What is the proper administration of Bicalutamide (Casodex)?

From the Guidelines

Bicalutamide should be taken orally once daily with or without food, typically at a dose of 50mg for prostate cancer treatment, as supported by the most recent guidelines 1. The administration of Bicalutamide (Casodex) is crucial for its effectiveness in treating prostate cancer.

• The recommended dose is 50mg, which can be taken with or without food.
• It is essential to swallow the tablet whole with water at approximately the same time each day to maintain consistent blood levels.
• The tablet should not be crushed or chewed.
• If a dose is missed, it should be taken as soon as remembered, unless it's almost time for the next dose, in which case the missed dose should be skipped.
• Bicalutamide works by blocking androgen receptors, preventing testosterone from binding to them, which helps suppress testosterone's effects in the body.
• Common side effects include breast tenderness or enlargement, hot flashes, and fatigue.
• Regular blood tests are necessary to monitor liver function, as bicalutamide can occasionally cause liver problems, as noted in studies 1.
• Alcohol should be limited while taking this medication.
• For those using it for prostate cancer, it's typically taken alongside another medication called a GnRH agonist (like leuprolide) to achieve complete androgen blockade. The most recent study 1 provides the strongest evidence for the administration of Bicalutamide, and its findings should be prioritized in clinical practice.

From the FDA Drug Label

The recommended dose for bicalutamide therapy in combination with an LHRH analog is one 50 mg tablet once daily (morning or evening). The proper administration of Bicalutamide (Casodex) is one 50 mg tablet once daily, which can be taken in the morning or evening, in combination with an LHRH analog 2 2.

• The dose is the same for the treatment of Stage D2 metastatic carcinoma of the prostate.
• It is not approved for use alone or with other treatments at a dose of 150 mg daily.

From the Research

Administration of Bicalutamide

The proper administration of Bicalutamide (Casodex) is as follows:

• As monotherapy, a 150-mg daily dose is considered effective for the treatment of early (localized or locally advanced) nonmetastatic prostate cancer 3.
• In combination with a luteinizing hormone-releasing hormone analogue or surgical castration, a 50-mg daily dose is used for the treatment of advanced prostate cancer 3, 4.
• The benefits of a 150-mg daily dose of bicalutamide as monotherapy include retention of libido and sexual potency, and as combination therapy, a lower incidence of diarrhea relative to flutamide 5.

Dosage Considerations

• A 50-mg daily dose of bicalutamide is sufficient when given in combination with an agent that lowers serum testosterone, but higher doses of bicalutamide may be needed when the drug is given as monotherapy 5.
• Dose-related effects of bicalutamide on serum PSA concentrations have been demonstrated in clinical trials, with a dose of 150 mg/day considered effective for monotherapy 5, 4.
• Bicalutamide is well tolerated when used as monotherapy or in combination with a LHRH-A, with a low incidence of treatment-related withdrawals 4.

Clinical Trials and Studies

• Clinical trials have evaluated the efficacy and tolerability of bicalutamide as monotherapy and as combination therapy for patients with advanced prostate cancer 5, 4, 6.
• A phase 2 trial of bicalutamide dose escalation from 50 mg to 150 mg in men with combined androgen blockade and castration resistance showed a PSA response rate of 22% 6.
• Real-world analysis using the SEER-Medicare database has shown that bicalutamide is often used as monotherapy or as part of combined androgen blockade, despite the lack of FDA indication for monotherapy 7.