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Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same

Patent ·
OSTI ID:1281082
; ; ;
Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula ##STR00001## where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.
Research Organization:
Univ. of Southern California, Los Angeles, CA (United States)
Sponsoring Organization:
USDOE
Assignee:
University of Southern California (Los Angeles, CA)
Patent Number(s):
9,403,875
Application Number:
12/695,125
OSTI ID:
1281082
Country of Publication:
United States
Language:
English

References (4)

Radiolabeled Multimeric Cyclic RGD Peptides as Integrin α v β 3 Targeted Radiotracers for Tumor Imaging journal July 2006
MicroPET and Autoradiographic Imaging of Breast Cancer α v -Integrin Expression Using 18 F- and 64 Cu-Labeled RGD Peptide journal January 2004
Synthesis, Copper(II) Complexation, 64 Cu-Labeling, and Bioconjugation of a New Bis(2-pyridylmethyl) Derivative of 1,4,7-Triazacyclononane journal March 2008
PET (positron emission tomography) imaging of biomolecules using metal–DOTA complexes: a new collaborative challenge by chemists, biologists, and physicians for future diagnostics and exploration of in vivo dynamics journal January 2008

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Related Subjects

62 RADIOLOGY AND NUCLEAR MEDICINE