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 analogues, estrogens, and progestogens. In addition, it includes both steroidal antiandrogen (SAAs) and nonsteroidal antiandrogen (NSAAs).

Androgen receptor antagonists Steroidal antiandrogens

17α-Hydroxyprogesterone derivatives Chlormadinone acetate Cyproterone acetate Megestrol acetate Osaterone acetate 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

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

Abiraterone acetate Ketoconazole Seviteronel

CYP11A1 (P450scc) inhibitors Aminoglutethimide

5α-Reductase inhibitors

Alfatradiol Dutasteride Epristeride Finasteride Saw palmetto extract

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