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Xenobiotica
the fate of foreign compounds in biological systems
Volume 29, 1999 - Issue 11
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Research Article

In vitro metabolism of mifepristone (RU-486) in rat, monkey and human hepatic S9 fractions: identification of three new mifepristone metabolites

W. N. Wu Department of Drug Metabolism, Division of Preclinical Development, The R. W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA
,
L. A. McKown Department of Drug Metabolism, Division of Preclinical Development, The R. W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA
,
M. D. Moyer Department of Drug Metabolism, Division of Preclinical Development, The R. W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA
,
T. B. Johannsen Department of Drug Metabolism, Division of Preclinical Development, The R. W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA
&
A. R. Takacs Department of Drug Metabolism, Division of Preclinical Development, The R. W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA
Pages 1089-1100 | Published online: 22 Sep 2008

References

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  • CHASSEROT -GOLAZ, S., BECK, G. and VENETIANER, A., 1993, Biotransformation of 17/3-hydroxy-11p-(4-dimethylaminopheny1)17a-1-propynyl-estra-4,9-dien-3-one (RU486) in rat hepatoma variants. Biochemical Pharmacology, 46, 2100–2103.
  • DERAEDT, R., BONNAR, C., BUSIGNY, M., CHATELET, P., COUSTY, C., MOUREA, M., PHILIBERT, D., POTTIER, J. and SALMON, J., 1985, Pharmacokinetics of RU 486. In E. E. Baulieu and S. Segal (eds), The Ant iprogestin Steroid RU 486 and Human fertility Control (New York: Plenum), pp. 103–122.
  • FOLDESI, I., FALKAY, G. and KOVACS, L., 1996, Determination of RU486 (mifepristone) in blood by radioreceptorassay: a pharmacokinetic study. Contraception, 54, 27–32.
  • HE, C., ZHAN G., BA', X., JIANG, N., ZHOU, W., GUI, Y., FAN, Q. and CHEN, J., 1994, Pharmacokinetics of mifepristone (RU486) and its metabolites in pregnant women. Shengzhi Yu Biyun, 14,280–286.
  • HEIKINHEINIO, O., KONTULA, K., CROXATTO, H., SPITZ, I. and LuuKKAINEN, T., 1987a, Plasma concentrations and receptor binding of RU 486 and its metabolites in humans. Journal of Steroid Biochemistry, 26, 279–284.
  • HEIKINHEINIO O., LAHTEENMAKI, P., KOIVUNEN, E., SHOUPE, D. and CROXATTO, H., 1987b, Metabolism and serum binding of RU 486 in women after various single doses. Human Reproduction, 2, 379–385.
  • JANG, G. R., WRIGHTON S. A. and BENET, L. Z., 1996, Identification of CYP3A4 as the principal enzyme catalyzing mifepristone (RU 486) oxidation in human liver microsomes. Biochemical Phar-macology, 52, 753–761.
  • LAHTEENMAKI, P., HEIKINHEIMO O., CROXATTO, H., SPITZ, I., SHOUPE, D., BIRGERSON, L. and Lc UKKAINEN, 1987, Phamcokinetics and metabolism of RU 486. Journal of Steroid Biochemistry, 27, 859–863.
  • NAGOSHI, K., HAYASHI, N. and SEKIBA, K., 1991, Automated direct assay system for RU38486, an antiprogesterone-anti-glucocorticoid agent, and its metabolites using high performance liquid chromatography. Acta Medica Okayama, 45, 81–87.
  • Soi, Y., YE, Z., HE, C., ZHANG, G., Xu, J., VAN, L. and FORTHERBY, K., 1993, pharmacokinetic study of RU 486 and its metabolites after oral administration of single doses to pregnant and non-pregnant women. Contraception, 48, 133–149.
  • ULMANN, A., TEUTSCH, G. and PHILIBERT, D., 1990, RU 486. Scientific American, 262,42–48.
  • Wu, W. N., McKowN, L. A. and TAKACS, A. R., 1997, Identification of three new mifepristone (RU-486) metabolites in rat, monkey, and human hepatic S9 fractions. In I SSX Proceedings, 45 (abstract, The 8th North American I SSX Meeting).

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