These bifunctional chelators are useful for radiolabeling targeting moieties with SPECT and PET radioisotopes for molecular imaging for diagnosis and/or treatment of cancer.

Available for licensing and commercial development are bifunctional metal chelators, metal chelator-targeting moiety complexes, metal chelator-targeting moiety-metal conjugates, kits, and methods of preparing them in a non-aqueous, automated peptide synthesizer system.  These bifunctional chelators are useful for radiolabeling targeting moieties with SPECT and PET radioisotopes for molecular imaging for diagnosis and/or treatment of cancer.  The metal chelators may be used in conventional synthetic methods to form targeting moieties [e.g., peptides, proteins, and Starburst polyamidoamine dendrimers (PAMAM)], capable of conjugating diagnostic and/or therapeutic metals.  The formulae for two such chelators may be viewed at http://www.ott.nih.gov/db/abstxt.asp?refno=999.

 

Publications:

1.     T Clifford et al. Validation of a novel CHX-A'' derivative suitable for peptide conjugation: small animal PET/CT imaging using yttrium-86-CHX-A''-octreotide. J Med Chem. 2006 Jul 13;49(14):4297-4304.  [PubMed abs]

2.     HS Chong et al. Synthesis and evaluation of novel macrocyclic and acyclic ligands as contrast enhancement agents for magnetic resonance imaging. J Med Chem. 2006 Mar 23;49(6):2055-2062.  [PubMed abs]

 

·     U.S. Provisional Application No. 60/603,781 filed 23 Aug 2004 (HHS Reference No. E-317-2004/1-US-01)

·     International Patent Application PCT/US2005/028125 filed 09 Aug 2005 (HHS Reference No. E-317-2004/1-PCT-02)

Inventors:  Martin W. Brechbiel and Thomas Clifford (NCI)

 

Licensees Sought:

Available for exclusive or non-exclusive licensing or collaborative research opportunity.