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Compositions for affecting weight loss

a composition and weight loss technology, applied in the field of compositions affecting weight loss, can solve the problems of obesity being generally considered a psychological problem, a global problem, and the user's death, and achieve the effects of increasing energy expenditure, increasing satiety in an individual, and weight loss

Inactive Publication Date: 2007-11-22
OREXIGEN THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.

Problems solved by technology

Obesity has been recognized as one of the leading causes of disease and is emerging as a global problem.
Prior to 1994, obesity was generally considered a psychological problem.
Unfortunately, it was discovered that fenfluramine caused heart-valve complications, which in some cases resulted in the death of the user.
There has been some limited success with other combination therapy approaches, particularly in the field of psychological eating disorders.
Of course, this disorder is an issue for only a small portion of the population.
In addition to those individuals who satisfy a strict definition of medical obesity, a significant portion of the adult population is overweight.

Method used

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  • Compositions for affecting weight loss
  • Compositions for affecting weight loss
  • Compositions for affecting weight loss

Examples

Experimental program
Comparison scheme
Effect test

example 1

Combination of Fluoxetine and Naltrexone

[0209] Individuals having a BMI of greater than 25 are identified. Each individual is instructed to take one 20 mg tablet of fluoxetine (PROZAC®) on a daily basis, in addition to one 50 mg tablet of naltrexone on a daily basis.

[0210] The individuals are monitored for a period of months. It is recommended that the dosage be adjusted so that each individual loses weight at a rate of 10% of initial weight every 6 months. However, the rate of weigh loss for each individual may be adjusted by the treating physician based on the individual's particular needs.

[0211] If the initial dosage is not effective, then the fluoxetine dosage can be increased by 20 mg per day, though never exceeding 80 mg total per day. If the initial dosage results in a more rapid weight loss than the above rate, the dosage of each of fluoxetine or naltrexone can be reduced.

[0212] Fluoxetine has a physiological half life of about 9 hours, whereas that of naltrexone is abou...

example 2

Combination of Fluoxetine and Nalmefene

[0213] Individuals having a BMI of greater than 25 are identified. Each individual is instructed to take one 20 mg tablet of fluoxetine (PROZAC®) on a daily basis. In addition, each individual is injected with 1 mL of a solution of 100 μg of nalmefene in 1 mL of saline, intravenously, intramuscularly, or subcutaneously.

[0214] The individuals are monitored for a period of months. It is recommended that the dosage be adjusted so that each individual loses weight at a rate of 10% of initial weight every 6 months. However, the rate of weigh loss for each individual may be adjusted by the treating physician based on the individual's particular needs.

[0215] If the initial dosage is not effective, then the fluoxetine dosage can be increased by 20 mg per day, though never exceeding 80 mg total per day. In addition, the dosage of nalmefene may be increased up to 2 mL of a solution of 1 mg of nalmefene in 1 mL of saline. If the initial dosage results ...

example 3

Combination of Fluoxetine and Naloxone

[0216] Individuals having a BMI of greater than 25 are identified. Each individual is instructed to take one 20 mg tablet of fluoxetine (PROZAC®) on a daily basis. In addition, each individual is injected with 1 mL of a solution of 400 μg of naloxone in 1 mL of saline, intravenously, intramuscularly, or subcutaneously.

[0217] The individuals are monitored for a period of months. It is recommended that the dosage be adjusted so that each individual loses weight at a rate of 10% of initial weight every 6 months. However, the rate of weigh loss for each individual may be adjusted by the treating physician based on the individual's particular needs.

[0218] If the initial dosage is not effective, then the fluoxetine dosage can be increased by 20 mg per day, though never exceeding 80 mg total per day. If the initial dosage results in a more rapid weight loss than the above rate, the dosage of each of fluoxetine or nalmefene can be reduced.

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Abstract

Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.

Description

RELATED APPLICATIONS [0001] This application is a continuation of application Ser. No. 10 / 828,795, filed Apr. 21, 2004, which claims the benefit under 35 USC § 119(e) of U.S. Provisional Application No. 60 / 466,838, filed on Apr. 29, 2003, the entire disclosures of which are incorporated herein by reference in their entirety.BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] The present invention is in the field of pharmaceutical compositions and methods for the treatment of obesity and for affecting weight loss in individuals. [0004] 2. Description of the Related Art [0005] Obesity is a disorder characterized by the accumulation of excess fat in the body. Obesity has been recognized as one of the leading causes of disease and is emerging as a global problem. Increased instances of complications such as hypertension, non-insulin dependent diabetes mellitus, arteriosclerosis, dyslipidemia, certain forms of cancer, sleep apnea, and osteoarthritis have been related to i...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/443A61K31/4525A61P3/04A61K31/135A61K31/138A61K31/485
CPCA61K31/135A61K31/138A61K31/485A61K45/06Y10S514/909Y10S514/964A61K2300/00A61P3/04A61K31/137A61P3/00A61P43/00A61K31/35
Inventor WEBER, ECKARDCOWLEY, MICHAEL ALEXANDER
Owner OREXIGEN THERAPEUTICS INC
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