XTANDI- enzalutamide capsule
Astellas Pharma US, Inc.
1 INDICATIONS AND USAGE
XTANDI� is indicated for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC).
2 DOSAGE AND ADMINISTRATION
2.1 Dosing Information
The recommended dose of XTANDI is 160 mg (four 40 mg capsules) administered orally once daily. XTANDI can be taken with or without food [see Clinical Pharmacology (12.3)]. Swallow capsules whole. Do not chew, dissolve, or open the capsules.
DOSAGE FORMS AND STRENGTHS
XTANDI 40 mg capsules are white to off-white oblong soft gelatin capsules imprinted in black ink with ENZ
DESCRIPTION
Enzalutamide is an androgen receptor inhibitor. The chemical name is 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl}-2-fluoro-N -methylbenzamide.
The molecular weight is 464.44 and molecular formula is C21 H16 F4 N4 O2 S. The structural formula is:
Structural formula of Enzalutamide
(click image for full-size original)
Enzalutamide is a white crystalline non-hygroscopic solid. It is practically insoluble in water.
XTANDI is provided as liquid-filled soft gelatin capsules for oral administration. Each capsule contains 40 mg of enzalutamide as a solution in caprylocaproyl polyoxylglycerides. The inactive ingredients are caprylocaproyl polyoxylglycerides, butylated hydroxyanisole, butylated hydroxytoluene, gelatin, sorbitol sorbitan solution, glycerin, purified water, titanium dioxide, and black iron oxide.
12 CLINICAL PHARMACOLOGY
12.1 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 inhibit androgen receptor nuclear translocation and 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.