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(111)Indium Labelling of Recombinant Activated Coagulation Factor VII: In Vitro and Preliminary In Vivo Studies in Healthy Rats.

Identifieur interne : 001023 ( Main/Exploration ); précédent : 001022; suivant : 001024

(111)Indium Labelling of Recombinant Activated Coagulation Factor VII: In Vitro and Preliminary In Vivo Studies in Healthy Rats.

Auteurs : RBID : pubmed:22518302

Abstract

The aim of this study is to investigate whether (111)Indium-labelled recombinant FVIIa (rFVIIa) could be a potential radiopharmaceutical for localization of bleeding sources. DTPA-conjugated rFVIIa was radiolabelled with (111)In chloride. In vitro binding efficiency of (111)In-DTPA-rFVIIa to F1A2-Mab-sepharose was 99% in buffer, while it was 88-82% in serum. The binding efficiency of (111)In-DTPA-rFVIIa to TF (1-209)-sepharose was 48% in buffer whereas 39%-36% in serum, respectively. In vivo experiment was conducted in healthy rats, and gamma camera images were taken immediately after iv. administration of 1.6-1.8 MBq (111)In-DTPA-rFVIIa up to 120-130 min. Five min after administration of (111)In-DTPA-rFVIIa, percentage of (111)In activity was 6.0% in the cardiac region and 24.5% in the liver region. After 2 hours activity was decreased to 3.3% in heart while it had increased to 42.0% in the liver. The (111)In-DTPA-rFVIIa might be a potential radiopharmaceutical for visualisation of tissues with significant TF expression such as acute bleeding lesions in the gastrointestinal tract.

DOI: 10.1155/2012/464810
PubMed: 22518302

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<name sortKey="Nalla, Amarnadh" uniqKey="Nalla A">Amarnadh Nalla</name>
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<nlm:affiliation>Institute of Biomedical Sciences, Faculty of Health Sciences, University of Copenhagen, DK-2200, Copenhagen, Denmark.</nlm:affiliation>
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<name sortKey="Buch, Inge" uniqKey="Buch I">Inge Buch</name>
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<name sortKey="Sigvardt, Maibritt" uniqKey="Sigvardt M">Maibritt Sigvardt</name>
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<name sortKey="Bodholdt, Rasmus Poul" uniqKey="Bodholdt R">Rasmus Poul Bodholdt</name>
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<name sortKey="Kjaer, Andreas" uniqKey="Kjaer A">Andreas Kjaer</name>
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<name sortKey="Hesse, Birger" uniqKey="Hesse B">Birger Hesse</name>
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<div type="abstract" xml:lang="en">The aim of this study is to investigate whether (111)Indium-labelled recombinant FVIIa (rFVIIa) could be a potential radiopharmaceutical for localization of bleeding sources. DTPA-conjugated rFVIIa was radiolabelled with (111)In chloride. In vitro binding efficiency of (111)In-DTPA-rFVIIa to F1A2-Mab-sepharose was 99% in buffer, while it was 88-82% in serum. The binding efficiency of (111)In-DTPA-rFVIIa to TF (1-209)-sepharose was 48% in buffer whereas 39%-36% in serum, respectively. In vivo experiment was conducted in healthy rats, and gamma camera images were taken immediately after iv. administration of 1.6-1.8 MBq (111)In-DTPA-rFVIIa up to 120-130 min. Five min after administration of (111)In-DTPA-rFVIIa, percentage of (111)In activity was 6.0% in the cardiac region and 24.5% in the liver region. After 2 hours activity was decreased to 3.3% in heart while it had increased to 42.0% in the liver. The (111)In-DTPA-rFVIIa might be a potential radiopharmaceutical for visualisation of tissues with significant TF expression such as acute bleeding lesions in the gastrointestinal tract.</div>
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<AbstractText>The aim of this study is to investigate whether (111)Indium-labelled recombinant FVIIa (rFVIIa) could be a potential radiopharmaceutical for localization of bleeding sources. DTPA-conjugated rFVIIa was radiolabelled with (111)In chloride. In vitro binding efficiency of (111)In-DTPA-rFVIIa to F1A2-Mab-sepharose was 99% in buffer, while it was 88-82% in serum. The binding efficiency of (111)In-DTPA-rFVIIa to TF (1-209)-sepharose was 48% in buffer whereas 39%-36% in serum, respectively. In vivo experiment was conducted in healthy rats, and gamma camera images were taken immediately after iv. administration of 1.6-1.8 MBq (111)In-DTPA-rFVIIa up to 120-130 min. Five min after administration of (111)In-DTPA-rFVIIa, percentage of (111)In activity was 6.0% in the cardiac region and 24.5% in the liver region. After 2 hours activity was decreased to 3.3% in heart while it had increased to 42.0% in the liver. The (111)In-DTPA-rFVIIa might be a potential radiopharmaceutical for visualisation of tissues with significant TF expression such as acute bleeding lesions in the gastrointestinal tract.</AbstractText>
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