A patent and literature review of CDK12 inhibitors

Ruijun Tang, Jing Liu, Shuyao Li, Junjie Zhang, Chunhong Yu, Honglu Liu, Fang Chen, Lu Lv, Qian Zhang, Kai Yuan, Hao Shao*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

4 Citations (Scopus)


Introduction: Cyclin-dependent kinase 12 (CDK12) belongs to the CDK family of serine/threonine protein kinases and is associated with cyclin K to exert its biological functions, including regulating gene transcription, mRNA processing, and translation. Increasing evidences demonstrate the importance of CDK12 in various human cancers, illustrating its potential as both biomarker and therapeutic target. In addition, CDK12 is also a promising target for the treatment of myotonic dystrophy type 1. Efforts have been taken to discover small molecule inhibitors to validate this important therapeutic target. Areas covered: This review covers the patented CDK12 inhibitors from 2016 to present, as well as these from peer-reviewed literature. It provides the reader an update of the discovery strategies, chemical structures, and molecular profiling of all available CDK12 inhibitors. Expert opinion: CDK12 inhibitors with various mechanism of actions have been discovered, and it is a great set of tools to evaluate the therapeutic potential of CDK12 in different disease models. CDK12 inhibitors have shown promising results in myotonic dystrophy type 1 mouse model and several preclinical cancer models either as single agent or combination with other anti-cancer agents. Its therapeutic value awaits more rigorous preclinical testing and further clinical investigation.

Original languageEnglish
Pages (from-to)1055-1065
Number of pages11
JournalExpert Opinion on Therapeutic Patents
Issue number10
Publication statusPublished - 2022


  • Anti-cancer agents
  • CDK12/cyclin K
  • DNA damage response
  • molecular-glue degrader
  • myotonic dystrophy type 1
  • transcription


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