| 1. |
- Albertsson, Per, 1964, et al.
(author)
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Astatine-211 based radionuclide therapy: Current clinical trial landscape
- 2023
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In: Frontiers in Medicine. - : Frontiers Media SA. - 2296-858X. ; 9
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Journal article (peer-reviewed)abstract
- Astatine-211 (At-211) has physical properties that make it one of the top candidates for use as a radiation source for alpha particle-based radionuclide therapy, also referred to as targeted alpha therapy (TAT). Here, we summarize the main results of the completed clinical trials, further describe ongoing trials, and discuss future prospects.
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| 2. |
- Aneheim, Emma, 1982, et al.
(author)
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Behaviour, use and safety aspects of astatine-211 solvated in chloroform after dry distillation recovery
- 2024
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In: SCIENTIFIC REPORTS. - 2045-2322. ; 14:1
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Journal article (peer-reviewed)abstract
- Targeted alpha therapy of disseminated cancer is an emerging technique where astatine-211 is one of the most promising candidate nuclides. Astatine-211 can be produced in medium energy cyclotrons by alpha particle bombardment of natural bismuth. The produced astatine is then commonly recovered from the irradiated solid target material through dry distillation. The dry distillation process often includes elution and solvation of condensed astatine with chloroform, forming Chloroform Eluate. In this work the handling and safe use of the high activity concentration Chloroform Eluate has been investigated. Correctly performed, evaporation of Chloroform Eluate results in a dry residue with complete recovery of the astatine. The dry residue can then serve as a versatile starting material, using appropriate oxidizing or reducing conditions, for subsequent downstream chemistry. However, it has been found that when evaporating the Chloroform Eluate, astatine can be volatilized if continuing the process beyond the point of dryness. This behavior is more pronounced when the Chloroform Eluate has received a higher absorbed dose. Upon water phase contact of the Chloroform Eluate, a major part of the astatine activity becomes water soluble, leaving the organic phase. A behavior which is also dependent on dose to the solvent.
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| 3. |
- Timperanza, Chiara, et al.
(author)
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Pretargeted Alpha Therapy of Disseminated Cancer Combining Click Chemistry and Astatine-211
- 2023
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In: Pharmaceuticals. ; 16:4
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Journal article (peer-reviewed)abstract
- To enhance targeting efficacy in the radioimmunotherapy of disseminated cancer, several pretargeting strategies have been developed. In pretargeted radioimmunotherapy, the tumor is pretargeted with a modified monoclonal antibody that has an affinity for both tumor antigens and radiolabeled carriers. In this work, we aimed to synthesize and evaluate poly-L-lysine-based effector molecules for pretargeting applications based on the tetrazine and trans-cyclooctene reaction using At-211 for targeted alpha therapy and I-125 as a surrogate for the imaging radionuclides I-123,I- 124. Poly-L-lysine in two sizes was functionalized with a prosthetic group, for the attachment of both radiohalogens, and tetrazine, to allow binding to the trans-cyclooctene-modified pretargeting agent, maintaining the structural integrity of the polymer. Radiolabeling resulted in a radiochemical yield of over 80% for astatinated poly-L-lysines and a range of 66-91% for iodinated poly-L-lysines. High specific astatine activity was achieved without affecting the stability of the radiopharmaceutical or the binding between tetrazine and transcyclooctene. Two sizes of poly-L-lysine were evaluated, which displayed similar blood clearance profiles in a pilot in vivo study. This work is a first step toward creating a pretargeting system optimized for targeted alpha therapy with At-211.
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