Tamoxifen is a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. Although it is an antagonist of ER action in breast tissue, it acts as an ER agonist in bone and blood vessels and a partial ER agonist in uterine tissues. α-hydroxy Tamoxifen is a reactive metabolite of tamoxifen that is formed by the action of cytochrome P450 3A4 in human liver. It can be further converted into genotoxic DNA adducts though a mechanism involving reversible O-sulfonation of the hydroxyl moiety, which in rats has been linked with hepatocarcinoma.
화학적 성질
Pale Yellow Solid
용도
A metabolite of the chemotherapeutic drug tamoxifen. Exhibits a more potent estrogen agonist/antagonist activity than the parent drug. Also active as an intramembranous inhibitor of lipid peroxidation.
