Bicalutamide
CASODEX
What it isNonsteroidal androgen-receptor antagonist; prostate cancer.
Why this oneIts main clinical niche is suppressing the testosterone flare when a GnRH agonist is initiated.
What limits itGynecomastia and breast tenderness are characteristic; hepatotoxicity requires liver monitoring.
FDA-approved for
- prostate cancer (1995)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Advanced prostate cancer (with LHRH analog) | Adult males | 50 mg QD | 50 mg QD | 50 mg QD |
Renal No adjustment needed
Hepatic No adjustment needed (incl. severe impairment, despite ~76% increase in half-life)
Instructions
- Take once daily (morning or evening) at same time each day, with or without food
- Start at same time as the LHRH analog
- If a dose is missed, take next dose at scheduled time; do not double
Contraindications
- Women (no indication) and pregnancy — can cause fetal harm
Cautions
- Severe hepatic injury / fatal hepatic failure — monitor transaminases at baseline, regularly for first 4 months, then periodically
- Hemorrhage with concomitant coumarin anticoagulants — monitor PT/INR
- Gynecomastia and breast pain
- Reduced glucose tolerance with LHRH agonists — monitor blood glucose
- Monitor PSA
Adverse reactions
- Hot flashes
- Pain (general, back, pelvic, abdominal)
- Asthenia
- Constipation, nausea, diarrhea
- Infection, peripheral edema
- Dyspnea, hematuria, nocturia, anemia
Pregnancy Contraindicated — can cause fetal harm; not indicated in females
Lactation Not indicated in females; no human milk data (detected in rat milk)
NO BOXED WARNINGS
Principal riskGynecomastia; hepatotoxicity needing liver monitoring
Cost, est. cash$10–$1,000/month
Generic entry2009
Classes and tags
Clinical profile
Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent
Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.
Mechanism of action: Bicalutamide ballicule
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