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Cumulated Activity Comparison of 64Cu-/177Lu-Labeled Anti-Epidermal Growth Factor Receptor Antibody in Esophageal Squamous Cell Carcinoma Model.

Abstract
This work aimed at estimating the kinetic parameters, and hence cumulated activity (AC), of a diagnostic/therapeutic convergence radiopharmaceutical, namely 64Cu-/177Lu-labeled antibody (64Cu-/177Lu-cetuximab), that acts as anti-epidermal growth factor receptor. Methods: In mice bearing esophageal squamous cell carcinoma tumors, to estimate uptake (K), release rate constant (kR), and hence AC, a kinetic model analysis was applied to recently published biodistribution data of immuno-PET imaging with 64Cu-cetuximab and of small-animal SPECT/CT imaging with 177Lu-cetuximab, including blood and TE-8 tumor. Results: K, kR, and AC were estimated to be 0.0566/0.0593 g⋅h-1⋅g-1, 0.0150/0.0030 h-1, and 2.3 × 1010/4.1 × 1012 disintegrations (per gram of TE-8 tumor), with an injected activity of 3.70/12.95 MBq, for 64Cu-/177Lu-cetuximab, respectively. Conclusion: A model is available for comparing kinetic parameters and AC of the companion diagnostic/therapeutic 64Cu-/177Lu-cetuximab that may be considered as a step for determining whether one can really use the former to predict dosimetry of the latter.
AuthorsEric Laffon, Matthieu Thumerel, Jacques Jougon, Roger Marthan
JournalJournal of nuclear medicine : official publication, Society of Nuclear Medicine (J Nucl Med) Vol. 58 Issue 6 Pg. 888-890 (06 2017) ISSN: 1535-5667 [Electronic] United States
PMID28082435 (Publication Type: Comparative Study, Journal Article)
Copyright© 2017 by the Society of Nuclear Medicine and Molecular Imaging.
Chemical References
  • Antibodies, Monoclonal
  • Copper Radioisotopes
  • Radioisotopes
  • Radiopharmaceuticals
  • Lutetium
  • ErbB Receptors
Topics
  • Animals
  • Antibodies, Monoclonal (pharmacokinetics)
  • Carcinoma, Squamous Cell (diagnostic imaging, metabolism, pathology)
  • Cell Line, Tumor
  • Computer Simulation
  • Copper Radioisotopes (pharmacokinetics)
  • ErbB Receptors (metabolism)
  • Esophageal Neoplasms (diagnostic imaging, metabolism, pathology)
  • Lutetium (pharmacokinetics)
  • Metabolic Clearance Rate
  • Mice
  • Models, Biological
  • Positron-Emission Tomography (methods)
  • Radiation Dosage
  • Radioisotopes (pharmacokinetics)
  • Radiopharmaceuticals (pharmacokinetics)
  • Tissue Distribution

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