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Medicine in use for diagnosing gastric cancer, and preparation method

A drug and a technology for gastric cancer, applied in the field of drugs for gastric cancer diagnosis and their preparation, can solve problems such as the influence of antibody activity, and achieve the effects of improving uptake, reducing influence and enhancing stability

Inactive Publication Date: 2007-12-26
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chinese patent 97108618.4 discloses an anti-human liver cancer monoclonal antibody HAb1 8 radioimmunodiagnostic agent, but there is no drug for the diagnosis of gastric cancer that is labeled with radionuclides by indirect methods at home and abroad
The labeling methods used in the above studies are all direct labeling methods, because reducing agents or oxidizing agents are added in the labeling process, so it has a relatively large impact on antibody activity

Method used

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  • Medicine in use for diagnosing gastric cancer, and preparation method
  • Medicine in use for diagnosing gastric cancer, and preparation method
  • Medicine in use for diagnosing gastric cancer, and preparation method

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0045] A drug for the diagnosis of gastric cancer, comprising an antibody and a radionuclide, the antibody is a monoclonal antibody 3H11, the radionuclide is labeled with a bifunctional linker to the monoclonal antibody 3H11, and the radionuclide is labeled The monoclonal antibody 3H11 is a colorless transparent liquid injection.

[0046] In the present invention, the monoclonal antibody 3H11 includes murine antibodies and fragments, single-chain antibodies (ScFv), double-chain antibodies (Diabody), miniaturized antibodies (Minibody) and chimeric antibodies (Chimeric) prepared by genetic engineering. .

[0047] In the present invention, the radionuclide is 99m Tc (technetium-99m), the bifunctional linker is S-HYNIC (succinimidyl-hydrazinonicotinamide, abbreviated as S-HYNIC), the radionuclide-labeled monoclonal antibody formed radiopharmaceuticals are 99m Tc-HYNIC-3H11.

[0048] The monoclonal antibody 3H11 is coupled and purified using the following methods:

[0049] Mix...

Embodiment 2

[0072] In this embodiment, the monoclonal antibody 3H11 is labeled with another radionuclide, which is 111 In (indium-111), the bifunctional linker is DOTA (1,4,7,10-tetraazacyclododecane-N′, N″, N, N″″-tetraacetic acid, 1, 4,7,10-tetraazacyclododecanetetraacetic acid), the radiopharmaceutical formed by the radionuclide-labeled monoclonal antibody is 111 In-DOTA-3H11.

[0073] In the present invention, the bifunctional linker includes a derivative of DOTA.

[0074] In the present invention, the bifunctional linker includes DTPA (diethylenetriaminepenta-acetic acid, diethylenetriaminepenta-acetic acid).

[0075] In the present invention, the bifunctional linker includes derivatives of DTPA

[0076] 111 In is another radionuclide with excellent physical properties, suitable for nuclear medicine imaging. 111 In-labeled antibodies still require indirect labeling, that is, introducing a bifunctional linker between the antibody and the radionuclide, generally DOTA and its deri...

Embodiment 3

[0094] A preparation method of a medicine for gastric cancer diagnosis, the steps are as follows:

[0095] 1. Mix 0.9mL concentration of 5.0mg / mL monoclonal antibody 3H11 solution with 5μL concentration of 1.55×10 -2 The mg / mL S-HYNIC solution was added to the reaction tube, and the reaction was carried out at 4°C in the dark for 5 hours; the molar ratio of S-HYNIC and monoclonal antibody 3H11 in this reaction was 8:1; the reaction solution was obtained after the reaction was completed ;

[0096] II. The reaction solution was dialyzed twice with a citric acid buffer solution with a pH value of 7.4 and a concentration of 20 mM, each dialysis time was 8 hours, and the citric acid buffer solution used contained 100 mM NaCl; The final reaction solution was dialyzed 2 times with a citric acid buffer solution with a pH value of 5.2 and a concentration of 20 mM. The dialysis time was 8 hours each time. The citric acid buffer solution used contained 100 mMNaCl. After the dialysis tre...

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Abstract

The present invention relates to a medicine for diagnosing carcinoma of stomach and its preparation method. Said medicine includes antibody and radioactive nuclide, the descried antibody is monoclonal antibody 3H11, and the described radioactive nuclide can utilize a bifunctional connecting agent to mark the described monoclonal antibody 3H11, and the monoclonal antibody marked by the described radioactive nuclide is a colourless transparent liquid injection. Because the tumor cell surface can express specific antigen, so that it can utilize the specific combination of antibody and antigen, and utilize said antibody to make the radioactive nuclide be loaded on the tumor region, and utilize nuclear medicine image technique to make diagnosis and location of tumor.

Description

technical field [0001] The invention relates to a medicine for diagnosing gastric cancer and a preparation method thereof. The medicine indirectly labels radionuclide to monoclonal antibody 3H11 through a bifunctional linker. Since the surface of tumor cells expresses a specific antigen, the specificity of the antibody and the antigen is utilized. Sexual binding, so that the labeled antibody is concentrated in the tumor site after injection into the body, and gastric cancer can be diagnosed by single photon tomography technology of nuclear medicine. Background technique [0002] Tumor is one of the major diseases that endanger human life and health. How to conduct early diagnosis and treatment is the goal pursued by biomedical workers for a long time. Specific antigens are expressed on the surface of tumor cells, and monoclonal antibodies have the specificity of recognizing antigens, so monoclonal antibodies can be used to diagnose diseases. Due to the specificity and high ...

Claims

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Application Information

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IPC IPC(8): A61K51/00
Inventor 王凡贾兵杨志
Owner PEKING UNIV
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