Antiandrogens

To stimulate prostate cells (both cancerous and noncancerous), testosterone must first bind to specific androgen receptors within the cells. Drugs called antiandrogens can bind to these receptors and prevent testosterone from stimulating the cells. Since antiandrogens do not block testosterone production—which sets them apart from other types of hormone therapy—their use may preserve erectile function in some patients. Three antiandrogens are approved by the FDA for the treatment of advanced prostate cancer: bicalutamide (Casodex), flutamide (Eulexin), and nilutamide (Nilandron).

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When used alone, antiandrogens may not be as effective as other forms of castration. In addition, antiandrogens can cause hot flashes, breast enlargement, diarrhea, and, in rare instances, liver damage. To monitor for liver damage, men taking an antiandrogen must have their liver function tested a few months after starting treatment. Signs of liver problems include nausea, vomiting, fatigue, and jaundice. Nilutamide may slow the ability of the eyes to adapt to darkness. This side effect lasts for about four to six weeks.

In 40 percent to 75 percent of men taking an antiandrogen, an increase in PSA levels occurs, indicating disease progression. But if the medication is discontinued, PSA levels will fall. Why this occurs is not clear. It is possible that a mutation in the cancer cells results in their response to stimulation by antiandrogens.