Synthesis of HBED–CC–tris(tert-butyl ester) using a solid phase and a microwave reactor

The development of peptide-based, radiometal-labeled PET imaging agents has seen an increase in attention due to the favorable properties the peptide backbone exhibits. These include high selectivity and affinity to proteins and cells directly linked to various types of cancers. In addition, rapid clearance from circulation and low toxicity allow for unique approaches to engineering a viable peptide-based imaging agent. Utilizing peptides as the backbone allows for various modifications to improve metabolic stability, target cell affinity, and image quality and imaging capabilities and reduce toxicity. Select radiolabeled peptides have already been FDA approved, with many more in late-stage trials. This review summarizes the current state of the radiometal-labeled PET peptide imaging field as well as explores methods used by researchers to modify peptides, concluding with a look at the future of peptide-based therapy and diagnostics.

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Modern Developments in Bifunctional Chelator Design for Gallium Radiopharmaceuticals

Davey

Paterson

2022

Molecules

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The positron-emitting radionuclide gallium-68 has become increasingly utilised in both preclinical and clinical settings with positron emission tomography (PET). The synthesis of radiochemically pure gallium-68 radiopharmaceuticals relies on careful consideration of the coordination chemistry. The short half-life of 68 min necessitates rapid quantitative radiolabelling (≤10 min). Desirable radiolabelling conditions include near-neutral pH, ambient temperatures, and low chelator concentrations to achieve the desired apparent molar activity. This review presents a broad overview of the requirements of an efficient bifunctional chelator in relation to the aqueous coordination chemistry of gallium. Developments in bifunctional chelator design and application are then presented and grouped according to eight categories of bifunctional chelator: the macrocyclic chelators DOTA and TACN; the acyclic HBED, pyridinecarboxylates, siderophores, tris(hydroxypyridinones), and DTPA; and the mesocyclic diazepines.

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Synthesis of HBED–CC–tris(tert-butyl ester) using a solid phase and a microwave reactor

Cited by 3 publications

References 20 publications

Synthesis and ex vivo biodistribution of two 68Ga-labeled tetrazine tracers: Comparison of pharmacokinetics

Synthesis and ex vivo biodistribution of two 68Ga-labeled tetrazine tracers: Comparison of pharmacokinetics

Peptide PET Imaging: A Review of Recent Developments and a Look at the Future of Radiometal-Labeled Peptides in Medicine

Modern Developments in Bifunctional Chelator Design for Gallium Radiopharmaceuticals

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