Ethylenedicysteine (EC)-drug conjugates, compositions and methods for tissue specific disease imaging
AssigneeBoard of Regents, The University of Texas System
InventorsDavid J. Yang, Chun W. Liu, Dong-Fang Yu, E. Edmund Kim
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Abstract
The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.
Claims26
A method of imaging a site within a subject comprising the steps of:
- a) administering to the subject an effective amount of a composition comprising a radionuclide-labeled bis-aminoethanethiol (BAT) dicarboxylic acid-targeting ligand conjugate, wherein the targeting ligand of the conjugate is a folate receptor targeting ligand, an agent that mimics glucose, annexin V, colchicine, glutamate pentapeptide, or a tumor hypoxia targeting ligand selected from the group consisting of nitroimidazole, mitomycin, and metronidazole;
- and
- b) detecting a radioactive signal from the site by emission tomography.
A method of imaging a site within a subject comprising the steps of:
- a) administering to the subject an effective amount of a composition comprising a radionuclide-labeled bis-aminoethanethiol (BAT) dicarboxylic acid-targeting ligand conjugate, wherein the radionuclide-labeled bis-aminoethanethiol (BAT) dicarboxylic acid-targeting ligand conjugate further comprises a linker conjugating the BAT dicarboxylic acid to the targeting ligand;
- and
- b) detecting a radioactive signal from the site by emission tomography, wherein said linker is glutamate peptide or poly-glutamic acid.
A method of imaging a site within a subject comprising the steps of:
- a) administering to the subject an effective amount of a composition comprising a radionuclide-labeled bis-aminoethanethiol (BAT) dicarboxylic acid-targeting ligand conjugate, wherein the radionuclide-labeled bis-aminoethanethiol (BAT) dicarboxylic acid-targeting ligand conjugate further comprises a linker conjugating the BAT dicarboxylic acid to the targeting ligand;
- and
- b) detecting a radioactive signal from the site by emission tomography, wherein the linker comprises a water soluble peptide, glutamic acid, aspartic acid, bromo ethylacetate, ethylene diamine, or lysine, and wherein the targeting ligand is estradiol, topotecan, paclitaxel, raloxifen, etoposide, doxorubricin, mitomycin C, endostatin, annexin V, LHRH, octreotide, VIP, methotrexate, or folic acid.
Dependencies are inferred from the claim text.