Method of hormonal therapy

• US 20030191096A1
• Filed: 10/09/2002
• Published: 10/09/2003
• Est. Priority Date: 04/03/2002
• Status: Abandoned Application

• Current Assignee: Barr Laboratories Incorporated (Teva Pharmaceutical Industries Limited)
• Original Assignee: Barr Laboratories Incorporated (Teva Pharmaceutical Industries Limited)
• Inventors: Leonard, Thomas W., Waldon, R. Forrest
• Application Number:
  US10/268,008
• Publication Number:
  US 20030191096A1
• Time in Patent Office: Days
• US Class Current: 514/170
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids

Abstract

The present invention combines the administration of estrogens with the administration of non-aromatizing androgens to treat frailty in women undergoing estrogen replacement therapy.

Claims

1. A method of treating sexual dysfunction and/or frailty in a woman comprising:

administering a therapeutic amount of a non-aromatizing androgenic compound in a daily dose in an amount of 0.1 to 10 mg of said non-aromatizing androgenic compound equivalent to oral dosages of oxandrolone of about 0.1 to 10 mg.

2. The method according to claim 1, wherein the non-aromatizing androgenic compound is selected from the group consisting of oxandrolone, oxymetholone, stanozolol, stanozolone, danazol and combinations of any of the foregoing.

3. The method according to claim 1, further comprising the administration of a therapeutic amount of an estrogenic compound.

4. The method according to claim 3, wherein the estrogenic compound is selected from the group consisting of estrone, 17α

-estradiol, 17β

-estradiol, equilin, 17α

-dihydroequilin, 17β

-dihydroequilin, equilenin, 17α

-dihydroequilenin, 17β

-dihydroequilenin, Δ

^8,9-dehydroestrone, 17α

Δ

^8,9-dehydroestradiol, 17β

Δ

^8,9-dehydroestradiol, 6-OH equilenin, 6-OH 17α

-dihydroequilenin, ethinyl estradiol, estradiol valerate, 6-OH 17α

-dihydroequilenin, and mixtures, conjugates and salts thereof.

5. The method according to claim 1, further comprising administering a progestin in a daily dose.

6. A method of treating frailty in a woman undergoing estrogen replacement therapy, the method comprising administering to said woman, continuously and uninterruptedly, a therapeutically effective amount of both estrogen and a non-aromatizing androgen in daily dosages, wherein said estrogenic compound is equivalent to oral estradiol dosages of about 0.05 to 3 mg, and said non-aromatizing androgenic compound is equivalent to oral dosages of about 0.1 to 10 mg of an androgenic compound.

7. The method of claim 6, wherein the estrogenic compound is selected from the group consisting of estrone, 17α

-estradiol, 17β

-estradiol, equilin, 17α

-dihydroequilin, 17β

-dihydroequilin, equilenin, 17α

-dihydroequilenin, 17β

-dihydroequilenin, Δ

^8,9-dehydroestrone, 17α

Δ

^8,9-dehydroestradiol, 17β

Δ

^8,9-dehydroestradiol, 6-OH equilenin, 6-OH 17α

-dihydroequilenin, ethinyl estradiol, estradiol valerate, 6-OH 17β

-dihydroequilenin, and mixtures, conjugates and salts thereof.

8. The method according to claim 6, wherein the non-aromatizing androgenic compound is selected from the group consisting of oxandrolone, oxymetholone, stanozolol, stanozolone danazol and combinations of any of the foregoing.

9. The method according to claim 6, further comprising administering a progestin in a daily dose.

10. A method of treating frailty in a woman undergoing estrogen replacement therapy comprising cyclically administering to said woman an estrogenic compound, and continuously and uninterruptedly administering to said woman a non-aromatizing androgenic compound.

11. The method according to claim 10, wherein the estrogenic compound is selected from the group consisting of estrone, 17α

-estradiol, 17β

-estradiol, equilin, 17α

-dihydroequilin, 17β

-dihydroequilin, equilenin, 17α

-dihydroequilenin, 17β

-dihydroequilenin, Δ

^8,9-dehydroestrone, 17α

Δ

^8,9-dehydroestradiol, 17β

Δ

^8,9-dehydroestradiol, 6-OH equilenin, 6-OH 17α

-dihydroequilenin, ethinyl estradiol, estradiol valerate, 6-OH 17β

-dihydroequilenin, and mixtures, conjugates and salts thereof.

12. The method according to claim 10, wherein the non-aromatizing androgenic compound is selected from the group consisting of oxandrolone, oxymetholone, stanozolol, danazol, pharmaceutically acceptable esters and salts thereof, and combinations of any of the foregoing.

13. The method according to claim 10, further comprising administering a progestin in a daily dose.

14. A method of treating weakness in a woman undergoing estrogen replacement therapy comprising continuously and uninterruptedly administering daily dosages of a therapeutically effective amount of an estrogenic compound equivalent to estradiol dosages of about 0.05 to 3 mg, and continuously and uninterruptedly administering to said woman a therapeutically effective amount of a non-aromatizing androgenic compound equivalent to oral dosages of oxandrolone of about 0.1 to 10 mg.

15. The method according to claim 14, wherein the estrogenic compound is selected from the group consisting of estrone, 17α

-estradiol, 17β

-estradiol, equilin, 17α

-dihydroequilin, 17β

-dihydroequilin, equilenin, 17α

-dihydroequilenin, 17β

-dihydroequilenin, Δ

^8,9-dehydroestrone, 17α

Δ

^8,9-dehydroestradiol, 17β

Δ

^8,9-dehydroestradiol, 6-OH equilenin, 6-OH 17α

-dihydroequilenin, ethinyl estradiol, estradiol valerate, 6-OH 17β

-dihydroequilenin, and mixtures, conjugates and salts thereof.

16. The method according to claim 14, wherein the non-aromatizing androgenic compound is selected from the group consisting of oxandrolone, oxymetholone, stanozolol, danazol and combinations of any of the foregoing.

17. The method according to claim 14, further comprising administering a progestin in a daily dose.

18. A method of treating frailty in a woman undergoing estrogen replacement therapy comprising cyclically administering to said woman a non-aromatizing androgenic compound.

19. The method according to claim 18 further comprising continuously and uninterruptedly administering to said woman an estrogenic compound.

20. The method according to claim 18, wherein the non-aromatizing androgenic compound is selected from the group consisting of oxandrolone, oxymetholone, stanozolol, danazol and combinations of any of the foregoing.

21. The method according to claim 20, wherein the estrogenic compound is selected from the group consisting of estrone, 17α

-estradiol, 17β

-estradiol, equilin, 17α

-dihydroequilin, 17β

-dihydroequilin, equilenin, 17α

-dihydroequilenin, 17β

-dihydroequilenin, Δ

^8,9-dehydroestrone, 17α

Δ

^8,9-dehydroestradiol, 17β

Δ

^8,9-dehydroestradiol, 6-OH equilenin, 6-OH 17α

-dihydroequilenin, ethinyl estradiol, estradiol valerate, 6-OH 17β

-dihydroequilenin, and mixtures, conjugates and salts thereof.

22. The method according to claim 18, further comprising administering a progestin in a daily dose.

23. A method of treating frailty in a woman undergoing estrogen replacement therapy comprising continuously and uninterruptedly administering daily dosages of a therapeutically effective amount of an estrogenic compound equivalent to estradiol dosages of about 0.05 to 3 mg, and continuously and uninterruptedly cyclically administering to said woman a therapeutically effective amount of a non-aromatizing androgenic compound equivalent to oral oxandrolone dosages of about 0.1 to 10 mg.

24. The method according to claim 23, wherein the estrogenic compound is selected from the group consisting of estrone, 17α

-estradiol, 17β

-estradiol, equilin, 17α

-dihydroequilin, 17β

-dihydroequilin, equilenin, 17α

-dihydroequilenin, 17β

-dihydroequilenin, Δ

^8,9-dehydroestrone, 17α

Δ

^8,9-dehydroestradiol, 17β

Δ

^8,9-dehydroestradiol, 6-OH equilenin, 6-OH 17α

-dihydroequilenin, ethinyl estradiol, estradiol valerate, 6-OH 17β

-dihydroequilenin, and mixtures, conjugates and salts thereof.

25. The method according to claim 23, wherein the non-aromatizing androgenic compound is selected from the group consisting of oxandrolone, oxymetholone, stanozolol, danazol and combinations of any of the foregoing.

26. The method according to claim 23, further comprising administering a progestin in a daily dose.

27. The method according to claim 23, wherein said frailty is selected from the group of muscle tone, balance and bone strength.

28. A method of treating sexual dysfunction and/or frailty in a woman comprising:

administering a therapeutic amount of an androgenic compound in a daily dose in an amount of 0.1 to 10 mg of said androgenic compound, wherein said androgenic compound comprises at least 50% of a non-aromatizing androgenic compound.

29. The method according to claim 28, wherein the non-aromatizing androgenic compound is selected from the group consisting of oxandrolone, oxymetholone, stanozolol, stanozolone, danazol and combinations of any of the foregoing.

30. The method according to claim 28, further comprising the administration of a therapeutic amount of an estrogenic compound.

31. The method according to claim 30, wherein the estrogenic compound is selected from the group consisting of estrone, 17α

-estradiol, 17β

-estradiol, equilin, 17α

-dihydroequilin, 17β

-dihydroequilin, equilenin, 17α

-dihydroequilenin, 17β

-dihydroequilenin, Δ

^8,9-dehydroestrone, 17α

Δ

^8,9-dehydroestradiol, 17β

Δ

^8,9-dehydroestradiol, 6-OH equilenin, 6-OH 17α

-dihydroequilenin, ethinyl estradiol, estradiol valerate, 6-OH 17α

-dihydroequilenin, and mixtures, conjugates and salts thereof.

32. The method according to claim 28, further comprising administering a progestin in a daily dose.

33. A method of treating sexual dysfunction and/or frailty in a woman comprising:

administering a therapeutic amount of a non-aromatizing androgenic compound in a dosing cycle in an amount of 0.1 to 10 mg of said non-aromatizing androgenic compound equivalent to oral dosages of oxandrolone of about 0.1 to 10 mg.

34. The method according to claim 33, wherein the non-aromatizing androgenic compound is selected from the group consisting of oxandrolone, oxymetholone, stanozolol, stanozolone, danazol and combinations of any of the foregoing.

35. The method according to claim 33, further comprising the administration of a therapeutic amount of an estrogenic compound.

36. The method according to claim 33, wherein the estrogenic compound is selected from the group consisting of estrone, 17α

-estradiol, 17β

-estradiol, equilin, 17α

-dihydroequilin, 17β

-dihydroequilin, equilenin, 17α

-dihydroequilenin, 17β

-dihydroequilenin, Δ

^8,9-dehydroestrone, 17α

Δ

^8,9-dehydroestradiol, 17β

Δ

^8,9-dehydroestradiol, 6-OH equilenin, 6-OH 17α

-dihydroequilenin, ethinyl estradiol, estradiol valerate, 6-OH 17α

-dihydroequilenin, and mixtures, conjugates and salts thereof.

37. The method according to claim 33, further comprising administering a progestin in dosing cycle.

38. The method according to claim 33, wherein the non-aromatizing compound is administered daily.

39. The method according to claim 33, wherein the non-aromatizing compound is administered every other day.

40. The method according to claim 33, wherein the non-aromatizing compound is administered every third day.

41. The method according to claim 33, wherein the non-aromatizing compound is administered once a week.