The NCX 4016 is significantly more effective than aspirin and placebo at preventing platelet activation induced by acute hyperglycemia in diabetic patients, according to results from a NicOx S.A. phase IIa study announced here.

Increased platelet activation is a feature of diabetes and contributes to the high incidence of cardiovascular events, which exert the greatest impact in terms of the number of deaths and reduced quality of life of diabetes patients. NCX 4016 is a novel antithrombotic and vascular anti-inflammatory agent, which is being developed by NicOx for the treatment of peripheral arterial obstructive disease (PAOD) and other cardiovascular related disorders.

This prospective, double-blind, randomized trial, was conducted at the Department of Internal Medicine of the University of Perugia and involved 40 type II diabetes patients, who were randomized between four parallel groups and treated for 14 days with: NCX 4016 (800 mg bid), aspirin (100 mg od), the combination of NCX 4016 and aspirin or placebo.

These results suggest NCX 4016 may be more effective than aspirin at inhibiting platelet activation in diabetic patients and may have relevance for the prevention of cardiovascular complications in diabetes.

Patients with diabetes typically suffer from accelerated arteriosclerosis (hardening of the arteries) and increased risk of cardiovascular complications, such as heart attack and stroke. It is known that acute hyperglycemia (abnormally high blood-sugar levels caused by diabetes) can strongly enhance platelet activation and clot formation and precipitate a cardiovascular event. Current guidelines recommend diabetes patients should be treated with low-dose aspirin to reduce the activation of platelets during clot formation and reduce the risk of major cardiovascular complications.

Professor Paolo Gresele, Professor of Internal Medicine at the University of Perugia and Principal Investigator on the trial, commented: " Clinical guidelines recommend the use of aspirin in diabetes patients, however, recent research suggests that aspirin may have a reduced effectiveness in these patients, which may partly explain the continued poor outcome of the disease. Research has shown that hyperglycemia can induce platelet activation through a mechanism involving shear stress, which is know to be resistant to aspirin inhibition. These results are highly encouraging because they indicate that NCX 4016 may be more effective than aspirin at preventing cardiovascular events in diabetic patients. This increased activity of NCX 4016 compared to aspirin may be due to a synergism between NO-donation and COX-1 inhibition."