Claims for Patent: 7,462,626

Summary for Patent: 7,462,626

Title:	Compositions for affecting weight loss
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 .alpha.-MSH activity.
Inventor(s):	Weber; Eckard (San Diego, CA), Cowley; Michael Alexander (Portland, OR)
Assignee:	Orexigen Therapeutics, Inc. (San Diego, CA)
Application Number:	11/356,839
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,462,626
Patent Claims:	1. A method of treating overweight or obesity, comprising diagnosing an individual as suffering from overweight or obesity by determining said individual has a body mass index of at least 25 kg/m.sup.2, and treating said overweight or obesity by administering to said individual a first compound and a second compound in order to treat said overweight or obesity, wherein said second compound is bupropion or a pharmaceutically acceptable salt thereof in an amount effective to induce weight loss in said individual, and said first compound is naltrexone or a pharmaceutically acceptable salt thereof in an amount effective to enhance weight loss activity of said bupropion or a pharmaceutically acceptable salt thereof. 2. The method of claim 1, wherein said naltrexone or a pharmaceutically acceptable salt thereof and said bupropion or a pharmaceutically acceptable salt thereof are administered together. 3. The method of claim 1, wherein said naltrexone or a pharmaceutically acceptable salt thereof is administered prior to or subsequent to said bupropion or a pharmaceutically acceptable salt thereof. 4. The method of claim 1, wherein said individual is not suffering from depression. 5. The method of claim 1, wherein administration of said second compound further comprises administration of a weight-affecting amount of zonisamide. 6. The method of claim 1, wherein at least one of said naltrexone or a pharmaceutically acceptable salt thereof and said bupropion or a pharmaceutically acceptable salt thereof are in a sustained-release formulation. 7. The method of claim 1, in which the method is effective to increase satiety in the individual. 8. The method of claim 1, in which the method is effective to suppress the appetite of the individual. 9. The method of claim 1, wherein said amount of naltrexone, or a pharmaceutically acceptable salt thereof, is about 5 mg to about 50 mg per day. 10. The method of claim 1, wherein said amount of bupropion, or a pharmaceutically acceptable salt thereof, is about 30 mg to about 500 mg per day. 11. The method of claim 1, wherein said amount of naltrexone, or a pharmaceutically acceptable salt thereof, is about 5 mg to about 50 mg per day, and wherein said amount of bupropion, or a pharmaceutically acceptable salt thereof, is about 30 mg to about 500 mg per day. 12. The method of claim 1, wherein said bupropion, or a pharmaceutically acceptable salt thereof is in a sustained release formulation. 13. The method of claim 1, wherein said naltrexone, or a pharmaceutically acceptable salt thereof is in a sustained release formulation. 14. The method of claim 1, wherein said individual has a body mass index of 30 kg/m.sup.2 or above. 15. The method of claim 1, wherein said bupropion, or pharmaceutically acceptable salt thereof, and said naltrexone, or pharmaceutically acceptable salt thereof are administered in a single oral dosage form. 16. The method of claim 6, wherein said bupropion, or pharmaceutically acceptable salt thereof, and said naltrexone, or pharmaceutically acceptable salt thereof, are administered in a single oral dosage form. 17. The method of claim 1, wherein said method further comprises adjusting said amount of said first compound, said amount of said second compound, or both, as needed to treat said individual's overweight or obesity. 18. The method of claim 1, wherein said method further comprises adjusting said amount of said first compound, said amount of said second compound, or both, so that said individual loses weight at a rate of 10% of initial weight every 6 months. 19. The method of claim 1, wherein said method further comprises instituting a regimen of diet and increased activity. 20. The method of claim 1, wherein said individual has been diagnosed as suffering from a complication of said overweight or obesity selected from the group consisting of hypertension, non-insulin dependent diabetes mellitus, arteriosclerosis, dyslipidemia, cancer, sleep apnea, and osteoarthritis. 21. The method of claim 1, wherein said individual is administered said bupropion or a pharmaceutically-acceptable salt thereof and naltrexone or a pharmaceutically-acceptable salt thereof at least once a day during said treatment. 22. The method of claim 21, wherein said treatment is continued for a period of at least 16 weeks. 23. The method of claim 21, wherein said treatment is continued for a period of at least 24 weeks. 24. The method of claim 21, wherein said treatment is continued until said individual has achieved at least 5% weight loss or said individual's body mass index is reduced to less than 25 kg/m.sup.2. 25. A method of treating overweight or obesity, comprising administering a weight loss effective amount of a first and second compound to an individual who has been diagnosed as suffering from overweight or obesity in order to treat said overweight or obesity, wherein said first compound is bupropion, or a pharmaceutically acceptable salt thereof, and said second compound is naltrexone, or a pharmaceutically acceptable salt thereof, and wherein the weight loss activity of said first and second compounds is enhanced compared to the administration of the same amount of either compound alone. 26. The method of claim 25, wherein said naltrexone, or a pharmaceutically acceptable salt thereof, and said bupropion, or a pharmaceutically acceptable salt thereof, are administered together. 27. The method of claim 25, wherein said naltrexone, or a pharmaceutically acceptable salt thereof, is administered prior to or subsequent to said bupropion, or a pharmaceutically acceptable salt thereof. 28. The method of claim 25, wherein said individual is not suffering from depression. 29. The method of claim 25, wherein administration of said second compound further comprises administration of a weight-affecting amount of zonisamide. 30. The method of claim 25, wherein at least one of said naltrexone, or pharmaceutically acceptable salt thereof, and said bupropion, or pharmaceutically acceptable salt thereof are in a sustained-release formulation. 31. The method of claim 30, wherein said bupropion, or pharmaceutically acceptable salt thereof, and said naltrexone, or pharmaceutically acceptable salt thereof, are administered in a single oral dosage form. 32. The method of claim 25, in which the method is effective to increase satiety in the individual. 33. The method of claim 25, in which the method is effective to suppress the appetite of the individual. 34. The method of claim 25, wherein said amount of naltrexone, or a pharmaceutically acceptable salt thereof, is about 5 mg to about 50 mg per day. 35. The method of claim 25, wherein said amount of bupropion, or a pharmaceutically acceptable salt thereof, is about 30 mg to about 500 mg per day. 36. The method of claim 25, wherein said amount of naltrexone, or a pharmaceutically acceptable salt thereof, is about 5 mg to about 50 mg per day, and wherein said amount of bupropion, or a pharmaceutically acceptable salt thereof, is about 30 mg to about 500 mg per day. 37. The method of claim 25, wherein said bupropion, or pharmaceutically acceptable salt thereof, is in a sustained release formulation. 38. The method of claim 25, wherein said naltrexone, or pharmaceutically acceptable salt thereof, is in a sustained release formulation. 39. The method of claim 25, wherein said individual has a body mass index of 25 kg/m.sup.2 or above. 40. The method of claim 25, wherein said individual has a body mass index of 30 kg/m.sup.2 or above. 41. The method of claim 25, wherein said bupropion, or pharmaceutically acceptable salt thereof, and said naltrexone, or pharmaceutically acceptable salt thereof, are administered in a single oral dosage form. 42. The method of claim 25, wherein said method further comprises adjusting said amount of said first compound, said amount of said second compound, or both, as needed to treat said individual's overweight or obesity. 43. The method of claim 25, wherein said method further comprises adjusting said amount of said first compound, said amount of said second compound, or both, so that said individual loses weight at a rate of 10% of initial weight every 6 months. 44. The method of claim 25, wherein said method further comprises instituting a regimen of diet and increased activity. 45. The method of claim 25, wherein said individual has been diagnosed as suffering from a complication of said overweight or obesity selected from the group consisting of hypertension, non-insulin dependent diabetes mellitus, arteriosclerosis, dyslipidemia, cancer, sleep apnea, and osteoarthritis. 46. The method of claim 25, wherein said individual is administered said bupropion, or pharmaceutically acceptable salt thereof, and naltrexone, or pharmaceutically acceptable salt, thereof at least once a day during said treatment. 47. The method of claim 46, wherein said treatment is continued for a period of at least 16 weeks. 48. The method of claim 46, wherein said treatment is continued for a period of at least 24 weeks. 49. The method of claim 46, wherein said treatment is continued until said individual has achieved at least 5% weight loss or said individual's body mass index is reduced to less than 25 kg/m.sup.2.