Currently the prime use of androgens are in the treatment of reproductive disorders, male hypogonadism and anabolic effects on non-gonadal disorders such as erythropoiesis, osteopenia, and wasting disease. The main problem for the indications is that the natural androgen testosterone has anabolic as well as androgenic effects acting equally on different tissues. But the discovery and development of tissue-selective androgens offers a huge opportunity to differentially regulate the androgen effects in various target tissues, thus minimising the interference to normal physiological processes while targeting desirable therapeutic goals.

Chemicals that modulate the transcriptional activity of the AR can be divided in two structural (steroidal and non-steroidal) and two functional (androgenic and antiandrogenic) classes. Androgens such as testosterone and related compounds are used clinically to treat androgen-deficiency. Steroidal anti-androgens like cypro-terone acetate (CPA) as well as non steroidal antagonists as bicalutamide or flu-tamide are used to counteract the undesirable effects of androgens as for treatment of PCa. A recent paper reviews the patent publications on tissue-selective andro-gens with different effects on non-reproductive target tissues (Chengalvala et al. 2003).

Non-steroidal synthetic compounds (e.g. tricyclic pyridinodihydroquinoline derivates) show promising anabolic effects without significant action on the prostate and seminal vesicle.

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