Clinical impact of patient population differences and genomic variation in efavirenz therapy

AIDS

Volumn 22, Issue 14, 2008, Pages 1709-1717

  King, Jennifer ^a   Aberg, Judith A ^b  

^a UNIVERSITY OF ALABAMA AT BIRMINGHAM   (United States)

^b NEW YORK UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Antiretroviral therapy; central nervous system; efavirenz; genetics; HIV; race ethnicity

Indexed keywords

ANTIRETROVIRUS AGENT; EFAVIRENZ; INDINAVIR; LAMIVUDINE PLUS ZIDOVUDINE; NEVIRAPINE; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ABNORMAL DREAMING; AREA UNDER THE CURVE; CENTRAL NERVOUS SYSTEM DISEASE; DIZZINESS; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG METABOLISM; DRUG WITHDRAWAL; ETHNICITY; GENETIC POLYMORPHISM; GENETIC VARIABILITY; GENOMICS; HALLUCINATION; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INSOMNIA; MENTAL CONCENTRATION; POPULATION DIFFERENTIATION; PRACTICE GUIDELINE; PRIORITY JOURNAL; REVIEW; SIDE EFFECT; SOMNOLENCE;

ANTIRETROVIRAL THERAPY, HIGHLY ACTIVE; ARYL HYDROCARBON HYDROXYLASES; BENZOXAZINES; ETHNIC GROUPS; HIV INFECTIONS; HUMANS; LIVER; OXIDOREDUCTASES, N-DEMETHYLATING; PATIENT COMPLIANCE; PHARMACOGENETICS; REVERSE TRANSCRIPTASE INHIBITORS; TREATMENT OUTCOME;

EID: 59849090678     PISSN: 02699370     EISSN: 14735571     Source Type: Journal    
DOI: 10.1097/QAD.0b013e32830163ad     Document Type: Review

References (68)

1. UNAIDS. Report on theglobal AIDS epidemic; December 2006. Available at: http://www.unaids.org/en/HIV-data/2006Global-Report/default.asp. [Accessed July 2007].
2. Holtgrave DR. Causes of the decline in AIDS deaths, United States, 1995-2002: prevention, treatment or both? IntJ STD AIDS 2005; 16:777-781.
3. Palella FJ Jr, Delaney KM, Moorman AC, Loveless MO, FuhrerJ, Satten GA, et al. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. N Engl J Med 1998; 338:853-860.
4. Sabin CA, Smith CJ, Youle M, Lampe FC, Bell DR, Puradiredja D, et al. Deaths in the era of HAART: contribution of late presentation, treatment exposure, resistance and abnormal laboratory markers. AIDS 2006; 20:67-71.
5. Centers for Disease Control and Prevention. HIV/AIDS Surveillance Report, 2005. US Department of Health and Human Services, CDC 2006; 17:1-54. Available at: http://www.cdc. gov/hiv/topics/surveillance/ resources/reports/. [Accessed July 2007].
6. Panel on Clinical Practices for the Treatment of HIV Infection. Guidelines for the use of antiretroviral agents in HIV-1 infected adults and adolescents; October 10, 2006. Available at: http://aidsinfo.nih.gov/ contentfiles/AdultandAdolescentGL.pdf. [Accessed July 2007].
7. Hammer SM, Saag MS, Schechter M, Montaner JS, Schooley RT, Jacobsen DM, et al. Treatment for adult HIV infection: 2006 recommendations of the International AIDS Society-USA panel. JAMA 2006; 296:827-843.
8. Staszewski S, Morales-RamirezJ, Tashima KT, Rachlis A, Skiest D, Stanford J, et al. 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 1999; 341:1865-1873.
9. Lucas GM, Chaisson RE, Moore RD. Comparison of initial combination antiretroviral therapy with a single protease inhibitor, ritonavir and saquinavir, or efavirenz. AIDS 2001; 15:1679-1686.
10. Keiser P, Nassar N, White C, Koen G, Moreno S. Comparison of nevirapine- and efavirenz-containing antiretroviral regimens in antiretroviral-naive patients: a cohort study. HIV Clin Trials 2002; 3:296-303.
11. Pulido F, ArribasJR, MiroJM, Costa MA, Gonzalez J, Rubio R, et al. Clinical, virologic, and immunologic response to efavir-enz-or protease inhibitor-based highly active antiretroviral therapy in a cohort of antiretroviral-naive patients with advanced HIV infection (EfaVIP 2 Study). J Acquir Immune Defic Syndr 2004; 35:343-350.
12. Gulick RM, Ribaudo HJ, Shikuma CM, Lustgarten S, Squires KE, Meyer WA III, et al. Triple-nucleoside regimens versus efavirenz-containing regimens for the initial treatment of HIV-1 infection. N EnglJ Med 2004; 350:1 850-1 861.
13. Bartlett JA, Johnson J, Herrera G, Sosa N, Rodriguez A, Liao Q, et al. Long-term results of initial therapy with abacavir and lamivudine combined with efavirenz, amprenavir/ritonavir, or stavudine. J Acquir Immune Defic Syndr 2006; 43:284-292.
14. Pulido F, Arribas J, Moreno S, Gatell J, Vendrell B, Serrano O. Similar virologic and immunologic response to efavirenz or lopinavir/ritonavir-based HAART in a large cohort of antiretroviral-naïve patients with advanced HIV infection. Eighth International Congress on Drug Therapy in HIV Infection; Glasgow; 2006 [abstract P9].
15. Haubrich RH, Riddler S, Ribaudo H, DiRienzo G, Garren K, George T, et al. Initial viral decay to assess the relative antiretroviral potency of PI-, NNRTI-, and NRTI-sparing regimens for first line therapy of HIV-1 infection: ACTG 5160s (sub-study of A5142). 14th Conference on Retroviruses and Opportunistic Infections; Los Angeles; 2007 [abstract 137].
16. Smith PF, DiCenzo R, Morse GD. Clinical pharmacokinetics of nonnucleoside reverse transcriptase inhibitors. Clin Pharma-cokinet 2001; 40:893-905.
17. Thomas SA. Anti-HIV drug distribution to the central nervous system. Curr Pharm Des 2004; 10:1313-1324.
18. Wynn HE, Brundage RC, Fletcher CV. Clinical implications of CNS penetration of antiretroviral drugs. CNS Drugs 2002; 16:595-609.
19. Taylor S, Reynolds H, Sabin CA, Drake SM, White DJ, Back DJ, et al. Penetration of efavirenz into the male genital tract: drug concentrations and antiviral activity in semen and blood of HIV-1-infected men. AIDS 2001; 15:2051-2053.
20. Cespedes MS, Aberg JA. Neuropsychiatric complications of antiretroviral therapy. Drug Saf 2006; 29:865-874.
21. Sustiva1 (efavirenz) capsules and tablets [US prescribing information]. Princeton, NJ: Bristol-Myers Squibb; January 2007.
22. Clifford DB, Evans S, Yang Y, Acosta EP, Goodkin K, Tashima K, et al. Impact of efavirenz on neuropsychological performance and symptoms in HIV-infected individuals. Ann Intern Med 2005; 143:714-721.
23. Marzolini C, Telenti A, Decosterd LA, Greub G, BiollazJ, Buclin T. Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients. AIDS 2001; 15:71-75.
24. Haas DW, Ribaudo HJ, Kim RB, Tierney C, Wilkinson GR, Gulick RM, et al. Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group Study. AIDS 2004; 18:2391-2400.
25. van Leth F, Phanuphak P, Ruxrungtham K, Baraldi E, Miller S, Gazzard B, et al. 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; 363:1253-1263.
26. Kappelhoff BS, van Leth F, Robinson PA, MacGregorTR, Baraldi E, Montella F, et al. Are adverse events of nevirapine and efavirenz related to plasma concentrations? Antivir Ther 2005; 10:489-498.
27. Fiske WD, Joshi AS, Labriola DF. An assessment of population pharmacokinetic parameters of efavirenz on nervous system symptoms and suppression of HIV RNA. The 41st Interscience Conference on Antimicrobial Agents and Chemotherapy; Chicago; 2001 [abstract 1727].
28. Fumaz CR, Munoz-Moreno JA, Molto J, Negredo E, Ferrer MJ, Sirera G, et al. Long-term neuropsychiatric disorders on efavir-enz-based approaches: quality of life, psychologic issues, and adherence. J Acquir Immune Defic Syndr 2005; 38:560-565.
29. Hirschel B, Flepp M, Bucher HC, Zellweger C, Telenti A, Wagels T, et al. Switching from protease inhibitors to efavirenz: differences in efficacy and tolerance among risk groups: a case-control study from the Swiss HIV Cohort. AIDS 2002; 16:381 -385.
30. Perez-Molina JA. Safety and tolerance of efavirenz in different antiretroviral regimens: results from a national multicenter prospective study in 1,033 HIV-infected patients. HIV Clin Trials 2002; 3:279-286.
31. Juethner SN, Seyfried W, Aberg JA. Tolerance of efavirenz-induced central nervous system side effects in HIV-infected individuals with a history of substance abuse. HIV Clin Trials 2003; 4:145-149.
32. Faggian F, Lattuada E, Lanzafame M, Antolini D, Concia E, Vento S. Recreational substance use and tolerance of efavirenz in HIV-1 infected patients. AIDS Care 2005; 17:908-910.
33. Hal man M. Management of depression and related neuro-pyschiatric symptoms associated with HIV/AIDS and antiretroviral therapy. Can J Infect Dis 2001; 12:9C-19C.
34. Seekins D, Lupo L, MaaJ, Bessen L, HodderS. Impact of race on nervous system side-effects of subjects taking efavirenz. Antivir Ther 2004; 9:L40.
35. Lupo LJ, Maa J-F, Dezil CM, Said D, Bessen L, Hodder S. Efficacy of efavirenz in different racial groups. Sixth International Congress on Drug Therapy in HIV Infection; Glasgow; 2002 [abstract P61].
36. Sension M, Jayaweera D, Lackey P, Farajallah A, MaaJ, Seekins D, et al. Impact of race on efficacy and the occurrence of nervous system symptoms (NSS) in HIV-infected patients following simplification from a twice-daily or more frequent HAART regimen to a once-daily efavirenz (EFV)-based HAART regimen. XVI International AIDS Conference; Toronto; 2006 [abstract THPE0141].
37. Silverberg MJ, Wegner SA, Milazzo MJ, McKaig RG, Williams CF, Agan BK, et al. Effectiveness of highly-active antiretroviral therapy by race/ethnicity. AIDS 2006; 20:1531-1538.
38. Barrett JS, Joshi AS, Chai M, Ludden TM, Fiske WD, Pieniaszek HJ Jr. Population pharmacokinetic meta-analysis with efavirenz. IntJ Clin Pharmacol Ther 2002; 40:507-519.
39. Csajka C, Marzolini C, Fattinger K, Decosterd LA, Fellay J, Telenti A, et al. Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection. Clin Pharmacol Ther 2003; 73:20-30.
40. 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; 26:267-270.
41. Pfister M, Labbe L, Hammer SM, Mellors J, Bennett KK, Rosenkranz S, et al. Population pharmacokinetics and pharma-codynamics of efavirenz, nelfinavir, and indinavir: an Adult AIDS Clinical Trial Group Study 398. Antimicrob Agents Chemother 2003; 47:130-137.
42. Lamba V, Lamba J, Yasuda K, Strom S, Davila J, Hancock ML, et al. Hepatic CYP2B6 expression: gender and ethnic differences and relationship to CYP2B6 genotype and CAR (constitutive androstane receptor) expression. J Pharmacol Exp Ther 2003; 307:906-922.
43. Burger D, van der Heiden I, la Porte C, van der Ende M, Groeneveld P, Richter C, et al. Interpatient variability in the pharmacokinetics of the HIV nonnucleoside reverse transcrip-tase inhibitor efavirenz: the effect of gender, race, and CYP2B6 polymorphism. Br J Clin Pharmacol 2006; 61:148-154.
44. 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.
45. LangT, Klein K, Fischer J, Nussler AK, Neuhaus P, Hofmann U, et al. Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver. Pharmacogenetics 2001; 11:399-415.
46. Zanger UM, Klein K, Saussele T, Blievernicht J, Hofmann H, Schwab M. Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance. Pharmacogenomics 2007; 8:743-759.
47. Rodriguez-Novoa S, Barreiro P, Rendon A, Jimenez-Nacher I, Gonzalez-LahozJ, Soriano V. Influence of 516G>T polymorphisms at the gene encoding the CYP450-2B6 isoenzyme on efavirenz plasma concentrations in HIV-infected subjects. Clin Infect Dis 2005; 40:1358-1361.
48. Rotger M, Colombo S, Furrer H, Bleiber G, Buclin T, Lee BL, et al. Influence of CYP2B6 polymorphism on plasma and intracellular concentrations and toxicity of efavirenz and nevirapine in HIV-infected patients. Pharmacogenet Genomics 2005; 15:1-5.
49. Klein K, Lang T, Saussele T, Barbosa-Sicard E, Schunck WH, Eichelbaum M, et al. Genetic variability of CYP2B6 in populations of African and Asian origin: allele frequencies, novel functional variants, and possible implications for anti-HIV therapy with efavirenz. Pharmacogenet Genomics 2005; 15:861-873.
50. LangT, Klein K, RichterT, Zibat A, Kerb R, Eichelbaum M, et al. Multiple novel nonsynonymous CYP2B6 gene polymorphisms in Caucasians: demonstration of phenotypic null alleles. I Pharmacol Exp Ther 2004; 311:34-43.
51. Rotger M, Tegude H, Colombo S, Cavassini M, Furrer H, Decosterd L, et al. Predictive value of known and novel alleles of CYP2B6 for efavirenz plasma concentrations in HIV-infected individuals. Clin Pharmacol Ther 2007; 81:557-566.
52. Desta Z, Saussele T, Ward B, Blievernicht J, Li L, Klein K, et al. Impact of CYP2B6 polymorphism on hepatic efavirenz metabolism in vitro. Pharmacogenomics 2007; 8:547-558.
53. WangJ, Sonnerborg A, Rane A, Josephson F, Lundgren S, Stahle L, et al. Identification of a novel specific CYP2B6 allele in Africans causing impaired metabolism of the HIV drug efavirenz. Pharmacogenet Genomics 2006; 16:191-198.
54. Tsuchiya K, Gatanaga H, Tachikawa N, Teruya K, Kikuchi Y, Yoshino M, et al. Homozygous CYP2B6 M6 (Q172H and K262R) correlates with high plasma efavirenz concentrations in HIV-1 patients treated with standard efavirenz-containing regimens. Biochem Biophys Res Commun 2004; 319:1322-1326.
55. Ribaudo HJ, Haas DW, Tierney C, Kim RB, Wilkinson GR, Gulick RM, et al. Pharmacogenetics of plasma efavirenz exposure after treatment discontinuation: an Adult AIDS Clinical Trials Group Study. Clin Infect Dis 2006; 42:401-407.
56. Shimada T, Yamazaki H, Mimura M, Inui Y, Guengerich FP. Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians. J Pharmacol Exp Ther 1994; 270:414-423.
57. Fellay J, Marzolini C, Meaden ER, Back DJ, Buclin T, ChaveJP, et al. Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study. Lancet 2002; 359:30-36.
58. Stormer E, von Moltke LL, Perloff MD, Greenblatt DJ. Differential modulation of P-glycoprotein expression and activity by nonnucleoside HI V-1 reverse transcriptase inhibitors in cell culture. Pharm Res 2002; 19:1038-1045.
59. Marzolini C, Leake B, SchwarzU, ChongS, Kim R. Evaluation of efavirenz transport by P-glycoprotein and uptake transporters. 13th Conference on Retroviruses and Opportunistic Infections; Denver; 2006 [abstract 565].
60. Myles O, Ehrenberg PH, Wortman G, Hawkes CA, Aronson NE, Blazes DL, et al. Impact of race on time to virologic failure in HIV-1 infected patients receiving efavirenz based therapy. XV International AIDS Conference; Bangkok; 2004 [abstract WePeA5625].
61. Haas DW, Smeaton LM, Shafer RW, Robbins GK, Morse GD, Labbe L, et al. Pharmacogenetics of long-term responses to antiretroviral regimens containing Efavirenz and/or Nelfinavir: an Adult AIDS Clinical Trials Group Study. J Infect Dis 2005; 192:1931-1942.
62. MotsingerAA, Ritchie MD, Shafer RW, Robbins GK, Morse GD, Labbe L, et al. Multilocus genetic interactions and response to efavirenz-containing regimens: an Adult AIDS Clinical Trials Group Study. Pharmacogenet Genomics 2006; 16: 837-845.
63. Gulick RM, Ribaudo HJ, Shikuma CM, Lalama C, Schackman BR, Meyer WA III, et al. Three- vs four-drug antiretroviral regimens for the initial treatment of HIV-1 infection: a randomized controlled trial. JAMA 2006; 296:769-781.
64. Schackman B, Ribaudo H, Krambrink A, Hughes V, Kuritzkes D, Gulick R. Racial differences in self-reported adherence and association with virologic failure on efavirenz (EFV)-containing regimens for initial HI V therapy: results from ACTG A5095. XVI International AIDS Conference; Toronto; 2006 [abstract TUPE0113].
65. Royal CD, Dunston GM. Changing the paradigm from 'race' to human genome variation. Nat Genet 2004; 36:S5-S7.
66. Jorde LB, Wooding SP. Genetic variation, classification and 'race'. Nat Genet 2004; 36:S28-S33.
67. Sehgal AR. Overlap between whites and blacks in response to antihypertensive drugs. Hypertension 2004; 43:566-572.
68. Destro-Bisol G, Maviglia R, Caglia A, Boschi I, Spedini G, Pascali V, et al. Estimating European admixture in African Americans by using microsatellites and a microsatellite haplotype (CD4/Alu). Hum Genet 1999; 104:149-157.