Version May 2024
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) (Ref).
Missed doses: If a dose is missed, skip the missed dose and take the next dose at the next scheduled time; do not double the next dose.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
No dosage adjustment necessary.
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.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Adverse reaction percentages reported as part of combination regimen with an LHRH analogue unless otherwise noted.
>10%:
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
Hypersensitivity to bicalutamide or any component of the formulation; use in women; pregnancy
Canadian labeling: Additional contraindications (not in the US labeling): Patients with localized prostate cancer undergoing watchful waiting; children
Concerns related to adverse effects:
• Gynecomastia: Bicalutamide may cause gynecomastia or breast pain at higher (off-label) doses.
• Hematologic: Anemia may occur with testosterone suppression; monitor CBC periodically as indicated.
• Hepatotoxicity: 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 treatment. Use with caution in moderate to severe hepatic dysfunction. Monitor transaminases (baseline and periodically); if clinical signs/symptoms suggestive of liver dysfunction (eg, nausea, vomiting, abdominal pain, fatigue, anorexia, flu-like symptoms, dark urine, jaundice, right upper quadrant pain) occur, promptly monitor liver function tests; discontinue if patients have jaundice or ALT is >2 × ULN.
• Hypersensitivity: Angioneurotic edema and urticaria have been reported.
• Interstitial lung disease: 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).
Disease-related concerns:
• 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; bicalutamide undergoes extensive hepatic metabolism. Limited data suggest 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:
• Warfarin: Excessive prolongation of prothrombin time (PT) and INR days to weeks after bicalutamide initiation in patients previously stable on warfarin therapy have been reported (postmarketing). Serious bleeding events, including intracranial, retroperitoneal, and GI events (requiring blood transfusion and/or phytonadione [vitamin K]), occurred. Monitor PT/INR in patients on concomitant warfarin therapy, and adjust warfarin dose as necessary.
Other warnings/precautions:
• 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.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Casodex: 50 mg
Generic: 50 mg
Yes
Tablets (Bicalutamide Oral)
50 mg (per each): $16.47 - $18.56
Tablets (Casodex Oral)
50 mg (per each): $131.85
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Casodex: 50 mg
Generic: 50 mg
Oral: 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.
Hazardous agent (NIOSH 2016 [group 1]).
Use appropriate precautions for receiving, handling, administration, and disposal. Gloves (single) should be worn during receiving, unpacking, and placing in storage. NIOSH recommends single gloving for administration of intact tablets or capsules (NIOSH 2016).
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
Locally advanced prostate cancer (monotherapy)
Bicalutamide may be confused with apalutamide, enzalutamide, flutamide, nilutamide.
Casodex may be confused with Kapidex [DSC]
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs that have a heightened risk of causing significant patient harm when used in error.
Casodex [US, Canada, and multiple international markets] may be confused with Capadex brand name for propoxyphene/acetaminophen [Australia, New Zealand]
Inhibits CYP3A4 (weak)
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
ALPRAZolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of ALPRAZolam. Risk C: Monitor therapy
Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Risk X: Avoid combination
Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical). Risk C: Monitor therapy
Astemizole: Bicalutamide may increase the serum concentration of Astemizole. Risk X: Avoid combination
CarBAMazepine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of CarBAMazepine. Risk C: Monitor therapy
Choline C 11: Antiandrogens may diminish the therapeutic effect of Choline C 11. Risk C: Monitor therapy
Cisapride: Bicalutamide may increase the serum concentration of Cisapride. Risk X: Avoid combination
CycloSPORINE (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of CycloSPORINE (Systemic). Risk C: Monitor therapy
Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Risk C: Monitor therapy
Finerenone: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Finerenone. Risk C: Monitor therapy
Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Risk C: Monitor therapy
Flotufolastat F18: Antiandrogens may diminish the diagnostic effect of Flotufolastat F18. Management: Therapies targeting the androgen pathway may result in changes in the uptake of flotufolastat F18 in prostate cancer. The impact of these therapies on the performance of flotufolastat F18 is unknown; consider use of alternative agents. Risk D: Consider therapy modification
Gallium Ga 68 PSMA-11: Antiandrogens may diminish the therapeutic effect of Gallium Ga 68 PSMA-11. Management: Therapies targeting the androgen pathway may result in changes in the uptake of gallium Ga 68 PSMA-11 (gozetotide) in prostate cancer. The impact on the performance of gallium Ga 68 PSMA-11 (gozetotide) is unknown; consider use of alternative agents. Risk D: Consider therapy modification
Indium 111 Capromab Pendetide: Antiandrogens may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Risk X: Avoid combination
Ixabepilone: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ixabepilone. Risk C: Monitor therapy
Lemborexant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Risk D: Consider therapy modification
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. Risk D: Consider therapy modification
Lonafarnib: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lonafarnib. Management: Avoid concurrent use of lonafarnib with weak CYP3A4 inhibitors. If concurrent use is unavoidable, reduce the lonafarnib dose to or continue at a dose of 115 mg/square meter. Monitor for evidence of arrhythmia, syncope, palpitations, or similar effects. Risk D: Consider therapy modification
Methoxsalen (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Methoxsalen (Systemic). Risk C: Monitor therapy
Midazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Midazolam. Risk C: Monitor therapy
NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Risk C: Monitor therapy
Piflufolastat F18: Antiandrogens may diminish the diagnostic effect of Piflufolastat F18. Management: Therapies targeting the androgen pathway may result in changes in the uptake of piflufolastat F18 in prostate cancer. The impact of these therapies on the performance of piflufolastat F18 is unknown; consider use of alternative agents. Risk D: Consider therapy modification
Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. Risk X: Avoid combination
Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Risk C: Monitor therapy
Simvastatin: CYP3A4 Inhibitors (Weak) may increase serum concentrations of the active metabolite(s) of Simvastatin. CYP3A4 Inhibitors (Weak) may increase the serum concentration of Simvastatin. Risk C: Monitor therapy
Sirolimus (Conventional): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Sirolimus (Conventional). Risk C: Monitor therapy
Sirolimus (Protein Bound): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Sirolimus (Protein Bound). Management: Reduce the dose of protein bound sirolimus to 56 mg/m2 when used concomitantly with a weak CYP3A4 inhibitor. Risk D: Consider therapy modification
Tacrolimus (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Terfenadine: Bicalutamide may increase the serum concentration of Terfenadine. Risk X: Avoid combination
Triazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Triazolam. Risk C: Monitor therapy
Ubrogepant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ubrogepant. Management: In patients taking weak CYP3A4 inhibitors, the initial and second dose (given at least 2 hours later if needed) of ubrogepant should be limited to 50 mg. Risk D: Consider therapy modification
Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Risk C: 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. Risk C: Monitor therapy
Based on the mechanism of action and findings in animal reproduction studies, bicalutamide may cause morphological changes in spermatozoa, inhibit spermatogenesis, and impair male fertility. Males with female partners of reproductive potential should use effective contraception during therapy and for 130 days after the last dose.
Bicalutamide is contraindicated for use in women, including pregnant women.
It is not known if bicalutamide is present in breast milk. Use is contraindicated in women.
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 and INR. Monitor adherence.
Cardiovascular monitoring for patients with prostate cancer: Comprehensive assessment prior to treatment including a history and physical examination, screening for cardiovascular disease risk factors such as hypertension, diabetes, dyslipidemia, obesity, and smoking; baseline and serial ECGs are recommended in patients at risk of QTc prolongation during androgen deprivation therapy (ADT); estimate 10-year cardiovascular disease risk in patients without cardiovascular disease at baseline; assess cardiovascular risk annually during ADT (ASCO [Armenian 2017]; ESC [Lyon 2022]).
Bicalutamide is a pure nonsteroidal androgen receptor inhibitor, specifically a competitive inhibitor for the binding of dihydrotestosterone and testosterone; prevents testosterone stimulation of cell growth in prostate cancer
Absorption: Well absorbed; unaffected by food
Protein binding: 96%
Metabolism: Extensively hepatic; glucuronidation and oxidation of the R (active) enantiomer to inactive metabolites; the S enantiomer is inactive
Half-life elimination: Active enantiomer: ~6 days (~10 days in severe hepatic impairment)
Time to peak, plasma: Active enantiomer: ~31 hours
Excretion: Urine and feces
Hepatic function impairment: The half-life is increased ~76% (to ~10 days) in patients with severe liver disease.
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