Promegestone (R 5020) is a potent progestin devoid of androgenic side-effects and has marked anti-estrogenic activity. Promegestone is an AChR noncompetitive antagonist that may alter AChR function by interactions at the lipid-protein interface. Promegestone is used in the treatment of gynecological disorders due to luteal insufficiency.

Norgestrienone is a synthetic progwstin which was used as an oral contraceptive under the names Ogyline and Planor.

Gestonorone is a progesterone analogue indicated for the treatment of benign prostatic hyperplasia and endometrial cancer. The drug is approved in many countries and used under the names Primostat and Depostat.

Normethandrone (Orgasteron; Metalutin; Methalutin) is a progestin and androgen/anabolic steroid agent which is used in combination with an estrogen in the treatment of menstruation disorders in women. Normethandrone is a modified form of nandrolone. It differs by the addition of a methyl group at carbon 17-alpha to protect the hormone during oral administration. Normethandrone is aromatized by the body, and converts to a synthetic estrogen with a high level of biological activity (17alpha-methyl-estradiol). Orgasteron has been used as progestational agent and as an androgen. Normethandrone is available in combination with methylestradiol or estradiol valerate in a few countries, including Brazil, Indonesia, and Venezuela. This is a controlled substance (anabolic steroid): 21 CFR, 1308.13, as defined in 1300.01. Normethandrone was first described in 1954. Shortly after, it was developed into a medicine by Organon (now Merck/MSD), which introduced it under the Orgasterone brand name in Belgium and Switzerland, and as Orgasteron in the Netherlands. This steroid had also been sold by other manufacturers in various parts of Europe as Methalutin, Lutenin, and Matdonal. Although a simple oral methylated nandrolone, with strong properties as an anabolic steroid, Normethandrone exhibits such strong progestational activity that it was marketed as an oral progestin. Its anabolic effects were more looked at as secondary applications for the drug, and accounted for very little medical interest.

Cyproterone belongs to a group of medications known as steroidal antiandrogens. It suppresses testosterone and its metabolites. It has approximately three-fold lower potency as an antagonist of the androgen receptor relative to cyproterone acetate. Cyproterone acetate is used to treat advanced prostate cancer and acne.

Demegestone, a norprogesterone derivative, is a progesterone receptor agonist that was previously used to treat luteal insufficiency. It was marketed in France as Lutionex, but has since been discontinued. Demegestone has also been studied in combination with estrogens as an oral contraceptive and treatment for infertility. Demegestone did not exercise androgenic activity. Demegestone is the potent inhibitor of estrone sulfatase activity.

Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog, which is used in topical estrogen therapy. Promestriene’s potential for treating vaginal atrophy symptoms associated with aromatase inhibitor treatment would be precluded if its minimal absorption leads to estrogen-like effects on cell proliferation and estrogen-responsive gene expression. The concern with absorbed vaginal estrogens or estrogen analogs is that they activate occult sites of residual breast cancer or negate the tumor suppressive effects of aromatase inhibitor adjuvant therapy. Promestriene has been studied in phase IV of the clinical trial on improvement of hormonal cytology, local and systemic climacteric complaints, as well as its endometrial security in patients with vaginitis atrophic pelvic; organ prolapse and endometrial hyperplasia. It has been also studied in phase III of the clinical trial in the post-operative patients with hypospadias. In addition, promestriene was in phase IV of the clinical trial to study its treatment of patients with vaginosis, bacterial, but that studied was terminated.

Moxestrol (11β-methoxy-17-ethynyl-estradiol) is estrogen receptor agonist. It is used in the studies of estrogen receptor activity and distribution. Moxestrol is rapidly metabolized by the liver. Hydroxylation was the main transformation pathway. Moxestrol yielded metabolites hydroxylated (or methoxylated) at C-2, C-15 and C-16, but not at C-6, and also gave rise to D-homo derivatives. It was considered as a potentially effective drug in the treatment of postmenopausal disturbances.

Cyclofenil is a anti-estrogen drug developed for the treatment of female infertility and for induction of ovulation. Cyclofenil exerts its action by binding to estrogen receptor beta and demonstrates agonism or antagonism depending on tissues type. The drug was withdrawn from the market due to high risk of hepatotoxicity.

Lasofoxifene is an active component of Fablyn. Fablyn is used for the treatment of osteoporosis in postmenopausal women. Lasofoxifene is a nonsteroidal selective estrogen receptor modulator. Lasofoxifene has no effect on CYP2E1- or CYP2D6-mediated drug metabolism and should not affect drugs metabolized by other cytochrome P450 isoenzymes. Common adverse reactions considered to be related to Fablyn therapy were muscle spasms, hot flush and vaginal discharge. Lasofoxifene approved in the EU in 2009 is now withdrawn from use in the European Union.