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Xenobiotica
the fate of foreign compounds in biological systems
Volume 30, 2000 - Issue 9
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Research Article

Identification of cytochrome P4503A as the major subfamily responsible for the metabolism of roquinimex in man

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Pages 905-914 | Published online: 22 Sep 2008

References

  • ANDERSEN, O., LYCKE, J., TOLLESSON, P. O., SVENNINGSSON, A., RUNMARKER, B., LINDE, A. S., ÁsTRöm, M., GjoRsTRuP, P. and EKHoLm, S., 1996, Linomide reduces the rate of active lesions in relapsing-remitting multiple sclerosis. Neurology, 47, 895–900.
  • BALDWIN, S. J., BLOOMER, J. C., SMITH, G. J., AYRTON, A. D., CLARKE, S. E. and CHENERY, R. J., 1995, Ketoconazole and sulphaphenazole as the respective inhibitors of P4503A and 2C9. Xenobiotica, 25, 261–270.
  • CARLILE, D. J., ZOMORODI, K. and HOUSTON, B., 1997, Scaling factors to relate drug metabolic clearance in hepatic microsomes, isolated hepatocytes and the intact liver. Drug Metabolism and Disposition, 25, 903–911.
  • GONZALEZ, F. J., SONG, B.-J. and HARDWICK, J. P., 1986, Pregnenolone 16-a carbonitrile-inducible P450 gene family: gene conversion and differential regulation. Molecular Cell Biology, 6, 2969–2976.
  • GROSS, D. J., SIDI, H., WEISS, L., KALLAND, T., ROSENMANN, E. and SLAVIN, S., 1994, Prevention of diabetes mellitus in non-obese diabetic mice by Linomide, a novel immunomodulating drug. Diabetologia, 37, 1195–1201.
  • GUENGERICH, F. P., 1990, Mechanism-based inactivation of human microsomal cytochrome P450 IIIA4 by gestodene. Chemical Research in Toxicology, 3, 363–371.
  • INABA, T., JuRimA, M., MAHON, W. A. and KALO W., 1985, In vitro inhibition studies of two isozymes of human liver cytochrome p-450: mephenytoin p-hydroxylase and sparteine monooxygenase. Drug Metabolism and Disposition, 13, 443–448.
  • KARUSSIS, D. M., LEHMANN, D., SLAVIN, S., KALLAND, T., VOURKA-KARUSSIS, U., MIZRACHI-KOLL, R., OVADIA, H. and ABRAMSKY, O., 1995, Immunomodulation of autoimmunity by Linomide. Israel Journal of Medical Sciences, 31, 38–41.
  • KARUSSIS, D. M., LEHMANN, D., SLAVIN, S., VOURKA-KARUSSIS, U., MIZRACHI-KOLL, R., OVADIA H., KALLAND, T. and ABRAMSKY, O., 1993, Treatment of chronic-relapsing experimental autoimmune encephalomyelitis with the synthetic immunomodulator Linomide (quinoline-3-carboxamide). Proceedings of the National Academy of Sciences, USA, 90, 6400–6404.
  • KUNZE, K. L. and TRAGER, W. F., 1993, Isoform selective mechanism-based inhibition of human CYP1A2 by furafylline. Chemical Research in Toxicology, 6, 649–656.
  • LASKER, J. M., HUANG, M. T. and CONNEY, A., 1984, In vitro and in vivo activation of oxidative drug metabolism by fiavonoids. Journal of Pharmacology and Experimental Therapeutics, 229, 162–170.
  • LEHMANN, D., KARUSSIS, D. M., FLURESCO, D., MIZRACHI-KOLL, R., OVADIA, H., SHEZEN, E., KALLAND, T. and ABRAMSKY, O., 1997, Immunomodulation of autoimmunity by linomide: inhibition of antigen presentation through down regulation of macrophage activity in the model of experimental autoimmune encephalomyelitis. Journal of Neuroimmunology, 74, 102–110.
  • LEWIS, D. F. V., DICKINS, M., WEAVERS, R. J., EDDERSHAW, P. J., GOLDFARB, P. S. and TARBIT, M. H., 1998, Molecular modelling of human CYP2C subfamily enzymes CYP2C9 and CYP2C19: rationalization of substrate specificity and site-directed mutagenesis experiments in the CYP2C subfamily. Xenobiotica, 28, 235–268.
  • NELSON, D. R., KOYMANS, L., KAMATAKI, T., STEGEMAN, J. J., FEYEREISEN, R., WAXMAN, D. J., WATERMAN, M. R., GOTOH, O., COON, M. J., ESTABROOK, R. W., GUNSALUS, I. C. and NEBERT, D. W., 1996, P450 superfamily: update on new sequences, gene mapping, accession numbers and nomenclature. Pharmacogenetics, 6, 1–42.
  • NIVED, O., STURFELT, G., NILSSON, B., TERMANDER, B., GUNNARSSON, P. O., STRANDGARDEN, K. and WOLLHEIM, F., 1994, Clinical pilot study of roquinimex (Linomide) in patients with autoimmune disease. Internationd Journal of Immunotherapy, 10, 49–59.
  • RELLING, M. V., AOYAMA, T., GONZALEZ, F. J. and MEIER, U. R., 1990, Tolbutamide and mephenytoin hydroxylation by cytochrome P45 Os in the 2C subfamily. Journal of Pharmacology and Experimental Therapeutics, 252, 442–427.
  • SAS/STAT, 1989, SAS I STAT User's Guide, Version 6, 4th edn, vol. 1 (Cary: SAS Institute, Inc.).
  • SHIMADA, T., YAMAZAKI, H., MIMURA, M., INUI, Y. and GUENGERICH, F. P., 1994, Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogenes and toxical chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians. Journal of Pharmacology and Experimental Therapeutics, 270, 414–423.
  • SHOU, M., GROGAN, J., MANCEWICZ, J.-A., KRAUSZ, K. W., GONZALEZ, F. J., GELBOIN, H. V. and KORZEKWA, K. R., 1994, Activation of CYP3A4: evidence for simultaneous binding of two substrates in a cytochrome P450 active site. Biochemistry, 33, 6450–6455.
  • SIMMONS, D. L., LALLEY, P. A. and KASPER, C. B., 1985, Chromosomal assignment of genes coding for component of the mixed-function oxidase system in mouse Journal of Biology and Chemistry, 260, 515–521.
  • STRANDGARDEN, K., HöGLUND, P., GRöNQUIST, L., SVENSSON, L. and GUNNARSSON, P. O., 2000, Absorption and disposition including circulation of 14C-roquinimex after oral administration to healthy volunteers. Biopharmaceutics and Drug Disposition (submitted).
  • TARKOWSKI, A., GUNNARSSON, K., NILSSON, L., LINDHOLM, L. and STALHANDSKE, T., 1986b, Successful treatment of autoimmunity in MRL/I mice with LS 2616, a new immunomodulator. Arthritis and Rheumatics, 29, 1405–1409.
  • TARKOWSKI, A., GUNNARSSON, K. and STALHANDSKE, T., 1986a, Effects of LS 2616 administration upon the autoimmune disease of (NZB NZW) F, hybrid mice. Immunology, 59, 589–594.
  • TUVESSON, H., STRANDGARDEN, K., NORDLE, O., GUNNARSSON, P. O., SEIDEGARD, J. and PERSSON, R., 1999, Microsomal metabolism of roquinimex in mouse and rat. Xenobiotica 2000,30, 371–380.
  • WILKINSON, G. R., 1996, Cytochrome P4503A (CYP3A) metabolism: prediction of in vivo activity in humans. Journal of Pharmacokinetics and Biopharmaceutics, 24, 475–490.

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