The article on the basis of literature survey and author’s data presents one of the fundamental problems of biology and medicine — the application of steroidal and non-steroidal competitive androgen antagonists — the androgen receptor blockers. Cellular and molecular mechanisms of the antiandrogen pharmacodynamics, pharmacokinetic issues and use of the antiandrogens in biological, biomedical research and clinical practice are overviewed. There is demonstrated efficacy of the antiandrogen administration in prostate cancer patients and in women with hyperandrogeny.
