BET inhibitors in metastatic prostate cancer: therapeutic implications and rational drug combinations

Research output: Contribution to journalReview articlepeer-review


Introduction: The bromodomain and extra-terminal (BET) family of proteins are epigenetic readers of acetylated histones regulating a vast network of protein expression across many different cancers. Therapeutic targeting of BET is an attractive area of clinical development for metastatic castration-resistant prostate cancer (mCRPC), particularly due to its putative effect on c-MYC expression and its interaction with the androgen receptor (AR). Areas covered: We speculate that a combination approach using inhibitors of BET proteins (BETi) with other targeted therapies may be required to improve the therapeutic index of BET inhibition in the management of prostate cancer. Preclinical data has identified several molecular targets that may enhance the effect of BET inhibition in the clinic. This review will summarize the known preclinical data implicating BET as an important therapeutic target in advanced prostate cancer, highlight the ongoing clinical trials targeting this protein family, and speculate on rationale combination strategies using BETi together with other agents in prostate cancer. A literature search using Pubmed was performed for this review. Expert opinion: Use of BETi in the treatment of mCRPC patients may require the addition of a second novel agent.

Original languageEnglish (US)
Pages (from-to)1391-1397
Number of pages7
JournalExpert Opinion on Investigational Drugs
Issue number12
StatePublished - Dec 2 2017


  • BET
  • Bromodomain
  • drug combinations
  • epigenetics
  • prostate cancer

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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