Bicalutamide is a non-steroidal androgen receptor inhibitor. It competitively inhibits the action of androgens by binding to cytosolic androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen-sensitive and responds to treatment that counteracts the effect of androgens and/or removes the source of androgen production.
Bicalutamide 50 mg daily is indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D2 metastatic carcinoma of the prostate.
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.
Bicalutamide is contraindicated in any patient who has shown a hypersensitivity reaction to the drug or any of the tablet’s components.
Bicalutamide has no indication for women and should not be used in this population.
Warnings and Precautions
Hemorrhage with concomitant use of Coumarin Anticoagulants: Closely monitor Prothrombin Time (PT) and International Normalized Ratio (INR) and adjust the anticoagulant dose as needed.
Gynecomastia and breast pain have been reported during treatment with Bicalutamide 150 mg when used as a single agent, as it causes a reduction in glucose tolerance in males.
Consideration should be given to monitoring blood glucose levels in patients receiving Bicalutamide in combination with LHRH agonists.
Monitoring Prostate-Specific Antigen (PSA) levels is recommended. Evaluate for clinical progression if PSA levels increase.
Adverse reactions that occurred in more than 10% of patients receiving Bicalutamide plus an LHRH analog included:
Hot flashes, pain (general, back, pelvic, and abdominal), asthenia, constipation, infection, nausea, peripheral edema, dyspnea, diarrhea, hematuria, nocturia, and anemia.
Pregnancy: Bicalutamide is contraindicated in pregnant women due to the risk of fetal harm.
Nursing Mothers: Bicalutamide is not indicated for use in females. There are no human data on its use in pregnant women.
Hepatic Impairment: Bicalutamide is extensively metabolized by the liver. It should be used with caution in patients with moderate to severe hepatic impairment.
Pediatric Use: The safety and effectiveness of Bicalutamide in pediatric patients have not been established.
R-bicalutamide is an inhibitor of CYP3A4; therefore, caution should be exercised when Bicalutamide is co-administered with CYP3A4 substrates.
PT/INR should be closely monitored in patients receiving coumarin anticoagulants who are started on Bicalutamide.
Long-term clinical trials have been conducted with dosages up to 200 mg of Bicalutamide daily, and these dosages have been well tolerated. A single dose that results in life-threatening overdose symptoms has not been established.
There is no specific antidote; treatment of an overdose should be symptomatic.
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
