hydroxytamoxifen

**hydroxytamoxifen** (4-hydroxytamoxifen, 4-OHT) is a metabolite of the antiestrogen drug tamoxifen, produced by hepatic cytochrome P450 enzymes. It exhibits a significantly higher affinity for estrogen receptors than tamoxifen and other metabolites, and possesses 50-100 fold higher potency in inhibiting proliferation of both breast cancer and normal breast cells in vitro compared to tamoxifen itself[4]. hydroxytamoxifen acts primarily as a selective estrogen receptor modulator, functioning as both a partial antagonist and agonist at estrogen receptors depending on tissue context. It efficiently prevents estrogen-stimulated cell proliferation and modulates estrogen-responsive gene expression, contributing to tamoxifen's overall antineoplastic efficacy. In addition to its antiestrogenic effects, hydroxytamoxifen has demonstrated antioxidant properties, including inhibition of lipid peroxidation and protection against oxidative stress in mitochondria[4]. hydroxytamoxifen is used primarily as a research chemical and tool compound in cell biology and oncology studies. It is not approved as a stand-alone pharmaceutical agent in clinical practice.

Other names

4-OHT4-hydroxytamoxifen4-hydroxy-tamoxifen