Lipidated incretin receptor ligand human immunoglobulin Fc-region fusion polypeptides

Patent metadata

Field	Value
Publication number	US-10137170-B2
Application number	US-201415102340-A
Country	US
Kind code	B2
Filing date	Dec 19, 2014
Priority date	Dec 20, 2013
Publication date	Nov 27, 2018
Grant date	Nov 27, 2018

Abstract

Herein is reported a fusion polypeptide comprising i) one, two, three or four incretin receptor ligand polypeptides, and ii) one human immunoglobulin Fc-region, wherein at least one of the incretin receptor ligand polypeptides comprises an amino acid that is covalently conjugated to a lipid, and wherein each of the one, two, three or four incretin receptor ligand polypeptides is covalently conjugated by a peptide bond to a terminus of the human immunoglobulin Fc-region, whereby to each terminus of the human immunoglobulin Fc-region only a single incretin receptor ligand polypeptide is conjugated.

First claim

What is claimed is:

1. A fusion polypeptide comprising
a lipidated incretin receptor ligand polypeptide, and
a human immunoglobulin Fc-region, wherein said lipidated incretin receptor ligand polypeptide comprises the amino acid sequence of SEQ ID NO: 125 and the Fc-region comprises SEQ ID NO: 53 and said Fc-region is conjugated to either the carboxy terminus or amino terminus of the incretin receptor ligand polypeptide.

2. A pharmaceutical composition comprising a fusion polypeptide according to claim 1 .

3. A method of reducing weight gain or inducing weight loss, said method comprising administering the pharmaceutical composition of claim 2 to a patient in need thereof.

Assignees

• Univ Indiana Res & Tech Corp
• Hoffmann La Roche

Inventors

• Belli Sara
• Bleicher Konrad
• Dimarchi Richard D
• Hoffmann Eike
• Kitas Eric A
• Konkar Anish A

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• C07K14/605

  Glucagons · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• C07K2319/30

  Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto · CPC title

• A61K38/00

  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 title