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Production and tumour uptake of [64Cu]Pyruvaldehyde-bis (N4-methylthiosemicarbazone) for PET and/or therapeutic purposes
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Abstract
BACKGROUND: Copper-64 (T1/2=12.7ºh) is an important radionuclide used both in PET imaging and therapy. [64Cu]-pyruvaldehyde- bis(N4-methylthiosemicarbazone) ([64Cu]-PTSM) has already been used in the detection of cerebral and myocardial blood flow. In this study, a simple production method and tumour accumulation of [64Cu]-PTSM in fibrosarcoma-bearing mice were reported.
MATERIAL AND METHODS: Cu-64 was produced via the 68Zn(p, αn)64Cu nuclear reaction. [64Cu]-PTSM was prepared using in-house made PTSM ligand and [64Cu]cuprous acetate and injected to fibrosarcoma-bearing mice.
RESULTS: Copper-64 was prepared in chloride form (≈ 200 mCi, > 95% chemical yield at 180º μA for 1.1 h irradiation, radionuclidic purity > 96%, copper-67 as impurity). The solution of 64Cu- PTSM was prepared in > 80% radiochemical yield and more than 98% radiochemical purity. A significant tumour uptake was observed 2 hours post injection in tumour-bearing mice (tu- mour/muscle: 9, tumour/blood: 6).
CONCLUSION: [64Cu]-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.
Abstract
BACKGROUND: Copper-64 (T1/2=12.7ºh) is an important radionuclide used both in PET imaging and therapy. [64Cu]-pyruvaldehyde- bis(N4-methylthiosemicarbazone) ([64Cu]-PTSM) has already been used in the detection of cerebral and myocardial blood flow. In this study, a simple production method and tumour accumulation of [64Cu]-PTSM in fibrosarcoma-bearing mice were reported.
MATERIAL AND METHODS: Cu-64 was produced via the 68Zn(p, αn)64Cu nuclear reaction. [64Cu]-PTSM was prepared using in-house made PTSM ligand and [64Cu]cuprous acetate and injected to fibrosarcoma-bearing mice.
RESULTS: Copper-64 was prepared in chloride form (≈ 200 mCi, > 95% chemical yield at 180º μA for 1.1 h irradiation, radionuclidic purity > 96%, copper-67 as impurity). The solution of 64Cu- PTSM was prepared in > 80% radiochemical yield and more than 98% radiochemical purity. A significant tumour uptake was observed 2 hours post injection in tumour-bearing mice (tu- mour/muscle: 9, tumour/blood: 6).
CONCLUSION: [64Cu]-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.
Keywords
Copper-64; PTSM; PET; targeted therapy; fibrosarcoma
About this articleTitle
Production and tumour uptake of [64Cu]Pyruvaldehyde-bis (N4-methylthiosemicarbazone) for PET and/or therapeutic purposes
Journal
Issue
Pages
6-11
Published online
2007-02-15
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797
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1545
Bibliographic record
Nucl. Med. Rev 2007;10(1):6-11.
Keywords
Copper-64
PTSM
PET
targeted therapy
fibrosarcoma
Authors
Amir Reza Jalilian
Pejman Rowshanfarzad
Yousef Yari Kamrani
Kamaleddin Shafaii
Mohammad Mirzaii
