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Drugs reference index «Bicalutamide»



Pronunciation: (BYE-ka-LOO-ta-mide)Class: Antiandrogen

Trade Names:Bicalutamide- Tablets 50 mg

Trade Names:Casodex- Tablets 50 mg

CO Bicalutamide (Canada)Novo-Bicalutamide (Canada)PMS-Bicaltamide (Canada)ratio-Bicalutamide (Canada)Sandoz Bicalutamide (Canada)


Bicalutamide inhibits the action of androgens.



Well absorbed. T max is 31.3 h (active isomer). C max is 0.77 mcg/mL (active isomer).


96% protein bound.


Undergoes stereospecific metabolism. The S-isomer (inactive) is metabolized by glucuronidation. The R-isomer (active) undergoes glucuronidation but is predominantly oxidized to an inactive metabolite.


Eliminated in urine and feces; half-life is 5.8 days (active isomer).

Special Populations

Renal Function Impairment

No dosage adjustment is necessary.

Hepatic Function Impairment

The half-life of the R-isomer is increased about 76% in patients with severe liver disease. No dosage adjustment is necessary.

Indications and Usage

Stage D 2 metastatic carcinoma of the prostate in combination with a luteinizing hormone–releasing hormone (LHRH) analog.


Women; pregnancy; hypersensitivity to the drug or any of the tablet components.

Dosage and Administration

Advanced Prostate CancerAdults

PO 50 mg (1 tablet) once daily at the same time of day with or without food.

General Advice

  • Start bicalutamide at the same time as treatment with an LHRH analog.


Store tablets at controlled room temperature (68° to 77°F).

Drug Interactions

CYP3A4 substrates (eg, midazolam)

Mean midazolam C max increased 1.5-fold and AUC increased 1.9-fold when given with bicalutamide. Use caution when coadministered with CYP3A4 substrates.


PT may increase when bicalutamide is initiated in patients stabilized on long-term warfarin therapy.

Laboratory Test Interactions

None well documented.

Adverse Reactions


Hot flashes (53%); hypertension (8%); angina pectoris, CHF, coronary artery disease, heart arrest, MI, syncope (2% to 5%).


Asthenia (22%); dizziness (10%); paresthesia (8%); headache, insomnia (7%); anxiety (5%); depression (4%); confusion, hypertonia, libido decreased, nervousness, neuropathy, somnolence (2% to 5%).


Rash (9%); sweating (6%); alopecia, dry skin, herpes zoster, pruritus, skin carcinoma, skin disorder (2% to 5%).


Constipation (22%); nausea (15%); diarrhea (12%); abdominal pain (11%); dyspepsia, liver enzymes increased (7%); anorexia, flatulence, vomiting (6%); dry mouth, dysphagia, GI carcinoma, GI disorder, melena, periodontal abscess, rectal hemorrhage (2% to 5%).


Hematuria, nocturia (12%); gynecomastia, UTI (9%); impotence (7%); breast pain, urinary frequency (6%); impaired urination, urinary retention (5%); urinary incontinence (4%); dysuria, hydronephrosis, urinary tract disorder, urinary urgency (2% to 5%).


Peripheral edema (13%); weight loss (7%); hyperglycemia (6%); alkaline phosphatase increased, weight gain (5%); BUN increased, creatinine increased, dehydration, edema, gout, hypercholesterolemia (2% to 5%).


Back pain (25%); bone pain (9%); myasthenia (7%); arthritis (5%); pathological fracture (4%); leg cramps, myalgia (2% to 5%).


Dyspnea (13%); cough increased, pharyngitis (8%); bronchitis (6%); pneumonia, rhinitis (4%); asthma, epistaxis, lung disorder, sinusitis (2% to 5%); interstitial lung disease, including interstitial pneumonitis and pulmonary fibrosis (postmarketing).


General pain (35%); pelvic pain (21%); infection (18%); anemia (11%); chest pain (8%); flu syndrome (7%); cataract specified, chills, cyst, fever, hernia, neck pain, neoplasm, sepsis (2% to 5%).



Regularly monitor prostate-specific antigen and evaluate for clinical progression if levels rise. Measure serum transaminase levels prior to starting bicalutamide, at regular intervals for the first 4 mo, and periodically thereafter. Discontinue if patient develops jaundice or if ALT rises above 2 times the ULN.


Category X .


Bicalutamide is not indicated for use in women.


Safety and efficacy not established.


Reactions, including angioneurotic edema and urticaria, have been reported.

Hepatic Function

Use bicalutamide with caution in patients with moderate to severe hepatic function impairment.


Administration of bicalutamide may lead to inhibition of spermatogenesis. Long-term effects are not known.

Hazardous Tasks

Somnolence has been reported during treatment with bicalutamide. Advise patients to use caution when driving or operating machinery.

Glucose tolerance

Reduction in glucose tolerance reported in men receiving LHRH agonists. Consider monitoring blood glucose in patients receiving bicalutamide in combination with LHRH agonists.

Gynecomastia/Breast pain

Reported in patients treated for prostate cancer.


Rare cases of death or hospitalization because of severe liver injury. Generally occurred within the first 3 to 4 mo of treatment.

Patient Information

  • Advise patients to notify health care provider if any of the following symptoms occur: abdominal pain, anorexia, dark urine, fatigue, “flu-like” symptoms, jaundice, nausea, right upper quadrant tenderness, vomiting.
  • Inform patients that bicalutamide and the LHRH analog will be initiated at the same time and not to interrupt or stop taking these medications without consulting health care provider.
  • Advise patients that bicalutamide may cause drowsiness and to use caution when driving or operating machinery.

Copyright © 2009 Wolters Kluwer Health.

  • Bicalutamide MedFacts Consumer Leaflet (Wolters Kluwer)
  • Bicalutamide Prescribing Information (FDA)
  • bicalutamide Advanced Consumer (Micromedex) - Includes Dosage Information
  • Casodex Prescribing Information (FDA)
  • Casodex Consumer Overview

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