Bicalutamide (Casodex) - Uses, Dose, Side effects

Bicalutamide (Casodex) is an anti-androgen drug that inhibits the binding of testosterone and dihydrotestosterone to its receptors. It is used to treat the following conditions:

    • Treatment of stage D metastatic prostate cancer in combination with an LHRH ( Luteinizing hormone-releasing hormone) agonist.

    • Treatment of locally advanced prostatic cancer as monotherapy (Off Label Use).

Adult dose:

Bicalutamide (casodex) in the treatment of metastatic Prostate cancer:

    • 50 mg orally once a day in combination with an LHRH analog.

Off-label use in the treatment of locally advanced Prostate cancer including those at a high risk of recurrence.

    • 150 mg orally once a day as monotherapy.
    • If a dose is missed, take the next dose at the next scheduled time. Do not double the next dose.

Use in Children:

Not applicable

Pregnancy Risk Factor X

    • It is not recommended for women.
    • Anti-androgens can adversely impact fetal development.
    • It can also impact male fertility.
    • Effective contraception should be used by males and female partners of reproductive age to prevent pregnancy.

Use during breastfeeding:

    • It is contraindicated for women, and especially during breastfeeding.

Bicalutamide dose in Renal Disease:

Adjustment in the dose is not necessary.

Bicalutamide dose in Liver Disease:

  • Hepatic impairment at baseline:

    • Adjustment in the dose is not necessary.
    • Patients with moderate to severe hepatic impairment should use the drug with caution.
  • Hepatic impairment during treatment:

    • Discontinue immediately if the ALT is more than twice the upper limits of normal or the patients develops jaundice.

Side effects:

Adverse reaction percentages reported as part of a combination regimen with an LHRH analog unless otherwise noted.

Common Side Effects of Bicalutamide (Casodex):

  • Cardiovascular:

    • Peripheral Edema
  • Central Nervous System:

    • Pain
  • Endocrine & Metabolic:

    • Hot Flash
    • Gynecomastia
  • Gastrointestinal:

    • Constipation
    • Nausea
    • Diarrhea
    • Abdominal Pain
  • Genitourinary:

    • Mastalgia
    • Pelvic Pain
    • Hematuria
    • Nocturia
  • Hematologic & Oncologic:

    • Anemia
  • Infection:

    • Infection
  • Neuromuscular & Skeletal:

    • Back Pain
    • Weakness
  • Respiratory:

    • Dyspnea

Less Common Side Effects of Bicalutamide:

  • Cardiovascular:

    • Chest Pain
    • Hypertension
    • Angina Pectoris
    • Cardiac Arrest
    • Cardiac Failure
    • Coronary Artery Disease
    • Edema
    • Myocardial Infarction
    • Syncope
  • Central Nervous System:

    • Dizziness
    • Paresthesia
    • Headache
    • Insomnia
    • Myasthenia
    • Anxiety
    • Chills
    • Confusion
    • Drowsiness
    • Hypertonia
    • Nervousness
    • Neuropathy
    • Depression
  • Dermatologic:

    • Skin Rash
    • Diaphoresis
    • Alopecia
    • Pruritus
    • Xeroderma
  • Endocrine & Metabolic:

    • Weight Loss
    • Hyperglycemia
    • Weight Gain
    • Decreased Libido
    • Dehydration
    • Gout
    • Hypercholesterolemia
  • Gastrointestinal:

    • Dyspepsia
    • Anorexia
    • Flatulence
    • Vomiting
    • Dysphagia
    • Hernia
    • Melena
    • Periodontal Abscess
    • Xerostomia
  • Genitourinary:

    • Urinary Tract Infection
    • Impotence
    • Difficulty In Micturition
    • Urinary Retention
    • Dysuria
    • Urinary Urgency
    • Urinary Incontinence
  • Hematologic & Oncologic:

    • Gastrointestinal Carcinoma
    • Rectal Hemorrhage
    • Skin Carcinoma
  • Hepatic:

    • Increased Liver Enzymes
    • Increased Serum Alkaline Phosphatase
  • Infection:

    • Herpes Zoster
    • Sepsis
  • Neuromuscular & Skeletal:

    • Ostealgia
    • Arthritis
    • Leg Cramps
    • Myalgia
    • Neck Pain
    • Pathological Fracture
  • Ophthalmic:

    • Cataract
  • Renal:

    • Polyuria
    • Hydronephrosis
    • Increased Blood Urea Nitrogen
    • Increased Serum Creatinine
  • Respiratory:

    • Cough
    • Pharyngitis
    • Flu-Like Symptoms
    • Bronchitis
    • Asthma
    • Epistaxis
    • Sinusitis
    • Pneumonia
    • Rhinitis
  • Miscellaneous:

    • Cyst
    • Fever

Contraindications to Bicalutamide:

      • Allergic reactions to bicalutamide and any component of this formulation
      • Use in women
      • Pregnancy
      • Children

Warnings and Precautions

o    Gynecomastia

      • Higher doses can cause breast pain and gynecomastia.

o    Hematologic:

      • It is important to monitor CBC regularly as anemia could result from testosterone suppression.

o    Hepatotoxicity:

      • Hepatotoxicity can occur in the first three to four months of therapy. It may lead to serious complications that could require discontinuation of therapy.
      • Patients with moderately severe or mild liver disease should be cautious when taking the drug.
      • It is important to monitor the patient for signs and symptoms of hepatotoxicity.
      • It is important to monitor the liver functions regularly and stop treatment if ALT exceeds twice the normal limit.

o    Hypersensitivity

      • Rarely, urticaria or Angioneurotic edema can occur.

o    Interstitial lung disease:

      • It is important to monitor patients for any worsening respiratory symptoms such as cough, fever, or shortness of breath. Interstitial lung disease has been reported in some cases.

o    Cardiovascular disease

      • Monitor ECG, Echocardiogram, electrolytes, and ECG periodically as androgen deprivation therapy can increase cardiovascular disease risk.

o    Reduced bone mineral density

      • It can lead to osteopenia or osteoporosis and increase the risk of bone fractures.

o    Diabetes:

      • Patients with diabetes may experience a decrease in glucose tolerance or loss of glycemic control.

Bicalutamide: Drug Interaction

Risk Factor C (Monitor therapy)

Aminolevulinic Acid (Topical)

Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical).


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.

Choline C 11

Antiandrogens may diminish the therapeutic effect of Choline C 11.


CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.


CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin.


CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine.


Photosensitizing Agents may enhance the photosensitizing effect of Porfimer.


Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin.

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 Factor D (Consider therapy modification)


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 Factor X (Avoid combination)

Aminolevulinic Acid (Systemic)

Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic).


Bicalutamide may increase the serum concentration of Astemizole.


Bicalutamide may increase the serum concentration of Cisapride.

Indium 111 Capromab Pendetide

Antiandrogens may diminish the diagnostic effect of Indium 111 Capromab Pendetide.


CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.


Bicalutamide may increase the serum concentration of Terfenadine.

Periodically Monitor:

  • CBC
  • ECG
  • echocardiogram
  • Serum testosterone
  • luteinizing hormone
  • prostate-specific antigen (PSA)
  • Liver function tests (at basleine and regularly in the first four months)
  • Blood glucose in patients with diabetes.
  • Monitor INR in patients on warfarin.

How to take Bicalutamide (Casodex)?

It is taken orally at the same time each day (either in the morning or in the evening). It may be administered with or without food.

It should be started concomitantly with an LHRH ( Luteinizing hormone-releasing hormone) analog for the treatment of metastasis.

Mechanism of action of Bicalutamide (Casodex):

  • It prevents the growth of prostate cancerous cells with testosterone by competitively inhibiting testosterone and dihydrotestosterone binding to the androgen receptors.

It works wellabsorbedIt is 96%Proteins boundIt is. It isMetabolizedThe liver is subject to oxidation and/or glucuronidation, which can lead to the formation of inactive metabolites.

It has been a half-life eliminationapproximately 6 days, and the time it takes to reachpeak plasma concentrationIt takes approximately 31 hours. It takes approximately 31 hours.excretedIn the urine and feces. 

International brand names of Bicalutamide:

  • ACH-Bicalutamide
  • ACT Bicalutamide
  • APO-Bicalutamide
  • Casodex
  • DOM-Bicalutamide
  • JAMP-Bicalutamide
  • MYLAN-Bicalutamide
  • PHL-Bicalutamide
  • PMS-Bicalutamide
  • PRO-Bicalutamide-50
  • RAN-Bicalutamide
  • SANDOZ Bicalutamide
  • TEVA-Bicalutamide
  • VAN-Bicalutamide
  • Androdex
  • Areclok
  • Bicadex
  • Bical
  • Bicalan
  • Bicalox
  • Bicalude
  • Bicapros
  • Bicatero
  • Bicatero 50
  • Bicloc
  • Bidrostat
  • Bikalen
  • Biprosta
  • Bosconar
  • Bypro
  • Calumid
  • Calutex
  • Calutide
  • Calutide-50
  • Calutol
  • Cosamide
  • Diproca
  • Gepeprostin
  • Lutam
  • Lutamidal
  • Procalut
  • Talum
  • Tosadex
  • Vicalud
  • Yonistib
  • Zolacos CP

Bicalutamide Brand Names in Pakistan:

Bicalutamide Tablets 50 mg

Calutide A. J. Mirza Pharma (Pvt) Ltd
Casodex ICI Pakistan Ltd.



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