Bisaminoethanethiol-targeting ligand conjugates and compositions

Abstract

The invention provides, in a general sense, a new labeling strategy employing 99m Tc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99m Tc 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.

1 - 51 . (canceled) 
     
     
         52 . A pharmaceutically acceptable composition comprising a bis-aminoethanethiol (BAT)-targeting ligand conjugate, wherein the targeting ligand is an agent that mimics glucose. 
     
     
         53 . The composition of  claim 52 , wherein the conjugate is further defined as an ethylene dicysteine-targeting ligand conjugate. 
     
     
         54 . The composition of  claim 52 , wherein the agent that mimics glucose is glucosamine, deoxyglucose, neomycin, kanamycin, gentamicin, paromycin, amikacin, tobramycin, netilmicin, ribostamycin, sisomicin, micromicin, lividomycin, dibekacin, isepamicin, astromicin, or an aminoglycoside. 
     
     
         55 . The composition of  claim 54 , wherein the agent that mimics glucose is glucosamine. 
     
     
         56 . The composition of  claim 55 , wherein the conjugate is further defined as EC-glucosamine. 
     
     
         57 . The composition of  claim 54 , wherein the agent that mimics glucose is deoxyglucose. 
     
     
         58 . The composition of  claim 57 , wherein the conjugate is further defined as EC-deoxyglucose. 
     
     
         59 . The composition of  claim 52 , wherein the conjugate further comprises a linker between said BAT and said targeting ligand. 
     
     
         60 . The composition of  claim 59 , wherein the linker is a water soluble peptide, glutamic acid, polyglutamic acid, aspartic acid, polyaspartic acid, bromoethylacetate, ethylenediamine or lysine. 
     
     
         61 . The composition of  claim 52 , wherein the bis-aminoethanethiol (BAT)-targeting ligand conjugate is labeled with a metal ion. 
     
     
         62 . The composition of  claim 61 , wherein the metal ion is a radionuclide. 
     
     
         63 . The composition of  claim 62 , wherein the radionuclide is  99m Tc,  188 Re,  186 Re,  183 Sm,  166 Ho,  90 Y,  89 Sr,  67 Ga,  68 Ga,  111 In,  153 Gd,  59 Fe,  225 Ac,  212 Bi,  211 At,  62 Cu, or  64 Cu. 
     
     
         64 . The composition of  claim 52 , wherein the BAT comprises two carboxylic acid moieties. 
     
     
         65 . The composition of  claim 64 , wherein a targeting ligand is conjugated to one of the carboxylic acid moieties of the BAT. 
     
     
         66 . The conjugate of  claim 64 , wherein a first targeting ligand is conjugated to one of the carboxylic acid moieties of the BAT and a second targeting ligand is conjugated to another carboxylic acid moiety of the BAT.