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Polypeptides PET developing agent for targeting EGFR and preparation method and application of polypeptides PET developing agent

A PET imaging agent and polypeptide technology, which is applied to the EGFR-targeting polypeptide PET imaging agent and its preparation and application fields, can solve the problems of difficult to meet clinical treatment, large side effects of chemotherapy, poor specificity, etc., and achieve good clinical results. Application and development prospects, strong water solubility and good stability

Active Publication Date: 2019-02-19
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For non-solid tumors and cancers with widespread systemic metastases, effective surgical treatment and radiotherapy cannot be performed, and chemotherapy has large side effects, poor specificity, and low curative effect, and it is difficult to meet the needs of clinical treatment.

Method used

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  • Polypeptides PET developing agent for targeting EGFR and preparation method and application of polypeptides PET developing agent
  • Polypeptides PET developing agent for targeting EGFR and preparation method and application of polypeptides PET developing agent
  • Polypeptides PET developing agent for targeting EGFR and preparation method and application of polypeptides PET developing agent

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preparation example Construction

[0030] The preparation method of the above-mentioned polypeptide PET imaging agent targeting EGFR comprises the following steps:

[0031] 1) Application of cyclotron bombardment 18 O water production 18 F, and then 18 F conducts in the anion exchange column, and then washes the 18 F is rinsed into the reaction flask and carried out azeotropic water removal, then added 2-ethyl bromopropionate and solvent, fully reacted to obtain 2- 18 F-ethyl propionate;

[0032] 2) to 2- 18 F-ethyl propionate is subjected to alkaline hydrolysis, after removing the reaction solvent, the hydrolyzate, bis(4-nitrophenyl)carbonate and solvent are mixed, fully reacted, and then semi-preparative HPLC separation and purification are carried out to obtain 18 F-NFP;

[0033] 3) Will 18Mix F-NFP, Lys-GE11 polypeptide, N,N-diisopropylethylamine and solvent, fully react, dilute with water, pass through Sep-Par C-18 column, wash C-18 column with water, and rinse with ethanol C-18 column, collect elu...

Embodiment 1

[0048] A preparation method of a polypeptide PET imaging agent targeting EGFR comprises the following steps:

[0049] 1) Application of medical cyclotron bombardment 18 O water, through 18 O(p n) 18 F nuclear reaction production 18 F, and then 18 F was conducted in an anion exchange column, and the activity was measured and washed with 1 mL of eluent (from 12 mg of 4,7,13,16,21,24-hexaoxo-1,10-diazabicyclo[8.8.8]26 Alkane + 3mg of K 2 CO 3 + 0.15mL water + 1.35mL acetonitrile) will 18 F was rinsed into the reaction bottle, and then continuously blown high-purity helium into the reaction bottle and heated to 110°C for azeotropic water removal, dried, then added 5 mg of ethyl 2-bromopropionate and 1 mL of acetonitrile, 100 ℃ reaction 10min, get 2- 18 F-ethyl propionate;

[0050] 2) In 2- 18 Add 0.5mL of potassium hydroxide solution with a concentration of 0.1mol / L to F-ethyl propionate, hydrolyze at 100°C for 10min, evaporate the solvent to dryness after the reaction i...

Embodiment 2

[0056] A preparation method of a polypeptide PET imaging agent targeting EGFR comprises the following steps:

[0057] 1) Application of medical cyclotron bombardment 18 O water, through 18 O(p n) 18 F nuclear reaction production 18 F, and then 18 F was conducted in an anion exchange column, and the activity was measured and washed with 1 mL of eluent (from 12 mg of 4,7,13,16,21,24-hexaoxo-1,10-diazabicyclo[8.8.8]26 Alkane + 3mg of K 2 CO 3 + 0.15mL water + 1.35mL acetonitrile) will 18 F was rinsed into the reaction bottle, and then continuously blown high-purity helium into the reaction bottle and heated to 110°C for azeotropic water removal, dried, then added 7 mg of ethyl 2-bromopropionate and 1 mL of acetonitrile, 100 ℃ for 15 minutes to obtain 2- 18 F-ethyl propionate;

[0058] 2) In 2- 18 Add 0.5mL of potassium hydroxide solution with a concentration of 0.1mol / L to F-ethyl propionate, hydrolyze at 100°C for 15min, evaporate the solvent to dryness after the react...

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Abstract

The invention discloses a polypeptides PET developing agent for targeting EGFR and a preparation method and application of the polypeptides PET developing agent. 18F-NFP serves as a radiochemistry labeled intermediate for 18F labeling to obtain THE high-purity PET developing agent 18F-FP-Lys-GE11, and is good in stability and high in water solubility, internal blood is removed quickly, the developing agent is mainly metabolized via the kidneys, is taken in obviously in PC-3 mice with tumors having positive expression on epidermal growth factor (EGFR), the developing contrast ratio of a tumor focus portion is high, the tumor resolution capability is high, and the polypeptides PET developing agent for targeting EGFR has good clinical application and development prospect in the aspect of tumor PET developing.

Description

technical field [0001] The invention relates to a polypeptide PET imaging agent targeting EGFR and its preparation method and application. Background technique [0002] Malignant tumors are one of the largest public health problems in the world, and they are extremely harmful to human health. "2017 China Cancer Report" released the data of cancer incidence and death in my country in 2013. The report shows that China is a big cancer country, and the number of cancer patients accounts for about 40% of the total number of cancer patients in the world. About 10,000 people are diagnosed with cancer every day in my country. Seven people are diagnosed every minute. Among all cancer cases, lung cancer, gastric cancer, colorectal cancer, liver cancer, breast cancer, and esophageal cancer are the most common, accounting for about 65% of all cancer cases. [0003] Traditional cancer treatment methods mainly include surgery, chemotherapy, and radiation therapy. For non-solid tumors and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K101/02
CPCA61K51/08
Inventor 黄顺胡孔珍韩彦江吴湖炳王全师
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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