A radiolabeled polypeptide complex and its preparation method and application

Abstract

The invention provides an RGD polypeptide coordination complex of a radioactive nuclide label. According to the structure of the coordination complex, the radioactive nuclide is selected from 64Cu, 68Ga, 111In, 62Cu, 67Cu, 67Ga, 86Y, 89Zr or 18F; the ligand is a ligand compound containing an RGD structure, which is shown in a formula (I). The coordination complex has stronger ligand stability and high target / non-target ratio, and the appetency of the ligand with integrin AlphavBeta3 is stronger. The invention further provides a preparation method of the coordination complex, and an application of the coordination complex in preparing tumor developers.

Description

technical field [0001] The invention relates to a radioactive complex, its preparation method and the application of the complex as a tumor imaging agent. Background technique [0002] According to the current trend of cancer incidence, the incidence of cancer worldwide will increase by 50% in 2020, and the number of new cancer patients worldwide will reach 15 million each year (the World Cancer Report recently published by the World Health Organization (WHO). Early detection and early treatment are the most effective ways to reduce cancer mortality. The implementation of a screening system for bowel cancer, cervical cancer, breast cancer, etc. can reduce the number of cancer deaths worldwide by one-third. Currently in developing countries, 80% of cancer patients are only discovered at the advanced stage of the disease. [0003] Although the exact mechanism of cancer development is still unclear, if the cancer can be diagnosed at an early stage and treated with surgery, ra...

AI Technical Summary

Problems solved by technology

US and MRI techniques can be used for anatomical analysis of solid tumors, but the disadvantage of these techniques is that they cannot detect biochemical changes in tumor tissue at the molecular level, because MRI and CT techniques require tumor tissue to contain many contrast agents to contrast with normal tissue. In strong contrast, another disadvantage of these techniques is their poor specificity and sensitivity for high-incidence tumors (such as breast, gallbladder, lung, and prostate cancers), so we urgently need to develop a new tumor Specific radiotracers, which can not only be used for early diagnosis of tumors, but also can monitor tumor growth and tumor response to drug treatment

[0006] From the perspective of ligand selection, the biological activity of the monomer is low, manifested as low receptor affinity, low tumor uptake, and high imaging background, which affect the final imaging quality of the tracer

The biological properties of dimers, tetramers and multimers are getting better and better, but the cost of synthesis will increase sharply, so it is most appropriate to choose dimers after comprehensive consideration

[0008] At present, copper-64 and gallium-68 are metal ions, which can generate labeled complexes through a simple coordination reaction. 18 F-labeled substances are prepared through a complex labeling process using an automatic synthesizer, which is time-consuming and expensive

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