# US 7,608,692 B2 · Exendins and exendin agonists modified with albumin

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- Number: US 7,608,692 B2
- Document ID: US7608692B2
- Status: Granted
- Kind: B2
- Application number: 12/101,689
- Filed: 2008-04-11
- Published: 2008-09-04
- Granted: 2009-10-27
- Earliest claimed: 1999-04-30
- Assignees: Amylin Pharmaceuticals, Inc.
- Inventors: Kathryn S. Prickett; Andrew A. Young
- Web page: https://patentgrep.com/patent/US7608692B2

## CPC

- C07K 14/605: Glucagons
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Modified exendins and exendin agonists having an exendin or exendin agonist linked to one or more polyethylene glycol polymers, for example, and related formulations and dosages and methods of administration thereof are provided. These modified exendins and exendin agonists, compositions and methods are useful in treating diabetes and conditions that would be benefited by lowering plasma glucose or delaying and/or slowing gastric emptying or inhibiting food intake.

## Claims

### Claim 1

An agonist exendin-4 peptide analog linked to one albumin through the N-terminal or C-terminal amino acid of said agonist exendin-4 peptide analog.

### Claim 2 (depends on 1)

The agonist exendin-4 peptide analog linked to one albumin according to claim 1, wherein the agonist exendin-4 peptide analog is linked to the one albumin through an amino or carboxyl group of the agonist exendin-4 peptide analog.

### Claim 3 (depends on 2)

The agonist exendin-4 peptide analog linked to one albumin according to claim 2, wherein the agonist exendin-4 peptide analog is linked to the one albumin through an amino group of the agonist exendin-4 peptide analog.

### Claim 4 (depends on 3)

The agonist exendin-4 peptide analog linked to one albumin according to claim 3, wherein the agonist exendin-4 peptide analog is linked to the one albumin through the C-terminal amino acid of the agonist exendin-4 peptide analog.

### Claim 5 (depends on 4)

The agonist exendin-4 peptide analog linked to one albumin according to claim 4, wherein the agonist exendin-4 peptide analog is linked to the one albumin through the epsilon amino group of a lysine amino acid.

### Claim 6 (depends on 1)

A pharmaceutical composition comprising the agonist exendin-4 peptide analog linked to one albumin according to claim 1 and a pharmaceutically acceptable carrier.

### Claim 7

An agonist exendin-4 peptide analog linked to one albumin through the N-terminal or C-terminal amino acid of said agonist exendin-4 peptide analog, wherein the agonist exendin-4 peptide analog comprises the amino acid sequence of:
His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly(SEQ ID NO: 3).

### Claim 8 (depends on 7)

The agonist exendin-4 peptide analog linked to one albumin according to claim 7, wherein the agonist exendin-4 peptide analog 4 is linked to the one albumin through an amino or carboxyl group of the agonist exendin-4 peptide analog.

### Claim 9 (depends on 8)

The agonist exendin-4 peptide analog linked to one albumin according to claim 8, wherein the agonist exendin-4 peptide analog is linked to the one albumin through an amino group of the agonist exendin-4 peptide analog.

### Claim 10 (depends on 9)

The agonist exendin-4 peptide analog linked to the one albumin according to claim 9, wherein the agonist exendin-4 peptide analog is linked to the one albumin through the C-terminal amino acid of the agonist exendin-4 peptide analog.

### Claim 11 (depends on 10)

The agonist exendin-4 peptide analog linked to one albumin according to claim 10, wherein the agonist exendin-4 peptide analog is linked to the one albumin through the epsilon amino group of a lysine amino acid of the agonist exendin-4 peptide analog.

### Claim 12 (depends on 7)

A pharmaceutical composition comprising the agonist exendin-4 peptide analog linked to one albumin according to claim 7 and a pharmaceutically acceptable carrier.
