Which is the optimal antiandrogen for use in combined androgen blockade of advanced prostate cancer? The transition from a first- to second-generation antiandrogen.

Many physicians use combined androgen blockade in the form of a luteinizing hormone-releasing hormone analog or bilateral orchiectomy in combination with a non-steroidal antiandrogen to offer patients a potentially more effective treatment than castration alone. Three non-steroidal anti-androgens are available in the US, i.e. flutamide (Eulexin), bicalutamide (Casodex) and nilutamide (Nilandron). Nilutamide offers patients no benefit over flutamide or bicalutamide and has the least favorable safety profile. Because of its short half-life, flutamide must be administered 3 times a day. Furthermore, flutamide therapy is associated with a relatively high incidence of diarrhea, often intolerable for some patients. Bicalutamide is available in a convenient one tablet, once-a-day dosing regimen, is at least as effective as flutamide and is better tolerated in terms of diarrhea. Therefore, bicalutamide would seem to represent an appropriate first choice in patients who are suitable candidates for combined androgen blockade.