Related Experiment Video

Updated: May 15, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
07:25

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer

Published on: March 6, 2018

Androgen receptor antagonists in castration-resistant prostate cancer

Dana Rathkopf1, Howard I Scher

  • 1Genitourinary Oncology Service, Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.

Cancer Journal (Sudbury, Mass.)
|January 23, 2013
PubMed

Insights

New androgen receptor (AR) antagonists like enzalutamide show promise for castration-resistant prostate cancer (CRPC) treatment. These drugs target persistent AR signaling, improving survival in advanced prostate cancer patients.

Area of Science:

  • Oncology
  • Pharmacology
  • Urology

Background:

  • Persistent androgen receptor (AR) signaling is a key challenge in castration-resistant prostate cancer (CRPC).
  • AR remains a relevant therapeutic target in CRPC, as evidenced by FDA-approved agents.

Purpose of the Study:

  • To review the role of the androgen receptor (AR) in CRPC.
  • To discuss next-generation AR antagonists, specifically enzalutamide and ARN-509, for advanced prostate cancer treatment.

Main Methods:

  • Review of current literature on AR signaling in CRPC.
  • Comparison of next-generation AR antagonists (enzalutamide, ARN-509) with conventional antiandrogens (bicalutamide).
  • Analysis of preclinical data on AR antagonist efficacy, including binding affinity, nuclear translocation inhibition, DNA binding prevention, and apoptosis induction.

Main Results:

  • Enzalutamide and ARN-509 demonstrate higher affinity binding to the AR compared to bicalutamide.
  • These agents effectively inhibit AR nuclear translocation and DNA binding.
  • Preclinical models show these antagonists induce apoptosis without agonist activity.

Conclusions:

  • Next-generation AR antagonists offer significant promise for patients with advanced CRPC.
  • The clinical success of these agents has transformed CRPC therapy.
  • Ongoing development aims to build upon this therapeutic platform for future treatment options.

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