Antiandrogens, or androgen antagonists, first discovered in the 1960s, prevent androgens from expressing their biological effects on responsive tissues.
 
Antiandrogens alter the androgen pathway by blocking the appropriate receptors, competing for binding sites on the cell's surface, or affecting androgen production. Antiandrogens can be prescribed to treat an array of diseases and disorders. In men, antiandrogens are most frequently used to treat prostate cancer. In women, antiandrogens are used to decrease levels of male hormones causing symptoms of hyperandrogenism. Antiandrogens present in the environment have become a topic of concern. Many industrial chemicals, pesticides and insecticides exhibit antiandrogenic effects.Certain plant species have also been found to produce antiandrogens. Environmental antiandrogens can have harmful effects on reproductive organ development in fetuses exposed in utero as well as their offspring.
 
Medical applications
 
Antiandrogenic pharmaceuticals are used to treat an array of medical conditions that are dependent on the androgen pathway. Antiandrogens are often prescribed for men with prostate cancer, benign prostatic hyperplasia, hypersexuality, male contraception, and for those that are undergoing gender reassignment. For women, antiandrogens are often prescribed for severe cases of acne, amenorrhea, seborrhea, hirsutism, androgenic alopecia, hidradenitis suppurativa, and hyperandrogenism.
 
Future research
Currently, further research is being conducted on the effects of antiandrogens. In the pharmaceutical industry, researchers continue to experiment with antiandrogenic drugs and other treatments in the hope of finding cures to diseases such as prostate cancer. Greater insight into the mechanisms and pathways of antiandrogens would provide more effective treatment that might decrease the likelihood of recurrent prostatic tumors.
The future of antiandrogenic drugs is believed to be peptide antagonists. Current androgen receptor antagonist drugs bind to the ligand binding domain on the receptors and inhibit receptor function. Androgen receptor peptide antagonists act in an alternative manner. A peptide antagonist interrupts androgen receptor protein interactions from the surface of the receptor.This approach is "mechanism-based" and has greater potential for blocking receptor activity than the traditional ligand-receptor binding approach. Researchers are trying to target the ligand-binding domain and N-terminal domain of androgen receptors.