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Human Biodistribution, Dosimetry and Clinical Use of Technetium(III)-99m-Q12

Institute H.S. Raffaele, Milano, INB-CNR, University of Milano, Sorin Biomedica, S.p.A., Saluggia, Italy
Mallinckrodt Medical Inc., St. Louis, Missouri

Correspondence: For correspondence or reprints contact: Ferrucio Fazio, MD, Dipartimento di Medicina Nucleare, Istituto Scientifico H.S. Raffaele, Via Olgettina, 60, 20132 Milano, Italy.

ABSTRACT

Technetium(III)-99m-Q12, trans-(1,2-bis(dihydro-2,2,5,5-tetramethyl - 3(2H)furanone- 4 - methyleneimino)ethane)bis(tris(3 - methoxy-1-propyl)-phosphine)technetium(III)-99m, is a nonreducible complex of Tc(III) which is herein evaluated as a myocardial perfusion imaging agent. Methods: The biodistribution and dosimetry of ^99mTc-Q12 were assessed in 10 normal volunteers, while its potential clinical use was evaluated in 70 patients. Results: Safety parameters measured up to 24 hr postinjection demonstrate no clinically significant drug-related adverse reactions. Technetium(III)-99m-Q12 exhibits good heart uptake (2.2% injected dose at 1 hr postinjection under resting conditions) and no detectable myocardial washout or redistribution up to 5 hr postinjection. The biodistribution is characterized by very rapid hepatobiliary clearance which allows effective myocardial imaging at times as short as 15 min postinjection. Blood and plasma clearances and myocardial uptake are rapid, while lung uptake is minimal. The heart-to-lung and heart-to-liver ratios are higher at stress than at rest, independent of the time elapsed between injection and image acquisition, and independent of whether the patient is fasted or fed after tracer administration. A preliminary correlation shows that 46/47 patients with angiographically demonstrated CAD also have perfusion defects demonstrated by ^99mTc-Q12. Conclusions: On the basis of the studies reported herein, ^99mTc-Q12 appears to be a promising myocardial perfusion imaging agent.

Key Words: myocardium • technetium-99m-Q12 • myocardial perfusion