Abstract
With the development of 68Ga and 177Lu radiochemistry, theranostic approaches in modern nuclear medicine enabling patient-centered personalized medicine applications have been growing in the last decade. In conjunction with the search for new relevant molecular targets, the design of innovative chelating agents to easily form stable complexes with various radiometals for theranostic applications has gained evident momentum. Initially conceived for magnetic resonance imaging applications, the chelating agent AAZTA features a mesocyclic seven-membered diazepane ring, conferring some of the properties of both acyclic and macrocyclic chelating agents. Described in the early 2000s, AAZTA and its derivatives exhibited interesting properties once complexed with metals and radiometals, combining a fast kinetic of formation with a slow kinetic of dissociation. Importantly, the extremely short coordination reaction times allowed by AAZTA derivatives were particularly suitable for short half-life radioelements (i.e., 68Ga). In view of these particular characteristics, the scope of this review is to provide a survey on the design, synthesis, and applications in the nuclear medicine/radiopharmacy field of AAZTA-derived chelators.
Highlights
IntroductionAccepted: 14 February 2022As an emerging approach in modern medicine, “theranostics” ( called “theragnostics”) consists of the combination of diagnostic and therapeutic tools to achieve personalized patient care [1]
Accepted: 14 February 2022As an emerging approach in modern medicine, “theranostics” consists of the combination of diagnostic and therapeutic tools to achieve personalized patient care [1]
Since its early patenting [109], AAZTA has positioned itself as a promising chelating agent for imaging applications, opening the way to a family of compounds halfway between the well-known linear and macrocyclic chelating agents
Summary
Accepted: 14 February 2022As an emerging approach in modern medicine, “theranostics” ( called “theragnostics”) consists of the combination of diagnostic and therapeutic tools to achieve personalized patient care [1]. Theranostic in nuclear medicine benefited from the rise of 68 Ga and 177 Lu radiochemistry, allowing easy radiolabeling of the same vector molecule by either a photon-emitting (i.e., 68 Ga for PET imaging) or a particle-emitting (i.e., 177 Lu, beta-emitter for therapy) radioelement. This approach is all the more convenient since the radioelements used are metals, which can be readily complexed by a vector molecule functionalized by a chelating group. New theranostic pairs have recently become increasingly popular, especially those involving scandium-44
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