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EN-100 EN-100 is eNOS Pharmaceuticals' primary drug candidate. EN-100 is an oral, sustained release delivery capsule consisting of statin in combination with L-Arginine in an eNOS Pharmaceuticals' proprietary formulation. eNOS Pharmaceuticals is pursuing the development of EN-100 for three indications: Cardiovascular Applications HMG CoA reductase inhibitors (statins) have been shown to improve endothelium-dependent vasodilation in both coronary and peripheral arteries independent of their lipid lowering effects. This improved vasodilation is likely due to the up-regulation of endothelial nitric oxide synthase (eNOS). eNOS is an enzyme having potent anti-atherogenic properties that include a decrease in leukocyte adhesion, platelet aggregation and vascular smooth muscle cell growth. Enhancement of eNOS production results in increased coronary endothelial NO production that enhances NO-dependent coronary vasodilation and NO-mediated regulation of myocardial oxygen consumption, yielding improved blood flow and increased endothelial function. Prophylactic treatment with EN-100 may reduce coronary events both by improving endothelial function and by decreasing the amount of atherosclerotic plaque in arteries. EN-100 induced increase of eNOS production would result in improved vasodilator response and increased endothelial function. Enhanced vasodilation would increase blood flow to ischemic tissue and, as a consequence, reduce or otherwise limit the tissue injury associated with such cardiovascular diseases as atherosclerosis, myocardial infarction and intermittent claudication. Alzheimer's Disease (AD) Applications Advancing age is closely associated with certain physiologic changes, among them changes in the vascular system including clogging of arteries and hardening and thickening of blood vessel walls. Along with this increase in vascular stenosis is a decrease in cerebral blood flow. Daily treatment with EN-100 would maintain cerebral blood flow at higher levels and counterbalance the vascular stenosis associated with the decreasing cognitive status found in Alzheimer's disease. Similarly, daily treatment of early stage AD patients with eNOS Pharmaceuticals' EN-100 product could slow the progression of the disease by maintaining blood vessel elasticity, thereby delaying vascular stenosis. Stroke Applications Ischemic stroke results in significant reduction in blood supply to brain tissues, starving them of oxygen and nutrients and causing impairment in neuronal electrical functioning. Up-regulation of eNOS correlates to increased cerebral blood flow (CBF). This increase in CBF restores oxygen and nutrients to brain cells, allowing them to survive the stroke event. Recovery of these cells to electrical functionality results in improved patient outcome after stroke. The benefits of daily EN-100 treatment extend to patients in high-risk categories for stroke, to TIA patients for improved outcomes and higher quality of life, and to stroke survivors for reduced risk of severe tissue injury in subsequent stroke events. Prophylactic treatment with EN-100 prior to undergoing various elective surgeries associated with high stroke risk could dramatically reduce the severity of tissue injury in a subsequent stroke. |
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to improve vascular function, thereby relieving vascular insufficiency and effectively treating various cardiovascular diseases;