Casodex: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on April 5, 2023.

1. How it works

• Casodex is a brand (trade) name for bicalutamide which is an anti-androgen that may be used to treat prostate cancer.
• Prostate cancer growth is increased or boosted by the male hormone testosterone, which is an androgen. In men with prostate cancer, testosterone acts on androgen receptors in the prostate to increase cancer growth. Casodex is an androgen receptor inhibitor that works by blocking the androgen receptors in the prostate, preventing any available testosterone from stimulating prostate cancer growth.
• Casodex is always given in combination with an LHRH agonist and they work together to slow prostate cancer growth.
• Casodex belongs to the class of medicines known as anti-androgens.

2. Upsides

• Casodex 50mg daily may be used in combination with a luteinizing hormone-releasing hormone (LHRH) agonist to treat Stage D2 metastatic prostate cancer. LHRH agonists reduce the amount of testosterone that is released from the testicles, meaning there is less testosterone available to stimulate prostate cancer growth.
• Casodex is not a form of chemotherapy.
• May be taken with or without food.
• Casodex is an oral tablet.
• No dosage adjustment is needed in people with kidney disease or mild-to-moderate liver disease.
• Casodex is available as a cost-saving generic.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Hot flashes were the most frequent side effect reported when Casodex was used in combination with an LHRH agonist, reported in 53% of men. Other common side effects included general pain, back pain, pelvic pain, lack of energy, infection, abdominal pain, chest pain, headache, constipation, nausea, diarrhea, anemia, edema, and dizziness. High blood pressure, photosensitivity, urinary problems, respiratory problems, and skin side effects were also reported.
• May cause gynecomastia and breast pain which often results in treatment discontinuation.
• May reduce glucose tolerance which can manifest as diabetes or a loss of glycemic control in those with pre‑existing diabetes. Consider more frequent monitoring of blood glucose levels.
• Casodex 150mg daily is NOT approved for use in the United States. Two studies showed that it was associated with a higher risk of death (25% and 31%) compared with men who were castrated. Do not exceed the recommended dose of 50mg/day.
• Casodex should be always prescribed in combination with an LHRH agonist. LHRH agonists available in the U.S. are leuprolide (Lupron, Eligard), goserelin (Zoladex), triptorelin (Trelstar), and histrelin (Vantas).
• Casodex should not be used in women and in those who have reported an allergy to it.
• Has been associated with severe liver injury (hepatic failure) causing hospitalization and death which generally occurred within the first three to four months of treatment. Measure serum transaminase levels before starting treatment with Casodex, then at regular intervals for the first four months of treatment, and periodically thereafter. Measure serum ALT with any symptoms suggestive of liver dysfunction such as nausea, vomiting, abdominal pain, fatigue, anorexia, “flu-like” symptoms, dark urine, jaundice, or right upper quadrant tenderness. Discontinue Casodex immediately if ALT rises above two times the upper limit of normal.
• May interact with coumarin anticoagulants causing serious bleeding including intracranial, retroperitoneal, and gastrointestinal requiring blood transfusion and/or administration of vitamin K. Closely monitor prothrombin time (PT) and International Normalized Ratio (INR) and consider a dosage reduction of warfarin.
• Advise men that Casodex can adversely affect sperm and a subsequent developing baby and that they and their partners should use adequate and effective contraception to ensure pregnancy does not happen while they are taking Casodex and for at least 130 days after the final dose. Casodex may also affect a man's long-term fertility.
• Casodex is extensively metabolized by the liver and should be used with caution in men with moderate-to-severe liver disease. Consider periodic liver function tests.
• The safety and effectiveness of Casodex in male children has not been established although it has been used in clinical trials to treat gonadotropin-independent precocious puberty in boys with familial male-limited precocious puberty, also known as testotoxicosis.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Casodex is an androgen receptor inhibitor that may be used in combination with an LHRH agonist (such as leuprolide or goserelin) for the treatment of prostate cancer. Hot flashes are the main side effect and it may also cause breast enlargement, pain, and gastrointestinal side effects.

5. Tips

• Casodex is usually always prescribed in combination with an LHRH agonist such as leuprolide (Lupron, Eligard), goserelin (Zoladex), triptorelin (Trelstar), and histrelin (Vantas). The LHRH agonist reduces testosterone levels and Casodex blocks testosterone from binding to androgen receptors. These two actions reduce the stimulation of prostate cancer growth.
• Take Casodex exactly as directed by your doctor. Do not take any more or any less. Do not share your Casodex with anyone; Casodex should never be given to women.
• Casodex may be taken with or without food.
• Casodex should be taken at the same time each day alongside the LHRH agonist.
• If you miss a dose of Casodex, do not take the missed dose, just take the next dose at the scheduled time. Do not double the next dose.
• If you are diabetic, you may need to monitor your blood glucose levels more regularly while you are taking Casodex.
• Casodex may cause drowsiness. Be careful operating machinery or performing hazardous tasks if Casodex affects you in this way.
• Casodex may cause breast enlargement and hot flashes. If you experience any other worrying or intolerable side effects with Casodex, talk to your doctor about these. Do not stop Casodex or your LHRH agonist without talking to your doctor first.
• Casodex may cause liver dysfunction. Call your doctor immediately if you experience nausea, vomiting, abdominal pain, fatigue, anorexia, “flu-like” symptoms, dark urine, jaundice, or right upper quadrant tenderness.
• Casodex can adversely affect sperm and a subsequent developing baby. You and your partner (if they are of childbearing age) should use adequate and effective contraception to ensure pregnancy does not happen while you are taking Casodex and for at least 130 days after the final dose. Casodex may also affect your long-term fertility.
• Casodex can make you more sensitive to sunlight. Always use sunscreen and sun-protective clothing when going outside and try to avoid direct exposure to excessive sunlight or UV‑light exposure.
• Always talk to your doctor or pharmacist before taking any other medications with Casodex including supplements or herbals or medicines brought from a supermarket or drug store.
• Store Casodex tablets at room temperature, 20°-25°C (68°-77°F).

6. Response and effectiveness

• When Casodex is used in combination with a luteinizing hormone-releasing hormone (LHRH) agonist (either leuprolide depot or goserelin implant) Casodex + an LHRH agonist is more effective than leuprolide on its own and just as effective as flutamide + leuprolide.
• Another clinical trial was completed comparing the treatment of Casodex + LHRH agonist with flutamide + LHRH agonist for Stage D2 Prostate Carcinoma. The results showed both treatment options had similar effects with no significant difference between survival time (time to death), time to tumor progression, and quality of life.
• Casodex is taken long-term. In a clinical trial, the median follow-up time was 160 weeks (approximately 3 years). The length of time a man will be on Casodex depends on his cancer stage, other cancer therapies he is using, how well he responds to Casodex, and the amount and severity of side effects.
• Consider regular assessments of serum Prostate Specific Antigen (PSA) to monitor the patient’s response. If PSA levels rise, evaluate the patient for disease progression.

7. Interactions

Medicines that interact with Casodex may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with Casodex. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

There are over 300 medications that have major or moderate interactions with Casodex. Some common medications that may interact with Casodex include:

• anticancer treatments, such as ceritinib or nilotinib
• antidepressants, such as amitriptyline, citalopram, escitalopram, or venlafaxine
• antifungals such as fluconazole or ketoconazole
• antihistamines, such as terfenadine or hydroxyzine
• antipsychotics, such as aripiprazole, haloperidol, thioridazine, or ziprasidone
• bisacodyl
• chloroquine
• cisapride
• corticosteroids, such as budesonide
• ergot derivatives, such as ergotamine
• heart medications, such as flecainide
• herbals, such as black cohosh or cannabidiol
• HIV medications, such as saquinavir
• leflunomide
• lithium
• magnesium salts
• methadone
• methotrexate
• mineral oil
• multiple sclerosis agents such as fingolimod or ozanimod
• moxifloxacin
• ondansetron
• papaverine
• PDE5 inhibitors such as sildenafil and tadalafil
• peginterferon
• pimozide
• procainamide
• quinidine
• salmeterol
• senna
• sotalol
• statins, such as atorvastatin or simvastatin
• tamoxifen
• warfarin (may cause serious bleeding in those already stabilized on coumarin anticoagulants. Closely monitor prothrombin time (PT) and International Normalized Ratio (INR) and consider a dosage reduction of warfarin).

There is no evidence that Casodex induces hepatic enzymes.

Note that this list is not all-inclusive and includes only common medications that may interact with Casodex. You should refer to the prescribing information for Casodex for a complete list of interactions.

References

• Casodex (bicalutamide) [Package Insert]. Updated 10/2022. AstraZeneca Pharmaceuticals LP. https://www.drugs.com/pro/casodex.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Casodex only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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