Antiandrogens in prostate cancer

Reid P, Kantoff P, Oh W (1999) Antiandrogens in prostate cancer. Invest New Dmgs 17 271-284... 

Al. Akakura, K., Akimoto, S., Furaya, Y., and Ito, H., Incidence and characteristics of antiandrogen withdrawal syndrome in prostate cancer after treatment with chlormadinone acetate. Eur. Urol. 33, 567-571 (1998). 

M5. Mahler, C., Verhelst, J., and Denis, L., Clinical pharmacokinetics of the antiandrogens and then-efficacy in prostate cancer. Clin. Pharmacokinet. 34, 405—417 (1998). 

Monotherapy with flutamide, bicalutamide, and nilutamide is no longer recommended due to decreased survival as compared with patients treated with LHRH agonist therapy or orchiectomy. Antiandrogens are indicated for advanced prostate cancer only when combined with an LHRH agonist (flutamide and bicalutamide]) or orchiectomy (nilutamide). In combination, antiandrogens can reduce the LHRH agonist-induced flare. 

The possible protective effect of isoflavonoids against prostate cancer has recently been reviewed and it is of particular interest that equol may be a novel antiandrogen that inhibits prostate growth and hormone feedback in rat studies. The role of isoflavonoids in the prevention of breast cancer is, however, the main focus of the next section of this chapter. 

Antiandrogens such as cyproterone acetate (5.54) or the nonsteroidal flutamide (5.55, a substituted anilide) are competitive antagonists on the cytosol receptor. They do not prevent DHT formation rather, they inhibit the nuclear retention of DHT in the prostate. They cause feminization in male fetuses and decrease libido in males. Cyproterone is also an active progestogen. In men, antiandrogens are used commonly in the treatment of prostatic cancer and uncommonly to inhibit sex drive in hypersexuality in women, antiandrogens are used to treat virilization. Bicalutamide (5.56) and nilutamide (5.57) are potent, orally active antiandrogens that may be used in the treatment of metastatic prostate carcinoma. 

Antiandrogens have proven to be very useful in treating benign prostatic hypertrophy, an aU too frequent accompaniment of aging. These agents, in addition, have a minor place in the treatment of prostatic cancer. They are also, on a more trivial note, used to... 

Fourcade R-O, McLeod D. Tolerability of antiandrogens in the treatment of prostate cancer. UroOncol 2004 4 5-13. 

Antiandrogens Bicalutamide Flutamide Nilutamide Inhibits the cellular uptake and effects of androgens in advanced, metastatic prostate cancer Nausea vomiting diarrhea decreased sex drive... 

Decensi AU, Boccardo F, Guameri D, Positano N, Paoletti MC, Costantini M, Martorana G, Giuliani L (1991) Monotherapy with nilutamide, a pure nonsteroidal antiandrogen, in untreated patients with metastatic carcinoma of the prostate. The Italian Prostatic Cancer Project. J Urol 146 377-381... 

Flutamide [FLEW tah mide] is a synthetic nonsteroidal antiandrogen used in the treatment of prostate cancer. It is metabolized to an active hydroxy derivative that binds to the androgen receptor. 

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