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18F marked affinity compound and preparation method and application thereof

A compound and labeling technology, applied in the fields of radiopharmaceuticals and nuclear medicine, can solve the problems of low tumor sensitivity, complex preparation methods, and large liver toxic and side effects, and achieve the effects of high radiochemical purity, short residence time, and small toxic and side effects.

Active Publication Date: 2016-08-24
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, on the one hand, tumors are 18 The uptake of F-FBEM-(ZHER2:342) is low, which leads to low tumor imaging sensitivity; on the other hand, the liver is sensitive to the above 18 The uptake of F-FBEM-(ZHER2:342) is higher, which leads to greater toxicity to the liver; in addition, the above 18 The preparation method of F-FBEM-(ZHER2:342) is complicated, which limits its clinical application to a certain extent

Method used

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  • 18F marked affinity compound and preparation method and application thereof
  • 18F marked affinity compound and preparation method and application thereof

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Embodiment 1

[0059] This embodiment is used in the kit for preparing the compound shown in formula (I), and its reagent comprises: the compound shown in 25nmol formula (II), 12nmol aluminum trichloride, 0.5mol / L, the acetic acid- Sodium acetate buffer;

[0060] The preparation method of the medicine box comprises the following steps:

[0061] (1) Dissolving the selected mole of the compound shown in formula (II) in 0.5 mol / L, pH 4.0 acetic acid-sodium acetate buffer solution to obtain solution A for subsequent use;

[0062] (2) dissolving selected moles of aluminum chloride in acetic acid-sodium acetate buffer solution of 0.5mol / L and pH of 4.0 to obtain solution B for subsequent use;

[0063] (3) Mix the solution A and the solution B uniformly to obtain the solution C for subsequent use;

[0064] (4) The solution C is subjected to sterile filtration, divided into controlled antibiotic bottles, freeze-dried for 24 hours, and sealed with a stopper.

[0065] The preparation method of the ...

Embodiment 2

[0070] This embodiment is used in the kit for preparing the compound shown in formula (I), and its reagent comprises: the compound shown in 1nmol formula (II), 1nmol aluminum trichloride, 0.4mol / L, the acetic acid- Sodium acetate buffer;

[0071] The preparation method of the medicine box comprises the following steps:

[0072] (1) Dissolving the selected mole of the compound shown in formula (II) in 0.4mol / L, pH 5.0 acetic acid-sodium acetate buffer solution to obtain solution A for subsequent use;

[0073] (2) dissolving selected moles of aluminum chloride in acetic acid-sodium acetate buffer solution of 0.4mol / L and pH of 5.0 to obtain solution B for subsequent use;

[0074] (3) Mix the solution A and the solution B uniformly to obtain the solution C for subsequent use;

[0075] (4) The solution C is subjected to sterile filtration, divided into controlled antibiotic bottles, freeze-dried for 24 hours, and sealed with a stopper.

[0076] The preparation method of the com...

Embodiment 3

[0081] This embodiment is used in the kit for preparing the compound shown in formula (I), and its reagent comprises: the compound shown in 5nmol formula (II), 1nmol aluminum trichloride, 0.6mol / L, the acetic acid- Sodium acetate buffer;

[0082] The preparation method of the medicine box comprises the following steps:

[0083] (1) Dissolving the selected mole of the compound shown in formula (II) in 0.6mol / L, pH 3.0 acetic acid-sodium acetate buffer solution to obtain solution A for subsequent use;

[0084] (2) dissolving selected moles of aluminum chloride in acetic acid-sodium acetate buffer solution of 0.6mol / L and pH of 3.0 to obtain solution B for subsequent use;

[0085] (3) Mix the solution A and the solution B uniformly to obtain the solution C for subsequent use;

[0086] (4) The solution C is subjected to sterile filtration, divided into controlled antibiotic bottles, freeze-dried for 24 hours, and sealed with a stopper.

[0087] The preparation method of the com...

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Abstract

The invention belongs to the field of radiopharmaceuticals and nuclear medicine, and particularly relates to an 18F marked affinity compound and a preparation method and application thereof. On the one hand, the uptake value of tumors on the 18F marked affinity compound is high, and tumor development sensitivity is high; on the other hand, the uptake value of the liver on the 18F marked affinity compound is low, and toxic and side effects on the liver are small. Animal experiments indicate that the uptake value of tumors on the 18F marked affinity compound is high, the residence time is short, the target / target-to-nontarget ratio is high, good pharmacokinetics characteristics are achieved, the biological properties are good, and the compound can be directly used as a tumor PET photographic developer targeted to an HER2 receptor. The preparation method of the 18F marked affinity compound is low in cost, easy and fast to operate, high in labeling rate and high in radiochemical purity of labeled products, and the prepared 18F marked affinity compound can be clinically applied and popularized as the tumor PET photographic developer targeted to the HER2 receptor.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals and nuclear medicine, and specifically relates to a 18 F-labeled affimer compound, preparation method and application. Background technique [0002] Positron emission tomography (PET) is a cutting-edge technology for biomedical research and clinical diagnosis in the 21st century. Gain insight into the activity of labeled drugs in normal or sick people. Compared with SPECT, PET has obvious advantages such as high resolution and quantitative analysis. [0003] 18 F has nearly 100% positron efficiency, low positron energy (0.64 MeV), and relatively short physical half-life (t 1 / 2 =109.7min) and other characteristics, it is an ideal PET imaging nuclide. [0004] Peptides have the advantages of rapid tissue penetration, rapid clearance in blood, and low immunogenicity. 18 Suitable carriers for F-labeled imaging agents. Human epidermal growth factor receptor-2 (human epithelial growth factor r...

Claims

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Application Information

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IPC IPC(8): C07K14/00C07K1/13A61K51/08A61K101/02
CPCA61K51/08C07K14/00
Inventor 杨敏徐宇平潘栋辉赵富宽严骏杰王立振杨润琳张波
Owner JIANGSU INST OF NUCLEAR MEDICINE
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