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
Clinical trials
- AFFIRM: Safety and Efficacy Study of MDV3100 in Patients With Castration-Resistant Prostate Cancer Who Have Been Previously Treated With Docetaxel-based Chemotherapy (AFFIRM)[4]
- PREVAIL: A Safety and Efficacy Study of Oral MDV3100 in Chemotherapy-Naive Patients With Progressive Metastatic Prostate Cancer (PREVAIL)
Patient drug information
- Enzalutamide (Xtandi) package insert[1]
- Enzalutamide (Xtandi) patient drug information (Chemocare)[5]
- Enzalutamide (Xtandi) patient drug information (UpToDate)[6]
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 needed to be after docetaxel).
Also known as
MDV3100.
References
- ↑ 1.0 1.1 Enzalutamide (Xtandi) package insert
- ↑ Enzalutamide (Xtandi) package insert (locally hosted backup)
- ↑ Xtandi manufacturer's website
- ↑ Scher HI, Fizazi K, Saad F, Taplin ME, Sternberg CN, Miller MD, de Wit R, Mulders P, Chi KN, Shore ND, Armstrong AJ, Flaig TW, Fléchon A, Mainwaring P, Fleming M, Hainsworth JD, Hirmand M, Selby B, Seely L, de Bono JS; the AFFIRM Investigators. Increased Survival with Enzalutamide in Prostate Cancer after Chemotherapy. N Engl J Med. 2012 Aug 15. [Epub ahead of print] link to original article contains verified protocol PubMed ClinicalTrials.gov
- ↑ Enzalutamide (Xtandi) patient drug information (Chemocare)
- ↑ Enzalutamide (Xtandi) patient drug information (UpToDate)