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Tamoxifen is an antagonist of the Estrogen receptor in breast tissue via its active metabolite, 4-hydroxytamoxifen.

Tamoxifen is the usual endocrine (anti-estrogen) therapy for ER+ Breast cancer in pre-menopausal women, and is also a standard in post-menopausal women although aromatase inhibitors are also frequently used in that setting.

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