- Metastatic castration-resistant prostate cancer (mCRPC)
- Non-metastatic castration-resistant prostate cancer (nmCRPC)
- Metastatic castration-sensitive prostate cancer (mCSPC)
Dose: OD 60 mg orally (4 × 40 mg capsules or 2 × 80 mg tablets),Can be taken with or without food,
Continue concurrent ADT or maintain surgical castration
- Capsules: 40 mg
- Tablets: 40 mg, 80 mg
- Take once daily at the same time
- Swallow whole, do not crush or chew
- Missed dose:
- If missed, take as soon as remembered unless more than 12 hours have passed—then skip and resume next dose
- Class: Androgen receptor inhibitor
- Mechanism of Action:
- Inhibits androgen receptor signaling by blocking:
- AR nuclear translocation
- DNA binding
- Coactivator recruitment
- ↓ Prostate cancer cell proliferation
- Inhibits androgen receptor signaling by blocking:
- Pharmacokinetics:
- Metabolized by: CYP2C8 and CYP3A4
- Half-life: ~5.8 days
- Highly protein-bound, hepatically cleared
- Fatigue
- Hot flashes
- Hypertension
- Back pain
- Diarrhea or constipation
- Arthralgia
- Headache
- Pregnancy (in female partners; not used in women)
- Hypersensitivity to enzalutamide or its components
- Caution in patients with a history of seizures, brain metastases, or stroke
- Strong CYP2C8 inhibitors (e.g., gemfibrozil):
- ↓ enzalutamide dose to 80 mg daily
- Strong CYP3A4 inducers (e.g., rifampin):
- May ↓ enzalutamide efficacy
- Enzalutamide induces CYP3A4, 2C9, and 2C19 → may ↓ effectiveness of:
- Warfarin
- Midazolam
- Clopidogrel
- Antiepileptics
- Avoid concurrent use with medications lowering seizure threshold
Drug Status
Availability | |
Pregnancy | |
Breastfeeding | |
Schedule |
BRAND NAME | STRENGTH | FORMULATION | PACK SIZE | MANUFACTURER | DISTRIBUTOR |
---|---|---|---|---|---|
Xtandi | 40mg | Capsule | 112’s | Astellas Pharma | Harley’s Ltd |