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Glycemic control using intrinsic factor bound to a vitamin B 12 conjugate of a glucagon-like peptide-1 receptor agonist

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اقرأ أكثر حفظ في قائمتي
  • Publication Date:
    October 03, 2023
  • معلومة اضافية
    • Patent Number:
      11771,772
    • Appl. No:
      17/239934
    • Application Filed:
      April 26, 2021
    • نبذة مختصرة :
      The present invention provides compositions and methods for lowering blood glucose. More specifically, the present invention provides compositions comprising a complex comprising IF and B12 conjugated to a peptide comprising a GLP-1 agonist. Advantageously, the composition may be delivered subcutaneously.
    • Inventors:
      Syracuse University (Syracuse, NY, US); Xeragenx LLC (St. Louis, MO, US)
    • Assignees:
      Syracuse University (Syracuse, NY, US), Xeragenx LLC (St. Louis, MO, US)
    • Claim:
      1. A method of lowering blood glucose in a subject in need thereof, wherein the method comprises subcutaneously or intraperitoneally administering to the subject an effective amount of a pharmaceutical composition comprising intrinsic factor (IF) complexed with a conjugate comprising B 12 or an analog thereof conjugated to a peptide comprising a glucagon-like peptide-1 (GLP-1) receptor agonist.
    • Claim:
      2. The method of claim 1 , wherein the lowering of blood glucose activity is increased relative to the lowering of blood glucose activity with the conjugate alone.
    • Claim:
      3. The method of claim 1 , wherein the pharmaceutical composition further comprises one or more pharmaceutically acceptable diluents, excipients, and/or carriers.
    • Claim:
      4. The method of claim 1 , wherein the peptide is conjugated to B 12 at the 5′ hydroxyl residue of the ribosyl group.
    • Claim:
      5. The method of claim 4 , wherein the 5′-hydroxyl residue of the ribose group is oxidized to a carboxylic acid prior to conjugation to the peptide.
    • Claim:
      6. The method of claim 1 , wherein the B 12 or analog thereof is conjugated to the peptide via a linker.
    • Claim:
      7. The method of claim 6 , wherein the linker comprises between three and six carbon atoms.
    • Claim:
      8. The method of claim 6 , wherein the linker comprises 4 carbon atoms.
    • Claim:
      9. The method of claim 1 , wherein the peptide comprises exendin-4 (EX-4).
    • Claim:
      10. The method of claim 1 , wherein the peptide comprises the sequence set forth in SEQ ID NO:1 or SEQ ID NO:2.
    • Claim:
      11. The method of claim 10 , wherein the peptide comprising SEQ ID NO:1 is conjugated to the 5′-hydroxyl residue of the ribose group of B 12 via the azido group at lysine 12 of SEQ ID NO:1.
    • Claim:
      12. The method of claim 1 , wherein the IF is purified from a transgenic plant.
    • Patent References Cited:
      20100184642 July 2010 Berglund
      WO-2008109068 September 2008
    • Other References:
      Clardy-James et al, Site-Selective Oxidation of Vitamin B12 Using 2-Iodoxybenzoic Acid, SYNLETT, 2012, 23, pp. 2363-2366. cited by examiner
    • Primary Examiner:
      Komatsu, Li N
    • Attorney, Agent or Firm:
      Nocilly, David L.
    • الرقم المعرف:
      edspgr.11771772