Clomegestone (clomagestone) is an investigational steroidal progestogen. Clomegestone exhibits anti-estrogenic activity in estrone stimulated immature mice when administered orally at 100 ug.

Inocoterone acetate (USAN) (also known as RU-38882, RU-882) is the acetate ester of inocoterone a steroid-like nonsteroidal antiandrogen (NSAA) that was developed for topical administration to treat acne but was never marketed. Inocoterone acetate is actually not a silent antagonist of the androgen receptor but rather a weak partial agonist, similarly to steroidal antiandrogens like cyproterone acetate. In this double-blind study of 126 male subjects with acne, a topical solution of the antiandrogen inocoterone produced a modest but statistically significant reduction in the number of inflammatory acne lesions.

Delmadinone is a steroid with progestogenic, anti-androgenic and weak glucocorticoid action, synthesized in Syntex S.A. Acetate ester of delmadinone is used in veterinary under tradenames Tardak for cats and dogs for the treatment of excessive or aberrant sexual behaviour, including vagrancy, for the relief of prostatic hypertrophy, circum-anal tumors and for the treatment of certain forms of aggressiveness, nervousness, epileptiform seizures and corticosteroid-resistant pruritus. Delmadinone acetate blocks androgen receptors inhibit 5-reductase, which catalyzes the transformation of testosterone to the more potent androgen 5-dihydrotestosterone and decreases the production of testosterone by inhibiting gonadotropin release.

Clogestone Acetate (AY-11440) is a steroidal progestin that was synthesized in 1964 and was investigated as a progestin-only contraceptive but was never marketed.

Trestolone is a synthetic androgen that inhibits the release of follicle-stimulating hormone and impairs spermatogenesis. Luteinizing hormone is also suppressed, which cuts production of testosterone. The azoospermia and oligospermia are reversible after discontinuation of trestolone. Trestolone has androgenic and anabolic properties and loss of secondary sex characteristics is not seen. Like testosterone, trestolone undergoes enzymatic aromatization to an estrogen. The use of trestolone instead of testosterone for androgen replacement therapy could have health-promoting effects by reducing the occurrence of prostate disease. Trestolone had been in phase II clinical trial for the andropause control. However, this development was discontinued.

Stenbolone is an anabolic–androgenic steroid of the dihydrotestosterone group patented by Schering AG but never marketed. Ester prodrug of stenbolone is used as an anabolic–androgenic steroid for depot intramuscular injection under the brand names Anatrofin and Stenobolone.

Nisterime is a dihydrotestosterone derivative. Nisterime acetate (ORF-9326) was shown to inhibit implantation in several species. It is also interrupts the postimplantation stage of gestation.