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Details for Patent: 5,783,170

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Details for Patent: 5,783,170

Title: Peptide-metal chelate conjugates
Abstract:This invention relates to diagnostic and radiodiagnostic agents, including radiolabeled scintigraphic imaging agents, and therapeutic and radiotherapeutic agents. The invention provides such agents and reagents for preparing such agents, and methods for producing and using such reagents. Specifically, the invention provides radiolabeled imaging agents and non-radioactively labeled imaging agents for imaging sites in a mammalian body and reagents for preparing these imaging agents. The invention also provides radiolabeled therapeutic agents, as well as non-radioactively labeled therapeutic agents, and reagents and methods for preparing these agents. The agents and reagents provided comprise a specific binding peptide, covalently linked to a metal ion-complexing moiety. Reagents, methods and kits for making such reagents, methods for labeling such reagents, and methods for using such labeled reagents are provided.
Inventor(s): Dean; Richard T. (Bedford, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:May 12, 1994
Application Number:08/241,625
Claims:1. A composition of matter comprising a specific binding peptide covalently linked to a metal ion-complexing moiety, wherein the peptide specifically binds to somatostatin receptors, and having formula:

wherein X is a metal ion complexing moiety having formula

wherein B is a thiol-containing moiety that is cysteine, homocysteine, isocysteine, or penicillamine;

(amino acid).sub.n and (amino acid).sub.m are each independently any primary .alpha.-or .beta.-amino acid that does not comprise a thiol group;

Z is --OH or --NH .sub.2 ;

n is an integer between 2 and 5; and

m is an integer between 0 and 5.

2. A composition of matter according to claim 1 having the formula:

3. A composition of matter according to claim 1 selected from the group consisting of:

cyclo(N-methyl)FYW.sub.D KV.Hcy.(CH.sub.2 CO.GGCR.amide)

cyclo(N-methyl)FYW.sub.D KV.Hcy.(CH.sub.2 CO.GGCRD.amide)

cyclo(N-methyl)FYW.sub.D KV.Hcy.(CH.sub.2 CO.GGCRK. amide)

cyclo(N-methyl)FYW.sub.D KV.Hcy.(CH.sub.2 CO.GGCRR.amide)

cyclo(N-methyl)FYW.sub.D KV.Hcy.(CH.sub.2 Co.GGCKK.amide) and

cyclo(N-methyl)FYW.sub.D KV.Hcy.(CH.sub.2 CO.KKC.amide).

4. A reagent for preparing a scintigraphic imaging agent for imaging a site within a mammalian body, comprising the composition of matter of claim 1.

5. A scintigraphic imaging agent comprising the reagent according to claim 4 wherein the radiolabel binding moiety is bound to technetium-99m.

6. A kit for preparing a radiopharmaceutical preparation, said kit comprising a sealed vial containing a predetermined quantity of the reagent of claim 4 and a sufficient amount of reducing agent to label the reagent with technetium -99m.

7. The composition of matter of claim 1 wherein the metal ion-complexing moiety is bound to a metal ion.

8. The composition of matter of claim 7 wherein the metal is rhenium, zinc or tin.

9. The composition of matter of claim 1 wherein the metal ion-complexing moiety is bound to a beta-particle emitting metal ion.

10. The composition of matter of claim 9 wherein the beta-particle emitting metal is rhenium-186 or rhenium-188.

11. The composition of matter of claim 1 wherein the metal ion-complexing moiety is bound to a conversion electron emitting metal ion.

12. The composition of matter of claim 11 wherein the conversion electron emitting metal is tin-117m.

13. A composition of matter according to claim 1 that is radioactively labeled with iodine- 125, iodine-131 or astatine-211.

14. A reagent for preparing a diagnostic agent for localizing a site within a mammalian body, comprising the composition of matter of claim 1.

15. A diagnostic agent comprising the reagent according to claim 14 wherein the metal ion complexing moiety is bound to a paramagnetic metal ion.

16. The diagnostic agent of claim 15 wherein the paramagnetic metal is iron or copper.

17. A diagnostic agent comprising the reagent according to claim 14 bound to a superparamagnetic particle.

18. A diagnostic imaging agent comprising the composition of claim 1 radiolabeled with iodine 123, iodine-125 or iodine-131.

19. A composition of matter having formula: ##STR4##

20. A composition of matter according to claim 19 that is radiolabeled with technetium-99m.

21. The reagent of claim 4 wherein the imaged site within a mammalian body is a site of a primary or metastatic, somatostatin receptor-expressing tumor.

22. An article of manufacture comprising a sealed vial containing a predetermined quantity of the composition of matter of claim 19 and a sufficient amount of reducing agent to label the composition with technetium-99m.

23. A kit for preparing a radiopharmaceutical preparation, said kit comprising a sealed vial containing a predetermined quantity of the reagent of claim 19 and a sufficient amount of reducing agent to label the reagent with technetium-99m.
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