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Tumor stroma developer and preparation method thereof

A tumor stroma and imaging agent technology, applied in the field of nuclear medicine, can solve the problems of toxicity, clinical application limitations, short half-life, etc., and achieve the effects of high intake, extended window period, high sensitivity and specificity

Pending Publication Date: 2022-02-22
SHANGHAI UNIV OF MEDICINE & HEALTH SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although 68 Ga-FAPI-4 has been proved to be better for tumor imaging, but due to 68 Ga has a short half-life (68 minutes) and is toxic, and it requires 68 Ga / 68 Ge generator or cyclotron liquid target bombardment can be obtained, but most domestic PET centers do not have the above conditions, so the clinical application is limited

Method used

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  • Tumor stroma developer and preparation method thereof
  • Tumor stroma developer and preparation method thereof
  • Tumor stroma developer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] (S)-[ 18 Preparation of F]-AlF-NOTA-Bn-FAPI-4

[0044]

[0045] Using a proton cyclotron 18 O(p,n) 18 The F reaction produces an activity of 150mCi 18 f - ; the resulting 18 f - Transfer to the anion exchange column QMA (QMA is a packable column) for capture through pipelines. After the capture is completed, use N 2 Dry the QMA, then rinse with 0.45ml pH=4.2 acetic acid-sodium acetate buffer solution, elute to get 18 f - The buffer solution, its activity is 135mCi;

[0046] to 0.45ml 18 f - Add 469.7μg labeled precursor (S)-NOTA-Bn-FAPI-4, 0.75ml acetonitrile and 0.05ml 0.4M AlCl to the buffer solution 3 aqueous solution and reacted at 80°C for 10min, then added 5ml of deionized water to quench the reaction, and then passed the reaction solution over Al 2 o 3 Column, obtain filtrate;

[0047] Pass the filtrate through C 18 -Plus column for enrichment, then rinse with 2ml ethanol and 10ml normal saline in sequence, and pass the rinse solution through a ...

Embodiment 2

[0050] Using a proton cyclotron 18 O(p,n) 18 The F reaction produces an activity of 150mCi 18 f - ; the resulting 18 f - Transfer to the anion exchange column QMA (QMA is a packable column) for capture through pipelines. After the capture is completed, use N 2 Dry the QMA, then rinse with 0.3ml pH=4.2 acetic acid-sodium acetate buffer solution, elute to get 18 f - The buffer solution, its activity is 125mCi;

[0051] to 0.3ml 18 f - Add 469.7μg labeled precursor (S)-NOTA-Bn-FAPI-4, 0.75ml acetonitrile and 0.05ml 0.4M AlCl to the buffer solution 3 aqueous solution and reacted at 80°C for 10min, then added 5ml of deionized water to quench the reaction, and then passed the reaction solution over Al 2 o 3 Column, obtain filtrate;

[0052] Pass the filtrate through C 18 -Plus column for enrichment, then rinse with 2ml ethanol and 10ml normal saline in sequence, and pass the rinse solution through a sterile filter membrane to obtain tumor stroma diagnostic imaging agent...

Embodiment 3

[0054] Using a proton cyclotron 18 O(p,n) 18 The F reaction produces an activity of 160mCi 18 f - ; the resulting 18 f - Transfer to the anion exchange column QMA (QMA is a packable column) for capture through pipelines. After the capture is completed, use N 2 Dry the QMA, then rinse with 0.45ml pH=4.2 acetic acid-sodium acetate buffer solution, elute to get 18 f - The buffer solution, its activity is 135mCi;

[0055] to 0.45ml 18 f - Add 469.7μg labeled precursor (S)-NOTA-Bn-FAPI-4, 0.75ml acetonitrile and 0.05ml 0.4M AlCl to the buffer solution 3 aqueous solution and reacted at 80°C for 10min, then added 5ml of deionized water to quench the reaction, and then passed the reaction solution over Al 2 o 3 Column, obtain filtrate;

[0056] Pass the filtrate through C 18 -Plus column for enrichment, then rinse with 2ml ethanol and 10ml normal saline in sequence, and pass the rinse solution through a sterile filter membrane to obtain tumor stroma diagnostic imaging age...

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Abstract

The invention discloses a tumor stroma developer, which has a chemical structural formula disclosed in the invention: wherein R is hydrogen or fluorine. Compared with the prior art, the tumor stroma developer has the advantages that the tumor stroma developer shows obvious affinity to FPA, the intake amount of the tumor stroma developer for FAP high-expression malignant tumors in the tumor stroma is high, the tumor stroma developer has high sensitivity and specificity for diagnosis of the malignant tumors, and false positive does not occur easily, so that the tumor stroma developer can be effectively and safely applied to diagnosis and treatment of various malignant tumors; the half-life period is longer, the window period is prolonged, and clinical use is more facilitated.

Description

technical field [0001] The invention belongs to the technical field of nuclear medicine, and in particular relates to a tumor interstitial imaging agent and a preparation method thereof. Background technique [0002] Tumor stroma is a general term for other components in tumor tissue except tumor cells. Its composition includes cellular components (interstitial cells) and non-cellular components. The interaction between tumor stroma and tumor cells jointly determines the biological behavior of tumors (growth, invasion, metastasis, etc.). Tumor interstitial response is the formation of a favorable interstitial microenvironment that promotes tumor progression during tumor formation. This process is accompanied by the activation of fibroblasts and the expression of fibroblast activated protein (FAP). FAP is a specific Expressed on the membrane surface of tumor-associated fibroblasts (CAF), its cytoplasmic, transmembrane and extracellular structures are composed of 6, 18 and 7...

Claims

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Application Information

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IPC IPC(8): A61K51/04C07F5/06A61K101/02
CPCA61K51/0459C07F5/069C07B2200/07C07B2200/05C07F5/06C07D401/14C07D215/50C07D401/12A61P35/00A61K31/4709A61K51/0497
Inventor 黄钢李斌
Owner SHANGHAI UNIV OF MEDICINE & HEALTH SCI
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