Drug intelligence / Profile preview

dydrogesterone + norethisterone acetate + ethinyl estradiol + drospirenone

Development stage
Discontinued
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination drug containing four active ingredients: dydrogesterone, norethisterone acetate, ethinyl estradiol, and drospirenone. All four are synthetic hormones used in various hormonal therapies and contraceptives. Dydrogesterone and norethisterone acetate are progestins (synthetic forms of progesterone), while ethinyl estradiol is a synthetic estrogen, and drospirenone is a progestin with additional antiandrogenic and antimineralocorticoid properties. - **Dydrogesterone** acts as an agonist at the progesterone receptor but does not inhibit ovulation; it is mainly used for luteal insufficiency, menstrual disorders, endometriosis, infertility due to luteal phase defects, premenstrual syndrome (PMS), menopausal hormone therapy (MHT), and prevention of miscarriage[9]. - **Norethisterone acetate** is also a progestin that acts as an agonist at the progesterone receptor; it is commonly combined with estrogens for contraception or hormone replacement therapy[6]. - **Ethinyl estradiol** is a potent synthetic estrogen that binds to the estrogen receptor to regulate reproductive function; it suppresses ovulation when combined with progestins[5][8]. - **Drospirenone** has multiple actions—it acts as an agonist at the progesterone receptor (progestogenic effect), antagonist at androgen receptors (antiandrogenic effect), antagonist at mineralocorticoid receptors (antimineralocorticoid effect), and weakly binds glucocorticoid receptors. It suppresses ovulation by inhibiting follicle-stimulating hormone (FSH) and luteinizing hormone (LH) release when combined with estrogens like ethinyl estradiol[3][7]. The combination of these agents would theoretically provide strong suppression of ovulation through multiple mechanisms—primarily via negative feedback on gonadotropins—and could be used for contraception or management of gynecological conditions such as endometriosis or severe menstrual disorders. However, there are no known marketed products containing all four agents together in one formulation.

02

Targets

PR (Progesterone receptor)GR (Glucocorticoid receptor)AR (Adrenergic receptors)MR (Mineralocorticoid receptor)ER (Estrogen receptor)

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