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Shelf-life of ɛ-lysyl-3-(trimethylstannyl)benzamide immunoconjugates, precursors for 211At labeling of antibodies

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  1. Sequential radioimmunotherapy with 177Lu- and 211At-labeled monoclonal antibody BR96 in a syngeneic rat colon carcinoma model

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  2. Comparison of (211)At-PRIT and (211)At-RIT of Ovarian Microtumors in a Nude Mouse Model

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  3. Evaluation of effects on the peritoneum after intraperitoneal α-radioimmunotherapy with (211)At

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  4. Intraperitoneal alpha-radioimmunotherapy in mice using different specific activities

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  5. Various functions of PBMC from colon cancer patients are not decreased compared to healthy blood donors.

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  1. Extraction of 211At from nitric acid solutions into various organic solvents for use as an α-source for radiation chemistry studies

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  2. Synthesis and Evaluation of Astatinated N-[2-(Maleimido)ethyl]-3-(trimethylstannyl)benzamide Immunoconjugates

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  3. Absorbed Doses and Risk Estimates of (211)At-MX35 F(ab')2 in Intraperitoneal Therapy of Ovarian Cancer Patients

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  4. N-[2-(maleimido)ethyl]-3-(trimethylstannyl)benzamide, a molecule for radiohalogenation of proteins and peptides

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  • Emma Aneheim
  • Jenny Halleröd
  • Per Albertsson
  • Holger Jensen
  • Stellan Holgersson
  • Sture Lindegren
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Astatine-211 is possibly the most promising radionuclide for targeted α-particle therapy when it comes to the treatment of occult disseminated cancer. Preclinical research has proven effective, and patient studies have been initiated based on these results. However, a lack of production capacity and the complex radiochemistry of (211)At are major obstacles for research and prospective clinical applications. In the present study, astatination of immunoconjugates, already prepared well in advance before radiolabeling, was performed to investigate the possibility of formulating a kit-like reagent for the production of (211)At radiopharmaceuticals. The shelf-life of ɛ-lysyl-3-(trimethylstannyl)benzamide immunoconjugates was evaluated, that is, the effect of different storage times on the quality of the immunoconjugates. The quality being referred to is the capacity to maintain a good radiochemical yield and good cell-binding property after labeling with (211)At. The stability of the conjugates was found to be pH dependent with high stability at pH≥7 and less stability at pH≤5.5. The immunoconjugates (based on trastuzumab) could be kept for more than 3 months in a phosphate buffered saline solution (pH 7.4) at 4°C before labeling, without compromising the quality of the labeled product. The conjugates are also unaffected by storage at -20°C. Conjugates with a good shelf-life compatible with distant shipping as well as improved radiochemistry are important steps to facilitate further clinical progress with (211)At.

Original languageEnglish
JournalCancer Biotherapy & Radiopharmaceuticals
Volume30
Issue number1
Pages (from-to)41-5
Number of pages5
ISSN1084-9785
DOIs
Publication statusPublished - Feb 2015

    Research areas

  • Antibodies, Monoclonal, Antibodies, Monoclonal, Humanized, Antineoplastic Agents, Astatine, Benzamides, Cell Line, Tumor, Drug Stability, Humans, Immunoconjugates, Isotope Labeling, Radiopharmaceuticals, Trastuzumab, Trimethyltin Compounds

ID: 46266306