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 Testosterone, the major endogenous androgen and the target mediator of antiandrogens.
This is a list of antiandrogens,[1] or drugs that prevent the effects of androgens like testosterone and dihydrotestosterone (DHT).[2] 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.[3] In addition, it includes both steroidal antiandrogen (SAAs) and nonsteroidal antiandrogen (NSAAs).
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
- 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
 Dutasteride, a 5α-reductase inhibitor and by extension a DHT synthesis inhibitor.
These drugs selectively inhibit the synthesis of DHT without affecting that of testosterone.
Antigonadotropins
 Leuprorelin, a GnRH agonist and hence an antigonadotropin.
See also
References
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Androgens
(incl. AASTooltip anabolic–androgenic steroid) | |
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| Antiandrogens | | ARTooltip Androgen receptor antagonists | |
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Steroidogenesis
inhibitors | |
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| 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)
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| Others | |
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GnRH modulators
(incl. analogues) | |
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| Gonadotropins | |
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Others
(indirect) | | Progonadotropins | |
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| 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)
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| ARTooltip Androgen receptor | | Agonists | |
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| SARMsTooltip Selective androgen receptor modulator | |
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| Antagonists | |
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| GPRC6A | |
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