Dosing & Uses
Dosage Forms & Strengths
tablet
- 50mg
Prostate Cancer
50 mg PO qDay
Use in combination with LHRH analog
Locally Advanced Prostate Cancer
150 mg PO qDay as monotherapy
Monitor
LFTs at baseline, regular intervals for 4 months, then periodically
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Hot flashes (53%)
General pain (35%)
Back pain (25%)
Asthenia (22%)
Constipation (22%)
Pelvic pain (21%)
Infection (18%)
Nausea (15%)
Dyspnea (13%)
Edema (13%)
Peripheral edema (13%)
Diarrhea (12%)
Hematuria (12%)
Nocturia (12%)
Abdominal pain (11%)
Anemia (11%)
1-10%
Gynecomastia (9%)
Rash (9%)
UTI (9%)
Chest pain (8%)
Hypertension (8%)
Vomiting (8%)
Flu like symptoms (7%)
Headache (7%)
LFTs elevation (7%)
Weight loss (7%)
Anorexia (6%)
Breast pain (6%)
Anxiety (5%)
Arthritis (5%)
Postmarketing reports
Photosensitivity
Interstitial lung disease including interstitial pneumonitis and pulmonary fibrosis
Warnings
Contraindications
Hypersensitivity
Female patients (esp pregnant-may harm fetus)
Cautions
Hepatic impairment
Severe liver injury resulting in hospitalization or death reported
Spermatogenesi inhibition reported
Gynecomastia and breast pain reported during therapy when used as single agent
May reduce glucose tolerance in males when used in combination with LHRH; monitor blood glucose
Monitor prostate specific antigen (PSA) progression if PSA increases
Antiandrogen therapy may cause morphological changes in spermatozoa; based on findings in animal reproduction studies and its mechanism of action, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 130 days after administering final dose administered
Based on animal studies, therapy can lead to inhibition of spermatogenesis and may impair fertility in males of reproductive potential; long-term effects on male fertility not studied
Pregnancy & Lactation
Pregnancy
Contraindicated for use in pregnant women because it can cause fetal harm; not indicated for use in females; there are no human data on use in pregnant women; in animal reproduction studies, oral administration of bicalutamide to pregnant rats during organogenesis caused abnormal development of reproductive organs in male fetuses at exposures approximately 0.7 to 2 times the human exposure at recommended dose
Lactation
Not indicated for use in pregnant women; there is no information available on presence of bicalutamide in human milk, or on effects on breastfed infant or on milk production; bicalutamide has been detected in rat milk
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Nonsteroidal antiandrogen, competitively binds androgen receptors and inhibits testosterone stimulation of cell growth in prostate cancer
Pharmacokinetics
Half-Life: 5.8 d
Peak plasma time: 31 hr
Peak plasma concentration: 0.77 mcg/mL
Protein Bound: 96%
Metabolism: Liver
Clearance: 0.32 L/hr
Excretion: Urine (36%), feces (42%)
Dialyzable: No
Images
Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
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Adding plans allows you to:
- View the formulary and any restrictions for each plan.
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- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
