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At a glance

Bicalutamide is a non-steroidal androgen receptor inhibitor used in the treatment of prostate cancer. It blocks the effects of male hormones such as testosterone, preventing the growth of prostate cancer cells.

Indications
  • Stage D2 metastatic carcinoma of the prostate (in combination with LHRH analog)
  • Locally advanced prostate cancer (monotherapy or adjuvant to surgery/radiotherapy)
Pharmacology

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.

Dosage

Adults:

In combination with LHRH analog (Stage D2 metastatic prostate cancer): 50 mg once daily (morning or evening), with or without food. May be started with or at least 3 days before starting LHRH analog therapy.

Monotherapy or adjuvant therapy in locally advanced prostate cancer: 150 mg once daily.

Hepatic impairment: Use with caution in moderate-to-severe hepatic impairment.

Children: Safety and effectiveness in pediatric patients have not been established.

Side effects

Common (>10% of patients):
Hot flashes, pain (including general, back, pelvic and abdominal), asthenia (weakness), constipation, infection, nausea, peripheral edema, dyspnea, diarrhea, hematuria (blood in urine), nocturia (frequent urination at night), anemia.

Other:
Rash, abdominal pain, gynecomastia (breast enlargement in males), breast tenderness, decreased appetite, decreased libido, depression, dizziness, indigestion, flatulence, sleepiness, weight gain, increased liver enzymes.

Use in pregnancy

Highly unsafe during pregnancy (FDA Category X). Animal and human studies have shown significant harmful effects to the developing baby. Contraindicated in pregnant women. Effective contraception by both males and females is important during treatment.

Pregnancy Category: X — always consult a doctor before taking during pregnancy.

Precautions & warnings
  • Risk of hemorrhage with concomitant coumarin anticoagulant use; closely monitor PT and INR.
  • Gynecomastia and breast pain may occur (especially with 150 mg monotherapy).
  • May cause reduction in glucose tolerance; diabetic patients should monitor blood glucose regularly.
  • Skin may become light-sensitive; avoid excessive sun exposure and use sunscreen.
  • Monitor PSA regularly; evaluate for clinical progression if PSA increases.
  • Periodic liver function tests should be considered, especially in hepatic-impaired patients on long-term therapy.
  • Does not usually affect ability to drive.
Overdose effects

Long-term clinical trials have been conducted with dosages up to 200 mg daily and these dosages have been well tolerated. A life-threatening overdose symptom dose has not been established. There is no specific antidote; treatment should be symptomatic.

Storage conditions

Store at temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.

Bicalutamide — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.