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68ga- and 64cu -nodaga-e[c(RGDYK)]2 for use as pet tracers in the imaging of angiogenesis in humans

An angiogenic, 68ga-based technique for use in the field of 68Ga- and 64Cu-NODAGA-E[c(RGDyK)]2 as a PET tracer in human angiogenesis imaging, capable of addressing issues such as low predictability

Pending Publication Date: 2020-07-31
RIGSHOSPITALET
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In this regard, many animal studies have been performed, but due to the low predictability of the applicability of this candidate PET tracer from animals to humans, more human clinical trials are needed for better human angiogenesis tracers

Method used

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  • 68ga- and 64cu -nodaga-e[c(RGDYK)]2 for use as pet tracers in the imaging of angiogenesis in humans
  • 68ga- and 64cu -nodaga-e[c(RGDYK)]2 for use as pet tracers in the imaging of angiogenesis in humans
  • 68ga- and 64cu -nodaga-e[c(RGDYK)]2 for use as pet tracers in the imaging of angiogenesis in humans

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Embodiment Construction

[0035] Since the active substance has never been obtained in isolated form ([ 68 Ga]NODAGA-E[c(RGDyK)] 2 ), but automatically formulates it into the final product. Data on the manufacture, characterization and analysis of active substances are essentially the same as for drug products, so this can be found below. [ 68 Ga]NODAGA-E[c(RGDyK)] 2by using ethanol as a scavenger in the presence of 1.4M sodium acetate buffer (stabilizer against radiolysis) 68 GaCl 3 Labeled acetate NODAGA-E[c(RGDyK)] 2 produced. Similarly, the corresponding 64Cu conjugates can be produced from 64Cu salts.

[0036]

[0037] The product is formulated as an isotonic sterile injectable solution. The labeled product was eluted from the solid phase extraction cartridge (C18) with 50% sterile ethanol solution and then passed through a vented 0.22 μm sterile filter into an empty 10 ml sterile vial. The labeled product is formulated in sterile saline solution which is passed through a C18 cartridge...

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Abstract

There is provided two angiogenesis clinical PET tracers, namely 68Ga-NODAGA- E[c(RGDyK)]2 and 64Cu-NODAGA-E[c(RGDyK)]2 for imaging of neo-angiogenesis in humans.

Description

[0001] field of invention [0002] The present invention relates to the use of [68Ga]NODAGA-E[c(RGDyK)]2 and [64Cu]NODAGA-E[c(RGDyK)]2 for diagnostic imaging in humans using positron emission tomography (PET) . More specifically, the present invention relates to the use of such compounds as tracers for imaging angiogenesis, which in turn is used as a diagnostic measure, risk assessment or as a vascular Companion diagnostics for angiogenesis and / or anti-angiogenic therapy. [0003] Background of the invention [0004] New blood vessels can be formed by two different mechanisms: vasculogenesis or angiogenesis. Angiogenesis is the formation of new blood vessels by branching from existing blood vessels. The main stimulus for this process can be the inability to provide enough nutrients and oxygen to the cells in the tissue (hypoxia). Cells may respond by secreting angiogenic factors, of which there are many; an often cited example is vascular endothelial growth factor (VEGF). ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/04A61K51/08A61K103/00C07F1/08C07F5/00C07K7/64
CPCC07K14/70557C07K7/64G01N33/57407G01N33/57415G01N33/57438G01N33/60G01N2800/324A61K51/088A61K51/082A61K51/0482
Inventor A·克贾尔J·麦德森M·布兰特-拉森J·奥克斯博埃尔
Owner RIGSHOSPITALET