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.

Material And 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).

Conclusion: [(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.