Last reviewed 2026-04-20 · How we verify

Xtandi (xtandi)

Enzalutamide competitively inhibits androgen binding to androgen receptors, blocking nuclear translocation and DNA interaction.

Xtandi (enzalutamide) is an androgen receptor inhibitor indicated for castration-resistant prostate cancer, metastatic castration-sensitive prostate cancer, and non-metastatic castration-sensitive prostate cancer with high-risk biochemical recurrence. It demonstrates strong protein binding (97-98%) and a half-life of 5.8 days, achieving steady-state by Day 28 with 8.3-fold AUC accumulation. Key risks include significant drug interactions with CYP2C8 inhibitors and CYP3A4 inducers requiring dosage adjustments. The drug shows dose-proportional pharmacokinetics and no clinically meaningful food effects, supporting its clinical utility in prostate cancer management.

At a glance

Mechanism of action

Enzalutamide is an androgen receptor inhibitor that acts on multiple steps in the androgen receptor signaling pathway. It competitively inhibits androgen binding to androgen receptors and consequently inhibits nuclear translocation of androgen receptors and their interaction with DNA. A major metabolite, N-desmethyl enzalutamide, exhibits similar in vitro activity to enzalutamide. In preclinical studies, enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro and decreased tumor volume in a mouse prostate cancer xenograft model.

Approved indications

• Malignant tumor of prostate
• Metastasis from malignant tumor of prostate

Common side effects

• Fatigue
• Back pain
• Nausea
• Arthralgia
• Hot flush
• Constipation
• Decreased appetite
• Diarrhoea
• Hypertension
• Asthenia
• Fall
• Headache

Drug interactions

• Strong CYP2C8 inhibitors (e.g., gemfibrozil)
• Strong CYP3A4 inducers (e.g., rifampin)
• CYP3A4, CYP2C9, or CYP2C19 substrates

Patents

Primary sources

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