Ruboxistaurin mesilate hydrate for diabetic retinopathy

Drugs Today (Barc). 2009 Apr;45(4):269-74. doi: 10.1358/dot.2009.45.4.1354195.

Abstract

Diabetic retinopathy remains a major worldwide cause of preventable blindness. The beta isoform of protein kinase C (PKC) may play an important role in the pathogenesis of this disorder. Ruboxistaurin mesylate hydrate is an orally bioavailable, highly-specific inhibitor of PKC beta, which has shown some efficacy in several large, multicenter, randomized clinical trials. The U.S. Food and Drug Administration issued an approvable letter for ruboxistaurin in 2006, but at this time the medication is not available for routine clinical use.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Diabetic Retinopathy / drug therapy*
  • Diabetic Retinopathy / enzymology
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / adverse effects
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use*
  • Humans
  • Indoles / adverse effects
  • Indoles / pharmacology
  • Indoles / therapeutic use*
  • Maleimides / adverse effects
  • Maleimides / pharmacology
  • Maleimides / therapeutic use*
  • Protein Kinase C / antagonists & inhibitors
  • Protein Kinase C beta
  • Randomized Controlled Trials as Topic

Substances

  • Enzyme Inhibitors
  • Indoles
  • Maleimides
  • ruboxistaurin
  • Protein Kinase C
  • Protein Kinase C beta