99mtc-labeled RGD (arginine-glycine-aspartic acid) polypeptide tumor diagnosis medicament and preparation method thereof

A 99mtc, 99mtc-hynic-k technology, applied in the direction of radioactive carriers, can solve the problem of accelerating the metabolism of imaging agents

Inactive Publication Date: 2012-07-11
安徽筑梦生物科技有限公司
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  • Abstract
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Problems solved by technology

However, the existing RGD polypeptide dimer imaging agents still have certain deficiencies in the metabolism of non-target organs. It is necessary to invent new RGD polypeptide dimer imaging agents to further accelerate imaging by changing the structure of the ligand. The metabolic rate of the drug in non-target organs such as lung, liver and kidney, thereby reducing the radioactive background and improving the image quality of tumor imaging

Method used

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  • 99mtc-labeled RGD (arginine-glycine-aspartic acid) polypeptide tumor diagnosis medicament and preparation method thereof
  • 99mtc-labeled RGD (arginine-glycine-aspartic acid) polypeptide tumor diagnosis medicament and preparation method thereof
  • 99mtc-labeled RGD (arginine-glycine-aspartic acid) polypeptide tumor diagnosis medicament and preparation method thereof

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Experimental program
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Embodiment Construction

[0018] One. The preparation method of RGD polypeptide radiopharmaceutical

[0019] 1. Materials and Equipment

[0020] The required chemicals were purchased from Sigma / Aldrich, USA and used without further purification. Boc-Lys(nicotinoyl)-OH and Lys(Boc) 2 -OSu was purchased from Bachem Biosciences, USA. RGD cyclic peptide, E[c(RGDfK)] 2 (RGD 2 ), G 3 -E[G 3 -c(RGDfK)] 2 (3G-RGD 2 ) and PEG 4 -E[PEG 4 -c(RGDfK)] 2 (3P-RGD 2 ) was manufactured by Peptides International Company (Louisville, KY) of the United States according to conventional processes.

[0021] The NMR (nuclear magnetic resonance) spectrum data is recorded by a 300MHz Bruzker ARX FT nuclear magnetic resonance spectrometer, and the displayed spectrum data is the chemical shift value (ppm) referenced to TMS (trimethylsilyl). ESI (electrospray ionization) mass spectrometry data were collected on a Finnigan LCQ conventional mass spectrometer. 99m TCO 4 - Purchased from Atom Hi-Tech Co., Ltd.

[0022...

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Abstract

The invention relates to three RGD (Arginine-Glycine-Aspartic acid) polypeptide radioactive medicaments for positive tumor diagnosis of an intergrinalphavbeta3 receptor and preparation methods thereof. The three RGD polypeptide radioactive medicaments are structurally RGD annular dipolymers, and radioactive nuclein 99mTc labeling is performed through a dual-functional chelating agent. The medicaments are mainly characterized in that: a [K(NIC)] structure which is connected with RGD is used for replacing the conventional 99mTc-labeled synergistic ligand, i.e., trisodium salt of tri(m-sulfonphenyl) phosphine (TPPTS), so that the molecular weight of a medicament structure is reduced, and the metabolism velocity of a radioactive medicament in a non-target organ is increased. The three radioactive medicaments include 99mTc-HYNIC-K(NIC)-RGD2, 99mTc-HYNIC-K(NIC)-3G-RGD2 and 99mTc-HYNIC-K(NIC)-3P-RGD2, and are colorless and transparent liquid injections.

Description

technical field [0001] The present invention relates to radiopharmaceuticals for tumor diagnosis, in particular to intergrin alpha v beta 3 Three RGD polypeptide radiopharmaceuticals for the diagnosis of receptor-positive tumors and their preparation methods. 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 radiotherapy techniques have become more standar...

Claims

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Application Information

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