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ERα antagonist

• Blocks ERα-driven transcription — antiproliferative in breast tissue
• Estrogen-deprivation effects — hot flashes

Drugs with this mechanism (2)

• Endoxifen — Tamoxifen's potent active metabolite — made by CYP2D6, which is why 2D6 inhibitors matter in breast cancer.
• Vepdegestrant — Oral PROTAC estrogen-receptor degrader for ESR1-mutated ER-positive/HER2-negative advanced breast cancer after endocrine therapy.

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