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

Abstract

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.

• Authors: Amir Reza Jalilian, Pejman Rowshanfarzad, Yousef Yari Kamrani, Kamaleddin Shafaii, Mohammad Mirzaii
• Journal: Nuclear medicine review. Central & Eastern Europe (Nucl Med Rev Cent East Eur) Vol. 10 Issue 1 Pg. 6-11 ( 2007) ISSN: 1506-9680 [Print] Poland
• PMID: 17694494 (Publication Type: Journal Article)

Chemical References

• Copper Radioisotopes
• Organometallic Compounds
• Radiopharmaceuticals
• Thiosemicarbazones
• copper (II) pyruvaldehyde bis(N(4)-dimethylthiosemicarbazone)

Topics

• Animals
• Copper Radioisotopes (pharmacokinetics, therapeutic use)
• Drug Stability
• Mice
• Mice, Inbred BALB C
• Organometallic Compounds (chemical synthesis, pharmacokinetics, therapeutic use)
• Positron-Emission Tomography
• Radiopharmaceuticals (chemical synthesis, pharmacokinetics, therapeutic use)
• Sarcoma, Experimental (diagnostic imaging, radiotherapy)
• Thiosemicarbazones (chemical synthesis, pharmacokinetics, therapeutic use)
• Tissue Distribution