Enzalutamide (2 brand names, 2 dosage forms, 1 route)
Available dosage forms: CAPSULE, TABLET.
Routes of administration: ORAL.
Brand Names
- ENZALUTAMIDE
- XTANDI
Indications and Usage
XTANDI® 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)
Contraindications
None.
Adverse Reactions
The following is discussed in more detail in other sections of the labeling: •Seizure [see Warnings and Precautions (5.1)] •Posterior Reversible Encephalopathy Syndrome (PRES) [see Warnings and Precautions (5.2)] •Hypersensitivity [see Warnings and Precautions (5.3)] •Ischemic Heart Disease [see Warnings and Precautions (5.4)] •Falls and Fractures [see Warnings and Precautions (5.5)] •Dysphagia or Choking [see Warnings and Precautions (5.7)]
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.
Overdosage
In the event of an overdosage, stop treatment with XTANDI and initiate general supportive measures taking into consideration the half-life of 5.8 days. In a dose escalation study, no seizures were reported at < 240 mg daily, whereas 3 seizures were reported, 1 each at 360 mg, 480 mg, and 600 mg daily. Patients may be at increased risk of seizure following an overdosage.