SBIR Phase II: Development of Agents to Promote Cellular Ga-67 (Gallium-67) Uptake

这个小企业创新研究第二阶段项目的重点是开发使用镓67选择性增强肿瘤成像的新药剂。硝苯地平的光降解产物硝西平已被发现选择性地增强肿瘤细胞对Ga67的摄取。亚硝西平的一种特定衍生物对放射性显像剂具有更好的选择性摄取。该项目将合成和测试其他亚硝西平的衍生物，并使用这些络合剂在动物模型中确定Ga67的摄取效果。这项技术的商业应用是在诊断成像领域。由于Ga67对肿瘤细胞的选择性很差，目前在肿瘤成像中的应用非常有限。相对于正常细胞，肿瘤细胞摄取的增强将扩大可以有效成像的肿瘤类型，并可能取代使用放射性氟化糖进行的更昂贵、更复杂的PET扫描成像。

This Small Business Innovation Research Phase II project focuses on the development of new pharmaceutical agents to selectively enhance tumor imaging using gallium 67. A photo-degradation product of nifedipine, nitrosipine, has been found to selectively enhance the uptake of Ga67 by tumor cells. A specific derivative of nitrosipine has an even better selective uptake of the radioactive imaging agent. This project will synthesize and test other nitrosipine derivatives and determine the efficacy of Ga67 uptake in animal models using these complexing agents.The commercial application of this technology is in the area of diagnostic imaging. The use of Ga67 in tumor imaging is currently very limited due to poor selectivity of the agent for tumor cells. Enhanced uptake in tumor cells relative to normal cells would expand the types of tumors that could be effectively imaged and possibly replace the more costly and complex PET scan imaging using radioactive fluorinated sugars.