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

Mohamed A. Said, Mohamed A. Abdelrahman, Mohammed A. S. Abourehab, Mohamed Farès, Wagdy M. Eldehna

2022Expert Opinion on Therapeutic Patents22 citationsDOI

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.

Topics & Concepts

Cyclin-dependent kinaseCyclin-dependent kinase 2PalbociclibDrug discoveryKinaseCancer researchBiologyCell cycleCancerBiochemistryProtein kinase ACellGeneticsMetastatic breast cancerBreast cancerAdvanced Breast Cancer TherapiesCancer-related Molecular PathwaysProtein Degradation and Inhibitors
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