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Updated: Sep 4, 2025

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
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Second generation androgen receptor antagonists and challenges in prostate cancer treatment

Yanhua Chen1, Qianqian Zhou1, William Hankey2

  • 1Academy of Integrative Medicine, Shanghai University of Traditional Chinese Medicine, 201203, Shanghai, China.

Cell Death & Disease
|July 21, 2022
PubMed

Insights

Androgen receptor (AR) antagonists improve survival for prostate cancer patients but do not cure the disease. Emerging challenges include resistance mechanisms and progression to neuroendocrine prostate cancer (NEPC).

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Prostate cancer is a hormone-dependent malignancy driven by the androgen receptor (AR) signaling pathway.
  • AR signaling pathway inhibitors are the primary treatment for metastatic prostate cancer.

Purpose of the Study:

  • To summarize current AR antagonist development for prostate cancer.
  • To highlight clinical application challenges and resistance mechanisms.
  • To explore potential combination therapies and novel AR-targeted treatments.

Main Methods:

  • Review of current literature on AR antagonist therapies.
  • Analysis of clinical trial data and resistance mechanisms.
  • Exploration of emerging therapeutic strategies.

Main Results:

  • Second-generation AR antagonists (enzalutamide, apalutamide, darolutamide) have improved patient survival.
  • These agents are effective in both androgen-dependent and castration-resistant prostate cancer.
  • Patients eventually progress to lethal neuroendocrine prostate cancer (NEPC) despite treatment.

Conclusions:

  • AR antagonists offer survival benefits but do not provide a cure for prostate cancer.
  • Resistance mechanisms and progression to NEPC present significant challenges.
  • Combination therapies and novel AR-targeted agents are needed to overcome resistance and improve outcomes.

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