IP Library Granted Patent US 9,877,943
Granted Patent B2
US 9,877,943 · App. 14/635,722 · Granted Jan 30, 2018

Compositions and methods comprising C16:1n7-palmitoleate

Inventor: Jeffrey Green (University Heights, OH)
Assignee: TERSUS LIFE SCIENCES, LLC
A61K31/201A23L33/115A61K31/22A61K31/231A61K45/06
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Quick Facts
Patent No.
US 9,877,943
App. No.
14/635,722
Granted
Jan 30, 2018
Kind
B2
Abstract

One embodiment described herein is related to methods and compositions, such as nutraceutical formulations and dietary supplements, comprising C16:1n7-palmitoleate or derivatives thereof. The methods and compositions comprising C16:1n7-palmitoleate, or derivatives thereof, safely and effectively prevent or mitigate manifestations of cardiovascular disease, including coronary artery disease and the accumulation of cholesterol or lipid deposits in the blood vessels of a subject.

Claims (25)

1. A method for improving heart health in a subject comprising administering to the subject an effective amount of a composition comprising a C16:1n7-palmitoleate derivative, a palmitate derivative and a C18:1n7-vaccenoate derivative, wherein the composition has a ratio of the C16:1n7-palmitoleate derivative to the C18:1n7-vaccenoate derivative of 1.1:1 to 100:1;

wherein each C16:1n7-palmitoleate derivative, palmitate derivative and C18:1n7-vaccenoate derivative is independently a free acid, pharmaceutically acceptable salt, (C 1 -C 4 )alkyl ester, monoglyceride, diglyceride, triglyceride, or a combination of any two or more thereof, and

wherein administration of the composition results in about a 5% increase in HDL after 30 days compared to that observed prior to administration.

2. The method of claim 1 , further comprising reducing plasma concentrations of LDL in the subject by about 8%.

3. The method of claim 1 , further comprising reducing cholesterol deposition within a blood vessel in the subject.

4. The method of claim 3 , wherein the lumen diameter of at least one blood vessel in the subject is increased by at least 10%.

5. The method of claim 3 , wherein the lumen diameter of at least one blood vessel in the subject is increased by at least 50%.

6. The method of claim 1 , further comprising reducing a cholesterol-associated lesion in a blood vessel in the subject.

7. The method of claim 1 , further comprising reducing blood pressure in the subject.

8. The method of claim 7 , wherein the subject exhibits at least a 10 mmHg reduction in systolic blood pressure.

9. The method of claim 7 , wherein the subject exhibits at least a 20 mmHg reduction in systolic blood pressure.

10. The method of claim 1 , further comprising reducing stenosis in the subject.

11. The method of claim 1 , further comprising reducing restenosis in the subject following angioplasty.

12. The method of claim 1 , wherein the blood lipid profile in the subject is improved.

13. The method of claim 1 , wherein the ratio of high-density lipoprotein (HDL) relative to low-density lipoprotein (LDL) in the blood serum of the subject is increased.

14. The method of claim 1 , further comprising increasing the ratio of apolipoprotein A1 (Apo-A1) relative to apolipoprotein B (Apo-B) in the blood serum of the subject.

15. The method of claim 1 , further comprising reducing triglyceride levels in the subject.

16. The method of claim 1 , further comprising reducing high sensitivity C-reactive protein (hsCRP) in the subject.

17. The method of claim 1 , wherein the subject exhibits one or more of the following outcomes: (a) reduced triglyceride levels compared to baseline; (b) reduced Apo B levels compared to baseline; (c) increased HDL-C levels compared to baseline; (d) no increase in LDL-C levels compared to baseline; (e) a reduction in LDL-C levels compared to baseline; (f) a reduction in non-HDL-C levels compared to baseline; (g) a reduction in vLDL levels compared to baseline; (h) an increase in apo A-I levels compared to baseline: (i) an increase in apo A-I/apo B ratio compared to baseline; (j) a reduction in lipoprotein A levels compared to baseline; (k) a reduction in LDL particle number compared to baseline; (l) an increase in LDL size compared to baseline; (min) a reduction in remnant-like particle cholesterol compared to baseline; (n) a reduction in oxidized LDL compared to baseline: (o) no change or a reduction in fasting plasma glucose (FPG) compared to baseline; (p) a reduction in hemoglobin Alc (HbAlc) compared to baseline; (q) a reduction in homeostasis model insulin resistance compared to baseline; (r) a reduction in lipoprotein associated phospholipase A2 compared to baseline; (s) a reduction in intracellular adhesion molecule-1 compared to baseline; (t) a reduction in interleukin-6 compared to baseline; (u) a reduction in plasminogen activator inhibitor-1 compared to baseline; (v) a reduction in high sensitivity C-reactive protein (hsCRP) compared to baseline; (w) an increase in serum or plasma C16:1n7-palmitoleate compared to baseline; (x) an increase in red blood cell (RBC) membrane C16:1n7-palmitoleate compared to baseline, and/or (y) a reduction or increase in one or more of serum phospholipid and/or red blood cell content of palmitic acid (PA), stearidonic acid (SA) or oleic acid (OA) compared to baseline.

18. The method of claim 1 , further comprising the administration of a medication selected from the group consisting of an angiotensin-converting enzyme inhibitor, angiotensin receptor blocker, beta-blocker, diuretic, vasodilator, α-blocker, calcium channel blocker, a HMG-CoA reductase inhibitor, ezetimibe therapy, and probucol.

19. The method of claim 18 , wherein the medication is a HMG-CoA reductase inhibitor.

20. A method for improving heart health in a subject comprising administering to the subject an effective amount of a composition comprising a C16:1n7-palmitoleate derivative, a palmitate derivative, an oleate derivative, and a C18:1n7-vaccenoate derivative, wherein the composition

(i) has a ratio of the C16:1n7-palmitoleate derivative to the oleate derivative of 6:1 to 100:1;

(ii) has a ratio of the C16:1n7-palmitoleate derivative to the C18:1n7-vaccenoate derivative of 1.1:1 to 100:1; and

wherein each C16:1n7-palmitoleate derivative, palmitate derivative, oleate derivative, and C18:1n7-vaccenoate derivative is independently a pharmaceutically acceptable salt, (C 1 -C 4 )alkyl ester, monoglyceride, diglyceride, triglyceride, or a combination of any two or more thereof, and wherein administration of the composition results in about a 5% increase in HDL after 30 days compared to that observed prior to administration.

Assignments (2)
CHANGE OF NAME Recorded Dec 19, 2017
From: TERSUS PHARMACEUTICALS, LLC
To: TERSUS LIFE SCIENCES, LLC
Reel/Frame 044914/0339 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2015
From: GREEN, JEFFREY
To: TERSUS PHARMACEUTICALS, LLC
Reel/Frame 035674/0878 →
Continuity (4)
Continuation 14242460 · Apr 1, 2014
Continuation 13411187 · Mar 2, 2012
Provisional Application 61449015 · Mar 3, 2011
Related Publication 20150224073A1 · Aug 13, 2015