This is a list of steroidal antiandrogens.

Progesterone derivatives

11α-Hydroxyprogesterone 11α-Hydroxyprogesterone (11α-OHP), or 11α-hydroxypregn-4-ene-3,20-dione is an endogenous steroid and metabolite of progesterone. It is a weak antiandrogen, and is devoid of androgenic, estrogenic, and progestogenic activity. 11α-OHP was in ...

= 11α-hydroxyprogesterone *

Chlormadinone acetate Chlormadinone acetate (CMA), sold under the brand names Belara, Gynorelle, Lutéran, and Prostal among others, is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy, as a component of menopausal hor ...

= 17α-acetoxy-6-chloro-δ⁶-progesterone * Clometerone (L-38000) = 6α-chloro-16α-methylprogesterone *

Cyproterone Cyproterone, also known by its developmental code name SH-80881, is a steroidal antiandrogen which was studied in the 1960s and 1970s but was never introduced for medical use. It is an analogue of cyproterone acetate (CPA), an antiandrogen, p ...

(SH-80881) = 1,2α-methylene-6-chloro-δ⁶-17α-hydroxyprogesterone *

Cyproterone acetate Cyproterone acetate (CPA), sold alone under the brand name Androcur or with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the treatment of androgen-dependent condition ...

= 1,2α-methylene-6-chloro-δ⁶-17α-acetoxyprogesterone * Edogestrone (PH-218) = 17α-acetoxy-3,3-ethylenedioxy-6-methylpregn-5-en-20-one *

Medrogestone Medrogestone, sold under the brand name Colprone among others, is a progestin medication which has been used in menopausal hormone therapy and in the treatment of gynecological disorders. It is available both alone and in combination with an est ...

= 6,17α-dimethyl-δ⁶-progesterone *

Megestrol acetate Megestrol acetate (MGA), sold under the brand name Megace among others, is a progestin medication which is used mainly as an appetite stimulant to treat wasting syndromes such as cachexia.https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/ ...

= 17α-acetoxy-δ⁶-6-methylprogesterone *

Nomegestrol acetate Nomegestrol acetate (NOMAC), sold under the brand names Lutenyl and Zoely among others, is a progestin medication which is used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders.http://www.ema. ...

= 17α-acetoxy-δ⁶-6-methyl-19-norprogesterone *

Osaterone acetate Osaterone (developmental code name TZP-5258), also known as 17α-hydroxy-6-chloro-2-oxa-6-dehydroprogesterone, as well as 2-oxachloromadinone, is a steroidal antiandrogen and progestin that was never marketed. The C17α acetate ester In chem ...

(TZP-4238) = 17α-acetoxy-6-chloro-2-oxa-δ⁶-progesterone

Testosterone derivatives

Abiraterone Abiraterone acetate, sold under the brand name Zytiga among others, is a medication used to treat prostate cancer. Specifically it is used together with a corticosteroid for metastatic castration-resistant prostate cancer (mCRPC) and metastat ...

(CB-7598) = 17-(3-pyridinyl)androsta-5,16-dien-3β-ol *

Abiraterone acetate Abiraterone acetate, sold under the brand name Zytiga among others, is a medication used to treat prostate cancer. Specifically it is used together with a corticosteroid for metastasis, metastatic Prostate cancer#Castration-resistant cancer, ca ...

= 17-(3-pyridinyl)androsta-5,16-dien-3β-ol acetate * Benorterone (SKF-7690, FC-612) = 17α-methyl-''B''-nortestosterone * BOMT (Ro 7-2340) = 6α-bromo-4-oxa-17α-methyl-4,5α-dihydrotestosterone * Delanterone (GBR-21162) = 17β-dehydroxy-1α-methyl-δ¹⁶-testosterone *

Dienogest Dienogest, sold under the brand name Visanne among others, is a progestin medication which is used in birth control pills and in the treatment of endometriosis. It is also used in menopausal hormone therapy and to treat heavy periods. Dienogest ...

= 17α-cyanomethyl-19-nor-δ⁹⁽¹⁰⁾-testosterone *

Epitestosterone Epitestosterone, or isotestosterone, also known as 17α-testosterone or as androst-4-en-17α-ol-3-one, is an endogenous steroid and an epimer of the androgen sex hormone testosterone. It is a weak competitive antagonist of the androgen recepto ...

= 17α-epitestosterone * Galeterone (TOK-001, VN/124-1) = 17-(1H-benzimidazol-1-yl)androsta-5,16-dien-3β-ol * Metogest (SC-14207) = 16,16-dimethyl-19-nortestosterone *

Mifepristone Mifepristone, also known as RU-486, is a medication typically used in combination with misoprostol to bring about a medical abortion during pregnancy and manage early miscarriage. This combination is 97% effective during the first 63 days of ...

= 11β- -(dimethylamino)phenyl17-(1-propynyl)-δ⁹-19-nortestosterone *

Oxendolone Oxendolone, sold under the brand names Prostetin and Roxenone, is an antiandrogen and progestin medication which is used in Japan in the treatment of enlarged prostate. However, this use is controversial due to concerns about its clinical effic ...

(TSAA-291) = 16β-ethyl-19-nortestosterone * Rosterolone (SH-434, 17α-propylmesterolone) = 1α-methyl-17α-propyl-4,5α-dihydrotestosterone * Topterone (WIN-17665) = 17α-propyltestosterone *

Trimethyltrienolone Trimethyltrienolone (TMT), also known by its developmental code name R-2956 or RU-2956, is an antiandrogen medication which was never introduced for medical use but has been used in scientific research. Side effects Due to its close relation to m ...

(R-2956, RU-2956) = 2α,2β,17α-trimethyl-19-nor-δ^9,11-testosterone * Zanoterone (WIN-49596) = (5α,17α)-1'-(methylsulfonyl)-1'-H-pregn-20-yno ,2-cyrazol-17-ol

Spirolactone derivatives

SC-5233 SC-5233, also known as 6,7-dihydrocanrenone or 20-spirox-4-ene-3,20-dione, is a synthetic, steroidal antimineralocorticoid of the spirolactone group which was developed by G. D. Searle & Company in the 1950s but was never marketed. It was the fi ...

(spirolactone) = 17α-(2-carboxyethyl)testosterone γ-lactone *

SC-8109 SC-8109 is a steroidal antimineralocorticoid of the spirolactone group which was never marketed. It is a potent antagonist of the mineralocorticoid receptor and is more potent than the related drug SC-5233 (of which SC-8109 is the 19-nor analog ...

= 19-norspirolactone *

Canrenone Canrenone, sold under the brand names Contaren, Luvion, Phanurane, and Spiroletan, is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone which is used as a diuretic in Europe, including in Italy and Belgium. It ...

(aldadiene) = Δ⁶-spirolactone *

Dicirenone Dicirenone (International Nonproprietary Name, INN, United States Adopted Name, USAN; developmental code name SC-26304; also known as 7α-carboxyisopropylspirolactone) is a synthetic compound, synthetic, steroidal antimineralocorticoid of the spi ...

(SC-26304) = 7α-carboxyisopropylspirolactone *

Drospirenone Drospirenone is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy and in menopausal hormone therapy, among other uses. It is available both alone under the brand name Slynd and in combination wi ...

= 6β,7β:15β,16β-dimethylenespirolactone * Mespirenone (ZK-94679) = Δ¹-7α-acetylthio-15β,16β-methylenespirolactone *

Mexrenone Mexrenone (code names ZK-32055, SC-25152) is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. It is the lactonic form of mexrenoic acid (mexrenoate), and mexrenoate potassium (SC-2 ...

(ZK-32055, SC-25152) = 7α-(methoxycarbonyl)spirolactone *

Prorenone Prorenone (developmental code name SC-23133) is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed. It is the lactonic form of prorenoic acid (prorenoate), and prorenoate potassium (S ...

(SC-23133) = 6α,7α-methylenespirolactone *

Spironolactone Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease. It is also used in the treatment of high blood press ...

= 7α-acetylthiospirolactone *

Spirorenone Spirorenone (INN) (developmental code name ZK-35973) is a steroidal antimineralocorticoid of the spirolactone group that was never marketed. Spirorenone possesses 5–8 times the antimineralocorticoid activity of spironolactone in animal studies ...

(ZK-35973) = Δ¹-6β,7β:15β,16β-dimethylenespirolactone *

Spiroxasone Spiroxasone (, ) is a synthetic, steroidal antimineralocorticoid of the spirolactone group which was developed as a diuretic and antihypertensive agent but was never marketed. It was synthesized and assayed in 1963. The drug is 7α-acetylthi ...

= 7α-acetylthiospirolactone with the ketone group removed from the C17α spirolactone ring

Cortisol derivatives

* 9,11-Dehydrocortexolone 17α-butyrate (CB-03-04) = 17α-(butyryloxy)-9,11-didehydrodeoxycorticosterone * Clascoterone (CB-03-01; cortexolone 17α-propionate, 11-deoxycortisol 17α-propionate) = 17α-(propionyloxy)deoxycorticosterone

Others

* Guggulsterone = pregna-4,17-diene-3,16-dione * Nordinone = 11α-hydroxy-17,17-dimethyl-18-norandrosta-4,13-dien-3-one

Progesterone derivatives

Testosterone derivatives

Spirolactone derivatives

Cortisol derivatives

Others

See also