(bye ka LOO ta mide)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Casodex: 50 mg
Generic: 50 mg
Brand Names: U.S.
- Antineoplastic Agent, Antiandrogen
Androgen receptor inhibitor; pure nonsteroidal antiandrogen that binds to androgen receptors; specifically a competitive inhibitor for the binding of dihydrotestosterone and testosterone; prevents testosterone stimulation of cell growth in prostate cancer
Well absorbed; unaffected by food
Extensively hepatic; glucuronidation and oxidation of the R (active) enantiomer to inactive metabolites; the S enantiomer is inactive
Urine and feces
Time to Peak
Active enantiomer: ~31 hours
Active enantiomer: ~6 days (~10 days in severe hepatic impairment)
Special Populations: Hepatic Function Impairment
The half-life is increased ~76% (to ~10 days) in patients with severe liver disease.
Use: Labeled Indications
Prostate cancer, metastatic: Treatment of stage D2 metastatic prostate cancer (in combination with an LHRH agonist)
Limitation of use: Bicalutamide 150 mg daily is not approved for use alone or with other treatments
Off Label Uses
Locally-advanced prostate cancer (monotherapy)
Data from a large randomized, double blind, placebo-controlled study in patients with prostate cancer suggests a benefit from the use of bicalutamide monotherapy in men with locally-advanced prostate cancer who are at higher risk for recurrence, although men at low risk for recurrence may not benefit from bicalutamide monotherapy [McLeod 2006]. Additional trials may be necessary to further define the role of bicalutamide in this condition.
Hypersensitivity to bicalutamide or any component of the formulation; use in women.
Canadian labeling: Additional contraindications (not in the US labeling): Patients with localized prostate cancer undergoing watchful waiting; children
Prostate cancer, metastatic: Oral: 50 mg once daily (in combination with an LHRH analogue)
Prostate cancer, locally-advanced, high recurrence risk (off-label use): Oral: 150 mg once daily (as monotherapy) (McLeod 2006). Additional trials may be necessary to further define the role of bicalutamide in this condition.
Refer to adult dosing.
Dosing: Renal Impairment
No dosage adjustment necessary.
Dosing: Hepatic Impairment
Hepatic impairment at treatment initiation: Mild, moderate, or severe impairment: No dosage adjustment is necessary. Use with caution in patients with moderate-to-severe impairment; clearance may be delayed in severe impairment (based on a limited number of patients).
Hepatic impairment during treatment: ALT >2 times ULN or development of jaundice: Discontinue immediately.
Dose should be taken at the same time each day, either in the morning or in the evening. May be administered with or without food. Treatment for metastatic cancer should be started concomitantly with an LHRH analogue.
Store at room temperature of 20°C to 25°C (68°F to 77°F).
Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Avoid combination
Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical). Monitor therapy
ARIPiprazole: CYP3A4 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy and/or indication. Consult full interaction monograph for specific recommendations. Monitor therapy
Astemizole: Bicalutamide may increase the serum concentration of Astemizole. Avoid combination
Choline C 11: Antiandrogens may diminish the therapeutic effect of Choline C 11. Monitor therapy
Cisapride: Bicalutamide may increase the serum concentration of Cisapride. Avoid combination
Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Monitor therapy
Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Monitor therapy
Indium 111 Capromab Pendetide: Antiandrogens may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Avoid combination
Lomitapide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Consider therapy modification
NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Monitor therapy
Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. Avoid combination
Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Monitor therapy
Terfenadine: Bicalutamide may increase the serum concentration of Terfenadine. Avoid combination
Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy
Vitamin K Antagonists (eg, warfarin): Bicalutamide may increase the serum concentration of Vitamin K Antagonists. Specifically, free concentrations of the vitamin K antagonists may be increased. Monitor therapy
Adverse reaction percentages reported as part of combination regimen with an LHRH analogue unless otherwise noted.
Cardiovascular: Peripheral edema (13%)
Central nervous system: Pain (35%)
Endocrine & metabolic: Hot flash (53%), gynecomastia (9%; monotherapy [150 mg]: 38% to 73% [McLeod 2006])
Gastrointestinal: Constipation (22%), nausea (15%), diarrhea (12%), abdominal pain (11%)
Genitourinary: Mastalgia (6%; monotherapy [150 mg]: 39% to 85% [McLeod 2006]), pelvic pain (21%), hematuria (12%), nocturia (12%)
Hematologic & oncologic: Anemia (11%)
Infection: Infection (18%)
Neuromuscular & skeletal: Back pain (25%), weakness (22%)
Respiratory: Dyspnea (13%)
≥2% to 10%:
Cardiovascular: Chest pain (8%), hypertension (8%), angina pectoris (2% to <5%), cardiac arrest (2% to <5%), cardiac failure (2% to <5%), coronary artery disease (2% to <5%), edema (2% to <5%), myocardial infarction (2% to <5%), syncope (2% to <5%)
Central nervous system: Dizziness (10%), paresthesia (8%), headache (7%), insomnia (7%), myasthenia (7%), anxiety (5%), chills (2% to <5%), confusion (2% to <5%), drowsiness (2% to <5%), hypertonia (2% to <5%), nervousness (2% to <5%), neuropathy (2% to <5%), depression (4%)
Dermatologic: Skin rash (9%), diaphoresis (6%), alopecia (2% to <5%), pruritus (2% to <5%), xeroderma (2% to <5%)
Endocrine & metabolic: Weight loss (7%), hyperglycemia (6%), weight gain (5%), decreased libido (2% to <5%), dehydration (2% to <5%), gout (2% to <5%), hypercholesterolemia (2% to <5%)
Gastrointestinal: Dyspepsia (7%), anorexia (6%), flatulence (6%), vomiting (6%), dysphagia (2% to <5%), hernia (2% to <5%), melena (2% to <5%), periodontal abscess (2% to <5%), xerostomia (2% to <5%)
Genitourinary: Urinary tract infection (9%), impotence (7%), difficulty in micturition (5%), urinary retention (5%), dysuria (2% to <5%), urinary urgency (2% to <5%), urinary incontinence (4%)
Hematologic & oncologic: Gastrointestinal carcinoma (2% to <5%), rectal hemorrhage (2% to <5%), skin carcinoma (2% to <5%)
Hepatic: Increased liver enzymes (7%), increased serum alkaline phosphatase (5%)
Infection: Herpes zoster (2% to <5%), sepsis (2% to <5%)
Neuromuscular & skeletal: Ostealgia (9%), arthritis (5%), leg cramps (2% to <5%), myalgia (2% to <5%), neck pain (2% to <5%), pathological fracture (4%)
Ophthalmic: Cataract (2% to <5%)
Renal: Polyuria (6%), hydronephrosis (2% to <5%), increased blood urea nitrogen (2% to <5%), increased serum creatinine (2% to <5%)
Respiratory: Cough (8%), pharyngitis (8%), flu-like symptoms (7%), bronchitis (6%), asthma (2% to <5%), epistaxis (2% to <5%), sinusitis (2% to <5%), pneumonia (4%), rhinitis (4%)
Miscellaneous: Cyst (2% to <5%), fever (2% to <5%)
<1%, postmarketing, and/or case reports: Decreased glucose tolerance, decreased hemoglobin, decreased white blood cell count, hepatic failure, hepatitis, hepatotoxicity, hypersensitivity (including angioedema and urticaria), increased serum ALT, increased serum AST, increased serum bilirubin, interstitial pneumonitis, interstitial pulmonary disease (most often at doses >50 mg), pulmonary fibrosis, skin photosensitivity
Concerns related to adverse effects:
• Gynecomastia: May cause gynecomastia or breast pain at higher (off-label) doses.
• Hematologic: Anemia may occur with testosterone suppression; monitor CBC periodically as indicated.
• Hepatotoxicity: Rare cases of death or hospitalization due to severe liver injury have been reported (postmarketing); hepatotoxicity generally occurs within the first 3 to 4 months of use. Use with caution in moderate-to-severe hepatic dysfunction. Monitor transaminases (baseline and periodically); if clinical signs/symptoms suggestive of liver dysfunction occur, promptly monitor liver function tests; discontinue if patients have jaundice or ALT is >2 times the upper limit of normal.
• Hypersensitivity: Angioneurotic edema and urticaria have been reported.
• Interstitial lung disease: Has been reported rarely (including fatalities) although mostly at dosages greater than what is recommended; promptly evaluate any worsening of respiratory symptoms (eg, dyspnea, cough and fever).
• Spermatogenesis: May lead to spermatogenesis inhibition.
• Cardiovascular disease: Androgen-deprivation therapy may increase the risk for cardiovascular disease (Levine 2010). Androgen deprivation therapy may cause prolongation of the QT/QTc interval (Garnick 2004); evaluate risk versus benefit in patients with congenital long QT syndrome, heart failure, frequent electrolyte abnormalities, and in patients taking medication known to prolong the QT interval. Correct electrolytes prior to initiation and consider periodic electrolyte and ECG monitoring.
• Decreased bone mineral density: Prolonged use of antiandrogen therapy is associated with decreased bone mineral density and an increased risk of osteoporosis and fracture (Smith 2003); alcohol abuse, familial history of osteoporosis, and/or chronic use of drugs capable of decreasing bone mass (eg, corticosteroids) may increase risk. Evaluate risk carefully before initiating therapy.
• Diabetes: When used in combination with LHRH agonists, a loss of glycemic control and decrease in glucose tolerance has been reported in patients with diabetes; monitor.
• Hepatic impairment: Use with caution in moderate-to-severe impairment; undergoes extensive hepatic metabolism. Limited data suggests excretion may be delayed in severe impairment leading to further drug accumulation. Consider periodic monitoring of liver function with prolonged therapy.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• Anti-androgen withdrawal syndrome: Discontinue use immediately if disease worsens; decreased prostate specific antigen (PSA) levels and/or clinical improvement may be observed in some patients when antiandrogen therapy is held due to worsening of disease.
Periodically monitor CBC, ECG, echocardiograms, serum testosterone, luteinizing hormone, and prostate specific antigen (PSA). Liver function tests should be obtained at baseline and repeated regularly during the first 4 months of treatment, and periodically thereafter; monitor for signs and symptoms of liver dysfunction. Monitor blood glucose in patients with diabetes. If initiating bicalutamide in patients who are on warfarin, closely monitor prothrombin time.
Bicalutamide is contraindicated in women. Androgen receptor inhibition during pregnancy may affect fetal development. In addition, male fertility may be impaired. Males with female partners of reproductive potential should use effective contraception during therapy and for 130 days after the last dose.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience nausea, diarrhea, fatigue, anxiety, constipation, sexual dysfunction, hot flashes, sensation of warmth, sweating a lot, back pain, abdominal pain, or pelvic pain. Have patient report immediately to prescriber signs of high blood sugar (confusion, fatigue, increased thirst, increased hunger, polyuria, flushing, fast breathing, or breath that smells like fruit), signs of infection, signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of a severe pulmonary disorder (lung or breathing problems like difficulty breathing, shortness of breath, or a cough that is new or worse), shortness of breath, excessive weight gain, swelling of arms or legs, enlarged breasts, breast pain, vision changes, urinary retention, change in amount of urine passed, angina, hematuria, severe dizziness, passing out, muscle weakness, severe loss of strength and energy, or severe headache (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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- Drug class: antiandrogens
Other brands: Casodex