Amino acid analogs for tumor imaging
Abstract
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.
- Inventors:
- Issue Date:
- Research Org.:
- Emory Univ., Atlanta, GA (United States)
- Sponsoring Org.:
- USDOE, Washington, DC (United States)
- OSTI Identifier:
- 675835
- Patent Number(s):
- 5817776
- Application Number:
- PAN: 8-744,444; TRN: 99:001158
- Assignee:
- Emory Univ., Atlanta, GA (United States)
- DOE Contract Number:
- FG05-93ER61737
- Resource Type:
- Patent
- Resource Relation:
- Other Information: PBD: 6 Oct 1998
- Country of Publication:
- United States
- Language:
- English
- Subject:
- 55 BIOLOGY AND MEDICINE, BASIC STUDIES; AMINO ACIDS; DIAGNOSIS; NEOPLASMS; RADIOPHARMACEUTICALS; IMAGE PROCESSING; UPTAKE
Citation Formats
Goodman, M M, and Shoup, T. Amino acid analogs for tumor imaging. United States: N. p., 1998.
Web.
Goodman, M M, & Shoup, T. Amino acid analogs for tumor imaging. United States.
Goodman, M M, and Shoup, T. Tue .
"Amino acid analogs for tumor imaging". United States.
@article{osti_675835,
title = {Amino acid analogs for tumor imaging},
author = {Goodman, M M and Shoup, T},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1998},
month = {10}
}