Article
Assessment of the impact of CYP3A polymorphisms on the formation of α-hydroxytamoxifen and N-desmethyltamoxifen in human liver microsomes.
Drug metabolism and disposition: the biological fate of chemicals - 1 Feb 2012
Mugundu Ganesh M, Sallans Larry, Guo Yingying, Shaughnessy Elizabeth A, Desai Pankaj B
Abstract excerpt
Tamoxifen, an antiestrogen used in the prevention and treatment of breast cancer, is extensively metabolized by cytochrome P450 enzymes. Its biotransformation to α-hydroxytamoxifen (α-OHT), which may be genotoxic, and to N-desmethyltamoxifen (N-DMT), which is partially hydroxylated to 4-hydroxy-N-DMT (endoxifen), a potent antiestrogen, is mediated by CYP3A enzymes. However, the potential contribution of CYP3A5...
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