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18 F-labeled affimer compound and its preparation method and application

A compound and labeling technology, applied in the field of 18F-labeled affinity compound and its preparation, can solve the problems of low tumor sensitivity, complex preparation method, large liver toxicity and side effects, etc., and achieve high radiochemical purity, short residence time, toxicity and so on. Effects with few side effects

Active Publication Date: 2019-07-16
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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  • <sup>18</sup> F-labeled affimer compound and its preparation method and application
  • <sup>18</sup> F-labeled affimer compound and its preparation method and application
  • <sup>18</sup> F-labeled affimer compound and its preparation method and application

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Embodiment 1

[0059] This embodiment is used in the kit for the preparation of the compound shown in formula (I), and its reagents include: 50nmol of the compound shown in formula (II), 12nmol of aluminum chloride, 0.5mol / L, 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 to obtain the product.

[0065] T...

Embodiment 2

[0070] This embodiment is used in the kit for preparing the compound shown in formula (I), and its reagent comprises: 1nmol compound shown in 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 to obtain the product.

[0076] The preparation...

Embodiment 3

[0081] This embodiment is used in the kit for preparing the compound shown in formula (I), and its reagent comprises: 5nmol compound shown in 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 to obtain the product.

[0087] The preparation...

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Abstract

The invention belongs to the field of radiopharmaceuticals, and particularly relates to an 18-labeling affinity type compound and a preparation method and application thereof. On one hand, the absorbing value of a tumor to the 18-labeling affinity type compound is high, and the tumor development sensitivity high; on the other hand, the absorbing value of the liver to the 18-labeling affinity type compound is low, and the toxic and side effect on the liver is little. Animal experiments show that the 18-labeling affinity type compound can serve as tumor PET photographic developer targeting an HER2 receiver due to the fact that the absorbing value of the tumor to the 18-labeling affinity type compound is high, the residence time is short, the target ratio / target-to-nontarget ratio is high, good pharmacokinetics characters are achieved, and the biological performance is excellent. The preparation method is low in cost, and easy, convenient and quick to operate, the labeling rate is high, the radiochemical purity of a labeled product is high, and the prepared 18-labeling affinity type compound serving as the tumor PET photographic developer tarting the HER2 receiver can be clinically applied and popularized easily.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals and nuclear medicine, and specifically relates to a 18 F-labeled affibody 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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