob Agents Chemother 2004 48 : 2388 2393.
27. Hennessy M, Clarke S, Spiers JP, Mulcahy F, Kelleher D, Meadon E, Maher B, Bergin C, Khoo S, Tjia J, Hoggard P, Back D, Barry M. Intracellular indinavir pharmacokinetics in HIV-infected patients: comparison with plasma pharmacokinetics. Antivir Ther 2003 8 : 191 198.
28. Chandler B, Detsika M, Owen A, Evans S, Hartkoorn RC, Cane PA, Back DJ, Khoo SH. Effect of transporter modulation on the emergence of nelfinavir resistance in vitro. Antivir Ther 2007 12 : 831 834.
29. Janneh O, Jones E, Chandler B, Owen A, Khoo SH. Inhibition of P-glycoprotein and multidrug resistance-associated proteins modulates the intracellular concentration of lopinavir in cultured CD4 T cells and primary human lymphocytes. J Antimicrob Chemother 2007 60 : 987 993.
30. Molto J, Santos JR, Perez-Alvarez N, Cedeno S, Miranda C, Khoo S, Else L, Llibre JM, Valle M, Clotet B. 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 : 3928 3932.