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Boron carrying agent for integrating tumor diagnosis and treatment

A carrier agent and tumor technology, applied in the field of boron carrier agent for the integration of tumor diagnosis and treatment, can solve the problems of poor effect of BNCT therapeutic agents, high misdiagnosis rate, unstable diagnosis and treatment integration technology, etc., and achieve high early diagnosis accuracy, Pain-reducing, less toxic effect

Inactive Publication Date: 2018-12-21
PEKING UNIV
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  • Abstract
  • Description
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  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problems existing in the existing technology 18 F-FDG PET / CT imaging false positive and false negative misdiagnosis rate is high, the effect of BNCT therapeutic agents is not good, and the integration of diagnosis and treatment technology is unstable. The present invention provides a new method for the integration of PET imaging diagnosis and BNCT treatment. boron carrier

Method used

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  • Boron carrying agent for integrating tumor diagnosis and treatment
  • Boron carrying agent for integrating tumor diagnosis and treatment
  • Boron carrying agent for integrating tumor diagnosis and treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、18

[0042] Embodiment 1, 18 Preparation of F-FBY

[0043] 1. Dissolve p-hydroxyphenylacetaldehyde (1eq) and R-tert-butylsulfinamide (1.2eq) in 100ml tetrahydrofuran, add tetraisopropyl titanate (2eq), stir overnight at room temperature, add water to quench the reaction, and filter After drying, the solvent was removed by rotary evaporation and separated by column chromatography to obtain the corresponding imine.

[0044] 2. The toluene solution of the imine (1eq) prepared in step 1 and the pinacol borate (2eq) was added in advance by tricyclohexylphosphine fluoroborate (1.2%eq), copper sulfate (1.2%eq) , In the catalyst prepared by benzylamine (5%eq), stir at room temperature for 24h.

[0045] 3. Add ethyl acetate to dilute the reaction product of step 2, add 4M hydrochloric acid and 3M potassium bifluoride solution, and add acetonitrile to dilute to a reaction system of acetonitrile: water = 1:1, stir at room temperature for 2 hours, and then remove the solvent by rotary evapor...

Embodiment 2、18

[0051] Embodiment 2, 18 PET images of F-FBY in tumor-bearing mice

[0052] About 3.7MBq 18 F-FBY was injected into tumor-bearing mice through the tail vein under isoflurane anesthesia, and 10 minutes of static acquisition was performed 60 minutes after the injection to obtain PET image data. The result is as image 3 as shown, image 3 show 18 F-FBY is mainly metabolized by the kidney and bladder. Except for the gallbladder, kidney, bladder and other major metabolic organs, there is no obvious uptake in other normal tissues, and the uptake in the tumor site is obvious.

[0053] Embodiment 3, 18 PET images of F-FBY applied to tumor-bearing mice at different doses

[0054] Under isoflurane anesthesia, approximately 3.7 MBq 18 F-FBY mixed with different doses of FBY (0.2mg, 1mg, 5mg, 25mg) was injected into the tumor-bearing mice through the tail vein, and 10min of static acquisition was performed 90min after the injection to obtain PET image data. The result is as Figu...

Embodiment 4、18

[0056] Embodiment 4, 18 Distribution of F-FBY in different organs of tumor-bearing mice

[0057] About 3.7MBq 18 F-FBY mixed with 25 mg of FBY was injected into the tumor-bearing mice through the tail vein under isoflurane anesthesia, and the PET image data was obtained by static acquisition for 10 min at 90 min after the injection ( Figure 5 ). Figure 5 The results indicated that FBY can be enriched in a large amount in the tumor site, which fully meets the boron content required by BNCT, and can be used as a potential boron carrier in BNCT.

[0058] Immediately after the static acquisition of PET image data scanning, the mice were sacrificed, and different organs (brain, muscle, tumor, etc.) were digested by microwave and the boron concentration was measured by ICP-OES ( Figure 6 ). Figure 6 The results showed that at different FBY doses, the boron content of each organ determined by ICP-OES had a good correspondence with the radioactive signal, indicating that the F...

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Abstract

The invention relates to a boron carrying agent for integrating tumor diagnosis and treatment. The boron carrying agent is tyrosine boron trifluoride (FBY) obtained by replacing a carboxyl group witha boron trifluoride group on the basis of tyrosine. FBY can be used for boron neutron capture therapy (BNCT) for treating malignant tumors; radioactive <18>F-labeled FBY can also be used for positronemission tomography (PET) imaging diagnosis. <18F>-FBY can simultaneously achieve imaging diagnosis and precise treatment of cancers.

Description

technical field [0001] The invention belongs to the field of tumor diagnosis and treatment, in particular to a reagent for tumor PET imaging diagnosis and / or BNCT precise treatment, in particular to a boron carrier derived from tyrosine for integrated tumor diagnosis and treatment. Background technique [0002] Tumor is still a common and frequently-occurring disease that seriously threatens the health of human beings, and is one of the main causes of death. Molecular imaging technology combines molecular probes and medical imaging technology to conduct qualitative and quantitative research on pathological and physiological processes in vivo at the cellular and molecular levels. Positron Emission Tomography (PET) is a molecular imaging technique based on radioactive molecular probes. PET technology is based on the detection of paired photons emitted by the annihilation of positrons. from 11C, 18 The positrons emitted from positron-decaying isotopes such as F quickly colli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/02A61K31/69A61K51/04A61K41/00A61P35/00C07B59/00A61K101/00A61K101/02
CPCA61K41/0095A61K51/0406A61P35/00C07B59/001C07B2200/05C07F5/02
Inventor 刘志博李纪元
Owner PEKING UNIV
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