SSTR2靶向药物68Ga-DOTATOC的应用进展

Progress in the application of SSTR2-targeted drug 68Ga-DOTATOC

  • 摘要: 生长抑素受体2(SSTR2)是一类 G蛋白偶联受体,在多种肿瘤中高表达。以SSTR2为靶点进行肿瘤的影像检查可有效诊断肿瘤的发生部位及转移,评估肿瘤的恶性程度、治疗效果及预后,具有良好的临床应用前景。68Ga-1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸-酪氨酸3-奥曲肽(DOTATOC)是一种放射性诊断药物,其通过与SSTR2高亲和力地结合,可用于多种恶性肿瘤的PET定位。笔者对68Ga-DOTATOC的药物信息、研发历程及作用机制进行了梳理,并对其在神经内分泌肿瘤(NEN)及非NEN中的应用进展进行了综述,同时对68Ga-DOTATOC的未来发展进行了展望。

     

    Abstract: Somatostatin receptor 2 (SSTR2) is a class of G protein-coupled receptor that are highly expressed in a variety of tumors. Imaging examination with SSTR2 as the target can effectively diagnose the location and metastasis of the tumor and evaluate the degree of malignancy, treatment efficacy and prognosis of the tumor, which has a good clinical application prospect. 68Ga-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr(3)-octreotide (DOTATOC) is a radiodiagnostic drug that can be used for PET localization of a variety of malignant tumors by binding to SSTR2 with high affinity. The authors sort out the drug information, development history and mechanism of action of 68Ga-DOTATOC, and review the application progress of 68Ga-DOTATOC in neuroendocrine neoplasms (NEN) and non NEN, and the future development prospects of 68Ga-DOTATOC was prospected.

     

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