title: Feasibility of the radioastatination of a monoclonal antibody with astatine-211 purified by wet extraction.
abstract: Astatine-211, a most promising α-particle emitter for targeted radiotherapy, is generally obtained by high-temperature distillation. However, a liquid-liquid extraction procedure (wet extraction) has also been described. The purpose of this study was to develop and optimize the labelling of the stannylated-activated ester N-hydroxysuccinimidyl-meta-trimethylstannylbenzoate ester (MeSTB) with astatine-211 extracted in di-isopropylether (DIPE) in the presence of the oxidant N-chlorosuccinimide (NCS). The effect of final volume, incubation duration and NCS amounts on radiolabelling yield was studied. The best yields (85-90%) of N-hydroxysuccinimidyl-meta-[(211)At]astatobenzoate ester (SAB) were obtained with 20 nmol of MeSTB, 100 nmol of NCS in 120 µL of DIPE after 15 min. The astatine-211-labelled-activated ester was then used to radiolabel a monoclonal antibody (mAb). The labelling yield was 20-25% and the radiochemical purity was 97-99%. These results show that mAbs may be efficiently labelled with astatine-211 obtained by wet extraction, a fully automatable technique that may prove to be a useful alternative to dry distillation for high activity labelling of radiopharmaceuticals. Copyright © 2008 John Wiley & Sons, Ltd.
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France. Mickael.Bourgeois@univ-nantes.fr, mickael.bourgeois@nantes.inserm.fr.|Department of Nuclear Medicine, CHU de Nantes-Hôtel Dieu, Nantes, France. Mickael.Bourgeois@univ-nantes.fr, mickael.bourgeois@nantes.inserm.fr.
authors.forename: Mickaël
authors.initials: M
authors.lastname: Bourgeois
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: François
authors.initials: F
authors.lastname: Guerard
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: Cyrille
authors.initials: C
authors.lastname: Alliot
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: Marie
authors.initials: M
authors.lastname: Mougin-Degraef
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: Holisoa
authors.initials: H
authors.lastname: Rajérison
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: Patricia
authors.initials: P
authors.lastname: Remaud-Le Saëc
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Gestin
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: François
authors.initials: F
authors.lastname: Davodeau
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: Michel
authors.initials: M
authors.lastname: Chérel
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.
authors.forename: Jacques
authors.initials: J
authors.lastname: Barbet
authors.affiliation: Centre de Recherche en Cancérologie de Nantes-Angers, Inserm, Institut de Biologie, Université de Nantes, U892, 9 quai Moncousu, 44093 Nantes Cedex 1, France.|Department of Nuclear Medicine, CHU de Nantes-Hôtel Dieu, Nantes, France.
authors.forename: Alain
authors.initials: A
authors.lastname: Faivre-Chauvet
keywords: SAB; astatine‐211; monoclonal antibody; radioimmunotherapy; α‐particle