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    Astatine-211 labeling: a study towards automatic production of astatinated antibodies

    Aneheim, Emma, Jensen, Holger, Albertsson, Per, Lindegren, Sture
    Journal of Radioanalytical and Nuclear Chemistry, 2015, Vol.303(1), pp.979-983 [Revue évaluée par les pairs]

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

    Cederkrantz, Elin, Andersson, Håkan, Bernhardt, Peter, Bäck, Tom, Hultborn, Ragnar, Jacobsson, Lars, Jensen, Holger, Lindegren, Sture, Ljungberg, Michael, Magnander, Tobias, Palm, Stig, Albertsson, Per
    International journal of radiation oncology, biology, physics, 01 November 2015, Vol.93(3), pp.569-576 [Revue évaluée par les pairs]

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

    Aneheim, Emma, Gustafsson, Anna, Albertsson, Per, Bäck, Tom, Jensen, Holger, Palm, Stig, Svedhem, Sofia, Lindegren, Sture
    Bioconjugate chemistry, 16 March 2016, Vol.27(3), pp.688-697 [Revue évaluée par les pairs]

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    Direct procedure for the production of 211At-labeled antibodies with an epsilon-lysyl-3-(trimethylstannyl)benzamide immunoconjugate

    Lindegren, Sture, Frost, Sofia, Bäck, Tom, Haglund, Elin, Elgqvist, Jörgen, Jensen, Holger
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine, September 2008, Vol.49(9), pp.1537-45 [Revue évaluée par les pairs]
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    Titre: Direct procedure for the production of 211At-labeled antibodies with an epsilon-lysyl-3-(trimethylstannyl)benzamide immunoconjugate
    Auteur: Lindegren, Sture; Frost, Sofia; Bäck, Tom; Haglund, Elin; Elgqvist, Jörgen; Jensen, Holger
    Sujet: Antibodies, Monoclonal -- Chemistry ; Astatine -- Chemistry ; Benzamides -- Chemistry
    Description: (211)At-labeled tumor-specific antibodies have long been considered for the treatment of disseminated cancer. However, the limited availability of the nuclide and the poor efficacy of labeling procedures at clinical activity levels present major obstacles to their use. This study evaluated a procedure for the direct astatination of antibodies for the production of clinical activity levels. The monoclonal antibody trastuzumab was conjugated with the reagent N-succinimidyl-3-(trimethylstannyl)benzoate, and the immunoconjugate was labeled with astatine. Before astatination of the conjugated antibody, the nuclide was activated with N-iodosuccinimide. The labeling reaction was evaluated in terms of reaction time, volume of reaction solvent, immunoconjugate concentration, and applied activity. The quality of the astatinated antibodies was determined by in vitro analysis and biodistribution studies in nude mice. The reaction proceeded almost instantaneously, and the results indicated a low dependence on immunoconjugate concentration and applied activity. Radiochemical labeling yields were in the range of 68%-81%, and a specific radioactivity of up to 1 GBq/mg could be achieved. Stability and radiochemical purity were equal to or better than those attained with a conventional 2-step procedure. Dissociation constants for directly astatinated, conventionally astatinated, and radioiodinated trastuzumab were 1.0+/-0.06 (mean+/-SD), 0.44+/-0.06, and 0.29+/-0.02 nM, respectively. The tissue distribution in non-tumor-bearing nude mice revealed only minor differences in organ uptake relative to that obtained with the conventional method. The direct astatination procedure enables the high-yield production of astatinated antibodies with radioactivity in the amounts required for clinical applications.
    Fait partie de: Journal of nuclear medicine : official publication, Society of Nuclear Medicine, September 2008, Vol.49(9), pp.1537-45
    Identifiant: 0161-5505 (ISSN); 18703591 Version (PMID); 10.2967/jnumed.107.049833 (DOI)

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    Labeling of Anti-HER2 Nanobodies with Astatine-211: Optimization and the Effect of Different Coupling Reagents on Their in Vivo Behavior

    Dekempeneer, Yana, Bäck, Tom, Aneheim, Emma, Jensen, Holger, Puttemans, Janik, Xavier, Catarina, Keyaerts, Marleen, Palm, Stig, Albertsson, Per, Lahoutte, Tony, Caveliers, Vicky, Lindegren, Sture, D’huyvetter, Matthias
    Molecular pharmaceutics, 05 August 2019, Vol.16(8), pp.3524-3533 [Revue évaluée par les pairs]