99mTc-3SPboroxime: A neutral 99mTc(III) radiotracer with high heart uptake and long myocardial retention

Xi, Xiaoying; Wang, Lei; Hsu, Bailing; Zhao, Zuoquan; Liu, Shuang; Fang, Wei

doi:10.1007/s12350-020-02087-3

Cited by 4 publications

(3 citation statements)

References 27 publications

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“…Pig model studies confirm that [ 99m Tc]Tc-3SPboroxime shows high initial heart uptake, comparable to that of [ 99m Tc]Tc-Teboroxime, but myocardial clearance is significantly delayed [28,30]. The high initial heart uptake, combined with longer myocardial retention and high heart/background ratios, suggests that this compound may become an attractive candidate for future clinical application by means of the new ultrafast SPECT detectors.…”

Section: Technetium-99m Teboroximementioning

confidence: 64%

“…A new [ 99m Tc]Tc-Teboroxime derivative was recently studied to increase retention in the myocardium. Xi et al [28] reported studies on Sprague Dawley rats of [ 99m Tc]Tc-3SPboroxime, [ 99m Tc]TcCl(CDO)(CDOH) 2 B-3SP)3SP-B(OH) 2 =3-(methylsulfonyl)pyridineboronic acid, another member of the adduct boronic acid complex [ 99m Tc]Tc (III). This compound has the same structural characteristics as the original [ 99m Tc]Tc-Teboroxime complex, except for the replacement of the methyl group added to the boron cap by a sulfonyl group [29] (Figure 2).…”

Section: Technetium-99m Teboroximementioning

confidence: 99%

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Technetium-99m Radiopharmaceuticals for Ideal Myocardial Perfusion Imaging: Lost and Found Opportunities

et al. 2022

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The favorable nuclear properties in combination with the rich coordination chemistry make technetium-99m the radioisotope of choice for the development of myocardial perfusion tracers. In the early 1980s, [99mTc]Tc-Sestamibi, [99mTc]Tc-Tetrofosmin, and [99mTc]Tc-Teboroxime were approved as commercial radiopharmaceuticals for myocardial perfusion imaging in nuclear cardiology. Despite its peculiar properties, the clinical use of [99mTc]Tc-Teboroxime was quickly abandoned due to its rapid myocardial washout. Despite their widespread clinical applications, both [99mTc]Tc-Sestamibi and [99mTc]Tc-Tetrofosmin do not meet the requirements of an ideal perfusion imaging agent due to their relatively low first-pass extraction fraction and high liver absorption. An ideal radiotracer for myocardial perfusion imaging should have a high myocardial uptake; a high and stable target-to-background ratio with low uptake in the lungs, liver, stomach during the image acquisition period; a high first-pass myocardial extraction fraction and very rapid blood clearance; and a linear relationship between radiotracer myocardial uptake and coronary blood flow. Although it is difficult to reconcile all these properties in a single tracer, scientific research in the field has always channeled its efforts in the development of molecules that are able to meet the characteristics of ideality as much as possible. This short review summarizes the developments in 99mTc myocardial perfusion tracers, which are able to fulfill hitherto unmet medical needs and serve a large population of patients with heart disease, and underlines their strengths and weaknesses, the lost and found opportunities thanks to the developments of the new ultrafast SPECT technologies.

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Section: Technetium-99m Teboroximementioning

confidence: 64%

Section: Technetium-99m Teboroximementioning

confidence: 99%

Technetium-99m Radiopharmaceuticals for Ideal Myocardial Perfusion Imaging: Lost and Found Opportunities

et al. 2022

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“…The SPECT image quality with [ 99m Tc]Tc-3SPboroxime in SD rats is better than that with [ 99m Tc]Tc-teboroxime. High heart uptake and long myocardial retention of 99m Tc-3SPboroxime have been confirmed in swine models [41].…”

Section: Myocardial Perfusion Imaging Agentsmentioning

confidence: 82%

Current status and future perspective of radiopharmaceuticals in China

Ji¹,

Li²,

Sui³

et al. 2021

Eur J Nucl Med Mol Imaging

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Reassessment of Radiation Exposure From Bone Scintigraphy

Tanyildizi-Kökkülünk,

Şenişik,

Yüksel

2023

CDM

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Aim: This study was aimed to re-determine the radiation dose rate emitted from the patients who underwent bone scintigraphy. Material and Methods: A mean of 20.87±2.54 mCi 99mTc-MDP was injected into patients. A GM counter was used to measure dose rates in 3 different periods, at intervals of 25, 50, 100, 150, and 200 cm from the patient's anterior for head, thorax, abdomen, and pelvis levels. Measurements were used to determine patient-induced environmental doses and radiation doses to personnel/patient relatives. Results and Discussion: There were strong correlations between mean dose rate (mRh-1mCi-1) and time at all regions and distances. The received dose for staff was calculated between a range of 0.01-0.02 mSv/mCi per patient. The total dose to be received by the companion was estimated to be between 0.019-0.039 and 0.011-0.022 mSv for public and personal vehicle transportation, respectively. The radiation dose exposed by nurses (4th, 6th, and 8th hours after injection) was found to be 0.012-0.064, 0.006-0.038, and 0.002-0.018 mSv/patient, respectively. Conclusion: The fact that the doses of personnel and patient relatives in the study were below the legal limits shows that the study was carried out within a safe range. However, in terms of radiation protection, it is necessary to limit the time spent with the patient as much as possible and increase the distance. Since the dangers of low radiation dosages are unknown, there is a need to inform the patient's relatives and staff about the potential risks.

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99mTc-3SPboroxime: A neutral 99mTc(III) radiotracer with high heart uptake and long myocardial retention

Cited by 4 publications

References 27 publications

Technetium-99m Radiopharmaceuticals for Ideal Myocardial Perfusion Imaging: Lost and Found Opportunities

Technetium-99m Radiopharmaceuticals for Ideal Myocardial Perfusion Imaging: Lost and Found Opportunities

Current status and future perspective of radiopharmaceuticals in China

Reassessment of Radiation Exposure From Bone Scintigraphy

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