Automated production of a sphingosine-1 phosphate receptor 1 (S1P1) PET radiopharmaceutical [11C]CS1P1 for human use. (October 2019) - Luo, Zonghua
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- 11 C)amino)propanoic acid ([ 11 C]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 ∼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. Highlights: Automated production of [ 11 C]CS1P1 was performed by a two-step-one-pot procedure under cGMP conditions. [ 11 C]CS1P1 was achieved with high molar activity and radiochemical purity. The procedure can be applied for a routine production of [ 11 C]CS1P1. The radiopharmaceutical [ 11 C]CS1P1 meets all quality control criteria for human use.