Title:Bifunctional Chelators in the Design and Application of Radiopharmaceuticals for Oncological Diseases
Volume: 19
Issue: 17
Author(s): D. Sarko, M. Eisenhut, U. Haberkorn and W. Mier
Affiliation:
Keywords:
Bifunctional chelating agent (BFCA), DOTA, nuclear medicine, radiochemistry, radiometals, radiopharmaceuticals, targeting,
theranostics
Abstract: Radiopharmaceuticals constitute diagnostic and therapeutic tools for both clinical and preclinical applications. They are a
blend of a tracer moiety that mediates a site specific accumulation and an effector: a radioisotope whose decay enables either molecular
imaging or exhibits cytotoxic effects. Radioactive halogens and lanthanides are the most commonly used isotopes for
radiopharmaceuticals. Due to their ready availability and the facile labeling metallic radionuclides offer ideal characteristics for
applications in nuclear medicine. A stable link between the radionuclide and the carrier molecule is the primary prerequisite for in vivo
applications. The radionuclide is selected according to its physical and chemical properties i.e. half-life, the type of decay, the energy
emitted and its availability. Bifunctional chelating agents are used to stably link the radiometal to the carrier moiety of the
radiopharmaceutical. The design of the bifunctional chelator has to consider the impact of the radiometal chelate on the biological
properties of the target-specific pharmaceutical. Here, with an emphasis on oncology, we review applications of radiopharmaceuticals
that contain bifunctional chelators, while highlighting successes and identifying the key challenges that need to be addressed for the
successful translation of target binding molecules into tracers for molecular imaging and endoradiotherapy.
