Nuclear Medicine and Biology
Volume 34, Issue 3 , Pages 315-323 , April 2007

The biodistribution of NC100668 and the effect of excess NC100668 on the biodistribution and kidney retention of 99mTc-NC100668 in the rat

  • David Edwards

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
    • Corresponding Author InformationCorresponding author. Tel.: +44 14 94 54 51 29; fax: +44 14 94 54 32 84.
  • ,
  • Joanne Lewis

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
  • ,
  • Mark Battle

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
  • ,
  • Rochelle Lear

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
  • ,
  • Gill Farrar

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
  • ,
  • David J. Barnett

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
  • ,
  • Vanessa Godden

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
  • ,
  • Catherine Edwards

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
  • ,
  • Alexandra Oliveira

      Affiliations

    • Research and Development, GE Healthcare Bio-Sciences, The Grove Centre, HP7 9LL Amersham, United Kingdom
  • ,
  • Håkan Ahlström

      Affiliations

    • Institution of Oncology, Radiology and Clinical Immunology, Section of Radiology, Uppsala University Hospital, SE-751 85 Uppsala, Sweden

Received 16 August 2006 ,Revised 24 January 2007 ,Accepted 25 January 2007.

References 

  1. Lijnen HR, Holmes WE, van Hoef B, Wiman B, Rodriguez H, Collen D. Amino-acid sequence of human α2-antiplasmin. Eur J Biochem. 1987;166:565–574
  2. Ichinose A, Tamaki T, Aoki N. Factor XIII-mediated cross-linking of NH2-terminal peptide of α2-plasmin inhibitor to fibrin. FEBS Lett. 1983;155:369–371
  3. Lee KN, Lee CS, Tae W-C, Jackson KW, Christiansen VJ, McKee PA. Crosslinking of α2-antiplasmin to fibrin. Ann N Y Acad Sci. 2001;936:335–339
  4. Jaffer FA, Tung CH, Wykrzykowska JJ, Ho NH, Houng AK, Reed GL, et al. Molecular imaging of factor XIIIa activity in thrombosis using a novel, near-infrared fluorescent contrast agent that covalently links to thrombi. Circulation. 2004;110:170–176
  5. Edwards D, Lewis J, Battle M, Lear R, Farrar G, Barnett DJ, et al. 99mTc-NC100668, a new tracer for imaging venous thromboemboli: pre-clinical biodistribution and incorporation into plasma clots in vivo and in vitro. Eur J Nucl Med. 2006;33:1258–1265
  6. Behr TM, Goldenberg DM, Becker W. Reducing the renal uptake of radiolabeled antibody fragments and peptides for diagnosis and therapy: present status, future prospects and limitations. Eur J Nucl Med. 1998;25:201–212
  7. Bernard BF, Krenning EP, Breeman WA, Rolleman EJ, Bakker WH, Visser TJ, et al. d-lysine reduction of indium-111 octreotide and yttrium-90 octreotide renal uptake. J Nucl Med. 1997;38:1929–1933
  8. Derrick EK, Barker JNWN, Khan A, Price ML, MacDonald DM. The tissue distribution of FXIIIa positive cells. Histopathology. 1993;22:157–162
  9. Thomázy V, Fésüs L. Differential expression of tissue transglutaminase on human cells. An immunohistochemical study. Cell Tissue Res. 1989;255:215–224
  10. Food and Drug Administration . Guidance for industry and reviewers: estimating the safe starting dose in clinical trials for therapeutics in adult healthy volunteers. The Food and Drug Administration; 2002;
  11. MacIomhair M, Lavelle SM. Thrombus weight as a measure of hypercoagulability induced by drugs. Thromb Haemost. 1979;42:1018–1021
  12. Donaldson HH. The rat: data and reference tables. 2nd ed. The Wistar Institute of Anatomy and Biology; 1924;
  13. Skotland T, Hustvedt SO, Oulie I, Jacobsen PB, Friisk GA, Langøy AS, et al. NC100668, a new tracer for imaging of venous thromboembolism: disposition and metabolism in rats. Drug Metab Dispos. 2006;34:111–120
  14. Kung MP, Stevenson DA, Plössl K, Meegalla S, Beckwith A, Essman WD, et al. [99mTc]TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent. Eur J Nucl Med. 1997;24:372–380
  15. Verwijnen SM, Krenning EP, Valkema R, Huijmans JGM, de Jong M. Oral versus intravenous administration of lysine: equal effectiveness in reduction or renal uptake of [111In-DTPA]octreotide. J Nucl Med. 2006;46:2057–2060
  16. DePalatis LR, Frazier KA, Cheng RC, Kotite NJ. Lysine reduces renal accumulation of radioactivity associated with injection of the [177Lu]alpha-[2-(4-aminophenyl) ethyl]-1,4,7,10-tetraaza-cyclodecane-1,4,7,10-tetraacetic acid-CC49 Fab radioimmunoconjugate. Cancer Res. 1995;55:5288–5295
  17. Barone R, Van Der Smissen P, Devuyst O, Beaujean V, Pauwels S, Coutoy PJ, et al. Endocytosis of the somatostatin analogue, octreotide, by the proximal tubule-derived opossum kidney (OK) cell line. Kidney Int. 2005;67:969–976
  18. Melis M, Krenning EP, Bernard BF, Barone R, Visser TJ, de Jong M. Localisation and mechanism of renal retention of radiolabelled somatostatin analogues. Eur J Nucl Med Mol Imaging. 2005;32:1136–1143
  19. Edwards D, Battle M, Lear R, Farrar G, Barnett DJ, Godden V, et al. The in vivo and in vitro metabolic profile of 99mTc-NC100668, a new tracer for imaging venous thromboembolism: identification and biodistribution of the principal radiolabeled metabolite. Drug Metab Dispos. 2006;34:1128–1135
  20. Edwards D, Lewis J, Battle M, Lear R, Farrar G, Barnett DJ, et al. 99mTc-NC100668, an agent for imaging venous thromboembolism. The effect of anticoagulant or thrombolytic therapy on the uptake and retention of radioactivity in blood clot in vivo. Nucl Med Commun. 2007;28:55–62

 The authors of this work are all employees of GE Healthcare, with the exception of Prof. H. Ahlström, who is a consultant for GE Healthcare.

PII: S0969-8051(07)00015-7

doi: 10.1016/j.nucmedbio.2007.01.008

Nuclear Medicine and Biology
Volume 34, Issue 3 , Pages 315-323 , April 2007