Effect of rifampicin and CYP2B6 genotype on long-term efavirenz autoinduction and plasma exposure in HIV patients with or without tuberculosis

Clinical Pharmacology and Therapeutics

Volumn 90, Issue 3, 2011, Pages 406-413

  Ngaimisi, E ^a,b   Mugusi, S ^a,c   Minzi, O ^b   Sasi, P ^b   Riedel, K D ^d   Suda, A ^a   Ueda, N ^a   Janabi, M ^c   Mugusi, F ^b   Haefeli, W E ^d   Bertilsson, L ^a   Burhenne, J ^d   Aklillu, E ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^b MUHIMBILI UNIVERSITY OF HEALTH AND ALLIED SCIENCES   (Tanzania)

^c MUHIMBILI NATIONAL HOSPITAL   (Tanzania)

^d UNIVERSITY OF HEIDELBERG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

8 HYDROXYEFAVIRENZ; DRUG METABOLITE; EFAVIRENZ; RIFAMPICIN; UNCLASSIFIED DRUG;

ADULT; ARTICLE; CONTROLLED STUDY; CYP2B6 GENE; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG EXPOSURE; FEMALE; GENE; GENE FREQUENCY; GENETIC VARIABILITY; GENOTYPE; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTED PATIENT; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LUNG TUBERCULOSIS; MAJOR CLINICAL STUDY; MALE; PRIORITY JOURNAL; PROSPECTIVE STUDY;

ALLELES; ANTI-HIV AGENTS; ANTIBIOTICS, ANTITUBERCULAR; ANTIRETROVIRAL THERAPY, HIGHLY ACTIVE; ARYL HYDROCARBON HYDROXYLASES; BENZOXAZINES; CYTOCHROME P-450 CYP3A; DRUG INTERACTIONS; ENZYME INDUCTION; FEMALE; GENOTYPE; HIV INFECTIONS; HIV-1; HUMANS; MALE; OXIDOREDUCTASES, N-DEMETHYLATING; P-GLYCOPROTEIN; POLYMORPHISM, SINGLE NUCLEOTIDE; REVERSE TRANSCRIPTASE INHIBITORS; RIFAMPIN; TUBERCULOSIS;

EID: 80052038032     PISSN: 00099236     EISSN: 15326535     Source Type: Journal    
DOI: 10.1038/clpt.2011.129     Document Type: Article

References (38)

1. Lawn, S.D., Myer, L., Bekker, L.G. & Wood, R. Burden of tuberculosis in an antiretroviral treatment programme in sub-Saharan Africa: impact on treatment outcomes and implications for tuberculosis control. AIDS 20, 1605-1612 (2006). (Pubitemid 44162402)
2. Cain, K.P. et al. Causes of death in HIV-infected persons who have tuberculosis, Thailand. Emerging Infect. Dis. 15, 258-264 (2009).
3. Manosuthi, W., Chottanapand, S., Thongyen, S., Chaovavanich, A. & Sungkanuparph, S. Survival rate and risk factors of mortality among HIV/tuberculosis-coinfected patients with and without antiretroviral therapy. J. Acquir. Immune Defic. Syndr. 43, 42-46 (2006). (Pubitemid 44306486)
4. World Health Organization. Treatment of Tuberculosis: Guidelines, 4th edn (2009).
5. P ozniak, A.L. et al. British HIV Association Guidelines for the Treatment of TB/HIV Co-infection 2009 1 (British HIV Association (BHIVA), London, 2009).
6. Hoffmann, C.J. et al. Hepatotoxicity in an African antiretroviral therapy cohort: the effect of tuberculosis and hepatitis B. AIDS 21, 1301-1308 (2007). (Pubitemid 46883484)
7. Faucette, S.R. et al. Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers. J. Pharmacol. Exp. Ther. 320, 72-80 (2007). (Pubitemid 46025721)
8. Ward, B.A., Gorski, J.C., Jones, D.R., Hall, S.D., Flockhart, D.A. & 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, 287-300 (2003). (Pubitemid 36734384)
9. Ogburn, E.T., Jones, D.R., Masters, A.R., 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, 1218-1229 (2010).
10. Itoh, M. et al. Induction of human CYP2A6 is mediated by the pregnane X receptor with peroxisome proliferator-activated receptor-gamma coactivator 1alpha. J. Pharmacol. Exp. Ther. 319, 693-702 (2006).
11. Cabrera, S.E. et al. Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients. Antimicrob. Agents Chemother. 53, 2791-2798 (2009).
12. Mukonzo, J.K. 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, 690-699 (2009).
13. Arab-Alameddine, M. et al.; Swiss HIV Cohort Study. Pharmacogeneticsbased population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals. Clin. Pharmacol. Ther. 85, 485-494 (2009).
14. López-Cortés, L.F. et al. Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis. Clin. Pharmacokinet. 41, 681-690 (2002).
15. Matteelli, A. et al. Multiple-dose pharmacokinetics of efavirenz with and without the use of rifampicin in HIV-positive patients. Curr. HIV Res. 5, 349-353 (2007). (Pubitemid 46785071)
16. T ang, C., Lin, J.H. & Lu, A.Y. Metabolism-based drug-drug interactions: what determines individual variability in cytochrome P450 induction? Drug Metab. Dispos. 33, 603-613 (2005). (Pubitemid 40593872)
17. Ngaimisi, E. et al. Long-term efavirenz autoinduction and its effect on plasma exposure in HIV patients. Clin. Pharmacol. Ther. 88, 676-684 (2010).
18. Marzolini, C., Telenti, A., Decosterd, L.A., 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 15, 71-75 (2001). (Pubitemid 32055781)
19. Bacheler, L.T. et al. Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy. Antimicrob. Agents Chemother. 44, 2475-2484 (2000). (Pubitemid 30650898)
20. Faucette, S.R. et al. Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers. Drug Metab. Dispos. 32, 348-358 (2004). (Pubitemid 38263894)
21. Wang, H., Faucette, S., Moore, R., Sueyoshi, T., Negishi, M. & LeCluyse, E. Human constitutive androstane receptor mediates induction of CYP2B6 gene expression by phenytoin. J. Biol. Chem. 279, 29295-29301 (2004). (Pubitemid 38915806)
22. S ueyoshi, T., Kawamoto, T., Zelko, I., Honkakoski, P. & Negishi, M. The repressed nuclear receptor CAR responds to phenobarbital in activating the human CYP2B6 gene. J. Biol. Chem. 274, 6043-6046 (1999). (Pubitemid 29111006)
23. Wang, H. et al. A novel distal enhancer module regulated by pregnane X receptor/constitutive androstane receptor is essential for the maximal induction of CYP2B6 gene expression. J. Biol. Chem. 278, 14146-14152 (2003). (Pubitemid 36799961)
24. Xie, W. et al. Reciprocal activation of xenobiotic response genes by nuclear receptors SXR/PXR and CAR. Genes Dev. 14, 3014-3023 (2000).
25. Desai, P.B. et al. Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen. Drug Metab. Dispos. 30, 608-612 (2002). (Pubitemid 34456986)
26. Faucette, S.R., Sueyoshi, T., Smith, C.M., Negishi, M., Lecluyse, E.L. & Wang, H. Differential regulation of hepatic CYP2B6 and CYP3A4 genes by constitutive androstane receptor but not pregnane X receptor. J. Pharmacol. Exp. Ther. 317, 1200-1209 (2006). (Pubitemid 43764125)
27. Kwara, A., Lartey, M., Sagoe, K.W. & Court, M.H. Paradoxically elevated efavirenz concentrations in HIV/tuberculosis-coinfected patients with CYP2B6 516TT genotype on rifampin-containing antituberculous therapy. AIDS 25, 388-390 (2011).
28. Mutlib, A.E. et al. Identification and characterization of efavirenz metabolites by liquid chromatography/mass spectrometry and high field NMR: species differences in the metabolism of efavirenz. Drug Metab. Dispos. 27, 1319-1333 (1999).
29. Cho, D.Y., Ogburn, E.T., Jones, D. & Desta, Z. Contribution of N-glucuronidation to efavirenz elimination in vivo in the basal and rifampin-induced metabolism of efavirenz. Antimicrob. Agents Chemother. 55, 1504-1509 (2011).
30. Soars, M.G., Petullo, D.M., Eckstein, J.A., Kasper, S.C. & Wrighton, S.A. An assessment of udp-glucuronosyltransferase induction using primary human hepatocytes. Drug Metab. Dispos. 32, 140-148 (2004). (Pubitemid 38112546)
31. Chen, J. & Raymond, K. Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor. Ann. Clin. Microbiol. Antimicrob. 5, 3 (2006).
32. Kwara, A., Lartey, M., Sagoe, K.W., Kenu, E. & Court, M.H. CYP2B6, CYP2A6 and UGT2B7 genetic polymorphisms are predictors of efavirenz mid-dose concentration in HIV-infected patients. AIDS 23, 2101-2106 (2009).
33. Gallicano, K.D. et al. Induction of zidovudine glucuronidation and amination pathways by rifampicin in HIV-infected patients. Br. J. Clin. Pharmacol. 48, 168-179 (1999). (Pubitemid 29349452)
34. Bélanger, A.S., Caron, P., Harvey, M., Zimmerman, P.A., Mehlotra, R.K. & Guillemette, C. Glucuronidation of the antiretroviral drug efavirenz by UGT2B7 and an in vitro investigation of drug-drug interaction with zidovudine. Drug Metab. Dispos. 37, 1793-1796 (2009).
35. di Iulio, J. et al.; Swiss HIV Cohort Study. In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function. Pharmacogenet. Genomics 19, 300-309 (2009).
36. Wen, X., Wang, J.S., Neuvonen, P.J. & Backman, J.T. Isoniazid is a mechanismbased inhibitor of cytochrome P450 1A2, 2A6, 2C19 and 3A4 isoforms in human liver microsomes. Eur. J. Clin. Pharmacol. 57, 799-804 (2002). (Pubitemid 34143338)
37. Burhenne, J. et al. No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment. Antimicrob. Agents Chemother. 54, 4185-4191 (2010).
38. US Food and Drug Administration. Guidance for Industry, Bioanalytical Method Validation (2001).