Kit for radiolabelling with 68ga comprising a metal inhibitor

Abstract

The present invention relates to a kit for radiolabelling a targeting agent with gallium-68. The present invention also relates to the use of said kit for radiolabelling a targeting agent, a method for radiolabelling a targeting agent with gallium-68 using said kit, said kit and a method of preparation.

1 - 29 . (canceled) 
     
     
         30 . A radiolabelling kit comprising:
 an acetate salt or buffer in an amount sufficient to balance at least the acidic pH eluate from a gallium-68 generator to a pH value ranging from 3 to 5 when said generator is eluted in the kit; and   an HBED-functionalized targeting agent, said HBED-functionalized targeting agent being able to chelate gallium-68 in radiolabelling conditions, wherein said acetate salt and HBED-functionalized targeting agent are co-lyophilized.   
     
     
         31 . The kit according to  claim 30 , wherein additionally a metal inhibitor is present selected from the group consisting of DOTA and its derivatives, DTPA and its derivatives, and sugars, wherein said metal inhibitor and said HBED-functionalized targeting agent are not chemically linked. 
     
     
         32 . The kit according to  claim 31 , wherein said metal inhibitor is selected from the group consisting of monosaccharides and disaccharides. 
     
     
         33 . The kit according to  claim 31 , wherein said metal inhibitor is co-lyophilized with the acetate buffer and HBED-functionalized targeting agent. 
     
     
         34 . The kit according to  claim 30 , wherein said HBED-functionalized targeting agent is PSMA-11. 
     
     
         35 . A method for radiolabelling an HBED-functionalized targeting agent with gallium-68, comprising the elution of a gallium-68 generator with an eluent comprising an acid, in a kit according to  claim 30  and allowing the HBED-functionalized targeting agent to be labelled with gallium-68. 
     
     
         36 . The method according to  claim 35 , wherein the acid is HCl. 
     
     
         37 . The method according to  claim 35 , wherein the radiolabelling is performed at a pH between 3 and 5. 
     
     
         38 . The method according to  claim 35 , wherein the radiolabeling reaction is carried out at ambient or room temperature. 
     
     
         39 . An in vivo method of imaging in a subject comprising the steps of:
 1) producing a gallium-68 radiolabeled HBED-functionalized targeting agent using the method according to  claim 35 ;   2) administering said gallium-68 radiolabeled HBED-functionalized targeting agent to the subject; and   3) detecting the said gallium-68 radiolabeled HBED-functionalized targeting agent in the subject using positron emission tomography (PET).   
     
     
         40 . The method according to  claim 39 , wherein said HBED-functionalized targeting agent is PSMA-11. 
     
     
         41 . The method according to  claim 35 , wherein the radiolabelling is performed at a pH between 3.5 and 4.5. 
     
     
         42 . The method according to  claim 35 , wherein the radiolabelling is performed at a pH between 3.9 and 4.3. 
     
     
         43 . The method according to  claim 35 , wherein the radiolabeling reaction is carried out at a temperature between 20 and 30° C.