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Updated: Feb 5, 2026

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

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Non-Steroidal Androgen Receptor Antagonists and Prostate Cancer: A Survey on Chemical Structures Binding this

Claudia Ferroni1, Greta Varchi1

  • 1Institute of Organic Synthesis and Photoreactivity - ISOF, Italian National Research Council, Bologna, Italy.

Current Medicinal Chemistry
|September 14, 2018
PubMed

Insights

This review explores non-steroidal androgen receptor (AR) antagonists for prostate cancer treatment. It highlights their mechanisms and efficacy against castration-resistant prostate cancer (CRPC) and drug resistance.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The Androgen Receptor (AR) pathway is critical in prostate cancer pathogenesis and progression.
  • AR signaling drives Castration-Resistant Prostate Cancer (CRPC) development and resistance to therapies like enzalutamide and abiraterone.
  • Drug resistance necessitates the development of novel therapeutic strategies targeting the AR pathway.

Purpose of the Study:

  • To review promising classes of non-steroidal androgen receptor antagonists.
  • To provide insights into the mechanisms of action of these antagonists.
  • To evaluate their efficacy in treating prostate cancer, particularly CRPC.

Main Methods:

  • Literature review of scientific publications.
  • Analysis of small molecule AR antagonists.
  • Survey of preclinical and clinical data on AR antagonist efficacy.
  • Examination of resistance mechanisms to current therapies.

Main Results:

  • Several classes of non-steroidal AR antagonists show significant therapeutic potential.
  • These agents target AR signaling through various mechanisms.
  • Efficacy is demonstrated in preclinical models and some clinical settings of prostate cancer.

Conclusions:

  • Non-steroidal AR antagonists represent a promising therapeutic avenue for prostate cancer.
  • Understanding their mechanisms is key to overcoming resistance.
  • Further development is crucial for effective CRPC treatment.
Keywords:
AR protein degradersAR-targeting conjugatesAndrogen receptorPROTACsantiandrogenscastration resistant prostate cancerpoint mutations.

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