Compound targeting prostate specific membrane antigen, and application of compound

Abstract

The invention provides an NOTA-Bi-PSMA compound or a salt of the NOTA-Bi-PSMA compound, a radiolabeled complex of the NOTA-Bi-PSMA compound or the salt of the NOTA-Bi-PSMA compound, and an applicationof the NOTA-Bi-PSMA compound or the salt of the NOTA-Bi-PSMA compound and the radiolabeled complex in the preparation of a product for detecting and / or treating cells and / or tissues expressing a prostate specific membrane antigen. The NOTA-Bi-PSMA compound or the salt of the NOTA-Bi-PSMA compound can be used as a precursor compound of a PSMA targeted tracing or treatment drug. The radiolabeled complex is high in binding force with PSMA, high in sensitivity, low in non-specific tissue uptake, high in tumor and background uptake value ratio and high in imaging definition.

Description

Technical field[0001]The invention belongs to the field of radiopharmaceutical labeling, and specifically relates to compounds targeting prostate specific membrane antigens and applications thereof.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 and99mTc-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 in PSAIt is often negative in patients with <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 imaging18F-FDG PET / CT has superior detection ability in most malignant tumors, but for prostate cancer, this imaging has low sensitivity in detecting high and moderately differentiated prostate cancer, and has limited va...

AI Technical Summary

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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