Oops, looks like you need to register to access this feature.
Select “Keep Exploring” to look around Scholars in Medicine. You have full access to all videos and podcasts for a limited time. Registration is provided at no cost exclusively for healthcare providers.
Sign Up or Log In

Bicalutamide

Brand and Other Names: Bicalutamide
Mechanism of Action:

Bicalutamide is a non-steroidal androgen receptor inhibitor. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen.

Indications:

Bicalutamide 50 mg is approved only in combination with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D metastatic prostate cancer.

Route: oral
Dose:

50 mg orally once daily, with or without food, at the same time each day.

Adverse Reactions:

Hot flashes (53%)

Pain (general/back/pelvic/abdominal)

Asthenia (22%)

Constipation, nausea, edema

Dyspnea, anemia, nocturia, hematuria

Contraindication:

Bicalutamide is contraindicated in:

  • Hypersensitivity

Bicalutamide is contraindicated in any patient who has shown a hypersensitivity reaction to the drug or any of the tablet’s components. Hypersensitivity reactions including angioneurotic edema and urticaria have been reported.

  • Women

Bicalutamide has no indication for women, and should not be used in this population.

  • Pregnancy

Bicalutamide can cause fetal harm when administered to a pregnant woman

Warnings and Precautions:

Hepatotoxicity:
Potentially fatal liver injury; monitor liver enzymes before and during treatment. Discontinue if ALT >2× ULN or jaundice occurs.

Bleeding Risk:
Serious bleeding events may occur when used with coumarin anticoagulants. Monitor INR/PT closely.

Gynecomastia and Breast Pain:
Seen especially with 150 mg dose (not approved), but possible at any level.

Glucose Tolerance Impairment:
Increased risk of diabetes or poor glycemic control when used with LHRH agonists.

Photosensitivity:
Cases reported. Patients should avoid UV/sunlight exposure and consider sunscreen use.

See package insert for full prescribing information.