Automated production of radiotracer [ 18 F]FZTA for imaging sphingosine-1-phosphate receptor 1 (S1PR1) in human.
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| Title: | Automated production of radiotracer [ 18 F]FZTA for imaging sphingosine-1-phosphate receptor 1 (S1PR1) in human. |
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| Authors: | Qiu L; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States. Electronic address: linqiu@wustl.edu., Bognar C; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States., Tangadanchu VKR; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States., Moerlein SM; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States., Gaehle GG; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States., Gropler RJ; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States., Perlmutter JS; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States; Department of Neurology, Neuroscience, Physical Therapy and Occupational Therapy, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States., Benzinger TLS; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States., Tu Z; Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri, 63110, United States. Electronic address: zhudetu@wustl.edu. |
| Source: | Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2025 Dec; Vol. 226, pp. 112136. Date of Electronic Publication: 2025 Aug 25. |
| Publication Type: | Journal Article |
| Language: | English |
| Journal Info: | Publisher: Pergamon Press Country of Publication: England NLM ID: 9306253 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1872-9800 (Electronic) Linking ISSN: 09698043 NLM ISO Abbreviation: Appl Radiat Isot Subsets: MEDLINE |
| Imprint Name(s): | Original Publication: Oxford ; New York : Pergamon Press, c1993- |
| MeSH Terms: | Fluorine Radioisotopes*/chemistry , Radiopharmaceuticals*/chemical synthesis , Radiopharmaceuticals*/chemistry , Sphingosine-1-Phosphate Receptors*/metabolism , Oxadiazoles*/chemical synthesis , Oxadiazoles*/chemistry, Humans ; Positron-Emission Tomography/methods ; Automation |
| Abstract: | Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. We report a reliable fully automated procedure to produce a promising F-18 labeled sphingosine-1-phosphate receptor 1 (S1PR1) PET ligand, 3-((2-fluoro-4-(5-(4-(2-(fluoro- 18 F)ethoxy)-3-(trifluoromethyl)phenyl)-1,2,4-oxadiazol-3-yl)benzyl) (methyl)amino)propan-1-ol ([ 18 F]FZTA) on the GE TRACERlab FX2N module, using a one-pot two-step procedure following current Good Manufacturing Practices (cGMP). The MOM-protected precursor 1 was fluorinated with no-carrier-added [ 18 F]KF, catalyzed by Kryptofix 222 under heat, to afford the intermediate [ 18 F]2. After deprotecting the MOM-group on [ 18 F]2 under acidic condition, the reaction was quenched into a neutralized solution, which was then loaded on semi-preparative HPLC for purification. The collected product [ 18 F]FZTA was trapped on Sep-Pak C18 cartridge and formulated in 10 % ethanol/saline solution for quality control. The radiosynthesis of [ 18 F]FZTA was accomplished in approximately 60 min with radiochemical yield of 13.9 ± 2.9 %, radiochemical purity >91 %, and molar activity >147 GBq/μmol (n = 3, decay corrected to end of synthesis (EOS)). We successfully achieved three consecutive validation runs and the radiopharmaceutical products met all quality control criteria and specifications of the exploratory Investigational New Drug (IND) application for use of the PET radiotracer in human subjects. (Copyright © 2025. Published by Elsevier Ltd.) |
| Contributed Indexing: | Keywords: Automated radiosynthesis; Fluorine-18; Positron emission tomography; Sphingosine-1-phosphate receptor 1; [(18)F]FZTA; cGMP |
| Substance Nomenclature: | 0 (Fluorine Radioisotopes) 0 (Radiopharmaceuticals) 0 (Sphingosine-1-Phosphate Receptors) GZ5I74KB8G (Fluorine-18) 0 (S1PR1 protein, human) 0 (Oxadiazoles) |
| Entry Date(s): | Date Created: 20250830 Date Completed: 20251113 Latest Revision: 20251113 |
| Update Code: | 20251113 |
| DOI: | 10.1016/j.apradiso.2025.112136 |
| PMID: | 40884909 |
| Database: | MEDLINE |
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Nájsť tento článok vo Web of Science | Abstract: | Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br />We report a reliable fully automated procedure to produce a promising F-18 labeled sphingosine-1-phosphate receptor 1 (S1PR1) PET ligand, 3-((2-fluoro-4-(5-(4-(2-(fluoro- <sup>18</sup> F)ethoxy)-3-(trifluoromethyl)phenyl)-1,2,4-oxadiazol-3-yl)benzyl) (methyl)amino)propan-1-ol ([ <sup>18</sup> F]FZTA) on the GE TRACERlab FX2N module, using a one-pot two-step procedure following current Good Manufacturing Practices (cGMP). The MOM-protected precursor 1 was fluorinated with no-carrier-added [ <sup>18</sup> F]KF, catalyzed by Kryptofix 222 under heat, to afford the intermediate [ <sup>18</sup> F]2. After deprotecting the MOM-group on [ <sup>18</sup> F]2 under acidic condition, the reaction was quenched into a neutralized solution, which was then loaded on semi-preparative HPLC for purification. The collected product [ <sup>18</sup> F]FZTA was trapped on Sep-Pak C18 cartridge and formulated in 10 % ethanol/saline solution for quality control. The radiosynthesis of [ <sup>18</sup> F]FZTA was accomplished in approximately 60 min with radiochemical yield of 13.9 ± 2.9 %, radiochemical purity >91 %, and molar activity >147 GBq/μmol (n = 3, decay corrected to end of synthesis (EOS)). We successfully achieved three consecutive validation runs and the radiopharmaceutical products met all quality control criteria and specifications of the exploratory Investigational New Drug (IND) application for use of the PET radiotracer in human subjects.<br /> (Copyright © 2025. Published by Elsevier Ltd.) |
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| ISSN: | 1872-9800 |
| DOI: | 10.1016/j.apradiso.2025.112136 |