Diagnostic and therapeutic integrated drug targeting tumor integrin α5β1 and its labeled precursor, preparation method and application
By conjugating a labeled precursor with a bicyclic peptide structure with a linker and a chelating agent, a radiotherapeutic drug targeting integrin α5β1 was prepared, solving the problems of insufficient stability and specificity of existing drugs and achieving efficient diagnosis and treatment of tumors and other diseases.
Patent Information
- Application Number
- CN202510076135.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-01-17
- Publication Date
- 2026-07-17
AI Technical Summary
Existing targeted integrin drugs have shortcomings in terms of stability, cell penetration and specificity, making them difficult to use effectively for the diagnosis and treatment of tumors.
A labeled precursor with a bicyclic peptide structure was used to synthesize a polypeptide compound via a solid-phase cyclization method. The compound was then coupled with a linker and a chelating agent to prepare a radiopharmaceutical targeting integrin α5β1. Radionuclide labeling was then used for diagnosis and treatment.
It improves the binding specificity and metabolic stability of drugs to integrin α5β1, reduces hepatotoxicity, and is suitable for integrated diagnosis and treatment of tumors and other diseases with high expression of integrin α5β1.
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