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Estetrol is an estrogen used in combination with drospirenone for oral contraception.
Estetrol is an estrogen used in combination with drospirenone for oral contraception.
Estetrol is a synthetic analogue of a naturally occurring estrogen present during pregnancy, demonstrating selectivity for both estrogen receptor-α (ER-α) and ER-β and suppressing ovulation. Estetrol binds with a low to moderate affinity human estrogen receptor alpha (ER alpha) and ER beta with a preference for ER alpha. Estetrol demonstrates a unique mechanism of action via tissue selective activity, showing estrogen receptor agonist activity on the vagina, the uterus and the endometrium, and negative estrogenic activity on breast tissue.
Estetrol is indicated in combination with drospirenone for the prevention of pregnancy.