Overview
Bicalutamide is a non-steroidal antiandrogen used in combination with LHRH analogs for the treatment of metastatic prostate cancer. It works by competitively inhibiting androgen binding at androgen receptors, blocking the effects of testosterone on prostate cancer cells. The 50 mg dose is approved for combination therapy, while the 150 mg dose is not FDA-approved.
Mechanism of Action
Bicalutamide is a non-steroidal antiandrogen that competitively inhibits androgen binding to androgen receptors in target tissues. It blocks the effects of testosterone and dihydrotestosterone on prostate cancer cells, inhibiting androgen-stimulated tumor growth.
Indications
- Combination therapy with LHRH analogs for Stage D metastatic prostate carcinoma
- Monotherapy or combination therapy with other treatments (50 mg dose only)
Common Doses
- 50 mg
Dosage
50 mg tablet taken orally once daily, typically in combination with LHRH analog therapy. The 150 mg dose is not FDA-approved.
Contraindications
- Hypersensitivity to bicalutamide or any tablet components
- Use in women
- Pregnancy
Side Effects
- Hot flashes
- Gynecomastia
- Breast pain
- Asthenia
- Constipation
- Nausea
- Diarrhea
- Back pain
- Pelvic pain
- Increased liver enzymes
Interactions
- Inhibits CYP 3A4 - use caution with substrates like midazolam
- Displaces coumarin anticoagulants from protein binding sites - monitor PT/INR
- No significant interaction with LHRH analogs (goserelin, leuprolide)
Counseling Points
- Take once daily at the same time each day
- May be taken with or without food
- Report signs of liver problems (jaundice, dark urine, abdominal pain)
- Use effective contraception if partner could become pregnant
- Monitor for signs of hypersensitivity reactions
- Regular follow-up with healthcare provider for monitoring