List of antiandrogens explained

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 analogues, estrogens, and progestogens.^[3] In addition, it includes both steroidal antiandrogen (SAAs) and nonsteroidal antiandrogen (NSAAs).

Androgen receptor antagonists

Steroidal antiandrogens

See main article: Steroidal antiandrogen and List of 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

See main article: Nonsteroidal antiandrogen.

• 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

See also: Steroidogenesis inhibitor.

CYP17A1 inhibitors

See main article: CYP17A1 inhibitor.

• Abiraterone acetate
• Ketoconazole
• Seviteronel

CYP11A1 (P450scc) inhibitors

• Aminoglutethimide

5α-Reductase inhibitors

See main article: 5α-Reductase inhibitor.

• Alfatradiol
• Dutasteride
• Epristeride
• Finasteride
• Saw palmetto extract

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

Antigonadotropins

See 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

• List of androgens/anabolic steroids

Notes and References

1. Web site: List of Antiandrogens (androgen antagonists) . 2022-03-27 . Drugs.com . en.
2. Web site: antiandrogen drug Britannica . 2022-03-27 . www.britannica.com . en.
3. Web site: Antiandrogen - an overview ScienceDirect Topics . 2022-03-27 . www.sciencedirect.com.