PREDICTING PHARMACOKINETICS AND DRUG INTERACTIONS IN PATIENTS FROM IN VITRO AND IN VIVO MODELS: THE EXPERIENCE WITH 5,6-DIMETHYLXANTHENONE-4-ACETIC ACID (DMXAA), AN ANTI-CANCER DRUG ELIMINATED MAINLY BY CONJUGATION

REFERENCES

• Li A.P. Screening for Human ADME/Tox Drug Properties in Drug Discovery. Drug Discov. Today 2001; 6: 357–366
   PubMed Web of Science ®Google Scholar
• Eddershaw P.J., Beresford A.P., Bayliss M.K. ADME/PK as Part of a Rational Approach to Drug Discovery. Drug Discov. Today 2000; 5: 409–414
   PubMed Web of Science ®Google Scholar
• Kennedy T. Managing the Drug Discovery/Development Interface. Drug Discov. Today 1997; 2: 436–444
   Web of Science ®Google Scholar
• Prentis R.A., Lis Y., Walker S.R. Pharmaceutical Innovation by the Seven UK-Owned Pharmaceutical Companies (1964–1985). Br. J. Clin. Pharmacol. 1988; 25: 387–396
   PubMed Web of Science ®Google Scholar
• Collins J.M. Inter-species Differences in Drug Properties. Chem.-Biol. Interact. 2001; 134: 237–242
   PubMed Web of Science ®Google Scholar
• Lin J.H., Lu A.Y.H. Role of Pharmacokinetics and Metabolism in Drug Discovery and Development. Pharmacol. Rev. 1997; 49: 403–449
   PubMed Web of Science ®Google Scholar
• Rodrigues A.D. Use of In Vitro Human Metabolism Studies in Drug Development. Biochem. Pharmacol. 1994; 48: 2147–2156
   PubMed Web of Science ®Google Scholar
• Eddershaw P.J., Dickins M. Advances in In Vitro Drug Metabolism Screening. Pharm. Sci. Technol. Today 1999; 2: 13–19
   PubMedGoogle Scholar
• Streetman D.S., Bertino J.S., Nafziger A.N. Phenotyping of Drug-Metabolizing Enzymes in Adults: A Review of In-Vivo Cytochrome P450 Phenotyping Probes. Pharmacogenetics 2000; 10: 187–216
   PubMedGoogle Scholar
• Lin J.H. Applications and Limitations of Interspecies Scaling and In Vitro Extrapolation in Pharmacokinetics. Drug Metab. Dispos. 1998; 26: 1202–1212
   PubMed Web of Science ®Google Scholar
• Boxenbaum H. Interspecies Variation in Liver Weight, Hepatic Weight, Hepatic Flow and Antipyrine Intrinsic Clearance in Extrapolation of Data to Benzodiazepines and Phenytoin. J. Pharmacokinet. Biopharm. 1980; 8: 165–176
   PubMedGoogle Scholar
• Balant L.P., Gex-Fabry M. Physiological Pharmacokinetic Modelling. Xenobiotica 1990; 20: 1241–1257
   PubMed Web of Science ®Google Scholar
• Houston J.B. Utility of In Vitro Drug Metabolism Data in Predicting In Vivo Metabolic Clearance. Biochem. Pharmacol. 1994; 47: 1469–1479
   PubMed Web of Science ®Google Scholar
• Obach R.S. Metabolism of Ezlopitant, a Nonpeptidic Substance P Receptor Antagonist, in Liver Microsomes: Enzyme Kinetics, Cytochrome P450 Isoform Identity, and In Vitro–In Vivo Correlation. Drug Metab. Dispos. 2000; 28: 1069–1076
   PubMed Web of Science ®Google Scholar
• Faed E.M. Properties of Acyl Glucuronide: Implications for Studies of the Pharmacokinetics and Metabolism of Acidic Drugs. Drug Metab. Rev. 1984; 15: 1213–1249
   PubMed Web of Science ®Google Scholar
• Radominska-Pandya A., Czernik P.J., Little J.M., Battaglia E., Mackenzie P.I. Structural and Functional Studies of UDP-Glucuronosyltransferases. Drug Metab. Rev. 1999; 31: 817–899
   PubMed Web of Science ®Google Scholar
• Kerr D.J., Kaye S.B. Flavone Acetic Acid Preclinical and Clinical Activity. Eur. J. Cancer Clin. Oncol. 1989; 25: 1271–1272
   PubMedGoogle Scholar
• Pang J.H., Cao Z., Joseph W.R., Baguley B.C., Ching L.-M. Antitumour Activity of the Novel Immune Modulator 5,6-Dimethylxanthenone-4-acetic Acid (DMXAA) in Mice Lacking the Interferon-Gamma Receptor. Eur. J. Cancer 1998; 34: 1282–1289
   PubMed Web of Science ®Google Scholar
• Thomsen L.L., Ching L.-M., Baguley B.C. Evidence for the Production of Nitric Oxide by Activated Macrophages Treated with the Antitumor Agents Flavone-8-acetic Acid and Xanthenone-4-acetic Acid. Cancer Res. 1990; 50: 6966–6970
   PubMed Web of Science ®Google Scholar
• Thomsen L.L., Ching L.-M., Zhuang L., Gavin J.B., Baguley B.C. Tumor-Dependent Increased Plasma Nitrate Concentrations as an Indication of the Antitumor Effect of Flavone-8-acetic Acid and Analogues in Mice. Cancer Res. 1991; 51: 77–81
   PubMed Web of Science ®Google Scholar
• Philpott M., Baguley B.C., Ching L.-M. Induction of Tumour Necrosis Factor-Alpha by Single and Repeated Doses of the Antitumour Agent 5,6-Dimethylxanthenone-4-acetic Acid. Cancer Chemother. Pharmacol. 1995; 36: 143–148
   PubMed Web of Science ®Google Scholar
• Ching L.-M., Baguley B.C. Enhancement of In Vitro Cytotoxicity of Mouse Peritoneal Exudate Cells by Flavone Acetic Acid (NSC 347512). Eur. J. Cancer Clin. Oncol. 1988; 24: 1521–1525
   PubMedGoogle Scholar
• Ching L.-M., Baguley B.C. Effect of Flavone Acetic Acid (NSC 347,512) on Splenic Cytotoxic Effector cells and Their Role in Tumour Necrosis. Eur. J. Cancer Clin. Oncol. 1989; 25: 821–828
   PubMedGoogle Scholar
• Zwi L.J., Baguley B.C., Gavin J.B., Wilson W.R. Blood Flow Failure as a Major Determinant in the Antitumor Action of Flavone Acetic Acid (NSC 347512). J. Natl Cancer Inst. 1989; 81: 1005–1013
   PubMed Web of Science ®Google Scholar
• Zwi L.J., Baguley B.C., Gavin J.B., Wilson W.R. Correlation Between Immune and Vascular Activities of Xanthenone Acetic Acid on Tumour Agents. Oncol. Res. 1994; 6: 79–85
   PubMed Web of Science ®Google Scholar
• Bibby M.C., Double J.A., Loadman P.M., Duke C.V. Reduction of Tumor Blood Flow by Flavone Acetic Acid: A Possible Component of Therapy. J. Natl Cancer Inst. 1989; 81: 216–220
   PubMed Web of Science ®Google Scholar
• Bibby M.C., Phillips R.M., Double J.A., Pratesi G. Anti-tumor Activity of Flavone Acetic Acid (NSC-347512) in Mice—Influence of Immune Status. Br. J. Cancer 1991; 63: 57–62
   PubMed Web of Science ®Google Scholar
• Ching L.-M., McKeage M.J., Joseph W.R., Kestell P., Zwi L.J., Baguley B.C. Haematological Effects in Mice of the Antitumour Agents Xanthenone-4-acetic Acid, 5,6-Dimethyl-xanthenone-4-acetic Acid and Flavone Acetic Acid. Cancer Chemother. Pharmacol. 1991; 28: 414–419
   PubMedGoogle Scholar
• Gram T.E., Okine L.K., Gram R.A. The Metabolism of Xenobiotics by Certain Extrahepatic Organs and Its Relation to Toxicity. Annu. Rev. Pharmacol. Toxicol. 1986; 26: 259–292
   PubMed Web of Science ®Google Scholar
• Krishna D.R., Klotz U. Extrahepatic Metabolism of Drugs in Humans. Clin. Pharmacokinet. 1994; 26: 144–160
   PubMed Web of Science ®Google Scholar
• Lohr J.W., Willsky G.R., Acara M.A. Renal Drug Metabolism. Pharmacol. Rev. 1998; 50: 107–141
   PubMed Web of Science ®Google Scholar
• Kroemer H.K., Klotz U. Glucuronidation of Drugs: A Re-evaluation of the Pharmacological Significance of the Conjugates and Modulation Factors. Clin. Pharmacokinet. 1992; 23: 292–310
   PubMed Web of Science ®Google Scholar
• Meech R., Mackenzie P.I. Structure and Function of Uridine Diphosphate Glucuronosyltransferases. Clin. Exp. Pharmacol. Physiol. 1997; 24: 907–915
   PubMed Web of Science ®Google Scholar
• Rendic S., Di Carlo F.J. Human Cytochrome P450 Enzyme: A Status Report Summarizing Their Reactions, Substrates, Induction, and Inhibitors. Drug Metab. Rev. 1997; 29: 413–580
   PubMed Web of Science ®Google Scholar
• Burchell B., Brierley C.H., Monaghan G., Clarke D.J. The Structure and Function of the UDP-Glucuronosyltransferase Gene Family. Adv. Pharmacol. 1998; 42: 335–338
   PubMedGoogle Scholar
• Tukey R.H., Strassburg C.P. Human UDP-Glucuronosyltransferases: Metabolism, Expression, and Disease. Annu. Rev. Pharmacol. Toxicol. 2000; 40: 581–616
   PubMed Web of Science ®Google Scholar
• Shimada T., Yamazaki H., Mimura M., Inui Y., Guengerich F.P. Interindividual Variations in Human Liver Cytochrome P450 Enzymes Involved in the Oxidation of Drugs, Carcinogens and Toxic Chemicals. J. Pharmacol. Exp. Ther. 1994; 270: 414–423
   PubMed Web of Science ®Google Scholar
• Bertz R.J., Granneman G.R. Use of In Vitro and In Vivo Data to Estimate the Likelihood of Metabolic Pharmacokinetic Interactions. Clin. Pharmacokinet. 1997; 32: 210–258
   PubMed Web of Science ®Google Scholar
• Kivisto K.T., Kroemer H.K., Eichelbaum M. The Role of Human Cytochrome P450 Enzymes in the Metabolism of Anticancer Agents—Implications for Drug Interactions. Br. J. Clin. Pharmacol. 1995; 40: 523–530
   PubMed Web of Science ®Google Scholar
• Crommentuyn K.M.L., Schellens J.H.M., Vandenberg J.D., Beijnen J.H. In-Vitro Metabolism of Anti-cancer Drugs, Methods and Applications—Paclitaxel, Docetaxel, Tamoxifen and Ifosfamide. Cancer Treat. Rev. 1998; 24: 345–366
   PubMed Web of Science ®Google Scholar
• Kamataki T., Yokoi T., Fujita K., Ando Y. Preclinical Approach for Identifying Drug Interactions. Cancer Chemother. Pharmacol. 1998; 42(Suppl.)S50–S53
   PubMedGoogle Scholar
• Huang Z.Q., Roy P., Waxman D.J. Role of Human Liver Microsomal CYP3A4 and CYP2B6 in Catalyzing N-dechloroethylation of Cyclophosphamide and Ifosfamide. Biochem. Pharmacol. 2000; 59: 961–972
   PubMed Web of Science ®Google Scholar
• Iyer L. Inherited Variations in Drug-Metabolizing Enzymes: Significance in Clinical Oncology. Mol. Diagn. 1999; 4: 327–333
   PubMedGoogle Scholar
• Tanaka E. Update: Genetic Polymorphism of Drug Metabolizing Enzymes in Humans. J. Clin. Pharm. Ther. 1999; 24: 323–329
   PubMed Web of Science ®Google Scholar
• Han X.M., Zhou H.H. Polymorphism of CYP450 and Cancer Susceptibility. Acta Pharmacol. Sin. 2000; 21: 673–679
   PubMed Web of Science ®Google Scholar
• Wormhoudt L.W., Commandeur J.N.M., Vermeulen N.P.E. Genetic Polymorphisms of Human N-Acetyltransferase, Cytochrome P450, Glutathione-S-transferase, and Epoxide Hydrolase Enzymes: Relevance to Xenobiotic Metabolism and Toxicity. Crit. Rev. Toxicol. 1999; 29: 59–124
   PubMed Web of Science ®Google Scholar
• Snyder R. Microsomal Enzyme Induction. Toxicol. Sci. 2000; 55: 233–234
   PubMed Web of Science ®Google Scholar
• Pelkonen O., Maenpaa J., Taavitsainen P., Rautio A., Raunio H. Inhibition and Induction of Human Cytochrome P450 (CYP) Enzymes. Xenobiotica 1998; 28: 1203–1253
   PubMed Web of Science ®Google Scholar
• Dresser G.K., Spence J.D., Bailey D.G. Pharmacokinetic–Pharmacodynamic Consequences and Clinical Relevance of Cytochrome P450 3A4 Inhibition. Clin. Pharmacokinet. 2000; 38: 41–57
   PubMed Web of Science ®Google Scholar
• Lin J.H., Lu A.Y. Interindividual Variability in Inhibition and Induction of Cytochrome P450 Enzymes. Annu. Rev. Pharmacol. Toxicol. 2001; 41: 535–567
   PubMed Web of Science ®Google Scholar
• Kestell P., Rewcastle G.W., Baguley B.C. Disposition of the Novel Antitumour Agent Xanthenone-4-acetic Acid in the Mouse: Identification of Metabolites and Routes of Elimination. Xenobiotica 1994; 24: 635–647
   PubMed Web of Science ®Google Scholar
• Cummings J., Double J.A., Bibby M.C., Farmer P., Evens S., Kerr D.J., Kaye S.B., Smyth J.F. Characterization of the Major Metabolites of Flavone Acetic Acid and Comparison of Their Disposition in Humans and Mice. Cancer Res. 1989; 49: 3587–3593
   PubMed Web of Science ®Google Scholar
• Webster L.K., Ellis A.G., Kestell P., Rewcastle G.W. Metabolism and Elimination of 5,6-Dimethylxanthenone-4-acetic Acid in the Isolated Perfused Rat Liver. Drug Metab. Dispos. 1995; 23: 363–368
   PubMed Web of Science ®Google Scholar
• Zhou S.F., Paxton J.W., Tingle M.D., McCall J., Kestell P. Determinaton of Two Major Metabolites of the Novel Anti-tumour Agent 5,6-Dimethylxanthenone-4-acetic acid in Hepatic Microsomal Incubations by High-Performance Liquid Chromatography with Fluorescence Detection. J. Chromatogr. B 1999; 734: 129–136
   PubMedGoogle Scholar
• Zhou S.F., Paxton J.W., Tingle M.D., Kestell P. Species Differences in the Metabolism and Inhibition of the Novel Antitumour Agent 5,6-Dimethylxanthenone-4-acetic Acid In Vitro: Implications for Prediction of Metabolic Interactions and Toxicity In Vivo. Xenobiotica 2002; 32: 87–107
   PubMed Web of Science ®Google Scholar
• Sallustio B.C., Purdie Y.J., Birkett D.J., Meffin P.J. Effect of Renal Dysfunction on the Individual Components of the Acyl-Glucuronide Futile Cycle. J. Pharmacol. Exp. Ther. 1989; 251: 288–294
   PubMed Web of Science ®Google Scholar
• Yue Q., von Bahr C., Odar-Cederlof I., Sawe J. Glucuronidation of Codeine and Morphine in Human Liver and Kidney Microsomes: Effect of Inhibitors. Pharmacol. Toxicol. 1990; 66: 221–226
   PubMedGoogle Scholar
• Brunelle F.M., Verbeeck R.K. Glucuronidation of Diflunisal in Liver and Kidney Microsomes of Rat and Man. Xenobiotica 1996; 26: 123–131
   PubMed Web of Science ®Google Scholar
• McGurk K.A., Brierley C.H., Burchell B. Drug Glucuronidation by Human Renal UDP-Glucuronosyltransferases. Biochem. Pharmacol. 1998; 55: 1005–1012
   PubMed Web of Science ®Google Scholar
• Davidson I.W.F., Parker J.C., Beliles R.P. Biological Basis for Extrapolation Across Mammalian Species. Regul. Toxicol. Pharmacol. 1986; 6: 211–237
   PubMed Web of Science ®Google Scholar
• Wong K.P. Measurement of Nanogram Quantities of UDP-Glucuronic acid in Tissues. Anal. Biochem. 1977; 82: 559–563
   PubMed Web of Science ®Google Scholar
• Cappiello M., Giuliani L., Pacifici G.M. Distribution of UDP-Glucuronosyltransferase and Its Endogenous Substrate Uridine 5′-Diphosphoglucuronic Acid in Human Tissues. Eur. J. Clin. Pharmacol. 1991; 41: 345–350
   PubMed Web of Science ®Google Scholar
• Kestell P., Paxton J.W., Rewcastle G.W., Dunlop I., Baguley B.C. Plasma Disposition, Metabolism and Excretion of the Experimental Antitumour Agent 5,6-Dimethylxanthenone-4-acetic Acid in the Mouse, Rat and Rabbit. Cancer Chemother. Pharmacol. 1999; 43: 323–330
   PubMed Web of Science ®Google Scholar
• Zhou S.F., Paxton J.W., Tingle M.D., Kestell P., Jameson M.B., Thomson P.I., Baguley B.C. Identification and Reactivity of the Major Metabolite (b-1-Glucuronide) of the Anti-tumour Agent 5,6-Dimethylxanthenone-4-acetic Acid (DMXAA) in Humans. Xenobiotica 2001; 31: 277–293
   PubMed Web of Science ®Google Scholar
• Zhou S.F., Paxton J.W., Tingle M.D., Kestell P. Identification of the Human Liver Cytochrome P450 Isozyme Responsible for the 6-Methylhydroxylation of the Novel Anticancer Drug 5,6-Dimethylxanthenone-4-acetic Acid. Drug Metab. Dispos. 2000; 28: 1449–1456
   PubMed Web of Science ®Google Scholar
• Miners J.O., Valente L., Lillywhite K.J., Mackenzie P.I., Burchell B., Baguley B.C., Kestell P. Preclinical Prediction of Factors Influencing the Elimination of 5,6-Dimethylxanthenone-4-acetic Acid, a New Anticancer Drug. Cancer Res. 1997; 57: 284–289
   PubMed Web of Science ®Google Scholar
• Burchell B., Brierley C.H., Rance D. Specificity of Human UDP-Glucuronosyl-Transferases and Xenobiotic Glucuronidation. Life Sci. 1995; 57: 1818–1831
   Google Scholar
• King C., Tang W., Ngui J., Tephly T., Braun M. Characterization of Rat and Human UDP-Glucuronosyltransferases Responsible for the In Vitro Glucuronidation of Diclofenac. Toxicol. Sci. 2001; 61: 49–53
   PubMed Web of Science ®Google Scholar
• Coffman B.L., Rios G.R., King C.D., Tephly T.R. Human UGT2B7 Catalyzes Morphine Glucuronidation. Drug Metab. Dispos. 1997; 25: 1–4
   PubMed Web of Science ®Google Scholar
• Innocenti F., Iyer L., Ramírez J., Green M.D., Ratain M.J. Epirubicin Glucuronidation Is Catalyzed by Human UDP-Glucuronosyltransferase 2B7. Drug Metab. Dispos. 2001; 29: 686–692
   PubMed Web of Science ®Google Scholar
• Ren Q., Murphy S.E., Zheng Z., Lazarus P. O-Glucuronidation of the Lung Carcinogen 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL) by Human UDP-Glucuronosyltransferases 2B7 and 1A9. Drug Metab. Dispos. 2000; 28: 1352–1360
   PubMed Web of Science ®Google Scholar
• Munzel P.A., Schmohl S., Heel H., Kalberer K., Bock-Hennig B.S., Bock K.W. Induction of Human UDP Glucuronosyltransferases (UGT1A6, UGT1A9, and UGT2B7) by t-Butylhydroquinone and 2,3,7,8-Tetrachlorodibenzo-p-dioxin in Caco-2 Cells. Drug Metab. Dispos. 1999; 27: 569–573
   PubMed Web of Science ®Google Scholar
• Mackenzie P.I., Miners J.O., McKinnon R.A. Polymorphisms in UDP Glucuronosyltransferase Genes: Functional Consequences and Clinical Relevance. Clin. Chem. Lab. Med. 2000; 38: 889–892
   PubMed Web of Science ®Google Scholar
• Raijmakers M.T.M., Jansen P.L.M., Steegers E.A.P., Peters W.H.M. Association of Human Liver Bilirubin UDP-Glucuronyltransferase Activity with a Polymorphism in the Promoter Region of the UGT1A1 Gene. J. Hepatol. 2000; 33: 348–351
   PubMed Web of Science ®Google Scholar
• Ciotti M., Marrone A., Potter C., Owens I.S. Genetic Polymorphism in the Human UGT1A6 (Planar Phenol) UDP-Glucuronosyltransferase—Pharmacological Implications. Pharmacogenetics 1997; 7: 485–495
   PubMedGoogle Scholar
• Levesque B., Beaulieu M., Hum D.W., Belanger A. Characterization and Substrate Specificity of UGT2B4 (E-458): A UDP-Glucuronosyltransferase Encoded by a Polymorphic Gene. Pharmacogenetics 1999; 9: 207–216
   PubMedGoogle Scholar
• Bhasker C.R., McKinnon W., Stone A., Lo A.C.T., Kubota T., Ishizaki T., Miners J.O. Genetic Polymorphism of UDP-Glucuronosyltransferase 2B7 (UGT2B7) at Amino Acid 268: Ethnic Diversity of Alleles and Potential Clinical Significance. Pharmacogenetics 2000; 10: 679–685
   PubMedGoogle Scholar
• Levesque E., Beaulieu M., Green M.D., Tephly T.R., Belanger A., Hum D.W. Isolation and Characterization of UGT2B15(Y-85)—A UDP-Glucuronosyltransferase Encoded by a Polymorphic Gene. Pharmacogenetics 1997; 7: 317–325
   PubMedGoogle Scholar
• Fisher M.B., VandenBranden M., Findlay K., Burchell B., Thummel K.E., Hall S.D., Wrighton S.A. Tissue Distribution and Interindividual Variation in Human UDP-Glucuronosyltransferase Activity: Relationship Between UGT1A1 Promoter Genotype and Variability in a Liver Bank. Pharmacogenetics 2000; 10: 727–739
   PubMedGoogle Scholar
• Jameson M.B., Thomson P.I., Baguley B.C., Evans B.D., Harvey V.J., McCrystal M.R., Kestell P. Phase I Pharmacokinetic and Pharmacodynamic Study of 5,6-Dimethylxanthenone-4-acetic Acid (DMXAA), a Novel Antivascular Agent. Proc. Annu. Meet. Am. Soc. Clin. Oncol. 2000; 19: 182
   Google Scholar
• Landi M.T., Sinha R., Lang N.P., Kadlubar F.F. Metabolic Polymorphisms and Susceptibility to Cancer, W. Ryder. IARC Scientific Publications, Lyon 1999; 173–195
   Google Scholar
• Miners J.O., Rees D.L.P., Valente L., Veronese M.E., Birkett D.J. Human Hepatic Cytochrome P450 2C9 Catalyzes the Rate-Limiting Pathway of Torsemide Metabolism. J. Pharmacol. Exp. Ther. 1995; 272: 1076–1081
   PubMed Web of Science ®Google Scholar
• Veronese M.E., Mackenzie P.I., Doecke C.J., McManus M.E., Miners J.O., Birkett D.J. Tolbutamide and Phenytoin Hydroxylation by cDNA-Expressed Human Liver Cytochrome P4502C9. Biochem. Biophys. Res. Commun. 1991; 175: 1112–1118
   PubMed Web of Science ®Google Scholar
• Tassaneeyakul W., Birkett D.J., Edwards J.W., Veronese M.E., Tassaneeyakul W., Tukey R.H., Miners J.O. Human Cytochrome P450 Isoform Specificity in the Regioselective Metabolism of Toluene and o-, m- and p-Xylene. J. Pharmacol. Exp. Ther. 1996; 276: 101–108
   PubMed Web of Science ®Google Scholar
• Gorrod J.W., Damani L.A. The Effect of Various Potential Inhibitors, Activators and Inducers on the N-oxidation of 3-Substituted Pyridines In Vitro. Xenobiotica 1979; 9: 219–226
   PubMed Web of Science ®Google Scholar
• Sesardic D., Boobis A.R., Murray B.P., Murray S., Segura J., De la Torre R., Davies D.S. Furafylline Is a Potent and Selective Inhibitor of Cytochrome P450IA2 in Man. Br. J. Clin. Pharmacol. 1990; 29: 651–663
   PubMed Web of Science ®Google Scholar
• Eagling V.A., Tjia J.F., Back D.J. Differential Selectivity of Cytochrome P450 Inhibitors Against Probes Substrates in Human and Rat Liver Microsomes. Br. J. Clin. Pharmacol. 1998; 45: 107–114
   PubMed Web of Science ®Google Scholar
• de Montellano P.R.O. Handbook of Drug Metabolism, T.E. Woolf. Marcel Dekker Pub., New York 1999; 203–227
   Google Scholar
• Lewis D.F., Ionnides C., Parke D.V. Cytochrome P450 and Species Differences in Xenobiotic Metabolism and Activation of Carcinogen. Environ. Health Perspect. 1998; 106: 633–641
   PubMed Web of Science ®Google Scholar
• Halpert J.R., Guengerich F.P., Bend J.R., Correia M.A. Selective Inhibitors of Cytochromes P450. Toxicol. Appl. Pharmacol. 1994; 125: 163–175
   PubMed Web of Science ®Google Scholar
• Boobis A.R., Sesardic D., Murray B.P., Edwards R.J., Singleton A.M., Rich K.J., Murray S., de la Torre R., Segura J., Pelkonen O., Pasanen M., Kobayashi S., Zhi-guang T., Davies D.S. Species Variation in the Response of the Cytochrome P450-Dependent Monooxygenase System to Inducers and Inhibitors. Xenobiotica 1990; 20: 1139–1161
   PubMed Web of Science ®Google Scholar
• Nedelcheva D., Gut I. P450 in the Rat and Man: Methods of Investigation, Substrate Specificities and Relevance to Cancer. Xenobiotica 1994; 24: 1151–1175
   PubMed Web of Science ®Google Scholar
• Zhou S.F., Chin R., Tingle M.D., Kestell P., Paxton J.W. Effects of Anti-cancer Drugs on the Metabolism of the Novel Anti-cancer Drug 5,6-Dimethylxanthenone-4-acetic Acid (DMXAA) in Human Liver Microsomes. Br. J. Clin. Pharmacol. 2001; 52: 129–136
   PubMed Web of Science ®Google Scholar
• Kestell P., Dunlop I.C., McCrystal M.R., Evans B.D., Paxton J.W., Gamage R.S., Baguley B.C. Plasma Pharmacokinetics of N-[2-(Dimethylamino)Ethyl]-Acridine-4-carboxamide in a Phase I Trial. Cancer Chemother. Pharmacol. 1999; 44: 45–50
   PubMed Web of Science ®Google Scholar
• Paul C., Liliemark J., Tidefelt U., Gahrton G., Peterson C. Pharmacokinetics of Daunorubicin and Doxorubicin in Plasma and Leukemic Cells from Patients with Acute Nonlymphoblastic Leukemia. Ther. Drug Monit. 1989; 11: 140–148
   PubMed Web of Science ®Google Scholar
• Olson R.E., Christ D.D. Plasma Protein Binding of Drugs. Ann. Rep. Med. Chem. 1996; 31: 327–336
   Web of Science ®Google Scholar
• Spahn-Lugguth H., Benet L.Z. Acyl Glucuronide Revisited: Is the Glucuronidation Process a Toxification as Well as a Detoxification Mechanism?. Drug Metab. Rev. 1992; 24: 5–48
   PubMed Web of Science ®Google Scholar
• Smith P.C., Song W.Q., Rodriguez R.J. Covalent Binding of Etodolac Acyl Glucuronide to Albumin In Vitro. Drug Metab. Dispos. 1992; 20: 962–965
   PubMed Web of Science ®Google Scholar
• Bischer A., Ziaamirhosseini P., Iwaki M., Mcdonagh A.F., Benet L.Z. Stereoselective Binding Properties of Naproxen Glucuronide Diastereomers to Proteins. J. Pharmacokinet. Biopharm. 1995; 23: 379–395
   PubMedGoogle Scholar
• Sallustio B.C., Foster D.J.R. Reactivity of Gemfibrozil 1-O-Gemfibrozil-b-d-glucuronide: Pharmacokinetics of Covalently Bound Gemfibrozil–Protein Adducts in Rats. Drug Metab. Dispos. 1995; 23: 892–899
   PubMed Web of Science ®Google Scholar
• Sallustio B.C., Fairchild B.A., Pannall P.R. Interaction of Human Serum Albumin with the Electrophilic Metabolite 1-O-Gemfibrozil-b-d-glucuronide. Drug Metab. Dispos. 1997; 25: 55–60
   PubMed Web of Science ®Google Scholar
• Shen S.J., Marchick M.R., Davis M.R., Doss G.A., Pohl L.R. Metabolic Activation of Diclofenac by Human Cytochrome P450 3A4: Role of 5-Hydroxydiclofenac. Chem. Res. Toxicol. 1999; 12: 214–222
   PubMed Web of Science ®Google Scholar
• Terrier N., Benoit E., Senay C., Lapicque F., Radominska-Pandya A., Magdalou J., Fournel-Gigleux S. Human and Rat Liver UDP-Glucuronosyltransferases Are Targets of Ketoprofen Acylglucuronide. Mol. Pharmacol. 1999; 56: 226–234
   PubMed Web of Science ®Google Scholar
• Sallustio B.C., Harkin L.A., Mann M.C., Krivickas S.J., Burcham P.C. Genotoxicity of Acyl Glucuronide Metabolites Formed from Clofibric Acid and Gemfibrozil: A Novel Role for Phase II-Mediated Bioactivation in the Hepatocarcinogenicity of the Parent Aglycone. Toxicol. Appl. Pharmacol. 1997; 147: 459–464
   PubMed Web of Science ®Google Scholar
• Chabot G.G., Gouyette A. Reactivity of Flavone Acetic Acid and Its Acyl Glucuronide. Biochem. Pharmacol. 1991; 42: 1145–1148
   PubMed Web of Science ®Google Scholar
• Zhou S.F., Kestell P., Tingle M.D., Paxton J.W. Determination of the Covalent Adducts of the Novel Anti-cancer Agent 5,6-Dimethylxanthenone-4-acetic Acid in Biological Samples by High-Performance Liquid Chromatography. J. Chromatogr. B 2001; 757: 343–348
   PubMedGoogle Scholar
• Benet L.Z., Spahn-Lugguth H., Iwakaw S.C.V., Mizuma T., Mayer S., Mutschler E., Lin E.T. Predictability of the Covalent Binding of Acidic Drugs in Man. Life Sci. 1993; 53: 141–146
   PubMed Web of Science ®Google Scholar
• Zia-amirhosseini P., Ojingwa J.C., Spahn-langguth H., Mcdonagh A.F., Benet L.Z. Enhanced Covalent Binding of Tolmetin to Proteins in Humans After Multiple Dosing. Clin. Pharmacol. Ther. 1994; 55: 21–27
   PubMed Web of Science ®Google Scholar
• Sallustio B.C., Knights K.M., Roberts B.J., Zacest R. In Vivo Covalent Binding of Clobibric Acid to Human Plasma Proteins and Rat Liver Proteins. Biochem. Pharmacol. 1991; 42: 1421–1425
   PubMed Web of Science ®Google Scholar
• Smith P.C., Benet L.Z., Mcdonagh A.F. Irreversible Binding of Zomepirac to Plasma Protein In Vitro and In Vivo. J. Clin. Investig. 1986; 77: 934–939
   PubMed Web of Science ®Google Scholar
• Meffin P.J., Zilm D.M., Veenendaal J.R. A Renal Mechanism for the Clofibric Acid–Probenecid Interaction. J. Pharmacol. Exp. Ther. 1983; 227: 739–742
   PubMed Web of Science ®Google Scholar
• Fichtl B., Nieciecki A., Walter K. Tissue Binding Versus Plasma Binding of Drugs: General Principles and Pharmacokinetic Consequences. Adv. Drug Res. 1991; 20: 117–166
   Google Scholar
• du Souich P., Verges J., Erill S. Plasma Protein Binding and Pharmacological Response. Clin. Pharmacokinet. 1993; 24: 435–440
   PubMed Web of Science ®Google Scholar
• Lin J.H. Species Similarities and Differences in Pharmacokinetics. Drug Metab. Dispos. 1995; 23: 1008–1021
   PubMed Web of Science ®Google Scholar
• Cassidy J., Kerr D.J., Setanoians A., Zaharko D.S., Kaye S.B. Could Interspecies Differences in the Protein Binding of Flavone Acetic Acid Contribute to the Failure to Predict Lack of Efficacy in Patients?. Cancer Chemother. Pharmacol. 1989; 23: 397–400
   PubMed Web of Science ®Google Scholar
• Chabot G.G., Bissery M.C., Corbett T.H., Rutkowski K., Baker L.H. Pharmacodynamics and Causes of Dose-Dependent Pharmacokinetics of Flavone-8-acetic Acid (LM-975; NSC-347512) in Mice. Cancer Chemother. Pharmacol. 1989; 24: 15–22
   PubMed Web of Science ®Google Scholar
• Perera P.Y., Barber S.A., Ching L.-M., Vogel S.N. Activation of LPS-Inducible Genes by the Antitumor Agent 5,6-Dimethylxanthenone-4-acetic Acid in Primary Murine Macrophages. Dissection of Signaling Pathways Leading to Gene Induction and Tyrosine Phosphorylation. J. Immunol. 1994; 153: 4684–4693
   PubMed Web of Science ®Google Scholar
• Ching L.-M., Joseph W.R., Crosier K.E., Baguley B.C. Induction of Tumour Necrosis Factor—A Messenger RNA in Humans and Murine Cells by the Flavone Acetic Acid Analogue 5,6-Dimethylxanthenone-4-acetic Acid (NSC 640488). Cancer Res. 1994; 54: 870–872
   PubMed Web of Science ®Google Scholar
• Zhou S.F., Kestell P., Tingle M.D., Paxton J.W. Determination of Unbound Concentration of the Novel Anti-tumour Agent 5,6-Dimethylxanthenone-4-acetic Acid in Human Plasma by Ultrafiltration Followed By High-Performance Liquid Chromatography with Fluorimetric Detection. J. Chromatogr. B 2001; 757: 359–363
   PubMedGoogle Scholar
• Zhou S.F., Paxton J.W., Kestell P., Tingle M.D. Reversible Binding of the Novel Anti-tumour Agent 5,6-Dimethylxanthenone-4-acetic Acid to Plasma Proteins and Blood Cells in Various Species. J. Pharm. Pharmacol. 2001; 53: 463–471
   PubMed Web of Science ®Google Scholar
• McKeage M.J., Kestell P., Denny W.A., Baguley B.C. Plasma Pharmacokinetics of the Antitumour Agents 5,6-Dimethylxanthenone-4-acetic Acid, Xanthenone-4-acetic Acid and Flavone-8-acetic Acid in Mice. Cancer Chemother. Pharmacol. 1991; 28: 409–413
   PubMed Web of Science ®Google Scholar
• Boxenbaum H. Interspecies Scaling, Allometry, Physiological Time, and the Ground Plan of Pharmacokinetics. J. Pharmacokinet. Biopharm. 1982; 10: 201–227
   PubMedGoogle Scholar
• Modenti J. Dosage Regimen Design for Pharmaceutical Studies Conducted in Animals. J. Pharm. Sci. 1986; 75: 852–856
   PubMed Web of Science ®Google Scholar
• Mahmood I., Balian J.D. The Pharmacokinetic Principles Behind Scaling from Preclinical Results to Phase I Protocols. Clin. Pharmacokinet. 1999; 36: 1–11
   PubMed Web of Science ®Google Scholar
• Zaharko D.S., Grieshaber C.K., Plowman J., Cradock J.C. Therapeutic and Pharmacokinetic Relationships of Flavone Acetic Acid: An Agent with Activity Against Solid Tumors. Cancer Treat. Rep. 1986; 70: 1415–1421
   PubMedGoogle Scholar
• Zhou S.F., Paxton J.W., Tingle M.D., Kestell P., Ching L.-M. In Vitro and In Vivo Kinetic Interactions of the Anti-tumour Agent 5,6-Dimethylxanthenone-4-acetic Acid with Thalidomide and Diclofenac. Cancer Chemother. Pharmacol. 2001; 47: 319–326
   PubMed Web of Science ®Google Scholar
• Kestell P., Zhao L., Ching L.-M., Baguley B.C., Paxton J.W. Modulation of the Plasma Pharmacokinetics of 5,6-Dimethylxanthenone-4-acetic Acid by Thalidomide in Mice. Cancer Chemother. Pharmacol. 2000; 46: 135–141
   PubMed Web of Science ®Google Scholar
• Zhou S.F., Kestell P., Tingle M.D., Ching L.-M., Paxton J.W. A Difference Between the Rat and Mouse in the Pharmacokinetic Interaction of 5,6-Dimethylxanthenone-4-acetic Acid with Thalidomide. Cancer Chemother. Pharmacol. 2001; 47: 541–544
   PubMed Web of Science ®Google Scholar
• Zhao L., Ketsell P., Zhuang L., Baguley B.C. Effects of the Serotonin Receptor Antagonist Cyproheptadine on the Activity and Pharmacokinetic of 5,6-Dimethylxanthenone-4-acetic (DMXAA). Cancer Chemother. Pharmacol. 2001; 47: 491–497
   PubMed Web of Science ®Google Scholar
• Ito K., Iwatsubo T., Kanamitsu S., Nukajima Y., Sugiyama Y. Quantitative Prediction of In Vivo Drug Clearance and Drug Interactions from In Vitro Data on Metabolism, Together with Binding and Transport. Annu. Rev. Pharmacol. Toxicol. 1998; 38: 461–499
   PubMed Web of Science ®Google Scholar
• Houston J.B., Carlile D.J. Incorporation of In Vitro Drug Metabolism Data into Physiologically-Based Pharmacokinetic Models. Toxicol. In Vitro 1997; 11: 473–478
   PubMed Web of Science ®Google Scholar
• von Moltke L.L., Greenblatt D.J., Schmider J., Wright C.E., Harmatz J.S., Shader R.I. In Vitro Approaches to Predicting Drug Interactions In Vivo. Biochem. Pharmacol. 1998; 55: 113–122
   PubMed Web of Science ®Google Scholar
• Ito K., Iwatsubo T., Kanamitsu S., Ueda K., Suzuki H., Sugiyama Y. Prediction of Pharmacokinetic Alterations Caused by Drug–Drug Interactions: Metabolic Interaction in the Liver. Pharmacol. Rev. 1998; 50: 387–411
   PubMed Web of Science ®Google Scholar
• Lave T., Coassolo P., Reigner B. Prediction of Hepatic Metabolic Clearance Based on Interspecies Allometric Scaling Techniques and In Vitro In Vivo Correlations. Clin. Pharmacokinet. 1999; 36: 211–231
   PubMed Web of Science ®Google Scholar
• Houston J.B., Kenworthy K.E. In Vitro–In Vivo Scaling of CYP Kinetic Data not Consistent with the Classical Michaelis–Menten Model. Drug Metab. Dispos. 2000; 28: 246–254
   PubMed Web of Science ®Google Scholar
• Ubeaud G., Schmitt C., Jaeck D., Lave T., Coassolo P.H.H. Bosentan, a New Endothelin Receptor Antagonist: Prediction of the Systemic Plasma Clearance in Man from Combined In Vivo and In Vitro Data. Xenobiotica 1995; 25: 1381–1390
   PubMed Web of Science ®Google Scholar
• Boxenbaum H. Interspecies Pharmacokinetic Scaling and the Evolutionary-Comparative Paradigm. Drug Metab. Rev. 1984; 15: 1071–1121
   PubMed Web of Science ®Google Scholar
• Mitsuhashi Y., Sugiyama Y., Ozawa S., Nitanai T., Sasahara K., Nakamura K., Tanaka M., Nishimura T., Inaba M., Kobayashi T. Prediction of ACNU Plasma Concentration–Time Profiles in Humans by Animal Scale-Up. Cancer Chemother. Pharmacol. 1990; 27: 20–26
   PubMed Web of Science ®Google Scholar
• Paxton J.W., Kim S.N., Whitefield L.R. Pharmacokinetic and Toxicity Scaling of the Antitumour Agents Amsacrine and CI-921, a New Analogue, in Mice, Rats, Rabbits, Dogs, and Humans. Cancer Res. 1990; 50: 2692–2697
   PubMed Web of Science ®Google Scholar
• Dogra S.C., Khanduja K.L., Sharma R.R. Hepatic Drug-Metabolising Enzymes in Lung Tumour-Bearing Rats. Biochem. Pharmacol. 1985; 34: 3190–3193
   PubMed Web of Science ®Google Scholar
• Relling M.V., Crom W.R., Pieper J.A., Cupit G.C., Rivera G.K., Evans W.E. Hepatic Drug Clearance in Children with Leukemia: Changes in Clearance of Model Substrates During Remission-Induction Therapy. Clin. Pharmacol. Ther. 1987; 41: 651–660
   PubMed Web of Science ®Google Scholar
• Lewis D.F. Quantitative Structure–Activity Relationships in Substrates, Inducers, and Inhibitors of Cytochrome P4501 (CYP1). Drug Metab. Rev. 1997; 29: 589–650
   PubMed Web of Science ®Google Scholar
• Dai R., Zhai S., Wei X., Pincus M.R., Vestal R.E., Friedman F.K. Inhibition of Human Cytochrome P450 1A2 by Flavone: A Molecular Modeling Study. J. Protein Chem. 1998; 17: 643–650
   PubMedGoogle Scholar
• Wei X.X., Dai R.K., Zhai S.P., Thummel K.E., Friedman F.K., Vestal R.E. Inhibition of Human Liver Cytochrome P-450 1A2 by the Class Ib Antiarrhythmics Mexiletine, Lidocaine, and Tocainide. J. Pharmacol. Exp. Ther. 1999; 289: 853–858
   PubMed Web of Science ®Google Scholar
• Lozano J.J., Pastor M., Cruciani G., Gaedt K., Centeno N.B., Gago F., Sanz F. 3D-QSAR Methods on the Basis of Ligand–Receptor Complexes. Application of COMBINE and GRID/GOLPE Methodologies to a Series of CYP1A2 Ligands. J. Comput.-Aided Mol. Des. 2000; 14: 341–353
   PubMed Web of Science ®Google Scholar
• Osborne C.K. Mechanisms for Tamoxifen Resistance in Breast Cancer: Possible Role of Tamoxifen Metabolism. J. Steroid Biochem. Mol. Biol. 1993; 47: 83–89
   PubMed Web of Science ®Google Scholar
• Stearns R.A., Miller R.R., Doss G.A., Chakravarty P.K., Rosegay A., Gatto G.J., Chiu S.H. The Metabolism of Dup 753, a Nonpeptide Angiotensin II Receptor Antagonist, by Rat, Monkey, and Human Liver Slices. Drug Metab. Dispos. 1992; 20: 281–287
   PubMed Web of Science ®Google Scholar
• Venkatakrishnan K., von Moltke L.L., Greenblatt D.J. Nortriptyline E-10-Hydroxylation In Vitro Is Mediated by Human CYP2D6 (High Affinity) and CYP3A4 (Low Affinity): Implications for Interactions with Enzyme-Inducing Drugs. J. Clin. Pharmacol. 1999; 39: 567–577
   PubMed Web of Science ®Google Scholar
• Iwatsubo T., Hirota N., Ooie T., Suzuki H., Shimada N., Chiba K., Ishizaki T., Green C.E., Tyson C.A., Sugiyama Y. Prediction of In Vivo Drug Metabolism in the Human Liver from In Vitro Metabolism Data. Pharmacol. Ther. 1997; 73: 147–171
   PubMed Web of Science ®Google Scholar
• Nakajima M., Nakamura S., Tokudome S., Shimada N., Yamazaki H., Yokoi T. Azelastine N-Demethylation by Cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in Human Liver Microsomes: Evaluation of Approach to Predict the Contribution of Multiple CYPs. Drug Metab. Dispos. 1999; 27: 1381–1391
   PubMed Web of Science ®Google Scholar
• Sai Y., Yang T.J., Krausz K.W., Gonzalez F.J., Gelboin H.V. An Inhibitory Monoclonal Antibody to Human Cytochrome P450 2A6 Defines Its Role in the Metabolism of Coumarin, 7-Ethoxycoumarin and 4-Nitroanisole in Human Liver. Pharmacogenetics 1999; 9: 229–237
   PubMedGoogle Scholar
• Mistry M., Houston J.B. Glucuronidation In Vitro and In Vivo: Comparison of Intestinal and Hepatic Conjugation of Morphine, Naloxone, and Bupreonorphine. Drug Metab. Dispos. 1987; 15: 710–717
   PubMed Web of Science ®Google Scholar
• Obach R.S. Nonspecific Binding to Microsomes: Impact on Scale-Up of In Vitro Intrinsic Clearance to Hepatic Clearance as Assessed Through Examination of Warfarin, Imipramine, and Propranolol. Drug Metab. Dispos. 1997; 25: 1359–1369
   PubMed Web of Science ®Google Scholar
• Komatsu T., Yamazaki H., Shimada N., Nakajima M., Yokoi T. Roles of Cytochromes P450 1A2, 2A6, and 2C8 in 5-Fluorouracil Formation from Tegafur, an Anticancer Prodrug, in Human Liver Microsomes. Drug Metab. Dispos. 2000; 28: 1457–1463
   PubMed Web of Science ®Google Scholar
• Walker D., Flinois J.P., Monkman S., Beloc C., Boddy A.V., Cholerton S., Daly A.K., Lind M.J., Pearson A.D.J., Beaune P.H., Idle J.R. Identification of the Major Human Hepatic Cytochrome P450 Involved in Activation and N-Dechloroethylation of Ifosfamide. Biochem. Pharmacol. 1994; 47: 1157–1163
   PubMed Web of Science ®Google Scholar
• Chang T.K., Yu L., Goldstein J.A., Waxman D.J. Identification of the Polymorphically Expressed CYP2C19 and the Wild-Type CYP2C9-ILE359 Allele as Low-Km Catalysts of Cyclophosphamide and Ifosfamide Activation. Pharmacogenetics 1997; 7: 211–221
   PubMedGoogle Scholar
• Cresteil T., Monsarrat B., Alvinerie P., Treluyer J.M., Vieira I., Wright M. Taxol Metabolism by Human Liver Microsomes: Identification of Cytochrome P450 Isozymes Involved in Its Biotransformation. Cancer Res. 1994; 54: 386–392
   PubMed Web of Science ®Google Scholar
• Harris J.W., Rahman A., Kim B.R., Guengerich F.P., Collins J.M. Metabolism of Taxol by Human Hepatic Microsomes and Liver Slices: Participation of Cytochrome P450 3A4 and an Unknown P450 Enzyme. Cancer Res. 1994; 54: 4026–4035
   PubMed Web of Science ®Google Scholar
• Kumar G.N., Walle U.K., Walle T. Cytochrome P450 3A-Mediated Human Liver Microsomal Taxol 6 Alpha-Hydroxylation. J. Pharmacol. Exp. Ther. 1994; 268: 1160–1165
   PubMed Web of Science ®Google Scholar
• Rahman A., Korzekwa K.R., Grogan J., Gonzalez F.J., Harris J.W. Selective Biotransformation of Taxol to 6 Alpha-Hydroxytaxol by Human Cytochrome P450 2C8. Cancer Res. 1994; 54: 5543–5546
   PubMed Web of Science ®Google Scholar
• Dehal S.S., Kupfer D. CYP2D6 Catalyzes Tamoxifen 4-Hydroxylation in Human Liver. Cancer Res. 1997; 57: 3402–3406
   PubMed Web of Science ®Google Scholar
• Relling M.V., Nemec J., Schuetz E.G., Schuetz J.D., Gonzalez F.J., Korzekwa K.R. O-Demethylation of Ipipodophyllotoxins Is Catalyzed by Human Cytochrome P450 3A4. Mol. Pharmacol. 1994; 45: 352–358
   PubMed Web of Science ®Google Scholar
• Kawashiro T., Yamashita K., Zhao X.J., Koyama E., Tani M., Chiba K., Ishizaki T. A Study on the Metabolism of Etoposide and Possible Interactions with Antitumor or Supporting Agents by Human Liver Microsomes. J. Pharmacol. Exp. Ther. 1998; 286: 1294–1300
   PubMed Web of Science ®Google Scholar
• Zhou-Pan X.R., Seree E., Zhou X.J., Placidi M., Maurel P., Barra Y., Rahmani R. Involvement of Human Liver Cytochrome 3A in Vinblastine Metabolism: Drug Interactions. Cancer Res. 1993; 53: 5121–5126
   PubMed Web of Science ®Google Scholar
• Kajita J., Kuwabara T., Kobayashi H., Kobayashi S. CYP3A4 Is Mainly Responsible for the Metabolism of a New Vinca Alkaloid, Vinorelbine, in Human Liver Microsomes. Drug Metab. Dispos. 2000; 28: 1121–1127
   PubMed Web of Science ®Google Scholar
• Marre F., Sanderink G.J., Desousa G., Gaillard C., Martinet M., Rahmani R. Hepatic Biotransformation of Docetaxel (Taxotere(r)) In Vitro—Involvement of the CYP3A Subfamily in Humans. Cancer Res. 1996; 56: 1296–1302
   PubMed Web of Science ®Google Scholar
• Shou M., Martinet M., Korzekwa K.R., Krausz K.W., Gonzalez F.J., Gelboin H.V. Role of Human Cytochrome P450 3A4 and 3A5 in the Metabolism of Taxotere and Its Derivatives: Enzyme Specificity, Interindividual Distribution and Metabolic Contribution in Human Liver. Pharmacogenetics 1998; 8: 391–401
   PubMedGoogle Scholar
• Nadin L., Murray M. Participation of CYP2C8 in Retinoic Acid 4-Hydroxylation in Human Hepatic Microsomes. Biochem. Pharmacol. 1999; 58: 1201–1208
   PubMed Web of Science ®Google Scholar