One approach to anticancer treatment is targeted anti-angiogenic
therapy (AAT) based on prevention of blood vessel formation around the developing
cancer cells. It is known that
vascular endothelial growth factor (
VEGF) and
vascular endothelial growth factor receptors (VEGFRs) play a pivotal role in angiogenesis process; hence, application of
angiogenesis inhibitors can be an effective approach in anticancer combination therapeutic strategies. Currently, several types of molecules have been utilised in targeted
VEGF/VEGFR anticancer
therapy, including human
VEGF ligands themselves and their derivatives, anti-
VEGF or anti-VEGFR
monoclonal antibodies,
VEGF binding
peptides and small molecular inhibitors of VEGFR
tyrosine kinases. These molecules labelled with diagnostic or therapeutic
radionuclides can become, respectively, diagnostic or therapeutic receptor
radiopharmaceuticals. In targeted anti-angiogenic
therapy, diagnostic radioagents play a unique role, allowing the determination of the emerging tumour, to monitor the course of treatment, to predict the treatment outcomes and, first of all, to refer patients for AAT. This review provides an overview of design, synthesis and study of radiolabelled
VEGF/VEGFR targeting and imaging agents to date. Additionally, we will briefly discuss their physicochemical properties and possible application in combination targeted
radionuclide tumour
therapy.