Chemistry and radiochemistry of As, Re and Rh isotopes relevant to radiopharmaceutical applications: high specific activity radionuclides for imaging and treatment

Feng, Yutian; Phelps, Tim; Carroll, Valerie; Gallazzi, Fabio; Sieckman, Gary L.; Hoffman, Timothy J.; Barnes, Charles L.; Ketring, Alan R.; Hennkens, Heather M.; Jurisson, Silvia S.

doi:10.1039/c7dt02407j

Cited by 18 publications

(17 citation statements)

References 78 publications

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“…Arsenic is an earth-abundant element and is present in oxidized forms. Arsenic(V) oxide is a commercially available and inexpensive reagent, whose derivatives such as arsonic acid and the material itself are often used as a precursor for synthesizing arsenic-based compounds. − The heavy-atom effect of arsenic can improve the efficiency of the ISC process. Further, organoarsenic compounds have high stability under oxidative condition, which suggests that they are tolerant in the presence of 1 O 2 .…”

Section: Introductionmentioning

confidence: 99%

Highly Efficient Singlet Oxygen Generation and High Oxidation Resistance Enhanced by Arsole-Polymer-Based Photosensitizer: Application as a Recyclable Photooxidation Catalyst

et al. 2020

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Photosensitizers have attracted considerable attention in various fields such as organic synthesis and medical care. For the development of high-performance photosensitizers, highly efficient and persistent singlet oxygen generators ( 1 O 2 ) having a high oxidation tolerance are strongly required. This study presents a detailed investigation of dithieno[3,2-b:2′,3′d]arsole-fluorene copolymer for its 1 O 2 generation ability and application as a photooxidation catalyst in vital organic reactions. Photoirradiation of an air-saturated solution of the polymer generates 1 O 2 , which was detected by 1 O 2 scavengers such as dihydronaphthoquinone and diphenylisobenzofuran. The polymer photosensitizer was completely stable in the presence of the strong oxidant 1 O 2 . The photosensitizer showed the highest quantum yield of 1 O 2 generation (Φ = 0.54) in single-component main-chain type π-conjugated polymers. The quantum yield of the arsenicfree analogue of the polymerbithiophene-fluorene copolymerwas significantly lower (Φ = 0.14), suggesting that the heavy-atom effect of arsenic can improve the efficiency of intersystem crossing (ISC) from the singlet excited state to the triplet excited state of the photosensitizer. In addition, when utilized as a recyclable photocatalyst for the oxidation reaction, the photosensitizer exhibited excellent oxidation resistance without losing its recognizable catalytic activity. Finally, we demonstrated the release of 1 O 2 into the air by a film of the present polymer. Persistent 1 O 2 generation was observed on film irradiation without polymer decomposition. These results suggested that the polymer exhibited excellent oxidation resistance in solution as well as in the solid state. The present molecular design concept of the photosensitizer using the main group element can facilitate the development of further functional optical materials.

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Section: Introductionmentioning

confidence: 99%

Highly Efficient Singlet Oxygen Generation and High Oxidation Resistance Enhanced by Arsole-Polymer-Based Photosensitizer: Application as a Recyclable Photooxidation Catalyst

et al. 2020

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“…2) show that the h8C3 melanin-binding antibody begins to accumulate in a murine melanoma tumor 24 h postinjection and remains present up to 9 d after initial treatment. As there is a selection of effective therapeutic radionuclides to choose from, [14][15][16] evaluation of this timeline allowed for the selection of one of the promising therapeutic radionuclides, 188 Re which was also utilized in clinical trial of 6D2 murine antibody.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of N-Succinimidyl S-Acetylthioacetate Ligand for Radiolabeling of Humanized Antibodies with¹⁸⁸Rhenium

Kjh

Jiao

et al. 2018

Cancer Biotherapy and Radiopharmaceuticals

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Radioimmunotherapy offers an effective way to direct ionizing radiation to cancer cells through attachment of radionuclides to antibodies while limiting negative effects of off-target irradiation. This, however, requires effective facile methods for attachment of therapeutic radionuclides onto antibodies. Herein, the authors report their efforts in evaluating N-succinimidyl S-acetylthioacetate (SATA), a commercially available reagent, for use as a bifunctional chelating agent (BCA) to attach Rhenium (Re) onto h8C3, a humanized IgG antibody that can effectively target extracellular melanin present in malignant melanoma. Micro single photon emission computer tomography/computer tomography was used to determine an effective timeline for antibody uptake in B16-F10 tumor bearing C57BL6 mice guiding the selection of Re with its 16.9 h physical half-life. Radio instant thin layer chromatography coupled with radio high-performance liquid chromatography was used to assess radioisotope incorporation, as well as stability during the labeling process for SATA conjugated h8C3. It was determined that despite the relatively mild conditions used, incorporation of the SATA conjugate resulted in antibody instability during labeling requiring a different BCA to facilitate rhenium incorporation onto the antibodies.

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“…The main difference between them is the energy of the β À particle, which is much higher in the case of 188 Re, resulting in higher tissue penetration, along with its higher abundance of the γ ray, making this radioisotope more attractive for imaging and therapy of larger-sized tumors. [164] Furthermore, the shorter half-life of 188 Re limits its use to agents with fast uptakes. Technetium was the first synthetic element ever reported.…”

Section: Generalmentioning

confidence: 99%

Recent Advances in Radiometals for Combined Imaging and Therapy in Cancer

et al. 2021

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Nuclear medicine is defined as the use of radionuclides for diagnostic and therapeutic applications. The imaging modalities positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are based on γ-emissions of specific energies. The therapeutic technologies are based on β À -particle-, α-particle-, and Auger electron emitters. In oncology, PET and SPECT are used to detect cancer lesions, to determine dosimetry, and to monitor therapy effectiveness. In contrast, radiotherapy is designed to irreparably damage tumor cells in order to eradicate or control the disease's progression. Radiometals are being explored for the development of diagnostic and therapeutic radiopharmaceuticals. Strategies that combine both modalities (diagnostic and therapeutic), referred to as theranostics, are promising candidates for clinical applications. This review provides an overview of the basic concepts behind therapeutic and diagnostic radiopharmaceuticals and their significance in contemporary oncology. Select radiometals that significantly impact current and upcoming cancer treatment strategies are grouped as clinically suitable theranostics pairs. The most important physical and chemical properties are discussed. Standard production methods and current radionuclide availability are provided to indicate whether a cost-efficient use in a clinical routine is feasible. Recent preclinical and clinical developments and outline perspectives for the radiometals are highlighted in each section.

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Chemistry and radiochemistry of As, Re and Rh isotopes relevant to radiopharmaceutical applications: high specific activity radionuclides for imaging and treatment

Cited by 18 publications

References 78 publications

Highly Efficient Singlet Oxygen Generation and High Oxidation Resistance Enhanced by Arsole-Polymer-Based Photosensitizer: Application as a Recyclable Photooxidation Catalyst

Highly Efficient Singlet Oxygen Generation and High Oxidation Resistance Enhanced by Arsole-Polymer-Based Photosensitizer: Application as a Recyclable Photooxidation Catalyst

Evaluation of N-Succinimidyl S-Acetylthioacetate Ligand for Radiolabeling of Humanized Antibodies with¹⁸⁸Rhenium

Recent Advances in Radiometals for Combined Imaging and Therapy in Cancer

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Chemistry and radiochemistry of As, Re and Rh isotopes relevant to radiopharmaceutical applications: high specific activity radionuclides for imaging and treatment

Cited by 18 publications

References 78 publications

Highly Efficient Singlet Oxygen Generation and High Oxidation Resistance Enhanced by Arsole-Polymer-Based Photosensitizer: Application as a Recyclable Photooxidation Catalyst

Highly Efficient Singlet Oxygen Generation and High Oxidation Resistance Enhanced by Arsole-Polymer-Based Photosensitizer: Application as a Recyclable Photooxidation Catalyst

Evaluation of N-Succinimidyl S-Acetylthioacetate Ligand for Radiolabeling of Humanized Antibodies with188Rhenium

Recent Advances in Radiometals for Combined Imaging and Therapy in Cancer

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Evaluation of N-Succinimidyl S-Acetylthioacetate Ligand for Radiolabeling of Humanized Antibodies with¹⁸⁸Rhenium