ERα antagonist
Estrogen receptor alpha (ERα) antagonist
- Antiproliferative in breast tissue → ↓ ER⁺ breast cancer growth
- Estrogen-deprivation effects — hot flashes
- 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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