One vial method for labeling protein/linker conjugates with technetium-99M
AssigneeCentocor, Inc.
InventorRichard T. Dean
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Abstract
A one vial method for labeling a protein, such as an antibody or antibody fragment, with a radiometal such as Tc-99m or a rhenium isotope, is disclosed. The method comprises contacting in a single vial a mixture comprised of a reducing agent and a protein molecule covalently bound to a sulfhydryl containing bifunctional coupling agent with Tc or Re in an oxidized state. A one vial kit for labeling a protein with Tc or Re is also disclosed.
Claims46
A one vial method for labeling a protein with a radioisotope selected from Tc-99m, Re-186, Re-188, Re-189 and Re-191, comprising (a) providing a vial containing a mixture comprising said protein having a sulfhydryl containing bisectional coupling agent bound thereto and a reducing agent;
- and (b) adding to said vial said radioisotope in an oxidized state, wherein said bisectional coupling agent is selected from compounds of the formula ##STR16## where a is an integer from 1 to 3 inclusive;
- c is an integer from 1 to 7 inclusive;
- f is an integer from 3 to 6 inclusive;
- R is selected from the group consisting of R.sub.1 CO-- and R.sub.1 S--;
- R.sub.1 is selected from the group consisting of optionally substituted lower alkyl and optionally substituted aryl;
- R.sub.3 is selected from the group consisting of hydrogen, optionally substituted lower alkyl, and optionally substituted aryl;
- and
- Z is selected from the group consisting of ClCH.sub.2 CONH--, BrCH.sub.2 CONH--, ICH.sub.2 COHN and N-substituted maleimido.
A one vial kit for labeling a protein with a radioisotope selected from Tc-99m, Re-186, Re-188, Re-189 and Re-191, comprising a vial containing a mixture comprising said protein having a sulfhydryl containing bifunctional coupling agent bound thereto and a reducing agent, wherein said bifunctional coupling agent is selected from compounds of the formula ##STR28## where a is an integer from 1 to 3 inclusive;
- c is an integer from 1 to 7 inclusive;
- f is an integer from 3 to 6 inclusive;
- R is selected from the group consisting of R.sub.1 CO-- and R.sub.1 R--;
- R.sub.1 is selected from the group consisting of optionally substituted lower alkyl and optionally substituted aryl;
- R.sub.3 is selected from the group consisting of hydrogen, optionally substituted lower alkyl, and optionally substituted aryl;
- and
- Z is selected from the group consisting of ClCH.sub.2 CONH--, BrCH.sub.2 CONH--, ICH.sub.2 CPNH and N-substituted maleimido.
Dependencies are inferred from the claim text.