Evaluation in dogs and humans of three potential technetium-99m myocardial perfusion agents

P. Gerundini, A. Savi, M. C. Gilardi, A. Margonato, G. Vicedomini, L. Zecca, W. Hirth, K. Libson, J. C. Bhatia, F. Fazio

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Abstract

The biodistribution of the three cationic 99mTc complexes [99mTc(TMP6]+, [99mTc(POM-POM)3]+, and [99mTc(TBIN)6]+ - where TMP represents trimethylphosphite, POM-POM represents 1,2-bis(dimethyoxyphosphino)ethane, and TBIN represents t-butylisonitrile - have been evaluated in humans and dogs. Each agent was studied in three normal volunteers at rest, while [99mTc(POM-POM)3]+ and [99mTc(TBIN)6]+ were each studied in one normal volunteer at exercise. Even though all three agents yield good myocardial images in dogs, none appear suitable for clinical use as myocardial perfusion imaging radiopharmaceuticals. In humans, [99mTc(TMP6]+ and [99mTc(POM-POM)3]+ clear very slowly from the blood and provide myocardial images only several hours after injection. [99mTc(TBIN)6]+ clears rapidly from the blood, but accumulation in the lung obscures the myocardial image for the first hour after injection; at later times, activity in the liver and spleen masks the apical wall. These results correlate with the blood-binding properties of the three complexes. [99mTc(TMP6]+ and [99mTc(POM-POM)3]+ bind tightly to the plasma of human blood, but not to the plasma of dog blood; [99mTc(TBIN)6]+ does not bind tightly to the plasma of either dog or human blood. Among the Tc(l) complexes studied to date in humans, [99mTc(TBIN)6]+ appears to be unique in biodistribution pattern, blood-binding properties, and the fact that exercise improves the ultimate myocardial image. All the Tc(l) complexes appear to undergo myocardial accumulation by a mechanism different from that utilized by Tc(l) complexes. Animal studies alone are not adequate to evaluate the potential utility of 99mTc cationic complexes for myocardial perfusion studies.

Original languageEnglish
Pages (from-to)409-416
Number of pages8
JournalJournal of Nuclear Medicine
Volume27
Issue number3
Publication statusPublished - 1986

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Technetium
Perfusion
Dogs
Healthy Volunteers
Exercise
Thymidine Monophosphate
Injections
Myocardial Perfusion Imaging
Ethane
Radiopharmaceuticals
Masks
Spleen
Lung
Liver

ASJC Scopus subject areas

  • Radiological and Ultrasound Technology

Cite this

Gerundini, P., Savi, A., Gilardi, M. C., Margonato, A., Vicedomini, G., Zecca, L., ... Fazio, F. (1986). Evaluation in dogs and humans of three potential technetium-99m myocardial perfusion agents. Journal of Nuclear Medicine, 27(3), 409-416.

Evaluation in dogs and humans of three potential technetium-99m myocardial perfusion agents. / Gerundini, P.; Savi, A.; Gilardi, M. C.; Margonato, A.; Vicedomini, G.; Zecca, L.; Hirth, W.; Libson, K.; Bhatia, J. C.; Fazio, F.

In: Journal of Nuclear Medicine, Vol. 27, No. 3, 1986, p. 409-416.

Research output: Contribution to journalArticle

Gerundini, P, Savi, A, Gilardi, MC, Margonato, A, Vicedomini, G, Zecca, L, Hirth, W, Libson, K, Bhatia, JC & Fazio, F 1986, 'Evaluation in dogs and humans of three potential technetium-99m myocardial perfusion agents', Journal of Nuclear Medicine, vol. 27, no. 3, pp. 409-416.
Gerundini, P. ; Savi, A. ; Gilardi, M. C. ; Margonato, A. ; Vicedomini, G. ; Zecca, L. ; Hirth, W. ; Libson, K. ; Bhatia, J. C. ; Fazio, F. / Evaluation in dogs and humans of three potential technetium-99m myocardial perfusion agents. In: Journal of Nuclear Medicine. 1986 ; Vol. 27, No. 3. pp. 409-416.
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abstract = "The biodistribution of the three cationic 99mTc complexes [99mTc(TMP6]+, [99mTc(POM-POM)3]+, and [99mTc(TBIN)6]+ - where TMP represents trimethylphosphite, POM-POM represents 1,2-bis(dimethyoxyphosphino)ethane, and TBIN represents t-butylisonitrile - have been evaluated in humans and dogs. Each agent was studied in three normal volunteers at rest, while [99mTc(POM-POM)3]+ and [99mTc(TBIN)6]+ were each studied in one normal volunteer at exercise. Even though all three agents yield good myocardial images in dogs, none appear suitable for clinical use as myocardial perfusion imaging radiopharmaceuticals. In humans, [99mTc(TMP6]+ and [99mTc(POM-POM)3]+ clear very slowly from the blood and provide myocardial images only several hours after injection. [99mTc(TBIN)6]+ clears rapidly from the blood, but accumulation in the lung obscures the myocardial image for the first hour after injection; at later times, activity in the liver and spleen masks the apical wall. These results correlate with the blood-binding properties of the three complexes. [99mTc(TMP6]+ and [99mTc(POM-POM)3]+ bind tightly to the plasma of human blood, but not to the plasma of dog blood; [99mTc(TBIN)6]+ does not bind tightly to the plasma of either dog or human blood. Among the Tc(l) complexes studied to date in humans, [99mTc(TBIN)6]+ appears to be unique in biodistribution pattern, blood-binding properties, and the fact that exercise improves the ultimate myocardial image. All the Tc(l) complexes appear to undergo myocardial accumulation by a mechanism different from that utilized by Tc(l) complexes. Animal studies alone are not adequate to evaluate the potential utility of 99mTc cationic complexes for myocardial perfusion studies.",
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AU - Savi, A.

AU - Gilardi, M. C.

AU - Margonato, A.

AU - Vicedomini, G.

AU - Zecca, L.

AU - Hirth, W.

AU - Libson, K.

AU - Bhatia, J. C.

AU - Fazio, F.

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