A patent review of anticancer CDK2 inhibitors (2017-present)

Expert Opin Ther Pat. 2022 Aug;32(8):885-898. doi: 10.1080/13543776.2022.2078193. Epub 2022 May 26.

Abstract

Introduction: The success of the CDK4/6 inhibitor Ibrance™ (Palbociclib) as an anticancer agent inspired and directed more efforts toward the discovery of selective cyclin-dependent kinase (CDKs) inhibitors. CDK2 is a member of the CDKs family that plays an important role in regulating the progression of cells into both S- and M-phases of the cell cycle. Studies suggest that overexpression of CDK2 may be implicated in tumor growth in cancer.

Areas covered: This review covers the patent literature of CDK2 inhibitors published between 2017 and 2021. We searched the online databases of the European Patent Office, American Chemical Society, and Google patents.

Expert opinion: Developing selective CDK2 inhibitors is challenging due to the absence of a previously approved selective CDK2 inhibitor. However, ongoing efforts by Incyte Corporation and Pfizer Inc., which are reported herein, may stand out as a new starting point and bring novel information critical for the medicinal chemistry and drug design scientists in the field of CDK2 inhibitors' development.

Keywords: Anticancer; CDK inhibitors; cell cycle; cyclins; kinase inhibitors.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Cell Cycle
  • Cyclin-Dependent Kinase 2* / antagonists & inhibitors
  • Humans
  • Neoplasms* / drug therapy
  • Patents as Topic

Substances

  • Antineoplastic Agents
  • CDK2 protein, human
  • Cyclin-Dependent Kinase 2