Enzalutamide therapy for advanced prostate cancer: efficacy, resistance and beyond

Simon Linder, Henk G. van der Poel, Andries M. Bergman, Wilbert Zwart, Stefan Prekovic

Research output: Contribution to journalArticleAcademicpeer-review

41 Citations (Scopus)
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The androgen receptor drives the growth of metastatic castration-resistant prostate cancer. This has led to the development of multiple novel drugs targeting this hormone-regulated transcription factor, such as enzalutamide – a potent androgen receptor antagonist. Despite the plethora of possible treatment options, the absolute survival benefit of each treatment separately is limited to a few months. Therefore, current research efforts are directed to determine the optimal sequence of therapies, discover novel drugs effective in metastatic castration-resistant prostate cancer and define patient subpopulations that ultimately benefit from these treatments. Molecular studies provide evidence on which pathways mediate treatment resistance and may lead to improved treatment for metastatic castration-resistant prostate cancer. This review provides, firstly a concise overview of the clinical development, use and effectiveness of enzalutamide in the treatment of advanced prostate cancer, secondly it describes translational research addressing enzalutamide response vs resistance and lastly highlights novel potential treatment strategies in the enzalutamide-resistant setting.

Original languageEnglish
Pages (from-to)R31-R52
Number of pages22
JournalEndocrine-related cancer
Issue number1
Publication statusPublished - Jan 2019


  • Androgen deprivation therapy
  • Androgen receptor
  • Biomarkers
  • Docetaxel
  • Enzalutamide
  • Mutations
  • Prostate cancer
  • Treatment resistance
  • androgen deprivation therapy
  • biomarkers
  • mCRPC
  • prostate cancer
  • androgen receptor
  • mutations
  • docetaxel
  • enzalutamide
  • treatment resistance
  • Humans
  • Drug Resistance, Neoplasm/drug effects
  • Male
  • Phenylthiohydantoin/analogs & derivatives
  • Prostatic Neoplasms, Castration-Resistant/drug therapy


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