Technetium-99m-1,2-bis[bis(2-ethoxyethyl) phosphino]ethane: human biodistribution, dosimetry and safety of a new myocardial perfusion imaging agent.
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.
Higley
B
B
Pharmaceuticals R&D, Amersham International plc, Buckinghamshire, UK.
Smith
F W
FW
Smith
T
T
Gemmell
H G
HG
Das Gupta
P
P
Gvozdanovic
D V
DV
Graham
D
D
Hinge
D
D
Davidson
J
J
Lahiri
A
A
D006321:Heart / Q000000981:diagnostic imaging*; D006801:Humans; D008297:Male; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D009943:Organophosphorus Compounds / Q000009:adverse effects / Q000493:pharmacokinetics*; D015609:Organotechnetium Compounds / Q000009:adverse effects / Q000493:pharmacokinetics*; D011829:Radiation Dosage; D011877:Radionuclide Imaging; D014018:Tissue Distribution
D009943:Organophosphorus Compounds; D015609:Organotechnetium Compounds; C078700:technetium tc-99m tetrofosmin