CASODEX

PURPOSE: To determine whether tamoxifen or anastrozole prevents gynecomastia and breast pain caused by bicalutamide (150 mg) without compromising efficacy, safety, or sexual functioning. PATIENTS AND METHODS: A double-blind, placebo-controlled trial was performed in patients with localized, locally advanced, or biochemically recurrent prostate cancer. Patients (N = 114) were randomly assigned to either bicalutamide (150 mg/d) plus placebo or in combination with tamoxifen (20 mg/d) or anastrozole (1 mg/d) for 48 weeks. Gynecomastia, breast pain, prostate-specific antigen (PSA), sexual functioning, and serum levels of hormones were assessed. RESULTS: Gynecomastia developed in 73% of patients in the bicalutamide group, 10% of patients in the bicalutamide-tamoxifen group, and 51% of patients in the bicalutamide-anastrozole group (P < .001); breast pain developed in 39%, 6%, and 27% of patients, respectively (P = .006). Baseline PSA level decreased by > or = 50% in 97%, 97%, and 83% of patients in the bicalutamide, bicalutamide-tamoxifen, and bicalutamide-anastrozole groups, respectively (P = .07); and adverse events were reported in 37%, 35%, and 69% of patients, respectively (P = .004). There were no major differences among treatments in sexual functioning parameters from baseline to month 6. Elevated testosterone levels occurred in each group; however, free testosterone levels remained unchanged in the bicalutamide-tamoxifen group because of increased sex hormone-binding globulin levels. CONCLUSION: Anastrozole did not significantly reduce the incidence of bicalutamide-induced gynecomastia and breast pain. In contrast, tamoxifen was effective, without increasing adverse events, at least in the short-term follow-up. These data support the need for a larger study to determine any effect on mortality.

Objective: To evaluate the efficacy of bicalutamide vs cyproterone acetate in preventing PSA flare (as a surrogate for tumour flare) for patients requiring luteinizing hormone-releasing hormone (LHRH) analogue therapy for prostate cancer.Patients and Methods: In this pilot study, 40 men were randomized 1 : 1 to bicalutamide 50 mg o.d. or cyproterone acetate 100 mg t.i.d. 5 days prior to goserelin acetate and continued for 21 days thereafter. PSA, luteinizing hormone (LH), follicle-stimulating hormone (FSH) and testosterone were obtained before treatment and on days 6, 8, 10, 16, 21 and 28. Primary end point was PSA. Hormone profile and clinical features including urinary symptoms and bone pain were secondary end points.Results: Both groups were equally matched apart from serum creatinine and ALP. The speed and magnitude of the percentage change in median PSA from baseline was increased for the CPA group but there was no statistically significant difference in the two groups. Although those receiving bicalutamide all showed a testosterone peak, this remained within the normal range. No difference in the frequency of drug-specific adverse events was found. None of the patients died or developed cord compression during the study period.Conclusion: Bicalutamide is able to suppress the initial PSA surge as effectively as cyproterone acetate albeit slightly delayed. A statement whether bicalutamide is equally good at preventing clinical flare cannot be made and should be assessed in an appropriately powered study.Prostate Cancer and Prostatic Diseases advance online publication, 15 February 2005; doi:10.1038/sj.pcan.4500784.

A randomized, double-blind, placebo-controlled multicenter trial involving 107 men receiving bicalutamide ('Casodex') 150 mg/day therapy following radical therapy for prostate cancer assessed tamoxifen ('Nolvadex') 20 mg/day and anastrozole ('Arimidex') 1 mg/day for the prophylaxis and treatment of gynecomastia/breast pain. Tamoxifen, but not anastrozole, significantly reduced the incidence of gynecomastia/breast pain when used prophylactically and therapeutically. Serum testosterone levels increased with tamoxifen relative to placebo but prostate-specific antigen levels declined in all treatment groups. Further studies are needed to define the optimum tamoxifen dose and to assess any impact on cancer control. The use of tamoxifen in this setting remains to be investigated.Prostate Cancer and Prostatic Diseases advance online publication, 1 February 2005; doi:10.1038/sj.pcan.4500782.

GENERIC NAME: bicalutamide
BRAND NAME: Casodex

DRUG CLASS AND MECHANISM: Bicalutamide is an oral medication that is used for treating cancer of the prostate. It belongs to a class of drugs called anti-androgens which includes flutamide (Eulexin) and nilutamide (Nilandron). Androgens (an example of which is testosterone) are hormones that are produced and released by the adrenal glands. They are responsible for supporting (stimulating) tissues that primarily are thought of as male, for example, the male prostate gland. Male traits that also are influenced by androgens include facial and body hair and small breasts. Anti-androgens prevent the action of androgens by blocking the receptors for androgens on the cells of tissues, for example, the cells of the prostate gland. In addition to normal prostate cells, androgens also have been shown to stimulate the growth of cancer cells within the prostate. Bicalutamide is thought to prevent the growth of prostate cancer by blocking the effects of androgens on the cancer cells. Bicalutamide was approved by the FDA in 1995.

PREPARATIONS: Bicalutamide is available as a 50mg tablet.

STORAGE: Bicalutamide should be stored at room temperature, 15-30°C(59-86°F).

PRESCRIBED FOR: Bicalutamide is used in combination with another medication, a gonadotrophin hormone releasing factor, to treat advanced prostate cancer.

DOSING: Bicalutamide should be taken as one 50mg tablet in the morning or the evening at the same time each day. It may be taken with or without food. Once bicalutamide therapy has begun, it should not be interrupted or stopped without consulting a physician.

DRUG INTERACTIONS: Bicalutamide may interact with warfarin (Coumadin). Therefore, the dose of Coumadin may need to be adjusted.

PREGNANCY: Bicalutamide can cause harm to a developing fetus; therefore, it should not be administered to pregnant women or women attempting to become pregnant.

NURSING MOTHERS: It is not known if bicalutamide is excreted in breast milk.

SIDE EFFECTS: When bicalutamide and a gonadotrophin releasing factor analog are given together, the most common side effect is hot flashes (50% of patients) and facial flushing. Alcohol may worsen this reaction, and so it should be cautiously consumed. Other common side effects of the combination are diarrhea, constipation and overall pain including pain in the back, hips and stomach. Less common side effects are breast enlargement and breast pain, which may be due to the bicalutamide alone. Glossary content Copyright © 1996-2002 MedicineNet, Inc. All rights reserved.

Caution! Before starting to take this medicine, it is vital that you should consult your doctor! Do not use it on your own initiative, without medical advice.