Aurora kinase inhibition: a new light in the sky?

J Med Chem. 2015 Jul 9;58(13):5186-8. doi: 10.1021/acs.jmedchem.5b00918. Epub 2015 Jun 25.

Abstract

The quest for potent and selective small molecule inhibitors of the Aurora kinases has been long and resource intensive with multiple agents progressed to the clinic. To definitively explore the potential for clinical efficacy at well-tolerated dosing schedules requires a well-characterized, selective inhibitor with pharmacokinetic properties, flexible dosing regimen, and suite of target engagement biomarkers suitable for clinical use. AMG900 is a promising opportunity to definitively test the clinical benefit of dual Aurora kinase A and B inhibition.

MeSH terms

  • Aurora Kinases / antagonists & inhibitors*
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Phthalazines / pharmacology*
  • Protein Kinase Inhibitors / pharmacology*

Substances

  • N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine
  • Phthalazines
  • Protein Kinase Inhibitors
  • Aurora Kinases