Automated production of a sphingosine-1 phosphate receptor 1 (S1P1) PET radiopharmaceutical [11C]CS1P1 for human use

被引：8

作者：

Luo, Zonghua ^{[1
]}

Gu, Jiwei ^{[1
]}

Dennett, Robert C. ^{[1
]}

Gaehle, Gregory G. ^{[1
]}

Perlmutter, Joel S. ^{[1
,2
]}

Chen, Delphine L. ^{[1
]}

Benzinger, Tammie L. S. ^{[1
]}

Tu, Zhude ^{[1
]}

机构：

[1] Washington Univ, Dept Radiol, Sch Med, St Louis, MO 63110 USA

[2] Washington Univ, Dept Neurol Neurosci Phys Therapy & Occupat Thera, Sch Med, St Louis, MO 63110 USA

来源：

APPLIED RADIATION AND ISOTOPES | 2019年 / 152卷

基金：

美国国家卫生研究院;

关键词：

Positron emission tomography; Sphingosine-1 phosphate receptor 1; Automation; Radiopharmaceutical; C-11]CS1P1; FTY720; FINGOLIMOD; EFFICACY; MODEL;

D O I：

10.1016/j.apradiso.2019.06.029

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

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.

引用

页码：30 / 36

页数：7

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