A novel peptide radiopharmaceutical targeting HER2 and its preparation method and application

A radiopharmaceutical and radionuclide technology, applied in the field of novel polypeptide radiopharmaceuticals and their preparation, can solve the problems of long cycle and high cost, and achieve the effect of good targeting performance

Active Publication Date: 2018-05-18
PEKING UNIV +2
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

What's more serious is that most breast cancer patients will eventually develop drug resistance during Trastuzumab treatment, and Trastuzumab immunotherapy is expensive and has a long cycle

Method used

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  • A novel peptide radiopharmaceutical targeting HER2 and its preparation method and application
  • A novel peptide radiopharmaceutical targeting HER2 and its preparation method and application
  • A novel peptide radiopharmaceutical targeting HER2 and its preparation method and application

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Embodiment Construction

[0027] Materials used in the examples of the present invention: succinic acid (succinic acid), disodium succinatehexahydrate (disodium succinate), trisodium triphenylpheosphine-3,3',3''-trisulfonate (TPPTS, sodium triphenylphosphine trisulfonate ), N,N-Dimethylformamide (DMF, N,N-dimethylformamide), and tricine (trimethylolglycine) were purchased from Sigma-Aldrich, USA. YLFFVFER polypeptide monomer was purchased from China CSBio Ltd. Company. Na 99m TCO 4 The eluent was purchased from Beijing Atomic Hi-Tech Co., Ltd.

[0028] In this example, a novel polypeptide radiopharmaceutical targeting HER2, namely 99m Take Tc-HYLF8 polypeptide radiopharmaceutical and its preparation method as an example.

[0029] The novel polypeptide radiopharmaceutical targeting HER2 includes HYLF8 polypeptide and radionuclide 99m Tc. The radionuclide 99m Tc marks the HYLF8 polypeptide through the bifunctional chelating group HYNIC, and the HYLF8 linear polypeptide is to link the polypeptide Y...

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Abstract

The invention provides a novel HER2-targeting polypeptide radioactive medicine and a preparation method and an application thereof. The novel HER2-targeting polypeptide radioactive medicine includes an HYLF8 polypeptide and radionuclide 99mTc; the HYLF8 polypeptide is prepared by connecting a polypeptide YLFFVFER with a bifunctional chelating agent HYNIC, namely HYNIC-YLFFVFER; the radionuclide 99mTc labels the HYLF8 polypeptide through the bifunctional chelating agent HYNIC, and thus the novel HER2-targeting polypeptide radioactive medicine, namely 99mTc-HYLF8, is obtained; the novel HER2-targeting polypeptide radioactive medicine is a colorless transparent liquid injection.

Description

technical field [0001] The invention relates to radiopharmaceuticals for tumor diagnosis, in particular to a novel polypeptide radiopharmaceutical targeting HER2 and its preparation method and application. Background technique [0002] Worldwide, breast cancer still ranks first among women's common tumors, and ranks second in mortality. Currently, routine clinical diagnostic methods for breast cancer include mammography, color Doppler ultrasound, and MRI. Compared with breast tissue biopsy, these imaging methods have the advantage of being non-invasive, but they also face disadvantages such as low accuracy, lack of specificity, and inability to provide molecular level information. As important modalities of molecular imaging, PET and SPECT have been widely used clinically. They are characterized by high sensitivity and can accurately quantify and provide tumor-associated molecular level information. Currently, 25% to 30% of breast cancer patients have high expression of H...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/02A61K51/08
CPCA61K51/025A61K51/088
Inventor 王凡董诚岩胡志远史继云贾兵王子华李立强吴越刘昭飞赵慧云
Owner PEKING UNIV
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