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

TY - JOUR

T1 - (111)Indium Labelling of Recombinant Activated Coagulation Factor VII

T2 - In Vitro and Preliminary In Vivo Studies in Healthy Rats

AU - Nalla, Amarnadh

AU - Buch, Inge

AU - Sigvardt, Maibritt

AU - Bodholdt, Rasmus Poul

AU - Kjaer, Andreas

AU - Hesse, Birger

PY - 2012

Y1 - 2012

N2 - 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.

AB - 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.

U2 - 10.1155/2012/464810

DO - 10.1155/2012/464810

M3 - Journal article

C2 - 22518302

SN - 2090-1712

VL - 2012

JO - International Journal of Molecular Imaging

JF - International Journal of Molecular Imaging

ER -