title: Cumulated Activity Comparison of64Cu-/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, namely64Cu-/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 with64Cu-cetuximab and of small-animal SPECT/CT imaging with177Lu-cetuximab, including blood and TE-8 tumor.Results:K, kR, and ACwere estimated to be 0.0566/0.0593 g⋅h-1⋅g-1, 0.0150/0.0030 h-1, and 2.3 × 1010/4.1 × 1012disintegrations (per gram of TE-8 tumor), with an injected activity of 3.70/12.95 MBq, for64Cu-/177Lu-cetuximab, respectively.Conclusion:A model is available for comparing kinetic parameters and ACof the companion diagnostic/therapeutic64Cu-/177Lu-cetuximab that may be considered as a step for determining whether one can really use the former to predict dosimetry of the latter.
authors.affiliation: CHU de Bordeaux, Departments of Nuclear Medicine, Thoracic Surgery, and Respiratory Medicine, Bordeaux, France; and elaffon@u-bordeaux2.fr.|University Bordeaux, Centre de Recherche Cardio-Thoracique de Bordeaux, INSERM U-1045, Bordeaux, France.
authors.forename: Eric
authors.initials: E
authors.lastname: Laffon
authors.affiliation: CHU de Bordeaux, Departments of Nuclear Medicine, Thoracic Surgery, and Respiratory Medicine, Bordeaux, France; and.
authors.forename: Matthieu
authors.initials: M
authors.lastname: Thumerel
authors.affiliation: CHU de Bordeaux, Departments of Nuclear Medicine, Thoracic Surgery, and Respiratory Medicine, Bordeaux, France; and.
authors.forename: Jacques
authors.initials: J
authors.lastname: Jougon
authors.affiliation: CHU de Bordeaux, Departments of Nuclear Medicine, Thoracic Surgery, and Respiratory Medicine, Bordeaux, France; and.|University Bordeaux, Centre de Recherche Cardio-Thoracique de Bordeaux, INSERM U-1045, Bordeaux, France.
authors.forename: Roger
authors.initials: R
authors.lastname: Marthan
mesh_terms: D000818:Animals; D000911:Antibodies, Monoclonal / Q000493:pharmacokinetics*; D002294:Carcinoma, Squamous Cell / Q000000981:diagnostic imaging / Q000378:metabolism* / Q000473:pathology; D045744:Cell Line, Tumor; D003198:Computer Simulation; D003301:Copper Radioisotopes / Q000493:pharmacokinetics*; D066246:ErbB Receptors / Q000378:metabolism*; D004938:Esophageal Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism* / Q000473:pathology; D008187:Lutetium / Q000493:pharmacokinetics*; D008657:Metabolic Clearance Rate; D051379:Mice; D008954:Models, Biological; D049268:Positron-Emission Tomography / Q000379:methods; D011829:Radiation Dosage; D011868:Radioisotopes / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D000911:Antibodies, Monoclonal; D003301:Copper Radioisotopes; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D008187:Lutetium; D066246:ErbB Receptors
keywords: 177Lu-labeled SPECT tracer; 64Cu-labeled PET tracer; EGFR; cumulated activity; kinetic model analysis