Sökning: WFRF:(Lindegren Sture 1960)
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Pretargeted Alpha T...
Pretargeted Alpha Therapy of Disseminated Cancer Combining Click Chemistry and Astatine-211
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- Timperanza, Chiara (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kliniska vetenskaper, Avdelningen för medicinsk strålningsvetenskap,Institute of Clinical Sciences, Department of Medical Radiation Sciences
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Jensen, H. (författare)
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- Bäck, Tom, 1964 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kliniska vetenskaper, Avdelningen för medicinsk strålningsvetenskap,Institute of Clinical Sciences, Department of Medical Radiation Sciences
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- Lindegren, Sture, 1960 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kliniska vetenskaper, Avdelningen för medicinsk strålningsvetenskap,Institute of Clinical Sciences, Department of Medical Radiation Sciences
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- Aneheim, Emma, 1982 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kliniska vetenskaper, Avdelningen för medicinsk strålningsvetenskap,Institutionen för kliniska vetenskaper, Avdelningen för onkologi,Institute of Clinical Sciences, Department of Medical Radiation Sciences,Institute of Clinical Sciences, Department of Oncology
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(creator_code:org_t)
- 2023
- 2023
- Engelska.
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Ingår i: Pharmaceuticals. ; 16:4
- Relaterad länk:
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https://gup.ub.gu.se...
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https://doi.org/10.3...
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Abstract
Ämnesord
Stäng
- 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.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Radiologi och bildbehandling (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Radiology, Nuclear Medicine and Medical Imaging (hsv//eng)
Nyckelord
- astatine-211
- targeted alpha therapy
- pretargeting
- click chemistry
- radioimmunotherapy
- radionuclide therapy
- drug design
- radiopharmaceuticals
- theranostics
- particle
- radioimmunotherapy
- antibodies
- pharmacokinetics
- at-211
- Pharmacology & Pharmacy
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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