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99mTc labeling galactosed arginyl-glycyl-aspartic acid (RGD) tumor diagnosis medicine and preparation method

A galactose and labeling technology, which is applied in the direction of radioactive carriers, can solve the problem of interfering with the imaging effect of abdominal tumors

Inactive Publication Date: 2013-01-09
安徽筑梦生物科技有限公司
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Problems solved by technology

However, the existing RGD polypeptide dimer imaging agents have more uptake in non-target organs, especially the intestines and other organs, and the background of the abdomen is high, which interferes with the imaging effect of abdominal tumors. It is necessary to invent a new type of RGD polypeptide Dimer imaging agent, by changing the structure of the ligand, further reduces the uptake of the imaging agent in non-target organs such as the intestine, thereby reducing the radioactive background and improving the image quality of tumor imaging

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  • 99mTc labeling galactosed arginyl-glycyl-aspartic acid (RGD) tumor diagnosis medicine and preparation method
  • 99mTc labeling galactosed arginyl-glycyl-aspartic acid (RGD) tumor diagnosis medicine and preparation method
  • 99mTc labeling galactosed arginyl-glycyl-aspartic acid (RGD) tumor diagnosis medicine and preparation method

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Embodiment Construction

[0015] one. Preparation method of galactosylated RGD polypeptide radiopharmaceutical

[0016] 1. materials and equipment

[0017] All chemical reagents were purchased from Sigma / Aldrich, USA without further purification. Galacto-RGD peptide dimer (Galacto-RGD 2 ) was manufactured by Peptides International Corporation (Louisville, KY) in the United States according to conventional processes. HYNIC-Osu was synthesized according to the methods in the literature.

[0018] ESI (electrospray ionization) mass spectrometry data were acquired on a Finnigan LCQ conventional mass spectrometer. 99m TCO 4 - Purchased from Atom Hi-Tech Co., Ltd.

[0019] 2. HPLC (High Performance Liquid Chromatography) Method

[0020] HPLC method 1: using LabAillance chromatographic system, including ultraviolet-visible light detector (wavelength 254 nm) and Zorbax C18 semi-preparative column (column width × column length is 9.4 nm × 250 mm, the pore size of the stationary phase is 100 ?, USA Avai...

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Abstract

The invention relates to an arginyl-glycyl-aspartic acid (RGD) polypeptide radioactive medicine and preparation method thereof for intergrin alpha-v-beta3 receptor positive tumor diagnosis. The medicine is a galactosed RGD cyclic dimer in structure, and the medicine is subjected to a radionuclide 99mTc labeling through a bifunctional chelator hydrazino nicotinamide (HYNIC). The medicine is characterized in that two galactoses are used as a joining chain of the RGD, the uptaking of the medicine in non-target organs of intestinal canal, lungs and the like is reduced, and thereby the image quality of tumor imaging is improved. The radioactive medicine is 99mTc-Galacto-RGD2 and is a colorless transparent liquid injection.

Description

technical field [0001] The present invention relates to radiopharmaceuticals for tumor diagnosis, in particular for intergrin α v beta 3 An RGD polypeptide radiopharmaceutical for the diagnosis of receptor-positive tumors and a preparation method thereof. Background technique [0002] According to the statistics of the World Health Organization (WHO), more than 11 million people are diagnosed with malignant tumors in the world every year, 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 radiotherapy techniques have become more stan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K103/10
Inventor 不公告发明人
Owner 安徽筑梦生物科技有限公司
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