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Testosterone , the major
endogenous androgen and the
target mediator of
antiandrogens .
This is a list of antiandrogens , or drugs that prevent the effects of androgens like testosterone and dihydrotestosterone (DHT). It includes direct antagonists of the androgen receptor (AR), androgen synthesis inhibitors like 5α-reductase inhibitors and CYP17A1 inhibitors , and antigonadotropins like GnRH analogues , estrogens , and progestogens . In addition, it includes both steroidal antiandrogen (SAAs) and nonsteroidal antiandrogen (NSAAs). Only antiandrogens that have been marketed are included in this list.
Androgen receptor antagonists [ ]
Steroidal antiandrogens [ ]
Cyproterone acetate , the most widely used steroidal antiandrogen.
Note that in addition to acting as AR antagonists, most SAAs also act as potent progestogens and therefore antigonadotropins.
Note that this list does not include pure progestogens, only SAAs also acting as AR antagonists.
Nonsteroidal antiandrogens [ ]
Bicalutamide , the most widely used nonsteroidal antiandrogen.
First-generation
Bicalutamide
Flutamide
Nilutamide
Second-generation
Others/non-generational
Note that, in contrast to most SAAs, NSAAs are pure/selective AR antagonists with no antigonadotropic activity.
Androgen synthesis inhibitors [ ]
CYP17A1 inhibitors [ ]
Abiraterone acetate , a
CYP17A1 inhibitor and by extension an androgen synthesis inhibitor.
CYP11A1 (P450scc) inhibitors [ ]
5α-Reductase inhibitors [ ]
Alfatradiol
Dutasteride
Epristeride
Finasteride
Saw palmetto extract
These drugs selectively inhibit the synthesis of DHT without affecting that of testosterone.
Antigonadotropins [ ]
Leuprorelin , a
GnRH agonist and hence an
antigonadotropin .
Main article: Antigonadotropin
Estrogens (e.g., estradiol (and its esters ), ethinylestradiol , conjugated estrogens , diethylstilbestrol )
GnRH analogues
GnRH agonists (e.g., goserelin , leuprorelin )
GnRH antagonists (e.g., cetrorelix )
Progestogens (e.g., chlormadinone acetate , cyproterone acetate , gestonorone caproate , medroxyprogesterone acetate , megestrol acetate )
See also [ ]
References [ ]
Androgens and antiandrogens
Androgens (incl. AAS )
AR agonists
Testosterone derivatives: Androstenediol dipropionate
Boldenone undecylenate
Clostebol
Clostebol acetate
Clostebol caproate
Clostebol propionate
Cloxotestosterone acetate
Prasterone (dehydroepiandrosterone, DHEA)
Prasterone enanthate (DHEA enanthate)
Prasterone sulfate (DHEA sulfate)
Quinbolone
Testosterone #
Testosterone esters (e.g., testosterone cypionate , testosterone enanthate , testosterone propionate , testosterone undecanoate , testosterone ester mixtures (Deposterona , Omnadren , Sustanon , Testoviron Depot ))
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
Antigonadotropins
D2 receptor antagonists (prolactin releasers ) (e.g., domperidone , metoclopramide , risperidone , haloperidol , chlorpromazine , sulpiride )
Estrogens (e.g., bifluranol , diethylstilbestrol , estradiol , estradiol esters , ethinylestradiol , ethinylestradiol 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 )
Others
# WHO-EM
‡ Withdrawn from market
Clinical trials :
† Phase III
§ Never to phase III
See also
Androgen receptor modulators
Estrogens and antiestrogens
Progestogens and antiprogestogens
List of androgens/anabolic steroids
GnRH modulators (incl. analogues )
Agonists
Peptide: Azagly-nafarelin
Buserelin
Deslorelin
Fertirelin
Gonadorelin
Goserelin
Histrelin
Lecirelin
Leuprorelin (leuprolide)
Nafarelin
Peforelin
Triptorelin
Antagonists
Peptide: Abarelix
Cetrorelix
Degarelix
Ganirelix
Gonadotropins
Preparations
Follicle-stimulating hormone
Human chorionic gonadotropin
Luteinizing hormone
Menotropin
Urofollitropin
Others (indirect)
Progonadotropins
Sex steroid antagonists (via disinhibition of the HPG axis ): Antiandrogens (e.g., flutamide , bicalutamide , enzalutamide )
Antiestrogens /SERMs (e.g., tamoxifen , clomifene , enclomifene )
Aromatase inhibitors (e.g., anastrozole )
GnRH agonists (e.g., GnRH )
Antigonadotropins
Sex steroid agonists (via negative feedback on the HPG axis ): Androgens /anabolic steroids (e.g., testosterone , nandrolone esters , oxandrolone )
D2 receptor antagonists (prolactin releasers ) (incl., domperidone , metoclopramide , risperidone , haloperidol , chlorpromazine , sulpiride )
Estrogens (incl., bifluranol , estradiol , estradiol esters , ethinylestradiol , diethylstilbestrol , paroxypropione )
Progestogens (incl. progestins , e.g., chlormadinone acetate , cyproterone acetate , hydroxyprogesterone caproate , gestonorone caproate , medroxyprogesterone acetate , megestrol acetate )
Others (mixed or unknown mechanism of action): Danazol
Gestrinone
Metallibure
# WHO-EM
‡ Withdrawn from market
Clinical trials :
† Phase III
§ Never to phase III
See also
GnRH and gonadotropin receptor modulators
Androgens and antiandrogens
Estrogens and antiestrogens
Progestogens and antiprogestogens
AR
Agonists
17α-Ethynyl-19-nortestosterone derivatives: Δ4 -Tibolone
Desogestrel
Etonogestrel
Etynodiol
Gestodene
Gestrinone
Levonorgestrel
Levonorgestrel esters (e.g., levonorgestrel butanoate )
Lynestrenol
Norethisterone
Norethisterone esters (e.g., norethisterone acetate , norethisterone enanthate )
Norgestrel
Norgestrienone
Quingestanol
Tibolone
Mixed (SARMs ) Antagonists
GPRC6A
Agonists
Cations (incl. aluminum , calcium , gadolinium , magnesium , strontium , zinc )
Dehydroandrosterone
Dihydrotestosterone
Estradiol
L -α-Amino acids (incl. L -arginine , L -lysine , L -ornithine )
Osteocalcin
SHBG
Testosterone