Modified exendins and exendin agonists

• US 8,445,647 B2
• Filed: 11/14/2011
• Issued: 05/21/2013
• Est. Priority Date: 04/30/1999
• Status: Expired due to Fees

• Current Assignee: Astrazeneca Pharmaceuticals LP (Astrazeneca PLC)
• Original Assignee: Astrazeneca Pharmaceuticals LP (Astrazeneca PLC), Amylin Pharmaceuticals Incorporated (Bristol-Myers Squibb Company)
• Inventors: Prickett, Kathryn S., Young, Andrew A.
• Primary Examiner(s): Rao, Manjunath
• Assistant Examiner(s): LIU, SAMUEL W
• Application Number:
  US13/296,120
• Publication Number:
  US 20120135922A1
• Time in Patent Office: 554 Days
• Field of Search: None
• US Class Current: 530/387.3
• CPC Class Codes: A61K 47/60 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/08 for glucose homeostasis pancreatic hormones A61P5/48
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: C07K 14/605 Glucagons

Abstract

Novel 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

1. A compound comprising exendin-4, or agonist analog of exendin-4, linked to a polyamino acid through the C-terminal amino acid of the exendin-4 or agonist analog of exendin-4 and wherein the polyamino acid is selected from the group consisting of poly(L-lysine), poly-glutamic acid, and poly-aspartic acid.

2. The compound according to claim 1, wherein the polyamino acid is poly(L-lysine).

3. The compound according to claim 1, wherein the compound comprises the exendin-4 linked to the polyamino acid.

4. The compound according to claim 3, wherein the polyamino acid is poly(L-lysine).

5. The compound according to claim 1, wherein the compound comprises the agonist analog of exendin-4 linked to a polyamino acid through the C-terminal amino acid of the agonist analog of exendin-4 and wherein the polyamino acid is selected from the group consisting of poly(L-lysine), poly-glutamic acid, and poly-aspartic acid.

6. The compound according to claim 5, wherein the polyamino acid is poly(L-lysine).