Bicalutamide

Bicalutamide

Generic Name:
Bicalutamide
Therapeutic Category:
Antineoplastic / Non-Steroidal Antiandrogen (NSAA)
Mechanism of Action:
Competitive androgen receptor antagonist. Bicalutamide attaches directly to androgen receptors on target tissues, completely blocking the binding of circulating male hormones like testosterone and dihydrotestosterone (DHT). Because prostate cancer cells rely on these androgens to grow and multiply, depriving them of hormone signals slows tumor progression and causes cell death.

Indications

Dosage & Administration

Contraindications & Precautions

Potential Side Effects

Indications (Therapeutic Uses)

Bicalutamide 50 mg is primarily used in oncology to treat advanced hormone-sensitive malignancies:

  • Advanced Prostate Cancer (Stage D2): Indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog (such as leuprolide or goserelin) for the management of metastatic carcinoma of the prostate.
  • Prevention of Tumor Flare: Administered prior to starting LHRH analog injections to suppress the temporary, painful spike in testosterone levels (“tumor flare”) that typically occurs during the first few weeks of therapy.

Dosage & Administration

Website Note: Bicalutamide is a potent hormonal medication. The treatment cycle, regular laboratory monitoring, and overall duration must be strictly managed by a registered oncologist or medical specialist.

  • Standard Adult Dose: The typical dose is 50 mg (one tablet) taken orally once daily.
  • Combination Rule: For the treatment of advanced prostate cancer, Bicalutamide therapy must be started at the exact same time as the LHRH analog treatment.
  • Administration Method: Tablets must be swallowed whole with a glass of water. They should not be crushed, split, or chewed.
  • Timing: Can be taken at any time of day, completely independent of food (with or without a meal). However, it should be taken at the exact same time each day to maintain steady therapeutic blood levels.

Contraindications & Precautions

  • Absolute Contraindications: Strictly contraindicated in individuals with a verified history of hypersensitivity to bicalutamide or any inactive ingredients in the tablet core. It is completely contraindicated in females, and it carries severe risks of fetal harm if exposed during pregnancy.
  • Hepatotoxicity Warning: Bicalutamide has been associated with severe liver injury, including rare cases of progressive hepatic failure, jaundice, and hospitalization. Serum transaminase levels (AST/ALT) must be measured before starting treatment and monitored at regular intervals during the first few months of therapy. Discontinue treatment immediately if significant elevations or signs of liver damage develop (e.g., dark urine, yellowing of skin or eyes, right upper abdominal pain).
  • Glucose Tolerance Changes: A reduction in glucose tolerance has been observed in males receiving combined antiandrogen therapy. Blood glucose levels should be monitored closely in individuals with pre-existing diabetes mellitus.
  • Cardiovascular Effects & QT Prolongation: Combined androgen deprivation therapy can prolong the cardiac QT interval. Clinicians should carefully weigh the risks in patients with congenital long QT syndrome, electrolyte imbalances, or congestive heart failure.
  • Gynecomastia and Breast Pain: Due to the shifting balance of hormones, breast enlargement (gynecomastia) and breast tenderness occur very frequently during single-agent use or long-term therapeutic regimens.

Potential Side Effects

  • Very Common / Expected: Hot flashes (sudden waves of heat), breast tenderness, gynecomastia, generalized weakness (asthenia), and localized pelvic or back pain.
  • Common / Mild: Nausea, constipation, diarrhea, localized edema (swelling of lower legs/ankles), decreased libido, erectile dysfunction, mild anemia, dizziness, weight gain, and dry skin.
  • Less Common / Severe: Severe drug-induced hepatotoxicity, interstitial lung disease (manifesting as sudden, unexplained shortness of breath or cough), hypersensitivity reactions (angioedema), and severe thrombocytopenia.
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