Iminodiacetic-acid-containing 99mTc-marked RGD polypeptide tumor diagnosis drug and preparation method thereof

Abstract

The invention provides a 99mTc complex taking iminodiacetic acid as a difunctional chelating agent. Structure of the complex is shown as a formula (1). The complex has the advantages of simplicity in preparation, low cost, high marking rate, radiochemical purity, target to non-target ratio and tumor uptake value, long residence time and low liver-kidney background. The complex can serve as a novel photographic developer marked by technetium-99m and used for positive tumor diagnosis of intergrin alpha v beta 3 receptor to be applied in the technical field of radioactive medicinal chemistry and clinical nuclear medicine.

Description

technical field [0001] The present invention relates to radiopharmaceuticals for tumor diagnosis, in particular to radiopharmaceuticals containing novel bifunctional linkers for intergrin α v beta 3 RGD polypeptide radiopharmaceutical for receptor positive tumor diagnosis and its preparation method. Background technique [0002] According to the statistics of the World Health Organization (WHO), more than 11 million people suffer from malignant tumors every year in the world, and more than 8 million people die from the disease. The incidence of malignant tumors is also showing a clear upward trend in my country. According to national health statistics, in the past two years, malignant tumors have accounted for the first cause of death among urban residents in my country, and there are about 2.2 million new patients every year. [0003] In recent years, the treatment methods for malignant tumors have been continuously developed. Not only traditional chemotherapy and radioth...

AI Technical Summary

Problems solved by technology

Currently reported RGD cyclic peptide dimer E[c(RGDxk)] 2 (E represents glutamic acid, c represents cyclization, R represents arginine, G represents glycine, D represents aspartic acid, x represents f or y, representing phenylalanine and tyrosine respectively), the two The distance between RGD modules is 6 bonds, because the distance is not long enough, so E[c(RGDxk)] 2 It is difficult for the two RGD motifs of the cell surface to be adjacent to the two integrinα at the same time v beta 3 receptor binding

However, the existing RGD polypeptide dimer imaging agents have a high uptake in non-target organs, especially the intestinal tract, and a high background in the abdomen, which interferes with the imaging effect of abdominal tumors, and high uptake in the liver and kidneys

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