Population pharmacokinetic/pharmacogenetic model for optimization of Efavirenz therapy in caucasian HIV-infected patients

Antimicrobial Agents and Chemotherapy

Volumn 55, Issue 11, 2011, Pages 5314-5324

  Sánchez, Almudena ^a   Cabrera, Salvador ^a,b   Santos, Dolores ^c   Valverde, M Paz ^a   Fuertes, Aurelio ^a   Domínguez Gil, Alfonso ^a,c   García, María J ^c   Cordero, Miguel ^d   Iglesias, Alicia ^d   Luna, Guillermo ^d   Bustos, Carmen ^d  

^a HOSPITAL UNIVERSITARIO DE SALAMANCA   (Spain)

^b UNIVERSIDAD AUSTRAL DE CHILE   (Chile)

^c UNIVERSITY OF SALAMANCA   (Spain)

^d NONE

Author keywords

[No Author keywords available]

Indexed keywords

ABC TRANSPORTER A1; BREAST CANCER RESISTANCE PROTEIN; CYTOCHROME P450 2A6; CYTOCHROME P450 2B6; CYTOCHROME P450 2C19; CYTOCHROME P450 2C8; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; CYTOCHROME P450 3A5; EFAVIRENZ; GAMMA GLUTAMYLTRANSFERASE; GLUCURONOSYLTRANSFERASE 2B7; MULTIDRUG RESISTANCE PROTEIN 1; MULTIDRUG RESISTANCE PROTEIN 2; MULTIDRUG RESISTANCE PROTEIN 4;

ALLELE; ARTICLE; CAUCASIAN; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG ELIMINATION; DRUG METABOLISM; DRUG TRANSPORT; GENOTYPE; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LABORATORY TEST; LIFESTYLE; PHARMACOGENETICS; POPULATION MODEL; PRIORITY JOURNAL; SINGLE NUCLEOTIDE POLYMORPHISM;

ADOLESCENT; ADULT; AGED; ANTI-HIV AGENTS; BENZOXAZINES; EUROPEAN CONTINENTAL ANCESTRY GROUP; FEMALE; HIV INFECTIONS; HUMANS; MALE; MIDDLE AGED; POLYMORPHISM, SINGLE NUCLEOTIDE; YOUNG ADULT;

EID: 80054699859     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.00194-11     Document Type: Article

References (61)

1. Arab-Alameddine, M., et al. 2009. Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals. Clin. Pharmacol. Ther. 85:485-494.
2. Reference deleted.
3. Beal, S. L., L. B. Sheiner, and A. J. Boeckmann (ed.). 2006. NONMEM user's guides. Icon Development Solutions, Ellicott City, MD.
4. Blanch, J., et al. 2001. Preliminary data of a prospective study on neuropsychiatric side effects after initiation of efavirenz. J. Acquir. Immune Defic. Syndr. 27:336-343. (Pubitemid 32729079)
5. Brendel, K., E. Comets, C. M. Laffont, C. Laveille, and F. Mentré. 2006. Metrics for external model evaluation with an application to the population pharmacokinetics of gliclazide. Pharm. Res. 23:2036-2049.
6. Brundage, R. C., et al. 2004. Intrapatient variability of efavirenz concentrations as a predictor of virologic response to antiretroviral therapy. Antimicrob. Agents Chemother. 48:979-984. (Pubitemid 38280352)
7. Burger, D., et al. 2006. Interpatient variability in the pharmacokinetics of the HIV non-nucleoside reverse transcriptase inhibitor efavirenz: the effect of gender, race, and CYP2B6 polymorphism. Br. J. Clin. Pharmacol. 61:148-154. (Pubitemid 43382608)
8. Cabrera, S., et al. 2010. Long-term efficacy and safety of efavirenz dose reduction to 200 mg once daily in a Caucasian patient with HIV. Clin. Drug Invest. 30:405-411.
9. Cabrera, S., et al. 2009. Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients. Antimicrob. Agents Chemother. 53:2791-2798.
10. Cabrera, S. E., et al. 2008. Efavirenz-rifampicin interaction: therapeutic drug monitoring to efavirenz dosage optimization in HIV/TBC patients. AIDS 22:2549-2551.
11. Chen, J., et al. 2010. CYP2B6 polymorphism and nonnucleoside reverse transcriptase inhibitor plasma concentrations in Chinese HIV-infected patients. Ther. Drug Monit. 32:573-578.
12. Cressey, T. R., and M. Lallemant. 2007. Pharmacogenetics of antiretroviral drugs for the treatment of HIV-infected patients: an update. Infect. Genet. Evol. 7:333-342. (Pubitemid 46187499)
13. Csajka, C., et al. 2003. Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection. Clin. Pharmacol. Ther. 73:20-30. (Pubitemid 36158483)
14. Department of Health and Human Services Panel on Antiretroviral Guidelines for Adults and Adolescents. 25 October 2010, accession date. Guidelines for the use of antiretroviral agents in HIV-infected adults and adolescents. HHS, Washington, DC. http://www.aidsinfo.nih.gov.
15. Di Iulio, J., et al. 2009. In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function. Pharmacogenet. Genomics 19:300-309.
16. Fellay, J., et al. 2002. Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study. Lancet 359:30-36. (Pubitemid 34119193)
17. Food and Drug Administration. 15 September 2010, accession date. Sustiva label information, approved 18 August 2008. FDA, Washington, DC. www.fda.gov/cder/foi/label/2008/020972s030,021360s019lbl.pdf.
18. Fumaz, C. R., et al. 2005. Long-term neuropsychiatric disorders on efavirenz-based approaches: quality of life, psychologic issues, and adherence. J. Acquir. Immune Defic. Syndr. 38:560-565. (Pubitemid 40524478)
19. Gallego, L., et al. 2004. Analyzing sleep abnormalities in HIV-infected patients treated with efavirenz. Clin. Infect. Dis. 38:430-432. (Pubitemid 38200124)
20. Gatanaga, H., et al. 2007. Successful efavirenz dose reduction in HIV type 1-infected individuals with cytochrome P450 2B6*6 and*26. Clin. Infect. Dis. 45:1230-1237. (Pubitemid 47580326)
21. Haas, D. W., et al. 2009. Associations between CYP2B6 polymorphisms and pharmacokinetics after a single dose of nevirapine or efavirenz in African Americans. J. Infect. Dis. 199:872-880.
22. Haas, D. W., et al. 2004. Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study. AIDS 18: 2391-2400. (Pubitemid 40065906)
23. Haas, D. W., et al. 2005. Pharmacogenetics of long-term responses to antiretroviral regimens containing efavirenz and/or nelfinavir: an Adult AIDS Clinical Trials Group study. J. Infect. Dis. 192:1931-1942. (Pubitemid 41681891)
24. Hasse, B., H. F. Gunthard, G. Bleiber, and M. Krause. 2005. Efavirenz intoxication due to slow hepatic metabolism. Clin. Infect. Dis. 40:e22-e23.
25. Ingelman-Sundberg, M., M. Oscarson, and R. A. McLellan. 1999. Polymorphic human cytochrome P450 enzymes; an opportunity for individualized drug treatment. Trends Pharmacol. Sci. 20:342-349. (Pubitemid 29366813)
26. Jonsson, E. N., and M. O. Karlsson. 1999. Xposec - an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for NONMEN. Comput. Methods Programs Biomed. 58:51-64. (Pubitemid 29049052)
27. Kappelhoff, B. S., et al. 2005. Population pharmacokinetics of efavirenz in an unselected cohort of HIV-1-infected individuals. Clin. Pharmacokinet. 44: 849-861. (Pubitemid 41126932)
28. Kappelhoff, B. S., et al. 2005. Nevirapine and efavirenz pharmacokinetics and covariate analysis in the 2NN study. Antivir. Ther. 10:145-155. (Pubitemid 40767640)
29. Kappelhoff, B. S., et al. 2005. Are adverse events of nevirapine and efavirenz related to plasma concentrations? Antivir. Ther. 10:489-498. (Pubitemid 41059195)
30. Knobel, H., et al. 2002. Validation of a simplified medication adherence questionnaire in a large cohort of HIV-infected patients: the GEEMA Study. AIDS 16:605-613. (Pubitemid 34218856)
31. Kwara, A., M. Lartey, K. W. Sagoe, E. Kenu, and M. H. Court. 2009. CYP2B6, CYP2A6 and UGT2B7 genetic polymorphisms are predictors of efavirenz mid-dose concentration in HIV-infected patients. AIDS 23:2101-2106.
32. Kwara, A., M. Lartey, K. W. Sagoe, N. L. Rzek, and M. H. Court. 2009. CYP2B6 (c.516G→T) and CYP2A6 (*9B and/or*17) polymorphisms are independent predictors of efavirenz plasma concentrations in HIV-infected patients. Br. J. Clin. Pharmacol. 67:427-436.
33. Leger, P., et al. 2009. CYP2B6 variants and plasma efavirenz concentrations during antiretroviral therapy in Port-au-Prince, Haiti. J. Infect. Dis. 200:955-964.
34. Marzolini, C., et al. 2001. Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients. AIDS 15:71-75. (Pubitemid 32055781)
35. Motsinger, A. A., et al. 2006. Multilocus genetic interactions and response to efavirenz-containing regimens: an Adult AIDS Clinical Trials Group study. Pharmacogenet. Genomics 16:837-845. (Pubitemid 44632298)
36. Mukonzo, J. K., et al. 2009. A novel polymorphism in ABCB1 gene, CYP2B6*6 and sex predict single-dose efavirenz population pharmacokinetics in Ugandans. Br. J. Clin. Pharmacol. 68:690-699.
37. Núñez, M., et al. 2001. Higher efavirenz plasma levels correlate with development of insomnia. J. Acquir. Immune Defic. Syndr. 28:399-400.
38. Nyakutira, C., et al. 2008. High prevalence of the CYP2B6 516G→T (*6) variant and effect on the population pharmacokinetics of efavirenz in HIV/ AIDS outpatients in Zimbabwe. Eur. J. Clin. Pharmacol. 64:357-365.
39. Reference deleted.
40. Owen, A. 2006. The impact of host pharmacogenetics on antiretroviral drug disposition. Curr. Infect. Dis. Rep. 8:401-408. (Pubitemid 44445715)
41. Pereira, S. A., et al. 2008. Intra-individual variability in efavirenz plasma concentrations supports therapeutic drug monitoring based on quarterly sampling in the first year of therapy. Ther. Drug Monit. 30:60-66. (Pubitemid 351161100)
42. Pfister, M., et al. 2003. Population pharmacokinetics and pharmacodynamics of efavirenz, nelfinavir and indinavir. Antimicrob. Agents Chemother. 47: 130-137.
43. Puzantian, T. 2002. Central nervous system adverse effects with efavirenz: case report and review. Pharmacotherapy 22:930-933. (Pubitemid 34743443)
44. Ribaudo, H. J., et al. 2010. Effect of CYP2B6, ABCB1, and CYP3A5 polymorphisms on efavirenz pharmacokinetics and treatment response: an AIDS Clinical Trials Group study. J. Infect. Dis. 202:717-722.
45. Rivero, A., J. A. Mira, and J. A. Pineda. 2007. Liver toxicity induced by non-nucleoside reverse transcriptase inhibitors. J. Antimicrob. Chemother. 59:342-346. (Pubitemid 47073440)
46. Rodríguez-Nóvoa, S., P. Barreiro, I. Jiménez-Nacher, A. Rendón, and V. Soriano. 2005. Pharmacogenetics in HIV therapy. AIDS 7:103-112. (Pubitemid 41079021)
47. Rodriguez-Novoa, S., et al. 2005. Influence of 516G→T polymorphisms at the gene encoding the CYP450-2B6 isoenzyme on efavirenz plasma concentrations in HIV-infected subjects. Clin. Infect. Dis. 40:1358-1361. (Pubitemid 40570249)
48. Rotger, M., C. Csajka, and A. Telenti. 2006. Genetic, ethnic, and gender differences in the pharmacokinetics of antiretroviral agents. Curr. HIV/ AIDS Rep. 3:118-125. (Pubitemid 44874997)
49. Rotger, M., et al. 2007. Predictive value of known and novel alleles of CYP2B6 for efavirenz plasma concentrations in HIV-infected individuals. Clin. Pharmacol. Ther. 81:557-566. (Pubitemid 46454205)
50. Saitoh, A., et al. 2007. Efavirenz pharmacokinetics in HIV-1-infected children are associated with CYP2B6-G516T polymorphism. J. Acquir. Immune Defic. Syndr. 45:280-285. (Pubitemid 47012374)
51. Saitoh, A., et al. 2005. An MDR1-3435 variant is associated with higher plasma nelfinavir levels and more rapid virologic response in HIV-1 infected children. AIDS 19:371-380. (Pubitemid 40446183)
52. Sistonen, J., S. Fuselli, A. Levo, and A. Sajantila. 2005. CYP2D6 genotyping by a multiplex primer extension reaction. Clin. Chem. 51:1291-1295. (Pubitemid 43079419)
53. SPSS Inc. 2006. SPSS Base 15.0.1 for Windows user's guide. SPSS Inc., Chicago, IL.
54. Staszewski, S., et al. 1999. Efavirenz plus zidovudine and lamivudine, efavirenz plus indinavir, and indinavir plus zidovudine and lamivudine in the treatment of HIV-1 infection in adults. N. Engl. J. Med. 341:1865-1873.
55. Stöhr, W., et al. 2008. Factors influencing efavirenz and nevirapine plasma concentration: effect of ethnicity, weight and co-medication. Antivir. Ther. 13:675-685.
56. Torno, M. S., M. D. Witt, A. Saitoh, and C. V. Fletcher. 2008. Successful use of reduced-dose efavirenz in a patient with human immunodeficiency virus infection: case report and review of the literature. Pharmacotherapy 28:782-787. (Pubitemid 351975381)
57. Tsuchiya, K., et al. 2004. 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. 319:1322-1326. (Pubitemid 38759555)
58. Reference deleted.
59. Wang, J., et al. 2006. Identification of a novel specific CYP2B6 allele in Africans causing impaired metabolism of the HIV drug efavirenz. Pharmacogenet. Genomics 16:191-198.
60. Ward, B. A., et al. 2003. 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. 306:287-300. (Pubitemid 36734384)
61. World Health Organization. 24 October 2010, accession date. Antiretroviral therapy for HIV infection in adults and adolescents: recommendations for a public health approach (2006 revision). WHO, Geneva, Switzerland. http:www.who.int/hiv/pub/guidelines/artadultguidelines.pdf.