# US 8,785,469 B2 · Method of treating atherogenic dyslipidemia

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- Number: US 8,785,469 B2
- Document ID: US8785469B2
- Status: Granted
- Kind: B2
- Application number: 13/774,388
- Filed: 2013-02-22
- Published: 2013-07-04
- Granted: 2014-07-22
- Earliest claimed: 2006-10-20
- Assignees: Neurendo Pharma, LLC
- Applicants: Neurendo Pharma, LLC
- Inventors: Anton H. Clemens
- Web page: https://patentgrep.com/patent/US8785469B2

## CPC

- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61K 31/4748: forming part of bridged ring systems (strychnine A61K31/475; morphinan derivatives A61K31/485)
- A61K 38/45: Transferases (2)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to methods of treating metabolic syndrome, Type 2 diabetes mellitus, atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion. The methods of the present invention comprise administration of a selective κ-receptor antagonist, such as guanidinylated naltrindole (GNTI), or pharmaceutically acceptable derivatives thereof to a subject in need thereof.

## Claims

### Claim 1

A method of treating atherogenic dyslipidemia, comprising administering to a subject a therapeutically effective amount of a selective kappa-receptor antagonist, or a pharmaceutically acceptable derivative thereof, wherein a μ-agonist is not co-administered and wherein the selective κ-receptor antagonist is characterized by its μ/κ antagonism Ke selectivity ratio, the ratio being greater than 35.

### Claim 2 (depends on 1)

The method of claim 1, wherein the selective kappa-receptor antagonist is guanidinylated naltrindole (GNTI).

### Claim 3 (depends on 1)

The method of claim 1, wherein the selective kappa-receptor antagonist is administered weekly or daily.

### Claim 4 (depends on 3)

The method of claim 3, wherein the selective kappa-receptor antagonist is administered weekly in an amount from about 30 ng to about 300 ng per kg of body weight weekly.

### Claim 5 (depends on 3)

The method of claim 3, wherein the selective kappa-receptor antagonist is administered daily in an amount from about 8 ng to about 80 ng per kg of body weight daily.

### Claim 6 (depends on 1)

The method of claim 1, wherein the selective kappa-receptor antagonist is administered sublingually, orally, enterally, parenterally, topically, systemically or injected intravascularly, subcutaneously, peritoneally.

### Claim 7 (depends on 1)

The method of claim 1, further comprising co-administration of an effective amount of an insulinogenic agent.

### Claim 8 (depends on 7)

The method of claim 7, wherein the insulinogenic agent is an extended release composition.