Stabilized Compositions and Methods for Radiolabeling Pharmaceuticals with Alpha-Particle Emitters
申请人:Zalutsky Michael Rod
公开号:US20090304585A1
公开(公告)日:2009-12-10
Oxidants (e.g., N-chlorosuccinimide) can be used to stabilize α-particle emitters (e.g.,
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At) in solution, prior to their subsequent reaction to form α-particle emitter labeled compounds (e.g., a radiolabeled pharmaceutical or a radiolabeled pre-cursor used to prepare it). In particular, the use of an oxidant has been found to maintain the α-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 α-particle emitters in this manner have wide-ranging therapeutic applications, particularly in the treatment of cancer.