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

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  • Amarnadh Nalla
  • Inge Buch
  • Maibritt Sigvardt
  • Rasmus Poul Bodholdt
  • Kjær, Andreas
  • Birger Hesse
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.
Original languageEnglish
JournalInternational Journal of Molecular Imaging
Volume2012
Number of pages7
ISSN2090-1712
DOIs
Publication statusPublished - 2012

ID: 41800604