Antiandrogens

Substances effective against natural androgens, especially synthetic steroids, which act by competitive inhibition at the androgen receptor of the successful organ. Substances such as cyproterone acetate and flutamide block androgen receptors, e.g. at the prostate, thus cancelling the effect of androgens. Possible side effects are male breast growth (gynecomastia), loss of libido and potency. For this reason, anti-androgens can also be used as part of chemical castration in the treatment of hormone-dependent prostate carcinoma.

5alpha-reductase inhibitors

• Finasteride
• Dutasteride

Inhibitors of androgen biosynthesis (inhibition of 17-alpha steroid hydroxylase)

• Abiaterone acetate

Androgen receptor antagonists (androgen receptor antagonists block the androgen receptors).

• Steroidal androgen receptor antagonists (derived from progesterone)
  • Cyproterone acetate (is the typical representative of this group).
• Non-steroidal androgen receptor antagonists
  • 1st generation non-steroidal androgen receptor antagonists
    • Nilutamide
    • Flutamid
    • Bicalutamide
  • 2nd generation non-steroidal androgen receptor antagonists
    • Darolutamide
    • Enzalutamide
    • Apalutamide

gonadorelin receptor agonists

• Busrelin
• Leuprorelin
• Triptorelin

gonadorelin receptor antagonists

• Abarelix
• Degarelix

1. Chi KN et al (2019) Apalutamide for Metastatic, Castration-Sensitive Prostate Cancer. N Engl J Med 381: 13-24
2. Davies ID et al(2019) Enzalutamide with Standard First-Line Therapy in Metastatic Prostate Cancer. N Engl J Med 381: 121-131
3. Moul JW et al (2015) Hormones naïve prostate cancer: predicting and maximizing response intervals. Asian J Androl17: 9290-9235
4. James ND et al (2017) Abiraterone for Prostate Cancer Not Previously Treated with Hormone Therapy. N Engl J Med 377: 338–351
5. Scher HI et al(2015) Prevalence of Prostate Cancer Clinical States and Mortality in the United States: Estimates Using a Dynamic Progression Model. PLoS One 10: d0139440