A compound targeting prostate specific membrane antigen and its application

Abstract

The present invention provides a NOTA-Bi-PSMA compound or a salt thereof, a radiolabeled complex thereof and its application in the preparation of a product for detecting and / or treating cells and / or tissues expressing prostate specific membrane antigen. The NOTA-Bi-PSMA compound or a salt thereof can be used as a precursor compound of PSMA targeted tracer or therapeutic drug; the radiolabeled complex has high binding force to PSMA, high sensitivity, low non-specific tissue uptake, tumor The ratio of the uptake value to the background is high, and the imaging resolution is high.

Description

technical field [0001] The invention belongs to the field of radiopharmaceutical labeling, in particular to a compound targeting prostate specific membrane antigen and its application. Background technique [0002] Worldwide, the incidence of prostate cancer ranks second among all malignant tumors in men. At present, the diagnosis and staging of prostate cancer mostly rely on CT, MRI and 99m Tc-MDP bone imaging, but these methods have shortcomings in whole body tumor imaging, such as insufficient sensitivity or inability to detect whole body tumors, and these imaging techniques are often negative in patients with PSA<10ng / ml. In recent years, PET has also begun to be used for the diagnosis and staging of the prostate. Although the most widely used clinical imaging 18 F-FDG PET / CT has superior detection ability in most malignant tumors, but for prostate cancer, the imaging has low sensitivity for the detection of well-differentiated prostate cancer, and has limited valu...

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Problems solved by technology

[0014] The second object of the present invention is to provide a radiolabeled complex, which includes a radionuclide and the above-mentioned NOTA-Bi-PSMA compound or a salt thereof, and the radiolabeled complex is in vivo Good pharmacokinetics, high tumor-to-background uptake ratio after 1-2 hours of injection of the radiolabeled complex, high binding to PSMA, high uptake by PSMA-expressed tumors, low PSA Cancer cells and / or tissues can be accurately detected under certain circumstances, and the ratio of tumor to background uptake value in imaging is high, and the definition is high, which can solve the problem of poor binding force, low sensitivity, and tumor Problems such as low ratio to background uptake

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