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
Drugs with this mechanism (3)
- Clomiphene — Estrogen-receptor modulator that induces ovulation.
- Endoxifen — Potent active tamoxifen metabolite made by CYP2D6; hence 2D6 inhibitors matter in breast cancer.
- Raloxifene — SERM that protects bone and lowers breast-cancer risk without stimulating the uterus.
Self-check
- What antiproliferative influence is lost with ERβ blockade?
ERβ’s counterbalance to ERα. - What determines the tissue effect of ERβ blockade?
The tissue’s ERα/ERβ balance.
All mechanisms · Open ERβ antagonist in the interactive console ↗