The Radiopharmaceutical Chemistry of Zirconium-89

Marquez-Nostra, Bernadette; Viola-Villegas, Nerissa

doi:10.1007/978-3-319-98947-1_21

Cited by 5 publications

(7 citation statements)

References 55 publications

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“…Production Method 89 Y(p,n) 89 Zr Decay process EC(77%)/β + (23%)→ 89m Y Half-life time 78.4 h γ ray abundance 909 keV (99.9%); 1657 keV (0.1%); 1713 keV (0.8%) 89 Zr is produced by medical cyclotron through the reaction of 89 Y(p,n) 89 Zr. The halflife time of 89 Zr is 78.4 h, and it decays through the process of positron emission (23%) and electron capture (77%) (Figure 10) [114,115].…”

Section: Nuclear Properties 89 Zrmentioning

confidence: 99%

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Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

Zhou¹,

Dong²,

Shen

2021

Molecules

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Hydroxypyridinones (HOPOs) have been used in the chelation therapy of iron and actinide metals. Their application in metal-based radiopharmaceuticals has also been increasing in recent years. This review article focuses on how multidentate HOPOs can be used in targeted radiometal-based diagnostic and therapeutic radiopharmaceuticals. The general structure of radiometal-based targeted radiopharmaceuticals, a brief description of siderophores, the basic structure and properties of bidentate HOPO, some representative HOPO multidentate chelating agents, radiopharmaceuticals based on HOPO multidentate bifunctional chelators for gallium-68, thorium-227 and zirconium-89, as well as the future prospects of HOPO multidentate bifunctional chelators in other metal-based radiopharmaceuticals are described and discussed in turn. The HOPO metal-based radiopharmaceuticals that have shown good prospects in clinical and preclinical studies are gallium-68, thorium-227 and zirconium-89 radiopharmaceuticals. We expect HOPO multidentate bifunctional chelators to be a very promising platform for building novel targeted radiometal-based diagnostic and therapeutic radiopharmaceuticals.

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Section: Nuclear Properties 89 Zrmentioning

confidence: 99%

“…Similar to gallium(III) ion, zirconium(IV) ion could be considered as hard Lewis acid due to its high charge and small ion radius. As a result, zirconium(IV) ion possesses a strong tendency to interact with hard Lewis bases such as oxygen donor atoms [114].…”

Section: Chemical Property Of 89 Zrmentioning

confidence: 99%

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

Zhou¹,

Dong²,

Shen

2021

Molecules

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“…However, the area of application of zirconium‐89 is not limited to immunoPET alone. 89 Zr is applied to create RPs based on peptides and antibody fragments 9–11 and to label various cells to study their tracking in vivo by PET 12–15 . As shown in publications, 89 Zr can be suitable for imaging at prolonged time intervals (up to 30 days) and estimation of the efficiency of radionuclide therapy with 177 Lu (e.g., in prostate cancer via the application of RPs based on ligands for the prostate‐specific membrane antigen [PSMA]) 16–19 …”

Section: Introductionmentioning

confidence: 99%

“…At the same time, the insufficient stability of DFO‐based conjugates and subsequent accumulation of “released” ionic 89 Zr (~10%ID/g) in bone tissue have been observed in several studies 42–46 . The research and development of more suitable chelators for 89 Zr is a relevant task 10,41,47 . The promising and already commercially available chelator for 89 Zr — DFO* — has been recently developed.…”

Section: Introductionmentioning

confidence: 99%

The impact of zirconium‐89 solution formulation on the efficiency of [⁸⁹Zr]Zr‐deferoxamine synthesis

Бубенщиков

Makichyan

Ларенков

2022

Labelled Comp Radiopharmac

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“…One way to overcome the limitations of IHC is through the use of companion diagnostic agents (CDx), which are imaging biomarkers that could help predict response to corresponding therapeutic drugs. Positron emission tomography (PET) imaging CDx can provide information on the biodistribution of the related therapeutic agents and determine antigen expression throughout the whole body in a noninvasive way [17,18]. In particular, PET imaging with 89 Zrlabeled antibodies has been increasingly used as a noninvasive tool to select patients likely to respond to antibody treatments [17].…”

Section: Introductionmentioning

confidence: 99%

Development of [89Zr]ZrDFO-amivantamab bispecific to EGFR and c-MET for PET imaging of triple-negative breast cancer

Cavaliere

Sun

Lee

et al. 2020

Eur J Nucl Med Mol Imaging

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Background Amivantamab is a novel bispecific antibody that simultaneously targets the epidermal growth factor receptor (EGFR) and the hepatocyte growth factor receptor (HGFR/c-MET) that are overexpressed in several types of cancer including triple-negative breast cancer (TNBC). Targeting both receptors simultaneously can overcome resistance to mono-targeted therapy. The purpose of this study is to develop 89 Zr-labeled amivantamab as a potential companion diagnostic imaging agent to amivantamab therapy using various preclinical models of TNBC for evaluation. Methods Amivantamab was conjugated to desferrioxamine (DFO) and radiolabeled with 89 Zr to obtain [ 89 Zr]ZrDFOamivantamab. Binding of the bispecific [ 89 Zr]ZrDFO-amivantamab as well as its mono-specific "single-arm" antibody controls were determined in vitro and in vivo. Biodistribution studies of [ 89 Zr]ZrDFO-amivantamab were performed in MDA-MB-468 xenografts to determine the optimal imaging time point. PET/CT imaging with [ 89 Zr]ZrDFO-amivantamab or its isotype control was performed in a panel of TNBC xenografts with varying levels of EGFR and c-MET expression. Results [ 89 Zr]ZrDFO-amivantamab was synthesized with a specific activity of 148 MBq/mg and radiochemical yield of ≥ 95%. Radioligand binding studies and western blot confirmed the order of EGFR and c-MET expression levels: HCC827 lung cancer cell (positive control) > MDA-MB-468 > MDA-MB-231 > MDA-MB-453. [ 89 Zr]ZrDFO-amivantamab demonstrated bispecific binding in cell lines co-expressed with EGFR and c-MET. PET/CT imaging with [ 89 Zr]ZrDFO-amivantamab in TNBCxenografted mice showed standard uptake value (SUV mean ) of 6.0 ± 1.1 in MDA-MB-468, 4.2 ± 1.4 in MDA-MB-231, and 1.5 ± 1.4 in MDA-MB-453 tumors, which are consistent with their receptors' expression levels on the cell surface. Conclusion We have successfully prepared a radiolabeled bispecific antibody, [ 89 Zr]ZrDFO-amivantamab, and evaluated its pharmacologic and imaging properties in comparison with its single-arm antibodies and non-specific isotype controls.[ 89 Zr]ZrDFO-amivantamab demonstrated the greatest uptake in tumors co-expressing EGFR and c-MET.

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The Radiopharmaceutical Chemistry of Zirconium-89

Cited by 5 publications

References 55 publications

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

The impact of zirconium‐89 solution formulation on the efficiency of [⁸⁹Zr]Zr‐deferoxamine synthesis

Development of [89Zr]ZrDFO-amivantamab bispecific to EGFR and c-MET for PET imaging of triple-negative breast cancer

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The Radiopharmaceutical Chemistry of Zirconium-89

Cited by 5 publications

References 55 publications

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

The impact of zirconium‐89 solution formulation on the efficiency of [89Zr]Zr‐deferoxamine synthesis

Development of [89Zr]ZrDFO-amivantamab bispecific to EGFR and c-MET for PET imaging of triple-negative breast cancer

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The impact of zirconium‐89 solution formulation on the efficiency of [⁸⁹Zr]Zr‐deferoxamine synthesis