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Nuclide-labeled trastuzumab and preparation method thereof

A trastuzumab and labeling technology, applied in the field of clinical nuclear medicine, to achieve good targeting effect, inhibit and destroy diseased tissue, and achieve individualized effects

Pending Publication Date: 2022-07-12
北京健康启航科技有限公司
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Problems solved by technology

ToGA results showed that the objective effective rate of anti-HER2 targeted therapy in patients with advanced gastric cancer with HER2 overexpression was only 47.3%

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  • Nuclide-labeled trastuzumab and preparation method thereof

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Embodiment

[0029] A radionuclide-labeled trastuzumab, which is a radionuclide 131I-labeled trastuzumab.

[0030] A preparation method of radionuclide-labeled trastuzumab, comprising the following steps:

[0031] S1: Weigh Iodogen in a test tube and dissolve it in dichloromethane, add 10 μL of Iodogen to the bottom of the reaction tube, and dry it with nitrogen to form a uniform film at the bottom of the reaction tube, and the concentration of dichloromethane is 1 g / L;

[0032] S2: Add 10.0 μg of trastuzumab and 10 μL of Na131I solution to the reaction tube coated with a certain amount of Iodogen in turn, shake gently, and react at room temperature for 8-10 minutes. The radioactivity of the Na131I solution is 22.2MBq;

[0033] S3: After the reaction is completed, add 250 μL of PB solution to the reaction tube of S2, and let it stand to obtain a reaction solution. The concentration of the PB solution is 0.05mol / L, and the standstill time is 5-8min;

[0034] S4: Purify the reaction solutio...

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Abstract

The invention discloses a radionuclide-labeled trastuzumab and a preparation method thereof, the radionuclide 131I-labeled trastuzumab is prepared by the following steps: weighing Idogen in a test tube, dissolving with dichloromethane, adding 10 [mu] L of Idogen to the bottom of a reaction tube, and blow-drying with nitrogen to form a uniform film at the bottom of the reaction tube; the method comprises the following steps: sequentially adding 10.0 mu g of trastuzumab and 10 mu L of a Na131I solution into a reaction tube coated with a certain amount of Iodogen, slightly shaking, and reacting for 8-10 minutes at room temperature; after the reaction is finished, adding 250 [mu] L of a PB solution into the reaction tube, and standing to obtain a reaction solution; and purifying the reaction liquid by using a SephadexG-50 column to obtain a target product. According to the nuclide-labeled trastuzumab and the preparation method thereof, proton nuclide 131I is used, so that sufficient ionizing radiation biological effect can be generated locally, the purpose of inhibiting and damaging diseased tissues is achieved, unnecessary radiation to adjacent normal tissues is avoided, and the problem that the existing trastuzumab is damaged is solved. The individualized and precise treatment of the targeted tumor medicine is realized.

Description

technical field [0001] The invention relates to the technical field of clinical nuclear medicine, in particular to a radionuclide-labeled trastuzumab and a preparation method thereof. Background technique [0002] With the in-depth development and integration of nuclear medicine and molecular biology, medical imaging technology has entered the era of molecular imaging. Among them, Positron Emission Tomography (PET) for functional imaging enables people to truly understand the molecular level. Begin to recognize and diagnose diseases, especially in the diagnosis and treatment of tumors. By tracking the changes of receptors in the diseased tissue and abnormal cell signal transduction, it can overcome the defects of modern diagnostic technology, provide the basis for the early diagnosis, clinical staging, and efficacy evaluation of tumors, and evaluate the prognosis. Targeted therapy for tumors. In addition to multimodal imaging devices with high resolution, high sensitivity,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K16/32C07K1/13C07K1/16A61K51/10A61P35/00A61P35/04A61K101/02
CPCC07K16/32A61K51/103A61P35/00A61P35/04Y02P20/55
Inventor 肖松涛
Owner 北京健康启航科技有限公司
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