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PSMA- PSMA-targeting radiopharmaceuticals for diagnosis and therapy of prostate cancer

机译:PSMA-靶向PSMA的放射性药物用于前列腺癌的诊断和治疗

摘要

The present invention relates to a pharmaceutical composition for diagnosing and treating prostate cancer, which is capable of PSMA-target. According to the structure of the compound provided by an embodiment of the present invention, chelator combined with radioactive metal is combined in a glutamine-urea-lysine compound and an aryl group is combined to be able to have an additional binding with PSMA protein. A bonding between the glutamine-urea-lysine compound and the chelator is formed in a polar spacer to reduce a nonspecific binding inside a living body, and has an effect of quickly removing the nonspecific binding from major organs besides prostate cancer. The feature of the present invention has advantages of lowering radiation exposure to normal tissues and organs caused by a compound bound to radioisotopes for treatment and thus, reducing side effects. In addition, the compound containing a phenyl group having a binding force to albumin has an effect of being accumulated more in prostate cancer by increasing residence time in blood.
机译:本发明涉及一种能够以PSMA为靶标的用于诊断和治疗前列腺癌的药物组合物。根据本发明的实施方案提供的化合物的结构,将与放射性金属结合的螯合剂结合在谷氨酰胺-尿素-赖氨酸化合物中,并且结合芳基以能够与PSMA蛋白具有额外的结合。谷氨酰胺-尿素-赖氨酸化合物与螯合剂之间的键合形成在极性间隔物中,以减少活体内的非特异性结合,并且具有快速去除前列腺癌以外的主要器官的非特异性结合的作用。本发明的特征具有降低由结合到放射性同位素上进行治疗的化合物引起的对正常组织和器官的辐射暴露的优点,并因此减少了副作用。另外,含有与白蛋白具有结合力的苯基的化合物具有通过增加在血液中的滞留时间而在前列腺癌中更加蓄积的作用。

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