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leuprorelin and bicalutamide

L02AE51

Forms & Strengths

Combination pack: Leuprorelin acetate depot injection (various strengths, e.g., 3.75 mg, 11.25 mg, 22.5 mg, 30 mg) + Bicalutamide tablets (50 mg)

Adult Dosing

Prostate cancer: Bicalutamide 50 mg orally once daily combined with a GnRH agonist (leuprorelin) administered according to depot schedule (e.g., monthly, every 3 months, or every 4 months)

Pediatric Dosing

Not indicated for use in pediatric patients

Indications

Palliative treatment of advanced prostate cancer

Mechanism of Action

Leuprorelin: GnRH agonist that, after initial stimulation, desensitizes pituitary GnRH receptors, leading to suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby reducing testosterone production to castration levels
Bicalutamide: Non-steroidal competitive androgen receptor antagonist that blocks peripheral androgen action in target tissues

Contraindications

Hypersensitivity to leuprorelin, bicalutamide, or any component of the formulations
Women who are or may become pregnant
Severe hepatic impairment (for bicalutamide component)

Adverse Reactions

Hot flashes and flushing
Decreased libido and erectile dysfunction
Gynecomastia and breast tenderness
Fatigue, asthenia, and pain
Elevated transaminases and hepatotoxicity
Decreased bone mineral density and increased fracture risk
Hyperglycemia and increased risk of diabetes
QT prolongation

Drug Interactions

CYP3A4 inducers (e.g., rifampin, carbamazepine) may decrease bicalutamide efficacy
CYP3A4 inhibitors (e.g., ketoconazole) may increase bicalutamide exposure
QT-prolonging drugs: Concomitant use with leuprorelin may increase risk of arrhythmias
Antidiabetic agents: Androgen deprivation may alter glycemic control, requiring adjustment of antidiabetic drugs

Curated Content: Needs Vetting Before Put to Clinical Use