Design and Challenges of Radiopharmaceuticals

This review describes general concepts with regard to radiopharmaceuticals for diagnostic or therapeutic applications that help to understand the specific challenges encountered during the design, (radio)synthesis, in vitro and in vivo evaluation and clinical translation of novel radiopharmaceuticals. The design of a radiopharmaceutical requires upfront decisions with regard to combining a suitable vector molecule with an appropriate radionuclide, considering the type and location of the molecular target, the desired application, and the time constraints imposed by the relatively short half-life of radionuclides. Well-designed in vitro and in vivo experiments allow nonclinical validation of radiotracers. Ultimately, in combination with a limited toxicology package, the radiotracer becomes a radiopharmaceutical for clinical evaluation, produced in compliance with regulatory requirements for medicines for intravenous (IV) injection.