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Chemical structure and preparation method of 99mTc-labeled RGD polypeptide trimer tumor imaging agent

A peptide trimer, 99mtc-4p-rgd3 technology, applied in the direction of radioactive carriers, can solve the problems of high radioactive background, interference with the imaging effect of tumor parts in abdominal organs, and high uptake value of non-target organs

Active Publication Date: 2015-06-03
刘丽 +1
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Problems solved by technology

[0007] Existing research results suggest that technetium-labeled RGD polypeptide dimer ( 99m Tc-3P-RGD 2 ) and technetium-labeled RGD galactose dimer ( 99m Tc-Galacto-RGD 2 ) imaging agent and integrin α in malignant tumors v beta 3 The expression has high affinity, and can be used as an economical drug for tumor diagnosis by SPECT or SPECT / CT imaging. However, the uptake of these two drugs in non-target organs in animals is relatively high, especially in abdominal organs. bottom, which can interfere with the imaging effect of tumor sites in abdominal organs

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  • Chemical structure and preparation method of 99mTc-labeled RGD polypeptide trimer tumor imaging agent
  • Chemical structure and preparation method of 99mTc-labeled RGD polypeptide trimer tumor imaging agent
  • Chemical structure and preparation method of 99mTc-labeled RGD polypeptide trimer tumor imaging agent

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Embodiment Construction

[0016] RGD polypeptide trimer single-photon radiopharmaceutical preparation method:

[0017] 1. Materials and instruments: Purified chemical reagents were purchased from Sigma / Aldrich Company in the United States (St.Louis, MO). RGD polypeptide trimer (4P-RGD 3 ) is specially customized to Peptides International, Inc of the United States (Louisville, KY). HYNIC-Osu was formulated according to the method described in the literature. MALDI (matrix-assisted laser desorption ionization) mass spectrometry data were collected by Applied Biosystems Voyager DE PRO mass spectrometer (Framingham, MA). 99m TCO 4 - Obtained through drug dealers.

[0018] 2. HPLC (high performance liquid chromatography) analysis method:

[0019] 1. Method 1: the semi-preparative high-performance liquid chromatography (HPLC) analysis method used is equipped with the LabAlliance high-performance liquid chromatography analysis system and the Zorbax C18 semi-preparative chromatographic column (9.4nm ×25...

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Abstract

The invention relates to a chemical structure and a preparation method of a tumor imaging agent, and in particular relates to a single photon emission computed tomography (SPECT) technetium (99mTc)-labeled RGD polypeptide trimer medicine, namely 99mTc-4P-RGD3. The tumor imaging medicine is combined with an integrin alphavbeta3 in a ligand mode so as to achieve an application of imaging a tumor part. The preparation method comprises the following implementing steps: linking HYNIC-Osu to 4P-RGD3 so as to obtain a ligand HYNIC-4P-RGD3, and chelating the HYNIC in the ligand with 99mTc so as to obtain the 99mTc-4P-RGD3 tumor imaging agent. A research on animal in-vivo distribution and a tumor imaging step proves that the tumor imaging agent is relatively high in tumor uptake and lower in background uptake to normal organs in a whole body, and the definition of tumor image of the whole body is improved; a drug metabolism experimental step shows that the 99mTc-4P-RGD3, after metabolized in an animal body, can be still discharged out of the body in a prototype mode. The technetium-labeled integrin alphavbeta3 tumor imaging agent (99mTc-4P-RGD3) prepared by the technical means disclosed by the invention can be used for solving a problem of high background uptake of other technetium-labeled RGD medicines in animal body, so that the technetium-labeled RGD medicine is more suitable for the assessment of tumors in whole body.

Description

【Technical field】 [0001] The present invention relates to the chemical structure and preparation method of a tumor imaging agent in single photon emission computed tomography (single photon emission computed tomography, SPECT), in particular to a technetium ( 99m Tc) labeled RGD (arginine-glycine-aspartic acid, Arg-Gly-Asp) polypeptide trimer drugs: 99m Tc-4P-RGD 3 , the drug can pass through the integrin (integrin) α in the tumor after intravenous injection v beta 3 Expressed, in a ligand manner, with integrin alpha v beta 3 The receptors combine with each other to achieve the purpose of imaging the tumor site. 【Background technique】 [0002] According to the [World Cancer Report] released by the World Health Organization (WHO), in recent years, the number of cancer patients in China has been 3.065 million, accounting for about 1 / 5 of the global incidence, and the number of cancer deaths is 2.205 million, accounting for about 20% of the global cancer deaths. 1 / 4, maki...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K103/10
Inventor 许百灵刘丽方纬
Owner 刘丽
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