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.^[1]^[2]^[3]
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

Patient drug information

History of changes in FDA indication

2012-08-31: Initial approval for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel. (Based on AFFIRM)
2014-09-10: Approved for the treatment of patients with metastatic castration-resistant prostate cancer (mCRPC). (No longer needs to be after docetaxel; based on PREVAIL and TERRAIN)
2018-07-13: Approved for patients with castration-resistant prostate cancer (CRPC). (No longer needs to be metatstatic; based on PROSPER_PrCA)
2019-12-16: Approved for patients with metastatic castration-sensitive prostate cancer (mCSPC). (No longer needs to be castration-resistant, if metastatic; based on ARCHES)

History of changes in EMA indication

2013-06-21: Initial marketing authorization as Xtandi

History of changes in Health Canada indication

2013-05-29: Initial notice of compliance

History of changes in PMDA indication

2014-03-24: Initial approval for the treatment of castration-resistant prostate cancer.
2020-05-29: New indication for the treatment of metastatic prostate cancer.

Also known as

Code name: MDV3100
Brand names: Azel, Bdenza, Bnyx, Capmide, Enzamide, Glenza, Indenza, Xtandi

References

[insert-1] 1.0 ^1.1 Enzalutamide (Xtandi) package insert

[2] Enzalutamide (Xtandi) package insert (locally hosted backup)

[3] Xtandi manufacturer's website

[4] Enzalutamide (Xtandi) patient drug information (Chemocare)

[5] Enzalutamide (Xtandi) patient drug information (UpToDate)

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