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Claims for Patent: 7,674,776

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Claims for Patent: 7,674,776

Title:Combination therapy for effecting weight loss and treating obesity
Abstract: The present invention features a novel therapy for effecting weight loss which involves treating a subject with a sympathomimetic agent (e.g., phentermine or a phentermine-like drug) in combination with an anticonvulsant sulfamate derivative (e.g., topiramate) such that the subject experiences weight loss. The combination methods of the present invention also are effective against symptoms associated with Syndrome X. The invention also features pharmaceutical compositions and kits for use in the practice of these novel therapies.
Inventor(s): Najarian; Thomas (Los Osos, CA)
Assignee: Vivus, Inc. (Mountain View, CA)
Application Number:11/385,233
Patent Claims: 1. A composition comprising an anticonvulsant agent and phentermine in amounts that in combination are effective to induce weight loss in a patient, wherein the anticonvulsant agent is an anticonvulsant sulfamate derivative having the structure of formula (I) ##STR00012## wherein X is CH.sub.2 or O, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are independently H or C.sub.1-C.sub.4 alkyl, and further wherein when X is O, then R.sub.2 and R.sub.3, and/or R.sub.4 and R.sub.5, may be taken together to form a methylene dioxy linkage of the formula --O--CR.sub.6R.sub.7--O-- in which R.sub.6 and R.sub.7 are independently H or C.sub.1-C.sub.3 alkyl, or may be taken together to form a cyclopentyl or cyclohexyl ring.

2. The composition of claim 1, comprising a dosage form that provides for immediate release of the phentermine and controlled release of the anticonvulsant agent.

3. The composition of claim 2, wherein the dosage form provides for delayed release of the anticonvulsant agent.

4. The composition of claim 3, wherein the dosage form additionally provides for sustained release of the anticonvulsant agent.

5. A method for effecting a desired weight loss in a subject, comprising a administering once daily to the subject the composition of claim 1 until the subject has experienced the desired weight loss.

6. The method of claim 5, wherein the subject is overweight.

7. The method of claim 6, wherein the subject is obese.

8. The method of claim 5, wherein the subject is neither overweight nor obese.

9. The method of claim 5, wherein the subject suffers from a condition that can be alleviated with loss of body weight.

10. A controlled release dosage form comprising phentermine and topiramate in amounts that in combination are effective to induce weight loss in a patient, wherein the dosage form provides for immediate release of the phentermine and delayed release of the topiramate.

11. The dosage form of claim 10, which further provides for sustained release of the topiramate.

12. The dosage form of claim 11, wherein a physiologically effective blood level of topiramate is provided over a 4-hour period.

13. The dosage form of claim 11, wherein a physiologically effective blood level of topiramate is provided over an 8-hour period.

14. The dosage form of claim 11, wherein a physiologically effective blood level of topiramate is provided over a 12-hour period.

15. The dosage form of claim 10, wherein release of topiramate is delayed by 4 hours following release of phentermine.

16. The dosage form of claim 10, wherein release of topiramate is delayed by 8 hours following release of phentermme.

17. The dosage form of claim 10, wherein release of topiramate is delayed by 12 hours following release of phentermine.

18. A method for effecting a desired weight loss in a subject, comprising administering once daily to the subject the controlled release dosage form of claim 10, until the subject has experienced the desired weight loss.

19. The method of claim 18, wherein the subject is overweight.

20. The method of claim 19, wherein the subject is obese.

21. The method of claim 18, wherein the subject is neither overweight nor obese.

22. The method of claim 18, wherein the subject suffers from a condition that can be alleviated with loss of body weight.

23. A controlled release dosage form comprising 15 mg of phentermine and 100 mg of topiramate, wherein the dosage form provides for immediate release of the phentermine and delayed release of the topiramate.

24. A controlled release dosage form comprising 8 mg of phentermine and 50 mg of topiramate, wherein the dosage form provides for immediate release of the phentermine and delayed release of the topiramate.

25. A controlled release formulation comprising phentermine and topiramate, wherein oral administration of the formulation results in immediate release of the phentermine and controlled release of the topiramate, and further wherein the topiramate is present in the form of granules, delayed release granules, granules within a matrix, or a combination with a polymeric mixture.

26. The formulation of claim 25, wherein the topiramate is present in the form of delayed release granules.

27. The formulation of claim 25, wherein the phentermine is in readily dissolvable form.

28. The formulation of claim 26, wherein the phentermine is in readily dissolvable form.

29. A controlled release formulation comprising 15 mg phentermine and 100 mg topiramate, wherein oral administration of the formulation results in immediate release of the phentermine and delayed release of the topiramate, and further wherein the topiramate is present in the form of granules, delayed release granules, granules within a matrix, or a combination with a polymeric mixture.

30. The formulation of claim 29, wherein the topiramate is present in the form of delayed release granules.

31. The formulation of claim 30, wherein the phentermine is in readily dissolvable form.

32. The formulation of claim 29, wherein the phentermine is in readily dissolvable form.

33. A controlled release formulation comprising a topiramate core and a layer of phentermine such that oral administration of the formulation provides for immediate release of the phentermine and delayed or sustained release of the topiramate.

34. The formulation of claim 33, wherein the formulation provides for delayed release of the topiramate.

35. The formulation of claim 34, further including a barrier layer between the core surface and the phentermine layer, said barrier layer serving to limit drug release from the surface of the core.

36. The formulation of claim 35, wherein the barrier layer prevents dissolution of the core when the formulation is first exposed to gastric fluid in the body.

37. The formulation of claim 35, wherein the barrier layer comprises a disintegrant.

38. The formulation of claim 35, wherein the barrier layer comprises a dissolution-retardant coating.

39. The formulation of claim 35, wherein the dissolution-retardant coating is polymeric.

40. The formulation of claim 39, wherein the dissolution-retardant coating is composed of an enteric polymer.

41. The formulation of claim 35, wherein the baffler layer comprises a hydrophobic coating.

42. A dosage form comprising phentermine in an immediate release, readily dissolvable form and delayed release granules of topiramate.

43. The dosage form of claim 42, comprising 8 mg phentermine.

44. The dosage form of claim 43, comprising 50 mg topiramate.

45. The dosage form of claim 44, comprising 15 mg phentermine.

46. The dosage form of claim 45, comprising 100 mg topiramate.

47. A method for effecting a desired weight loss in a subject, comprising administering 15 mg of phentermine and 100 mg topiramate to said subject on a daily basis until the subject has experienced the desired weight loss.

48. The method of claim 47, wherein the subject is overweight.

49. The method of claim 48, wherein the subject is obese.

50. The method of claim 47, wherein the subject is neither overweight nor obese.

51. The method of claim 47, wherein the subject suffers from a condition that can be alleviated with loss of body weight.

52. A method for effecting a desired weight loss in a subject, comprising administering 8 mg of phentermine and 50 mg topiramate to said subject on a daily basis until the subject has experienced the desired weight loss.

53. The method of claim 52, wherein the subject is overweight.

54. The method of claim 53, wherein the subject is obese.

55. The method of claim 52, wherein the subject is neither overweight nor obese.

56. The method of claim 52, wherein the subject suffers from a condition that can be alleviated with loss of body weight.

57. A method for effecting a desired weight loss in a subject in need thereof comprising administering to said subject, on a daily basis and until the desired weight loss is achieved, a therapeutically effective amount of phentermine, and an amount of an anticonvulsant agent selected to prevent the loss of effectiveness of the phentermine, wherein the anticonvulsant agent is an anticonvulsant sulfamate derivative having the structure of formula (I) ##STR00013## wherein X is CH.sub.2 or O, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are independently H or C.sub.1-C.sub.4 alkyl, and further wherein when X is O, then R.sub.2 and R.sub.3, and/or R.sub.4 and R.sub.5 may be taken together to form a methylene dioxy linkage of the formula --O--CR.sub.6R.sub.7--O-- in which R.sub.6 and R.sub.7 are independently H or C.sub.1-C.sub.3 alkyl, or may be taken together to form a cyclopentyl or cyclohexyl ring.

58. A method for treating at least one side effect associated with obesity comprising administering to a subject, on a daily basis and until the side effect associated with obesity is effectively treated, a therapeutically effective amount of phentermine, and an amount of an anticonvulsant agent selected to prevent the loss of effectiveness of the phentermine, wherein the anticonvulsant agent is an anticonvulsant sulfamate derivative having the structure of formula (I) ##STR00014## wherein X is CH.sub.2 or O, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are independently H or C.sub.1-C.sub.4 alkyl, and further wherein when X is O, then R.sub.2 and R.sub.3, and/or R.sub.4 and R.sub.5 may be taken together to form a methylene dioxy linkage of the formula --O--CR.sub.6R.sub.7--O-- in which R.sub.6 and R.sub.7 are independently H or C.sub.1-C.sub.3 alkyl, or may be taken together to form a cyclopentyl or cyclohexyl ring.

59. A method for treating Syndrome X in a subject comprising administering to the subject, on a daily basis and until Syndrome X is effectively treated, a therapeutically effective amount of phentermine, and an amount of an anticonvulsant agent selected to prevent the loss of effectiveness of the phentermine, wherein the anticonvulsant agent is an anticonvulsant sulfamate derivative having the structure of formula (I) ##STR00015## wherein X is CH.sub.2 or O, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are independently H or C.sub.1-C.sub.4 alkyl, and further wherein when X is O, then R.sub.2 and R.sub.3, and/or R.sub.4 and R.sub.5, may be taken together to form a methylene dioxy linkage of the formula --O--CR.sub.6R.sub.7--O-- in which R.sub.6 and R.sub.7 are indevendently H or C.sub.1-C.sub.3 alkyl, or may be taken together to form a cyclopentyl or cyclohexyl ring.
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