Galeterone (TOK-001)

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General information

Class/mechanism: Antiandrogen with multiple mechanisms of action: androgen receptor inhibitor (ARI), androgen biosynthesis inhibitor (CYP17 inhibitor), and accelerates degradation of the androgen receptor. Galeterone is believed to decrease prostate cancer proliferation and trigger cell death by interfering with testosterone-mediated pathways and signaling mechanisms used by prostate cancer cells.[1][2]
Route: PO
Extravasation: n/a

For conciseness and simplicity, 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.

Patient drug information

No information available.

Also known as

  • Code names: AR-V7, TOK-001, VN/124-1


  1. Robert B. Montgomery, Mario A. Eisenberger, Elisabeth I. Heath, A. Oliver Sartor, Franklin Chu, Neal D. Shore, William Jeffery Edenfield, Alan J. Koletsky, David Uri Lipsitz, James S. Cochran, Luke T. Nordquist, Jennifer Roberts, Mary-Ellen Taplin. Galeterone in men with CRPC: Results in four distinct patient populations from the ARMOR2 study. 2014 ASCO Annual Meeting abstract 5029. link to abstract
  2. Galeterone Shows Activity in Variant Form of Castration-Resistant Prostate Cancer The ASCO Post, 11/19/2014