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NicOx S.A. (NYSE Euronext Paris: COX) today announced that preclinical results for NCX 226, a novel nitric oxide (NO)-donating new molecular entity (NME), were presented at the annual European League Against Rheumatism (EULAR) congress in London (May 25–28). NCX 226 is a prototype compound developed by NicOx’s Research team in a program targeting pulmonary arterial hypertension (PAH).
NCX 226 has been designed to release both bosentan (an endothelin receptor antagonist commonly used in the treatment of PAH) and NO. The EULAR presentation concerned the evaluation of NCX 226, in comparison with bosentan, in a preclinical model of pulmonary fibrosis induced by bleomycin. Pulmonary fibrosis is a condition commonly associated with PAH, in which lung tissue gradually becomes thickened, stiff and scarred. Results demonstrate that NCX 226 and bosentan counteract lung inflammation and airway stiffness in this preclinical model. NCX 226 shows improved efficacy over bosentan in preventing bleomycin-induced airway stiffness and in reducing key inflammatory parameters, such as leukocyte infiltration, secretion of the profibrotic cytokine TGF-beta and oxidative stress markers.
PAH is an orphan condition defined by a progressive and sustained elevation of pulmonary vascular resistance (resistance of the lungs vasculature which must be overcome so that blood can flow through the circulatory system). Recent findings on its pathological mechanism recognise the role played by NO in endothelium dysfunction (disorder of the cells lining the inside of blood vessels) and pulmonary vascular resistance.
Patients suffering from PAH may experience a number of symptoms, including breathlessness on exertion and chest pain. In advanced stages of the disease, symptoms may occur during minimal activity or at rest. Current treatment options include oral endothelin (ET-1) receptor antagonists (such as bosentan) and phosphodiesterase (PDE5) inhibitors, as well as inhaled prostacyclins. Despite these options, there is still a high medical need in PAH, which can lead to heart failure and necessitate lung transplants.
Further preclinical results obtained with NCX 226 in a reference PAH preclinical model will be presented at the 2011 World Congress on Inflammation, which will be held in Paris from June 25 to 29. NicOx is currently looking for potential partners for this research programme.