首页> 外国专利> PSMA-TARGETED RADIOPHARMACEUTICAL FOR DIAGNOSING AND TREATING PROSTATE CANCER

PSMA-TARGETED RADIOPHARMACEUTICAL FOR DIAGNOSING AND TREATING PROSTATE CANCER

机译:PSMA靶向放射性药物,用于诊断和治疗前列腺癌

摘要

The present invention relates to a pharmaceutical composition for diagnosing and treating prostate cancer, capable of targeting PSMA, and a compound provided by one aspect of the present invention has a glutamine-urea-lysine compound to which a radioactive metal-coupled chelator is structurally coupled and to which an aryl group that can additionally bind to PSMA protein is coupled. Coupling between the glutamine-urea-lysine compound and the chelator includes a polar spacer so as to serve the role of reducing in vivo nonspecific coupling and exhibit an effect of being rapidly removed from vital organs, but not from prostate cancer. These characteristics lower the radiation exposure, which is caused by a therapeutic radioisotope-coupled compound, to normal tissue and organs, and thus reduce side effects. In addition, a compound that contains a phenyl group having a coupling force with albumin has an increased residence time in the blood, thereby becoming more accumulated in prostate cancer.
机译:本发明涉及用于诊断和治疗能够靶向PSMA的前列腺癌的药物组合物,并且本发明的一个方面提供的化合物具有谷氨酰胺 - 脲酰赖氨酸化合物,放射性金属耦合螯合剂在结构上耦合到其中并且可以另外与PSMA蛋白结合的芳基偶联。谷氨酰胺 - 尿素 - 赖氨酸化合物和螯合剂之间的偶联包括极性间隔物,以便用于减少体内非特异性偶联的作用,并且表现出从重要器官迅速除去的效果,而不是从前列腺癌中脱离。这些特性降低了辐射曝光,这是由治疗性放射性同位素偶联的化合物引起的正常组织和器官引起的,从而减少副作用。另外,含有具有白蛋白的偶联力的苯基的化合物在血液中具有增加的停留时间,从而在前列腺癌中变得更加积累。

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