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Amino acid analogs for tumor imaging

Patent ·
OSTI ID:871844

The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of 1-amino-cycloalkyl-1-carboxylic acids, namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes including fluorine-18, iodine-123, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77 and bromine-82. In one aspect, the invention features amino acid compounds that have a high specificity for target sites when administered to a subject in vivo. Preferred amino acid compounds show a target to non-target ratio of at least 5:1, are stable in vivo and substantially localized to target within 1 hour after administration. An especially preferred amino acid compound is ›.sup.18 F!-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC). In another aspect, the invention features pharmaceutical compositions comprised of an .alpha.-amino acid moiety attached to either a four, five, or a six member carbon-chain ring. In addition, the invention features analogs of .alpha.-aminoisobutyric acid.

Research Organization:
Oak Ridge National Laboratory (ORNL), Oak Ridge, TN
DOE Contract Number:
FG05-93ER61737
Assignee:
Emory University (Atlanta, GA)
Patent Number(s):
US 5808146
Application Number:
08/554906
OSTI ID:
871844
Country of Publication:
United States
Language:
English

References (2)

Direct synthesis of .alpha.-halogenomethyl-.alpha.-amino acids from the parent .alpha.-amino acids journal July 1979
Radiopharmaceuticals II: Proceedings 2nd International Symposium on Radiopharmaceuticals, March 19–22, 1979, Seattle, Washington journal December 1980