bicalutamide: clinical use

Prescribing considerations

• Specialist initiation and supervision are required.
• Use caution in moderate or severe hepatic impairment because elimination may be slower.
• Assess QT-prolongation risk, interacting medicines and cardiovascular history.
• Consider effects on fertility and the need for effective contraception.
• The product contains lactose.

Contraindications and cautions

• Hypersensitivity to bicalutamide or an excipient
• Use in females
• Use in children or adolescents
• Concurrent terfenadine, astemizole or cisapride

Monitoring

• Periodic liver-function testing, particularly early in treatment; stop if hepatic changes are severe.
• PSA and objective disease progression.
• Blood glucose when combined with an LHRH agonist, especially with diabetes or impaired glucose control.
• PT/INR with warfarin or another coumarin anticoagulant.
• Clinical and ECG risk assessment where QT prolongation is relevant.
• Adverse effects including anaemia, cardiovascular symptoms and interstitial lung disease.

Clinical pharmacology

Bicalutamide is a racemic, non-steroidal androgen-receptor antagonist whose activity resides mainly in the R-enantiomer. It is well absorbed, highly protein-bound, extensively metabolised by oxidation and glucuronidation, and eliminated through urine and bile; the active enantiomer has a long elimination half-life.

Formulation and product differences

• The selected product is a white to off-white, circular, biconvex film-coated tablet marked “485” on one side.
• It contains lactose monohydrate and is essentially sodium-free.
• It is supplied in PVC/aluminium blister packs; not every authorised pack size may be marketed.

Tablet

Route: Oral

Strengths: 50 mg, 150 mg