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

@article{Korhonen2008IdentificationOT,
  title={Identification of the human cytochrome P450 enzymes involved in the in vitro biotransformation of lynestrenol and norethindrone},
  author={Tuomas Korhonen and Miia Turpeinen and Ari Tolonen and Kari Laine and Olavi Pelkonen},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2008},
  volume={110},
  pages={56-66}
}
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… Expand
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