Targeted Therapy / Oncology — Prostate Cancer

Xtandi (enzalutamide)

Astellas / Pfizer · Androgen Receptor Inhibitor

FDA Approved 2012 Oral capsule or tablet Specialty Medication
Xtandi enzalutamide capsules, Astellas Pfizer, androgen receptor inhibitor prostate cancer

What is Xtandi? Xtandi (enzalutamide) is an androgen receptor inhibitor by Astellas/Pfizer approved for castration-resistant prostate cancer (CRPC) and metastatic castration-sensitive prostate cancer (mCSPC), used with or without androgen deprivation therapy.

About Xtandi

Brand NameXtandi
Generic / INNenzalutamide
Drug ClassAndrogen Receptor Inhibitor
ManufacturerAstellas / Pfizer
AdministrationOral capsule or tablet
FDA Approval2012
📦 Available as 40 mg soft gelatin capsules and 40 mg tablets. Standard dose: 160 mg (4 × 40 mg) once daily.

FDA-Approved Uses for Xtandi

Indications are based on FDA approval. Your healthcare provider determines appropriate use based on your specific diagnosis, stage, biomarker status, and overall clinical picture.

  • Metastatic castration-resistant prostate cancer (mCRPC)
  • Non-metastatic castration-resistant prostate cancer (nmCRPC)
  • Metastatic castration-sensitive prostate cancer (mCSPC) — with androgen deprivation therapy
Biomarker Note: No required biomarker. AR splice variant testing (AR-V7) may inform treatment sequencing in later-line mCRPC settings. BRCA status increasingly relevant for combination approaches.

How Does Xtandi Work?

Enzalutamide competitively inhibits the androgen receptor (AR) — blocking testosterone and DHT binding, inhibiting AR nuclear translocation, and preventing AR-DNA binding and gene transcription. Unlike first-generation antiandrogens (bicalutamide), enzalutamide has no agonist activity and effectively blocks AR signaling even in cells overexpressing AR.

Dosage & Administration

160 mg (four 40 mg capsules) orally once daily, with or without food. Dose reductions for toxicity. Avoid strong CYP3A4/CYP2C8 inhibitors and strong inducers (significantly alters enzalutamide exposure).

⚠️ Important

Dosing is individualized by the prescribing clinician. Never adjust your dose without consulting your healthcare provider. This information is educational only and does not replace the official prescribing information.

Warnings, Precautions & Side Effects

General Warning

Seizures — contraindicated in patients with seizure disorder or risk factors without careful consideration. Posterior reversible encephalopathy syndrome (PRES). Ischemic heart disease. Falls and fractures. Hypertension. Embryo-fetal toxicity.

⛔ Serious Warnings & Precautions
  • Seizures
  • PRES
  • Ischemic cardiovascular events
  • Falls and fractures
  • Embryo-fetal toxicity

Common Side Effects

  • Fatigue
  • Hot flush
  • Hypertension
  • Headache
  • Falls
  • Arthralgia
  • Nausea
  • Diarrhea
  • Weight loss
  • Cognitive effects

This is not a complete list. Always report new or worsening symptoms to your healthcare provider promptly.

Storage & Handling

Store at room temperature 25°C (77°F). Keep in original container.

BiologicHealthPlus provides temperature-monitored cold-chain specialty delivery for medications requiring refrigeration. Never use a medication if its storage conditions have been compromised.

Insurance Coverage, Prior Authorization & Patient Assistance

🛡️ Commercial Insurance

Xtandi is covered by most major commercial insurance plans when medically necessary and prior authorized. Coverage tier and cost-sharing vary by plan.

✅ Prior Authorization

Prior authorization is required by virtually all insurance plans for Xtandi. BiologicHealthPlus handles the complete prior authorization process at no cost to patients or providers.

🏥 Medicare Coverage

Medicare Part D covers this oral specialty medication. Medicaid coverage varies by state.

🆓 Patient Assistance

Manufacturer patient assistance programs may be available for eligible uninsured or underinsured patients. Contact BiologicHealthPlus for a confidential eligibility review.

Prior Authorization Patient Assistance Insurance & Savings Medication Costs

Frequently Asked Questions — Xtandi

Xtandi is a second-generation androgen receptor inhibitor approved for castration-resistant and castration-sensitive prostate cancer. Unlike older antiandrogens, it has no agonist activity and blocks multiple steps of AR signaling.

Both are AR inhibitors approved for similar prostate cancer settings. Key differences include chemical structure, CNS penetration, seizure risk, and drug interaction profiles. Clinical selection depends on individual patient factors and prior therapy.

Seizures have been reported with enzalutamide. Use with extreme caution in patients with a history of seizure, brain injury, or conditions predisposing to seizure.

Xtandi is covered by commercial insurance and Medicare Part D with prior authorization for approved prostate cancer indications.

Related Medications

Erleada (apalutamide)  ·  Nubeqa (darolutamide)  ·  Abiraterone Acetate  ·  Akeega (niraparib + abiraterone)

Related Conditions

Metastatic castration-resistant prostate cancer (mCRPC)  ·  Non-metastatic CRPC (nmCRPC)  ·  Castration-sensitive prostate cancer (mCSPC)

Comparisons

Erleada Abiraterone Acetate

Authoritative References

Medical Disclaimer: This page is for general educational purposes only and does not constitute medical advice, diagnosis, or treatment. Always consult your oncologist, hematologist, or licensed healthcare professional before making any treatment decisions. Last reviewed: August 2026 by the BiologicHealthPlus Clinical Team.