RADIOPHARMACEUTICALS BASED ON FIBROBLAST ACTIVATION PROTEIN INHIBITORS IN ONCOLOGICAL PRACTICE.

D O Dzhuzha, S D Myasoyedov
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Abstract

The review is devoted to the application of the new perspective class of radionuclide tracers, based on inhibitors of the fibroblast activation protein (FAP), which is a marker of cancer-associated fibroblasts of microenvironment of most malignant tumors. FAP inhibitors (FAPI) can be labeled by a wide spectrum of radionuclides, which can provide both radionuclide diagnostics and radionuclide therapy. It was showed, that the diagnostic efficacy of FAPI positron emission tomography/computed tomography (PET/CT) in various cancers is similar to 18F-fluorodesoxyglu-cose-PET/CT or superior. The FAPI radiopharmaceuticals (RP) have some advantage compared to 18F-fluorodesoxy-glucose (FDG): no need for special preparation and diet, fast imaging with high contrast, and increased sensitivity in region with high glucose metabolism. FAPI-PET/CT may be an important addition to conventional methods in all stages of diagnostic process in oncology, especially when 18F-FDG cannot be used. It is need to further wide prospective investigations for assessing of diagnostic efficacy of FAPI-RP and determination of indications for its using.

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基于成纤维细胞活化蛋白抑制剂的放射性药物在肿瘤治疗中的应用。
这篇综述专门介绍了基于成纤维细胞活化蛋白(FAP)抑制剂的放射性核素示踪剂新视角类别的应用,成纤维细胞活化蛋白是大多数恶性肿瘤微环境中癌症相关成纤维细胞的标记物。FAP 抑制剂(FAPI)可被多种放射性核素标记,既可用于放射性核素诊断,也可用于放射性核素治疗。研究表明,FAPI 正电子发射断层扫描/计算机断层扫描(PET/CT)对各种癌症的诊断效果与 18F-氟脱氧葡萄糖-PET/CT 相似,甚至更好。与 18F-氟脱氧葡萄糖(FDG)相比,FAPI 放射性药物(RP)具有一些优势:无需特殊准备和饮食,成像速度快,对比度高,对高糖代谢区域的敏感性更高。在肿瘤学诊断过程的各个阶段,尤其是无法使用 18F-FDG 时,FAPI-PET/CT 可作为传统方法的重要补充。需要进一步开展广泛的前瞻性研究,以评估 FAPI-RP 的诊断效果并确定其使用适应症。
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Problemy radiatsiinoi medytsyny ta radiobiolohii
Problemy radiatsiinoi medytsyny ta radiobiolohii Medicine-Radiology, Nuclear Medicine and Imaging
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