Casodex tablet for treatment of metastatic prostate cancer

Casodex is a tablet containing bicalutamide, used in combination with luteinizing hormone-releasing hormone (LHRH) analogs for managing Stage D2 metastatic prostate cancer in adult males. It acts as an androgen receptor inhibitor to block male hormones that contribute to prostate cancer growth.

Casodex 50 mg daily tablets are indicated for use only in adult males as part of combination therapy with an LHRH analog to treat Stage D2 metastatic carcinoma of the prostate. It is not approved for use as monotherapy or for use in females or children.

bicalutamide

Bicalutamide, the active ingredient in Casodex, works by blocking androgen receptors, which prevents male hormones like testosterone from stimulating prostate cancer cells. This antiandrogen effect helps slow the growth and spread of prostate cancer when given alongside LHRH analogs that reduce hormone production.

The recommended dose of Casodex for use with an LHRH analog is one 50 mg tablet orally once daily, at the same time each day, with or without food. Treatment should begin simultaneously with the LHRH analog. If a dose is missed, take the next dose at the usual time; do not double doses or take missed doses late.

No dose adjustments are needed for patients with renal impairment or mild to moderate liver impairment. Patients with severe liver impairment showed increased drug half-life, but no dose adjustment is required.

• Hypersensitivity to bicalutamide or any component of the tablet.
• Women, as Casodex is not indicated for use in females.
• Pregnancy, due to potential fetal harm.

• Hepatotoxicity: Severe liver injury including fatal hepatic failure has occurred, typically within the first 3–4 months. Monitor liver enzymes before starting treatment, regularly during the first 4 months, and periodically thereafter. Stop Casodex immediately if jaundice or ALT rise above twice normal occurs.
• Bleeding Risk with Coumarin Anticoagulants: Casodex can increase prothrombin time (PT) and INR leading to serious bleeding events. Patients on coumarin anticoagulants require close monitoring and dose adjustment as needed.
• Gynecomastia and Breast Pain: Reported with 150 mg daily dosing, but the approved Casodex dose is 50 mg in combination therapy.
• Glucose Tolerance: LHRH analogs may reduce glucose tolerance, sometimes causing diabetes or worsening control in diabetic patients. Monitor blood glucose during combination therapy.
• Prostate Specific Antigen (PSA) Monitoring: Regular PSA testing is advised to evaluate treatment response. Rising PSA may indicate disease progression requiring clinical assessment.

Common adverse reactions (≥10%) reported with Casodex plus LHRH analog include hot flashes (53%), pain (general, back, pelvic, abdominal), asthenia, constipation, infection, nausea, peripheral edema, dyspnea, diarrhea, hematuria, nocturia, and anemia.

Other side effects reported in ≥5% of patients in clinical trials include hypertension, increased liver enzymes, dyspepsia, flatulence, anorexia, vomiting, anemia, hyperglycemia, peripheral edema, bone pain, dizziness, paresthesia, insomnia, anxiety, depression, rash, sweating, gynecomastia, breast pain, impotence, and urinary symptoms.

Postmarketing reports include rare but serious interstitial lung disease (including pneumonitis and pulmonary fibrosis) especially at doses exceeding 50 mg, photosensitivity reactions, and bleeding complications due to interactions with anticoagulants.

• Casodex may increase blood levels of CYP3A4 substrates, such as midazolam, potentially increasing their effects. Exercise caution when co-administering with CYP3A4 substrates.
• Casodex can displace coumarin anticoagulants from protein binding sites, increasing PT/INR and bleeding risk. Close monitoring and dose adjustment of anticoagulants are required.
• No interactions have been found between Casodex and LHRH analogs.

Pregnancy: Casodex is contraindicated during pregnancy as it can cause fetal harm. Animal studies demonstrated abnormal development of reproductive organs in male fetuses following maternal exposure.

Contraception: Male patients should use effective contraception during treatment and for 130 days after finishing Casodex therapy.

Lactation: It is unknown if bicalutamide is present in human milk. Animal studies detected it in rat milk. Breastfeeding is not recommended.