Androgenrelated Antitumor Agents

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Androgens are steroidal hormones that stimulate and control the masculine primary and secondary characteristics. They exert their action by binding to a nuclear receptor called the androgen receptor (AR)36 and the complex acts as a transcription factor, in a similar way to estrogens. The main androgens are testosterone and its reduced metabolite 5a-dihydrotestosterone (DHT), which has a higher affinity for the AR and three- to tenfold greater molar potency than testosterone.

Testosterone 5a - Dihydrotestosterone

Most prostatic tumors are androgen dependent, and for this reason hormone treatment of prostate cancer is based on the modulation of testosterone to achieve medical castration levels. This can be achieved directly by administration of antiandrogens or indirectly by inhibition of 5a-reductase, the enzyme responsible for the reduction of testosterone to its more active metabolite. Androgen production can also be controlled by inhibition of the release of LH (see Section 7).

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