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.
J Nucl Med. 2017 Jun;58(6):888-890. doi: 10.2967/jnumed.116.180521. Epub 2017 Jan 12.
This work aimed at estimating the kinetic parameters, and hence cumulated activity (A), of a diagnostic/therapeutic convergence radiopharmaceutical, namely Cu-/Lu-labeled antibody (Cu-/Lu-cetuximab), that acts as anti-epidermal growth factor receptor. In mice bearing esophageal squamous cell carcinoma tumors, to estimate uptake (K), release rate constant (k), and hence A, a kinetic model analysis was applied to recently published biodistribution data of immuno-PET imaging with Cu-cetuximab and of small-animal SPECT/CT imaging with Lu-cetuximab, including blood and TE-8 tumor. K, k, and A were estimated to be 0.0566/0.0593 g⋅h⋅g, 0.0150/0.0030 h, and 2.3 × 10/4.1 × 10 disintegrations (per gram of TE-8 tumor), with an injected activity of 3.70/12.95 MBq, for Cu-/Lu-cetuximab, respectively. A model is available for comparing kinetic parameters and A of the companion diagnostic/therapeutic Cu-/Lu-cetuximab that may be considered as a step for determining whether one can really use the former to predict dosimetry of the latter.
本工作旨在估算一种诊断/治疗融合放射性药物（即 Cu-/Lu 标记的抗体（Cu-/Lu-西妥昔单抗））的动力学参数，从而得出累积活度（A）。该放射性药物作为抗表皮生长因子受体。在携带食管鳞状细胞癌肿瘤的小鼠中，为了估算摄取（K）、释放速率常数（k），从而得出 A，应用动力学模型分析方法对最近发表的 Cu-西妥昔单抗免疫 PET 成像和 Lu-西妥昔单抗小动物 SPECT/CT 成像的生物分布数据进行了分析，包括血液和 TE-8 肿瘤。分别估算出 Cu-/Lu-cetuximab 的 K、k 和 A 值为 0.0566/0.0593 g⋅h⋅g、0.0150/0.0030 h 和 2.3×10/4.1×10 次衰变（每克 TE-8 肿瘤），注射活度为 3.70/12.95 MBq。对于诊断/治疗用的 Cu-/Lu-西妥昔单抗，该模型可用于比较动力学参数和 A，这可能是确定是否可以真正使用前者来预测后者的剂量学的一个步骤。
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