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Technetium-94m-Teboroxime: Synthesis, Dosimetry and Initial PET Imaging Studies

Departments of Medical Physics, Medicine (Cardiology) and Radiology (Nuclear Medicine), University of Wisconsin, Madison, Wisconsin
Bristol-Myers Squibb, New Brunswick, New Jersey

Correspondence: For correspondence or reprints contact: Prof. R.J. Nickles, Department of Medical Physics, 1530 Medical Science Center, University of Wisconsin Medical School, 1300 University Ave., Madison, WI 53706.

ABSTRACT

Technetium-94m(T_1/2 = 53 min) allows the in vivo study of technetium radiopharmaceuticals with positron emission tomography (PET). PET provides a quantitative assay of radioactivity with excellent temporal and spatial resolution, revealing biodistributions that were previously available only through in vitro assay methods. Technetium-94m, produced by the proton irradiation of natural molybdenum on an 11 MeV cyclotron, was extracted with an electrochemical etching technique. Technetium-94m-pertechnetate was prepared to make the myocardial perfusion agent teboroxime in an identical manner as ^99mTcO^–₄. The increased absorbed radiation dose requires a sevenfold reduction in administered activity compared to ^99mTc-teboroxime. Eleven clinical PET studies were performed and visually compared to ¹³N-ammonia. The clearance half-time for ^99mTc-teboroxime was 8 min, with a peak myocardial extraction of 3% of the injected dose into a 400-g heart. These results confirm the potential of ^99mTc PET for quantitatively studying the pharmacokinetics of new, and old, technetium agents in man.

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