FAPI在肿瘤放射性核素治疗中的研究进展

Research progress of FAPI in tumor radionuclide therapy

  • 摘要: 成纤维细胞活化蛋白(FAP)在大多数实体瘤中表达上调,成为肿瘤诊疗的热门靶点。FAP靶向药物中的成纤维细胞活化蛋白抑制剂(FAPI)凭借其高亲和力和特异性得到广泛关注,其具有在肿瘤中大量聚集和在正常组织快速清除的特点,适合用作放射性核素靶向治疗的配体。近年来,大量文献报道了以FAPI作为放射性核素治疗配体的研究,相关临床前研究通过药物设计延长了肿瘤滞留时间,改善了药代动力学;而相关临床应用研究则初步证实了FAPI相关放射性核素治疗的有效性和安全性。笔者对FAPI在肿瘤放射性核素治疗中的研究进行综述,以期为后续的相关研究提供参考。

     

    Abstract: Fibroblast activation protein (FAP) is up-regulated in most solid tumors, making it a hot target for cancer diagnosis and therapy. Among FAP-targeting drugs, fibroblast activation protein inhibitor (FAPI) have gained significant attention by virtue of their high affinity and specificity, and are suitable to be used as ligands for radionuclide-targeted therapies due to their high aggregation in tumors and rapid clearance in normal tissues. In recent years, a large number of studies using FAPI as ligands for radionuclide therapy have been reported in the literature, and the relevant preclinical studies have prolonged the tumor retention time and improved the pharmacokinetics by drug design, while the relevant clinical studies have preliminarily demonstrated the effectiveness and safety of FAPI-associated radionuclide therapy. The authors reviewed current research on FAPI in tumor radionuclide therapy, aiming to provid references for subsequent related studies.

     

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