[Cell cycle inhibitors in endocrine receptor positive breast cancer]

Bull Cancer. 2017 Feb;104(2):114-122. doi: 10.1016/j.bulcan.2016.12.005. Epub 2017 Jan 23.
[Article in French]

Abstract

Dysregulation of cellular cycle is a key component of carcinogenesis and its targeting represents an interesting approach. Recently, the development of selective inhibitors of the cycle targeting the cyclin-dependent kinases (CDK) 4 and 6 revived interest in this therapeutic class after the failure of pan-inhibitors. Palbociclib, ribociclib, and abemaciclib are the 3 drugs with the most advanced development. They demonstrated preclinical activity in luminal breast cancer models and are under clinical evaluation. The first available studies demonstrate the value of these compounds with an improved prognosis of metastatic patients in combination with endocrine therapy (palbociclib, ribociclib) or in monotherapy (abemaciclib). The results of ongoing studies will clarify the role of these agents in our new strategies and the individualisation of biomarkers will help to define patients who benefit most from this approach.

Keywords: Abemaciclib; Breast cancer; CDK4/6 inhibitors; Cancer du sein; Cellular cycle; Cycle cellulaire; Inhibiteurs de CDK4/6; Palbociclib; Ribociclib.

MeSH terms

  • Aminopyridines / adverse effects
  • Aminopyridines / therapeutic use
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / therapeutic use*
  • Benzimidazoles / adverse effects
  • Benzimidazoles / therapeutic use
  • Breast Neoplasms / chemistry
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / pathology
  • Cell Cycle / physiology
  • Cell Cycle Checkpoints
  • Clinical Trials as Topic
  • Cyclin-Dependent Kinase 4 / antagonists & inhibitors*
  • Cyclin-Dependent Kinase 4 / physiology
  • Cyclin-Dependent Kinase 6 / antagonists & inhibitors*
  • Cyclin-Dependent Kinase 6 / physiology
  • Female
  • Humans
  • Neoplasms, Hormone-Dependent / chemistry
  • Neoplasms, Hormone-Dependent / drug therapy*
  • Piperazines / adverse effects
  • Piperazines / therapeutic use
  • Protein Kinase Inhibitors / adverse effects
  • Protein Kinase Inhibitors / therapeutic use*
  • Purines / adverse effects
  • Purines / therapeutic use
  • Pyridines / adverse effects
  • Pyridines / therapeutic use

Substances

  • Aminopyridines
  • Antineoplastic Agents
  • Benzimidazoles
  • Piperazines
  • Protein Kinase Inhibitors
  • Purines
  • Pyridines
  • abemaciclib
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 6
  • palbociclib
  • ribociclib