Enzalutamide (Xtandi)

General information

Class/mechanism: Antiandrogen; androgen receptor inhibitor (ARI) or androgen receptor signaling inhibitor (ARSI). Enzalutamide competitively inhibits testosterone from binding to the androgen receptor, interferes with translocation of the androgen receptor to the nucleus, and inhibits binding to DNA, resulting in decreased prostate cancer proliferation and cell death.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• Breast cancer, triple negative
• Prostate cancer

Patient drug information

• Enzalutamide (Xtandi) package insert
• Enzalutamide (Xtandi) patient drug information (Chemocare)
• Enzalutamide (Xtandi) patient drug information (UpToDate)

History of changes in FDA indication

• 8/31/2012: Initial FDA approval "for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel."
• 9/10/2014: FDA approved "for the treatment of patients with metastatic castration-resistant prostate cancer (mCRPC)." (no longer needs to be after docetaxel)

Also known as

• Code name: MDV3100
• Brand name: Xtandi