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A patent review of BRD4 inhibitors (2020-present)

Yanfang Chen1, Huanmin Zhou2, Jiamin Yu3,4

  • 1Key Laboratory of Microbial Pathogenesis and Interventions of Fujian Province University, the Key Laboratory of Innate Immune Biology of Fujian Province, Biomedical Research Center of South China, College of Life Sciences, Fujian Normal University, Fuzhou, China.

Expert Opinion on Therapeutic Patents
|February 7, 2025
PubMed
Abstract

Insights

Bromodomain-containing protein 4 (BRD4) is a key target for cancer therapy. Recent patents focus on selective BRD4 inhibitors to improve efficacy and reduce side effects compared to older pan-BET inhibitors.

Area of Science:

  • Epigenetics and Gene Regulation
  • Cancer Therapeutics
  • Drug Discovery

Background:

  • Bromodomain-containing protein 4 (BRD4) is part of the BET family, regulating gene expression.
  • BRD4's role in various cancers makes it a significant therapeutic target.
  • Existing pan-BET inhibitors face challenges with dose-limiting toxicities.

Purpose of the Study:

  • To review patent applications for BRD4 inhibitors from 2020 to the present.
  • To summarize recent advancements in BRD4-targeted therapies.
  • To highlight the shift towards selective BRD4 inhibitors.

Main Methods:

  • Searched patent databases (SciFinder, PubMed, The lens) using the keyword 'BRD4'.
  • Focused on applications published from 2020 to the present.
  • Analyzed a total of 70 patent applications.

Main Results:

  • Identified a growing number of patent applications related to BRD4 inhibitors.
  • Observed a trend towards developing selective inhibitors for BRD4's BD1 or BD2 domains.
  • Highlighted the potential of these selective inhibitors over pan-BET inhibitors.

Conclusions:

  • Selective BRD4 inhibitors show promise for overcoming the limitations of pan-BET inhibitors.
  • These targeted approaches may lead to more effective cancer treatments.
  • Further research in selective BRD4 inhibition is crucial for both fundamental and translational science.
Keywords:
BETBRD4cancer treatmentinhibitorselectivity

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