Progress of CDK4/6 Inhibitor Palbociclib in the Treatment of Cancer

Anticancer Agents Med Chem. 2018;18(9):1241-1251. doi: 10.2174/1871521409666170412123500.

Abstract

The Cyclin-Dependent Kinases (CDKs) and their cyclin partners are key regulators of the cell cycle. These kinases are closely related to oncogenesis and have been proved to be attractive targets for designing novel anticancer agents. The CDK inhibitors can effectively suppress the excessive proliferation of tumor cells by inducing cell cycle arrest. In recent years, a large number of CDK inhibitors have entered pre-clinical and/or clinical trials. Among these compounds, the selective CDK4/6 inhibitor Palbociclib has been approved by FDA for breast cancer treatment. Moreover, Palbociclib demonstrated promising antitumor potential as monotherapy or combined therapy in numerous clinical trials. Herein, we provide a brief review focused on the recent progress of clinical studies about Palbociclib.

Keywords: Cyclin-Dependent Kinases (CDKs); anti-cancer; cell cycle arrest; combined therapy; monotherapy; palbociclib..

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Cell Cycle Checkpoints / drug effects
  • Cyclin-Dependent Kinase 4 / antagonists & inhibitors*
  • Cyclin-Dependent Kinase 4 / metabolism
  • Cyclin-Dependent Kinase 6 / antagonists & inhibitors*
  • Cyclin-Dependent Kinase 6 / metabolism
  • Drug Development
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Piperazines / chemistry
  • Piperazines / pharmacology
  • Piperazines / therapeutic use*
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Pyridines / therapeutic use*

Substances

  • Antineoplastic Agents
  • Piperazines
  • Protein Kinase Inhibitors
  • Pyridines
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 6
  • palbociclib