GIP-based mixed agonists for treatment of metabolic disorders and obesity

• US 9,062,124 B2
• Filed: 06/16/2009
• Issued: 06/23/2015
• Est. Priority Date: 06/17/2008
• Status: Active Grant

• Current Assignee: Indiana University Research & Technology Corporation (Indiana University)
• Original Assignee: Indiana University Research & Technology Corporation (Indiana University)
• Inventors: Dimarchi, Richard D., Ma, Tao
• Primary Examiner(s): Kemmerer, Elizabeth C
• Assistant Examiner(s): Deberry, Regina M
• Application Number:
  US12/999,285
• Publication Number:
  US 20110166062A1
• Time in Patent Office: 2,198 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61K 38/26 Glucagons
• 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 1/00 Drugs for disorders of the alimentary tract or the digestive system
• 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 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/10 Antimycotics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07K 14/605 Glucagons

Abstract

Glucagon peptides that exhibit GIP agonist activity in addition to glucagon and/or GLP-I activity are provided. Pharmaceutical compositions comprising such glucagon peptides and therapeutic methods of using such peptides are also provided.

Claims

1. A peptide comprising the amino acid sequence of SEQ ID NO:

105.

2. A conjugate comprising the peptide of claim 1 linked to a conjugate moiety.

3. The conjugate of claim 2, wherein the conjugate moiety is selected from the group consisting of a targeting agent, an immunoglobulin or portion thereof, a plasma protein, a label, a radioisotope, fluorophore, enzymatic label, a polymer, and a water soluble polymer.

4. A fusion peptide comprising the peptide of claim 1 and a second peptide comprising the amino acid sequence of any of SEQ ID NOs:

95-98 fused to a terminus of the peptide of claim 1.

5. A pharmaceutical composition comprising the peptide of claim 1, and a pharmaceutically acceptable carrier.

6. A method of reducing weight gain or inducing weight loss, comprising administering to a patient in need thereof a pharmaceutical composition of claim 5 in an amount effective to reduce weight gain or induce weight loss.

7. A method of treating Type II diabetes or insulin resistance, comprising administering to a patient in need thereof a pharmaceutical composition of claim 5 in an amount effective to lower blood glucose levels.

8. A kit comprising a pharmaceutical composition of claim 5 and a device for administering said pharmaceutical composition to a patient.

9. A peptide consisting of the amino acid sequence of SEQ ID NO:

105.

10. A conjugate comprising the peptide of claim 9 linked to a conjugate moiety.

11. The conjugate of claim 10, wherein the conjugate moiety is selected from the group consisting of a targeting agent, an immunoglobulin or portion thereof, a plasma protein, a label, a radioisotope, fluorophore, enzymatic label, a polymer, and a water soluble polymer.

12. A fusion peptide comprising the peptide of claim 9 and a second peptide comprising the amino acid sequence of any of SEQ ID NOs:

95-98 fused to a terminus of the peptide of claim 9.

13. A pharmaceutical composition comprising the peptide of claim 9, and a pharmaceutically acceptable carrier.

14. A kit comprising a pharmaceutical composition of claim 13 and a device for administering said pharmaceutical composition to a patient.