Bicalutamide is a nonsteroidal antiandrogen with a long elimination ha
lf-life (t 1/2) that permits once-daily administration. When combined
with a gonadorelin (gonadotrophin releasing hormone; GnRH) agonist in
maximum androgen blockade (MAB) regimens, bicalutamide 50mg once daily
is at least as effective as flutamide 250mg 3 times daily, as shown i
n a large randomised trial. Rate of treatment failure, the primary end
-point, was significantly lower at 49 weeks with bicalutamide in this
study, mainly because of a lower rate of withdrawal due to adverse eve
nts. Final results at a median follow-up of 160 weeks revealed longer
median times to progression and death with bicalutamide than flutamide
, but between-group differences were not significant overall. Although
early trials demonstrated clinical benefits with bicalutamide 50 mg/d
ay as monotherapy, the drug in this dosage is less effective than cast
ration. Increasing the dosage to 150 mg/day has improved its efficacy
in patients with non-metastatic disease: combined data from 2 trials d
emonstrate similar survival with bicalutamide in this dosage compared
with castration. Accumulating evidence from these and other studies in
dicates that sexual interest appears to be better preserved with bical
utamide than with castration. The tolerability profile of bicalutamide
is characteristic of antiandrogens, with breast pain and gynaecomasti
a occurring most often. Bicalutamide has not been causally associated
with problems such as interstitial pneumonitis and difficulty with lig
ht/dark adaptation seen with nilutamide, and in a 50 mg/day dosage cau
ses a lower incidence of diarrhoea than flutamide 750 mg/day. Changes
in hepatic function are generally transient and resolve or improve dur
ing therapy or after bicalutamide treatment is withdrawn. Conclusion.
Bicalutamide, with its once-daily regimen and good tolerability, is an
attractive option when combined with a GnRH agonist in patients with
advanced prostate cancer who are suitable to receive MAB regimens. The
role of bicalutamide as monotherapy in the management of this common
malignancy is currently being assessed.