Synonyms: 15 α-hydroxyestriol | 15 alpha-hydroxyestriol | Drovelis® (EMA); ; estetrol monohydrate + drospirenone | E4 | Lydisilka® (EMA); ; estetrol monohydrate + drospirenone | Nextstellis® (US); estetrol monohydrate + drospirenone
estetrol is an approved drug (EMA & FDA (2021))
Compound class:
Synthetic organic
Comment: Estetrol is a natural estrogen that is produced exclusively during pregnancy by the fetal liver. It is produced synthetically (from a plant source) for medicinal use. Estetrol has tissue selective actions [4-5], with estrogenic activity in the uterus, vagina and endometrium and estrogen antagonist activity in breast tissue.
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Bioactivity Comments |
Dissociation constants derived from in vitro binding assays are provided in patent WO2004006936A1 [1]. Ki vs. ERα is 4.9 nM, and vs. ERβ the Ki is 19 nM. For both receptor subtypes estetrol was displacing [3H]17β-estradiol ([3H]estradiol). |