Radioactive nuclide marked RGD polypeptide medicament and preparation method thereof

A radionuclide and labeling technology, applied in the field of radionuclide-labeled RGD polypeptide drugs and their preparation, can solve problems such as insufficient distance, achieve good diagnosis and treatment effects, enhance binding affinity, and improve pharmacokinetic properties.

Inactive Publication Date: 2009-07-22
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently reported RGD cyclic peptide dimer E[c(RGDxK)] 2 (E represents glutamic acid, c represents cyclization, R represents arginine, G represents glycine, D represents aspartic acid, x represents f or y, representing phenylalanine or tyrosine respectively), two of them The distance between the RGD modules is 6 bonds, because the distance is not long enough, so E[c(RGDxK)] 2 It is difficult for the two RGD motifs of the cell surface to be adjacent to the two integrin α at the same time v beta 3 Receptor binding (see figure 1 )

Method used

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  • Radioactive nuclide marked RGD polypeptide medicament and preparation method thereof
  • Radioactive nuclide marked RGD polypeptide medicament and preparation method thereof
  • Radioactive nuclide marked RGD polypeptide medicament and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] In this example, the radionuclide 99m Tc-labeled RGD peptide drug 99m Tc-MAG 2 -PEG 4 -E[PEG 4 -c(RGDfK)] 2 (referred to as 99m Tc-MAG 2 -3PEG 4 -dimer) and its preparation method as an example.

[0034] exist 99m Tc-MAG 2 -PEG 4 -E[PEG 4 -c(RGDfK)] 2 Among them, the RGD cyclic peptide dimer is the linker PEG 4 Linked with RGD polypeptide monomer c (RGDfK), and then two linked with PEG 4 The RGD cyclic peptide dimer synthesized by the dimerization of the RGD polypeptide monomer, that is, E[PEG 4 -c(RGDfK)] 2 , radionuclide 99m Tc through a bifunctional chelator MAG 2 labeling the RGD cyclic peptide dimer, and a pharmacokinetic modification molecule PEG is also connected between the RGD cyclic peptide dimer and the bifunctional chelating agent 4 , the radionuclide-labeled RGD polypeptide drug is a colorless transparent liquid injection.

[0035] The drug first combines four molecules of polyethylene glycol (PEG 4 , PEG=Polyethylene glycol) is connecte...

Embodiment 2

[0055] In this example, the radionuclide 188 Re-labeled RGD peptide drug 188 Re-MAG 2 -PEG 4 -E[PEG 4 -c(RGDfK)] 2 (referred to as 188 Re-MAG 2 -3PEG 4 -dimer) as an example.

[0056] exist 188 Re-MAG 2 -PEG 4 -E[PEG 4 -c(RGDfK)] 2 Among them, the RGD cyclic peptide dimer is the linker PEG 4 Linked with RGD polypeptide monomer c (RGDfK), and then two linked with PEG 4 The RGD cyclic peptide dimer synthesized by the dimerization of the RGD polypeptide monomer, that is, E[PEG 4 -c(RGDfK)] 2 , radionuclide 188 Re through a bifunctional chelating agent MAG 2 labeling the RGD cyclic peptide dimer, and a pharmacokinetic modification molecule PEG is also connected between the RGD cyclic peptide dimer and the bifunctional chelating agent 4 , the radionuclide-labeled RGD polypeptide drug is a colorless transparent liquid injection.

[0057] The radionuclide-labeled RGD polypeptide drug of the present embodiment is 188 Re-MAG 2 -PEG 4 -E[PEG 4 -c(RGDfK)]2 , the dr...

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Abstract

The invention relates to a radionuclide-marked RGD polypeptide medicine and a preparation method thereof. The medicine comprises RGD polypeptide, a bifunctional Chelator and radioactive Nuclide, wherein the RGD polypeptide is RGD cyclic peptide dimer, namely E(L-c(RGDxK))2, which is synthesized by connecting a connecting agent L and an RGD polypeptide monomer and dimerizing two RGD polypeptide monomers connected with the connecting agent L; the radioactive Nuclide marks the RGD cyclic peptide dimer through the bifunctional Chelator; and a pharmacokinetic modified molecule PKM is also connected between the RGD cyclic peptide dimer and the bifunctional Chelator. The radionuclide-marked RGD polypeptide medicine is Nuclide-Chelator-PKM-E(L-c(RGDxK))2, and is a colorless and transparent liquid injection solution. The radionuclide-marked RGD polypeptide medicine is used for diagnosing and treating integrin alpha v beta 3 positive tumor.

Description

technical field [0001] The present invention relates to radiopharmaceuticals for tumor diagnosis and treatment, in particular to integrin α v beta 3 Radionuclide-labeled RGD polypeptide medicine for positive tumor diagnosis and treatment and its preparation method. Background technique [0002] A critical part of the tumor growth process is tumor angiogenesis. No new angiogenic tumors can no longer grow after reaching a size of a few centimeters. Tumor angiogenesis is regulated by various protein molecules, including integrin α v beta 3 . integrin alpha v beta 3 It is an extracellular matrix receptor, which is a heterodimeric transmembrane glycoprotein composed of α and β subunits. integrin alpha v beta 3 It is an important member of the integrin family. As one of the molecular markers related to neovascularization, it is highly expressed on the surface of neovascular endothelial cells and some tumor cells (neuroblastoma, osteosarcoma, glioblastoma , breast and pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K9/08A61P35/00A61K103/10
Inventor 王凡史继云贾兵
Owner PEKING UNIV
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