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Details for Patent: 6,017,510

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Details for Patent: 6,017,510

Title: Technetium-99M labeled peptides for imaging inflammation
Abstract:This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to technetium-99m (Tc-99m) labeled leukocyte-binding peptides, methods and kits for making such peptides, and methods for using such peptides to image sites of infection and inflammation in a mammalian body.
Inventor(s): Dean; Richard T. (Bedford, NH), Lees; Robert S. (Brookline, MA), Buttram; Scott (Derry, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jun 27, 1994
Application Number:08/266,178
Claims:1. A peptide reagent comprising:

a) a chemically synthesized chernotactic peptide selected from the group consisting of a peptide derived from platelet factor 4, a peptide derived from a bacterially-derived chemotactic peptide, a peptide derived from elastin, a peptide derived from tuftsin, a peptide derived from fibrinopeptide B and a peptide derived from fibrinogen B.beta.-chain; and

b) a technetium-99m chelating moiety covalently linked to said peptide said moiety being capable of forming a neutral complex with technetium-99m; wherein the reagent when radiolabeled with technetium-99m provides an imaging agent capable of accumulating at a site of inflammation in a mammalian body in an amount sufficient to allow detection of said site by gamma scintigraphy.

2. A peptide reagent comiprising:

a) a chemotactic peptide selected from the group consisting of a peptide derived from platelet factor 4, a peptide derived from a bacterially-derived chemotactic peptide, a peptide derived from elastin, a peptide derived from tuftsin, a peptide derived from fibrinopeptide B and a peptide derived from fibrinogen B.beta.-chain; and

b) a technetium-99m chelating moiety covalently linked to said peptide, said moiety being capable of forming a complex with technetium-99m having a net charge of -1;

wherein the reagent when radiolabeled with technetium-99m provides an imaging agent capable of accumulating at a site of inflammation in a mammalian body in an amount sufficient to allow detection of said site by gamma scintigraphy.

3. A peptide reagent comprising a chemically synthesized chemotactic peptide which binds to receptors on surfaces of leukocytes and which is covalently linked to a technetium-99m chelating moiety capable of forming a neutral complex with technetium-99m, wherein the reagent when radiolabeled with technetium-99m provides an imaging agent capable of accumulating at a site of inflammation in a mammalian body in an amount sufficient to allow detection of said site by gamma scintigraphy.

4. The reagent of claim 3 wherein the technetium-99m chelating moiety has a formula: ##STR3## wherein each R is independently H, a lower alkyl having 1 to 6 carbon atoms, a phenyl, or a phenyl substituted with a lower alkyl or a lower alkoxy, and wherein each n is independently 1 or 2.

5. The reagent of claim 4 wherein the technetium-99m chelating moiety has a formula: ##STR4##

6. A kit for preparing a radiopharmaceutical preparation, said kit comprising a sealed vial containing the reagent of claims 1, 2 or 3 and a sufficient amount of a reducing agent to label the reagent with technetium-99m.

7. A peptide reagent comprising a chemically synthesized chemotactic peptide which binds to receptors on surfaces of leukocytes and which is covalently linked to a technetium-99m chelating moiety capable of forming a complex with technetium-99m having a net charge of -1, wherein the reagent when radiolabeled with technetium-99m provides an imaging agent capable of accumulating at a site of inflammation in a mammalian body in an amount sufficient to allow detection of said site by gamma scintigraphy.

8. A kit for preparing a radiopharmaceutical preparation, said kit comprising a sealed vial containing the reagent of claims 1, 2, or 7 and a sufficient amount of a reducing agent to label the reagent with technetium-99m.
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