Neutrophil elastase inhibitor POL6014
POL6014 is a neutrophil elastase inhibitor that can be applied by inhalation to treat chronic obstructive pulmonary disease (COPD) and other pulmonary diseases. COPD is a complex disease with chronic bronchitis and inflammation resulting in destruction of the lung tissue which is essential for uptake of oxygen in the lung (emphysema). Characteristic of COPD is the chronic narrowing of the airways (bronchi) due to inflammatory and remodeling processes. This leads to a limitation of the airflow to and from the lungs causing shortness of breath and insufficient uptake of oxygen. In contrast to asthma, the limitation of airflow is poorly reversible and progressively worsens the destruction of lung tissue and thus the symptoms of COPD over time.
In 1997 the World Health Organization (WHO) and the National Institutes of Health (NIH) have initiated the initiative called GOLD (Global Initiative for Chronic Obstructive Lung Disease) for an optimized worldwide approach of diagnosis and treatment of COPD. A study published in 2007 in Salzburg (Austria) showed that approximately a quarter of the examined people above forty years of age suffer from COPD. In the USA, COPD is the fourth largest cause of death and affects 24 million people, half of them undiagnosed. COPD is one of the few life threatening chronic diseases with increasing incidence and prevalence.
Preclinical pharmacological studies have shown that POL6014 inhibits the aggressive, tissue degrading enzyme neutrophil elastase in a highly potent, selective and reversible manner. After local application to the lungs by inhalation POL6014 reaches high concentrations in the lung while the systemic exposure remains low, thus reducing the risk of side-effects. Exploratory toxicology studies suggest that POL6014 is well tolerated when chronically inhaled as an aerosol. POL6014 is ready to enter preclinical development.
