Enzalutamide

What it is and how it works

Mechanism of Action Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor signaling pathway. Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors; and consequently, inhibits nuclear translocation of androgen receptors and their interaction with DNA. A major metabolite, N‑desmethyl enzalutamide, exhibited similar in vitro activity to enzalutamide. Enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro , and decreased tumor volume in a mouse prostate cancer xenograft model.

Mechanism class: Androgen Receptor Antagonists · Cytochrome P450 3A4 Inducers · Cytochrome P450 2C9 Inducers

Indications

® is indicated for the treatment of patients with: • castration-resistant prostate cancer (CRPC) • metastatic castration-sensitive prostate cancer (mCSPC) • non‑metastatic castration‑sensitive prostate cancer (nmCSPC) with biochemical recurrence at high risk for metastasis (high-risk BCR) XTANDI is an androgen receptor inhibitor indicated for the treatment of patients with: • castration-resistant prostate cancer. • metastatic castration-sensitive prostate cancer. • non‑metastatic castration‑sensitive prostate cancer with biochemical recurrence at high risk for metastasis.

Dosage and administration (summary)

• Take XTANDI 160 mg administered orally once daily with or without food. • Advise patients to take each capsule or tablet whole with a sufficient amount of water to ensure that all medication is successfully swallowed. ( 2.1 , 5.7 ) • Patients receiving XTANDI for castration-resistant prostate cancer, or metastatic castration-sensitive prostate cancer should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy. • Patients with non-metastatic castration-sensitive prostate cancer with biochemical recurrence at high risk for metastasis may be treated with or without a GnRH analog.

Contraindications

None. None.

Warnings and precautions

• Seizure occurred in 0.6% of patients receiving XTANDI. In patients with predisposing factors, seizures were reported in 2.2% of patients. Permanently discontinue XTANDI in patients who develop a seizure during treatment. • Posterior reversible encephalopathy syndrome (PRES): Discontinue XTANDI. • Hypersensitivity: Discontinue XTANDI. • Ischemic Heart Disease: Optimize management of cardiovascular risk factors.

Pregnancy

Pregnancy Risk Summary The safety and efficacy of XTANDI have not been established in females. Based on animal reproductive studies and mechanism of action, XTANDI can cause fetal harm and loss of pregnancy. There are no human data on the use of XTANDI in pregnant females.

Storage and supply

(enzalutamide) 40 mg capsules are supplied as white to off-white oblong soft gelatin capsules imprinted in black ink with ENZ and are available in the following package size: • Bottles of 120 capsules with child resistant closures (NDC 0469-0125-99) XTANDI (enzalutamide) 40 mg tablets are supplied as yellow, round, film-coated tablets debossed with…

Source: Enzalutamide (Xtandi) — US FDA prescribing information, 2026-07-28, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.