Contents

Bicalutamide

Indication

Advanced prostate cancer in combination w/ luteinizing hormone-releasing hormone (LHRH) analogue therapy or surgical castration. Monotherapy or as adjuvant to radical prostatectomy or radiotherapy in patients w/ locally advanced prostate cancer at high risk for disease progression.

Dosage / Direction For Use

Adult including elderly 50 mg once daily either 3 days before or at the same time w/ LHRH analogue or surgical castration. Monotherapy 150 mg once daily taken continuously for at least 2 yr or until progression.

Overdosage

There is no human experience of overdose. There is no specific antidote; treatment should be symptomatic. Dialysis may not be helpful, since bicalutamide is highly protein bound and is not recovered unchanged in the urine. General supportive care, including frequent monitoring of vital signs, is indicated.

Administration

Should be taken with food.

Contraindication

Hypersensitivity. Terfenadine, astemizole or cisapride. Females. Childn.

Special Precaution

May prolong the QT interval. Reduced glucose tolerance. Somnolence may occur. Co-administration w/ CVYP3A4, coumarin anticoagulants. Patients w/ moderate to severe hepatic impairment

Adverse Reactions

–

Drug Interaction

Closely monitor w/ ciclosporin. Other medicinal products inhibiting drug oxidation eg, cimetidine & ketoconazole. Increased effect of warfarin & other coumarin anticoagulants. May induce torsade de pointes eg, class IA (quinidine, disopyramide) or class III (amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic products, methadone, moxifloxacin, antipsychotics.

Storage

Store at temperatures not exceeding 25°C.

Description

Each film-coated tablet contains: Bicalutamide 50 mg.

Action

Pharmacotherapeutic group: Endocrine therapy, hormone antagonists and related agents, anti-androgens.Pharmacology: Pharmacodynamics: Mechanism of action: Bicalutamide is a non-steroidal antiandrogen, devoid of other endocrine activity. It binds to androgen receptors without activating gene expression, and thus inhibits the androgen stimulus. Regression of prostatic tumours results from this inhibition. Clinically, discontinuation of bicalutamide can result in antiandrogen withdrawal syndrome in a subset of patients.Bicalutamide is a racemate with its antiandrogenic activity being almost exclusively in the (R)-enantiomer.Clinical efficacy and safety: Bicalutamide 150 mg was studied as a treatment for patients with localised (T1-T2, N0 or NX, M0) or locally advanced (T3-T4, any N, M0; T1-T2, N+, M0) non metastatic prostate cancer in a combined analysis of three placebo controlled, double-blind studies in 8,113 patients, where bicalutamide 150 mg was given as immediate hormonal therapy or as adjuvant to radical prostatectomy or radiotherapy, (primarily external beam radiation). At 7.4 years median follow up, 27.4% and 30.7% of all bicalutamide and placebo treated patients, respectively, had experienced objective disease progression.A reduction in risk of objective disease progression was seen across most patient groups but was most evident in those at highest risk of disease progression. Therefore, clinicians may decide that the optimum medical strategy for a patient at low risk of disease progression, particularly in the adjuvant setting following radical prostatectomy, may be to defer hormonal therapy until signs that the disease is progressing.No overall survival difference was seen at 7.4 years median follow up with 22.9% mortality (HR=0.99; 95% CI 0.91 to 1.09). However, some trends were apparent in exploratory subgroup analyses.Progression-free survival and overall survival data for patients with locally advanced disease are summarised in the following tables: See Table 1 and Table 2.