ERα antagonist
Estrogen receptor alpha (ERα) antagonist
- Antiproliferative in breast tissue → ↓ ER⁺ breast cancer growth
- Estrogen-deprivation effects — hot flashes
Drugs with this mechanism (2)
- Endoxifen — Potent active tamoxifen metabolite made by CYP2D6; hence 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.
Self-check
- Which breast tumors are affected by ERα antagonism?
ER-positive tumors. - What estrogen-deprivation symptom can ERα antagonism cause?
Hot flashes.
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