ERβ antagonist
Estrogen receptor beta (ERβ) antagonist
- Removes ERβ’s antiproliferative counterbalance to ERα
- Net tissue effect depends on the ERα/ERβ balance in that tissue
- Blocks ERβ — removes its antiproliferative, ERα-counterbalancing tone
Drugs with this mechanism (3)
- Clomiphene — Estrogen-receptor modulator that induces ovulation.
- Endoxifen — Tamoxifen's potent active metabolite — made by CYP2D6, which is why 2D6 inhibitors matter in breast cancer.
- Raloxifene — SERM that protects bone and lowers breast-cancer risk without stimulating the uterus.
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