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Title: 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:
;
Publication Date:
Research Org.:
Emory University
Sponsoring Org.:
USDOE, Washington, DC (United States)
OSTI Identifier:
672678
Patent Number(s):
US 5,808,146/A/
Application Number:
PAN: 8-554,906; TRN: 99:001108
Assignee:
Emory Univ., Atlanta, GA (United States) PTO; SCA: 550601; PA: EDB-98:121761; SN: 98002026834
DOE Contract Number:  
FG05-93ER61737
Resource Type:
Patent
Resource Relation:
Other Information: PBD: 15 Sep 1998
Country of Publication:
United States
Language:
English
Subject:
55 BIOLOGY AND MEDICINE, BASIC STUDIES; IMAGE PROCESSING; DIAGNOSTIC USES; AMINO ACIDS; NEOPLASMS; RADIOPHARMACEUTICALS; UPTAKE; SPECIFICITY

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_672678,
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 = {Tue Sep 15 00:00:00 EDT 1998},
month = {Tue Sep 15 00:00:00 EDT 1998}
}