Anti-obesity agent comprising high-purity EPA

Patent metadata

Field	Value
Publication number	US-9345681-B2
Application number	US-201214129890-A
Country	US
Kind code	B2
Filing date	Jul 6, 2012
Priority date	Jul 7, 2011
Publication date	May 24, 2016
Grant date	May 24, 2016

Abstract

The present invention provides an agent for preventing the increase in a body weight (or for decreasing a body weight) or an anti-obesity agent each comprising at least one component selected from the group consisting of EPA and pharmaceutically acceptable salts, esters and derivatives thereof as an active ingredient for obesity in which the increase in the formation of hepatic lipid or the occurrence of fatty liver is mild, preferably the increase in the formation of hepatic lipid or the occurrence of fatty liver is not observed.

First claim

The invention claimed is:

1. A method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having cholesteryl ester transforming protein (CETP) comprising the step of:
administering a composition comprising:
an agent for suppressing body weight gain or reducing body weight, or an anti-obesity agent containing at least one member selected from the group consisting of EPA, a pharmaceutically acceptable salt thereof, an ester thereof, and a derivative thereof as its effective component,
less than 2% by weight of at least one member selected from the group consisting of docosahexaenoic acid (DHA), a pharmaceutically acceptable salt thereof, an ester thereof, and a derivative thereof, and
less than 2% by weight of a long chain unsaturated fatty acid of arachidonic acid,

to a patient suffering from obesity, or obesity of a type wherein enhancement of hepatic lipogenesis or fatty liver is mild, the patient being a mammal having CETP,
wherein a content of said EPA, pharmaceutically acceptable salt thereof, ester therof, and derivative thereof in an entire fatty acid content of the composition is at least 45% by weight.

2. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 1 , wherein the effective component is ethyl icosapentate (EPA-E).

3. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity according to claim 1 , wherein purity of the effective component is as high as 90% by weight or more.

4. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 1 , wherein the effective component is administered at an effective dose for suppressing increase of (i) cholesteryl ester transfer protein (CETP) activity, (ii) low-density lipoprotein Cholesterol (LDL-C) level, or (iii) CETP activity and LDL-C level.

5. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 1 , wherein the agent is free from DHA, a pharmaceutically acceptable salt thereof, an ester thereof, or a derivative thereof.

6. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 1 , wherein the obesity is induced by intake of high fat diet.

7. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 1 , comprising the step of administering a blended drug containing at least one member selected from EPA, a pharmaceutically acceptable salt thereof, an ester thereof, and a derivative thereof as its first effective component and at least one cholesteryl ester transfer protein (CETP) inhibitor as its second effective component.

8. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 7 , wherein the cholesteryl ester transfer protein (CETP) inhibitor is dalcetrapib or anacetrapib.

9. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 2 , wherein purity of EPA-E is as high as 90% by weight or more.

10. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 2 , wherein the effective component is administered at an effective dose for suppressing increase of (i) cholesteryl ester transfer protein (CETP) activity, (ii) low-density lipoprotein Cholesterol (LDL-C) level, or (iii) CETP activity and LDL-C level.

11. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 2 , wherein the agent is free from DHA, a pharmaceutically acceptable salt thereof, an ester thereof, or a derivative thereof.

12. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 2 , wherein the obesity is induced by intake of high fat diet.

13. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 2 , comprising the step of administering a blended drug containing at least one member selected from EPA, a pharmaceutically acceptable salt thereof, an ester thereof, and a derivative thereof as its first effective component and at least one cholesteryl ester transfer protein (CETP) inhibitor as its second effective component.

14. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 2 , wherein the cholesteryl ester transfer protein (CETP) inhibitor is dalcetrapib or anacetrapib.

15. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 1 , wherein the patient is suffering from obesity of a type wherein enhancement of hepatic lipogenesis or fatty liver is not recognized.

16. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 6 , wherein the obesity is induced by continuous intake of high fat diet.

17. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 12 , wherein the obesity is induced by continuous intake of high fat diet.

18. A method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having cholesteryl ester transfer protein (CETP), comprising the step of administering a composition comprising:
an agent for suppressing body weight gain or reducing body weight or an anti-obesity agent containing at least one member selected from EPA, a pharmaceutically acceptable salt thereof, an ester thereof, and a derivative thereof as its effective component,
less than 2% by weight of at least one member selected from the group consisting of docosahexaenoic acid (DHA), a pharmaceutically acceptable salt thereof, an ester thereof, and a derivative thereof, and
less than 2% by weight of a long chain unsaturated fatty acid of arachidonic acid;
for combined administration with at least one compound selected from cholesteryl ester transfer protein (CETP) inhibitors which is a second effective component.

19. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 18 , comprising the step of administering a blended drug containing at least one member selected from EPA, a pharmaceutically acceptable salt thereof, an ester thereof, and a derivative thereof as its first effective component and at least one CETP inhibitor as its second effective component.

20. The method for suppressing body weight gain, reducing body weight, or preventing, alleviating, or treating obesity of a mammal having CETP according to claim 18 ,

Assignees

• Ishida Takayuki
• Kawano Hiroyuki
• Mochida Pharm Co Ltd

Inventors

• Ishida Takayuki
• Kawano Hiroyuki

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61K31/202

  having three or more double bonds, e.g. linolenic (eicosanoids, e.g. leukotrienes A61K31/557) · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K31/421

  1,3-Oxazoles, e.g. pemoline, trimethadione · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title