Evolution of androgen receptor targeted therapy for advanced prostate cancer

Nat Rev Clin Oncol. 2014 Jun;11(6):365-76. doi: 10.1038/nrclinonc.2014.72. Epub 2014 May 20.


The discovery of androgen dependence in prostate cancer in 1941 by Huggins and colleagues has remained the backbone for the treatment of this disease. However, although many patients initially respond to androgen depletion therapy, they almost invariably relapse and develop resistance with transition of the disease to a castration-resistant state. Over the past decade, the better understanding of the mechanisms that drive resistance to castration has led to the development of next-generation androgen receptor targeting agents such as abiraterone acetate and enzalutamide. This Review aims to revisit the discovery and evolution of androgen receptor targeting therapeutics for the treatment of advanced-stage prostate cancer over the years and to discuss the upcoming future and challenges in the treatment of this common cancer.

Publication types

  • Review

MeSH terms

  • Androgen Antagonists / therapeutic use*
  • Humans
  • Male
  • Molecular Targeted Therapy
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms, Castration-Resistant / drug therapy
  • Prostatic Neoplasms, Castration-Resistant / metabolism
  • Receptors, Androgen / metabolism*


  • Androgen Antagonists
  • Receptors, Androgen