Use of in vitro human metabolism studies in drug development. An industrial perspective.

[1]  M. Grant,et al.  Human adult hepatocytes in primary monolayer culture. Maintenance of mixed function oxidase and conjugation pathways of drug metabolism. , 1987, Biochemical pharmacology.

[2]  F. Guengerich,et al.  Metabolism of N-nitrosodialkylamines by human liver microsomes. , 1988, Cancer research.

[3]  S. H. Chiu.  The use of in vitro metabolism studies in the understanding of new drugs. , 1993, Journal of pharmacological and toxicological methods.

[4]  J. Rothuizen,et al.  A species comparison of tolbutamide metabolism in precision-cut liver slices from rats and dogs. Qualitative and quantitative sex differences. , 1993, Drug metabolism and disposition: the biological fate of chemicals.

[5]  A. Vickers,et al.  Cyclosporin A metabolism in human liver, kidney, and intestine slices. Comparison to rat and dog slices and human cell lines. , 1992, Drug metabolism and disposition: the biological fate of chemicals.

[6]  B. Burchell,et al.  Validation and use of cloned, expressed human drug-metabolizing enzymes in heterologous cells for analysis of drug metabolism and drug-drug interactions. , 1993, Biochemical pharmacology.

[7]  F. Gonzalez,et al.  Human cytochromes P450: problems and prospects. , 1992, Trends in pharmacological sciences.

[8]  M. J. Coon,et al.  The P450 superfamily: update on new sequences, gene mapping, accession numbers, early trivial names of enzymes, and nomenclature. , 1993, DNA and cell biology.

[9]  D Lalka,et al.  The Hepatic First‐Pass Metabolism of Problematic Drugs , 1993, Journal of clinical pharmacology.

[10]  F. Gonzalez,et al.  DNA-expressed human cytochrome P450s: a new age of molecular toxicology and human risk assessment. , 1991, Mutation research.

[11]  M. Butler,et al.  Human cytochrome P-450PA (P-450IA2), the phenacetin O-deethylase, is primarily responsible for the hepatic 3-demethylation of caffeine and N-oxidation of carcinogenic arylamines. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[12]  M. Jackson,et al.  Development of human liver UDP-glucuronosyltransferases. , 1989, Developmental pharmacology and therapeutics.

[13]  A. Boobis,et al.  Furafylline is a potent and selective inhibitor of cytochrome P450IA2 in man. , 1990, British journal of clinical pharmacology.

[14]  P. Beaune,et al.  Hydroxylation of chlorzoxazone as a specific probe for human liver cytochrome P-450IIE1 , 1990 .

[15]  F. Guengerich,et al.  Oxidation of the antihistaminic drug terfenadine in human liver microsomes. Role of cytochrome P-450 3A(4) in N-dealkylation and C-hydroxylation. , 1993, Drug metabolism and disposition: the biological fate of chemicals.

[16]  A. Parkinson,et al.  Species differences and interindividual variation in liver microsomal cytochrome P450 2A enzymes: effects on coumarin, dicumarol, and testosterone oxidation. , 1992, Archives of biochemistry and biophysics.

[17]  M. Gibaldi.  Stereoselective and isozyme-selective drug interactions. , 1993, Chirality.

[18]  Iwata Nobuhisa,et al.  Interindividual variability of carbonyl reductase levels in human livers , 1993 .

[19]  R. Tukey,et al.  Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. , 1993, The Journal of pharmacology and experimental therapeutics.

[20]  D. Ziegler,et al.  Dimethylaniline N-oxidase and aminopyrine N-demethylase activities of human liver tissue. , 1973, Xenobiotica; the fate of foreign compounds in biological systems.

[21]  G. Siest,et al.  The UDP glucuronosyltransferase gene superfamily: suggested nomenclature based on evolutionary divergence. , 1991, DNA and cell biology.

[22]  J. Idle,et al.  The role of individual human cytochromes P450 in drug metabolism and clinical response. , 1992, Trends in pharmacological sciences.

[23]  D A Smith,et al.  Speculations on the substrate structure-activity relationship (SSAR) of cytochrome P450 enzymes. , 1992, Biochemical pharmacology.

[24]  F. Guengerich,et al.  Oxidation of quinidine by human liver cytochrome P-450. , 1986, Molecular pharmacology.

[25]  E. Vesell,et al.  Metabolism of nicotine. , 1991, Drug metabolism reviews.

[26]  C. Wolf,et al.  The effects of inducing agents on cytochrome P450 and UDP-glucuronyltransferase activities in human HEPG2 hepatoma cells. , 1993, Biochemical pharmacology.

[27]  T. Aoyama,et al.  Hydroxylation of warfarin by human cDNA-expressed cytochrome P-450: a role for P-4502C9 in the etiology of (S)-warfarin-drug interactions. , 1992, Chemical research in toxicology.

[28]  S. Wrighton,et al.  Two monoclonal antibodies recognizing different epitopes on rat cytochrome IIB1 react with human IIE1. , 1992, Molecular pharmacology.

[29]  M. B. Grivell,et al.  Techniques for pharmacological and toxicological studies with isolated hepatocyte suspensions. , 1992, Life sciences.

[30]  B. Burchell,et al.  The expression of UDP-glucuronosyltransferases of the UGT1 family in human liver and kidney and in response to drugs. , 1993, Biochemical pharmacology.

[31]  D. Weiner,et al.  Bioavailability of terfenadine in man. , 1981, Biopharmaceutics & drug disposition.

[32]  A. Guillouzo,et al.  Cultured human adult hepatocytes: a new model for drug metabolism studies. , 1983, Biochemical pharmacology.

[33]  A. Guillouzo,et al.  Species differences in metabolism of ketotifen in rat, rabbit and man: demonstration of similar pathways in vivo and in cultured hepatocytes. , 1987, Life sciences.

[34]  P. Maurel,et al.  Omeprazole is an aryl hydrocarbon-like inducer of human hepatic cytochrome P450. , 1990, Gastroenterology.

[35]  D. Wortham,et al.  Terfenadine-ketoconazole interaction. Pharmacokinetic and electrocardiographic consequences. , 1993, JAMA.

[36]  A. D. Rodrigues,et al.  Measurement of liver microsomal cytochrome p450 (CYP2D6) activity using [O-methyl-14C]dextromethorphan. , 1994, Analytical biochemistry.

[37]  M. Grant,et al.  Cryopreservation of human adult hepatocytes for use in drug metabolism and toxicity studies. , 1993, Xenobiotica; the fate of foreign compounds in biological systems.

[38]  I. Sipes,et al.  Liver slices in dynamic organ culture. I. An alternative in vitro technique for the study of rat hepatic drug metabolism. , 1991, Xenobiotica; the fate of foreign compounds in biological systems.

[39]  R. Temple.  Trends in Pharmaceutical Development , 1993 .

[40]  A. Breckenridge,et al.  Clinical Implications of Enzyme Induction and Enzyme Inhibition , 1981, Clinical pharmacokinetics.

[41]  G. Powis,et al.  Human and dog, but not rat, isolated hepatocytes have decreased foreign compound-metabolizing activity compared to liver slices. , 1989, Drug metabolism and disposition: the biological fate of chemicals.

[42]  M. T. Donato,et al.  Effect of xenobiotics on monooxygenase activities in cultured human hepatocytes. , 1990, Biochemical pharmacology.

[43]  S. Emiliani,et al.  Isolation and characterization of a cytochrome P450 of the IIA subfamily from human liver microsomes. , 1991, European journal of biochemistry.

[44]  D. Johns.  Human liver aldehyde oxidase: differential inhibition of oxidation of charged and uncharged substrates. , 1967, The Journal of clinical investigation.

[45]  G. Powis.  The use of human liver for foreign compound metabolism and toxicity studies. , 1989, Drug metabolism reviews.

[46]  D. Grant,et al.  Biotransformation of caffeine, paraxanthine, theophylline, and theobromine by polycyclic aromatic hydrocarbon-inducible cytochrome(s) P-450 in human liver microsomes. , 1987, Drug metabolism and disposition: the biological fate of chemicals.

[47]  J. Miners,et al.  In vitro approaches can predict human drug metabolism. , 1993, Trends in pharmacological sciences.

[48]  T. Shimada,et al.  Human liver microsomal cytochrome P-450 enzymes involved in the bioactivation of procarcinogens detected by umu gene response in Salmonella typhimurium TA 1535/pSK1002. , 1989, Cancer research.

[49]  A. Guillouzo,et al.  Maintenance of cytochrome P-450 in cultured adult human hepatocytes. , 1985, Biochemical pharmacology.

[50]  S. Wrighton,et al.  The human hepatic cytochromes P450 involved in drug metabolism. , 1992, Critical reviews in toxicology.

[51]  H. Yamazaki,et al.  Characterization of cytochrome P-450 2B6 in human liver microsomes. , 1993, Drug metabolism and disposition: the biological fate of chemicals.

[52]  C. Krumdieck,et al.  A new instrument for the rapid preparation of tissue slices. , 1980, Analytical biochemistry.

[53]  P. Maurel,et al.  Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes. , 1990, Drug metabolism and disposition: the biological fate of chemicals.

[54]  F. Guengerich.  Characterization of human cytochrome P450 enzymes , 1992, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[55]  T. Kronbach,et al.  High-performance liquid chromatographic assays for bufuralol 1'-hydroxylase, debrisoquine 4-hydroxylase, and dextromethorphan O-demethylase in microsomes and purified cytochrome P-450 isozymes of human liver. , 1987, Analytical biochemistry.

[56]  O. Pelkonen,et al.  Inhibition of human hepatic and placental xenobiotic monooxygenases by imidazole antimycotics. , 1988, Biochemical pharmacology.

[57]  C. Hunt,et al.  Effect of age and gender on the activity of human hepatic CYP3A. , 1992, Biochemical pharmacology.

[58]  E. Sellers,et al.  Inhibition by fluoxetine of cytochrome P450 2D6 activity , 1993, Clinical pharmacology and therapeutics.

[59]  P. Dogterom.  Development of a simple incubation system for metabolism studies with precision-cut liver slices. , 1993, Drug metabolism and disposition: the biological fate of chemicals.

[60]  J. S. Miles,et al.  Relative expression of cytochrome P450 isoenzymes in human liver and association with the metabolism of drugs and xenobiotics. , 1992, The Biochemical journal.

[61]  W. Trager,et al.  Isoform-selective mechanism-based inhibition of human cytochrome P450 1A2 by furafylline. , 1993, Chemical research in toxicology.

[62]  R. Woosley,et al.  Changes in the pharmacokinetics and electrocardiographic pharmacodynamics of terfenadine with concomitant administration of erythromycin , 1992, Clinical pharmacology and therapeutics.

[63]  P. Maurel,et al.  Effects of imidazole derivatives on cytochromes P450 from human hepatocytes in primary culture , 1992, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[64]  B J Blaauboer,et al.  Comparison of cytochrome P450 isoenzyme profiles in rat liver and hepatocyte cultures. The effects of model inducers on apoproteins and biotransformation activities. , 1991, Biochemical pharmacology.

[65]  O. Fardel,et al.  Use of human hepatocyte cultures for drug metabolism studies. , 1993, Toxicology.

[66]  A. J. Gandolfi,et al.  Tissue slicing and culturing revisited , 1987 .

[67]  Tucker Gt,et al.  The rational selection of drug interaction studies: implications of recent advances in drug metabolism. , 1992 .

[68]  A. Guillouzo,et al.  Effects of various inducers on the expression of cytochromes P-450 IIC8, 9, 10 and IIIA in cultured adult human hepatocytes. , 1990, Toxicology in vitro : an international journal published in association with BIBRA.

[69]  M. Gibaldi,et al.  Characteristics of warfarin hydroxylation catalyzed by human liver microsomes. , 1989, Drug metabolism and disposition: the biological fate of chemicals.

[70]  R Temple,et al.  Understanding consequences of concurrent therapies. , 1993, JAMA.

[71]  U. Meyer,et al.  Polymorphic formation of morphine from codeine in poor and extensive metabolizers of dextromethorphan: Relationship to the presence of immunoidentified cytochrome P‐450IID1 , 1990, Clinical pharmacology and therapeutics.

[72]  F. Guengerich,et al.  Role of human cytochrome P-450 IIE1 in the oxidation of many low molecular weight cancer suspects. , 1991, Chemical research in toxicology.

[73]  A. Okey.  Enzyme induction in the cytochrome P-450 system. , 1990, Pharmacology & therapeutics.

[74]  M. Barry,et al.  Enzyme induction and inhibition. , 1990, Pharmacology & therapeutics.

[75]  C. Fenselau,et al.  Species-dependent glucuronidation of drugs by immobilized rabbit, rhesus monkey, and human UDP-glucuronyltransferases. , 1987, Drug metabolism and disposition: the biological fate of chemicals.

[76]  J. Miners,et al.  Relationship between phenytoin and tolbutamide hydroxylations in human liver microsomes. , 1991, British journal of clinical pharmacology.

[77]  J. Miners,et al.  Tolbutamide hydroxylation by human liver microsomes. Kinetic characterisation and relationship to other cytochrome P-450 dependent xenobiotic oxidations. , 1988, Biochemical pharmacology.

[78]  R. Chenery,et al.  Comparative drug metabolism of diazepam in hepatocytes isolated from man, rat, monkey and dog. , 1989, Biochemical pharmacology.

[79]  E. Kharasch,et al.  Human liver microsomal enflurane defluorination catalyzed by cytochrome P-450 2E1. , 1993, Drug metabolism and disposition: the biological fate of chemicals.

[80]  H. Yamazaki,et al.  Cytochrome P450 2E1 and 2A6 enzymes as major catalysts for metabolic activation of N-nitrosodialkylamines and tobacco-related nitrosamines in human liver microsomes. , 1992, Carcinogenesis.