Identification of the human cytochrome P450 enzymes involved in the in vitro biotransformation of lynestrenol and norethindrone

  title={Identification of the human cytochrome P450 enzymes involved in the in vitro biotransformation of lynestrenol and norethindrone},
  author={T. Korhonen and M. Turpeinen and A. Tolonen and K. Laine and O. Pelkonen},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  • T. Korhonen, M. Turpeinen, +2 authors O. Pelkonen
  • Published 2008
  • Chemistry, Medicine
  • The Journal of Steroid Biochemistry and Molecular Biology
  • This study examined the cytochrome P450 (CYP) enzyme selectivity of in vitro bioactivation of lynestrenol to norethindrone and the further metabolism of norethindrone. Screening with well-established chemical inhibitors showed that the formation of norethindrone was potently inhibited by CYP3A4 inhibitor ketoconazole (IC(50)=0.02 microM) and with CYP2C9 inhibitor sulphaphenazole (IC(50)=2.13 microM); the further biotransformation of norethindrone was strongly inhibited by ketoconazole (IC(50)=0… CONTINUE READING
    32 Citations
    Interactions between human cytochrome P450 enzymes and steroids: physiological and pharmacological implications
    • Y. Zhang, L. Yang
    • Biology, Medicine
    • Expert opinion on drug metabolism & toxicology
    • 2009
    • 23
    Clinical drug‐drug interaction assessment of ivacaftor as a potential inhibitor of cytochrome P450 and P‐glycoprotein
    • 29
    Determination and identification of estrogenic compounds generated with biosynthetic enzymes using hyphenated screening assays, high resolution mass spectrometry and off-line NMR.
    • 42
    Drug–Drug Interactions with the NS3/4A Protease Inhibitor Simeprevir
    • 54
    • PDF
    The Influence of in Vitro Gill and Liver Metabolism of Xenobiotics on Fish Bioconcentration
    • Highly Influenced
    • PDF


    Selective inhibition of CYP2B6-catalyzed bupropion hydroxylation in human liver microsomes in vitro.
    • 104
    • PDF
    Role of CYP2C9 polymorphism in losartan oxidation.
    • 154
    • PDF
    Warfarin-fluconazole. I. Inhibition of the human cytochrome P450-dependent metabolism of warfarin by fluconazole: in vitro studies.
    • 157
    Multiple P450 substrates in a single run: rapid and comprehensive in vitro interaction assay.
    • 118
    Cytochrome P450 (CYP) inhibition screening: comparison of three tests.
    • M. Turpeinen, L. E. Korhonen, +4 authors O. Pelkonen
    • Chemistry, Medicine
    • European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
    • 2006
    • 59