First Human Use of a Radiopharmaceutical Prepared by Continuous-Flow Microfluidic Radiofluorination: Proof of Concept with the Tau Imaging Agent [F]T807
Despite extensive preclinical imaging with radiotracers developed by continuous-flow microfluidics, a positron emission tomographic (PET) radiopharmaceutical has not been reported for human imaging studies by this technology. The goal of this study was to validate the synthesis of the tau radiopharm...
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| Format: | Article |
| Language: | English |
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SAGE Publishing
2014-10-01
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| Series: | Molecular Imaging |
| Online Access: | https://doi.org/10.2310/7290.2014.00025 |
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| author | Steven H. Liang Daniel L. Yokell Marc D. Normandin Peter A. Rice Raul N. Jackson Timothy M. Shoup Thomas J. Brady Georges El Fakhri Thomas L. Collier Neil Vasdev |
| author_facet | Steven H. Liang Daniel L. Yokell Marc D. Normandin Peter A. Rice Raul N. Jackson Timothy M. Shoup Thomas J. Brady Georges El Fakhri Thomas L. Collier Neil Vasdev |
| author_sort | Steven H. Liang |
| collection | DOAJ |
| description | Despite extensive preclinical imaging with radiotracers developed by continuous-flow microfluidics, a positron emission tomographic (PET) radiopharmaceutical has not been reported for human imaging studies by this technology. The goal of this study was to validate the synthesis of the tau radiopharmaceutical 7-(6-fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole ([ 18 F]T807) and perform first-in-human PET scanning enabled by microfluidic flow chemistry. [ 18 F]T807 was synthesized by our modified one-step method and adapted to suit a commercial microfluidic flow chemistry module. For this proof of concept, the flow system was integrated to a GE Tracerlab FX FN unit for high-performance liquid chromatography purification and formulation. Three consecutive productions of [ 18 F]T807 were conducted to validate this radiopharmaceutical. Uncorrected radiochemical yields of 17 ± 1% of crude [ 18 F]T807 (≈ 500 mCi, radiochemical purity 95%) were obtained from the microfluidic device. The crude material was then purified, and > 100 mCi of the final product was obtained in an overall uncorrected radiochemical yield of 5 ± 1% ( n = 3), relative to starting [ 18 F]fluoride (end of bombardment), with high radiochemical purity (≥ 99%) and high specific activities (6 Ci/μmol) in 100 minutes. A clinical research study was carried out with [ 18 F]T807, representing the first reported human imaging study with a radiopharmaceutical prepared by this technology. |
| format | Article |
| id | doaj-art-9337f32030384aeebaedb871c7a68b2a |
| institution | DOAJ |
| issn | 1536-0121 |
| language | English |
| publishDate | 2014-10-01 |
| publisher | SAGE Publishing |
| record_format | Article |
| series | Molecular Imaging |
| spelling | doaj-art-9337f32030384aeebaedb871c7a68b2a2025-08-20T02:43:25ZengSAGE PublishingMolecular Imaging1536-01212014-10-011310.2310/7290.2014.0002510.2310_7290.2014.00025First Human Use of a Radiopharmaceutical Prepared by Continuous-Flow Microfluidic Radiofluorination: Proof of Concept with the Tau Imaging Agent [F]T807Steven H. LiangDaniel L. YokellMarc D. NormandinPeter A. RiceRaul N. JacksonTimothy M. ShoupThomas J. BradyGeorges El FakhriThomas L. CollierNeil VasdevDespite extensive preclinical imaging with radiotracers developed by continuous-flow microfluidics, a positron emission tomographic (PET) radiopharmaceutical has not been reported for human imaging studies by this technology. The goal of this study was to validate the synthesis of the tau radiopharmaceutical 7-(6-fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole ([ 18 F]T807) and perform first-in-human PET scanning enabled by microfluidic flow chemistry. [ 18 F]T807 was synthesized by our modified one-step method and adapted to suit a commercial microfluidic flow chemistry module. For this proof of concept, the flow system was integrated to a GE Tracerlab FX FN unit for high-performance liquid chromatography purification and formulation. Three consecutive productions of [ 18 F]T807 were conducted to validate this radiopharmaceutical. Uncorrected radiochemical yields of 17 ± 1% of crude [ 18 F]T807 (≈ 500 mCi, radiochemical purity 95%) were obtained from the microfluidic device. The crude material was then purified, and > 100 mCi of the final product was obtained in an overall uncorrected radiochemical yield of 5 ± 1% ( n = 3), relative to starting [ 18 F]fluoride (end of bombardment), with high radiochemical purity (≥ 99%) and high specific activities (6 Ci/μmol) in 100 minutes. A clinical research study was carried out with [ 18 F]T807, representing the first reported human imaging study with a radiopharmaceutical prepared by this technology.https://doi.org/10.2310/7290.2014.00025 |
| spellingShingle | Steven H. Liang Daniel L. Yokell Marc D. Normandin Peter A. Rice Raul N. Jackson Timothy M. Shoup Thomas J. Brady Georges El Fakhri Thomas L. Collier Neil Vasdev First Human Use of a Radiopharmaceutical Prepared by Continuous-Flow Microfluidic Radiofluorination: Proof of Concept with the Tau Imaging Agent [F]T807 Molecular Imaging |
| title | First Human Use of a Radiopharmaceutical Prepared by Continuous-Flow Microfluidic Radiofluorination: Proof of Concept with the Tau Imaging Agent [F]T807 |
| title_full | First Human Use of a Radiopharmaceutical Prepared by Continuous-Flow Microfluidic Radiofluorination: Proof of Concept with the Tau Imaging Agent [F]T807 |
| title_fullStr | First Human Use of a Radiopharmaceutical Prepared by Continuous-Flow Microfluidic Radiofluorination: Proof of Concept with the Tau Imaging Agent [F]T807 |
| title_full_unstemmed | First Human Use of a Radiopharmaceutical Prepared by Continuous-Flow Microfluidic Radiofluorination: Proof of Concept with the Tau Imaging Agent [F]T807 |
| title_short | First Human Use of a Radiopharmaceutical Prepared by Continuous-Flow Microfluidic Radiofluorination: Proof of Concept with the Tau Imaging Agent [F]T807 |
| title_sort | first human use of a radiopharmaceutical prepared by continuous flow microfluidic radiofluorination proof of concept with the tau imaging agent f t807 |
| url | https://doi.org/10.2310/7290.2014.00025 |
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