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Radiopharmaceutical targeting galectin-1 and preparation method thereof

A technology of galectin and radiopharmaceuticals, applied in the direction of in vivo radioactive preparations, radioactive carriers, drug combinations, etc., can solve the problems of weakening the effectiveness of radiotherapy, poor prognosis, and treatment failure, so as to improve the metabolism in the body and increase water solubility , good targeted effect

Active Publication Date: 2020-02-04
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Radiotherapy tolerance weakens the effectiveness of radiotherapy in treatment, leading to poor prognosis such as treatment failure and recurrence

Method used

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  • Radiopharmaceutical targeting galectin-1 and preparation method thereof
  • Radiopharmaceutical targeting galectin-1 and preparation method thereof
  • Radiopharmaceutical targeting galectin-1 and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] In this example, the radionuclide 68 Ga-labeled NOTA-PEG4-TDGd as an example. 68 Ga-NOTA-PEG4-TDGd radiopharmaceutical consists of TDGd, polyethylene glycol PEG4, bifunctional chelator NOTA and radionuclide 68 Ga composition. Among them, the bifunctional chelating agent NOTA can be replaced by DOTA, 68 Ga radionuclides can be replaced by 64 Cu or 18 F( figure 1 and figure 2 shown). by 68 Ga-NOTA-PEG4-TDGd is an example, its preparation method is as follows image 3 shown, including the following steps:

[0037] a.NH 2 - Preparation of PEG4-TDGd: Dissolve 6 μmol of TDGd in 500 μL of PBS, then add 36 μmol of Alkyne-PEG4-NH 2 , 0.6 μmol equivalent of CuSO 4 , 3 μmol of sodium tretinoin, mix well and react at room temperature for 3 to 5 hours, then filter the reaction mixture through a microporous membrane and inject it into semi-preparative HPLC for separation and purification. The product peaks were collected, acetonitrile was removed by rotary evaporation, ...

Embodiment 2

[0049] In this example, the radionuclide 18 F-labeled NOTA-PEG4-TDGd as an example. 18 F-NOTA-PEG4-TDGd radiopharmaceutical consists of TDGd, polyethylene glycol PEG4, bifunctional chelator NOTA and radionuclide 18 F composition. in 18 Radiolabeling of F with NOTA-PEG4-TDGd by AlCl 3 Realized, its preparation method is as Figure 5 shown, including the following steps:

[0050] a. The preparation of NOTA-PEG4-TDGd is the same as in Example 1.

[0051] b. 18 Preparation of F radionuclide-bifunctional chelator-PEG4-TDGd: Dissolve 20 μg of NOTA-PEG4-TDGd in a solution containing 2 mM AlCl 3 0.1M NaOAc buffer (pH = 4.0), and then add 150μL of acetonitrile and 20mCi of 18 F, heated in a water bath at 110°C for 15 minutes. After the reaction mixture was cooled to room temperature, it was diluted with 5 mL of pure water and purified by a Sep-Pak C18 column to obtain the inventive 18 F-NOTA-PEG4-TDGd radiopharmaceutical.

Embodiment 68

[0053] This embodiment takes 68 Taking Ga-NOTA-PEG4-TDGd as an example, the in vivo and in vitro binding specificity identification and PET imaging application of galectin-1 targeting radiopharmaceuticals are given. in, 68 Ga-NOTA-PEG4-TDGd can also be 68 Ga-DOTA-PEG4-TDGd, 64 Cu-NOTA-PEG4-TDGd, 64 Cu-DOTA-PEG4-TDGd or 18 F-NOTA-PEG4-TDGd. 68 Binding specificity of Ga-NOTA-PEG4-TDGd to Galectin-1:

[0054] After coating the recombinant mouse galectin-1 or human galectin-1 on the high adsorption ELISA plate, the 68 Ga-NOTA-PEG4-TDGd was added to perform a radioactive binding experiment, in which an excess of unlabeled TDG was added to the blocking group to detect 68 Binding specificity of Ga-NOTA-PEG4-TDGd to galectin-1. The experimental results showed that after blocking with TDG 68Binding of Ga-NOTA-PEG4-TDGd to either mouse galectin-1 or human galectin-1 was significantly reduced (see Figure 6 ), demonstrating its specific binding to mouse galectin-1 and human gal...

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Abstract

The invention discloses the radiopharmaceutical targeting galectin-1 and a preparation method thereof. The radiopharmaceutical is the conjugate of radionuclide, a difunctional chelating agent and PEG4-TDGd. The PEG4-TDGd is marked by the radionuclide through the difunctional chelating agent. According to the radiopharmaceutical targeting galectin-1, in vivo, because of specific recognition of TDGdto galectin-1 and modification of PEG4 according to pharmacokinetics, radionuclide is delivered to the surfaces of tumor cells with galectin-1 highly expressed or the hypoxia parts of a tumor with galectin-1 highly expressed, nuclear medicine positron emission computed tomography on the specificity of the tumor and the hypoxia areas of the tumor can be implemented, and monitoring on the therapeutic effect by adopting interventional treatment means such as radiotherapy on the tumor can be implemented.

Description

technical field [0001] The invention relates to the technical field of radiopharmaceuticals for disease imaging diagnosis, in particular to novel small molecule radiopharmaceuticals for nuclear medicine positron emission tomography (PET) imaging diagnosis of tumor hypoxia and a preparation method thereof. Background technique [0002] Radiotherapy is currently an important clinical treatment for a variety of malignant tumors. Worldwide, radiotherapy is commonly used in the treatment of 50% to 60% of cancer patients. Radiotherapy has a good curative effect in early and middle-stage tumors, but in stage IV tumors, obvious tolerance can be observed. Radiotherapy resistance weakens the effectiveness of radiotherapy in treatment, leading to poor prognosis such as treatment failure and recurrence. At present, sufficient evidence has proved that radiotherapy tolerance is closely related to tumor hypoxia. In hypoxic tumors, about three times the radiation dose is required to achi...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K51/04A61P35/00A61K101/02A61K103/00
CPCA61K51/0491A61K47/549A61P35/00
Inventor 刘昭飞王凡赖建豪卢德华
Owner PEKING UNIV
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