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A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Clinical safety of the selective PKC-beta inhibitor, ruboxistaurin
Janet B McGill1, George L King, Paul H Berg
1Washington University School of Medicine, 660 S. Euclid, Campus Box 8127, St. Louis, MO 63110, USA. jmcgill@im.wustl.edu
Abstract:
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.
Insights
Ruboxistaurin mesylate (RBX), a protein kinase C-beta inhibitor, demonstrated a comparable safety profile to placebo in long-term diabetes patient trials. Serious adverse events were less frequent in patients receiving RBX.
Area of Science:
- Pharmacology
- Clinical Trials
- Diabetology
Background:
- Protein kinase C-beta (PKC-beta) inhibitors are investigated for diabetic complications.
- Ruboxistaurin mesylate (RBX; LY333531) is a selective PKC-beta inhibitor.
- Long-term safety data for RBX in diabetic patients is crucial.
Purpose of the Study:
- To report the safety profile of ruboxistaurin mesylate (RBX) in patients with diabetes.
- To evaluate adverse events and tolerability of RBX over a period of up to 4 years.
- To compare the safety of RBX with placebo in a large patient cohort.
Main Methods:
- Combined data from 11 placebo-controlled, double-masked studies.
- Inclusion of 1396 patients treated with RBX (32 mg/day) and 1408 patients on placebo.
- Systematic collection and analysis of serious adverse events and drug reactions.
Main Results:
- The incidence of serious adverse events was lower in the RBX group (20.8%) compared to placebo (23.2%).
- No deaths were attributed to study drug by investigators.
- Common adverse drug reactions in the RBX group included dyspepsia and elevated creatine phosphokinase.
Conclusions:
- Ruboxistaurin mesylate (RBX) exhibits an adverse event profile comparable to placebo in diabetic patients.
- RBX was well tolerated in controlled, randomized clinical trials.
- The long-term safety data supports the tolerability of RBX in this patient population.
