System-dependent outcomes during the evaluation of drug candidates as inhibitors of cytochrome P450 (CYP) and uridine diphosphate glucuronosyltransferase (UGT) enzymes: Human hepatocytes versus liver microsomes versus recombinant enzymes

Drug Metabolism and Pharmacokinetics

Volumn 25, Issue 1, 2010, Pages 16-27

  Parkinson, Andrew ^a   Kazmi, Faraz ^a   Buckley, David B ^a   Yerino, Phyllis ^a   Ogilvie, Brian W ^a   Paris, Brandy L ^a  

^a XenoTech LLC   (United States)

Author keywords

Cell; Cytochrome P450; Drug; Hepatocytes; Inhibition; Microsomes; Organelle; UDP glucuronosyltransferase; Xenobiotics

Indexed keywords

AMFEBUTAMONE; AMIODARONE; ASTEMIZOLE; CERIVASTATIN; CISAPRIDE; CYTOCHROME P450; CYTOCHROME P450 2C19; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; DESIPRAMINE; DEXTROMETHORPHAN; DIAZEPAM; EZETIMIBE; EZETIMIBE PLUS SIMVASTATIN; FLUOXETINE; GEMFIBROZIL; GLUCURONOSYLTRANSFERASE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; KETOCONAZOLE; MIBEFRADIL; OMEPRAZOLE; PIOGLITAZONE; RECOMBINANT ENZYME; REPAGLINIDE; ROSIGLITAZONE; SIMVASTATIN; STATIN; TERFENADINE; UNINDEXED DRUG; VENLAFAXINE;

AREA UNDER THE CURVE; CARDIOTOXICITY; DRUG ACTIVITY; DRUG ANTAGONISM; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG METABOLISM; DRUG POTENCY; DRUG POTENTIATION; DRUG STRUCTURE; DRUG TRANSPORT; DRUG WITHDRAWAL; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME METABOLISM; GLUCURONIDATION; HUMAN; HYDROXYLATION; IC 50; IN VITRO STUDY; KIDNEY FAILURE; LIVER CELL; LIVER MICROSOME; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; QT PROLONGATION; REVIEW; RHABDOMYOLYSIS;

EID: 77949285974     PISSN: 13474367     EISSN: 18800920     Source Type: Journal    
DOI: 10.2133/dmpk.25.16     Document Type: Review

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