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Details for Patent: 5,780,007

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Details for Patent: 5,780,007

Title: Technetium-99m labeled peptides for imaging
Abstract:This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via a radiolabel-binding moiety which forms a neutral complex with Tc-99m.
Inventor(s): Dean; Richard T. (Bedford, NH), Buttram; Scott (Derry, NH), McBride; William (Manchester, NH), Lister-James; John (Bedford, NH), Civitello; Edgar R. (Londonderry, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jun 06, 1995
Application Number:08/470,152
Claims:1. A composition comprising a specific binding peptide and a radiolabel-binding moiety covalently linked thereto, wherein the moiety forms a complex with technetium-99m, and wherein the complex is electrically neutral, thereby avoiding interference of the complex with specific binding of the peptide to a target in vivo.

2. The composition of claim 1 wherein the peptide and the radiolabel-binding moiety are covalently linked through one or more amino acids.

3. The composition of claim 1 wherein the peptide is selected from the group consisting of:

formyl-MLF,

(VGVAPG).sub.3 amide,

(VPGVG).sub.4 amide,

RALVDTLKFVTQAEGAKamide,

RALVDTEFKVKQEAGAKamide,

PLARITLPDFRLPEIAIPamide,

GQQHHLGGAKAGDV,

PLYKKIIKKLLES,

LRALVDTLKamide,

GGGLRALVDTLKamide,

GGGLRALVDTLKFVTQAEGAKamide,

GGGRALVDTLKALVDTLamide,

GHRPLDKKREEAPSLRPAPPPISGGGYR,

PSPSPIHPAHHKRDRRQamide,

GGGF.sub.D.Dpa.YW.sub.D KTFTamide, ##STR8## (SYNRGDSTC(S-maleimido)CH.sub.2 CH.sub.2 -).sub.3 N, GGGLRALVDTLKamide,

GCGGGLRALVDTLKamide,

GCYRALVDTLKFVTQAEGAKamide

and

GC(VGVAPG).sub.3 amide.

4. The composition of claim 1, wherein the complex is formed with technetium-99m in the presence of a reducing agent.

5. The composition of claim 4, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion and a ferrous ion.

6. A composition comprising a specific binding peptide covalently linked to a radiolabel-binding moiety selected from the group consisting of: ##STR9## wherein X=H or a protecting group;

(amino acid)=any amino acid;

and a bisamino bisthiol radiolabel-binding moiety having a formula selected from the group consisting of: ##STR10## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 ;

each (pgp).sup.S is independently a thiol protecting group or H;

m, n and p are independently 2 or 3;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof;

and ##STR11## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 ;

m, n and p are independently 2 or 3;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof;

V=H or --CO-peptide;

R'=H or peptide;

and wherein when V=H, R'=peptide and when R'=H, V=--CO-peptide; wherein the radiolabel-binding moiety forms a complex with technetium-99m and the complex is electrically neutral, thereby avoiding interference of the complex with specific binding of the peptide to a target in vivo.

7. The composition of claim 6 wherein the complex is formed by ligand exchange of a prereduced technetium-99m complex.

8. The composition of claim 6 wherein the peptide and the radiolabel-binding moiety are covalently linked through one or more amino acids.

9. The composition of claim 6 wherein the peptide is selected from the group consisting of:

formyl-MLF,

(VGVAPG).sub.3 amide,

(VPGVG).sub.4 amide,

RALVDTLKFVTQAEGAKamide,

RALVDTEFKVKQEAGAKamide,

PLARITLPDFRLPEIAIPamide,

GQQHHLGGAKAGDV,

PLYKKIIKKLLES,

LRALVDTLKamide,

GGGLRALVDTLKamide,

GGGLRALVDTLKFVTQAEGAKamide,

GGGRALVDTLKALVDTLamide,

GHRPLDKKREEAPSLRPAPPPISGGGYR,

PSPSPIHPAHHKRDRRQamide,

GGGF.sub.D.Cpa.YW.sub.D KTFTamide, ##STR12## (SYNRGDSTC(S-maleimido)CH.sub.2 CH.sub.2 --).sub.3 N, GGGLRALVDTLKamide,

GCGGGLRALVDTLKamide,

GCYRALVDTLKFVTQAEGAKamide

and

GC(VGVAPG).sub.3 amide.

10. The composition of claim 6 wherein the amino acid is glycine and wherein X is an acetamidomethyl protecting group in the radiolabel-binding moieties having formula: ##STR13##

11. The composition of claim 6, wherein the complex is formed with technetium-99m in the presence of a reducing agent.

12. The composition of claim 11, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion and a ferrous ion.
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