{"title":"[18F]FEDAC：18-kDa 转运蛋白的新型 PET 示踪剂的首次人体研究。","authors":"Kentaro Tamura, Ryuichi Nishii, Kotaro Tani, Hiroki Hashimoto, Kazunori Kawamura, Ming-Rong Zhang, Takamasa Maeda, Kana Yamazaki, Tatsuya Higashi, Masahiro Jinzaki","doi":"10.1007/s12149-023-01895-0","DOIUrl":null,"url":null,"abstract":"<div><h3>Purpose</h3><p>N-benzyl-N-methyl-2-[7, 8-dihydro-7-(2-[<sup>18</sup>F] fluoroethyl) -8-oxo-2-phenyl-9H-purin-9-yl] acetamide ([<sup>18</sup>F] FEDAC) is a novel positron emission tomography (PET) tracer that targets the translocator protein (TSPO; 18 kDa) in the mitochondrial outer membrane, which is known to be upregulated in various diseases such as malignant tumors, neurodegenerative diseases, and neuroinflammation. This study presents the first attempt to use [<sup>18</sup>F]FEDAC PET/CT and evaluate its biodistribution as well as the systemic radiation exposure to the radiotracer in humans.</p><h3>Materials and Methods</h3><p>Seventeen whole-body [<sup>18</sup>F]FEDAC PET/CT (injected dose, 209.1 ± 6.2 MBq) scans with a dynamic scan of the upper abdomen were performed in seven participants. Volumes of interest were assigned to each organ, and a time–activity curve was created to evaluate the biodistribution of the radiotracer. The effective dose was calculated using IDAC-Dose 2.1.</p><h3>Results</h3><p>Immediately after the intravenous injection, the radiotracer accumulated significantly in the liver and was subsequently excreted into the gastrointestinal tract through the biliary tract. It also showed high levels of accumulation in the kidneys, but showed minimal migration to the urinary bladder. Thus, the liver was the principal organ that eliminated [<sup>18</sup>F] FEDAC. Accumulation in the normal brain tissue was minimal. The effective dose estimated from biodistribution in humans was 19.47 ± 1.08 µSv/MBq, and was 3.60 mSV for 185 MBq dose.</p><h3>Conclusion</h3><p>[<sup>18</sup>F]FEDAC PET/CT provided adequate image quality at an acceptable effective dose with no adverse effects. Therefore, [<sup>18</sup>F]FEDAC may be useful in human TSPO-PET imaging.</p></div>","PeriodicalId":8007,"journal":{"name":"Annals of Nuclear Medicine","volume":"38 4","pages":"264 - 271"},"PeriodicalIF":2.5000,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10954948/pdf/","citationCount":"0","resultStr":"{\"title\":\"A first-in-man study of [18F] FEDAC: a novel PET tracer for the 18-kDa translocator protein\",\"authors\":\"Kentaro Tamura, Ryuichi Nishii, Kotaro Tani, Hiroki Hashimoto, Kazunori Kawamura, Ming-Rong Zhang, Takamasa Maeda, Kana Yamazaki, Tatsuya Higashi, Masahiro Jinzaki\",\"doi\":\"10.1007/s12149-023-01895-0\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Purpose</h3><p>N-benzyl-N-methyl-2-[7, 8-dihydro-7-(2-[<sup>18</sup>F] fluoroethyl) -8-oxo-2-phenyl-9H-purin-9-yl] acetamide ([<sup>18</sup>F] FEDAC) is a novel positron emission tomography (PET) tracer that targets the translocator protein (TSPO; 18 kDa) in the mitochondrial outer membrane, which is known to be upregulated in various diseases such as malignant tumors, neurodegenerative diseases, and neuroinflammation. This study presents the first attempt to use [<sup>18</sup>F]FEDAC PET/CT and evaluate its biodistribution as well as the systemic radiation exposure to the radiotracer in humans.</p><h3>Materials and Methods</h3><p>Seventeen whole-body [<sup>18</sup>F]FEDAC PET/CT (injected dose, 209.1 ± 6.2 MBq) scans with a dynamic scan of the upper abdomen were performed in seven participants. Volumes of interest were assigned to each organ, and a time–activity curve was created to evaluate the biodistribution of the radiotracer. The effective dose was calculated using IDAC-Dose 2.1.</p><h3>Results</h3><p>Immediately after the intravenous injection, the radiotracer accumulated significantly in the liver and was subsequently excreted into the gastrointestinal tract through the biliary tract. It also showed high levels of accumulation in the kidneys, but showed minimal migration to the urinary bladder. Thus, the liver was the principal organ that eliminated [<sup>18</sup>F] FEDAC. Accumulation in the normal brain tissue was minimal. The effective dose estimated from biodistribution in humans was 19.47 ± 1.08 µSv/MBq, and was 3.60 mSV for 185 MBq dose.</p><h3>Conclusion</h3><p>[<sup>18</sup>F]FEDAC PET/CT provided adequate image quality at an acceptable effective dose with no adverse effects. Therefore, [<sup>18</sup>F]FEDAC may be useful in human TSPO-PET imaging.</p></div>\",\"PeriodicalId\":8007,\"journal\":{\"name\":\"Annals of Nuclear Medicine\",\"volume\":\"38 4\",\"pages\":\"264 - 271\"},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2024-01-29\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10954948/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Annals of Nuclear Medicine\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s12149-023-01895-0\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Annals of Nuclear Medicine","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s12149-023-01895-0","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING","Score":null,"Total":0}
A first-in-man study of [18F] FEDAC: a novel PET tracer for the 18-kDa translocator protein
Purpose
N-benzyl-N-methyl-2-[7, 8-dihydro-7-(2-[18F] fluoroethyl) -8-oxo-2-phenyl-9H-purin-9-yl] acetamide ([18F] FEDAC) is a novel positron emission tomography (PET) tracer that targets the translocator protein (TSPO; 18 kDa) in the mitochondrial outer membrane, which is known to be upregulated in various diseases such as malignant tumors, neurodegenerative diseases, and neuroinflammation. This study presents the first attempt to use [18F]FEDAC PET/CT and evaluate its biodistribution as well as the systemic radiation exposure to the radiotracer in humans.
Materials and Methods
Seventeen whole-body [18F]FEDAC PET/CT (injected dose, 209.1 ± 6.2 MBq) scans with a dynamic scan of the upper abdomen were performed in seven participants. Volumes of interest were assigned to each organ, and a time–activity curve was created to evaluate the biodistribution of the radiotracer. The effective dose was calculated using IDAC-Dose 2.1.
Results
Immediately after the intravenous injection, the radiotracer accumulated significantly in the liver and was subsequently excreted into the gastrointestinal tract through the biliary tract. It also showed high levels of accumulation in the kidneys, but showed minimal migration to the urinary bladder. Thus, the liver was the principal organ that eliminated [18F] FEDAC. Accumulation in the normal brain tissue was minimal. The effective dose estimated from biodistribution in humans was 19.47 ± 1.08 µSv/MBq, and was 3.60 mSV for 185 MBq dose.
Conclusion
[18F]FEDAC PET/CT provided adequate image quality at an acceptable effective dose with no adverse effects. Therefore, [18F]FEDAC may be useful in human TSPO-PET imaging.
期刊介绍：
Annals of Nuclear Medicine is an official journal of the Japanese Society of Nuclear Medicine. It develops the appropriate application of radioactive substances and stable nuclides in the field of medicine.
The journal promotes the exchange of ideas and information and research in nuclear medicine and includes the medical application of radionuclides and related subjects. It presents original articles, short communications, reviews and letters to the editor.
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