Sex-hormonal agent

Sex-hormonal agents are used in medicine for a variety of purposes including hormone therapy (e.g., menopausal hormone therapy, androgen replacement therapy, transgender hormone therapy), antihormone therapy (e.g., androgen deprivation therapy, estrogen deprivation therapy), and hormonal contraception, among others.

Types and examples

Androgen receptor (AR) modulators

• Androgens and anabolic steroids (AR agonists)
  • Examples: testosterone, androstanolone (dihydrotestosterone), prasterone (dehydroepiandrosterone), nandrolone (nortestosterone), methyltestosterone, metandienone (methandrostenolone), oxandrolone, stanozolol, danazol
• Selective androgen receptor modulators (AR mixed agonists/antagonists)
  • Examples: enobosarm (ostarine; GTx-024, MK-2866), andarine (GTx-007)
• Antiandrogens (AR antagonists)
  • Examples: cyproterone acetate, chlormadinone acetate, spironolactone, flutamide, bicalutamide, enzalutamide, apalutamide

Estrogen receptor (ER) modulators

• Estrogens (ER agonists)
  • Examples: estradiol, estrone, estriol, estetrol, conjugated estrogens (Premarin), ethinylestradiol, diethylstilbestrol (stilbestrol), chlorotrianisene
• Selective estrogen receptor modulators (ER mixed agonists/antagonists)
  • Examples: tamoxifen, clomifene, cyclofenil, raloxifene, toremifene, lasofoxifene, ospemifene, bazedoxifene
• Antiestrogens (ER antagonists)
  • Examples: fulvestrant, ICI-164384, TAS-108 (SR-16234), ZB716 (fulvestrant-3-boronic acid), ethamoxytriphetol (MER-25)

Progesterone receptor (PR) modulators

• Progestogens and progestins (PR agonists)
  • Examples: progesterone, medroxyprogesterone acetate, norethisterone (norethindrone), levonorgestrel, drospirenone, dydrogesterone
• Selective progesterone receptor modulators (PR mixed agonists/antagonists)
  • Examples: mifepristone, ulipristal acetate, telapristone (CDB-4124), vilaprisan (BAY-1002670)
• Antiprogestogens (PR antagonists)
  • Examples: aglepristone, onapristone (ZK-89299)

Indirect sex-hormonal agents

Drugs that indirectly influence sex hormone systems, such as antigonadotropins like GnRH analogues and prolactin releasers (e.g., D₂ receptor antagonists), progonadotropins like GnRH agonists, and steroidogenesis inhibitors like aromatase inhibitors and androgen synthesis inhibitors, are also sex-hormonal agents.