Wolf W, Shani J
Int J Rad Appl Instrum B. 1986;13(4):319-24. doi: 10.1016/0883-2897(86)90004-8.
Efficient labeling of monoclonal antibodies depends on a number of key factors, mostly related to the characteristics of the radionuclide itself and to the manner of its incorporation into the protein. Such factors include the physical half-life, the photon or particle energy of the radionuclide and its selective deposition of energy in tissues, the method of labeling used (covalent binding or chelation), and the effect that the chemical changes inherent in the labeling process may have on the properties of the protein or of its fragments. The major biological factor in determining the radionuclide of choice for labeling is the projected use of the labeled antibody. When the intended use is diagnostic, then what is required is high-photon density for achieving the high resolution needed for imaging, whereas therapeutic use requires radionuclides with high energy deposition at the target sites, i.e. beta or alpha emitters. A further consideration is to be given to the mode of administration of the radiolabeled monoclonal antibody: determination of the radiopharmacokinetic parameters of compartmental models of biodistribution of the labeled monoclonal antibody and/or its fragments may also assist in selecting which radionuclide may be best to use for radiolabeling a given monoclonal antibody intended for either tumor diagnosis, prognosis and/or therapy.
单克隆抗体的有效标记取决于许多关键因素，这些因素大多与放射性核素本身的特性及其掺入蛋白质的方式有关。这些因素包括物理半衰期、放射性核素的光子或粒子能量及其在组织中的能量选择性沉积、所使用的标记方法（共价结合或螯合），以及标记过程中固有的化学变化可能对蛋白质或其片段性质产生的影响。决定用于标记的放射性核素的主要生物学因素是标记抗体的预期用途。当预期用途是诊断时，需要高光子密度以实现成像所需的高分辨率，而治疗用途则需要在靶位点具有高能量沉积的放射性核素，即β或α发射体。还需要进一步考虑放射性标记单克隆抗体的给药方式：确定标记单克隆抗体和/或其片段生物分布的房室模型的放射性药代动力学参数，也可能有助于选择哪种放射性核素最适合用于标记用于肿瘤诊断、预后和/或治疗的给定单克隆抗体。
