Stabilized compositions and methods for radiolabeling...

Details Stabilized compositions and methods for radiolabeling... Stabilized compositions and methods for radiolabeling...

C - Chemistry, Metallurgy

07

B

C07B 59/00 (2006.01) A61K 51/02 (2006.01) C01B 7/00 (2006.01) C07K 1/13 (2006.01) C07K 16/00 (2006.01)

Patent

CA 2634666

Oxidants (e.g., N-chlorosuccinimide) can be used to stabilize .alpha.-particle emitters (e.g., 211At) in solution, prior to their subsequent reaction to form .alpha.-particle emitter labeled compounds (e.g., a radiolabeled pharmaceutical or a radiolabeled precursor used to prepare it). In particular, the use of an oxidant has been found to maintain the .alpha.- particle emitter in a chemical form that facilitates this reaction, which may involve a number of possible mechanisms including electrophilic substitution, nucleophilic substitution, complexation, exchange, or metallic bonding. Compounds labeled with .alpha.- particie emitters in this manner have wide-ranging therapeutic applications, particularly in the treatment of cancer.

Selon l'invention des oxydants (p. ex., la N-chlorosuccinimide) peuvent être utilisés pour stabiliser les émetteurs de particules .alpha. (p. ex., 211At) en solution, avant de les faire réagir afin de former des composés marqués par des émetteurs de particules .alpha. (p. ex., un produit pharmaceutique radiomarqué ou un précurseur radiomarqué utilisé pour préparer ce produit). On a notamment découvert que l'utilisation d'un oxydant conserve l'émetteur de particules .alpha. dans un forme chimique qui facilite cette réaction, ce qui peut impliquer un certain nombre de mécanismes possibles comprenant la substitution électrophile, la substitution nucléophile, la complexation, l'échange ou la liaison métallique. Ainsi, les composés marqués au moyen d'émetteurs de particules .alpha. trouvent une large gamme d'applications thérapeutiques, notamment dans le traitement du cancer.

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