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Rk polypeptide radiopharmaceutical targeting HER2 and preparation method thereof

A technology of radiopharmaceuticals and radionuclides, which is applied in the field of new tumor diagnostic radiopharmaceuticals and its preparation, can solve the problems of biopsy trauma and inconsistency, and achieve the effects of increasing uptake, enhancing drug uptake, and improving metabolic stability

Pending Publication Date: 2019-10-18
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Clinically, surgery or needle biopsy is usually used to obtain pathological tissue, and then the expression level of HER2 is judged by IHC or FISH, but the biopsy is traumatic, and the expression level of HER2 between the primary tumor and the metastases has a high rate of inconsistency (6%- 48%), and the small sample size does not necessarily represent the HER2 expression status of the entire tumor

Method used

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  • Rk polypeptide radiopharmaceutical targeting HER2 and preparation method thereof
  • Rk polypeptide radiopharmaceutical targeting HER2 and preparation method thereof
  • Rk polypeptide radiopharmaceutical targeting HER2 and preparation method thereof

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Embodiment 99

[0048] This embodiment takes 99m Tc-HYNIC-PEG 4 -(Aoc-rk) 2 Polypeptide radiopharmaceuticals and their preparation methods are taken as examples.

[0049] 99m Tc-HYNIC-PEG 4 -(Aoc-rk) 2 Among them, the rk polypeptide monomer is a D-type amino acid linear polypeptide rnwelrlk, and the rk polypeptide dimer is formed by linking the linker Aoc with the rk polypeptide monomer, and then dimerizing two rk polypeptide monomers connected with Aoc Polypeptide dimers, radionuclides 99m Tc marks the rk polypeptide dimer through a bifunctional chelating agent HYNIC, and a pharmacokinetic modification molecule PEG is also connected between the rk polypeptide dimer and the bifunctional chelating agent 4 , the rk polypeptide radiopharmaceutical is 99m Tc-HYNIC-PEG 4 -(Aoc-rk) 2 , the structural formula of the marker is as figure 2 As shown, the rk polypeptide radiopharmaceutical is a colorless transparent liquid injection.

[0050] 99m Tc-HYNIC-PEG 4 -(Aoc-rk) 2 The preparation...

Embodiment 2

[0061] This embodiment takes 99m Tc-HYNIC-PEG 4 -(PEG 4 -rk) 2 Polypeptide radiopharmaceuticals and their preparation methods are taken as examples.

[0062] 99m Tc-HYNIC-PEG 4 -(PEG 4 -rk) 2 Among them, the rk polypeptide monomer is a D-type amino acid linear polypeptide rnwelrlk, and the rk polypeptide dimer is a linker PEG 4 Linked with rk polypeptide monomer, and then two linked with PEG 4 The rk polypeptide dimer formed by the dimerization of the rk polypeptide monomer, radionuclide 99m Tc marks the rk polypeptide dimer through a bifunctional chelating agent HYNIC, and a pharmacokinetic modification molecule PEG is also connected between the rk polypeptide dimer and the bifunctional chelating agent 4 , the rk polypeptide radiopharmaceutical is 99m Tc-HYNIC-PEG 4 -(PEG 4 -rk) 2 , the rk polypeptide radiopharmaceutical is a colorless transparent liquid injection.

[0063] 99m Tc-HYNIC-PEG 4 -(PEG 4 -rk) 2 The preparation method is as follows:

[0064] HYN...

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Abstract

The invention discloses an rk polypeptide radiopharmaceutical targeting HER2 and a preparation method thereof. The rk polypeptide radiopharmaceutical comprises an rk polypeptide dimer and a radionuclide, wherein the radionuclide marks the rk polypeptide dimer through a chelating agent, the rk polypeptide dimer is a polypeptide dimer formed by connecting PKM and rk polypeptide monomers and then dimerizing the two rk polypeptide monomers connected with the PKM; each rk polypeptide monomer is a D-type amino acid linear 8-membered polypeptide, and the sequence of the rk polypeptide monomer is as follows: Arg-Asn-Trp-Glu-Leu-Arg-Leu-Lys; the PKM represents a pharmacokinetic modifying molecule. The radiopharmaceutical is used for imaging diagnosis of HER2 positive tumor patients, medication guidance and real-time curative effect monitoring of patients treated by anti-cancer drug trastuzumab monoclonal antibodies.

Description

technical field [0001] The invention relates to a novel radiopharmaceutical for tumor diagnosis and a preparation method thereof, in particular to imaging diagnosis for patients with HER2 positive tumors, as well as medication guidance and real-time curative effect monitoring for patients treated with anticancer drug trastuzumab. Background technique [0002] Breast cancer is one of the most common malignant tumors in women, accounting for about 25% of female malignant tumors, and it tends to become younger, which seriously threatens women's life and health. Human epidermal growth factor receptor 2 (human epidermal growth factor receptor 2, HER2) is a proto-oncogene. The abnormal amplification of HER2 and the overexpression of its protein can lead to malignant transformation of cells, and are associated with the invasion, metastasis and recurrence of breast cancer. closely related. In clinical cases, about 30% of breast cancer patients are HER2 positive. [0003] Statistic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/06
CPCA61K51/065A61K51/088C07K7/06
Inventor 王凡史继云杜帅樊贾兵
Owner PEKING UNIV
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