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Targeted imaging and/or therapy using the [3+2] azide-alkyne cycloaddition

A targeting and imaging technology, which can be applied in preparations for in vivo experiments, nano-drugs, medical preparations with non-active ingredients, etc., can solve the problem of low application of pharmacokinetic imaging

Inactive Publication Date: 2009-08-19
KONINK PHILIPS ELECTRONICS NV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] Pretargeting techniques have proven useful for antibody-based imaging because although antibodies are highly selective and specific for antigens, their pharmacokinetics are often too low for imaging applications [Sung et al. (1992), Cancer Res. 52, 377-384; Juweid et al. (1992) Cancer Res. 52, 5144-5153]

Method used

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  • Targeted imaging and/or therapy using the [3+2] azide-alkyne cycloaddition
  • Targeted imaging and/or therapy using the [3+2] azide-alkyne cycloaddition
  • Targeted imaging and/or therapy using the [3+2] azide-alkyne cycloaddition

Examples

Experimental program
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Embodiment approach

[0070] According to one embodiment, the invention is used for targeted imaging. According to this embodiment, imaging of a specific primary target is achieved by specific binding of the primary targeting moiety of the targeting probe and detection of this binding using a detectable label.

[0071] According to the present invention, the primary target may be selected from any suitable target in the human or animal body or on a pathogen or parasite, including, for example, cells such as cell membranes and cell walls, receptors such as cell membrane receptors, intracellular structures such as the Golgi apparatus or mitochondrial enzymes, receptors, DNA, RNA, viruses or virus particles, antibodies, proteins, carbohydrates, monosaccharides, polysaccharides, cytokines, hormones, steroids, somatostatin receptors, monoamine oxidase, muscarinic sex receptors, cardiac sympathetic nervous system, leukotriene receptors, e.g. on leukocytes, urokinase plasminogen activator receptor (uPAR),...

Embodiment 1

[0130] Example 1: Pretargeted Imaging of Neuroendocrine Tumors

[0131] Injecting into the subject a targeting probe comprising a somatostatin receptor-binding peptide; e.g., according to figure 2 Representative primary targeting moieties are attached, for example, to an azido group as a secondary target. Imaging probes are injected into subject (e.g. animal or human), the imaging probe includes 18 F-label (ie radioactivity attached to the cyclooctynyl group which acts as a secondary targeting moiety); here it binds the immobilized azide. Thus, the presence of the neuroendocrine tumor can be visualized by radioisotopes that provide contrast. Alternatively, the secondary targeting moiety of the imaging probe contains an azide and cyclooctyne is the cyclooctyne in the targeting probe. Cyclooctyne-labeled (2) amino acids or azide-labeled (3) amino acids can be introduced into receptor binding peptides for the preparation of targeting probes.

[0132]

Embodiment 2

[0133] Example 2: Treatment Planning for Pretargeted Imaging of Breast Cancer Tissue

[0134] A targeting probe consisting of an azide-estrogen derivative is administered to a breast cancer patient. After estrogen receptor binding, it will couple to 99m Cyclooctynyl implantation of the Tc chelate acts as an imaging probe and binds and images immobilized azide. Several breast cancer-targeting structures functionalized with azide are known. However, none of these have been used for imaging methods based on [3+2]azide-alkyne cycloadditions.

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Abstract

The use of a selective chemical and bioorthogonal reaction providing a covalent ligation such as the [3+2] cycloaddition, in targeted molecular imaging and therapy is presented, more specifically with interesting applications for pre-targeted imaging or therapy. Current pre-targeted imaging is hampered by the fact that it relies solely on natural / biological targeting constructs (biotin / streptavidin). Size considerations and limitations associated with their endogenous nature severely limit the number of applications. The present invention describes how the use of an abiotic, bio-orthogonal reaction which forms a stable adduct under physiological conditions, by way of a small or undetectable bond, can overcome these limitations.

Description

field of invention [0001] The present invention relates to novel compounds, kits and methods for medical imaging and therapy. The present invention also relates to novel compounds for pre-targeted imaging and / or therapy, methods of their production and their use. Background of the invention [0002] Chemoselective linkages based on [3+2] azide-alkyne cycloadditions are known in the art ( figure 1 ). [0003] In medical imaging modalities, the use of contrast agents (substances that increase image contrast, for example between different organs or tissues or between normal and abnormal tissues) is well established. Imaging specific molecular targets associated with disease allows for earlier diagnosis of disease and better disease. Therefore, of particular interest are contrast agents that are preferentially distributed to specific parts of the body, such as tumor cells, by active targeting. Such active targeting is achieved by directly or indirectly binding the contrast-e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K49/00A61K51/02
CPCA61K47/48353A61K51/0495A61K49/10A61K47/4813A61K47/48061A61K51/04A61K47/48123B82Y5/00A61K49/14A61K47/48092A61K49/085A61K47/48084A61K47/545A61K47/548A61K47/549A61K47/554A61K47/555A61K47/665
Inventor M·S·罗比亚尔H·格吕尔
Owner KONINK PHILIPS ELECTRONICS NV
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