1. Automated production of a sphingosine-1 phosphate receptor 1 (S1P1) PET radiopharmaceutical [11C]CS1P1 for human use
- Author
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Zhude Tu, Robert C. Dennett, Tammie L.S. Benzinger, Jiwei Gu, Joel S. Perlmutter, Delphine L. Chen, Gregory G. Gaehle, and Zonghua Luo
- Subjects
Radiation ,Trifluoromethyl ,Human studies ,Sphingosine-1-phosphate receptor ,Radiochemistry ,Pet imaging ,010403 inorganic & nuclear chemistry ,01 natural sciences ,030218 nuclear medicine & medical imaging ,0104 chemical sciences ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Propanoic acid ,chemistry ,Human use ,Yield (chemistry) - Abstract
Automated synthesis of a radiopharmaceutical 3-((2-fluoro-4-(5-(2′-methyl-2-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)-1,2,4-oxadiazol-3-yl)benzyl) (methyl-11C)amino)propanoic acid ([11C]CS1P1) for PET imaging sphingosine-1 phosphate receptor 1 (S1P1) was accomplished by a two-step-one-pot procedure in a Siemens CTI methylation automated module using TR-19 cyclotron. The synthesis of [11C]CS1P1 was successfully validated under current Good Manufacturing Practices (cGMP) conditions, resulting in a consistent average radiochemical yield of ∼15%, molar activity of ∼3129 GBq/μmol (decay corrected to end of bombardment, EOB), and radiochemical purity > 95%. The radiopharmaceutical product meets all quality control criteria for human use for an Investigational New Drug (IND) application to permit human studies.
- Published
- 2019