Enzalutamide
XTANDI
What it isAndrogen receptor antagonist blocking binding, nuclear translocation and DNA interaction; prostate cancer.
Why this oneTriple blockade of the receptor pathway gives survival benefit where first-generation antiandrogens fail.
What limits itSeizure risk, fatigue and falls. A strong CYP3A4 inducer, so co-prescribed drugs fail.
FDA-approved for
- prostate cancer (2012)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Prostate cancer (CRPC, mCSPC, or nmCSPC with high-risk BCR) | adult male | 160 mg PO QD | 160 mg PO QD | 160 mg PO QD |
Renal No adjustment for mild–moderate (CrCl >=30 mL/min); not studied in severe impairment/ESRD.
Hepatic No adjustment needed
Instructions
- Swallow capsules/tablets whole with water; do not chew, dissolve, or open capsules, or cut/crush/chew tablets
- With or without food
- CRPC/mCSPC: also give a GnRH analog concurrently or have prior bilateral orchiectomy
- For >=Grade 3 or intolerable toxicity, withhold ~1 week until <=Grade 2, then resume at same or reduced dose (120 mg or 80 mg)
Cautions
- Seizure (permanently discontinue if it occurs)
- Posterior reversible encephalopathy syndrome (PRES)
- Hypersensitivity
- Ischemic heart disease
- Falls and fractures
- Embryo-fetal toxicity / loss of pregnancy — male contraception advised
- Severe dysphagia/choking related to tablet size
Adverse reactions
- Musculoskeletal pain
- Fatigue
- Hot flush
- Constipation
- Decreased appetite
- Diarrhea
- Hypertension
- Hemorrhage
- Falls
- Fracture
- Headache
Pregnancy Can cause fetal harm and loss of pregnancy (not indicated in females); based on animal data and mechanism of action.
Lactation Not indicated in females; no human data.
NO BOXED WARNINGS
Principal riskSeizure risk; a strong CYP3A4 inducer
Cost, est. cash$500–$15,000/month
Generic entry2027 est.
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: Enzalutamide ballicule
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