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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Pharmacological Options for Treatment of Hyperandrogenic Disorders

Author(s): P. Reismann, I. Liko, P. Igaz, A. Patocs and K. Racz

Volume 9, Issue 9, 2009

Page: [1113 - 1126] Pages: 14

DOI: 10.2174/138955709788922692

Price: $65


Hyperandrogenic disorders are frequent in women. The most common cause is polycystic ovary syndrome, a condition found up to 7% in women of reproductive age. The effects of testosterone and dihydrotestosterone are elicited via androgen receptors. Androgen receptor acts as a ligand-dependent transcription factor that regulates the expression of several target genes. There are several pharmacological possibilities for the treatment of androgen excess, as inhibition of the biologic activity of androgens can be carried out at different levels. The androgen receptor, the 5α-reductase enzyme, and the hypothalamic-pituitary-gonad axis are the most frequent targets of antiandrogenic therapies. This review summarizes the structural and chemical features of currently available antiandrogenic drugs, including cyproterone acetate, spironolactone, flutamide and finasteride. Also, it presents some recent advances in the chemistry and pharmacology of novel steroidal and non-steroidal antiandrogens, and 5α-reductase inhibitors. Finally, recent knowledge on non-classical antiandrogenic drugs, such as insulin-sensitizers, ketoconazole, and GnRH-agonists are briefly discussed.

Keywords: Antiandrogen therapy, 5α-reductase inhibitors, androgen receptor antagonists, androgen excess

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