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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 5ÃÂ±-reductase inhibitors and CYP17A1 inhibitors, and antigonadotropins like analogues, estrogens, and progestogens. In addition, it includes both steroidal antiandrogen (SAAs) and nonsteroidal antiandrogen (NSAAs).

Androgen receptor antagonists

Steroidal antiandrogens

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

First-generation
Bicalutamide
Flutamide
Nilutamide
Second-generation
Apalutamide
Darolutamide
Enzalutamide
Proxalutamide
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

CYP11A1 (P450scc) inhibitors

Aminoglutethimide

5ÃÂ±-Reductase inhibitors

These drugs selectively inhibit the synthesis of DHT without affecting that of testosterone.

Antigonadotropins

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

List of androgens/anabolic steroids

References