CA2470235A1 - Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof - Google Patents

Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof Download PDF

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Publication number
CA2470235A1
CA2470235A1 CA002470235A CA2470235A CA2470235A1 CA 2470235 A1 CA2470235 A1 CA 2470235A1 CA 002470235 A CA002470235 A CA 002470235A CA 2470235 A CA2470235 A CA 2470235A CA 2470235 A1 CA2470235 A1 CA 2470235A1
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Canada
Prior art keywords
composition
patient
administering
reducing
pharmaceutically acceptable
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
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CA002470235A
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French (fr)
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CA2470235C (en
Inventor
Ezio Ghigo
Aart Jan Van Der Lely
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Millendo Therapeutics SAS
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Individual
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Publication date
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Priority to CA2470235A priority Critical patent/CA2470235C/en
Priority claimed from PCT/CA2002/001964 external-priority patent/WO2003051389A2/en
Publication of CA2470235A1 publication Critical patent/CA2470235A1/en
Application granted granted Critical
Publication of CA2470235C publication Critical patent/CA2470235C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/27Growth hormone [GH] (Somatotropin)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The present invention relates to compositions containing unacetylaed ghrelin and derivatives thereof and their uses in the control of glycemia in ageing patients, GH deficient patients, diabetic patients and obese patients.

Claims (57)

WHAT IS CLAIMED IS:
1. A composition for preventing and/or reducing postprandial induction of insulin resistance comprising a therapeutically effective amount of at least one of unacylated ghrelin, an analog thereof and a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier.
2. The composition of claim 1, wherein said unacylated ghrelin is having an amino acid as set forth in SEQ ID NO:1.
3. A method for reducing postprandial induction of insulin resistance in a patient comprising the step of administering a therapeutically effective amount of the composition of one of claims 1 and 2 to said patient.
4. The method of claim 3, wherein said administering is through a route selected from the group consisting of intravenous, subcutaneous, transdermal, oral, buccal, sublingual, nasal and by inhalation.
5. The method of claim 3, wherein said administering is in a dose varying from about 0,001 µg/kg to 10,0 µg/kg.
6. The method of claim 3, wherein said administering is in a dose varying from about 1 µg/kg to 1 mg/kg.
7. Use of the composition of one of claims 1 and 2 for reducing postprandial induction of insulin resistance in a patient.
8. Use of the composition of one of claims 1 and 2 for the preparation of a medicament for reducing postprandial induction of insulin resistance in a patient.
9. A composition for preventing and/or reducing dawn phenomenon in type I diabetes patient comprising a therapeutically effective amount of at least one of unacylated ghrelin, an analog thereof and a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier.
10. The composition of claim 9, wherein said unacylated ghrelin is having an amino acid as set forth in SEQ ID NO:1.
11. A method for preventing and/or reducing dawn phenomenon in type I diabetes patient comprising the step of administering a therapeutically effective amount of the composition of one of claims 9 and to said patient.
12. The method of claim 11, wherein said administering is through a route selected from the group consisting of intravenous, subcutaneous, transdermal, oral, buccal, sublingual, nasal and by inhalation.
13. The method of claim 11, wherein said administering is in a dose varying from about 0,001 µg/kg to 10,0 µg/kg.
14. The method of claim 11, wherein said administering is in a dose varying from about 1 µg/kg to 1 mg/kg.
15. Use of the composition of one of claims 9 and 10 for preventing and/or reducing dawn phenomenon in type I diabetes patient.
16. Use of the composition of one of claims 9 and 10 for the preparation of a medicament for preventing and/or reducing dawn phenomenon in type I diabetes patient.
17. A composition for reducing body weight increased in a patient suffering from at least one of type II diabetes and syndrome X comprising a therapeutically effective amount of at least one of unacylated ghrelin, an analog thereof, and a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier.
13. The composition of claim 17, wherein said unacylated ghrelin is having an amino acid as set forth in SEQ ID NO:1.
19. The composition of claim 17, wherein said patient is treated with oral antidiabetic drugs.
20. A method for reducing a body weight increased encountered by a patient suffering from at least one of type II diabetes and syndrome X
comprising the step of administering a therapeutically effective amount of the composition of one of claims 17 to 19.
21. The method of claim 20, wherein said administering is through a route selected from the group consisting of intravenous, subcutaneous, transdermal, oral, buccal, sublingual, nasal and by inhalation.
22. The method of claim 20, wherein said administering is in a dose varying from about 0,001 µg/kg to 10,0 µg/kg.
23. The method of claim 20, wherein said administering is in a dose varying from about 1 µg/kg to 1 mg/kg.
24. Use of the composition of one of claims 17 to 19 for reducing a body weight increased encountered by a patient suffering from at least one of type II diabetes and syndrome X.
25. Use of the composition of one of claims 17 to 19 for the preparation of a medicament for reducing a body weight increased encountered by a patient suffering from at least one of type II diabetes and syndrome X.
26. A composition for facilitating treatment of an insulin-resistant patient comprising a therapeutically effective amount of at least one of unacylated ghrelin, an analog thereof and a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier.
27. The composition of claim 26, wherein said unacylated ghrelin is having an amino acid as set forth in SEQ ID No:1.
28. A method for facilitating treatment of insulin-resistant patient comprising the step of administering a therapeutically effective amount of the composition of one of claims 26 and 27 to said patient.
29. The method of claim 28, wherein said administering is through a route selected from the group consisting of intravenous, subcutaneous, transdermal, oral, buccal, sublingual, nasal and by inhalation.
30. The method of claim 28, wherein said administering is in a dose varying from about 0,001 µg/kg to 10,0 µg/kg.
31. The method of claim 28, wherein said administering is in a dose varying from about 1 µg/kg to 1 mg/kg.
32. Use of the composition of one of claims 26 and 27 for facilitating treatment of insulin-resistant patient.
33. Use of the composition of one of claims 26 and 27 for the preparation of a medicament for facilitating treatment of insulin-resistant patient.
34. A composition for decreasing tat mass in a growth hormone-deficient patient comprising a therapeutically effective amount of at least one of unacylated ghrelin, an analog thereof and a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier.
35. The composition of claim 34, wherein said unacylated ghrelin is having an amino acid as set forth in SEQ ID NO:1.
36. A method for decreasing fat mass in a growth hormone-deficient patient comprising the step of administering a therapeutically effective amount of the composition of one of claims 34 and 35 to said patient.
37. The method of claim 36, wherein said administering is through a route selected from the group consisting of intravenous, subcutaneous, transdermal, oral, buccal, sublingual, nasal and by inhalation.
38. The method of claim 36, wherein said administering is in a dose varying from about 0,001 µg/kg to 10,0 µg/kg.
39. The method of claim 36, wherein said administering is in a dose varying from about 1 µg/kg to 1 mg/kg.
40. Use of the composition of one of claims 34 and 35 for decreasing fat mass in a growth hormone-deficient patient.
41. Use of the composition of one of claims 34 and 35 for the preparation of a medicament for decreasing fat mass in a growth hormone-deficient patient.
42. A composition for decreasing fat mass in an ageing patient having a high body mass index comprising a therapeutically effective amount of at least one of unacylated ghrelin, an analog thereof and a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier.
43. The composition of claim 42, wherein said unacylated ghrelin is having an amino acid as set forth in SEQ ID NO:1.
44. A method for decreasing fat mass in an ageing patient having a high body mass index comprising the step of administering a therapeutically effective amount of the composition of one of claims 42 and 43 to said patient.
45. The method of claim 44, wherein said administering is through a route selected from the group consisting of intravenous, subcutaneous, transdermal, oral, buccal, sublingual, nasal and by inhalation.
46. The method of claim 44, wherein said administering is in a dose varying from about 0,001 µg/kg to 10,0 µg/kg.
47. The method of claim 44, wherein said administering is in a dose varying from about 1 µg/kg to 1 mg/kg.
48. Use of the composition of one of claims 42 and 43 for decreasing fat mass in an ageing patient having a high body mass index.
49. Use of the composition of one of claims 42 and 43 for the preparation of a medicament for decreasing fat mass in an ageing patient having a high body mass index.
50. A composition for preventing and/or reducing insulin resistance in a patient comprising a therapeutically effective amount of at least one of unacylated ghrelin, an analog thereof and a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier.
51. The composition of claim 50, wherein said unacylated ghrelin is having an amino acid as set forth in SEQ ID NO:1.
52. A method for preventing and/or reducing insulin resistance in a patient in severe catabolism comprising the step of administering to said patient a therapeutically effective amount of the composition of one of claims 50 and 51.
53. The method of claim 52, wherein said administering is through a route selected from the group consisting of intravenous, subcutaneous, transdermal, oral, buccal, sublingual, nasal and by inhalation.
54. The method of claim 52, wherein said administering is in a dose varying from about 0,001 µg/kg to 10,0 µg/kg.
55. The method of claim 52, wherein said administering is in a dose varying from about 1 µg/kg to 1 mg/kg.
56. ~Use of the composition of one of claims 50 and 51 for preventing and/or reducing insulin resistance in a patient in severe catabolism.
57. ~Use of the composition of one of claims 50 and 51 for the preparation of a medicament for preventing and/or reducing insulin resistance in a patient in severe catabolism.
CA2470235A 2001-12-18 2002-12-18 Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof Expired - Fee Related CA2470235C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2470235A CA2470235C (en) 2001-12-18 2002-12-18 Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CA2365704 2001-12-18
CA2,365,704 2001-12-18
PCT/CA2002/001964 WO2003051389A2 (en) 2001-12-18 2002-12-18 Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof
CA2470235A CA2470235C (en) 2001-12-18 2002-12-18 Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof

Publications (2)

Publication Number Publication Date
CA2470235A1 true CA2470235A1 (en) 2003-06-26
CA2470235C CA2470235C (en) 2012-02-07

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005039624A1 (en) * 2003-10-24 2005-05-06 Theratechnologies Inc. Use of ghrelin and unacylated ghrelin compostions in insulin-related disease conditions
US7485620B2 (en) 2001-12-18 2009-02-03 Alizé Pharma SAS Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof
US7666833B2 (en) 2001-12-18 2010-02-23 Alizé Pharma SAS Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof
US8222217B2 (en) 2007-05-31 2012-07-17 Alize Pharma Sas Unacylated ghrelin as therapeutic agent in the treatment of metabolic disorders
US8318664B2 (en) 2007-05-31 2012-11-27 Alize Pharma Sas Unacylated ghrelin fragments as therapeutic agent in the treatment of obesity
US8476408B2 (en) 2008-06-13 2013-07-02 Alize Pharma Sas Unacylated ghrelin and analogs as therapeutic agents for vascular remodeling in diabetic patients and treatment of cardiovascular disease
US9550821B2 (en) 2011-12-15 2017-01-24 Alize Pharma Sas Modulation of ghrelin levels and ghrelin/unacylated ghrelin ratio using unacylated ghrelin

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7485620B2 (en) 2001-12-18 2009-02-03 Alizé Pharma SAS Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof
US7666833B2 (en) 2001-12-18 2010-02-23 Alizé Pharma SAS Pharmaceutical compositions comprising unacylated ghrelin and therapeutical uses thereof
US8071368B2 (en) 2001-12-18 2011-12-06 Alizé Pharma SAS Methods for promoting growth and survival of insulin-secreting cells
WO2005039624A1 (en) * 2003-10-24 2005-05-06 Theratechnologies Inc. Use of ghrelin and unacylated ghrelin compostions in insulin-related disease conditions
US7825090B2 (en) 2003-10-24 2010-11-02 Alizé Pharma SAS Use of ghrelin and unacylated ghrelin compositions for treating insulin resistance
US8222217B2 (en) 2007-05-31 2012-07-17 Alize Pharma Sas Unacylated ghrelin as therapeutic agent in the treatment of metabolic disorders
US8318664B2 (en) 2007-05-31 2012-11-27 Alize Pharma Sas Unacylated ghrelin fragments as therapeutic agent in the treatment of obesity
US8476408B2 (en) 2008-06-13 2013-07-02 Alize Pharma Sas Unacylated ghrelin and analogs as therapeutic agents for vascular remodeling in diabetic patients and treatment of cardiovascular disease
US9550821B2 (en) 2011-12-15 2017-01-24 Alize Pharma Sas Modulation of ghrelin levels and ghrelin/unacylated ghrelin ratio using unacylated ghrelin

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Publication number Publication date
CA2470235C (en) 2012-02-07

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