PET molecular probe targeting PD-L1 as well as preparation method and application of PET molecular probe

A technology of PD-L1 and molecular probes, applied in the direction of radioactive carriers, etc., can solve the problems of distortion of results, reflection of PD-L1 expression and dynamic changes, etc.

Pending Publication Date: 2021-11-16
XIANGYA HOSPITAL CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional puncture pathological biopsy and immunohistochemistry are limited by invasive operations, and the results are distorted by tumor heterogeneity. It is difficult to accurately monitor the dynamic changes of the immune checkpoint PD-L1 in real time; CT, MRI and ultrasound are based on tumor morphological changes. Structural imaging technology cannot reflect the expression and dynamic changes of PD-L1 at the molecular level

Method used

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  • PET molecular probe targeting PD-L1 as well as preparation method and application of PET molecular probe
  • PET molecular probe targeting PD-L1 as well as preparation method and application of PET molecular probe
  • PET molecular probe targeting PD-L1 as well as preparation method and application of PET molecular probe

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Embodiment 1

[0044] This embodiment provides a PET molecular probe targeting PD-L1, the structural formula of the molecular probe is as follows:

[0045]

[0046] In this embodiment 1 The PET molecular probe targeting PD-L1 is named 68 Ga-NOTA-NF12.

[0047] the above 68 The specific preparation steps of Ga-NOTA-NF12 are as follows:

[0048] (1) Add 1 mL of 0.25M NaOAc aqueous solution to the EP tube containing the labeled precursor compound NOTA-NF12 (25-30 μg), and mix well to obtain the NOTA-NF12 solution;

[0049] (2) The NOTA-NF12 solution was transferred to a 20mL reaction tube; 68 Wash Ga into the reaction tube, the radioactivity is about 10-50mCi, react at 90°C for 10min;

[0050] (3) Add 10 mL of deionized water to quench the reaction to obtain a reaction system;

[0051] (4) the reaction system of step (3) is passed through C 18 Plus column for enrichment, and wash C with 10mL deionized water 18 Plus column;

[0052] (5) Wash the product sequentially with 1mL ethanol a...

Embodiment 2

[0056] This embodiment provides a PET molecular probe targeting PD-L1, the structural formula of the molecular probe is as follows:

[0057]

[0058] In this embodiment 2 The PET molecular probe targeting PD-L1 is named 18 F-AIF-NOTA-NF12.

[0059] abovementioned 18 The specific preparation steps of F-AIF-NOTA-NF12 are as follows:

[0060] 1) Produced by GE's Qilin cyclotron 18 F (250-300mCi) and transferred to the anion exchange column QMA (QMA^READI-CLING TM type column) for capture, with N 2 Dry the QMA;

[0061] 2) Add 300ug AIF-NOTA-NF12, 1.0ml acetonitrile, 0.03ml 0.4M A1C13 solution and 0.5mL acetate buffer solution with pH=4.0 to the reaction tube in advance;

[0062] 3) 0.3mL 0.9% NaCl will 18 F rinse until the reaction tube rinse into the reaction tube, the emissive activity is 200-250mCi, 110°C, react for 10min;

[0063] 4) Add 5mL of deionized water, and collect the product peak (80-120mci) after HPLC purification;

[0064] 5) The product solution is ...

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Abstract

The invention provides a PET molecular probe targeting PD-L1 as well as a preparation method and application of the PET molecular probe, and belongs to the field of nuclear medicine and radiopharmaceuticals. The invention provides a PD-L1 targeting PET molecular probe as well as a preparation method and application thereof, and realizes high-specificity and high-sensitivity imaging in a plurality of animal tumor models. The prepared PET molecular probe targeting PD-L1 is further verified at the clinical human body level, and the expression level of PD-L1 in lung cancer patients with high expression of PD-L1 can be well subjected to noninvasive in-vivo imaging; in this way, a new imaging means is expected to be provided for early noninvasive screening of PD-L1 patients and monitoring of the expression level of PD-L1 in the immunotherapy process.

Description

technical field [0001] The invention belongs to the field of nuclear medicine and radiopharmaceuticals, and in particular relates to a PET molecular probe targeting PD-L1 and its preparation method and application. Background technique [0002] Tumor immunotherapy has become the fourth largest tumor treatment after surgery, radiotherapy and chemotherapy, and it is also the most popular tumor treatment at present. For example, immunotherapy targeting the PD-1 / PD-L1 signaling pathway has achieved great success in the treatment of clinical tumor patients, for which it won the 2018 Nobel Prize in Medicine. However, not all tumor patients respond to this treatment; and due to its different mechanism of action, compared with previous treatments, tumor treatment response patterns are diverse, such as delayed response, pseudoprogression, hyperprogression, immune-related Phenomena such as adverse events have brought difficulties and challenges to clinical treatment decision-making a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K101/02A61K103/00
CPCA61K51/08
Inventor 周明胡硕张现忠王晓博陈蓓饶婉倩
Owner XIANGYA HOSPITAL CENT SOUTH UNIV
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