Cyproterone prostatic cancer

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. 

Although flutamide is sufficiently well tolerated in prostatic cancer, the much older drug cyproterone acetate continues to show up favorably. In a direct comparison between the two drugs in 310 men the two were equally... 

Schroder FH, Whelan P, De Reijke TM, Kurth KH, Pavone-Macaluso M, Mattelaer J, Van Velthoven RF, Debois M, Collette L. Metastatic prostate cancer treated by flutamide versus cyproterone acetate final analysis of the European Organization for Research and Treatment of Cancer (EORTC) protocol 30892. Eur Urol 2004 45 457-64. 

In a randomized study of men treated hormonally for prostatic cancer (3), cardiovascular adverse effects were reported more often in patients treated with diethylstilbestrol than in those treated with cyproterone acetate. The risk was highest during the first 6 months of treatment. 

Pavone-Macaluso M, de Voogt HJ, Viggiano G, Barasolo E, Lardennois B, de Pauw M, Sylvester R. Comparison of diethylstilbestrol, cyproterone acetate and medroxyprogesterone acetate in the treatment of advanced prostatic cancer final analysis of a randomized phase III trial of the European Organization for Research on Treatment of Cancer Urological Group. J Urol 1986 136(3) 624-31. 

Prostatic cancer is androgen-dependent and metastatic disease can be helped by orchidectomy, or by a gonadorelin analogue, e.g. buserelin, goserelin, leuprorelin or triptorelin. These cause a transient stimulation of luteinising hormone and thus testosterone release, before inhibition occurs some patients may experience exacerbation of tumour effects, e.g. bone pain, spinal cord compression. Where this can be anticipated, prior orchidectomy or antiandrogen treatment, e.g. with cyproterone or flutamide, is protective. 

Uses. C3 roterone is used for reducing male hypersexuality and in prostatic cancer and severe female hirsutism. A formulation of cyproterone plus ethinylestradiol (Dianette) is offered for this latter purpose as well as for severe acne in women this... 

P. (1998) Liarozole - a novel treatment approach for advanced prostate cancer results of a large randomized trial versus cyproterone acetate. Liarozole Study Group. Urology, 52, 72-81. 

Cyproterone acetate is an anti-androgen, which is indicated for the treatment of prostate cancer and male hypersexuality. It is an inhibitor of 21-hydrolase. 

Cyproterone is used in high doses as an ANTICANCER agent for cancer of the prostate gland. It is also used in relatively moderate doses, for the treatment of precocious puberty in males, and for hypersexuality or sexual deviation in men (in whom the drug causes a condition of reversible sterility through a reduction in the production of sperm and a decrease in libido). It works by being a derivative of... 

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