Drug intelligence / Profile preview

estetrol + drospirenone

Development stage
Phase 4
Lead developer
Mithra Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Estetrol + drospirenone is a fixed-dose combination oral contraceptive containing estetrol, a plant-synthesized natural estrogen, and drospirenone, a well-established progestin. Estetrol acts as an agonist at estrogen receptor alpha (ERα) with tissue-selective activity and behaves as a selective estrogen receptor modulator. Drospirenone is an analog of spironolactone with anti-mineralocorticoid and antiandrogenic properties, acting as an antagonist at mineralocorticoid and androgen receptors while being an agonist at the progesterone receptor. The primary mechanism of action for this combination is suppression of ovulation to prevent pregnancy. Estetrol/drospirenone was developed to offer effective contraception with potentially lower thrombotic risk compared to traditional ethinylestradiol-containing pills[3][6][7]. It was approved in 2021 in Canada, the US, and Europe for use as a combined oral contraceptive[6][7].

Brand names
NextstellisDrovelisLydisilka
Other names
estetrol + drospirenonedrospirenone/estetrol
02

Targets

AR (Adrenergic receptors)PR (Progesterone receptor)MR (Mineralocorticoid receptor)ESR1 (ERα)

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