Opportunities and potential challenges of using terbium-161 for targeted radionuclide therapy in clinics

Müller, Cristina; Meulen, Nicholas P. van der; Schibli, Roger

doi:10.1007/s00259-023-06316-y

Cited by 10 publications

(4 citation statements)

References 33 publications

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“…In our quest for the magic bullet it has always been postulated that the isotope of choice will transition from beta to alpha to Auger, the pace of this transition has surprised all as 161 Tb is the first Auger emitter (although a combination with betas) that is now becoming widely discussed. A recent review takes stock of 161 Tb; where it is in the drug development pipeline and the potential challenges it will face reaching the clinic (Müller et al 2023 ).…”

Section: Opportunities and Potential Challenges Of Using Terbium-161 ...mentioning

confidence: 99%

Highlight selection of radiochemistry and radiopharmacy developments by editorial board

DaSilva,

Decristoforo,

Mach

et al. 2023

EJNMMI radiopharm. chem.

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Background The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biannual highlight commentary to update the readership on trends in the field of radiopharmaceutical development. Main body This selection of highlights provides commentary on 21 different topics selected by each coauthoring Editorial Board member addressing a variety of aspects ranging from novel radiochemistry to first-in-human application of novel radiopharmaceuticals. Conclusion Trends in radiochemistry and radiopharmacy are highlighted. Hot topics cover the entire scope of EJNMMI Radiopharmacy and Chemistry, demonstrating the progress in the research field in many aspects.

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Section: Opportunities and Potential Challenges Of Using Terbium-161 ...mentioning

confidence: 99%

Highlight selection of radiochemistry and radiopharmacy developments by editorial board

DaSilva,

Decristoforo,

Mach

et al. 2023

EJNMMI radiopharm. chem.

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“…Also, their similar chemical properties allow for the use of identical targeting vectors and bifunctional chelators to label these metals with little to no modification. These similarities allow for a “one size fits all” approach to radio lanthanide labeling and theranostic applications . However, the similarity of chemical properties across the lanthanide series has its downsides, one of which is that the separation of lanthanides from each other is challenging .…”

Section: Introductionmentioning

confidence: 99%

High Separation Factor, High Molar Activity, and Inexpensive Purification Method for the Production of Pure ¹⁶⁵Er

Saghez,

Yang,

Radchenko

2024

Inorg. Chem.

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Introduction: Auger electron-emitting radionuclides with low (0.001−1 keV) energy, short-range (2−500 nm), and high linear energy transfer (4−26 keV/μm) can play an important role in the targeted radionuclide therapy (TRT) of cancer. 165 Er is a pure Auger electron-emitting radionuclide, making it a useful tool for the fundamental studies of the biological effects of Auger electrons. This work develops a simple, inexpensive, high separation factor, and high molar activity radiochemical isolation process for the production of 165 Er (t 1/2 10.36 h) suitable for TRT in vitro and in vivo studies using irradiated nat Ho solid targets. Methods: Small medical cyclotron proton-irradiation of nat Ho targets produced 165 Er in GBq scale quantities. 165 Er was isolated using cation exchange chromatographic resin (AG 50W-X8, 200− 400 mesh, 20 mL, under atmospheric pressure) using α-hydroxyisobutyric acid (70 mM, pH 4.75) followed by extraction using TK212, TK211, and TK221 extraction chromatographic columns. Radio nuclidic and chemical purity of the final 165 Er were confirmed using HPGe Gamma spectrometry and induction coupled plasma−mass spectrometry analysis, respectively. The purified 165 Er was radiolabeled with two radiometal chelators (DOTA and Crown) and used to produce a new Auger electron-emitting radiopharmaceutical, [ 165 Er]Er-Crown-TATE. Results: Irradiation of 200 mg nat Ho targets with 20−30 μA of 12.8 MeV protons produced 165 Er at 25 ± 5 MBq•μA −1 •h −1 . The 4.5 ± 0.5 h radiochemical isolation yielded GBq scale of 165 Er in 0.05 M HCl (2 mL) with a radiochemical yield of 78.0 ± 5.6% decay corrected to the end of bombardment (EoB) and a Ho/ 165 Er separation factor of (1.14 ± 0.25) × 10 6 . The product showed high radio nuclidic purity and chemical purity. Concentration-dependent radiolabeling experiments with Crown and DOTA were performed resulting in the successful labeling of 165 Er with high (>90%) radiochemical yield. Radiolabeling experiments with Crown-TATE were performed 8 h after EoB and synthesized [ 165 Er]Er-Crown-TATE at molar activities of 202.4 MBq•nmol −1 at the end of synthesis (EoS). Conclusions: A 3 h cyclotron irradiation and 4.5 h radiochemical separation produced GBq-scale 165 Er suitable for producing radiopharmaceuticals at molar activities satisfactory for investigations of targeted radionuclide therapeutic effects of Auger electron emissions. This will enable future fundamental radiation biology experiments of pure Auger electron-emitting therapeutic radiopharmaceuticals, such as [ 165 Er]Er-Crown-TATE, which will be used to understand the impact of Auger electrons in TRT.

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“…This creates better imaging and avoids the concerns of photobleaching by the traditional fluorophores. 11,12 Moreover, Terbium has higher penetrance, 13,14 facilitating deeper tissue visualization, 15−17 and tracking of disease progression 18,19 in a much more efficient manner. These special luminescence qualities can also be used as real-time medication release tracking techniques, providing accurate therapeutic management.…”

Section: Introductionmentioning

confidence: 99%

“…Terbium possesses a unique light emission mechanism, which is known as up conversion luminescence. , A process involves the absorption of low-energy photons and the emission of high-energy photons. This creates better imaging and avoids the concerns of photobleaching by the traditional fluorophores. , Moreover, Terbium has higher penetrance, , facilitating deeper tissue visualization, − and tracking of disease progression , in a much more efficient manner. These special luminescence qualities can also be used as real-time medication release tracking techniques, providing accurate therapeutic management. , Due to the magnetic properties of this metal, it can be utilized in magnetic resonance imaging (MRI) as a contrast agent for visualizing scan results with higher specificity at lower energy emissions owing to disease diagnosis and real-time monitoring.…”

Section: Introductionmentioning

confidence: 99%

Potential Biomedical Applications of Terbium-Based Nanoparticles (TbNPs): A Review on Recent Advancement

Mohanto,

Biswas,

Gholap

et al. 2024

ACS Biomater. Sci. Eng.

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The scientific world is increasingly focusing on rare earth metal oxide nanomaterials due to their consequential biological prospects, navigated by breakthroughs in biomedical applications. Terbium belongs to rare earth elements (lanthanide series) and possesses remarkably strong luminescence at lower energy emission and signal transduction properties, ushering in wide applications for diagnostic measurements (i.e., bioimaging, biosensors, fluorescence imaging, etc.) in the biomedical sectors. In addition, the theranostic applications of terbium-based nanoparticles further permit the targeted delivery of drugs to the specific site of the disease. Furthermore, the antimicrobial properties of terbium nanoparticles induced via reactive oxygen species (ROS) cause oxidative damage to the cell membrane and nuclei of living organisms, ion release, and surface charge interaction, thus further creating or exhibiting excellent antioxidant characteristics. Moreover, the recent applications of terbium nanoparticles in tissue engineering, wound healing, anticancer activity, etc., due to angiogenesis, cell proliferation, promotion of growth factors, biocompatibility, cytotoxicity mitigation, and anti-inflammatory potentials, make this nanoparticle anticipate a future epoch of nanomaterials. Terbium nanoparticles stand as a game changer in the realm of biomedical research, proffering a wide array of possibilities, from revolutionary imaging techniques to advanced drug delivery systems. Their unique properties, including luminescence, magnetic characteristics, and biocompatibility, have redefined the boundaries of what can be achieved in biomedicine. This review primarily delves into various mechanisms involved in biomedical applications via terbium-based nanoparticles due to their physicochemical characteristics. This review article further explains the potential biomedical applications of terbium nanoparticles with in-depth significant mechanisms from the individual literature. This review additionally stands as the first instance to furnish a "single-platted" comprehensive acquaintance of terbium nanoparticles in shaping the future of healthcare as well as potential limitations and overcoming strategies that require exploration before being trialed in clinical settings.

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Opportunities and potential challenges of using terbium-161 for targeted radionuclide therapy in clinics

Cited by 10 publications

References 33 publications

Highlight selection of radiochemistry and radiopharmacy developments by editorial board

Highlight selection of radiochemistry and radiopharmacy developments by editorial board

High Separation Factor, High Molar Activity, and Inexpensive Purification Method for the Production of Pure ¹⁶⁵Er

Potential Biomedical Applications of Terbium-Based Nanoparticles (TbNPs): A Review on Recent Advancement

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Opportunities and potential challenges of using terbium-161 for targeted radionuclide therapy in clinics

Cited by 10 publications

References 33 publications

Highlight selection of radiochemistry and radiopharmacy developments by editorial board

Highlight selection of radiochemistry and radiopharmacy developments by editorial board

High Separation Factor, High Molar Activity, and Inexpensive Purification Method for the Production of Pure 165Er

Potential Biomedical Applications of Terbium-Based Nanoparticles (TbNPs): A Review on Recent Advancement

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Product

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High Separation Factor, High Molar Activity, and Inexpensive Purification Method for the Production of Pure ¹⁶⁵Er