PI3Kgamma inhibition: towards an 'aspirin of the 21st century'?

Nat Rev Drug Discov. 2006 Nov;5(11):903-18. doi: 10.1038/nrd2145. Epub 2006 Oct 13.


Class IB phosphatidylinositol 3-kinase p110gamma (PI3Kgamma) has gained increasing attention as a promising drug target for the treatment of inflammatory disease. Extensive target-validation data are available, which are derived from studies using both pharmacological and genetic tools. More recent findings have uncovered further therapeutic applications for PI3Kgamma inhibitors, opening up potentially huge opportunities for these drugs. Several companies have been pursuing small-molecule PI3Kgamma inhibitor projects, but none of them has progressed to the clinic yet. Here, we discuss the insights gained so far and the main challenges that are emerging on the path to developing PI3Kgamma inhibitors for the treatment of human disease.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Aspirin / pharmacology*
  • Chemokines / physiology
  • Enzyme Inhibitors / pharmacology*
  • Hematopoiesis / drug effects
  • Humans
  • Mice
  • Phosphoinositide-3 Kinase Inhibitors*
  • Receptors, Chemokine / drug effects
  • Receptors, Chemokine / physiology


  • Anti-Inflammatory Agents, Non-Steroidal
  • Chemokines
  • Enzyme Inhibitors
  • Phosphoinositide-3 Kinase Inhibitors
  • Receptors, Chemokine
  • Aspirin