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Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
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Molecular Mechanisms of Enzalutamide Resistance in Prostate Cancer

Zoran Culig1

  • 1Experimental Urology, Department of Urology, Medical University of Innsbruck, Anichstrasse 35, A-6020 Innsbruck, Austria.

Current Molecular Biology Reports
|December 8, 2017
PubMed
Abstract

Insights

Prostate cancer can develop resistance to enzalutamide through various mechanisms, including androgen receptor (AR) alterations and oncogene overexpression. Understanding these heterogeneous resistance pathways is crucial for developing effective post-enzalutamide treatments.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Prostate cancer treatment often involves androgen deprivation therapy.
  • Older anti-androgens like hydroxyflutamide and bicalutamide have been used, but resistance develops.
  • Enzalutamide is a newer anti-androgen with improved efficacy, yet resistance remains a challenge.

Purpose of the Study:

  • To review the compensatory mechanisms driving resistance to enzalutamide in prostate cancer.
  • To explore the molecular heterogeneity of enzalutamide resistance.
  • To identify potential therapeutic targets for overcoming resistance.

Main Methods:

  • Review of existing literature on enzalutamide resistance in prostate cancer.
  • Analysis of molecular alterations in androgen receptor (AR) and associated pathways.
  • Examination of pre-clinical models and patient data.

Main Results:

  • Enzalutamide resistance involves diverse mechanisms, including AR alterations and oncogene overexpression.
  • Androgen receptor splice variants and the AR F876L mutation are associated with resistance.
  • Glucocorticoid receptor overexpression is observed in resistant prostate cancer.

Conclusions:

  • Enzalutamide resistance in prostate cancer is complex and heterogeneous.
  • Targeting AR alterations and other oncogenic pathways is necessary for novel therapies.
  • Developing effective treatments post-enzalutamide remains a significant clinical challenge.
Keywords:
Anti-androgensCytokinesEnzalutamideMutationsTruncated androgen receptor

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