Preliminary imaging studies of [[61]Cu] diacetyl-bis [N[4]-methylthiosemi-carbazone] in normal and hypoxic tumor models

[[61]Cu] diacetyl-bis [N[4] -methylthiosemicarbazone] [[[61]Cu] ATSM] is a well-established hypoxia imaging tracer with simple production and significant specifity. In this work the accumulation of the tracer is studied in wild-type, necrotic and hypoxic fibrosarcoma tumors. [[61] Cu] ATSM was prepared using ATSM ligand and [[61]Cu] CuOAc followed by i.v. administration and imaging studies in wid-type rats and hypoxic fibrosarcoma-bearing mic.e [[61] Cu] ATSM with high radiochemical purity [>99%, HPLC, RTLC] was injected to wild-type rats as well as hypoxic and necrotic fibrosarcoma-bearing mice followed by imaging up to 3 hours. [[61] Cu] ATSM was mainly accumulated in liver, as well as kidney and bladder and less but still significant in brain of wild-type rats. A significant and hypoxia-specific tumor/non tumor ratio in hypoxic models was observed by co-incidence imaging 2h post inection, while in necrotic and 12-week tumor-induced mice very slight tumor uptakes were detected. [[61]Cu] ATSM is a positron emission tomography [PET] radiotracer for selective tumor hypoxia imaging from necrotic and proliferative tumors

Production, quality control and imaging of [64]Cu-ATSM in healthy rabbits for clinical applications

[[64]Cu]diacetyl-bis[N[4]-methylthiosemicarbazone] [[[64]Cu]ATSM] is a well-established hypoxia imaging tracer with reproducible production and significant specifity. In this work the high yield production and quality control as well as imaging studies in healthy rabbits is reported. Copper-64 produced via the [68]Zn[p, alpha n] [64]Cu nuclear reaction [30 MeV protons at 180 micro A] was used for the preparation of [[64]Cu]diacetyl-bis[N4-methylthiosemicarbazone][[ [64]Cu]ATSM]. Followed by quality control and administration to healthy rats as well as healthy rabbits for biodistribution and imaging studies respectively. [64]Cu[2+] [500 mCi, separation yield> 95%, radionuclide purity>96%] was used for [[64]Cu]ATSM production [radiochemical purity>99%, specific activity of 300 Ci/mmol] followed by administration to healthy rabbits and coincidence imaging demonstrating uptake in liver, kidney and bowel as shown by other reports in various rodents and human. [[64]Cu]ATSM radiopharmaceutical is produced and now available in large quantities for research and/or clinical trials in the country

Biodistribution of [64 Cu] pyruvaldehyde-bis [N4-methylthiosemicarbazone] complex in fibrosarcoma-bearing rats

[64]Cu-pyruvaldehyde-bis [N[4]-methylthiosemicarbazone] [64]Cu-PTSM] is one of the most important copper radiopharmaceuticals used in clinical experiments. In this work, copper-64 [T[1/2]=12.33 h] production has been presented followed by the synthesis of the complexing agent, PTSM, and its structure was confirmed by common spectroscopic methods followed by radiolabeling with [64] Cu-actetate. The tracer was finally administered to fibrosarcoma-bearing rats and the biodistribution was determined in critical tissues as well as tumor. The final radiopharmaceutical solution underwent common quality control tests for animal injection a radiochemical purity >95% was determined. A significant tracer tumor uptake was observed 2 hours post injection. Tumonmuscle and tumonblood ratios were shown to be 8 and 6 respectively. [64]Cu-PTSM prepared in this report is a good candidate for tumor therapy as well as diagnosis for national use