Production and tumour uptake of [64Cu]Pyruvaldehyde-bis (N4-methylthiosemicarbazone) for PET and/or therapeutic purposes

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 tum...

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Bibliographic Details
Published in:Nuclear medicine review. Central & Eastern Europe 2007, Vol.10 (1), p.6-11
Main Authors: Jalilian, Amir Reza, Rowshanfarzad, Pejman, Kamrani, Yousef Yari, Shafaii, Kamaleddin, Mirzaii, Mohammad
Format: Article
Language:English
Subjects:
Animals
Copper Radioisotopes - pharmacokinetics
Copper Radioisotopes - therapeutic use
Drug Stability
Mice
Mice, Inbred BALB C
Organometallic Compounds - chemical synthesis
Organometallic Compounds - pharmacokinetics
Organometallic Compounds - therapeutic use
Positron-Emission Tomography
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - pharmacokinetics
Radiopharmaceuticals - therapeutic use
Sarcoma, Experimental - diagnostic imaging
Sarcoma, Experimental - radiotherapy
Thiosemicarbazones - chemical synthesis
Thiosemicarbazones - pharmacokinetics
Thiosemicarbazones - therapeutic use
Tissue Distribution
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Summary: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. 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. 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). [(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.
ISSN:1506-9680