# US 5,346,686 A · Labelled interleukin-8 and medical uses thereof

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- Number: US 5,346,686 A
- Document ID: US5346686A
- Status: Granted
- Kind: A
- Application number: 07/956,863
- Filed: 1992-10-05
- Granted: 1994-09-13
- Earliest claimed: 1992-10-05
- Assignees: Mallinckrodt Medical, Inc.; Curators of the University of Michigan
- Inventors: Leon R. Lyle; Steven L. Kunkel
- Web page: https://patentgrep.com/patent/US5346686A

## CPC

- A61K 51/08: Peptides, e.g. proteins {, carriers being peptides, polyamino acids, proteins}
- A61K 2123/00: Preparations for testing in vivo
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A method of imaging a target site in an animal's body in which a labelled CXC chemokine is introduced into the animal's body and allowed to accumulate at a target site which includes Interleukin-8 receptor molecules. The accumulated, labelled CXC chemokine is then detected so as to image the target site of the body.

## Claims

### Claim 1

A method of imaging a target site in an animal body, comprising providing a radionuclide-labelled CXC chemokine, wherein C stands for cysteine and X stands for an amino acid, introducing a detectable amount of said labelled CXC chemokine into an animal's body, allowing the labelled CXC chemokine to accumlate at a target site of the animal's body, wherein neutrophils having Interleukin-8 receptor molecules are located at said target site, and detecting the accumulated, labelled CXC chemokine so as to image said target site.

### Claim 2 (depends on 1)

The method of claim 1 wherein said target site is an inflamed or diseased portion of said animal's body.

### Claim 3 (depends on 1)

The method of claim 1 wherein said labelled CXC chemokine is radiolabelled CXC chemokine.

### Claim 4 (depends on 3)

The method of claim 3 wherein said CXC chemokine is labelled with indium-111, iodine-123, technetium-99m or copper-62.

### Claim 5 (depends on 4)

The method of claim 4 wherein said indium-111 is carried by a lysine of said CXC chemokine.

### Claim 6 (depends on 4)

The method of claim 4 wherein said CXC chemokine is labelled with indium-111 utilizing a chelating agent.

### Claim 7 (depends on 6)

The method of claim 6 wherein said chelating agent is C-DTPA.

### Claim 8 (depends on 6)

The method of claim 6 wherein said CXC chemokine is human Interleukin-8.

### Claim 9 (depends on 4)

The method of claim 4 wherein said iodine-123 is carried by a tyrosine, iodophenyl derivative or lysine of said CXC chemokine.

### Claim 10 (depends on 4)

The method of claim 4 wherein said CXC chemokine is labelled with iodine-123 utilizing chloramine-T hydrate.

### Claim 11 (depends on 10)

The method of claim 10 wherein said CXC chemokine is human Interleukin-8.

### Claim 12 (depends on 4)

The method of claim 4 wherein said CXC chemokine is labelled with technetium-99m.

### Claim 13 (depends on 12)

The method of claim 12 wherein said technetium-99m is carried by a lysine or an added free cysteine of said CXC chemokine.

### Claim 14 (depends on 1)

The method of claim 1 wherein said CXC chemokine is labelled utilizing a chelating agent.

### Claim 15 (depends on 14)

The method of claim 14 wherein said chelating agent is a triamide thiolate ligand, a diamide dithiolate ligand or a diamide diphenolic ligand.

### Claim 16 (depends on 15)

The method of claim 15 wherein said CXC chemokine is labelled with technetium-99m or copper-62 and said chelating agent is a triamide thiolate ligand.

### Claim 17 (depends on 12)

The method of claim 12 wherein said CXC chemokine is human Interleukin-8.

### Claim 18 (depends on 1)

The method of claim 1 wherein said CXC chemokine is human Interleukin-8.

### Claim 19

A method of delivering a labeling agent to a target site of an animal's body, comprising introducing into an animal's body a CXC chemokine carrying a radionuclide labeling agent, wherein C stands for cysteine and X stands for an amino acid, and allowing the labeling agent-carrying CXC chemokine to accumulate at a target site, wherein neutrophils having Interleukin-8 receptor molecules are located at said target site, so as to deliver said labeling agent to said target site.

### Claim 20

A method of delivering a radioactive agent to a target site of an animal's body comprising introducing into an animal's body a CXC chemokine carrying a radioactive agent, wherein C stands for cysteine and X stands for an amino acid, and allowing the radioactive agent-carrying CXC chemokine to accumulate at a target site, wherein neutrophils having Interleukin-8 receptor molecules are located at said target site, so as to deliver said radioactive agent to said target site.

### Claim 21

A composition comprising a CXC chemokine carrying a radioactive labeling agent, wherein said radioactive labeling agent is selected from the group consisting of indium-111, and technetium-99m.

### Claim 22 (depends on 21)

The composition of claim 21 wherein said CXC chemokine is labelled with said radioactive labeling agent by utilizing a chelating agent which is conjugated to said CXC chemokine.

### Claim 23 (depends on 22)

The composition of claim 22 wherein said chelating agent is a triamide thiolate ligand, diamide dithiolate ligand or diamide diphenolic ligand.
