Small-molecule kinase inhibitors: an analysis of FDA-approved drugs

Drug Discov Today. 2016 Jan;21(1):5-10. doi: 10.1016/j.drudis.2015.07.008. Epub 2015 Jul 23.


Small-molecule kinase inhibitors (SMKIs), 28 of which are approved by the US Food and Drug Administration (FDA), have been actively pursued as promising targeted therapeutics. Here, we assess the key structural and physicochemical properties, target selectivity and mechanism of function, and therapeutic indications of these approved inhibitors. Our analysis showed that >30% of approved SMKIs have a molecule weight (MW) exceeding 500 and all have a total ring count of between three and five. The assumption that type II inhibitors tend to be more selective than type I inhibitors has been proved to be unreliable. Although previous SMKI research was concentrated on tyrosine kinase inhibitors for cancer treatment, recent progress indicates diversification of SMKI research in terms of new targets, mechanistic types, and therapeutic indications.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Approval / methods
  • Drugs, Investigational / therapeutic use*
  • Humans
  • Molecular Weight
  • Protein Kinase Inhibitors / therapeutic use*
  • United States
  • United States Food and Drug Administration


  • Drugs, Investigational
  • Protein Kinase Inhibitors