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Mark product of <89>Zr marked denosumab, and preparation method and application thereof

A technology of denosumab and 89zr, which is applied in the direction of radioactive carriers, can solve the problems of inaccurate imaging results, objectivity, low radiochemical purity, and the inability to achieve long-term experiments and inspections, and achieve imaging results Objective, radiochemically pure effect

Inactive Publication Date: 2015-05-27
NANJING PET TRACER
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The first technical problem to be solved by the present invention is that the radioactive chemical purity of the bone imaging agent in the prior art is not high, which causes the result of the imaging to be inaccurate and objective, and the half-life is relatively short, so it is impossible to realize long-time experiments and experiments. Check the problem, and then provide a labeled product with accurate and reliable imaging results and a suitable half-life

Method used

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  • Mark product of &lt;89&gt;Zr marked denosumab, and preparation method and application thereof
  • Mark product of &lt;89&gt;Zr marked denosumab, and preparation method and application thereof
  • Mark product of &lt;89&gt;Zr marked denosumab, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] In this example, the used 89 Zr oxalic acid solution was purchased from PerkinElmer. The Df-Bz-NCS-denosumab used was obtained by:

[0035] Take NaHCO with a concentration of 0.1mol / L and a pH value of 8.4 3 Dissolve denosumab in the solution so that the concentration of denosumab is 10mg / ml, and then use 0.1mol / L Na 2 CO 3 Solution is adjusted to its pH value to 9.0; Then add bifunctional chelating agent ferric isothiocyanate (abbreviation " BFC (Df-Bz-NCS) " wherein, namely hereinafter the same) concentration of 2mmol / L dimethyl sulfoxide (abbreviated as DMSO, hereinafter the same) solution, so that the molar ratio of bifunctional chelating agent and denosumab is 5:1, after mixing, react at 37 ℃ for 60min, namely Obtain Df-Bz-NCS-denosumab crude product; The obtained Df-Bz-NCS-denosumab crude product is purified by PD10 column, after purification, adding physiological saline and gentisic acid solution with a concentration of 3.5 mg / ml as a stabilizer, Store at -...

Embodiment 2

[0049] In this embodiment, adopt the same method as in Embodiment 1 89 Zr oxalic acid solution. The Df-Bz-NCS-denosumab used is obtained in the following way: taking NaHCO with a concentration of 0.1mol / L and a pH value of 8.4 3 Dissolve denosumab in the solution so that the concentration of denosumab is 10mg / ml, and then use 0.1mol / L Na 2 CO 3 The solution adjusts its pH value to 8.9; Then the concentration of BFC (Df-Bz-NCS) added thereto is the DMSO solution of 2mmol / L, makes the mol ratio of bifunctional chelating agent and denosumab be 5:1, after mixing, at 37 The crude product of Df-Bz-NCS-denosumab was obtained by reacting at ℃ for 60 minutes; the obtained crude product of Df-Bz-NCS-denosumab was purified by PD10 column, after purification, physiological saline and gentisic acid solution with a concentration of 3.5mg / ml were added As a stabilizer, store at -80°C until use.

[0050] In this embodiment 89 The method for Zr marking denosumab specifically comprises the...

Embodiment 3

[0060] In this embodiment, the same Df-Bz-NCS-denosumab and 89 Zr oxalic acid solution.

[0061] In this embodiment 89 The method for Zr marking denosumab specifically comprises the following steps:

[0062] Take 100 μl of 4 mCi radioactivity 89 Zr oxalic acid solution, with the concentration being 0.1mol / L, the sodium carbonate solution that pH value is 10 and described 89 Zr oxalic acid solution to a pH value of 7.2, then, adding 0.3ml of sodium edetate buffer solution with a concentration of 0.1mol / L and a pH value of 6.8, then adding Df-Bz-NCS-denosumab therein, and mixing evenly, The reaction solution was formed and reacted at 25°C for 40 minutes to obtain the labeled product [ 89 Zr]-Df-Bz-NCS-denosumab.

[0063] Using the method in Example 1 to obtain the labeled product [ 89 The stability and radiochemical purity of Zr]-Df-Bz-NCS-denosumab were measured, and the results were as follows:

[0064] (1) iTLC method for measuring radiochemical purity: calculate [ 89...

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Abstract

The invention relates to a mark product of <89>Zr marked denosumab. The mark product is [<89>Zr]-Df-Bz-NCS-denosumab; and Df-Bz-NCS-denosumab is marked by adopting <89>Zr. The mark product disclosed by the invention is accurate and reliable in development result, proper in half-life period, good in specificity, targeting property and in-vitro stability and higher in radioactive chemical purity; a good imaging effect can be realized; for bone imaging, the mark product is capable of responding internal metabolism conditions of drugs objectively and accurately; and therefore, osteoporosis and solid tumour osseous metastasis can be diagnosed earlier.

Description

technical field [0001] The invention belongs to the technical field of radioactive labeling, and specifically relates to 89 A labeled product of Zr-labeled denosumab and a preparation method thereof. Background technique [0002] At present, the only clinically used PET bone imaging agents are 18 F-NaF, 18 F-NaF is an osteotropic metabolic imaging agent, 18 in F-NaF 18 F ions can be exchanged with hydroxyl groups in hydroxyapatite crystals in bones, and deposited in bones to visualize the bones of the whole body, whether it is osteolytic or osteogenic lesions, 18 Both F-NaF accumulated and PET imaging could be realized. However, if using 18 F mark, there is a free 18 The phenomenon of F deposition in bone, and it is not possible to determine whether the signal received in PET imaging is 18 Emitted by F-NaF labeling, i.e., due to 18 The radioactive chemical purity of F-NaF is not high, resulting in imaging results that are not objective and accurate enough; and, 18 ...

Claims

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Application Information

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IPC IPC(8): A61K51/10A61K103/00
Inventor 王正方鹏罗志刚李世红
Owner NANJING PET TRACER
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