Issues and progress with protein kinase inhibitors for cancer treatment

Nat Rev Drug Discov. 2003 Apr;2(4):296-313. doi: 10.1038/nrd1066.


Identification of the key roles of protein kinases in cancer has led to extensive efforts to develop kinase inhibitors for the treatment of a wide range of cancers, and more than 30 such agents are now in clinical trials. Here, we consider the crucial issues in the development of kinase inhibitors for cancer, and discuss strategies to address the challenges raised by these issues in the light of preclinical and clinical experiences so far.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Clinical Trials as Topic
  • Drug Design
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Forecasting
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Protein Kinase Inhibitors*
  • Signal Transduction / drug effects


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Protein Kinase Inhibitors