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Bicalutamide

Non-steroidal antiandrogen · Antineoplastic

Also known as Casodex

START
50 mg PO once daily with LHRH analogue (start ≥3 days before/with LHRH for flare prevention)
TYPICAL MAX
50 mg/day (combined); 150 mg/day monotherapy where licensed
STOP IF
Significant hepatotoxicity (jaundice/ALT >2×ULN), ILD, severe QT
WATCH
LFTs at baseline, regularly first 4 months then periodically; QT if cardiac risk; testosterone/PSA response
CDSCO approvedJan AushadhiATC L02BB03
Dose laddermg/d
50start150ceiling
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment at any eGFR≥90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1dONSET1.3dPEAK5.8dt½1dDURATION
ONSET
1d · AR blockade onset
PEAK
1.3d · Cmax (~31 h)
t½
5.8d · plasma t½ (~5.8 days)
DURATION
1d · once-daily dosing
EXCRETION
Hepatic metabolism; renal + faecal metabolites
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Contraindicated — not for use in women; teratogenic
FDA category + note
Top interactionssee all 12 →
  • Aminolevulinic AcidSevereDatabaseDDInter
  • AmiodaroneSevereDatabaseDDInter
  • AmisulprideSevereDatabaseDDInter
  • AnagrelideSevereDatabaseDDInter
Available in India

27 branded formulations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Competitive androgen-receptor antagonist (peripheral) blocking testosterone/DHT action on prostate cancer cells; used with LHRH analogue (combined androgen blockade) or as monotherapy/flare prevention.

Indications

Metastatic prostate cancer (with LHRH analogue)Flare prevention when starting an LHRH agonistLocally advanced prostate cancer (monotherapy, region-dependent)

Dosing

Adult
50 mg PO once daily with LHRH analogue (combined blockade). 150 mg/day for monotherapy (locally advanced, where licensed).
Pediatric
Not indicated.
Renal adjustment
No adjustment.
Hepatic adjustment
Caution; avoid/closely monitor in moderate–severe impairment (hepatotoxicity, reduced clearance).
Geriatric
No specific adjustment.
Max dose
50 mg/day (combined blockade); 150 mg/day (monotherapy)

Pharmacokinetics

Onset
Testosterone-independent AR blockade within days
Peak effect
Steady state ~4–12 weeks (long t½)
Duration
Once daily
Half-life
~5.8 days (active R-enantiomer ~1 week)
Bioavailability
Well absorbed (food-independent)
Protein binding
>96%
Metabolism
Hepatic (oxidation/glucuronidation; CYP3A4 for inactive S-enantiomer; R-enantiomer glucuronidation)
Excretion
Renal and faecal (roughly equal; metabolites)

Contraindications

  • Women and children
  • Concomitant terfenadine/astemizole/cisapride (historical CYP3A4 — QT)
  • Severe hepatic impairment
  • Hypersensitivity to bicalutamide

Side effects

Common
Gynaecomastia and breast tendernessHot flushesAsthenia/fatigueDecreased libido/erectile dysfunction
Serious
  • Hepatotoxicity (incl. fulminant — monitor LFTs)
  • Interstitial lung disease (rare)
  • QT prolongation
  • Severe hypersensitivity (rare)

Pregnancy & lactation

Pregnancy

Contraindicated — not for use in women; teratogenic

Lactation

Not applicable (male indication)

Drug interactions

Aminolevulinic Acid
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Anagrelide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Arsenic Trioxide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Bedaquiline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Bepridil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cabozantinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cisapride
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Citalopram
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Clozapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Tobacco-related cancer prevention
ICMR · Oncology · 2021
Breast cancer
ESMO · Oncology · 2024
Cervical cancer screening and management
ICMR · Oncology · 2022
Breast cancer
ICMR · Oncology · 2022
Initial monotherapy for newly diagnosed epilepsy
ILAE · Neurology · 2013

Ask House about Bicalutamide

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19