Production and tumour uptake of [64Cu]Pyruvaldehyde-bis (N4-methylthiosemicarbazone) for PET and/or therapeutic purposes.
BACKGROUND
Copper-64 (T(1/2)=12.7 degrees h) is an important radionuclide used both in PET imaging and therapy. [(64)Cu]-pyruvaldehyde- bis(N(4)-methylthiosemicarbazone) ([64Cu]-PTSM) has already been used in the detection of cerebral and myocardial blood flow. In this study, a simple production method and tumor accumulation of [(64)Cu]-PTSM in fibrosarcoma-bearing mice were reported.


METHODS
Cu-64 was produced via the 68Zn(p, alpha n)(64)Cu nuclear reaction. [(64)Cu]-PTSM was prepared using in-house made PTSM ligand and [(64)Cu]cuprous acetate and injected to fibrosarcoma-bearing mice.


RESULTS
Copper-64 was prepared in chloride form ( approximately 200 mCi, > 95% chemical yield at 180 degrees microA for 1.1 h irradiation, radionuclidic purity > 96%, copper-67 as impurity). The solution of (64)Cu- PTSM was prepared in > 80% radiochemical yield and more than 98% radiochemical purity. A significant tumor uptake was observed 2 hours post injection in tumor-bearing mice (tumor/muscle: 9, tumor/blood: 6).


CONCLUSIONS
[(64)Cu]-PTSM was prepared on a radiopharmaceutical scale using readily available zinc-68, with high quality and was shown to possess application in the therapy and/or imaging of fibrosarcoma.
Jalilian
Amir Reza
AR
Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine (NRCAM), Karaj, Iran. ajalilian@nrcam.org
Rowshanfarzad
Pejman
P
Kamrani
Yousef Yari
YY
Shafaii
Kamaleddin
K
Mirzaii
Mohammad
M
D000818:Animals; D003301:Copper Radioisotopes / Q000493:pharmacokinetics / Q000627:therapeutic use; D004355:Drug Stability; D051379:Mice; D008807:Mice, Inbred BALB C; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D012513:Sarcoma, Experimental / Q000000981:diagnostic imaging / Q000532:radiotherapy; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D014018:Tissue Distribution
D003301:Copper Radioisotopes; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; D013882:Thiosemicarbazones; C063293:copper (II) pyruvaldehyde bis(N(4)-dimethylthiosemicarbazone)