Metabolism of cerivastatin by human liver microsomes in vitro: Characterization of primary metabolic pathways and of cytochrome P450 isozymes involved

Drug Metabolism and Disposition

Volumn 25, Issue 3, 1997, Pages 321-331

  Boberg, Michael ^a   Angerbauer, Rolf ^b   Fey, Peter ^b   Kanhai, Wolfgang K ^b   Karl, Wolfgang ^b   Kern, Armin ^b   Ploschke, Jürgen ^b   Radtke, Martin ^b  

^a BAYER AG   (Germany)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

CERIVASTATIN; CYTOCHROME P450; DRUG METABOLITE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR;

ARTICLE; CONTROLLED STUDY; DRUG ISOLATION; DRUG METABOLISM; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TRANSFORMATION; ENZYME POLYMORPHISM; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HYPERCHOLESTEROLEMIA; LIVER MICROSOME; PRIORITY JOURNAL;

ANTICHOLESTEREMIC AGENTS; CYTOCHROME P-450 ENZYME SYSTEM; ENZYME INHIBITORS; HUMANS; ISOENZYMES; MAGNETIC RESONANCE SPECTROSCOPY; MASS SPECTROMETRY; MICROSOMES, LIVER; MIXED FUNCTION OXYGENASES; OXIDATION-REDUCTION; PYRIDINES; SUBSTRATE SPECIFICITY;

STAPHYLOCOCCUS PHAGE 3A;

EID: 0030893455     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (6)

1. R. Angerbauer, H. Bischoff, W. Steinke, and W. Ritter: BAY w 6228. Drugs Fut. 19, 537-541 (1994).
2. R. Angerbauer, P. Fey, W. Huebsch, T. Philipps, H. Bischoff, D. Petzinna, D. Schmidt, and G. Thomas: Substituted pyridyl-dihydroxy-heptenoic acid and its salts. US-5,177,080 (1993).
3. C. L. Crespi, and W. G. Thilly: Assay for gene mutation in a human lymphoblast line, AHH-1, competent for xenobiotic metabolism. Mutat. Res. 128, 221-230 (1984).
4. R. W. Wang, P. H. Kari, A. Y. H. Lu, P. E. Thomas, F. P. Guengerich, and K. P. Vyas: Biotransformation of lovastatin IV. Identification of CYP450 3A proteins as the major enzymes responsible for the oxidative metabolism of lovastatin in rat and human liver microsomes. Arch. Biochem. Biophys. 290, 355 (1991).
5. D. J. Newton, R. W. Wang, and A. Y. H. Lu: Cytochrome P450 inhibitors; evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metab. Dispos. 23, 154-158 (1995).
6. R. J. Clay, T. A. Collom, G. L. Karrick, and J. Wemple: A safe, economical method for the preparation of β-oxo esters. Synthesis 290, (1993).