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Method of radio-labelling biomolecules

A radioactive labeling, biomolecule technology, applied in the directions of radioactive physical shape, radioactive carrier, radioactive preparation in vivo, etc., can solve the problems of non-imaging agent, low tumor ratio, low activity, etc.

Inactive Publication Date: 2005-06-29
VISTATEC YORK
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This study shows that although some uptake of Tc-sTf by tumor cells occurs (0.36% of the injected dose), this uptake is still very low compared to the activity of non-specific binding
In fact the authors claim that Tc-labeled transferrin does not appear to be a suitable imaging agent due to the low tumor to blood ratio after injection

Method used

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  • Method of radio-labelling biomolecules
  • Method of radio-labelling biomolecules
  • Method of radio-labelling biomolecules

Examples

Experimental program
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Effect test

Embodiment 1

[0097] Apo-lactotransferrin (aLf) was pre-incubated with 35 [mu]M of 2-mercaptoethanol overnight at 4[deg.]C prior to use and then labeled with 1.6 [mu]M of labeled protein at 7% efficiency. Labeled proteins were repeatedly washed and 92% of the label was still attached after 60 min incubation in PBS. The results are shown in Table 3.

Embodiment 2

[0099] Apotransferrin (aTf) was pre-incubated overnight at 4°C with various concentrations of 2.6 μM, 12 μM and 26 μM 2-mercaptoethanol (2-ME) before use, yielding 8%, 25% and 60% labeling, respectively efficiency. Repeating the lowest concentration of 2-ME gave labeling efficiencies of 7% and 8.5%. After washing and 90 min incubation at 37°C in PBS, 97% of the highest labeled concentration of aTf remained on the protein. The results are shown in Table 3.

Embodiment 3

[0101] DTPA is an exemplary chelating moiety in the prior art and forms stable chelates with various metals. The amount of labeling on aTf decreased by about 10% after 2 h incubation in the presence of DTPA, from 97% to 87%, indicating removal of weakly bound radionuclides from biomolecules.

[0102] Incubation of aTf in acidic conditions also resulted in a reduction in the amount of bound radionuclides. The amount of label on the protein decreased by about 23% after 2 hours of incubation at pH 5, from 97% to 75%, see Table 4.

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Abstract

A method of radiolabeling a biomolecule comprising contacting the biomolecule with a source of a radionuclide, such as technetium, in the presence of a weak transfer ligand, and then optionally passing the mixture through a size exclusion filtration step. Also claimed are kits comprising the novel composition, in particular lactotransferrin coupled to a chemotherapeutic agent, and the use thereof.

Description

[0001] The present invention relates to methods of labeling biomolecules with radionuclides, in particular, but not exclusively, technetium, kits comprising components / elements for carrying out the methods, novel compositions and uses thereof. Background of the Invention [0002] Radiolabeling of biomolecules is used as a means of tracking and detecting the pathway or location of specific biomolecules when they are administered to a patient or individual. Such radiolabeled biomolecules emit detectable and precise targeting of low-level radiation to organs or other substrates. Radionuclides, such as rhenium-186m and especially technetium-99m, are useful for the labeling of biomolecules because they are known to form relatively stable bonds with a variety of biomolecules. In quantitative terms, technetium (Tc) compounds are by far the most important radiopharmaceuticals used, with an estimated market share of greater than 80%. [0003] For radiomedical purposes, isotopes 99 Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/337A61K31/704A61K33/24A61K38/00A61K45/00A61K48/00A61K51/00A61K51/08A61K51/12A61P7/02A61P9/10A61P31/00A61P33/00A61P35/00A61P43/00
CPCA61K51/08A61K51/088A61K51/1282A61P31/00A61P33/00A61P35/00A61P43/00A61P7/02A61P9/10
Inventor P·瓦尔顿T·史密斯
Owner VISTATEC YORK