IP Library Granted Patent US 10,317,418
Granted Patent B2
US 10,317,418 · App. 15/052,110 · Granted Jun 11, 2019

Use of ghrelin or functional ghrelin receptor agonists to prevent and treat stress-sensitive psychiatric illness

Inventor: Ki Ann Goosens (Cambridge, MA)
Assignee: Massachusetts Institute of Technology
G01N33/74A61K31/165A61K31/395A61K31/40A61K31/404A61K31/415A61K31/4439A61K31/4545A61K31/7076A61K38/25G01N2800/30G01N2800/54
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Quick Facts
Patent No.
US 10,317,418
App. No.
15/052,110
Granted
Jun 11, 2019
Kind
B2
Abstract

The invention relates to methods of treating stress-sensitive psychiatric diseases arising from trauma in a subject by enhancing ghrelin signaling in the BLA of the subject. The invention also relates to methods of reversing ghrelin resistance.

Claims (42)

1. A method of treating a stress-sensitive psychiatric disease in a subject comprising administering to the subject a therapeutically effective amount of ghrelin or a functional ghrelin receptor (GHSR) agonist, within a memory consolidation period following a trauma exposure, wherein the stress-sensitive psychiatric disease is selected from the group consisting of: Post-traumatic Stress Disorder (PTSD), Depressive Disorder, Major Depressive Disorders, Bipolar Disorder, Acute Stress Disorder, Generalized Anxiety Disorder, Obsessive-Compulsive Disorder, Panic Disorders, and Trichotillomania, wherein the functional GHSR agonist is not adenosine.

2. The method of claim 1 , wherein the ghrelin or the functional GHSR agonist is administered within 24 hours following the trauma exposure.

3. The method of claim 1 , wherein the ghrelin or the functional GHSR agonist is administered within 48 hours following the trauma exposure.

4. The method of claim 1 , wherein the ghrelin or the functional GHSR agonist is administered within 1 week following the trauma exposure.

5. The method of claim 1 , wherein ghrelin is administered to the subject.

6. The method of claim 5 , wherein the ghrelin is in the form of acyl-ghrelin.

7. The method of claim 1 , wherein a functional GHSR agonist is administered to the subject.

8. The method of claim 7 , wherein the functional GHSR agonist is selected from the group consisting of: alexamorelin, Anamorelin, Capromorelin, CP-464709, Cortistatin-14, Examorelin (hexarelin), Growth Hormone Releasing Peptide-1 (GHRP-1), Growth Hormone Releasing Peptide-3 (GHRP-3), Growth Hormone Releasing Peptide-4 (GHRP-4), Growth Hormone Releasing Peptide 5 (GHRP-5), Growth Hormone Releasing Peptide-6 (GHRP-6), Ibutamoren (MK-677), Ibutamoren mesylate (IBU), Ipamorelin, L-692585, LY-426410, LY-444711, Macimorelin, Pralmorelin, Relamorelin, SM-130,686, Tabimorelin, Ulimorelin, and combination thereof.

9. The method of claim 8 , wherein the functional GHSR agonist is ibutamoren mesylate (IBU).

10. The method of claim 1 , wherein the administering is via systemic administration, injection, or infusion directly into the BLA of the subject.

11. The method of claim 1 , wherein the subject is unstressed.

12. The method of claim 1 , wherein the subject is a human.

13. A method of treating a stress-sensitive psychiatric disease in a subject comprising administering to the subject a therapeutically effective amount of ghrelin or a functional ghrelin receptor (GHSR) agonist, within a memory re-consolidation period following re-activation of a memory of a previous trauma exposure,

wherein the stress-sensitive psychiatric disease is selected from the group consisting of: Post-traumatic Stress Disorder (PTSD), Depressive Disorder, Major Depressive Disorders, Bipolar Disorder, Acute Stress Disorder, Generalized Anxiety Disorder, Obsessive-Compulsive Disorder, Panic Disorders, and Trichotillomania, wherein the ghrelin agonist is not adenosine.

14. The method of claim 13 , wherein the ghrelin or the functional GHSR agonist is administered within 24 hours following the re-activation of a memory of a previous trauma exposure.

15. The method of claim 13 , wherein the ghrelin or the functional GHSR agonist is administered within 48 hours following the re-activation of a memory of a previous trauma exposure.

16. The method of claim 13 , wherein the ghrelin or the functional GHSR agonist is administered within 1 week following the re-activation of a memory of a previous trauma exposure.

17. The method of claim 13 , wherein ghrelin is administered to the subject.

18. The method of claim 17 , wherein the ghrelin is in the form of acyl-ghrelin.

19. The method of claim 13 , wherein a functional GHSR agonist is administered to the subject.

20. The method of claim 19 , wherein the functional GHSR agonist is selected from the group consisting of: alexamorelin, Anamorelin, Capromorelin, CP-464709, Cortistatin-14, Examorelin (hexarelin), Growth Hormone Releasing Peptide-1 (GHRP-1), Growth Hormone Releasing Peptide-3 (GHRP-3), Growth Hormone Releasing Peptide-4 (GHRP-4), Growth Hormone Releasing Peptide 5 (GHRP-5), Growth Hormone Releasing Peptide-6 (GHRP-6), Ibutamoren (MK-677), Ibutamoren mesylate (IBU), Ipamorelin, L-692585, LY-426410, LY-444711, Macimorelin, Pralmorelin, Relamorelin, SM-130,686, Tabimorelin, Ulimorelin, and combination thereof.

21. The method of claim 20 , wherein the functional GHSR agonist is ibutamoren mesylate (IBU).

22. The method of claim 13 , comprising administering to the subject a therapeutically effective amount of ghrelin and a functional ghrelin receptor (GHSR) agonist.

23. The method of claim 13 , wherein the administering is via systemic administration, injection, or infusion directly into the basolateral complex of the amygdala (BLA) of the subject.

24. The method of claim 13 , wherein the subject is unstressed.

25. The method of claim 13 , wherein the subject is a human.

26. The method of claim 13 , wherein the memory of the previous trauma exposure is a long-term memory.

27. A method of treating a stress-sensitive psychiatric disease in a subject who has been exposed to chronic stress, comprising:

(a) upregulating the endogenous level of ghrelin receptors (GHSRs) in the subject, the upregulating comprising administering to the subject a therapeutically effective amount of a ghrelin antagonist or a GHSR antagonist; and

(b) administering to the subject a therapeutically effective amount of ghrelin or a functional GHSR agonist, within a memory consolidation period following a trauma exposure, wherein the stress-sensitive psychiatric disease is selected from the group consisting of: Post-traumatic Stress Disorder (PTSD), Depressive Disorder, Major Depressive Disorders, Bipolar Disorder, Acute Stress Disorder, Generalized Anxiety Disorder, Obsessive-Compulsive Disorder, Panic Disorders, and Trichotillomania.

28. The method of claim 27 , wherein the ghrelin antagonist is an anti-ghrelin vaccine.

29. The method of claim 27 , wherein the ghrelin antagonist inhibits ghrelin acylation.

30. The method of claim 27 , wherein the ghrelin or the functional GHSR agonist is administered within 24 hours following the trauma exposure.

31. The method of claim 27 , wherein the ghrelin or the functional GHSR agonist is administered within 48 hours following the trauma exposure.

32. The method of claim 27 , wherein the ghrelin or the functional GHSR agonist is administered within 1 week following the trauma exposure.

33. The method of claim 27 , wherein the functional GHSR agonist is selected from the group consisting of: Adenosine, alexamorelin, Anamorelin, Capromorelin, CP-464709, Cortistatin-14, Examorelin (hexarelin), Growth Hormone Releasing Peptide-1 (GHRP-1), Growth Hormone Releasing Peptide-3 (GHRP-3), Growth Hormone Releasing Peptide-4 (GHRP-4), Growth Hormone Releasing Peptide-5 (GHRP-5), Growth Hormone Releasing Peptide-6 (GHRP-6), Ibutamoren (MK-677), Ibutamoren mesylate (IBU), Ipamorelin, L-692585, LY-426410, LY-444711, Macimorelin, Pralmorelin, Relamorelin, SM-130,686, Tabimorelin, Ulimorelin, and combination thereof.

34. The method of claim 27 , wherein the step of upregulating further comprises measuring the endogenous ghrelin levels in the subject.

35. The method of claim 27 , wherein the subject who have been exposed to chronic stress has elevated endogenous ghrelin levels compared to that of a control.

36. The method of claim 35 , wherein the control is a subject not exposed to chronic stress.

37. The method of claim 27 , wherein the subject is a human.

38. The method of claim 29 , wherein the ghrelin antagonist inhibits ghrelin O-acyltransferase (GOAT).

39. The method of claim 38 , wherein the ghrelin antagonist is an anti-GOAT vaccine.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jun 22, 2016
From: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 039114/0855 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 16, 2016
From: GOOSENS, KI ANN
To: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Reel/Frame 038104/0371 →
Continuity (2)
Provisional Application 62119898 · Feb 24, 2015
Related Publication 20160243197A1 · Aug 25, 2016