Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same

• US 5,424,286 A
• Filed: 05/24/1993
• Issued: 06/13/1995
• Est. Priority Date: 05/24/1993
• Status: Expired due to Term

• Current Assignee: John Eng
• Original Assignee: John Eng
• Inventors: Eng, John
• Primary Examiner(s): Draper, Garnette D.
• Assistant Examiner(s): KEMMERER, ELIZABETH
• Application Number:
  US08/066,480
• Time in Patent Office: 750 Days
• Field of Search: 514/2, 514/866, 424/88, 435/69.1, 530/324
• US Class Current: 514/5.9
• 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: C07K 14/57563 Vasoactive intestinal peptide [VIP]; Related peptides

Abstract

This invention encompasses pharmaceutical compositions containing exendin-3 or exendin-4, fragments thereof, or any combination thereof, and methods for the treatment of diabetes mellitus and the prevention of hyperglycemia.

Claims

1. A polypeptide having the amino acid sequence:

HGEGTFTSDL SKQMEEEAVR LFIEWLKNGG P[SEQ ID No;

3].

3. A pharmaceutical composition which comprises an effective insulinotropic amount of a substantially pure polypeptide, synthetic or purified from natural sources, having the amino acid sequence of claim 1 in a suitable carrier, which will stimulate the secretion of insulin in vivo.

2. A polypeptide having the amino acid sequence:

HGEGTFTSDL SKQMEEEAVR LFIEWLKNGG Y[SEQ ID No;

4].

4. A pharmaceutical composition which comprises an effective insulinotropic amount of a substantially pure polypeptide, synthetic or purified form natural sources, having the amino acid sequence of claim 2 in a suitable carrier, which will stimulate the secretion of insulin in vivo.

5. A method of stimulating insulin release in a mammal comprising administering an effective insulinotropic amount of a substantially pure polypeptide, synthetic or purified from natural sources, having the amino acid sequence:

space="preserve" listing-type="equation">HSDGTFITSDL SKQMEEEAVR LFIEWLKNGG PSSGAPPPS (SEQ ID NO;

     1),

wherein the resulting insulinotropic effect is greater than that attainable by administration of GLP-1.

6. A method of stimulating insulin release in a mammal comprising administering an effective insulinotropic amount of a substantially pure polypeptide, synthetic or purified from natural sources, having the amino acid sequence:

space="preserve" listing-type="equation">HGEGTFTSDL SKQMEEEAVR LFIEWLKNGG PSSGAPPPS (SEQ ID NO;

     2),

wherein the resulting insulinotropic effect is greater than that attainable by administration of GLP-1.

7. A method of inhibiting insulin release in a mammal comprising administering an effective amount of a substantially pure polypeptide, synthetic or purified from natural sources, having the amino acid sequence:

space="preserve" listing-type="equation">DL SKQMEEEAVR LFIEWLKNGG PSSGAPPPS (SEQ ID NO;

     5).