CYP2B6 genotype-based efavirenz dose recommendations during rifampicin-based antituberculosis cotreatment for a sub-Saharan Africa population

Pharmacogenomics

Volumn 17, Issue 6, 2016, Pages 603-613

  Mukonzo, Jackson K ^a   Bisaso, Ronald K ^a   Ogwal Okeng, Jasper ^a   Gustafsson, Lars L ^b   Owen, Joel S ^c   Aklillu, Eleni ^b  

^a MAKERERE UNIVERSITY   (Uganda)

^b KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^c UNION UNIVERSITY   (United States)

Author keywords

African population; cotreatment; dose recommendations; efavirenz; HIV TB

Indexed keywords

ALANINE AMINOTRANSFERASE; ALBUMIN; COTRIMOXAZOLE; CREATININE; CYTOCHROME P450 2A6; CYTOCHROME P450 2B6; CYTOCHROME P450 3A5; EFAVIRENZ; LAMIVUDINE; LAMIVUDINE PLUS ZIDOVUDINE; MULTIDRUG RESISTANCE PROTEIN 1; RIFAMPICIN; TATA BINDING PROTEIN; UREA; ZIDOVUDINE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; BENZOXAZINE DERIVATIVE; CYP2B6 PROTEIN, HUMAN; RNA DIRECTED DNA POLYMERASE INHIBITOR; TUBERCULOSTATIC AGENT;

AFRICA SOUTH OF THE SAHARA; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CD4 LYMPHOCYTE COUNT; CD4+ T LYMPHOCYTE; CONTROLLED STUDY; FEMALE; GENOTYPE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; MAJOR CLINICAL STUDY; MALE; RECOMMENDED DRUG DOSE; TUBERCULOSIS; UGANDAN; VIRUS LOAD; ADULT; COINFECTION; DRUG EFFECTS; GENETICS; HIV INFECTIONS; HUMAN IMMUNODEFICIENCY VIRUS 1;

ADULT; AFRICA SOUTH OF THE SAHARA; ANTI-HIV AGENTS; ANTITUBERCULAR AGENTS; BENZOXAZINES; COINFECTION; CYTOCHROME P-450 CYP2B6; FEMALE; GENOTYPE; HIV INFECTIONS; HIV-1; HUMANS; LAMIVUDINE; MALE; REVERSE TRANSCRIPTASE INHIBITORS; RIFAMPIN; TUBERCULOSIS; VIRAL LOAD; ZIDOVUDINE;

EID: 84966349291     PISSN: 14622416     EISSN: 17448042     Source Type: Journal    
DOI: 10.2217/pgs.16.7     Document Type: Article

References (42)

1. WHO/HTM/TB/420: Treatment of tuberculosis: guidelines (4th Ed). WHO Library Cataloguing-in-Publication Data. (2009). http://whqlibdoc.who.int/
2. Ngaimisi E, Habtewold A, Minzi O et al. Importance of ethnicity, 2B6 and ABCB1 genotype for efavirenz pharmacokinetics and treatment outcomes: a parallel-group prospective cohort study in two sub-Saharan Africa populations. PLoS ONE 8(7), e67946 (2013).
3. Brennan-Benson P, Lyus R, Harrison T, Pakianathan M, Macallan D. Pharmacokinetic interactions between efavirenz and rifampicin in the treatment of HIV and tuberculosis: one size does not fit all. AIDS 19(14), 1541-1543 (2005).
4. 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. 306(1), 287-300 (2003).
5. Ogburn ET, Jones DR, Masters AR, Xu C, Guo Y, Desta Z. Efavirenz primary and secondary metabolism in vitro and in vivo: identification of novel metabolic pathways and cytochrome P450 2A6 as the principal catalyst of efavirenz 7-hydroxylation. Drug Metab. Dispos. 38(7), 1218-1229 (2010).
6. Haas DW, Kwara A, Richardson DM et al. Secondary metabolism pathway polymorphisms and plasma efavirenz concentrations in HIV-infected adults with CYP2B6 slow metabolizer genotypes. J. Antimicrob. Chemother. 69(8), 2175-2182 (2014).
7. di Iulio J, Fayet A, Arab-Alameddine M et al. In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function. Pharmacogenet. Genomics 19(4), 300-309 (2009).
8. Ngaimisi E, Mugusi S, Minzi O et al. Long-term efavirenz autoinduction and its effect on plasma exposure in HIV patients. Clin. Pharmacol. Ther. 88(5), 676-684 (2010).
9. Miller DS, Bauer B, Hartz AM. Modulation of P-glycoprotein at the blood-brain barrier: opportunities to improve central nervous system pharmacotherapy. Pharmacol. Rev. 60(2), 196-209 (2008).
10. Dirson G, Fernandez C, Hindlet P et al. Efavirenz does not interact with the ABCB1 transporter at the blood-brain barrier. Pharm. Res. 23(7), 1525-1532 (2006).
11. Mukonzo JK, Roshammar D, Waako P et al. A novel polymorphism in ABCB1 gene, CYP2B6∗6 and sex predict single-dose efavirenz population pharmacokinetics in Ugandans. Br. J. Clin. Pharmacol. 68(5), 690-699 (2009).
12. Swart M, Ren Y, Smith P, Dandara C. ABCB1 4036A>G and 1236C>T polymorphisms affect plasma efavirenz levels in South African HIV/AIDS Patients. Front Genet 3, 236 (2012).
13. Elens L, Vandercam B, Yombi JC, Lison D, Wallemacq P, Haufroid V. Influence of host genetic factors on efavirenz plasma and intracellular pharmacokinetics in HIV-1-infected patients. Pharmacogenomics 11(9), 1223-1234 (2010).
14. Fellay J, Marzolini C, Meaden ER et al. Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study. Lancet 359(9300), 30-36 (2002).
15. Mukonzo JK, Owen JS, Ogwal-Okeng J et al. Pharmacogenetic-based efavirenz dose modification: suggestions for an African population and the different CYP2B6 genotypes. PLoS ONE 9(1), e86919 (2014).
16. Owen A, Goldring C, Morgan P, Park BK, Pirmohamed M. Induction of P-glycoprotein in lymphocytes by carbamazepine and rifampicin: the role of nuclear hormone response elements. Br. J. Clin. Pharmacol. 62(2), 237-242 (2006).
17. Niemi M, Backman JT, Fromm MF, Neuvonen PJ, Kivisto KT. Pharmacokinetic interactions with rifampicin: clinical relevance. Clin. Pharmacokinet. 42(9), 819-850 (2003).
18. Csajka C, Marzolini C, Fattinger K et al. Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection. Clin. Pharmacol. Ther. 73(1), 20-30 (2003).
19. Lopez-Cortes LF, Ruiz-Valderas R, Viciana P et al. Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis. Clin. Pharmacokinet. 41(9), 681-690 (2002).
20. Pozniak AL, Coyne KM, Miller RF et al. British HIV Association guidelines for the treatment of TB/HIV coinfection 2011. HIV Med. 12(9), 517-524 (2011).
21. Habtewold A, Makonnen E, Amogne W et al. Is there a need to increase the dose of efavirenz during concomitant rifampicin-based antituberculosis therapy in sub-Saharan Africa? The HIV-TB pharmagene study. Pharmacogenomics 16(10), 1047-1064 (2015).
22. Ngaimisi E, Mugusi S, Minzi O et al. Effect of rifampicin and CYP2B6 Genotype on long-term efavirenz autoinduction and plasma exposure in HIV patients with or without tuberculosis. Clin. Pharmacol. Ther. 90(3), 406-413 (2011)
23. Ramachandran G, Hemanth Kumar AK, Rajasekaran S et al. CYP2B6 G516T polymorphism but not rifampin coadministration influences steady-state pharmacokinetics of efavirenz in human immunodeficiency virus-infected patients in south India. Antimicrob. Agents Chemother. 53(3), 863-868 (2009).
24. Cohen K, Grant A, Dandara C et al. Effect of rifampicin-based antitubercular therapy and the cytochrome P450 2B6 516G>T polymorphism on efavirenz concentrations in adults in South Africa. Antivir. Ther. 14(5), 687-695 (2009).
25. Boulle A, Van Cutsem G, Cohen K et al. Outcomes of nevirapine- and efavirenz-based antiretroviral therapy when coadministered with rifampicin-based antitubercular therapy. JAMA 300(5), 530-539 (2008).
26. Sant'Anna FM, Velasque L, Costa MJ et al. Effectiveness of highly active antiretroviral therapy (HAART) used concomitantly with rifampicin in patients with tuberculosis and AIDS. Braz. J. Infect. Dis. 13(5), 362-366 (2009).
27. Mukonzo JK, Nanzigu S, Waako P, Ogwal-Okeng J, Gustafson LL, Aklillu E. CYP2B6 genotype, but not rifampicin-based anti-TB cotreatments, explains variability in long-term efavirenz plasma exposure. Pharmacogenomics 15(11), 1423-1435 (2014).
28. Arab-Alameddine M, Di Iulio J, Buclin T et al. Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals. Clin. Pharmacol. Ther. 85(5), 485-494 (2009).
29. Mukonzo JK, Okwera A, Nakasujja N et al. Influence of efavirenz pharmacokinetics and pharmacogenetics on neuropsychological disorders in Ugandan HIV-positive patients with or without tuberculosis: a prospective cohort study. BMC Infect. Dis. 13, 261 (2013).
30. Habtewold A, Amogne W, Makonnen E et al. Long-term effect of efavirenz autoinduction on plasma/peripheral blood mononuclear cell drug exposure and CD4 count is influenced by UGT2B7 and CYP2B6 genotypes among HIV patients. J. Antimicrob. Chemother. 66(10), 2350-2361 (2011).
31. Ngaimisi E, Mugusi S, Minzi O et al. Effect of rifampicin and CYP2B6 Genotype on long-term efavirenz autoinduction and plasma exposure in HIV patients with or without tuberculosis. Clin. Pharmacol. Ther. 90(3), 406-413 (2011).
32. Rotger M, Csajka C, Telenti A. Genetic, ethnic, and gender differences in the pharmacokinetics of antiretroviral agents. Curr. HIV/AIDS Rep. 3(3), 118-125 (2006).
33. Burger D, van der Heiden I, la Porte C et al. 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(2), 148-154 (2006).
34. Torno MS, Witt MD, Saitoh A, Fletcher CV. Successful use of reduced-dose efavirenz in a patient with human immunodeficiency virus infection: case report and review of the literature. Pharmacotherapy 28(6), 782-787 (2008).
35. Gatanaga H, Hayashida T, Tsuchiya K et al. Successful efavirenz dose reduction in HIV type 1-infected individuals with cytochrome P450 2B6 ∗6 and ∗26. Clin. Infect. Dis. 45(9), 1230-1237 (2007).
36. Group ES, Carey D, Puls R et al. Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomised, double-blind, placebo-controlled, non-inferiority ENCORE1 study. Lancet Infect. Dis. 15(7), 793-802 (2015).
37. Group ES, Puls R, Amin J et al. Efficacy of 400 mg efavirenz versus standard 600 mg dose in HIV-infected, antiretroviral-naive adults (ENCORE1): a randomised, double-blind, placebo-controlled, non-inferiority trial. Lancet 383(9927), 1474-1482 (2014).
38. Fayet Mello A, Buclin T, Decosterd LA et al. Successful efavirenz dose reduction guided by therapeutic drug monitoring. Antivir. Ther. 16(2), 189-197 (2011).
39. Hamers RL, Wallis CL, Kityo C et al. HIV-1 drug resistance in antiretroviral-naive individuals in sub-Saharan Africa after rollout of antiretroviral therapy: a multicentre observational study. Lancet Infect. Dis. 11(10), 750-759 (2011).
40. Yimer G, Ueda N, Habtewold A et al. Pharmacogenetic & pharmacokinetic biomarker for efavirenz based ARV and rifampicin based anti-TB drug induced liver injury in TB-HIV infected patients. PLoS ONE 6(12), e27810 (2011).
41. Yimer G, Amogne W, Habtewold A et al. High plasma efavirenz level and CYP2B6∗6 are associated with efavirenz-based HAART-induced liver injury in the treatment of naive HIV patients from Ethiopia: a prospective cohort study. Pharmacogenomics J. 12(6), 499-506 (2012).
42. Mugusi S, Ngaimisi E, Janabi M et al. Liver enzyme abnormalities and associated risk factors in HIV patients on efavirenz-based HAART with or without tuberculosis coinfection in Tanzania. PLoS ONE 7(7), e40180 (2012).