Inhibit Blood clots block the blood supply to vital parts of the body, including the brain and the heart.
About
Novel Inhibitors of Thrombotic Clot Formation for Pre-hospital Treatment of Myocardial Infarction The single most common cause of morbidity and mortality in the United States is arterial thrombosis, which is the formation of blood clots in the major blood vessels that block the blood supply to vital parts of the body, including the brain and the heart. These clots form because the body perceives that the blood vessels are injured, either due to atherosclerotic plaques or cardiac interventions such as angioplasty or stent placements. The clots themselves are composed of fibrin and platelets, which are small cellular fragments in the blood that aggregate by binding a protein called fibrinogen. It is thus important to identify compounds that inhibit platelets from forming these clots. Our scientists identified novel small compounds that specifically block the platelet αIIbβ3 receptor through a novel mechanism that may have therapeutic benefits over existing agents used for this purpose. In addition, they are formulating the lead compounds so that they can be given by autoinjector immediately after the onset of symptoms of a heart attack, the point at which there is the greatest opportunity for benefit. This blockage inhibits or reduces the binding of platelets to fibrinogen and the aggregation of platelets, thus potentially preventing the formation of clots. In addition our scientists have analyzed the structural interaction to better elucidate the mechanism of action. They have also collected in vivo data that supports effective anti-thrombotic effects in murine models. Area of Application Pre-hospital treatment of myocardial infarction Stage of Development In vivo studies demonstrated anti-thrombotic effects in two different mouse models. Pharmokinetic and pharmacodynamic studies in rats and non-human primates are ongoing. Pre-IND dose ranging toxicology studies in non-human primates are completed and IND-enabling toxicology studies are under development. Large scale manufacturing and salt selection are ongoing in preparation for formulation of material for IND-enabling studies. Lead Inventor Barry Coller Patent Information Issued US Patents 8,173,661; 9,073,945; 9,066,948 S. patent application 14/372,488 and foreign filings pending