A targeting radioactive drug of CSPG4 and a preparation method and use thereof

By preparing radiopharmaceuticals targeting CSPG4 and combining them with PET/SPECT imaging technology, the problem of the inability to detect CSPG4 in real time and dynamically in existing technologies has been solved, enabling specific imaging and treatment of CSPG4-positive tumors.

CN122272850APending Publication Date: 2026-06-26FUDAN UNIV SHANGHAI CANCER CENT
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
FUDAN UNIV SHANGHAI CANCER CENT
Filing Date
2024-12-25
Publication Date
2026-06-26

AI Technical Summary

Technical Problem

Existing CSPG4 expression detection methods cannot provide real-time, dynamic, and comprehensive visualization at the in vivo level, thus failing to achieve early and accurate diagnosis of tumors and evaluation of treatment efficacy.

Method used

Radiopharmaceuticals targeting CSPG4 are prepared by binding radionuclides with linear polypeptides consisting of 10 or 11 amino acids and bifunctional chelating groups to form diagnostic or therapeutic drugs. PET/SPECT imaging technology is then used to achieve specific imaging and treatment of CSPG4-positive tumors.

Benefits of technology

It enables specific nuclear medicine imaging and treatment of CSPG4-positive tumors, has good pharmacokinetic properties, can clearly visualize a variety of tumors, and has the potential for diagnosis and treatment of tumors with high CSPG4 expression.

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Abstract

This invention discloses a radiopharmaceutical targeting chondroitin sulfate proteoglycan 4 (CSPG4) with a linear polypeptide and its preparation method. The radiopharmaceutical comprises a CSPG4-targeting polypeptide, a radionuclide, and a bifunctional chelating agent. The radionuclide is labeled with the CSPG4-targeting polypeptide by the bifunctional chelating agent, wherein the targeting polypeptide has a linear structure consisting of 10 or 11 amino acids. This series of radiopharmaceuticals can achieve specific nuclear medicine positron emission tomography (PET) or single-photon emission computed tomography (SPECT) imaging diagnosis of CSPG4-positive lesions, such as tumors, autoimmune diseases, cardiovascular diseases, and neurodegenerative diseases, in vivo.
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