I. Basic Drug Information

Generic Name: Bicalutamide

Brand Names: Casodex, Kangshide, Zhaohuixian

Dosage Form/Specification: 50 mg/tablet; 28 tablets/box

Active Ingredient: Bicalutamide

Manufacturer: Eczacıbaşı Pharmaceuticals (Turkey)

Storage: Store below 30°C, protected from light and moisture.

II. Indications

Indicated for the combination therapy of advanced prostate cancer:

1. Metastatic prostate cancer: Used in combination with LHRH analogues (e.g., goserelin) or surgical orchiectomy to block androgen action.

2. Special populations: Not applicable to postmenopausal women; contraindicated in women and children.

III. Dosage and Administration

Standard Regimen

| Population | Dosage and Administration | Treatment Duration and Combination Requirements |

| :--- | :--- | :--- |

| Adult males (including the elderly) | 50 mg orally once daily (with or without food) | Must be initiated concurrently with LHRH analogue injection or orchiectomy; continue until disease progression or intolerance |

| Patients with hepatic impairment | Mild: No adjustment needed; Moderate/Severe: Use with caution (potential for accumulation) | Close monitoring of liver function required |

| Patients with renal impairment | No dosage adjustment needed | |

Key Notes

Missed dose: Take immediately; if close to the time for the next dose, skip the missed dose; do not take a double dose.

Contraindicated combinations:

Terfenadine, astemizole, cisapride (risk of severe cardiac events);

Anticoagulants such as warfarin (increased risk of bleeding). IV. Adverse Reactions

Common adverse reactions (>10%)

| System Classification | Main Symptoms | Incidence

| General | Hot flashes (53%), fatigue (22%), pain (35%) | High

| Digestive System | Nausea (15%), constipation (22%), diarrhea (12%) | Moderate-High

| Genitourinary System | Gynecomastia (9%), impotence (7%), nocturia (12%) | Moderate

| Metabolic & Cardiovascular | Peripheral edema (13%), anemia (11%), hypertension (8%) | Moderate

Serious adverse reactions

1. Hepatotoxicity:

- Elevated transaminases, jaundice (approx. 7%); hepatic failure is rare;

- Mostly occurs within the first 6 months of treatment; regular monitoring of liver function is required.

2. Cardiovascular events:

- Heart failure, myocardial infarction (especially in patients with a history of coronary artery disease).

3. Pulmonary disorders: Interstitial pneumonia, pulmonary fibrosis (rare but potentially fatal).

4. Allergic reactions: Angioedema, Stevens-Johnson syndrome.

V. Contraindications

Contraindicated in the following populations:

1. Women and children: Teratogenic risk (exposure during pregnancy may cause fetal malformations);

2. Patients with a history of allergy: Hypersensitivity to bicalutamide or excipients (contains lactose);

3. Severe hepatic impairment (Child-Pugh Class B-C);

4. Contraindicated combinations: Terfenadine, astemizole, cisapride.

VI. Precautions

1. Liver function monitoring:

- Monitor transaminases monthly during the first 6 months of treatment, followed by periodic re-examination;

- Discontinue the drug immediately if jaundice or severe liver injury occurs.

2. Cardiovascular risk:

- Use with caution in patients with coronary artery disease; seek emergency medical attention if chest pain or dyspnea occurs. 3. Drug Interactions:

CYP3A4 inhibitors (e.g., ketoconazole): May increase bicalutamide plasma concentrations;

Warfarin: Potentiates anticoagulant effects; frequent INR monitoring is required.

4. Photosensitivity: Avoid exposure to intense light during treatment; use high-SPF sunscreen.

VII. Use in Special Populations

Men of reproductive potential: Contraceptive measures must be used during treatment and for at least 130 days after discontinuation (due to potential teratogenic risk).

Elderly: No dose adjustment required, but enhanced monitoring of liver function and cardiovascular status is necessary.

Lactating/Pregnant women: Strictly contraindicated (the drug is excreted via body fluids; caregivers must wear gloves when handling contaminated materials).

VIII. Pharmacological Mechanism and Pharmacokinetics

Mechanism of action: A non-steroidal anti-androgen that competitively inhibits the binding of androgens to receptors on prostate cells, thereby blocking tumor growth signals.

Pharmacokinetics:

- Completely absorbed after oral administration; time to peak plasma concentration is 1–2 hours;

- Metabolized in the liver (CYP3A4); half-life is approximately 7 days;

- Clearance is reduced in patients with mild-to-moderate hepatic impairment; potential for drug accumulation exists.

Summary and Warnings: Casodex is a core therapeutic agent for advanced prostate cancer; however, strict adherence to combination therapy principles (concomitant use with LHRH agonists or surgery) is required, alongside vigilance regarding hepatotoxicity and cardiovascular risks. Regularly monitor liver function, complete blood counts (CBC), and cardiovascular parameters during treatment; do not adjust the dosage without medical authorization. Please follow the specific regimen prescribed by the attending physician. Specifications

Product Name: Casodex (Bicalutamide) Tablets 50mg × 28 tablets/box

Common Name: Bicalutamide Tablets

Active Ingredient: Bicalutamide

Dosage Form: Tablet

Specification: 50mg/tablet; 28 tablets/box

Manufacturer: Eczacıbaşı Pharmaceuticals (Turkey)

Indications: Indicated for the combination therapy of advanced prostate cancer:

1. Metastatic prostate cancer: Used in combination with LHRH analogues (e.g., goserelin) or surgical castration to block androgen action.

2. Special populations: Not applicable to postmenopausal women; contraindicated in women and children.

Dosage and Administration: 1. Advanced prostate cancer (in combination with LHRH analogues)

Oral dosage: 50mg (1 tablet) once daily; it is recommended to take the medication at a fixed time (e.g., morning or evening).

Duration of treatment: Continue treatment until disease progression or the occurrence of intolerable adverse reactions.

2. Adjuvant therapy for early-stage prostate cancer (post-surgery or post-radiotherapy)

Oral dosage: 150mg once daily; the duration of treatment is usually determined by the physician based on the patient's condition (e.g., continued for 2–3 years).