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A comparison of [18F]AlF- and 68Ga-labeled dual targeting heterodimer FAPI-RGD in malignant tumor: preclinical evaluation and pilot clinical PET/CT imaging

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作者：
Liu Nan[1] ; Wan Qiang[2] ; Wu Xiaoming[3] ; Zhao Tianzhi[4,5,6] ; Jakobsson Vivianne[4,5,6] ; Yuan Hongmei[7] ; Chen Xiaoyuan[4,5,6,8,9] ; Zhang Jingjing[4,5,6] ; Zhang Wei[1] ;
机构： [1]Department of Nuclear Medicine, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 610072, China. [2]Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, Luzhou, 646000, China. [3]College of Nuclear Science and Technology, Harbin Engineering University, Harbin, 150001, China. [4]Department of Diagnostic Radiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 119074, Singapore. [5]Clinical Imaging Research Centre, Centre for Translational Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117599, Singapore. [6]Nanomedicine Translational Research Program, NUS Center for Nanomedicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117597, Singapore. [7]Department of Pharmaceutics, School of Pharmacy, Southwest Medical University, Jiangyang District, Luzhou, 646000, China. [8]Department of Diagnostic Radiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 119074, Singapore. [9]Clinical Imaging Research Centre, Centre for Translational Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117599, Singapore. [10]Nanomedicine Translational Research Program, NUS Center for Nanomedicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117597, Singapore. [11]Departments of Surgery, Chemical and Biomolecular Engineering, and Biomedical Engineering, Yong Loo Lin School of Medicine and College of Design and Engineering, National University of Singapore, Singapore, 119074, Singapore. [12]Institute of Molecular and Cell Biology, Agency for Science, Technology, and Research (A*STAR), National University of Singapore, 61 Biopolis Drive, Proteos, Singapore, 138673, Singapore. [13]Department of Diagnostic Radiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 119074, Singapore. [14]Clinical Imaging Research Centre, Centre for Translational Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117599, Singapore. [15]Nanomedicine Translational Research Program, NUS Center for Nanomedicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117597, Singapore. [16]Department of Nuclear Medicine, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 610072, China.
出处：
DOI： 10.1007/s00259-023-06587-5
ISSN：

关键词： [18F]AlF- radiolabeling PET imaging Heterodimer Fibroblast activation protein Integrin αvβ3 FAPI-RGD

摘要：
Due to the heterogeneity of tumors, strategies to improve the effectiveness of dual-targeting tracers in tumor diagnostics have been intensively practiced. In this study, the radiolabeled [18F]AlF-NOTA-FAPI-RGD (denoted as [18F]AlF-LNC1007), a dual-targeting heterodimer tracer targeting both fibroblast activation protein (FAP) and integrin αvβ3 to enhance specific tumor uptake and retention, was synthesized and evaluated. The tracer was compared with [68Ga]Ga-LNC1007 in preclinical and clinical settings.The preparation of [18F]AlF- and 68Ga-labeled FAPI-RGD was carried out with an optimized protocol. The stability was tested in PBS and fetal bovine serum (FBS). Cellular uptake and in vivo distribution of the two products were compared and carried out on the U87MG cell line and its xenograft model. The safety and dosimetry of [18F]AlF-LNC1007 PET/CT scan were evaluated in six patients with malignant tumors.Two radiolabeling protocols of [18F]AlF-/[68Ga]Ga-LNC1007 were developed and optimized to give a high yield of tracers with good stability. In vivo microPET images showed that the two tracers exhibited comparable pharmacokinetic characteristics, with high tumor uptake and prolonged tumor retention. In vivo distribution data showed that the target-to-non-target ratios of [18F]AlF-LNC1007 were similar to[68Ga]Ga-LNC1007. A total of six patients underwent [18F]AlF-LNC1007 PET/CT evaluation while two had head-to-head [18F]FDG PET/CT scans. The total body effective dose was 9.94E-03 mSv/MBq. The biodistribution curve showed optimal normal organ uptake with high tumor uptake and long retention of up to 3h p.i., and notably, the tumor-to-background ratio increased over time.We successfully prepared an [18F]AlF-LNC1007 dual-targeting PET probe with comparable performances as [68Ga]Ga-LNC1007. With prolonged tumor retention and tumor specificity, it produced good imaging quality in preclinical and clinical translational studies, indicating that [18F]AlF-LNC1007 is a promising non-invasive tracer for detecting tumors expressing FAP and/or integrin avβ3, with the prospect of clinical implementation.© 2024. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.

基金：
This work was supported by the Natural Science Foundation of Sichuan Province of China (2023NSFSC0635), the National University of Singapore (NUHSRO/2021/097/Startup/13; NUHSRO/ 2020/133/Startup/08; NUHSRO/2023/008/NUSMed/TCE/ LOA), National Medical Research Council (MOH-001334–00, MOH- 001388–00, MOH-001254–01, CG21APR1005), the Singapore Ministry of Education (FY2022) Tier 1 Grant (NUHSRO/2022/093/T1/Seed- Sep/06), and the NUS School of Medicine Nanomedicine Translational Research Programme (NUHSRO/2021/034/TRP/09/Nanomedicine).
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外文
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中科院(CAS)分区：
出版当年[2023]版：
大类 | 1 区 医学
小类 | 1 区 核医学
最新[2023]版：
大类 | 1 区 医学
小类 | 1 区 核医学
JCR分区：
出版当年[2023]版：
Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING
最新[2023]版：
Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING

影响因子： 最新[2023版] 最新五年平均 出版当年[2023版] 出版当年五年平均 出版前一年[2023版]

第一作者：
第一作者机构： [1]Department of Nuclear Medicine, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 610072, China.
共同第一作者：
通讯作者：
通讯机构： [4]Department of Diagnostic Radiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 119074, Singapore. [5]Clinical Imaging Research Centre, Centre for Translational Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117599, Singapore. [6]Nanomedicine Translational Research Program, NUS Center for Nanomedicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117597, Singapore. [8]Department of Diagnostic Radiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 119074, Singapore. [9]Clinical Imaging Research Centre, Centre for Translational Medicine, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, 117599, Singapore.
推荐引用方式(GB/T 7714)：
Liu Nan,Wan Qiang,Wu Xiaoming,et al.A comparison of [18F]AlF- and 68Ga-labeled dual targeting heterodimer FAPI-RGD in malignant tumor: preclinical evaluation and pilot clinical PET/CT imaging[J].EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING.2024,51(6):1685-1697.doi:10.1007/s00259-023-06587-5.
APA：
Liu Nan,Wan Qiang,Wu Xiaoming,Zhao Tianzhi,Jakobsson Vivianne...&Zhang Wei.(2024).A comparison of [18F]AlF- and 68Ga-labeled dual targeting heterodimer FAPI-RGD in malignant tumor: preclinical evaluation and pilot clinical PET/CT imaging.EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,51,(6)
MLA：
Liu Nan,et al."A comparison of [18F]AlF- and 68Ga-labeled dual targeting heterodimer FAPI-RGD in malignant tumor: preclinical evaluation and pilot clinical PET/CT imaging".EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING 51..6(2024):1685-1697

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