Abstract
This presentation describes the metabolism of triphenylethylene derivatives, chlorotrianisene (TACE) and tamoxifen by hepatic microsomal enzymes in rat and human. Both compounds appear to exhibit partial agonist/antagonist estrogen activity in the rat. The antiestrogenic activity of triphenylethylenes is thought to involve the interactions of these compounds and/or of their respective metabolites with the estrogen receptor (ER). However, the exact mechanism of their antiestrogenic action, has not been fully elucidated.
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© 1995 Springer-Verlag Berlin Heidelberg
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Kupfer, D. (1995). Metabolism of Antiestrogenic Anti-Cancer Agents by Cytochromne P450 and Flavin-Containing Monooxygenases. Mechanism of Action Involving Metabolites. In: Arinç, E., Schenkman, J.B., Hodgson, E. (eds) Molecular Aspects of Oxidative Drug Metabolizing Enzymes. NATO ASI Series, vol 90. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-79528-2_23
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DOI: https://doi.org/10.1007/978-3-642-79528-2_23
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