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Synonyms
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Casodex: Targeted Androgen Blockade for Advanced Prostate Cancer
Casodex (bicalutamide) is a non-steroidal anti-androgen medication specifically developed for the treatment of advanced prostate cancer. It functions as a competitive antagonist at androgen receptors, effectively blocking the action of testosterone and dihydrotestosterone on prostate cancer cells. When used in combination with a luteinizing hormone-releasing hormone (LHRH) analog, Casodex provides complete androgen blockade, representing a cornerstone in the management of metastatic prostate cancer. Its well-established efficacy profile and generally favorable tolerability make it a fundamental component of advanced prostate cancer treatment protocols worldwide.
Features
- Contains bicalutamide as the active pharmaceutical ingredient
- Available in 50 mg film-coated tablets
- Exhibits high affinity binding to androgen receptors
- Demonstrates pure anti-androgenic activity without intrinsic hormonal effects
- Features a long elimination half-life (approximately 5-6 days)
- Administered as once-daily oral therapy
- Shows minimal impact on libido compared to other anti-androgens
- Maintains stable pharmacokinetic profile with consistent absorption
Benefits
- Effectively suppresses testosterone stimulation of prostate cancer growth
- Delays disease progression in advanced prostate cancer stages
- Provides palliative relief from cancer-related symptoms including bone pain
- Extends progression-free survival when combined with LHRH therapy
- Offers convenient once-daily dosing regimen for patient compliance
- Maintains quality of life through targeted hormonal manipulation
Common use
Casodex is primarily indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of advanced prostate cancer. This combination approach provides maximal androgen blockade by simultaneously suppressing testicular testosterone production (via LHRH analog) and blocking androgen receptor binding at the cellular level (via Casodex). The medication is typically initiated concurrently with LHRH therapy or may be started several days before LHRH administration to prevent disease flare. Clinical evidence supports its use in metastatic prostate cancer (stage D2) where it has demonstrated significant improvements in time to progression and overall survival compared to monotherapy approaches.
Dosage and direction
The standard adult dosage for Casodex in combination with an LHRH analog is one 50 mg tablet administered orally once daily. Administration should occur at approximately the same time each day, with or without food, as pharmacokinetic studies show no significant effect of food on absorption. Tablets should be swallowed whole with water and not chewed or crushed. Treatment is typically continued until disease progression or unacceptable toxicity occurs. For patients with hepatic impairment, dosage adjustment may be necessary based on liver function parameters. No dosage adjustment is required for renal impairment, though careful monitoring is advised.
Precautions
Regular monitoring of liver function tests is mandatory during treatment with Casodex, particularly during the first four months of therapy and periodically thereafter. Patients should be advised about potential hepatotoxicity and instructed to report symptoms including jaundice, dark urine, pruritus, right upper quadrant pain, or unexplained flu-like symptoms immediately. Periodic complete blood counts should be performed to monitor for potential hematological effects. Patients with pre-existing cardiac conditions require careful cardiovascular monitoring due to potential QT interval prolongation. Regular bone density assessments may be warranted in long-term users due to accelerated bone mineral density loss associated with androgen deprivation therapy.
Contraindications
Casodex is contraindicated in patients with known hypersensitivity to bicalutamide or any component of the formulation. It should not be administered to women, particularly those who are pregnant or may become pregnant, due to potential teratogenic effects. The medication is contraindicated in patients with severe hepatic impairment (Child-Pugh Class C) unless the potential benefits outweigh the risks and appropriate monitoring can be ensured. Concomitant use with terfenadine, astemizole, or cisapride is contraindicated due to potential QT prolongation and arrhythmia risk.
Possible side effect
The most frequently reported adverse reactions include hot flashes (49%), pain (generalized) (18%), constipation (12%), asthenia (16%), nausea (11%), and diarrhea (8%). Hepatic abnormalities may occur, with elevated transaminases reported in approximately 6% of patients. Cardiovascular effects including hypertension (7%) and peripheral edema (5%) have been observed. Gynecomastia (38%) and breast pain (39%) are common due to the anti-androgenic mechanism of action. Less frequently, patients may experience dyspnea, anemia, rash, or weight gain. Serious but rare adverse events include hepatotoxicity, interstitial pneumonitis, and QT interval prolongation.
Drug interaction
Casodex is primarily metabolized by cytochrome P450 3A4 (CYP3A4), creating potential for significant drug interactions. Concomitant administration with strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir) may increase bicalutamide exposure, necessitating dose reduction or increased monitoring. Inducers of CYP3A4 (rifampin, carbamazepine, phenytoin) may decrease bicalutamide concentrations, potentially reducing efficacy. Warfarin co-administration requires careful monitoring of prothrombin time due to potential enhancement of anticoagulant effect. Casodex may increase concentrations of drugs metabolized by CYP2C9, CYP2C19, and CYP3A4, though clinical significance varies. Concomitant use with other QT-prolonging agents should be avoided or carefully monitored.
Missed dose
If a dose of Casodex is missed, the patient should take it as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Consistency in dosing is important for maintaining stable drug concentrations, but single missed doses are unlikely to significantly impact overall efficacy due to the drug’s long half-life. Patients should be instructed to maintain a regular dosing routine and consider using reminder systems if adherence issues persist.
Overdose
There is no specific antidote for Casodex overdose. Reported cases of overdose have been limited, with no specific pattern of toxicity identified. Management should consist of supportive measures and symptomatic treatment. Given the drug’s extensive protein binding and large volume of distribution, dialysis is unlikely to be effective. Gastrointestinal decontamination may be considered if presentation occurs shortly after ingestion. Monitoring should include assessment of hepatic function, electrolyte balance, and cardiac rhythm due to potential QT prolongation. Supportive care should be maintained until the drug is eliminated, considering the prolonged half-life of approximately 5-6 days.
Storage
Casodex tablets should be stored at controlled room temperature between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). The medication should be kept in its original container with the lid tightly closed to protect from moisture and light. Tablets should not be stored in bathroom cabinets or other areas subject to high humidity. Keep out of reach of children and pets. Do not use tablets that show signs of physical damage, discoloration, or that are beyond the expiration date printed on the packaging. Proper storage conditions are essential for maintaining pharmaceutical stability and efficacy.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Casodex is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Treatment decisions should be made based on individual patient characteristics, comprehensive clinical assessment, and consideration of all available therapeutic options. The prescribing physician should be consulted for specific dosage recommendations and management of potential adverse effects. Patients should not alter their treatment regimen without medical guidance. While every effort has been made to ensure accuracy, medical knowledge evolves, and current prescribing information should always be consulted.
Reviews
Clinical studies demonstrate that Casodex in combination with LHRH analogs significantly improves progression-free survival compared to monotherapy (HR 0.80, 95% CI 0.72-0.89). Meta-analyses of randomized controlled trials show a consistent overall survival benefit with combined androgen blockade versus LHRH alone in advanced prostate cancer. Patient-reported outcomes indicate better preservation of physical capacity and quality of life measures compared to alternative anti-androgens. Oncologists frequently note the favorable side effect profile, particularly reduced incidence of diarrhea and improved hepatic safety compared to first-generation anti-androgens. Long-term follow-up data support its position as a well-tolerated component of combination therapy for advanced prostate cancer management.
