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Medicine in use for treating gastric cancer, and preparation method

A drug and gastric cancer technology, which is applied in the field of drugs for the treatment of gastric cancer and its preparation, can solve problems such as the impact of antibody activity, and achieve the effects of increasing intake, reducing impact, 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 CN1166988A discloses an anti-human liver cancer monoclonal antibody HAb18 radioimmunotherapy agent, but there is no drug for the treatment of gastric cancer that is labeled with radionuclides by an indirect method at home and abroad
The labeling methods used in the above studies are all direct labeling methods. Since reducing agents or oxidizing agents are added during the labeling process, it has a relatively large impact on antibody activity.

Method used

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

Examples

Experimental program
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Effect test

Embodiment 1

[0038] A drug for treating 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 liquid injection.

[0039] 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.

[0040] In the present invention, the radionuclide is 90 Y, the bifunctional linker is DOTA (1,4,7,10-tetraazacyclododecane-N′, N″, N, N′-tetraacetic acid, 1,4,7,10 -tetraazacyclododecanetetraacetic acid), the radionuclide-labeled monoclonal antibody is 90 Y-DOTA-3H11.

[0041] In the present invention, the bifunctional linker includes derivatives of DOTA.

[0042] In the present invention, th...

Embodiment 2

[0073] In this embodiment, the monoclonal antibody 3H11 is labeled with another radionuclide, which is 177 Lu (lutetium-177), the bifunctional linker is DOTA (1,4,7,10-tetraazacyclododecane-N', N", N, N""-tetraacetic acid, 1, 4,7,10-tetraazacyclododecanetetraacetic acid), the radiopharmaceutical is 177 Lu-DOTA-3H11.

[0074] In the present invention, the bifunctional linker includes derivatives of DOTA.

[0075] In the present invention, the bifunctional linker includes DTPA (diethylenetriaminepentaacetic acid, diethylenetriaminepentaacetic acid).

[0076] In the present invention, the bifunctional linker includes a derivative of DTPA.

[0077] 177 Preparation and quality control methods of Lu-DOTA-3H11 and 90 Same for Y-DOTA-3H11.

[0078] The coupling and purification methods of DOTA derivatives, DTPA and its derivatives and antibody 3H11 are the same as the coupling and purification methods of DOTA and antibody 3H11. 177 Lu labeling method and quality control method...

Embodiment 3

[0081] A preparation method of a medicine for treating gastric cancer, the specific steps are as follows:

[0082] 1. Add 1.2 mL of monoclonal antibody 3H11 solution with a concentration of 5.0 mg / mL and 1 mL of EDTA solution with a concentration of 1.0 mM into ultrafiltration centrifuge tubes, and centrifuge at 5,000 rpm for 45 minutes at 4°C. ;

[0083] II. In the ultrafiltration centrifuge tube, add a pH value of 7.5 and a concentration of 0.1M Na 2 HPO 4 Solution 2.0mL, centrifuge at 5000 rpm for 45 minutes at 4°C for the second time;

[0084] III. In the ultrafiltration centrifuge tube, add a pH value of 7.5 and a concentration of 0.1M Na 2 HPO 4 Solution 2.0mL, centrifuge at 5000 rpm for 45 minutes at 4°C for the third time;

[0085] IV, adding pH value to 7.5 in the ultrafiltration centrifuge tube, concentration is the Na of 0.1M 2 HPO 4 Solution 2.0mL, centrifuge at 5000 rpm for 45 minutes at 4°C for the fourth time;

[0086] V. The monoclonal antibody 3H11 sol...

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Abstract

The present invention relates to a medicine for curing carcinoma of stomach and its preparation method. Said medicine includes antibody and radioactive nuclide. Said antibody is monoclonal antibody 3H11, said radioactive nuclide can utilize a bifunctional connecting agent to mark the described monoclonal antibody 3H11. Because the tumor cell surface can express specific antigen, so that it can utilize the specific combination of antibody and antigen, and can utilize antibody to make the radioactive nuclide be loaded on the tumor region, and utilize beta-particles released by radioactive nuclide decay to kill carcinoma cell so as to attain the goal of curing carcinoma.

Description

technical field [0001] The invention relates to a medicine for treating 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 concentrates on the tumor site after injection into the body, and uses the β released by the decay of the radionuclide - Particles kill cancer cells to achieve the purpose of treatment. Background technique [0002] Tumor is one of the major diseases that endanger human life and health. How to diagnose and treat early 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 treat diseases. Due to the specificity a...

Claims

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Application Information

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IPC IPC(8): A61K51/00A61K39/395A61K47/48A61P35/00A61K47/68
Inventor 王凡贾兵杨志
Owner PEKING UNIV
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