FDA-approved small-molecule kinase inhibitors

Trends Pharmacol Sci. 2015 Jul;36(7):422-39. doi: 10.1016/j.tips.2015.04.005. Epub 2015 May 12.


Kinases have emerged as one of the most intensively pursued targets in current pharmacological research, especially for cancer, due to their critical roles in cellular signaling. To date, the US FDA has approved 28 small-molecule kinase inhibitors, half of which were approved in the past 3 years. While the clinical data of these approved molecules are widely presented and structure-activity relationship (SAR) has been reported for individual molecules, an updated review that analyzes all approved molecules and summarizes current achievements and trends in the field has yet to be found. Here we present all approved small-molecule kinase inhibitors with an emphasis on binding mechanism and structural features, summarize current challenges, and discuss future directions in this field.

Keywords: cancer; crystal structure; lipid kinase; protein kinase; serine/threonine kinase; tyrosine kinase.

Publication types

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

MeSH terms

  • Drug Approval*
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Models, Molecular
  • Molecular Structure
  • Phosphatidylinositol 3-Kinases / chemistry
  • Phosphoinositide-3 Kinase Inhibitors
  • Phosphotransferases / antagonists & inhibitors*
  • Phosphotransferases / chemistry
  • Protein Binding
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology
  • Protein-Serine-Threonine Kinases / antagonists & inhibitors
  • Protein-Serine-Threonine Kinases / chemistry
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Protein-Tyrosine Kinases / chemistry
  • Receptor Protein-Tyrosine Kinases / antagonists & inhibitors
  • Receptor Protein-Tyrosine Kinases / chemistry
  • United States
  • United States Food and Drug Administration


  • Enzyme Inhibitors
  • Phosphoinositide-3 Kinase Inhibitors
  • Protein Kinase Inhibitors
  • Phosphotransferases
  • Protein-Tyrosine Kinases
  • Receptor Protein-Tyrosine Kinases
  • Protein-Serine-Threonine Kinases