Combination of an insulin and a glp-1-agonist

Patent metadata

Field	Value
Publication number	US-2025161416-A1
Application number	US-202519029209-A
Country	US
Kind code	A1
Filing date	Jan 17, 2025
Priority date	Oct 17, 2008
Publication date	May 22, 2025
Grant date	—

Abstract

The invention relates to a drug comprising at least one insulin and at least one GLP-1 receptor agonist.

First claim

1 . A medicament comprising at least one insulin and at least one GLP-1 agonist, the medicament being formulated and/or compounded in such a way that it comprises the insulin and the GLP-1 agonist each in a predetermined amount and can be administered in a dose adapted to the individual requirement of a patient.

2 . A medicament as claimed in claim 1 for adjusting the fasting, postprandial and/or postabsorptive blood glucose concentration in diabetes patients.

3 . A medicament as claimed in claim 1 or 2 for improving glucose tolerance.

4 . A medicament a claimed in any of the preceding claims for preventing hypoglycemia.

5 . A medicament as claimed in any of the preceding claims for preventing loss of function of the pancreatic β-cells.

6 . A medicament as claimed in any of the preceding claims for weight loss and/or for preventing weight gain.

7 . A medicament as claimed in any of the preceding claims , comprising a first pharmaceutical composition and a second pharmaceutical composition, and, optionally, at least one further pharmaceutical composition, which each comprise at least one insulin and at least one GLP-1 agonist and contain the at least one insulin and/or the at least one GLP-1 agonist in different weight fractions relative to the total weight of the composition.

8 . A medicament as claimed in claim 7 , the weight fractions of the at least one insulin and of the at least one GLP-1 agonist in the first pharmaceutical composition, in the second pharmaceutical composition, and in—where used—the at least one further pharmaceutical composition being selected such that the pharmaceutical compositions contain different proportions of insulin to GLP-1 agonist, based on the weight fraction.

9 . A medicament as claimed in claim 7 or 8 , the first, second, and, where used, further compositions comprising the at least one insulin in a substantially identical weight fraction and the at least one GLP-1 agonist in different weight fractions.

10 . A medicament as claimed in claim 7 or 8 , the first, second, and, where used, further compositions comprising the at least one GLP-1 agonist in a substantially identical weight fraction and the at least one insulin in different weight fractions.

11 . A medicament as claimed in any of claims 1 to 6 , comprising a first pharmaceutical composition and a second pharmaceutical composition, the first pharmaceutical composition comprising at least one insulin and the second pharmaceutical composition comprising at least one GLP-1 agonist, the medicament being formulated and/or compounded for the independent administration of the first and second pharmaceutical compositions.

12 . A medicament as claimed in any of claims 1 to 6 , comprising a first pharmaceutical composition and a second pharmaceutical composition, and, optionally, at least one further pharmaceutical composition, the first pharmaceutical composition comprising at least one insulin, and the second pharmaceutical composition comprising at least one insulin and at least one GLP-1 agonist, and the at least one further pharmaceutical composition comprising at least one insulin and at least one further active compound.

13 . A medicament as claimed in claim 12 , the first pharmaceutical composition, the second pharmaceutical composition, and—where used—the at least one further composition comprising the insulin in substantially identical weight fractions relative to the total weight of the composition.

14 . A medicament as claimed in any of the preceding claims , the at least one insulin being independently selected from human insulins, analogs, derivatives, and metabolites thereof.

15 . A medicament as claimed in claim 14 , the at least one insulin being independently selected from the group consisting of Gly(A21)-Arg(B31)-Arg(B32) human insulin, Lys B28 Pro B29 human insulin, B28 Asp human insulin, and B29Lys(ε-tetradecanoyl), desB30 human insulin.

16 . A medicament as claimed in any of the preceding claims , the at least one GLP-1 agonist being independently selected from the group consisting of GLP-1, analogs and derivatives thereof, exendin-3, analogs and derivatives thereof, exendin-4, analogs and derivatives thereof, and pharmacologically tolerable salts thereof.

17 . A medicament as claimed in claim 16 , the at least one CLP-1 agonist being independently selected from the group consisting of exendin-4, desPro 36 exendin-4(1-39)-Lys 6 -NH 2 [AVE0010], and Arg 34 , LYS 26 (N ε (γ-glutamyl(N α -hexadecanoyl)))GLP-1(7-37) [liraglutide], and pharmacologically tolerable salts thereof.

18 . A medicament as claimed in claim 17 , the at least one GLP-1 agonist being independently selected from the group consisting of exendin-4, analogs, derivatives, and pharmacologically tolerable salts thereof.

19 . A medicament as claimed in claim 18 , the at least one GLP-1 agonist being desPro 36 exendin-4(1-39)-Lys 6 -NH 2 .

20 . A medicament as claimed in any of the preceding claims , the insulin being Gly(A21)-Arg(B31)-Arg(B32) human insulin and the GLP-1 agonist being desPro 36 exendin-4(1-39)-Lyse-NH 2 or a pharmaceutically tolerable salt thereof.

21 . A kit comprising a medicament as claimed in any of claims 1 to 18 .

22 . A combination of Gly(A21)-Arg(B31)-Arg(B32) human insulin and desPro 36 exendin-4(1-39)-Lys 6 NH 2 and/or a pharmaceutically tolerable salt thereof.

23 . The use of at least one insulin and at least one GLP-1 agonist for preparing a medicinal product for treating a patient with diabetes, more particularly type 1 or 2 diabetes, for adjusting the fasting, postprandial and/or postabsorptive blood glucose concentration, for improving glucose tolerance, for preventing hypoglycemia, for preventing loss of function of the pancreatic β-cells, for weight loss and/or for preventing weight gain.

24 . A method of treating a patient with a medicament as claimed in claim 7 or with a kit comprising such a medicament, comprising
(a) selecting a dose of the at least one insulin that is to be administered,
(b) selecting a dose of the at least one GLP-1 agonist that is to be administered,
(c) selecting a composition, from the first, second, and, where used, at least one further compositions of the medicament that comprises the doses from (a) and (b) in a concentration such that the doses from (a) and (b) are present in the same volume, and
(d) determining and administering an amount which corresponds to the doses from (a) and (b).

25 . A method as claimed in claim 24 for adjusting the fasting, postprandial and/or postabsorptive blood glucose concentration, for improving glucose tolerance, for preventing hypoglycemia, for preventing loss of function of the pancreatic β-cells, for weight loss and/or for preventing weight gain.

26 . A method as claimed in claim 24 or 25 , step (c) being carried out on the basis of a table.

27 . A method of treating a patient with a medicament as claimed in claim 13 or with a kit comprising such a medicament, the medicament comprising:
(i.) selecting a dose of the at least one insulin that is to be administered, and determining the total amount of the first, second, and, where used, at least one further composition, so that the selected dose of the at least one insulin is present in the total amount,
(ii.) selecting a dose of the at least one GLP-1 agonist that is to be administered and determining the amount of the second comp

Assignees

• Sanofi Aventis Deutschland

Inventors

• Werner Ulrich
• Rotthauser Baerbel

Classifications

• A61K38/26 Primary

  Glucagons · CPC title

• A61K38/28 Primary

  Insulins · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P5/50

  for increasing or potentiating the activity of insulin · CPC title

• A61K38/17

  from animals; from humans {(enzyme inhibitors A61K38/005)} · CPC title