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Dual TACE/MMP inhibitors as candidate therapies for asthma and COPD Asthma is now thought to affect 155 million people worldwide. In the United States alone there has been a two-fold increase in the number of cases of asthma driving market values up as high as $8 billion worldwide. A large number of drugs are available to clinicians, although most of these treat respiratory disfunction associated with asthma rather than underlying immunological causes of this disease. This in part explains why up to 15% of patients suffer from uncontrollable disease symptoms, increasing the demand for novel therapies that possess new modes of action. Immunomodulatory drugs offer promise for the treatment of asthma as well as COPD. COPD, including chronic obstructive bronchitis and emphysema, affects 600 million people world-wide, with some three million dying from the disease each year representing a global market of US$2.8 billion. LeadDiscovery in collaboration with field-leading researcher, Peter Barnes, have analyzed emerging anti-inflammatory targets for airway disease (click here for access). Two key therapeutic classes discussed were metaloproteinase (MMP) inhibitors and TNF-alpha blockers. It is of interest therefore that Novartis researchers have recently published data describing the efficacy of two new inhibitors of TACE/MMPs (PKF242-484, PKF241-466) in models of airway inflammation. At low nanomolar concentrations PKF242-484 and PKF241-466 were broad spectrum inhibitors of MMP isoforms and both compounds also inhibited TNF-alpha release from activated human peripheral blood mononuclear cells. PKF242-484 and PKF241-466 had beneficial effects in two different murine models of acute lung inflammation in vivo, preventing the influx of inflammatory cells and subsequent release of myeloperoxidase and elastase into the airways following LPS challenge or acute allergic lung inflammation. PKF242-484 and PKF241-466 could therefore have beneficial effects in airway inflammatory conditions such as asthma and COPD. Link to journal abstract:
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