Androgen receptor antagonists

The androgen receptor antagonists are divided between:

• steroidal androgen receptor antagonists (like the androgens themselves)
• and
• non-steroidal androgen receptor antagonist

differentiated.

Steroidal androgen receptor antagonists: The steroidal antiandrogens are derived from progesterone and are less selective than the newer non-steroidal agents. Cyproterone acetate (CPA), is the typical representative of this group. Cyproterone acetate is chemically speaking a progesterone derivative. The active ingredient acts as a competitive antagonist at the androgen receptor. Indications are: hirsutism, severe acne vulgaris, sexual dullness and palliative treatment of prostate cancer.

Non-steroidal androgen receptor antagonists: The non-steroidal androgen receptor antagonists have common structural elements with the exception of darolutamide. The representatives of the family of non-steroidal antiandrogens are potent antagonists at the androgen receptor. The second generation androgen receptor antagonists (enzalutamide and apalutamide) have the highest affinity to the androgen receptor. Androgen receptor antagonists lead to an increase in the release of gonadotropin and must therefore be used together with GnrH analogues. Various relevant study results support the importance of the androgen receptor signaling pathway in the treatment of prostate cancer. The non-steroidal antiandrogens can be divided into:

• 1st generation non-steroidal androgen receptor antagonists
  • Nilutamide
  • Flutamid
  • Bicalutamide
• 2nd generation non-steroidal androgen receptor antagonists
  • Darolutamide
  • Enzalutamide
  • Apalutamide