Abstract
The interest in zirconium-89 (89Zr) as a positron-emitting radionuclide has grown considerably over the last decade due to its standardized production, long half-life of 78.2 h, favorable decay characteristics for positron emission tomography (PET) imaging and its successful use in a variety of clinical and preclinical applications. However, to be utilized effectively in PET applications it must be stably bound to a targeting ligand, and the most successfully used 89Zr chelator is desferrioxamine B (DFO), which is commercially available as the iron chelator Desferal®. Despite the prevalence of DFO in 89Zr-immuno-PET applications, the development of new ligands for this radiometal is an active area of research. This review focuses on recent advances in zirconium-89 chelation chemistry and will highlight the rapidly expanding ligand classes that are under investigation as DFO alternatives.
Highlights
Over the last four decades, molecular imaging has had a transformative effect on the way research is conducted in academia, industry and on how medical care is managed in the clinic [1,2,3,4,5,6,7,8]
Of the modalities available to preclinical researchers and clinicians, the popularity of the nuclear medicine technique positron emission tomography (PET) has surged since it provides physiological data relating to disease pathophysiology, receptor expression levels, enzyme activity and cellular metabolism non-invasively and quantitatively [9,10,11,12]
While research in these areas has provided numerous societal benefits including heat and corrosion resistant coatings; fracture resistant ceramics; and the development of catalysts that play a role in the petroleum, plastics, and pharmaceutical industries, it has been difficult to translate this knowledge into the research fields of radiochemistry and molecular imaging
Summary
Over the last four decades, molecular imaging has had a transformative effect on the way research is conducted in academia, industry and on how medical care is managed in the clinic [1,2,3,4,5,6,7,8]. It ejects a positron from its nucleus, which after travelling a short distance, undergoes a process called annihilation with an electron to release two 511 keV γ rays 180◦ apart. These coincident gamma rays have sufficient energy to escape the organism and can be detected by the PET scanner. PET isotopes such as 18 F, 15 O, 13 N, 11 C and 68 Ga; which have relatively short half-lives, were developed for use with small molecules or peptides that demonstrated rapid target tissue accumulation and clearance, and facilitated the imaging of physiological processes within the first 24 h of radiopharmaceutical injection [15]. Its impact on antibody and nanoparticle development, clinical trials and precision medicine strategies has been reviewed extensively [14,15,16,20,21,22,23,24,25,26,27,28,29,30,31,32,33,34,35,36,37,38,39,40,41,42,43,44,45,46]
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