Tissue-selective ERα partial agonist
Tissue-selective estrogen receptor alpha (ERα) partial agonist
- Agonist in bone/lipids, antagonist in breast
- Tissue-selective ("SERM") behavior — also agonist in endometrium
- Net effect set by tissue coactivator/corepressor context
- ↑ thromboembolism risk
- Hot flashes
Drugs with this mechanism (6)
- Bazedoxifene — SERM paired with conjugated estrogens to protect the endometrium without a progestin; thromboembolism risk remains.
- Clomiphene — Estrogen-receptor modulator that induces ovulation.
- Ospemifene — Oral SERM for dyspareunia from vulvovaginal atrophy.
- Raloxifene — SERM that protects bone and lowers breast-cancer risk without stimulating the uterus.
- 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
- How does tissue-selective ERα partial agonism differ between bone and breast?
Agonism in bone; antagonism in breast. - What sets the net tissue effect of an ERα partial agonist?
Coactivator/corepressor context.
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