MAGNETIC THALLIUM FOR MRI OF ISCHEMIC HEART DISEASE

EVP 1001是一种独特的细胞内心脏特异性磁共振成像（MRI）试剂，可特异性增强心肌和脉管系统。它将满足目前尚未得到满足的对缺血性心脏病的快速、非侵入性诊断和治疗规划的需求，包括同时评估结构和功能（狭窄、闭塞、室壁运动、心肌灌注和存活心肌与非存活心肌的描绘）。1期临床前研究将增强EVP 1001的心脏安全性，并将确定其药代动力学与MR增强之间的关系。将从这些数据中描述提供有效的心脏和血管MR增强的方案。EVP 1001的独特磁性预期在低剂量下与当前的钆试剂（3-15 μ mol/kg对100-200 μ mol/kg）相比提供增强。第二阶段将评估EVP 1001在心肌缺血模型中的安全性和有效性，为人体试验奠定基础。一旦获得批准，这种造影剂将最佳利用MRI强大的诊断潜力及其快速的技术发展，成为诊断冠状动脉疾病的“一站式商店”，并取代更昂贵和侵入性的检查。拟议的商业应用：这项研究的长期目标是在美国和其他地方注册EVP 1001作为心血管MRI的造影剂。通过结合心脏结构和功能的非侵入性评估，该试剂应提供比超声心动图，核灌注/功能成像和X射线血管造影更经济有效的诊断和治疗计划。此外，其作为血管增强剂的用途可以扩展到身体的其他区域。

EVP 1001 is intended to be a unique, intracellular, cardiac specific magnetic resonance imaging (MRI) agent which specifically enhances both the myocardium and the vasculature. It will satisfy currently-unmet needs for the rapid, non-invasive diagnosis and treatment planning of ischemic heart disease, including simultaneous assessment of both structure and function (stenosis, occlusion, wall motion, myocardial perfusion and delineation of viable versus non-viable myocardium). The preclinical research proposed for Phase 1 will augment the cardiac safety of EVP 1001 and will define the relationship between its pharmacokinetics and its MR enhancement. Does regimens which provide effective cardiac and vascular MR enhancements will be delineated from these data. The unique magnetic properties of EVP 1001 are expected to provide enhancement at low doses compared to current gadolinium agents (3-15 versus 100-200 mumol/kg). Phase 2 will assess the safety and efficacy of EVP 1001 in models of cardiac ischemia, laying the foundation for human trials. When approved, this contrast agent will make optimal use of the powerful diagnostic potential of MRI and its rapid technical evolution, becoming the "one-stop shop" for diagnosis of coronary artery disease and replacing more costly and invasive tests. PROPOSED COMMERCIAL APPLICATIONS: The long-term goal of this research is to register EVP 1001 in the U.S. and elsewhere as a contrast agent for cardiovascular MRI. By combining the noninvasive assessment of both cardiac structure and function, this agent should provide more cost-effective diagnosis and treatment planning than echocardiography, nuclear perfusion/functional imaging, and x-ray angiography. In addition, its use as a vascular enhancement agent may be extended to other regions of the body.