Non-Steroidal Anti-Androgen Pregnancy: Contraindicated in females and must not be given to pregnant women; contraindicated during breast-feeding (eMC §4.6). US labelling: can cause fetal harm; not indicated in females.

Bicalutamide

Brand names: Casodex

Bicalutamide is an oral non-steroidal anti-androgen used in prostate cancer, either with a GnRH analogue for advanced disease or as monotherapy in locally advanced disease. The overview context here is androgen-deprivation therapy for prostate cancer.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 150 mg (one film-coated tablet)

Route: Oral

Frequency: Once daily

eMC §4.2 (Bicalutamide 150 mg) — same SPC as the general bicalutamide entry; this is the urology-context listing. Adult males including older people. Take continuously for at least 2 years or until disease progression. Initiation should be under the direct supervision of a specialist. No dose adjustment for renal impairment or mild hepatic impairment; increased accumulation may occur in moderate to severe hepatic impairment (use with caution). Contraindicated in females and children. US labelling describes a different indication/dose: bicalutamide 50 mg once daily in combination with an LHRH analog for advanced prostate cancer — verify which UK indication/strength applies before use.

Dose adjustments

Renal

No dosage adjustment necessary for renal impairment (eMC §4.2).

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Females and children
Hypersensitivity to the active substance or any excipient
Co-administration of terfenadine, astemizole or cisapride

Side effects

Rash (very common); gynaecomastia and breast tenderness (very common); asthenia (very common)
Anaemia, hot flush, abdominal pain, constipation, nausea (common)
Hepatotoxicity, jaundice, hypertransaminasaemia (common); hepatic failure — fatal outcomes reported (rare)
Decreased libido, depression, dizziness, erectile dysfunction (common)
Interstitial lung disease — fatal outcomes reported (uncommon); QT prolongation (not known)

Interactions

Terfenadine, astemizole, cisapride — contraindicated
CYP3A4 substrates — bicalutamide inhibits CYP3A4; use with caution
Coumarin anticoagulants — potentiation of effect (increased PT/INR, bleeding risk); monitor PT/INR closely and consider dose adjustment
Drugs prolonging the QT interval — assess benefit-risk (androgen deprivation therapy may prolong QT)

Clinical monograph

How it works

It competitively blocks androgen receptors in prostatic tissue, preventing testosterone and dihydrotestosterone from stimulating tumour growth.

Prescribing in practice

Hepatotoxicity can occur, so liver function should be checked before and during treatment and the drug stopped if severe derangement develops.
When combined with a GnRH agonist for metastatic disease, start the anti-androgen first or concurrently to cover the initial testosterone 'flare'.
Gynaecomastia and breast tenderness are common, particularly with monotherapy, and prophylactic measures may be considered per the SPC.

Monitoring

Monitor liver function tests periodically and review PSA and clinical response to gauge disease control.

Counselling the patient

Report yellowing of the skin or eyes, dark urine, or unusual tiredness promptly.
Breast swelling or tenderness is a recognised effect that can be managed.
Take regularly at the same time each day as directed.

Evidence & guidelines

Established in prostate cancer through randomised trials supporting its use in combined androgen blockade and as monotherapy in locally advanced disease.

Reference: NICE NG131 (Prostate Cancer); MHRA Drug Safety Update (bicalutamide hepatotoxicity); EAU Guidelines 2024; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

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