Automated production of a sphingosine-1 phosphate receptor 1 (S1P1) PET radiopharmaceutical [11C]CS1P1 for human use
Automated production of a sphingosine-1 phosphate receptor 1 (S1P1) PET radiopharmaceutical [11C]CS1P1 for human use
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DOI:
10.1016/j.apradiso.2019.06.029
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发表时间:
2019-10-01
影响因子:
1.6
通讯作者:
Tu, Zhude
中科院分区:
文献类型:
--
作者:
Luo, Zonghua;Gu, Jiwei;Tu, Zhude
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-(11) C)amino)propanoic acid ([C-11]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 [(11) C]CS1P1 was successfully validated under current Good Manufacturing Practices (cGMP) conditions, resulting in a consistent average radiochemical yield of similar to 15%, molar activity of similar to 3129 GBq/mu mol (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.