Chaohuixian Bicalutamide Tablets

1. Indications and Usage
Advanced Prostate Cancer: Treatment of advanced prostate cancer in combination with a Luteinizing Hormone-Releasing Hormone (LHRH) analogue or surgical castration.
Locally Advanced Prostate Cancer: Treatment of patients with locally advanced, non-metastatic prostate cancer who are not suitable or unwilling to undergo surgical castration or other medical treatments.
Metastatic Prostate Cancer: Treatment of metastatic prostate cancer after the failure of first-line hormonal therapy (i.e., intermittent or continuous combined androgen blockade).
2. Dosage and Administration
Standard Regimen: The recommended dose is 50 mg taken orally once daily.
Administration: Treatment should continue until disease progression. For monotherapy (150 mg daily), treatment should continue until disease progression or unacceptable toxicity.
Dose Adjustments: In patients with mild hepatic impairment, no dose adjustment is necessary. In patients with moderate or severe hepatic impairment, use with caution. If signs of severe liver injury occur (e.g., jaundice, dark urine), therapy must be discontinued immediately.
3. Mechanism of Action
Androgen Receptor Antagonism: Bicalutamide is a non-steroidal antiandrogen that competitively inhibits the binding of androgens (testosterone and dihydrotestosterone) to androgen receptors in target tissues.
Therapeutic Effect: This blockade inhibits the growth and proliferation of androgen-dependent prostate cancer cells, complementing the effects of LHRH analogues or castration.
4. Safety and Warnings
Hepatotoxicity: Serious liver injury, including acute liver failure and death, has been reported. Liver function tests (LFTs) must be monitored regularly, especially during the first 6 months of therapy.
Cardiovascular Disorders: There have been reports of myocardial infarction and heart failure, particularly when used in combination with LHRH analogues.
Pulmonary Disorders: Rare cases of interstitial pneumonitis and pulmonary fibrosis have been reported.
Embryo-Fetal Toxicity: The drug is contraindicated for use in women and children.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: Gynecomastia, breast pain, hot flushes, fatigue, nausea, vomiting, diarrhea, constipation, and alopecia.
Clinical Research: Clinical trials have demonstrated significant improvements in overall survival and time to disease progression when used in combination regimens for advanced prostate cancer.
6. Drug Interactions
Warfarin and Other Coumarin Derivatives: Bicalutamide may prolong prothrombin time and INR. Close monitoring is required when co-administered.
CYP3A4 Substrates: Bicalutamide may inhibit CYP3A4. Caution is advised when co-administered with substrates such as terfenadine, astemizole, or cisapride due to the risk of QT prolongation.
CYP3A4 Inhibitors/Inducers: Strong inhibitors or inducers of CYP3A4 may alter bicalutamide plasma concentrations.
7. Pharmaceutical Information
Active Ingredient: Bicalutamide.
Appearance: Film-coated tablets, white to pale yellow.
Storage: Store at room temperature. Protect from moisture.