CYP3A induction and inhibition by different antiretroviral regimens reflected by changes in plasma 4β-hydroxycholesterol levels

European Journal of Clinical Pharmacology

Volumn 64, Issue 8, 2008, Pages 775-781

  Josephson, F ^a   Bertilsson, L ^a   Bottiger Y ^a   Flamholc, L ^b   Gisslen M ^c   Ormaasen, V ^d   Sonnerborg A ^a   Diczfalusy, U ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^b LUND UNIVERSITY HOSPITAL   (Sweden)

^c UNIVERSITY OF GOTHENBURG   (Sweden)

^d ULLEVÅL UNIVERSITY HOSPITAL   (Norway)

Author keywords

4 Hydroxycholesterol; Antiretroviral; Biomarker; CYP3A; Induction; Inhibition

Indexed keywords

4BETA HYDROXYCHOLESTEROL; ANTIRETROVIRUS AGENT; ATAZANAVIR PLUS RITONAVIR; CHOLESTEROL DERIVATIVE; CYTOCHROME P450 3A; EFAVIRENZ; LOPINAVIR PLUS RITONAVIR;

ADULT; AGED; ANTIVIRAL THERAPY; ARTICLE; CHOLESTEROL BLOOD LEVEL; CONTROLLED STUDY; ENZYME INDUCTION; ENZYME INHIBITION; FEMALE; HUMAN; MAJOR CLINICAL STUDY; MALE; PRIORITY JOURNAL;

EID: 45849151673     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00228-008-0492-8     Document Type: Article

References (22)

1. Breuer O (1995) Identification and quantitation of cholest-5-ene-3 beta,4 beta-diol in rat liver and human plasma. J Lipid Res 36:2275-2281
2. Bodin K, Bretillon L, Aden Y, Bertilsson L, Broome U, Einarsson C et al (2001) Antiepileptic drugs increase plasma levels of 4beta-hydroxycholesterol in humans: evidence for involvement of cytochrome p450 3A4. J Biol Chem 276:38685-38689
3. Breuer O, Dzeletovic S, Lund E, Diczfalusy U (1996) The oxysterols cholest-5-ene-3 beta,4 alpha-diol,cholest-5-ene-3 beta,4 beta-diol and cholestane-3 beta,5 alpha,6 alpha-triol are formed during in vitro oxidation of low density lipoprotein, and are present in human atherosclerotic plaques. Biochim Biophys Acta 1302:145-152
4. Bodin K, Andersson U, Rystedt E, Ellis E, Norlin M, Pikuleva I et al (2002) Metabolism of 4 beta -hydroxycholesterol in humans. J Biol Chem 277:31534-31540
5. Diczfalusy U, Miura J, Roh HK, Mirghani RA, Sayi J, Larsson H et al (2008) 4beta-hydroxycholesterol is a new endogenous CYP3A marker: relationship to CYP3A5 genotype, quinine 3-hydroxylation and sex in Koreans, Swedes and Tanzanians. Pharmacogenet Genomics 18:201-208
6. Mouly S, Lown KS, Kornhauser D, Joseph JL, Fiske WD, Benedek IH et al (2002) Hepatic but not intestinal CYP3A4 displays dose-dependent induction by efavirenz in humans. Clin Pharmacol Ther 72:1-9
7. Sustiva SPC, Bristol-Myers Squibb (2007) Available at: http://www.emea.europa.eu/humandocs/PDFs/EPAR/Sustiva/H-249-PI-en.pdf. Accessed 12 Aug 2007
8. Hsu A, Granneman GR, Bertz RJ (1998) Ritonavir. Clinical pharmacokinetics and interactions with other anti-HIV agents. Clin Pharmacokinet 35:275-291
9. Norvir SPC, Abbott (2007) Available at: http://www.emea.europa.eu/ humandocs/PDFs/EPAR/Norvir/H-127-PI-en.pdf. Accessed 12 August 2007
10. Reyataz SPC, Bristol-Myers Squibb (2007) Available at: http://www.emea.europa.eu/humandocs/PDFs/EPAR/reyataz/H-494-PI-en.pdf. Accessed 12 Aug 2007
11. Yeh RF, Gaver VE, Patterson KB, Rezk NL, Baxter-Meheux F, Blake MJ et al (2006) Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. J Acquir Immune Defic Syndr 42:52-60
12. Shikuma CM, Yang Y, Glesby MJ, Meyer WA 3rd, Tashima KT, Ribaudo HJ et al (2007) Metabolic effects of protease inhibitor-sparing antiretroviral regimens given as initial treatment of HIV-1 Infection (AIDS Clinical Trials Group Study A5095). J Acquir Immune Defic Syndr 44:540-550
13. Kaletra SPC, Abbott (2007) Available at: http://www.emea.europa.eu/ humandocs/PDFs/EPAR/kaletra/H-368-PI-en.pdf. Accessed at 12 Aug 2007
14. Malan N, Kranz E, David N, Kastango K, Frederick D, Matthew M et al (2006) Efficacy and safety of atazanavir-based therapy in antiretroviral naive HIV-1 infected subjects, both with and without ritonavir: 48-week results form AI424-089 (abstract no.107LB). In: 13th Conf Retroviruses Opportunistic Infections. Denver, CO.
15. Galteau MM, Shamsa F (2003) Urinary 6beta-hydroxycortisol: a validated test for evaluating drug induction or drug inhibition mediated through CYP3A in humans and in animals. Eur J Clin Pharmacol 59:713-733
16. Kaletra, Scientific Discussion. Abbott (2007) Available at: http://www.emea.europa.eu/humandocs/PDFs/EPAR/kaletra/453001en6.pdf. Accessed 12 Aug 2007
17. Vishnuvardhan D, Moltke LL, Richert C, Greenblatt DJ (2003) Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. Aids 17:1092-1094
18. Anonymous. Study No: APV10018. Available at: http://ctr.gsk.co.uk/ Summary/fosamprenavir/studylist.asp. Accessed 12 Aug 2007
19. Prezista SPC, Janssen Cilag (2007) Available at: http://www.emea.europa. eu/humandocs/PDFs/EPAR/prezista/H-707-PI-en.pdf.. Accessed 12 Aug 2007
20. van der Lee MJ, Dawood L, ter Hofstede HJ, de Graaff-Teulen MJ, van Ewijk-Beneken Kolmer EW, Caliskan-Yassen N et al (2006) Lopinavir/ritonavir reduces lamotrigine plasma concentrations in healthy subjects. Clin Pharmacol Ther 80:159-168
21. Burger DM, Huisman A, van Ewijk N, Neisingh H, Rongen G, Koopmans PP et al (2007) The effect of atazanavir and atazanavir/ritonavir on UGT1A4 using lamotrigine as a phenotypic probe (abstract no. 566) In: 14th Conf Retroviruses Opportunistic Infections). Los Angeles, CA
22. Fromm MF, Schwilden H, Bachmakov I, Konig J, Bremer F, Schuttler J (2007) Impact of the CYP3A5 genotype on midazolam pharmacokinetics and pharmacodynamics during intensive care sedation. Eur J Clin Pharmacol 63:1129-1133