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.

CN122404493APending Publication Date: 2026-07-17INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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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

Technical Problem

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.

Method used

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.

Benefits of technology

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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Abstract

本发明属于医药技术领域,公开了靶向肿瘤整合素α5β1的诊疗一体化药物及其标记前体、制备方法和应用,具体公开了该诊疗药物的制备方法,包括将核素溶液和标记前体混合后得到反应体系,将该反应体系进行孵育处理,制备得到所述诊疗一体化药物的步骤;该标记前体为x‑r‑g结构,其中,x为螯合剂,r为连接臂,g为多肽化合物,该连接臂的氨基侧与该螯合剂相连,该连接臂的羧基侧与该多肽化合物的N端第一个氨基酸的氨基相连。本发明制备得到的诊疗一体化药物具有良好的体内稳定性,与肿瘤α5β1靶点结合特异性好,肿瘤滞留时间较长,在多肽靶向核药的肿瘤诊疗一体化中具有重要的临床参考价值。
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