Clinical safety of the selective PKC-beta inhibitor, ruboxistaurin

Expert Opin Drug Saf. 2006 Nov;5(6):835-45. doi: 10.1517/14740338.5.6.835.


The aim of this manuscript is to report the safety profile of patients treated with ruboxistaurin mesylate (RBX; LY333531), a selective protein kinase C-beta (PKC-beta) inhibitor, for up to 4 years. Data from patients with diabetes (1396 RBX 32 mg/day; 1408 placebo) were combined from 11 placebo-controlled, double-masked studies. The proportion of patients who reported one or more serious adverse events was greater in the placebo group than in the RBX-treated group (23.2 versus 20.8%, respectively). There were 51 deaths (21 RBX; 30 placebo) reported in this patient cohort; none of the deaths was attributed to study drug by the investigators. Common adverse drug reactions (> or = 1/100 - < 1/10 patients) that were reported in the RBX-treated patients were dyspepsia and increased blood creatine phosphokinase. In controlled, randomised clinical trials, RBX had an adverse event profile comparable to placebo, and was well tolerated.

Publication types

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

MeSH terms

  • Humans
  • Indoles / adverse effects*
  • Maleimides / adverse effects*
  • Protein Kinase C / antagonists & inhibitors*
  • Protein Kinase C / metabolism
  • Protein Kinase C beta
  • Protein Kinase Inhibitors / adverse effects*
  • Randomized Controlled Trials as Topic / trends*


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