Automatic Production and Preliminary PET Imaging of a New Imaging Agent [18F]AlF-FAPT
BackgroundFibroblast activating protein (FAP) has become an important target for cancer diagnostic imaging and targeted radiotherapy. In particular, [18F]FAPI-42 has been successfully applied to positron emission tomography (PET) imaging of various tumors. However, it exhibits high hepatobiliary met...
| Main Authors: | , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Frontiers Media S.A.
2022-01-01
|
| Series: | Frontiers in Oncology |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/articles/10.3389/fonc.2021.802676/full |
| _version_ | 1828147477331574784 |
|---|---|
| author | JiaWen Huang LiLan Fu KongZhen Hu Shun Huang YanJiang Han Run Lin WanBang Xu Ganghua Tang Yonghui Huang |
| author_facet | JiaWen Huang LiLan Fu KongZhen Hu Shun Huang YanJiang Han Run Lin WanBang Xu Ganghua Tang Yonghui Huang |
| author_sort | JiaWen Huang |
| collection | DOAJ |
| description | BackgroundFibroblast activating protein (FAP) has become an important target for cancer diagnostic imaging and targeted radiotherapy. In particular, [18F]FAPI-42 has been successfully applied to positron emission tomography (PET) imaging of various tumors. However, it exhibits high hepatobiliary metabolism and is thus not conducive to abdominal tumor imaging. This study reports a novel 18F-labeled FAP inhibitor, [18F]AlF-FAPT, a better FAPI imaging agent than [18F]FAPI-42.Materials and MethodsThe precursor of [18F]AlF-FAPT (NOTA-FAPT) was designed and synthesized using the standard FMOC solid phase synthesis method. [18F]AlF-FAPT was subsequently synthesized and radiolabeled with 18F using the AllInOne synthesis module. Dynamic MicroPET and biodistribution studies of [18F]AlF-FAPT were then conducted in xenograft tumor mouse models to determine its suitability.ResultsThe precursors NOTA-FAPT were obtained with a chemical purity of > 95%. [18F]AlF-FAPT was synthesized automatically using the cassette-based module AllInOne within 40 min. The non-decay corrected radiochemical yield was 25.0 ± 5.3% (n=3). In vivo imaging and biodistribution studies further demonstrated that compared with [18F]-FAPI-42, [18F]AlF-FAPT had a lower hepatobiliary uptake than [18F]FAPI-42, which was advantageous for imaging abdominal tumors.Conclusion[18F]AlF-FAPT can be synthesized automatically using a one-step method of aluminum fluoride. Collectively, [18F]AlF-FAPT is a better FAPI imaging agent than [18F]FAPI-42. This study proves the feasibility of using [18F]AlF-FAPT as a new radioactive tracer for PET imaging. |
| first_indexed | 2024-04-11T21:00:55Z |
| format | Article |
| id | doaj.art-41a4de59888743e6bda0b1438260bcc9 |
| institution | Directory Open Access Journal |
| issn | 2234-943X |
| language | English |
| last_indexed | 2024-04-11T21:00:55Z |
| publishDate | 2022-01-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Oncology |
| spelling | doaj.art-41a4de59888743e6bda0b1438260bcc92022-12-22T04:03:29ZengFrontiers Media S.A.Frontiers in Oncology2234-943X2022-01-011110.3389/fonc.2021.802676802676Automatic Production and Preliminary PET Imaging of a New Imaging Agent [18F]AlF-FAPTJiaWen Huang0LiLan Fu1KongZhen Hu2Shun Huang3YanJiang Han4Run Lin5WanBang Xu6Ganghua Tang7Yonghui Huang8Department of Interventional Radiology, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, ChinaDepartment of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, ChinaDepartment of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, ChinaDepartment of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, ChinaDepartment of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, ChinaDepartment of Interventional Radiology, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, ChinaDepartment of Traditional Chinese Medicine, Guangdong Institute for Drug Control, Guangzhou, ChinaDepartment of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, ChinaDepartment of Interventional Radiology, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, ChinaBackgroundFibroblast activating protein (FAP) has become an important target for cancer diagnostic imaging and targeted radiotherapy. In particular, [18F]FAPI-42 has been successfully applied to positron emission tomography (PET) imaging of various tumors. However, it exhibits high hepatobiliary metabolism and is thus not conducive to abdominal tumor imaging. This study reports a novel 18F-labeled FAP inhibitor, [18F]AlF-FAPT, a better FAPI imaging agent than [18F]FAPI-42.Materials and MethodsThe precursor of [18F]AlF-FAPT (NOTA-FAPT) was designed and synthesized using the standard FMOC solid phase synthesis method. [18F]AlF-FAPT was subsequently synthesized and radiolabeled with 18F using the AllInOne synthesis module. Dynamic MicroPET and biodistribution studies of [18F]AlF-FAPT were then conducted in xenograft tumor mouse models to determine its suitability.ResultsThe precursors NOTA-FAPT were obtained with a chemical purity of > 95%. [18F]AlF-FAPT was synthesized automatically using the cassette-based module AllInOne within 40 min. The non-decay corrected radiochemical yield was 25.0 ± 5.3% (n=3). In vivo imaging and biodistribution studies further demonstrated that compared with [18F]-FAPI-42, [18F]AlF-FAPT had a lower hepatobiliary uptake than [18F]FAPI-42, which was advantageous for imaging abdominal tumors.Conclusion[18F]AlF-FAPT can be synthesized automatically using a one-step method of aluminum fluoride. Collectively, [18F]AlF-FAPT is a better FAPI imaging agent than [18F]FAPI-42. This study proves the feasibility of using [18F]AlF-FAPT as a new radioactive tracer for PET imaging.https://www.frontiersin.org/articles/10.3389/fonc.2021.802676/fullcancer-associated fibroblastsPET/CTfibroblast activation protein[18F]AlF-FAPTautomatic synthesis |
| spellingShingle | JiaWen Huang LiLan Fu KongZhen Hu Shun Huang YanJiang Han Run Lin WanBang Xu Ganghua Tang Yonghui Huang Automatic Production and Preliminary PET Imaging of a New Imaging Agent [18F]AlF-FAPT Frontiers in Oncology cancer-associated fibroblasts PET/CT fibroblast activation protein [18F]AlF-FAPT automatic synthesis |
| title | Automatic Production and Preliminary PET Imaging of a New Imaging Agent [18F]AlF-FAPT |
| title_full | Automatic Production and Preliminary PET Imaging of a New Imaging Agent [18F]AlF-FAPT |
| title_fullStr | Automatic Production and Preliminary PET Imaging of a New Imaging Agent [18F]AlF-FAPT |
| title_full_unstemmed | Automatic Production and Preliminary PET Imaging of a New Imaging Agent [18F]AlF-FAPT |
| title_short | Automatic Production and Preliminary PET Imaging of a New Imaging Agent [18F]AlF-FAPT |
| title_sort | automatic production and preliminary pet imaging of a new imaging agent 18f alf fapt |
| topic | cancer-associated fibroblasts PET/CT fibroblast activation protein [18F]AlF-FAPT automatic synthesis |
| url | https://www.frontiersin.org/articles/10.3389/fonc.2021.802676/full |
| work_keys_str_mv | AT jiawenhuang automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt AT lilanfu automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt AT kongzhenhu automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt AT shunhuang automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt AT yanjianghan automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt AT runlin automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt AT wanbangxu automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt AT ganghuatang automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt AT yonghuihuang automaticproductionandpreliminarypetimagingofanewimagingagent18falffapt |