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J Nucl Med. 2008; 49 (Supplement 1):284P
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Radiopharmaceutical Chemistry: Dosimetry/Radiobiology

Dosimetry/Radiobiology Posters

Generator/kit produced 62Cu-ETS, a PET perfusion agent with minimized plasma binding

Jeffrey Lacy1, Leticia Guerrero1, Regina Chiu2, Avery Stephens1, Zhiwei Yue1, Liang Sun1, Lance Hall2 and Charles Stone2

1 Proportional Technologies, Inc, Houston, Texas; 2 U of Wisc-Madison, Madison, Wisconsin

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Objectives: 62Cu-ETS [62Cu-ethylglyoxal bis(thiosemicarbazone)], is a PET perfusion tracer selected for reduced plasma binding and potentially enhanced hyperemic response. Proportional Technologies, Inc. has filed an Investigational New Drug application for 62Cu-ETS (75018) and has completed the Phase I safety and biodistribution study.

Methods: Whole body PET imaging was performed in 4 male and 6 female normal volunters. Physical exams, blood chemistry, ECG, and urinalysis were obtained pre and post injection and data was compiled and compared using paired t-tests. Three sequential 20 minute PET scans were performed from head to upper thigh. Uptake of major organs was quantified, and residence times were calculated to obtain complete human dosimetry estimates.

Results: No significant changes were seen in any of the safety variables. Kidney was identified as the critical organ receiving 0.151 rem/mCi, defining the maximum single injection dose at 33 mCi. Uptake of major organs were (units in %ID): blood – 15.24, brain – 1.45, intestine – 2.82, kidneys – 6.19, liver – 10.29, lungs – 12.35, myocardium – 1.37, salivary glands – 0.04, spleen – 2.60, and thyroid – 0.14. Taking the %ID/cc of tissue, kidney uptake was 2.0 times that of myocardium, and liver uptake was 1.1 times myocardium. For 62Cu-PTSM the corresponding ratios are 1.3 and 1.9.

Conclusions: This study confirmed the safety and absence of toxicity of 62Cu-ETS. The high renal uptake and renal to heart ratio compared to 62Cu-PTSM suggests favorable hyperemic response. The substantially lower liver to heart ratio is an added benefit for myocardial imaging. Phase II studies will begin shortly to investigate both renal and myocardial perfusion applications of this promising tracer.

Research Support: NIH SBIR Grants DK058466 and CA110154





This Article
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Google Scholar
Right arrow Articles by Lacy, J.
Right arrow Articles by Stone, C.
PubMed
Right arrow Articles by Lacy, J.
Right arrow Articles by Stone, C.