BICALOX

What it is

BICALOX is a non-steroidal anti-androgen, devoid of other endocrine activity. It is supplied as white film-coated tablets containing 50 mg bicalutamide. It binds to androgen receptors without activating gene expression, and thus inhibits the androgen stimulus, which impairs the growth and encourages apoptosis in androgen-dependent tumour cells and regression of prostatic tumours.

Approved indications

— Treatment of advanced prostate cancer in combination with LHRH agonist therapy.

Dosing overview

The recommended dose for adult males, including the elderly, is one tablet (50 mg) once a day, and treatment should be started at the same time as treatment with a LHRH agonist.

Key safety warnings

In patients with metastatic prostate cancer, treatment with bicalutamide monotherapy has been associated with reduced survival compared to castration, and should therefore not be used without concomitant LHRH agonist therapy in these patients. Rare cases of death or hospitalisation due to severe liver injury have been observed with bicalutamide, and therapy should be discontinued if at any time a patient develops jaundice or if serum ALT rises above two times the upper limit of normal. A reduction in glucose tolerance has been observed in males receiving LHRH agonists, which may manifest as diabetes or loss of glycaemic control in those with pre-existing diabetes, and consideration should therefore be given to monitoring blood glucose in patients receiving bicalutamide in combination with LHRH agonists. Potentiation of coumarin anticoagulant effects have been reported in patients receiving concomitant bicalutamide therapy, which may result in increased Prothrombin Time and International Normalised Ratio, with some cases associated with risk of bleeding, and close monitoring of PT/INR is advised with anticoagulant dose adjustment to be considered. Androgen deprivation therapy may prolong QT/QTc interval, and prescribers should consider whether the benefits outweigh the potential risks in patients with congenital long QT syndrome, congestive heart failure, frequent electrolyte abnormalities and in patients taking drugs known to prolong the QT interval, with electrolyte imbalances to be corrected and periodic monitoring of electrocardiograms and electrolytes considered.

Contraindications

Bicalutamide is contraindicated in females and children, and in patients with known hypersensitivity to bicalutamide or any other constituents of the formulation. Co-administration of terfenadine, astemizole or cisapride with bicalutamide is contraindicated.

Regulatory history

BICALOX bicalutamide 50 mg film-coated tablets were first registered on the ARTG on 24 May 2007, with two presentations listed in bottle and blister pack formats under licence category RE.