RGD polypeptide radiopharmaceutical for integrin alphav beta3 positive tumor and preparation method thereof

A radiopharmaceutical and radionuclide technology, applied in the field of RGD polypeptide radiopharmaceuticals and their preparation, can solve problems such as insufficient distance

Active Publication Date: 2009-07-08
广东瑞迪奥科技有限公司
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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 t

Method used

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  • RGD polypeptide radiopharmaceutical for integrin alphav beta3 positive tumor and preparation method thereof
  • RGD polypeptide radiopharmaceutical for integrin alphav beta3 positive tumor and preparation method thereof
  • RGD polypeptide radiopharmaceutical for integrin alphav beta3 positive tumor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 111

[0036] This embodiment takes 111 In-DOTA-PEG 4 -E[PEG 4 -c(RGDfK)] 2 (referred to as 111 In-DOTA-3PEG 4 -dimer) RGD polypeptide radiopharmaceutical and its preparation method as an example.

[0037] 111 In-DOTA-PEG 4 -E[PEG 4 -c(RGDfK)] 2 (referred to as 111 In-DOTA-3PEG 4 -dimer) polypeptide radiopharmaceuticals including RGD cyclic peptide dimer, bifunctional chelator DOTA and radionuclide 111 In. The RGD cyclic peptide dimer is the linker PEG 4 Linked with RGD polypeptide monomer c (RGDfK), and then two linked with PEG 4 RGD polypeptide monomer PEG 4 The RGD cyclic peptide dimer synthesized by dimerization of -c(RGDfK), that is, E[PEG 4 -c(RGDfK)] 2 , radionuclide 111 In labels the RGD cyclic peptide dimer with a bifunctional chelating agent DOTA, and a pharmacokinetic modification molecule PEG is also connected between the RGD cyclic peptide dimer and the bifunctional chelating agent 4 , the RGD polypeptide radiopharmaceutical is 111 In-DOTA-PEG 4 -E[PEG ...

Embodiment 2

[0064] In this example, the RGD polypeptide radiopharmaceutical of the present invention uses bifunctional chelating agent DOTA or TETA or its derivatives to label radionuclide 64 Cu, when linker L is PEG 4 、Pharmacokinetic modification molecule PKM is PEG 4 When, the drug of the present invention is 64 Cu-DOTA-PEG4 -E[PEG 4 -c(RGDfK)] 2 ( 64 Cu-DOTA-3PEG 4 -dimer) or 64 Cu-TETA-PEG 4 -E[PEG 4 -c(RGDfK)] 2 ( 64 Cu-TETA-3PEG 4 -dimer), its preparation method is the same as in Example 1. Pharmacokinetic modifier molecules PKM can also be G 2 or G 4 .

[0065] When linker L is G 3 , pharmacokinetic modification molecule PKM is G 3 When, the drug of the present invention is 64 Cu-DOTA-G 3 -E[G 3 -c(RGDfK)] 2 ( 64 Cu-DOTA-3G 3 -dimer) or 64 Cu-TETA-G 3 -E[G 3 -c(RGDfK)] 2 ( 64 Cu-TETA-3G 3 -dimer), its preparation method is the same as above. Pharmacokinetic modifier molecules PKM can also be G 2 or G 4 .

[0066] In this example, the RGD polypeptide...

Embodiment 3

[0068] In this example, the RGD polypeptide radiopharmaceutical of the present invention uses bifunctional chelating agent DOTA or NOTA or its derivatives to label radionuclide 68 Ga. When linker L is PEG 4 、Pharmacokinetic modification molecule PKM is PEG 4 When, the drug of the present invention is 68 Ga-DOTA-PEG 4 -E[PEG 4 -c(RGDfK)] 2 ( 68 Ga-DOTA-3PEG 4 -dimer) or 68 Ga-NOTA-PEG 4 -E[PEG 4 -c(RGDfK)] 2 ( 68 Ga-NOTA-3PEG 4 -dimer), its preparation method is the same as in Example 1. Pharmacokinetic modifier molecules PKM can also be G 2 or G 4 .

[0069] When linker L is G 3 , pharmacokinetic modification molecule PKM is G 3 When, the drug of the present invention is 68 Ga-DOTA-G 3 -E[G 3 -c(RGDfK)] 2 ( 68 Ga-DOTA-3G 3 -dimer) or 68 Ga-NOTA-G 3 -E[G 3 -c(RGDfK)] 2 ( 68 Ga-NOTA-3G 3 -dimer). Pharmacokinetic modifier molecules PKM can also be G 2 or G 4 .

[0070] In this example, the RGD polypeptide radiopharmaceutical of the present invent...

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Abstract

The invention relates to a RGD polypeptide radiopharmaceutical used for integrin alphavbeta3 positive tumor. The RGD polypeptide radiopharmaceutical comprises RGD polypeptide, difunctional Chelator and radioactive Nuclide. The RGD polypeptide is RGD cyclic peptide dimer which is RGD cyclic peptide dimer E(L-c(RGDxK))2 which is synthesized by connecting the coupling agent L with RGD polypeptide monomer c(RGDfK) and dimerizing two RGD polypeptide monomer L-c(RGDfK) which are connected with the coupling agent L. The radioactive nuclide marks the RGD cyclic peptide dimer by one difunctional Chelator, and pharmacokinetic modifying molecule PKM is connected between the RGD cyclic peptide dimer and the difunctional chelator. The RGD polypeptide radiopharmaceutical is Nuclide-Chelator-PKM-E(L-c(RGDxK))2, and the RGD polypeptide radiopharmaceutical is colorless transparent liquid injection.

Description

technical field [0001] The present invention relates to radiopharmaceuticals for tumor diagnosis and treatment, in particular to integrin α v beta 3 RGD polypeptide radiopharmaceutical for positive tumor and preparation method thereof. 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. integrinα 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 prostate cancer, etc.), but no or ver...

Claims

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Application Information

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IPC IPC(8): A61K51/00A61P35/00A61K103/00A61K103/20A61K103/30A61K103/32
Inventor 王凡史继云贾兵
Owner 广东瑞迪奥科技有限公司
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