List of steroidal antiandrogens

Cyproterone acetate, the most well-known and widely used steroidal antiandrogen.

Steroid ring system.

This is a list of steroidal antiandrogens.

Progesterone derivatives

11α-Hydroxyprogesterone = 11α-hydroxyprogesterone
Chlormadinone acetate = 17α-acetoxy-6-chloro-δ⁶-progesterone
Clometerone (L-38000) = 6α-chloro-16α-methylprogesterone
Cyproterone (SH-80881) = 1,2α-methylene-6-chloro-δ⁶-17α-hydroxyprogesterone
Cyproterone acetate = 1,2α-methylene-6-chloro-δ⁶-17α-acetoxyprogesterone
Edogestrone (PH-218) = 17α-acetoxy-3,3-ethylenedioxy-6-methyl-5-pregnen-20-one
Medrogestone = 6,17α-dimethyl-δ⁶-progesterone
Megestrol acetate = 17α-acetoxy-δ⁶-6-methylprogesterone
Nomegestrol acetate = 17α-acetoxy-δ⁶-6-methyl-19-norprogesterone
Osaterone acetate (TZP-4238) = 17α-acetoxy-6-chloro-2-oxa-δ⁶-progesterone

Testosterone derivatives

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 = 17α-cyanomethyl-19-nor-δ⁹⁽¹⁰⁾-testosterone
Epitestosterone = 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 = 11β-[p-(dimethylamino)phenyl]-17-(1-propynyl)-δ⁹-19-nortestosterone
Oxendolone (TSAA-291) = 16β-ethyl-19-nortestosterone
Rosterolone (SH-434, 17α-propylmesterolone) = 1α-methyl-17α-propyl-4,5α-dihydrotestosterone
Topterone (WIN-17665) = 17α-propyltestosterone
Trimethyltrienolone (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[3,2-c]pyrazol-17-ol

Spirolactone derivatives

SC-5233 (spirolactone) = 17α-(2-carboxyethyl)testosterone γ-lactone
SC-8109 = 19-norspirolactone
Canrenone (aldadiene) = Δ⁶-spirolactone
Dicirenone (SC-26304) = 7α-carboxyisopropylspirolactone
Drospirenone = 6β,7β:15β,16β-dimethylenespirolactone
Mespirenone (ZK-94679) = Δ¹-7α-acetylthio-15β,16β-methylenespirolactone
Mexrenone (ZK-32055, SC-25152) = 7α-(methoxycarbonyl)spirolactone
Prorenone (SC-23133) = 6α,7α-methylenespirolactone
Spironolactone = 7α-acetylthiospirolactone
Spirorenone (ZK-35973) = Δ¹-6β,7β:15β,16β-dimethylenespirolactone
Spiroxasone = 7α-acetylthiospirolactone with the ketone group removed from the C17α spirolactone ring

Others

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

Notes

^? = Chemical names that are unverified.

Androgens and antiandrogens

Androgens
(incl. AAS)

AR agonists	Testosterone derivatives: Boldenone undecylenate Clostebol Clostebol acetate Clostebol caproate Clostebol propionate Cloxotestosterone acetate Dehydroepiandrosterone (DHEA) (androstenolone, prasterone) DHEA enanthate (prasterone enanthate) Quinbolone Testosterone^# Testosterone acetate Testosterone capropate Testosterone cyclohexylpropionate Testosterone cypionate Testosterone decanoate Testosterone enanthate Testosterone ester mixtures (Deposterona, Omnadren, Sustanon) Testosterone furoate Testosterone hexahydrobenzoate Testosterone hexahydrobenzylcarbonate Testosterone hexyloxyphenylpropionate Testosterone isobutyrate Testosterone isocaproate Testosterone ketolaurate Testosterone nicotinate Testosterone phenylacetate Testosterone phenylpropionate Testosterone phosphate Testosterone propionate Testosterone undecanoate Testosterone valerate Dihydrotestosterone derivatives: Bolazine capronate Dihydrotestosterone (DHT) (androstanolone, stanolone) Dihydrotestosterone acetate Dihydrotestosterone benzoate Dihydrotestosterone butyrate Dihydrotestosterone enanthate Dihydrotestosterone formate Dihydrotestosterone propionate Dihydrotestosterone valerate Drostanolone propionate (dromostanolone propionate) Epitiostanol Mepitiostane Mesterolone Metenolone acetate (methenolone acetate) Metenolone enanthate (methenolone enanthate) Stenbolone acetate 19-Nortestosterone derivatives: Bolandiol dipropionate Nandrolone caproate Nandrolone cypionate Nandrolone cyclohexanecarboxylate Nandrolone cyclohexylpropionate Nandrolone decanoate Nandrolone furylpropionate Nandrolone hexyloxyphenylpropionate Nandrolone hydrogen succinate Nandrolone laurate Nandrolone phenylpropionate Nandrolone propionate Nandrolone sulfate sodium Nandrolone undecanoate Norclostebol Norclostebol acetate Oxabolone cipionate (oxabolone cypionate) Trenbolone acetate Trenbolone hexahydrobenzylcarbonate (trenbolone cyclohexylmethylcarbonate) 17α-Alkylated testosterone derivatives: Bolasterone Calusterone Chlorodehydromethyltestosterone (CDMT) Fluoxymesterone Formebolone Metandienone (methandienone, methandrostenolone) Methandriol (methylandrostenediol) Methandriol bisenanthoyl acetate Methandriol dipropionate Methandriol propionate Methyltestosterone Oxymesterone Penmesterol Tiomesterone (thiomesterone) 17α-Alkylated dihydrotestosterone derivatives: Androisoxazole Furazabol Mebolazine (dimethazine) Mestanolone Oxandrolone Oxymetholone Stanozolol 17α-Alkylated 19-nortestosterone derivatives: Ethylestrenol Mibolerone Norethandrolone Normethandrone (methylestrenolone, normethisterone) Propetandrol (propethandrol) 17α-Vinyltestosterone derivatives: Norvinisterone (vinylnortestosterone) 17α-Ethynyltestosterone derivatives: Danazol Gestrinone Progestins (e.g., ethisterone (ethynyltestosterone), levonorgestrel, norgestrel, norethisterone (norethindrone), lynestrenol, norgestrienone) Tibolone Progesterone derivatives: Medroxyprogesterone acetate

Progonadotropins	Antiestrogens (e.g., tamoxifen, clomifene) GnRH agonists (e.g., GnRH (gonadorelin), leuprorelin) Gonadotropins (e.g., LH, hCG)

Antiandrogens

AR antagonists

Steroidogenesis
inhibitors

5α-Reductase	Alfatradiol Dutasteride Epristeride Finasteride Saw palmetto extract

Others	Abiraterone acetate Aminoglutethimide Bifluranol Cyproterone acetate Flutamide Ketoconazole Nilutamide Seviteronel^† Spironolactone

Antigonadotropins

D₂ receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, sulpiride)
Estrogens (e.g., bifluranol, diethylstilbestrol, estradiol, estradiol esters, ethinyl estradiol, ethinyl estradiol sulfonate, paroxypropione)
GnRH agonists (e.g., leuprorelin)
GnRH antagonists (e.g., cetrorelix)
Progestogens (incl., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone caproate, gestonorone caproate, medroxyprogesterone acetate, megestrol acetate)

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

See also: Estrogens and antiestrogens • Progestogens and antiprogestogens • Glucocorticoids and antiglucocorticoids • Mineralocorticoids and antimineralocorticoids • Gonadotropins and GnRH

Androgen receptor modulators

Agonists	Testosterone derivatives: 4-Androstenediol 4-Androstenedione 4-Dehydroepiandrosterone (4-DHEA) 4-Hydroxytestosterone 5-Androstenediol 5-Androstenedione 11-Ketotestosterone 11β-Hydroxyandrostenedione Adrenosterone (11-ketoandrostenedione, 11-oxoandrostenedione) Atamestane Boldenone Boldenone undecylenate Boldione (1,4-androstadienedione) Clostebol Clostebol acetate Clostebol caproate Clostebol propionate Cloxotestosterone Cloxotestosterone acetate DHEA (androstenolone, prasterone; 5-DHEA) DHEA enanthate (prasterone enanthate) DHEA sulfate Exemestane Formestane Plomestane Quinbolone Silandrone Testosterone^# Testosterone acetate Testosterone acetate butyrate Testosterone acetate propionate Testosterone benzoate Testosterone butyrate Testosterone buciclate Testosterone capropate Testosterone cyclohexylpropionate Testosterone cypionate Testosterone decanoate Testosterone diacetate Testosterone dipropionate Testosterone enanthate Testosterone formate Testosterone furoate Testosterone hexahydrobenzoate Testosterone hexahydrobenzylcarbonate Testosterone hexyloxyphenylpropionate Testosterone isobutyrate Testosterone isocaproate Testosterone isovalerate Testosterone ketolaurate Testosterone nicotinate Testosterone palmitate Testosterone phenylacetate Testosterone phenylbutyrate Testosterone phenylpropionate Testosterone phosphate Testosterone propionate Testosterone stearate Testosterone sulfate Testosterone undecanoate Testosterone valerate Dihydrotestosterone derivatives: 1-Androstenediol 1-Androstenedione 1-Androsterone (1-andro, 1-DHEA) 1-Testosterone 3α-Androstanediol 5α-Androst-2-en-17-one 7β-Hydroxyepiandrosterone 11-Ketodihydrotestosterone Androsterone Bolazine Bolazine capronate Dihydrotestosterone (androstanolone, stanolone) Dihydrotestosterone acetate Dihydrotestosterone benzoate Dihydrotestosterone butyrate Dihydrotestosterone enanthate Dihydrotestosterone formate Dihydrotestosterone propionate Dihydrotestosterone valerate Drostanolone Drostanolone propionate Epiandrosterone Epitiostanol Mepitiostane Mesabolone Mesterolone Nisterime Nisterime acetate Prostanozol Stenbolone Stenbolone acetate 19-Nortestosterone derivatives: 7α-Methyl-19-norandrostenedione (MENT dione, trestione) 11β-Methyl-19-nortestosterone 11β-Methyl-19-nortestosterone dodecylcarbonate 19-Nor-5-androstenediol 19-Nor-5-androstenedione Bolandiol Bolandiol dipropionate Bolandione (19-nor-4-androstenedione) Bolmantalate (nandrolone adamantoate) Dienedione Dienolone Dimethandrolone Dimethandrolone buciclate Dimethandrolone dodecylcarbonate Dimethandrolone undecanoate LS-1727 (nandrolone 17β-N-(2-chloroethyl)-N-nitrosocarbamate) Methoxydienone (methoxygonadiene) Nandrolone Nandrolone acetate Nandrolone caproate Nandrolone cypionate Nandrolone cyclohexanecarboxylate Nandrolone cyclohexylpropionate Nandrolone cyclotate Nandrolone decanoate Nandrolone formate Nandrolone furylpropionate Nandrolone hexyloxyphenylpropionate Nandrolone hydrogen succinate Nandrolone laurate Nandrolone phenylpropionate Nandrolone propionate Nandrolone sulfate Nandrolone sulfate sodium Nandrolone undecanoate Norclostebol Norclostebol acetate Normethandrone (methylestrenolone, normethisterone) Oxabolone Oxabolone cipionate (oxabolone cypionate) Trenbolone Trenbolone acetate Trenbolone enanthate Trenbolone hexahydrobenzylcarbonate Trestolone (MENT) Trestolone acetate Dihydrotestosterone and 19-nortestosterone derivatives: 5α-Dihydronandrolone 19-Norandrosterone 17α-Alkylated testosterone derivatives: Bolasterone Calusterone Chlorodehydromethylandrostenediol (CDMA) Chlorodehydromethyltestosterone (CDMT) Chloromethylandrostenediol (CMA) Enestebol Ethyltestosterone Fluoxymesterone Formebolone Hydroxystenozole Metandienone (methandrostenolone) Methandriol (methylandrostenediol) Methandriol bisenanthoyl acetate Methandriol diacetate Methandriol dipropionate Methandriol propionate Methylclostebol (chloromethyltestosterone) Methyltestosterone Oxymesterone Penmesterol Tiomesterone 17α-Alkylated dihydrotestosterone derivatives: Androisoxazole Desoxymethyltestosterone Furazabol Mebolazine (dimethazine) Mestanolone Metenolone Metenolone acetate Metenolone enanthate Methasterone Methyl-1-testosterone Methylepitiostanol Methylstenbolone Oxandrolone Oxymetholone Stanozolol 17α-Alkylated 19-nortestosterone derivatives: Bolenol Dimethyltrienolone (7α-methylmetribolone, 7α,17α-dimethyltrenbolone) Ethyldienolone Ethylestrenol Methyldienolone Methylhydroxynandrolone (MOHN, MHN) Metribolone Mibolerone Norboletone Norethandrolone Propetandrol Tetrahydrogestrinone 17α-Vinyltestosterone derivatives: Norvinisterone (vinylnortestosterone) Vinyltestosterone 17α-Ethynyltestosterone derivatives: Δ⁴-Tibolone Chloroethynyl norgestrel Danazol Desogestrel Ethisterone (ethynyltestosterone) Etonogestrel Etynodiol Etynodiol diacetate Gestodene Gestrinone Levonorgestrel Levonorgestrel butanoate Lynestrenol Norethisterone Norethisterone acetate Norethisterone acetate oxime Norethisterone enanthate Norgestrel Norgestrienone Quingestanol Quingestanol acetate Tibolone Progesterone derivatives: Medroxyprogesterone acetate Others/unsorted: Cl-4AS-1

Mixed (SARMs)	Non-steroidal: 198RL26 ACP-105 AC-262,356 Acetothiolutamide Andarine (acetamidoxolutamide, androxolutamide, GTx-007, S-4) BMS-564,929 Enobosarm (ostarine, MK-2866, GTx-024, S-22) FTBU-1 GSK-4336A GSK-8698 LG-121071 (LGD-121071) LGD-2226 LGD-2941 (LGD-122941) LGD-3303 LGD-4033 JNJ-26146900 JNJ-28330835 JNJ-37654032 ORM-11984 RAD140 R-1 R-2 R-3 S-1 S-23 S-40503 S-101479 Steroidal: MK-0773 TFM-4AS-1 YK-11

Antagonists	Steroidal: 3α-Hydroxytibolone 3β-Hydroxytibolone 9,11-Dehydrocortexolone 17α-butyrate (CB-03-04) 11α-Hydroxyprogesterone 15β-Hydroxycyproterone acetate Abiraterone acetate Allyltestosterone Benorterone BOMT Canrenoic acid Canrenone Chlormadinone acetate Clometerone Cortexolone 17α-propionate (CB-03-01) Cyproterone Cyproterone acetate Delanterone Dienogest Drospirenone Edogestrone Epitestosterone Galeterone Guggulsterone Medrogestone Megestrol acetate Mespirenone Metogest Mexrenone Mifepristone Nomegestrol acetate Nordinone Osaterone Osaterone acetate Oxendolone Potassium canrenoate Prorenone Rosterolone SC-5233 (spirolactone) Spironolactone Spirorenone Topterone Trimethyltrienolone (R-2956) Zanoterone Non-steroidal: AA560 Apalutamide Atraric acid AZD-3514 BAY-1024767 Bicalutamide Bisphenols (e.g., BADGE, BFDGE, bisphenol A, bisphenol F, bisphenol S) BMS-641,988 Cimetidine Cioteronel Darolutamide DDT (via metabolite p,p’-DDE) Dieldrin DIMP Endosulfan Enzalutamide EPI-001 EPI-506 Fenarimol Flutamide Hydroxyflutamide Inocoterone Inocoterone acetate Ketoconazole Lavender oil LG-105 LG-120907 Linuron Methiocarb N-Butylbenzenesulfonamide N-Desmethylenzalutamide Nilutamide ONC1-13B ORM-15341 Pentomone PF-998425 Phenothrin Prochloraz Procymidone RU-22930 RU-58642 RU-58841 Seviteronel Thalidomide Topilutamide (fluridil) Valproic acid Vinclozolin

GPRC6A

Agonists	Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium) Dehydroandrosterone Dihydrotestosterone Estradiol L-α-Amino acids (incl. L-arginine, L-lysine, L-ornithine) Osteocalcin Testosterone

See also: Estrogenics • Glucocorticoidics • Mineralocorticoidics • Progestogenics • Steroid hormone metabolism modulators • List of androgens/anabolic steroids

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