Advances in kinase targeting: current clinical use and clinical trials

Trends Pharmacol Sci. 2014 Nov;35(11):604-20. doi: 10.1016/ Epub 2014 Oct 10.


Phosphotransferases, also known as kinases, are the most intensively studied protein drug target category in current pharmacological research, as evidenced by the vast number of kinase-targeting agents enrolled in active clinical trials. This development has emerged following the great success of small-molecule, orally available protein kinase inhibitors for the treatment of cancer, starting with the introduction of imatinib (Gleevec®) in 2003. The pharmacological utility of kinase-targeting has expanded to include treatment of inflammatory diseases, and rapid development is ongoing for kinase-targeted therapies in a broad array of indications in ophthalmology, analgesia, central nervous system (CNS) disorders, and the complications of diabetes, osteoporosis, and otology. In this review we highlight specifically the kinase drug targets and kinase-targeting agents being explored in current clinical trials. This analysis is based on a recent estimate of all established and clinical trial drug mechanisms of action, utilizing private and public databases to create an extensive dataset detailing aspects of more than 3000 approved and experimental drugs.

Keywords: clinical trials; drug targets; phosphotransferase; protein kinase; serine/threonine-protein kinase; tyrosine-protein kinase.

Publication types

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

MeSH terms

  • Animals
  • Clinical Trials as Topic / methods*
  • Enzyme Activators / therapeutic use*
  • Humans
  • Molecular Targeted Therapy
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein Kinases / metabolism*


  • Enzyme Activators
  • Protein Kinase Inhibitors
  • Protein Kinases