Comparison of two endogenous biomarkers of CYP3A4 activity in a drug-drug interaction study between midostaurin and rifampicin

European Journal of Clinical Pharmacology

Volumn 70, Issue 8, 2014, Pages 915-920

  Dutreix, Catherine ^a   Lorenzo, Sebastien ^a   Wang, Yanfeng ^a,b  

^a NOVARTIS PHARMA AG   (Switzerland)

^b ISIS PHARMACEUTICALS   (United States)

Author keywords

4 hydroxycholesterol; 6 hydroxycortisol to cortisol ratio; CYP3A4 biomarker; Midostaurin; Rifampicin

Indexed keywords

4BETA HYDROXYCHOLESTEROL; 6BETA HYDROXYHYDROCORTISONE; CYTOCHROME P450 3A4; MIDOSTAURIN; PLACEBO; RIFAMPICIN; UNCLASSIFIED DRUG; 4'-N-BENZOYLSTAUROSPORINE; 6 BETA-HYDROXYCORTISOL; BIOLOGICAL MARKER; CHOLEST-5-ENE-3,4-DIOL; CHOLESTEROL DERIVATIVE; CYP3A4 PROTEIN, HUMAN; CYTOCHROME P450 3A; CYTOCHROME P450 3A INDUCER; HYDROCORTISONE; PROTEIN KINASE INHIBITOR; STAUROSPORINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROL GROUP; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG BLOOD LEVEL; DRUG INTERACTION; ENZYME ACTIVITY; ENZYME INDUCTION; FEMALE; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; ANALOGS AND DERIVATIVES; BLOOD; METABOLISM; MIDDLE AGED; URINE; YOUNG ADULT;

ADULT; BIOLOGICAL MARKERS; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 CYP3A INDUCERS; DRUG INTERACTIONS; FEMALE; HUMANS; HYDROCORTISONE; HYDROXYCHOLESTEROLS; MALE; MIDDLE AGED; PROTEIN KINASE INHIBITORS; RIFAMPIN; STAUROSPORINE; YOUNG ADULT;

EID: 84905119053     PISSN: 00316970     EISSN: 14321041     Source Type: Journal    
DOI: 10.1007/s00228-014-1675-0     Document Type: Article

References (24)

1. Frye RF (2004) Probing the world of cytochrome P450 enzymes. Mol Interv 4:157-162
2. Foti RS, Rock DA, Wienkers LC, Wahlstrom JL (2010) Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation. Drug Metab Dispos 38:981-987
3. Lamba JK, Lin YS, Schuetz EG, Thummel KE (2002) Genetic contribution to variable human CYP3A-mediated metabolism. Adv Drug Deliv Rev 54:1271-1294 (Pubitemid 35284253)
4. Lepper ER, Baker SD, Permenter M, Ries N, van Schaik RH, Schenk PW, Price DK, Ahn D, Smith NF, Cusatis G, Ingersoll RG, Bates SE, Mathijssen RH, Verweij J, Figg WD, Sparreboom A (2005) Effect of common CYP3A4 and CYP3A5 variants on the pharmacokinetics of the cytochrome P450 3A phenotyping probe midazolam in cancer patients. Clin Cancer Res 11:7398-7404 (Pubitemid 41507700)
5. Racha JK, Zhao ZS, Olejnik N, Warner N, Chan R, Moore D, Satoh H (2003) Substrate dependent inhibition profiles of fourteen drugs on CYP3A4 activity measured by a high throughput LCMS/MS method with four probe drugs, midazolam, testosterone, nifedipine and terfenadine. Drug Metab Pharmacokinet 18:128-138
6. Ged C, Rouillon JM, Pichard L, Combalbert J, Bressot N, Bories P, Michel H, Beaune P, Maurel P (1989) The increase in urinary excretion of 6 beta-hydroxycortisol as a marker of human hepatic cytochrome P450IIIA induction. Br J Clin Pharmacol 28:373-387 (Pubitemid 19269774)
7. Bodin K, Bretillon L, Aden Y, Bertilsson L, Broome U, Einarsson C, Diczfalusy U (2001) Antiepileptic drugs increase plasma levels of 4beta-hydroxycholesterol in humans: evidence for involvement of cytochrome p450 3A4. J Biol Chem 276:38685-38689
8. Chen YC, Gotzkowsky SK, Nafziger AN, Kulawy RW, Rocci ML Jr, Bertino JS Jr, Kashuba AD (2006) Poor correlation between 6beta-hydroxycortisol: cortisol molar ratios and midazolam clearance as measure of hepatic CYP3Aactivity. Br J Clin Pharmacol 62:187-195 (Pubitemid 44316429)
9. Diczfalusy U, Kanebratt KP, Bredberg E, Andersson TB, Bottiger Y, Bertilsson L (2009) 4beta-hydroxycholesterol as an endogenous marker for CYP3A4/5 activity. Stability and half-life of elimination after induction with rifampicin. Br J Clin Pharmacol 67:38-43
10. Tomalik-Scharte D, Lutjohann D, Doroshyenko O, Frank D, Jetter A, Fuhr U (2009) Plasma 4beta-hydroxycholesterol: an endogenous CYP3A metric? Clin Pharmacol Ther 86:147-153
11. Diczfalusy U, Nylen H, Elander P, Bertilsson L (2011) 4beta-Hydroxycholesterol, an endogenous marker of CYP3A4/5 activity in humans. Br J Clin Pharmacol 71:183-189
12. Bjorkhem-Bergman L, Backstrom T, Nylen H, Ronquist-Nii Y, Bredberg E, Andersson TB, Bertilsson L, Diczfalusy U (2013) Comparison of endogenous 4beta-hydroxycholesterol with midazolam as markers for CYP3A4 induction by rifampicin. Drug Metab Dispos 41:1488-1493
13. Marde Arrhen Y, Nylen H, Lovgren-Sandblom A, Kanebratt KP, Wide K, Diczfalusy U (2013) A comparison of 4beta-hydroxycholesterol/cholesterol and 6beta-hydroxycortisol/cortisol as markers of CYP3A4 induction. Br J Clin Pharmacol 75:1536-1540
14. Shin KH, Choi MH, Lim KS, Yu KS, Jang IJ, Cho JY (2013) Evaluation of endogenous metabolic markers of hepatic CYP3A activity using metabolic profiling and midazolam clearance. Clin Pharmacol Ther 94:601-609
15. Tran JQ, Kovacs SJ, McIntosh TS, Davis HM, Martin DE (1999) Morning spot and 24-hour urinary 6 beta-hydroxycortisol to cortisol ratios: intraindividual variability and correlation under basal conditions and conditions of CYP 3A4 induction. J Clin Pharmacol 39:487-494 (Pubitemid 29356469)
16. Stone RM, DeAngelo DJ, Klimek V, Galinsky I, Estey E, Nimer SD, Grandin W, Lebwohl D, Wang Y, Cohen P (2005) Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412. Blood 105:54-60 (Pubitemid 40053063)
17. Gotlib J, DeAngelo DJ, George TI, Corless CL, Linder A, Langford C, Dutreix C, Gross S, Nikolova Z, Graubert T (2010) KIT inhibitor midostaurin exhibits a high rate of clinically meaningful and durable responses in advanced systemic mastocytosis: report of a fully accrued phase II trial. Blood 116:abstract 316
18. Gotlib J, Kluin-Nelemans HC, George TI, Akin C, Sotlar K, Hermine O, Awan F, Hexner E, Mauro M, Morariu R, Squier M, Villeneuve M, Emery-Salbert F, Hartmann K, Horny HP, Valent P, Reiter A (2012) KIT inhibitor midostaurin in patients with advanced systemic mastocytosis: results of a planned interim analysis of the global CPKC412D2201 trial. Blood 120:799
19. Gotlib J, Kluin-Nelemans HC, George TI, Akin C, Sotlar K, Hermine O, Awan F, Hexner E, Mauro M, Morariu R, Squier M, Villeneuve M, Emery-Salbert F, Coombs J, Hartmann K, Horny H, Valent P, Reiter A (2013) Durable responses and improved quality of life with midostaurin (PKC412) in advanced systemic mastocytosis (SM): updated stage 1 results of the global D2201 trial. Blood 122:106
20. Dutreix C, Munarini F, Lorenzo S, Roesel J, Wang Y (2013) Investigation of CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers. Cancer Chemother Pharmacol 72:1223-1234
21. Bodin K, Andersson U, Rystedt E, Ellis E, Norlin M, Pikuleva I, Eggertsen G, Bjorkhem I, Diczfalusy U (2002)Metabolism of 4 beta-hydroxycholesterol in humans. J Biol Chem 277:31534-31540
22. Diczfalusy U, Miura J, Roh HK, Mirghani RA, Sayi J, Larsson H, Bodin KG, Allqvist A, Jande M, Kim JW, Aklillu E, Gustafsson LL, Bertilsson L (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 (Pubitemid 351323234)
23. Lee C (1995) Urinary 6 beta-hydroxycortisol in humans: analysis, biological variations, and reference ranges. Clin Biochem 28:49-54
24. Weitzman ED, Fukushima D, Nogeire C, Roffwarg H, Gallagher TF, Hellman L (1971) Twenty-four hour pattern of the episodic secretion of cortisol in normal subjects. J Clin Endocrinol Metab 33:14-22