ERβ partial agonist
Estrogen receptor beta (ERβ) partial agonist
- Modulates and counterbalances ERα-driven proliferation
- Net tissue effect depends on the ERα/ERβ balance in that tissue
Drugs with this mechanism (4)
- Bazedoxifene — SERM paired with conjugated estrogens to protect the endometrium without a progestin; thromboembolism risk remains.
- Ospemifene — Oral SERM for dyspareunia from vulvovaginal atrophy.
- Tamoxifen — The classic breast-cancer SERM; a prodrug activated by CYP2D6.
- Toremifene — SERM for metastatic breast cancer in postmenopausal patients; QT prolongation, thromboembolism, and endometrial cancer risks.
Self-check
- Which proliferative signal does partial ERβ activation counterbalance?
ERα-driven proliferation. - What determines the tissue effect of partial ERβ activation?
The tissue’s ERα/ERβ balance.
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