Second-generation ALK inhibitors: filling the non "MET" gap

Cancer Discov. 2014 Jun;4(6):634-6. doi: 10.1158/2159-8290.CD-14-0410.

Abstract

Ceritinib and other second-generation inhibitors have demonstrated promising anticancer activity in anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC). Specifically, they can overcome resistance due to certain gatekeeper mutations acquired following crizotinib exposure. These agents now provide new options for the management of ALK-positive NSCLC.

MeSH terms

  • Anaplastic Lymphoma Kinase
  • Antineoplastic Agents / therapeutic use*
  • Carbazoles / therapeutic use
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / genetics
  • Crizotinib
  • Drug Resistance, Neoplasm / genetics
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / genetics
  • Mutation
  • Piperidines / therapeutic use
  • Protein Kinase Inhibitors / therapeutic use*
  • Pyrazoles / therapeutic use
  • Pyridines / therapeutic use
  • Pyrimidines / therapeutic use
  • Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Sulfones / therapeutic use

Substances

  • Antineoplastic Agents
  • Carbazoles
  • Piperidines
  • Protein Kinase Inhibitors
  • Pyrazoles
  • Pyridines
  • Pyrimidines
  • Sulfones
  • Crizotinib
  • ALK protein, human
  • Anaplastic Lymphoma Kinase
  • RON protein
  • Receptor Protein-Tyrosine Kinases
  • ceritinib
  • alectinib