Bicalutamide is used in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analogue for the treatment of Stage D2 metastatic prostate cancer.

Bicalutamide is a non-steroidal androgen receptor inhibitor that works by competitively blocking the action of androgens through binding to cytosolic androgen receptors in target tissues. Prostate cancer is typically androgen-dependent and responds to therapies that block androgen effects or reduce androgen production.

The recommended dose for Bicalutamide therapy in combination with an LHRH analog is one 50 mg tablet once daily (morning or evening), with or without food.

Pediatric Use: The safety and effectiveness of Bicalutamide in pediatric patients have not been established.

Hepatic Impairment: Bicalutamide is extensively metabolized by the liver. It should be used with caution in patients with moderate-to-severe hepatic impairment.

• R-bicalutamide inhibits CYP3A4; therefore, caution is advised when it is used together with drugs metabolized by CYP3A4.
• PT/INR should be carefully monitored in patients already receiving coumarin anticoagulants when Bicalutamide is initiated.

Bicalutamide is contraindicated in patients with known hypersensitivity to the drug or any of its components. It is not indicated for use in women and should not be used in this population.

Common adverse reactions (occurring in more than 10% of patients receiving Bicalutamide with an LHRH analogue) include hot flashes, pain (general, back, pelvic, abdominal), weakness, constipation, infection, nausea, peripheral edema, shortness of breath, diarrhea, hematuria, nocturia, and anemia.

Bicalutamide is contraindicated in pregnant women as it may cause fetal harm. It is not indicated for use in females. There are no adequate human data regarding its use during pregnancy.

• Hemorrhage may occur when used with coumarin anticoagulants. Monitor Prothrombin Time (PT) and International Normalized Ratio (INR) closely and adjust anticoagulant dose if required.
• Gynecomastia and breast pain have been reported with Bicalutamide 150 mg when used as monotherapy, possibly due to decreased glucose tolerance in males.
• Blood glucose levels should be monitored in patients receiving Bicalutamide along with LHRH agonists.
• Monitoring of Prostate Specific Antigen (PSA) is recommended. Evaluate for disease progression if PSA levels rise.

Pediatric Use: The safety and effectiveness of Bicalutamide in pediatric patients have not been established.

Hepatic Impairment: Periodic liver function tests should be considered in patients with hepatic impairment during long-term therapy.

Renal Impairment: Renal impairment does not significantly affect the elimination of total bicalutamide or its active R-enantiomer.

Long-term studies have evaluated daily doses up to 200 mg of Bicalutamide, which were generally well tolerated. There is no evidence that a single overdose is life-threatening. No specific antidote exists; management should be symptomatic.

Hormonal Chemotherapy

Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.