Treatment with omega-3 fatty acids and ppar agonist and/or antagonist and a combination product thereof

A fatty acid, agonist technology, applied in obesity, to address problems that do not show synergistic effects of hyperlipidemia and hyperlipoproteinemia

Inactive Publication Date: 2008-01-02
RELIANT PHARMACEUTICALS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] Combinations of certain fish oils with gemfibrozil or clofibrate have not shown any synergy in the treatment of hyperlipidemia and hyperlipoproteinemia in the past

Method used

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  • Treatment with omega-3 fatty acids and ppar agonist and/or antagonist and a combination product thereof
  • Treatment with omega-3 fatty acids and ppar agonist and/or antagonist and a combination product thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] The following formulations can be prepared according to the present invention:

[0058] Recipe 1

[0059] Element

Mg / capsule

K85EE

1000

Fenofibrate

32.5～100

[0060] Recipe 2

[0061] Element

Mg / capsule

K80EE

1000

Dehydrated ethanol

50

Propylene glycol monocaprylate (ester)

20

Fenofibrate

15～100

[0062] Recipe 3

[0063] Element

Mg / capsule

K85EE

1000

Glycerin

35

Polyethoxylated castor oil

25

Biglitazone

5～50

[0064] Recipe 4

[0065] Element

Embodiment 2

[0067] A 51-year-old man presented with acute pancreatitis and was diagnosed with familial hypertriglyceridemia. On a strict diet and started fenofibrate treatment (Antara  130mg QD), the pancreatitis improved and the patient was discharged. However, after about 2 weeks of fenofibrate treatment, the patient still maintained a triglyceride (TG) level of 749 mg / dL. Thereafter, the patient started Omacor  Treatment (90% omega-3 acid ethyl ester, 4 g per day, QD) while continuing fenofibrate treatment. After one month of combination therapy, the patient's TG was reduced by 69% to 235 mg / dL. In addition, the patient's total cholesterol level was reduced by 46% (from 280 mg / dL to 151 mg / dL) after combination therapy. See Table 1.

[0068] Table 1

[0069] Fenofibrate only

[0070] The above results show that when Omacor  Synergistic effect when administered with fenofibrate. Since the general experience is that either agent alone reduces total cholesterol by o...

Embodiment 3

[0072] Omacor was administered to 24 patients  Studies with fenofibrate. As shown in Figure 1, it was observed that Omacor  Blood levels (AUC) of fenofibric acid were reduced by nearly 30% compared to fenofibrate (circle). The results in Figure 1 show that when fenofibrate and Omacor  When administered together, the increased elimination constant of fenofibrate was consistent with the decreased half-life compared to when fenofibrate was administered alone.

[0073] As it is well known that the addition of fatty or oily substances (e.g. fatty meat) to fenofibrate increases blood levels (AUC) of fenofibrate, the observed results were unpredictable (see e.g. Antara  Prescribing Information for Fenofibrate Capsules). However, joining Omacor  , an oily substance mainly composed of fatty acid esters, has the opposite effect. Without being bound by theory, the observed decrease in systemic levels of fenofibrate may be related to enhanced metabolism of fenofibrate. Thus, t...

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PUM

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Abstract

A method and composition for blood lipid therapy that comprises administering to the subject an effective amount of a PPAR agonist and / or antagonist and an omega-3 fatty acid. The methods and compositions include combination products or concomitant therapy for the treatment of subjects with hypertriglyceridemia, hypercholesteremia, mixed dyslipidemia, vascular disease, a rtheroscl erotic disease and related conditions, obesity, the prevention or reduction of cardiovascular and vascular events, the reduction of insulin resistance, fasting glucose levels and postprandial glucose levels, and / or the reduction of incidence and / or the delay of onset of diabetes.

Description

[0001] This application claims priority to Provisional Patent Application 60 / 633,125, filed December 6,2004. This provisional application is hereby incorporated by reference in its entirety. technical field [0002] The present invention relates to a method for the treatment of hypertriglyceridemia, hypercholesterolemia, mixed dyslipidemia, vascular disease, arteriosclerotic disease (artherosclerotic disease) using PPAR agonists and / or antagonists and omega-3 fatty acids ) and related diseases, obesity, preventing or reducing cardiovascular and vascular morbidity, reducing insulin resistance, fasting glucose levels and postprandial glucose levels, and / or reducing the incidence of diabetes, and / or delaying the onset of diabetes. The invention also relates to combinations of PPAR agonists and / or antagonists and omega-3 fatty acids. Background technique [0003] In humans, cholesterol and triglycerides are part of the lipoprotein complexes in the bloodstream and can be separat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/20A61K31/19
CPCA61K31/202A61K31/192A61K31/426A61K31/22A61K45/06A61P3/04A61P3/06A61P3/08A61P3/10A61P9/00A61P9/10A61K2300/00
Inventor 乔治·博博泰斯鲁洛夫·M.·L.·龙根罗伯特·A.·MS.·沙尔维特斯
Owner RELIANT PHARMACEUTICALS INC
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