Abiraterone acetate: redefining hormone treatment for advanced prostate cancer

Drug Discov Today. 2012 Mar;17(5-6):221-6. doi: 10.1016/j.drudis.2011.12.012. Epub 2011 Dec 19.


Prostate cancer has long since been recognised as being hormonally driven via androgen receptor signalling. Abiraterone acetate (AA) is a rationally designed CYP17 inhibitor that blocks the conversion of androgens from non-gonadal precursors effectively, thus reducing testosterone to undetectable levels. AA has recently been proved to extend survival for men with metastatic castration-resistant prostate cancer who have progressive disease after first-line chemotherapy treatment. In addition, it is currently being tested in a Phase III trial in the pre-chemotherapy setting. This paper will review the preclinical discovery and clinical development of AA and will outline the strategy of parallel translational research.

Publication types

  • Review

MeSH terms

  • Abiraterone Acetate
  • Androgen Antagonists / pharmacology
  • Androgen Antagonists / therapeutic use
  • Androstadienes / pharmacology*
  • Androstadienes / therapeutic use*
  • Animals
  • Clinical Trials as Topic
  • Drug Evaluation, Preclinical
  • Hormone Replacement Therapy / methods
  • Humans
  • Male
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / metabolism


  • Androgen Antagonists
  • Androstadienes
  • Abiraterone Acetate