Roles of different cyp enzymes in the formation of specific fluvastatin metabolites by human liver microsomes

Basic and Clinical Pharmacology and Toxicology

Volumn 105, Issue 5, 2009, Pages 327-332

  Toda, Takaki ^a,b   Eliasson, Erik ^a   Ask, Birgitta ^a   Inotsume, Nobuo ^a,b   Rane, Anders ^a  

^a KAROLINSKA INSTITUTE   (Sweden)

^b HOKKAIDO INSTITUTE OF TECHNOLOGY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

5 HYDROXY FLUVASTATIN; 6 HYDROXY FLUVASTATIN; CYTOCHROME; CYTOCHROME P450 2C19; CYTOCHROME P450 2C8; CYTOCHROME P450 2C9; CYTOCHROME P450 3A; FLUINDOSTATIN; KETOCONAZOLE; MONOCLONAL ANTIBODY; N DESISOPROPYL FLUVASTATIN; QUERCETIN; SULFAPHENAZOLE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG METABOLISM; HUMAN; HUMAN CELL; LIVER MICROSOME; PRIORITY JOURNAL;

ANTIBODIES, MONOCLONAL; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 ENZYME SYSTEM; DRUG INTERACTIONS; FATTY ACIDS, MONOUNSATURATED; HUMANS; HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITORS; INDOLES; KETOCONAZOLE; MICROSOMES, LIVER; QUERCETIN; SULFAPHENAZOLE;

EID: 70350025073     PISSN: 17427835     EISSN: 17427843     Source Type: Journal    
DOI: 10.1111/j.1742-7843.2009.00453.x     Document Type: Article

References (30)

1. Banga JD, Jacotot B, Pfister P, Mehra M. Long-term treatment of hypercholesterolemia with fluvastatin: a 52-week multicenter safety and efficacy study. French-Dutch Fluvastatin Study Group. Am J Med 1994 96 : 87S 93S.
2. Davidson MH. Fluvastatin Long-Term Extension Trial (FLUENT): summary of efficacy and safety. Am J Med 1994 96 : 41S 4S.
3. Serruys PW, de Feyter P, Macaya C, Kokott N, Puel J, Vrolix M et al. Fluvastatin for prevention of cardiac events following successful first percutaneous coronary intervention: a randomized controlled trial. JAMA 2002 287 : 3215 3222.
4. Herd JA, Ballantyne CM, Farmer JA, Ferguson JJ III., Jones PH, West MS et al. Effects of fluvastatin on coronary atherosclerosis in patients with mild to moderate cholesterol elevations (Lipoprotein and Coronary Atherosclerosis Study [LCAS]). Am J Cardiol 1997 80 : 278 286.
5. Ayalasomayajula SP, Vaidyanathan S, Kemp C, Prasad P, Balch A, Dole WP. Effect of clopidogrel on the steady-state pharmacokinetics of fluvastatin. J Clin Pharmacol 2007 47 : 613 619.
6. Kantola T, Backman JT, Niemi M, Kivistö KT, Neuvonen PJ. Effect of fluconazole on plasma fluvastatin and pravastatin concentrations. Eur J Clin Pharmacol 2000 56 : 225 229.
7. Scripture CD, Pieper JA. Clinical pharmacokinetics of fluvastatin. Clin Pharmacokinet 2001 40 : 263 281.
8. Kivistö KT, Kantola T, Neuvonen PJ. Different effects of itraconazole on the pharmacokinetics of fluvastatin and lovastatin. Br J Clin Pharmacol 1998 46 : 49 53.
9. Tse FL, Jaffe JM, Troendle A. Pharmacokinetics of fluvastatin after single and multiple doses in normal volunteers. J Clin Pharmacol 1992 32 : 630 638.
10. Dain JG, Fu E, Gorski J, Nicoletti J, Scallen TJ. Biotransformation of fluvastatin sodium in humans. Drug Metab Dispos 1993 21 : 567 572.
11. Fischer V, Johanson L, Heitz F, Tullman R, Graham E, Baldeck JP et al. The 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor fluvastatin: effect on human cytochrome P-450 and implications for metabolic drug interactions. Drug Metab Dispos 1999 27 : 410 416.
12. Lowry OH, Rosebrough NJ, Farr AL, Randall RJ. Protein measurements with the Folin phenol reagent. J Biol Chem 1951 193 : 265 275.
13. Sullivan-Klose TH, Ghanayem BI, Bell DA, Zhang ZY, Kaminsky LS, Shenfield GM et al. The role of the CYP2C9-Leu359 allelic variant in the tolbutamide polymorphism. Pharmacogenetics 1996 6 : 341 349.
14. Yasar U, Eliasson E, Dahl ML, Johansson I, Ingelman-Sundberg M, Sjöqvist F. Validation of methods for CYP2C9 genotyping: frequencies of mutant alleles in a Swedish population. Biochem Biophys Res Commun 1999 254 : 628 631.
15. Krausz KW, Goldfarb I, Buters JT, Yang TJ, Gonzalez FJ, Gelboin HV. Monoclonal antibodies specific and inhibitory to human cytochromes P450 2C8, 2C9, and 2C19. Drug Metab Dispos 2001 29 : 1410 1423.
16. Lundblad MS, Stark K, Eliasson E, Oliw E, Rane A. Biosynthesis of epoxyeicosatrienoic acids varies between polymorphic CYP2C enzymes. Biochem Biophys Res Commun 2005 327 : 1052 1057.
17. Clarke SE. In vitro assessment of human cytochrome P450. Xenobiotica 1998 28 : 1167 1202.
18. Venkatakrishnan K, Von Moltke LL, Greenblatt DJ. Human drug metabolism and the cytochromes P450: application and relevance of in vitro models. J Clin Pharmacol 2001 41 : 1149 1179.
19. Donato MT, Castell JV. Strategies and molecular probes to investigate the role of cytochrome P450 in drug metabolism: focus on in vitro studies. Clin Pharmacokinet 2003 42 : 153 178.
20. Sai Y, Dai R, Yang TJ, Krausz KW, Gonzalez FJ, Gelboin HV et al. Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450. Xenobiotica 2000 30 : 327 343.
21. Gelboin HV, Krausz K. Monoclonal antibodies and multifunctional cytochrome P450: drug metabolism as paradigm. J Clin Pharmacol 2006 46 : 353 372.
22. Baldwin SJ, Bloomer JC, Smith GJ, Ayrton AD, Clarke SE, Chenery RJ. Ketoconazole and sulphaphenazole as the respective selective inhibitors of P4503A and 2C9. Xenobiotica 1995 25 : 261 270.
23. Mancy A, Dijols S, Poli S, Guengerich P, Mansuy D. Interaction of sulfaphenazole derivatives with human liver cytochromes P450 2C: molecular origin of the specific inhibitory effects of sulfaphenazole on CYP 2C9 and consequences for the substrate binding site topology of CYP 2C9. Biochemistry 1996 35 : 16205 16212.
24. Newton DJ, Wang RW, Lu AY. Cytochrome P450 inhibitors. Evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metab Dispos 1995 23 : 154 158.
25. Dierks EA, Stams KR, Lim HK, Cornelius G, Zhang H, Ball SE. A method for the simultaneous evaluation of the activities of seven major human drug-metabolizing cytochrome P450s using an in vitro cocktail of probe substrates and fast gradient liquid chromatography tandem mass spectrometry. Drug Metab Dispos 2001 29 : 23 9.
26. Walsky RL, Obach RS, Gaman EA, Gleeson JP, Proctor WR. Selective inhibition of human cytochrome P4502C8 by montelukast. Drug Metab Dispos 2005 33 : 413 418.
27. Ong CE, Coulter S, Birkett DJ, Bhasker CR, Miners JO. The xenobiotic inhibitor profile of cytochrome P4502C8. Br J Clin Pharmacol 2000 50 : 573 580.
28. Yasar U, Eliasson E, Forslund-Bergengren C, Tybring G, Gadd M, Sjöqvist F et al. The role of CYP2C9 genotype in the metabolism of diclofenac in vivo and in vitro. Eur J Clin Pharmacol 2001 57 : 729 735.
29. Parkinson A, Mudra DR, Johnson C, Dwyer A, Carroll KM. The effects of gender, age, ethnicity, and liver cirrhosis on cytochrome P450 enzyme activity in human liver microsomes and inducibility in cultured human hepatocytes. Toxicol Appl Pharmacol 2004 199 : 193 209.
30. Kirchheiner J, Kudlicz D, Meisel C, Bauer S, Meineke I, Roots I et al. Influence of CYP2C9 polymorphisms on the pharmacokinetics and cholesterol-lowering activity of (-)-3S,5R-fluvastatin and (+)-3R,5S-fluvastatin in healthy volunteers. Clin Pharmacol Ther 2003 74 : 186 194.