List 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.

Testosterone, the major endogenous androgen and the target mediator of antiandrogens.

Androgen receptor antagonists

Steroidal antiandrogens

Cyproterone acetate, the most widely used steroidal antiandrogen.

17α-Hydroxyprogesterone derivatives
19-Norprogesterone derivatives
- Nomegestrol acetate
19-Nortestosterone derivatives
- Dienogest
- Oxendolone
17α-Spirolactone derivatives
- Drospirenone
- Spironolactone
Others
- Medrogestone

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
- Cimetidine
- Topilutamide

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

Aminoglutethimide

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.

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)

gollark: > it might not be portable to other places.I have explained why I think this.

gollark: It's interesting to actually look at the ethics and underlying causes and whatever instead of just "no discussing this"? We have a cool and rare thing here and it might not be portable to other places.

gollark: Well, you might have, but we don't seem to have had particularly in-depth discussions of possibilities, and one person looking over it isn't great.

gollark: This is obviously just heav trying to speak gollariously, ignore it.

gollark: > Isolating that elsewhere is also not good for various reasons I indicated before.

References

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