Interpatient variability in the pharmacokinetics of the HIV non-nucleoside reverse transcriptase inhibitor efavirenz: The effect of gender, race, and CYP2B6 polymorphism

British Journal of Clinical Pharmacology

Volumn 61, Issue 2, 2006, Pages 148-154

  Burger, David ^a   Van Der Heiden, Ilse ^b   La Porte, Charles ^a   Van Der Ende, Marchina ^b   Groeneveld, Paul ^c   Richter, Clemens ^d   Koopmans, Peter ^a   Kroon, Frank ^e   Sprenger, Herman ^f   Lindemans, Jan ^b   Schenk, Paul ^b   Van Schaik, Ron ^b  

^a RADBOUD UNIVERSITY MEDICAL CENTER   (Netherlands)

^b ERASMUS MEDICAL CENTER   (Netherlands)

^c Isala Hospital Zwolle   (Netherlands)

^d RIJNSTATE HOSPITAL   (Netherlands)

^e LEIDEN UNIVERSITY MEDICAL CENTER   (Netherlands)

^f UNIVERSITY MEDICAL CENTER GRONINGEN   (Netherlands)

Author keywords

CYP2B6 polymorphism; Efavirenz; Ethnicity; Gender; HIV infection; Non nucleoside reverse transcriptase inhibitor; Pharmacokinetics

Indexed keywords

CONTRACEPTIVE AGENT; CYTOCHROME P450 2B6; EFAVIRENZ; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ADULT; AGE DISTRIBUTION; ARTICLE; BODY HEIGHT; BODY WEIGHT; CONTROLLED STUDY; DATA ANALYSIS; DEMOGRAPHY; DNA POLYMORPHISM; DRUG BLOOD LEVEL; DRUG MONITORING; FEMALE; GENETIC ASSOCIATION; GENETIC VARIABILITY; HORMONAL CONTRACEPTION; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MAJOR CLINICAL STUDY; MALE; MULTIVARIATE ANALYSIS; PHARMACOGENOMICS; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; RACE; RESTRICTION FRAGMENT LENGTH POLYMORPHISM; SEX RATIO; STATISTICAL SIGNIFICANCE;

ADULT; ANTHROPOMETRY; ANTI-HIV AGENTS; ARYL HYDROCARBON HYDROXYLASES; CONTINENTAL POPULATION GROUPS; FEMALE; HIV-1 REVERSE TRANSCRIPTASE; HUMANS; MALE; MIDDLE AGED; OXAZINES; OXIDOREDUCTASES, N-DEMETHYLATING; PHARMACOGENETICS; POLYMORPHISM, SINGLE NUCLEOTIDE; REVERSE TRANSCRIPTASE INHIBITORS; SEX CHARACTERISTICS;

EID: 33644910426     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2005.02536.x     Document Type: Article

References (26)

1. Panel on clinical practices for treatment of HIV infection, convened by the Department of Health and Human Services DHHS Guidelines for the Use of Antiretroviral Agents in HIV-1 Infected Adults and Adolescents March 23 2004
2. Staszewski S Morales-Ramirez J Tashima KT Rachlis A Skiest D Stanford J Stryker R Johnson P Labriola DF Farina D Manion DJ Ruiz NM Efavirenz plus zidovudine and lamivudine, efavirenz plus indinavir, and indinavir plus zidovudine and lamivudine in the treatment of HIV-1 infection in adults. Study 006 Team N Engl J Med 1999 341 1865 73
3. Van Leth F Phanuphak P Ruxrungtham K Baraldi E Miller S Gazzard B Cahn P Lalloo UG van der Westhuizen IP Malan DR Johnson MA Santos BR Mulcahy F Wood R Levi GC Reboredo G Squires K Cassetti I Petit D Raffi F Katlama C Murphy RL Horban A Dam JP Hassink E van Leeuwen R Robinson P Wit FW Lange JM Comparison of first-line antiretroviral therapy with regimens including nevirapine, efavirenz, or both drugs, plus stavudine and lamivudine: a randomised open-label trial, the 2NN Study Lancet 2004 363 1253 63
4. Gulick RM Ribaudo HJ Shikuma CM Lustgarten S Squires KE Meyer WA III Acosta EP Schackman BR Pilcher CD Murphy RL Maher WE Witt MD Reichman RC Snyder S Klingman KL Kuritzkes DR Triple-nucleoside regimens versus efavirenz-containing regimens for the initial treatment of HIV-1 infection N Engl J Med 2004 350 1850 61
5. Smith PF DiCenzo R Morse GD Clinical pharmacokinetics of non-nucleoside reverse transcriptase inhibitors Clin Pharmacokinet 2001 40 893 905
6. Pfister M Labbe L Hammer SM Mellors J Bennett KK Rosenkranz S Sheiner LB Population pharmacokinetics and pharmacodynamics of efavirenz, nelfinavir, and indinavir: Adult AIDS Clinical Trial Group Study 398 Antimicrob Agents Chemother 2003 47 130 7
7. Brundage RC Yong FH Fenton T Spector SA Starr SE Fletcher CV Intrapatient variability of efavirenz concentrations as a predictor of virologic response to antiretroviral therapy Antimicrob Agents Chemother 2004 48 979 84
8. Csajka C Marzolini C Fattinger K Decosterd LA Fellay J Telenti A Biollaz J Buclin T Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection Clin Pharmacol Ther 2003 73 20 30
9. Marzolini C Telenti A Decosterd LA Greub G Biollaz J Buclin T Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients AIDS 2001 15 71 5
10. Joshi AS Barrett JS Fiske WD Pieniaszek HJ Ludden TM Bacheler LT Ruiz NM Population pharmacokinetics of efavirenz in phase II studies and relationship with efficacy 39th ICAAC, September 26-29 1999 San Francisco, Califormia, USA, (Abstract) 1201, 2000
11. Stahle L Moberg L Svensson JO Sonnerborg A Efavirenz plasma concentrations in HIV-infected patients: inter- and intraindividual variability and clinical effects Ther Drug Monit 2004 26 267 70
12. Nunez M Gonzalez dR Gallego L Jimenez-Nacher I Gonzalez-Lahoz J Soriano V Higher efavirenz plasma levels correlate with development of insomnia J Acquir Immune Defic Syndr 2001 28 399 400
13. Anonymous. Optimising TDM in HIV clinical care. A practical guide to performing therapeutic drug monitoring (TDM) for antiretroviral agents. Available:. Last visited March 2, 2005
14. Burger DM La Porte C Van der Ende M Miesen J Koopmans P Gender-related differences in efavirenz pharmacokinetics 4th International Workshop on Clinical Phamacology of HIV Therapy March 27-29 2003 Cannes, France
15. Aarnoutse RE Grintjes KJ Telgt DS Stek M Jr. Hugen PW Reiss P Koopmans PP Hekster YA Burger DM The influence of efavirenz on the pharmacokinetics of a twice-daily combination of indinavir and low-dose ritonavir in healthy volunteers Clin Pharmacol Ther 2002 71 57 67
16. Lang T Klein K Fischer J Nussler AK Neuhaus P Hofmann U Eichelbaum M Schwab M Zanger UM Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver Pharmacogenetics 2001 11 399 415
17. Gandhi M Aweeka F Greenblatt RM Blaschke TF Gender differences in pharmacokinetics and pharmacodynamics Annu Rev Pharmacol Toxicol 2004 44 499 523
18. Spire B Carrieri P Garzot MA L'henaff M Group T Obadia Y Factors associated with Efavirenz discontinuation in a large community-based sample of patients AIDS Care 2004 16 558 64
19. Palovaara S Pelkonen O Uusitalo J Lundgren S Laine K Inhibition of cytochrome P450 2B6 activity by hormone replacement therapy and oral contraceptive as measured by bupropion hydroxylation Clin Pharmacol Ther 2003 74 326 33
20. Stocrin®. Summary of Product Characteristics. Merck Sharp & Dohme Limited Hertfordshire, United Kingdom 2002
21. Tsuchiya K Gatanaga H Tachikawa N et al. Homozygous CYP2B6*6 (Q172H and K262R) correlates with high plasma efavirenz concentrations in HIV-1 patients treated with standard efavirenz-containing regimens Biochem Biophys Res Commun 2004 319 1322 6
22. Lamba V Lamba J Yasuda K Strom S Davila J Hancock ML Fackenthal JD Rogan PK Ring B Wrighton SA Schuetz EG Hepatic CYP2B6 expression: gender and ethnic differences and relationship to CYP2B6 genotype and CAR (constitutive androstane receptor) expression J Pharmacol Exp Ther 2003 307 906 22
23. Kirchheiner J Klein C Meineke I Sasse J Zanger UM Murdter TE Roots I Brockmoller J Bupropion and 4-OH-bupropion pharmacokinetics in relation to genetic polymorphisms in CYP2B6 Pharmacogenetics 2003 13 619 26
24. Ingelman-Sundberg M Human drug metabolising cytochrome P450 enzymes: properties and polymorphisms Naunyn Schmiedebergs Arch Pharmacol 2004 369 89 104
25. Haas DW Ribaudo HJ Kim RB Tierney C Wilkinson GR Gulick RM Clifford DB Hulgan T Marzolini C Acosta EP Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study AIDS 2004 18 2391 400
26. Ward BA Gorski JC Jones DR Hall SD Flockhart DA Desta Z The cytochrome P450 2B6 (CYP2B6) is the main catalyst of efavirenz primary and secondary metabolism: implication for HIV/AIDS therapy and utility of efavirenz as a substrate marker of CYP2B6 catalytic activity J Pharmacol Exp Ther 2003 306 287 300