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Androgen receptor splice variants in the era of enzalutamide and abiraterone

Mary Nakazawa1, Emmanuel S Antonarakis, Jun Luo

  • 1The James Buchanan Brady Urological Institute and Department of Urology, The Johns Hopkins School of Medicine, 600 N Wolfe St, 411 Marburg Bldg, Baltimore, MD, 21287, USA.

Hormones & Cancer
|July 23, 2014
PubMed

Insights

Prostate cancer cells remain addicted to androgen receptor (AR) signaling, leading to resistance against therapies like enzalutamide and abiraterone. Androgen receptor splice variants (AR-Vs) are key drivers of this resistance, necessitating new drug development for advanced prostate cancer.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Enzalutamide and abiraterone target androgen receptor (AR) signaling in prostate cancer.
  • Resistance to these therapies is characterized by the restoration of AR signaling.
  • Prostate cancer exhibits a dependence on the AR pathway, even in castration-resistant forms.

Purpose of the Study:

  • To review mechanisms of resistance to AR-directed therapies in prostate cancer.
  • To focus on the role of androgen receptor splice variants (AR-Vs) in treatment resistance.
  • To discuss the implications for developing new therapies for advanced prostate cancer.

Main Methods:

  • Literature review of preclinical and clinical studies.
  • Analysis of molecular mechanisms underlying castration resistance.
  • Discussion of drug resistance patterns in advanced prostate cancer.

Main Results:

  • Prostate cancer cells show a strong "addiction" to AR signaling, persisting despite therapeutic interventions.
  • Androgen receptor splice variants (AR-Vs), especially AR-V7, are implicated in resistance to enzalutamide and abiraterone.
  • Current AR-directed drugs are ineffective against AR-V-driven resistance.

Conclusions:

  • Resistance to enzalutamide and abiraterone is often mediated by sustained AR signaling.
  • AR-Vs represent a significant challenge in treating advanced prostate cancer.
  • Development of novel drugs targeting AR-V-associated castration-resistant prostate cancer is crucial.

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