ATC Group: G03X Other sex hormones and modulators of the genital system

Danazol is a synthetic steroid derived from ethisterone an is indicated for the treatment of endometriosis and benign fibrocystic breast disease.

Mifepristone is a synthetic steroid with an antiprogestational action as a result of competition with progesterone at the progesterone receptors.

Ospemifene and its major metabolite have an oestrogen like effect in the vagina increasing the cellular maturation and mucification of the vaginal epithelium. Ospemifene’s biological actions are mediated through the binding of ospemifene and its major metabolite to oestrogen receptors leading to activation of some oestrogenic pathways (agonism) and blockade of other (antagonism).

Prasterone, i.e. dehydroepiandrosterone (DHEA), biochemically and biologically identical to the endogenous human DHEA, is a precursor steroid which is inactive by itself and it is converted into oestrogens and androgens. Intrarosa is thus different from the oestrogens preparations since it delivers also androgen metabolites.

As a selective oestrogen receptor modulator (SERM), raloxifene has selective agonist or antagonist activities on tissues responsive to oestrogen. It acts as an agonist on bone and partially on cholesterol metabolism (decrease in total and LDL-cholesterol), but not in the hypothalamus or in the uterine or breast tissues.

Ulipristal is an orally-active synthetic selective progesterone receptor modulator which acts via high-affinity binding to the human progesterone receptor. When used for emergency contraception the mechanism of action is inhibition or delay of ovulation via suppression of the luteinising hormone (LH) surge. Pharmacodynamic data show that even when taken immediately before ovulation is scheduled to occur (when LH has already started to rise), ulipristal acetate is able to postpone follicular rupture for at least 5 days.