TY - JOUR
T1 - Automated production of a sphingosine-1 phosphate receptor 1 (S1P1) PET radiopharmaceutical [11C]CS1P1 for human use
AU - Luo, Zonghua
AU - Gu, J.
AU - Dennett, Robert C.
AU - Gaehle, Gregory G.
AU - Perlmutter, Joel S.
AU - Chen, Delphine L.
AU - Benzinger, Tammie L.S.
AU - Tu, Z.
N1 - Publisher Copyright:
© 2019 Elsevier Ltd
PY - 2019/10
Y1 - 2019/10
N2 - 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.
AB - 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.
KW - Automation
KW - Positron emission tomography
KW - Radiopharmaceutical
KW - Sphingosine-1 phosphate receptor 1
KW - [C]CS1P1
UR - http://www.scopus.com/inward/record.url?scp=85068268217&partnerID=8YFLogxK
U2 - 10.1016/j.apradiso.2019.06.029
DO - 10.1016/j.apradiso.2019.06.029
M3 - Article
C2 - 31280104
AN - SCOPUS:85068268217
SN - 0969-8043
VL - 152
SP - 30
EP - 36
JO - Applied Radiation and Isotopes
JF - Applied Radiation and Isotopes
ER -