Figure 1: Schematic sketch of the general design of tumour targeting radiotracers.
Table 1: Examples of radionuclides for different applications in nuclear medicine.

Radiopharmaceuticals of interest in nuclear oncology are conjugates that combine a radionuclide specific for a given application (Table 1) with a biological vector that is specific for a recognition element overexpressed by tumour cells (Figure 1). Depending on the application, the nature of the radionuclide and the vector molecule, different chemical and biological techniques are required for their preparation.
For preclinical evaluation, the radiopharmaceuticals are first tested in vitro (on cells), which usually includes experiments determining cellular uptake, affinity towards a given receptor/antigen, and other parameters (e.g., metabolic stability, hydrophilicity (logD), plasma protein binding etc.). Promising candidates are then carried forwards to in vivo investigations (in mice) for determination of their pharmacokinetic and -dynamic properties employing biodistribution experiments and/or small animal imaging by µSPECT/PET/CT.

Bioinorganic Radiochemistry

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