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.
CN101485891AInactive Publication Date: 2009-07-22PEKING UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
PEKING UNIV
Publication Date
2009-07-22
Estimated Expiration
Not applicable · inactive patent

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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.
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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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