Optimalisering: Novel drug candidates for Chronic Obstructive Pulmonary Disease treatment

The primary objective of this project was to produce a First-in-Class drug candidate for treatment of Chronic Obstructive Pulmonary Disease (COPD). COPD is estimated to become the third leading death cause worldwide by 2030. COPD refers to a group of chronic respiratory diseases, which are particularly debilitating for the patients. Unfortunately existing therapies can at best alleviate the symptoms. We propose to target the underlying pathological mechanisms for a beneficial treatment that should have fewer side effects. Drug discovery is a demanding endeavour, both in terms of time and money. During the last years, we have worked to obtain results to reach our final goal, ie finding a new treatment for KOLS, but also and especially to attract investment in our idea so that we can pursue it later. We are very excited about our progresses and our main results are: - We have several stable, soluble strong inhibitors for a protein called Proteinase 3 that is our target for medicinal treatment of COPD. These are our drug candidates - We know that PR3 is an important target for COPD. - With the help of Vestlandets Innovasjonsselskap AS (VIS) we have developed a business model and a strategy for IP rights protection.

The molecules we found are promising candidates for treatment against lung inflammation and COPD.

The primary objective of this project is to produce a First-in-Class drug candidate for treatment of Chronic Obstructive Pulmonary Disease (COPD) targeting the underlying pathological processes. This will serve our secondary objective; finding industrial partners for commercialization of our product. COPD refers to a group of chronic respiratory diseases with debilitating long-term effects and is estimated to become the third leading death cause worldwide by 2030. The COPD market is projected to reach a value of $15.6 billion by 2019. There is no cure for COPD; the existing therapies involving bronchodilators and corticosteroids can at best alleviate the symptoms. We instead propose to target the underlying pathological processes for a beneficial treatment with less side effects and clear socio-economic benefits. We have identified eleven novel synthetic drug-like inhibitors of Proteinase 3, a protease considered a drug target for COPD. We identified the lead compounds from high-throughput screening and showed that the two most promising candidates have nanomolar IC50s. Our proof-of-principle analysis will address the most challenging aspects for bringing our concept to a proof-of-concept stage: lead optimization and target validation. Our team consists of medicinal chemists, pulmonary clinicians and researchers as well as toxicologists and molecular biologists. There is an unmet clinical need for novel anti-inflammatory therapies associated with COPD. This is clearly reflected in drug development directions in the pharmaceutical industry during the last 20 years, however with an extremely low rate of First-in-Class drugs approved for COPD. To our knowledge none of these companies are working to gain a market share for our target. Pharmaceutical companies with COPD in their pipelines will be target customers for our technology. We plan to commercialize our product by out-licensing and we have been discussing the venture already with major players in the industry.