2003
DOI: 10.1259/bjr/30385847
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Comparison between human pharmacokinetics and imaging properties of two conjugation methods for99mTc-Annexin A5

Abstract: Annexin A5 (AnxA5) is a protein with high affinity for phosphatidyl serine, a phospholipid exposed on the cell surface during apoptosis. This phenomenon has been used for determination of cell death after myocardial infarction. To evaluate the potential of (99m)Tc-AnxA5 for in vivo scintigraphy of apoptotic cells, the pharmacokinetics and imaging properties of two radiopharmaceuticals, (99m)Tc-(n-1-imino-4-mercaptobutyl)-AnxA5 (I-AnxA5) and (99m)Tc-(4,5-bis(thioacetamido)pentanoyl)-AnxA5 (B-AnxA5), were studie… Show more

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Cited by 42 publications
(34 citation statements)
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“…In humans, Tc-labeled annexin V has been used to detect apoptosis in the hearts of patients with acute myocardial infarction (34) as well as during acute cardiac rejection (56) and in an intracardiac tumor (57). More recently, 99m Tc-labeled annexin V was used in a quantitative tumor apoptosis imaging study using singlephoton emission computed tomography in patients with head and neck carcinoma (35,36). Biodistribution and dosimetry measurements of various forms of 99m Tc-labeled annexin V in humans point to the safety of this tracer and its suitability for use in a clinical setting (58 -60).…”
Section: Discussionmentioning
confidence: 99%
See 1 more Smart Citation
“…In humans, Tc-labeled annexin V has been used to detect apoptosis in the hearts of patients with acute myocardial infarction (34) as well as during acute cardiac rejection (56) and in an intracardiac tumor (57). More recently, 99m Tc-labeled annexin V was used in a quantitative tumor apoptosis imaging study using singlephoton emission computed tomography in patients with head and neck carcinoma (35,36). Biodistribution and dosimetry measurements of various forms of 99m Tc-labeled annexin V in humans point to the safety of this tracer and its suitability for use in a clinical setting (58 -60).…”
Section: Discussionmentioning
confidence: 99%
“…Annexin V labeled with a fluorescent tag is routinely used for histological and cell-sorting studies to identify apoptotic cells (32). In vivo, annexin has been conjugated to technetium-99m ( 99m Tc) for scintigraphy (33)(34)(35)(36), superparamagnetic iron oxide nanoparticles for apoptosis detection by magnetic resonance imaging (37), and the Cy5.5 fluorescent dye for near-infrared optical imaging (38,39).…”
mentioning
confidence: 99%
“…As a radiolabeled probe, it is thus employed to detect apoptotic changes in tissues of live animals. However, in such scenarios the protein accumulates mainly in the kidney, liver, and gastrointestinal tract, which limits its usefulness for imaging of ongoing apoptosis in the abdominal and thoracic region (4,31,36). The exceptionally high kidney uptake of radiolabeled annexin A5, together with a comparatively long half-life of 24 h, could be an indication of specific biological interactions of the protein with renal epithelial cells.…”
Section: Annexin A5mentioning
confidence: 99%
“…[41][42][43][44] The first clinical imaging studies of therapy induced tumor apoptosis were conducted using human rh-annexin V labeled with 99m Tc-pertechnetate by the penthioate radioligand (N 2 S 2 ) method. 45 This method begins with the chelation of 99m Tc in the presence of stannous gluconate to yield 99m Tc-gluconate which is then reacted with acidified phenthioate ligand under heating to form a stable 99m Tc-N 2 S 2 complex. The 99m Tc-N 2 S 2 -TFP ester complex is then randomly conjugated to the N-H groups of lysine of the protein at basic pH.…”
mentioning
confidence: 99%