ERα agonist
Estrogen receptor alpha (ERα) agonist
- Nuclear receptor → gene transcription
- Drives endometrial and breast epithelial proliferation
- Relieves menopausal symptoms
- ↑ hepatic clotting-factor synthesis → thromboembolism risk
- ↓ bone resorption
- Classic nuclear receptor → transcriptional activation; proliferative/metabolic effects
- Drives endometrial and breast epithelial proliferation; ↑ hepatic clotting-factor synthesis → thromboembolism risk
Drugs with this mechanism (7)
- Conjugated estrogens — Estrogen mixture for menopausal symptoms.
- Estradiol — Principal human estrogen; available systemically or locally for menopausal symptoms.
- Estradiol transdermal — Skin-delivered estrogen for menopausal symptoms; avoids first-pass hepatic exposure.
- Estradiol vaginal — Local estrogen for menopausal genitourinary symptoms; little systemic exposure.
- Estriol — Relatively weak estrogen prominent in pregnancy; used vaginally for menopausal symptoms in some countries, but not FDA-approved.
- Estrone — Major circulating estrogen after menopause, formed largely by peripheral aromatization; interconverts with the more potent estradiol.
- Ethinyl estradiol — The synthetic estrogen in most combined oral contraceptives.
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