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A patent review of CHK1 inhibitors (2019 - present)

Tao Liu1, Mingbo Su2, Yuxuan Wang3

  • 1Institute of Drug Discovery and Design, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.

Expert Opinion on Therapeutic Patents
|August 18, 2025
PubMed
Abstract

Insights

Checkpoint kinase 1 (CHK1) inhibitors are crucial for DNA damage response in cancer. While many are in clinical trials, none are approved, highlighting the need for novel, selective CHK1 inhibitors in cancer therapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Checkpoint kinase 1 (CHK1) is vital for DNA damage response (DDR), regulating cell cycle checkpoints, DNA repair, and apoptosis.
  • CHK1 inhibitors are investigated as cancer therapeutics, with over 15 in clinical trials, but none have reached market approval.

Purpose of the Study:

  • To conduct a comprehensive patent review of CHK1 inhibitors in oncology.
  • To analyze combination products and structural insights of CHK1 inhibitors.
  • To assess the current landscape and future directions for CHK1 inhibitor development.

Main Methods:

  • A patent literature review from January 2019 to December 2024.
  • Searches conducted across Scopus, Espacenet, Web of Science, WIPO, Google Patents, Cortellis, and USPTO databases.

Main Results:

  • Identified numerous CHK1 inhibitors in various stages of development.
  • Highlighted the importance of novel skeletons and combination therapies.
  • Emphasized the ongoing research in rational drug design and biomarker identification.

Conclusions:

  • Development of potent, selective CHK1 inhibitors with novel structures is critical for cancer treatment.
  • Combination therapies and biomarker-guided strategies hold significant promise.
  • Further advancements in CHK1 inhibitor research are essential for effective cancer therapeutics.
Keywords:
CHK1CHK1 inhibitorDDRcancer therapycombinationpatentpredictive biomarker

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