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The Journal of Nuclear Medicine Vol. 34 No. 1 30-38
© 1993 by Society of Nuclear Medicine
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Technetium-99m-1,2-bis[bis(2-Ethoxyethyl) Phosphino]Ethane: Human Biodistribution, Dosimetry and Safety of a New Myocardial Perfusion Imaging Agent

Brian Higley, Francis W. Smith, Terry Smith, Howard G. Gemmell, Prabir Das Gupta, Dragouten V. Gvozdanovic, David Graham, David Hinge, Joyce Davidson and Avijit Lahiri

Pharmaceuticals R&D, Amersham International plc, Amersham, Buckinghamshire, UK
Department of Nuclear Medicine, Aberdeen Royal Infirmary, Foresterhill, Aberdeen, UK
Department of Cardiology, Northwick Park Hospital and Section of Medical Physics, Clinical Research Centre, Harrow, Middlesex, UK

Correspondence: For correspondence or reprints contact: Brian Higley, Pharmaceuticals R&D, Amersham Intl. plc, White Lion Rd., Amersham, Buckinghamshire, HP7, 9LL, UK.

ABSTRACT

A novel 99mTc complex (1,2-bis[bis(2-ethoxyethyl)phosphino] ethane, 99mTc-tetrofosmin) has been developed to replace 201Tl in myocardial perfusion imaging. Biodistribution, safety and dosimetry of 99mTc-tetrofosmin were studied in 12 male volunteers, each at rest and during exercise. Safety parameters measured to 48 hr postinjection revealed no clinically significant long-term drug-related changes. Biodistribution was studied by acquiring whole-body or serial static images up to 48 hr postinjection. Technetium-99m-tetrofosmin shows good heart uptake (1.2%) with retention. Clearance is excellent from blood (<5% by 10 min), liver (<4.5% by 60 min) and lung. Sequestration of activity by skeletal muscle is enhanced during exercise. Radiation dosimetry calculations indicate that the effective dose, assuming a 3.5 hr bladder voiding period, is 32.9 x 10–3 rad/mCi (8.9 x 10–3 mSv/MBq) at rest and 26.7 x 10–3 rad/mCi (7.1 x 10–3 mSv/MBq) after exercise. Technetium-99m-tetrofosmin can produce high quality myocardial images from 5 min to several hours postinjection.




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