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Updated: Apr 29, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Evolution of androgen receptor targeted therapy for advanced prostate cancer
Yien Ning Sophia Wong1, Roberta Ferraldeschi2, Gerhardt Attard3
1Prostate Targeted Therapy Group, The Institute of Cancer Research and Royal Marsden NHS Foundation Trust, 15 Cotswold Road, Sutton, London SM2 5NG, UK.
Abstract:
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.
Insights
Prostate cancer treatment relies on androgen depletion, but resistance is common. Newer androgen receptor therapies offer hope, with ongoing research addressing future challenges in advanced prostate cancer.
Area of Science:
- Oncology
- Urology
- Pharmacology
Background:
- Androgen dependence is fundamental to prostate cancer treatment since 1941.
- Most patients develop castration-resistant prostate cancer after initial androgen depletion therapy response.
Purpose of the Study:
- To review the historical development of androgen receptor (AR) targeting agents.
- To discuss current and future challenges in advanced prostate cancer therapeutics.
Main Methods:
- Literature review of androgen receptor targeting agents.
- Analysis of mechanisms driving resistance to castration.
- Discussion of next-generation AR-targeting drugs like abiraterone acetate and enzalutamide.
Main Results:
- Androgen depletion therapy (ADT) is a cornerstone but leads to inevitable resistance.
- Understanding resistance mechanisms has spurred development of novel AR-targeting agents.
- Abiraterone acetate and enzalutamide represent significant advancements in managing advanced prostate cancer.
Conclusions:
- The evolution of AR-targeting agents has transformed advanced prostate cancer treatment.
- Continued research is crucial to overcome resistance and improve patient outcomes.
- Future strategies must address the complexities of castration-resistant prostate cancer.
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