Generic
Bicalutamide
4 brands available in the market
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.
Description
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.
Bicalutamide is used in combination with LHRH analogs for the treatment of Stage D2 metastatic carcinoma of the prostate. It may also be used as monotherapy or as adjuvant therapy to surgery or radiotherapy in locally advanced prostate cancer.
Indications
- Stage D2 metastatic carcinoma of the prostate (in combination with LHRH analog)
- Locally advanced prostate cancer (monotherapy or adjuvant to surgery/radiotherapy)
Therapeutic class
Hormonal Chemotherapy
Pharmacological class
Non-steroidal Antiandrogen
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.
Mechanism of action
Bicalutamide competitively binds to androgen receptors, thereby blocking the action of androgens of adrenal and testicular origin. This prevents the growth of normal and malignant prostatic tissue.
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.
Administration
Take this medicine in the dose and duration as advised by your doctor. Swallow the tablet whole. Do not chew, crush or break it. May be taken with or without food, preferably at a fixed time every day.
Missed dose
If you miss a dose, take it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
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.
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.
Contraindications
- Hypersensitivity to bicalutamide or any tablet component
- Use in females (contraindicated in pregnancy and lactation)
- Use in children
Drug interactions
- R-bicalutamide is an inhibitor of CYP 3A4; caution when co-administered with CYP 3A4 substrates.
- Enhances the effect of coumarin anticoagulants (e.g., warfarin); closely monitor PT/INR and adjust anticoagulant dose as needed.
Food interactions
It is not known whether it is safe to consume alcohol with Bicalutamide. Please consult your doctor.
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.
Use in lactation
Information regarding the use of Bicalutamide during breastfeeding is not available. Bicalutamide is not indicated for use in females. Please consult your doctor.
Pediatric use
Safety and effectiveness in pediatric patients have not been established.
Geriatric use
No specific dose adjustment required for elderly patients, but liver and renal function should be monitored.
Renal / hepatic impairment
Hepatic impairment: Bicalutamide is extensively metabolized by the liver. Use with caution in moderate-to-severe hepatic impairment. Periodic liver function tests should be considered during long-term therapy.
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.
Chemical structure
Bicalutamide