典型文献
Preclinical evaluation and pilot clinical study of[18F]AlF-labeled FAPI-tracer for PET imaging of cancer associated fibroblasts
文献摘要：
In recent years,fibroblast activation protein(FAP)has emerged as an attractive target for the diag-nosis and radiotherapy of cancers using FAP-specific radioligands.Herein,we aimed to design a novel 18F-labeled FAP tracer([18F]A1F-P-FAPI)for FAP imaging and evaluated its potential for clinical application.The[18F]A1F-P-FAPI novel tracer was prepared in an automated manner within 42 min with a non-decay cor-rected radiochemical yield of 32±6％(n=8).Among A549-FAP cells,[1 8F]A1F-P-FAPI demonstrated spe-cific uptake,rapid internalization,and low cellular efflux.Compared to the patent tracer[18F]FAPI-42,[18F]A1F-P-FAPI exhibited lower levels of cellular efflux in the A549-FAP cells and higher stability in vivo.Micro-PET imaging in the A549-FAP tumor model indicated higher specific tumor uptake of[18F]A1F-P-FAPI(7.0±1.0％ID/g)compared to patent tracers[18F]FAPI-42(3.2±0.6％ID/g)and[68Ga]Ga-FAPI-04(2.7±0.5％ID/g).Furthermore,in an initial diagnostic application in a patient with nasopharyngeal cancer,[18F]A1F-P-FAPI and[18F]FDG PET/CT showed comparable results for both primary tumors and lymph node metastases.These results suggest that[18F]A1F-P-FAPI can be conveniently prepared,with promising charac-teristics in the preclinical evaluation.The feasibility of FAP imaging was demonstrated using PET studies.
文献关键词：
中图分类号：
作者姓名：
Kongzhen Hu;Junqi Li;Lijuan Wang;Yong Huang;Li Li;Shimin Ye;Yanjiang Han;Shun Huang;Hubing Wu;Jin Su;Ganghua Tang
作者机构：
Department of Nuclear Medicine,Nanfang Hospital,Southern Medical University,Guangzhou 510515,China;Shenzhen International Institute for Biomedical Research,Shenzhen 518116,China;National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital&Shenzhen Hospital,Chinese Academy of Medical Sciences and Peking Union Medical College,Shenzhen 518116,China;State Key Laboratory of Respiratory Disease,National Clinical Research Center for Respiratory Disease,Guangzhou Institute of Respiratory Health,the First Affiliated Hospital of Guangzhou Medical University,Guangzhou 510182,China
文献出处：
引用格式：
[1]Kongzhen Hu;Junqi Li;Lijuan Wang;Yong Huang;Li Li;Shimin Ye;Yanjiang Han;Shun Huang;Hubing Wu;Jin Su;Ganghua Tang-.Preclinical evaluation and pilot clinical study of[18F]AlF-labeled FAPI-tracer for PET imaging of cancer associated fibroblasts)[J].药学学报（英文版）,2022(02):867-875
A类：
radioligands,A1F
B类：
Preclinical,evaluation,pilot,study,18F,AlF,labeled,FAPI,PET,imaging,associated,fibroblasts,In,recent,years,activation,protein,has,emerged,attractive,target,nosis,radiotherapy,cancers,using,specific,Herein,aimed,design,novel,evaluated,its,potential,application,was,prepared,automated,manner,within,decay,cor,rected,radiochemical,yield,Among,A549,cells,demonstrated,uptake,rapid,internalization,cellular,efflux,Compared,patent,exhibited,lower,levels,higher,stability,vivo,Micro,model,indicated,ID,compared,tracers,68Ga,Furthermore,initial,diagnostic,patient,nasopharyngeal,FDG,showed,comparable,results,both,primary,tumors,lymph,node,metastases,These,suggest,that,conveniently,promising,charac,teristics,preclinical,feasibility,studies
AB值：
0.446901
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