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68ga-labeled peptide-based radiopharmaceuticals

A residue, pharmaceutical technology, applied in the αvβ3 integrin receptor, peptide-based compounds as target carriers, the field of integrin receptors

Inactive Publication Date: 2009-09-09
GE HEALTHCARE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, peptides containing multiple cysteine ​​residues suffer from the disadvantage that multiple disulfide isomers may exist

Method used

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  • 68ga-labeled peptide-based radiopharmaceuticals
  • 68ga-labeled peptide-based radiopharmaceuticals
  • 68ga-labeled peptide-based radiopharmaceuticals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0064]

[0065] In most cases it is preferred that the amino acids in the peptide are all in the L-configuration. However, in some embodiments of the invention, one, two, three or more amino acids in the peptide are preferably in the D-configuration. Inclusion of this D-configuration amino acid can have a significant effect on the serum stability of the compound. According to the present invention, any amino acid residue as defined in formula I may preferably represent a naturally occurring amino acid and be independently either of the D or L conformation.

[0066] Some compounds of the present invention are high affinity RGD-based carriers. The term "high-affinity RGD-based carrier" as used herein refers to a compound having a Ki < 10 nM and preferably < 5 nM in a competitive binding assay for αvβ3 integrin, wherein said Ki value is determined by binding to a known high-affinity ligand. Cyclostatin competition was determined. Methods for performing such competition assa...

Embodiment

[0118] Ga of Cys2-6 68 mark;

[0119] c[CH 2 CO-Lys(DOTA)-Cys-Arg-Gly-Asp-Cys-Phe-Cys]-CCX 6 -NH 2 )

[0120] (DOTA-AH-110847-02)

[0121]

[0122] Material

[0123] DOTA-AH-110847-02(C 66 h 105 N 19 o 24 S 3 , Molecular Weight = 1644.88) was received from Amersham Health (Dept. of Synthetic Chemistry, Amersham Health, Olso, Norway). HEPES (4-(2 hydroxyethyl)piperazine-1-ethanesulfonic acid) and double distilled hydrochloric acid (Riedel de ) were obtained from Sigma-Aldrich Sweden (Stockholm, Sweden). Monosodium hydrogen phosphate, disodium hydrogen phosphate and trifluoroacetic acid (TFA) were obtained from Merck (Darmstadt, Germany). Purchased chemicals were used without further purification. Deionized water (18.2 MΩ) prepared with a Purelab Maxima Elga system (Bucks, UK) was used in all reactions.

[0124] 68 Preparation of Ga

[0125] 68 Ga(T 1 / 2 = 68min, β + =89% and EC=11%) can be obtained from 68 Ga / 68 Ge generator system...

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Abstract

The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.

Description

field of invention [0001] The present invention relates to novel radiolabeled peptide-based compounds and their use in diagnostic imaging, pre-treatment dosimetry, treatment planning, treatment monitoring or radiotherapy. More particularly the present invention relates to the use of such peptide-based compounds as targeting vectors that bind to receptors associated with angiogenesis, in particular integrin receptors such as alpha v beta 3 Integrin receptors. Such imaging agents are thus useful in the diagnosis of, for example, malignancies, heart disease, endometriosis, inflammation-related diseases, rheumatoid arthritis, and Kaposi's sarcoma. Furthermore such reagents are useful in pre-treatment dosimetry, treatment planning and treatment monitoring for these diseases. Background of the invention [0002] New blood vessels can form by two different mechanisms: vasculogenesis or angiogenesis. Angiogenesis is the formation of new blood vessels by branching from existing b...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61P35/00C07K7/56
CPCC07K7/56A61K51/088A61P1/02A61P1/04A61P1/16A61P15/00A61P17/00A61P17/06A61P19/02A61P25/00A61P27/02A61P29/00A61P35/00A61P35/04A61P43/00A61P9/00A61P9/10
Inventor B·朗斯特伦I·维利克彦M·贝里斯特伦O·林赫
Owner GE HEALTHCARE LTD