Uses
Prostate Cancer
Palliative treatment of metastatic (stage D2) prostate cancer; should be used in conjunction with a luteinizing hormone-releasing hormone (LHRH) analog (e.g., goserelin, leuprolide acetate).
Dosage and Administration
General
Administration
Oral Administration
Administer orally once daily at the same time each day (morning or evening) without regard to meals.
Dosage
Adults
Prostate Cancer
Oral
50 mg once daily. Duration of combined therapy with LHRH analog depends on clinical response.
Cautions
Contraindications
- Known hypersensitivity to bicalutamide or any ingredient in the formulation.
- Should not be used in women, particularly for conditions that are not serious or life-threatening.
- Women who are or may become pregnant. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)
Warnings/Precautions
Warnings
Fetal/Neonatal Morbidity and Mortality
May cause fetal harm; contraindicated in pregnant women.
If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.
Hepatic Effects
Severe liver injury reported, sometimes resulting in hospitalization and/or death; manifestations generally occurred within first 3–4 months.
Possible hepatitis or marked increases in serum concentrations of hepatic transaminases.
Measure serum transaminase concentrations prior to initiation of therapy, at regular intervals during the first 4 months, and periodically thereafter.
Immediately measure serum transaminase (especially ALT) concentrations if manifestations suggestive of liver dysfunction occur.
Immediately discontinue if jaundice develops or serum ALT concentration is >2 times ULN; monitor liver function closely thereafter.
General Precautions
Regularly monitor serum PSA to assess response; if PSA increases, evaluate for possible disease progression.
For patients with objective progression of disease and elevated serum PSA, consider temporarily withdrawing bicalutamide while continuing LHRH analog. Withdrawal of bicalutamide may be associated with PSA decrease.
Specific Populations
Pregnancy
Category X. (See Fetal/Neonatal Morbidity and Mortality and also Contraindications under Cautions.)
Lactation
Not known whether bicalutamide is distributed into milk; use caution.
Pediatric Use
Safety and efficacy not established.
Hepatic Impairment
Use with caution in patients with moderate to severe hepatic impairment.
Consider periodic liver function tests in patients with hepatic impairment receiving long-term therapy.
Women
Not intended for use in women, particularly for nonserious or nonlife-threatening conditions.
Common Adverse Effects
Combined therapy with LHRH analog: hot flashes, pain (including abdominal, back, and pelvic pain), asthenia, constipation, infection, nausea, dyspnea, diarrhea.
Gynecomastia and breast pain frequent if bicalutamide used as monotherapy.
Drug Interactions
Does not induce CYP isoenzymes. Pharmacokinetic interaction unlikely with drugs metabolized by CYP isoenzymes.
Specific Drugs
| Drug |
Interaction |
Comments |
| Alcohol |
Increased risk of facial flushing |
Avoid alcohol consumption during therapy |
| LHRH analog (e.g., goserelin, leuprolide) |
Pharmacokinetic interaction unlikely |
|
| Warfarin and other coumarins |
Decreased anticoagulant protein binding and increased plasma concentrations; increased anticoagulant effects |
Monitor PT; adjust anticoagulant dosage as needed |
Pharmacokinetics
Absorption
Bioavailability
Well-absorbed following oral administration; absolute bioavailability is unknown.
Food
Food has no clinically important effect on rate or extent of absorption.
Distribution
Plasma Protein Binding
96%.
Elimination
Metabolism
Undergoes stereospecific metabolism in the liver.
Active R-enantiomer is predominantly oxidized to an inactive metabolite followed by glucuronidation. Inactive S-enantiomer is principally metabolized by glucuronidation.
S-enantiomer is rapidly cleared relative to the R-enantiomer; R-enantiomer accounts for about 99% of total steady-state plasma concentrations.
Elimination Route
Both parent and metabolite glucuronides are eliminated in urine and feces.
Half-life
Approximately 6 days.
Special Populations
Half-life of R-enantiomer was increased approximately 76% in patients with severe hepatic impairment.
Stability
Storage
Oral
Tablets
20–25°C.
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