Reversible and irreversible inhibition of CYP3A enzymes by tamoxifen and metabolites.

@article{Zhao2002ReversibleAI,
  title={Reversible and irreversible inhibition of CYP3A enzymes by tamoxifen and metabolites.},
  author={X Zhao and David R. Jones and Yinghong Wang and Scott W. Grimm and Stephen D. Hall},
  journal={Xenobiotica; the fate of foreign compounds in biological systems},
  year={2002},
  volume={32 10},
  pages={863-78}
}
1. Preliminary studies have identified cytochrome P450 (CYP) 3A4 and CYP1B1 as the human CYPs inhibited by tamoxifen. To quantify the inhibitory potency of tamoxifen and its major metabolites, the metabolism of three substrates of CYP3A, midazolam, diltiazem and testosterone, and 7-ethoxyresorufin as a substrate of CYP1B1 were examined in catalytic assays carried out using human liver microsomes and cDNA-expression systems. 2. Tamoxifen, N-desmethyltamoxifen, 4-hydroxytamoxifen and 3… CONTINUE READING

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