BI ELIGARD CP

What it is

BI ELIGARD CP is a composite pack containing bicalutamide and leuprorelin acetate. Bicalutamide is supplied as 50 mg white film-coated tablets. Leuprorelin ELIGARD is a sterile polymeric matrix formulation of leuprorelin acetate for subcutaneous injection, designed to deliver leuprorelin acetate at a controlled rate over a therapeutic period. Leuprorelin acetate is a synthetic nonapeptide analogue of naturally occurring gonadotropin releasing hormone that, when given continuously, inhibits pituitary gonadotropin secretion and suppresses testicular steroidogenesis. BI ELIGARD CP is available in 1 month and 3 month formulations. Bicalutamide is a non-steroidal anti-androgen that binds to androgen receptors without activating gene expression, thereby inhibiting the androgen stimulus and impairing the growth and encouraging apoptosis in androgen-dependent tumour cells and regression of prostatic tumours.

Approved indications

— Treatment of advanced prostate cancer in combination with LHRH agonist therapy (bicalutamide component). — Palliative treatment of advanced prostate cancer (leuprorelin component).

Dosing overview

Bicalutamide: one tablet (50 mg) once daily in adult males including the elderly, with treatment starting at the same time as LHRH agonist therapy. Leuprorelin: one injection every month for ELIGARD 1 month, or one injection every three months for ELIGARD 3 month.

Key safety warnings

In patients with metastatic prostate cancer, treatment with bicalutamide monotherapy has been associated with reduced survival compared to castration, and bicalutamide 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 a patient develops jaundice or if serum ALT rises above two times the upper limit of normal. Potentiation of coumarin anticoagulant effects have been reported in patients receiving concomitant bicalutamide therapy, which may result in increased PT and INR and some cases have been associated with risk of bleeding, and close monitoring of PT/INR is advised with anticoagulant dose adjustment considered. ELIGARD, like other LH-RH agonists, causes a transient increase in serum concentrations of testosterone during the first week of treatment, and patients may experience worsening of symptoms or onset of new signs and symptoms during the first few weeks, including bone pain, neuropathy, haematuria, or bladder outlet obstruction; isolated cases of ureteral obstruction and spinal cord compression have been observed. Hyperglycemia and an increased risk of developing diabetes have been reported in men receiving GnRH agonists, and blood glucose and glycosylated haemoglobin should be monitored periodically. Increased risk of developing myocardial infarction, sudden cardiac death and stroke has been reported in association with use of GnRH agonists in men, though the risk appears low, and patients should be monitored for symptoms and signs suggestive of cardiovascular disease. 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.

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. ELIGARD is contraindicated in patients with hypersensitivity to GnRH, GnRH agonist analogues or any of the components. ELIGARD is contraindicated in women who are breastfeeding, pregnant or intending to become pregnant and in paediatric patients. ELIGARD is contraindicated in patients who previously underwent orchiectomy. ELIGARD is contraindicated as a sole treatment in prostate cancer patients with spinal cord compression or evidence of spinal metastases.

Regulatory history

BI ELIGARD CP was first registered on the ARTG on 24 May 2016 for the 3-month formulation with 28 tablets, with the 1-month and additional 3-month formulations registered on 25 May 2016.