Purpose: The safety, efficacy and pharmacokinetics of bicalutamide were investigated in 150 patients with stage D2 prostate cancer.
Materials and methods: Patients received 50 mg. bicalutamide daily in an open label multicenter North American trial.
Results: The objective response rate (modified European Organization for Research in Cancer Therapy criteria) was 70%. Of 150 patients 59 (39%) met prostate specific antigen criteria for partial response, and 88 (59%) reached treatment failure end points and withdrew. Extent of disease was a significant predictor of response but baseline testosterone was not. Breast pain and gynecomastia developed in 76% and 60% of patients, respectively. Mean drug plasma concentration was 8,528 +/- 2,928 ng/ml.
Conclusions: Bicalutamide (50 mg.) daily was well tolerated and efficacious. However, suboptimal effects on prostate specific antigen have led to additional trials to evaluate monotherapy at higher doses.