Cyproterone

Information about Cyproterone

Cyproterone is a steroidal antiandrogen that has been used in the treatment of prostate cancer in many countries of the world, but not in the United States. 

Liver safety of Cyproterone

Cyproterone therapy can be associated with serum enzyme elevations during therapy and has been linked to many instances of clinically apparent acute liver injury, some of which were fatal. 

Mechanism of action of Cyproterone

Cyproterone (sye pro' ter one) is a synthetic steroidal antiandrogen that has been used to treat prostate cancer in many countries of the world, but was never approved for this use in the United States.  Cyproterone is a derivative of hydroxyprogesterone and has mild progesterone-like effects.  Its mechanism of action, however, appears to be via blocking of the androgen receptor.  Alone or when combined with other agents, cyproterone has been found to be palliative in patients with advanced prostate cancer.  Cyproterone has also been evaluated for hormonally sensitive benign conditions such as endometriosis, precocious puberty and infertility, but has not been formally recommended for these uses.  Because of its potential to cause liver injury and its inferior efficacy in comparison to other antiandrogens, cyproterone is now rarely used. 

Dosage and administration for Cyproterone

The typical dose regimen is 50 to 100 mg two to three times daily, often in combination with a gonadotropin releasing hormone agonist such as leuprolide, goserelin, histrelin or triptorelin. 

Side effects of Cyproterone

Common side effects include hot flashes, sexual dysfunction, nausea, diarrhea, weight change and fluid retention.

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  Cyproterone