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Details for Patent: 5,066,478

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Details for Patent: 5,066,478

Title: Radio labeled organic amine phosphonic acid complexes for the treatment of calcific tumors
Abstract:Particle-emitting radionuclides, e.g. Gd-159, Ho-166, Lu-177 and Yb-175, have been complexed with organic aminoalkylenephosphonic acids wherein the nitrogen and phosphorus are interconnected by an alkylene group or substituted alkylene group. These complexes have been found useful in compositions for the therapeutic treatment of calcific tumors in animals and in relief of bone pain.
Inventor(s): Simon; Jaime (Angleton, TX), Wilson; David A. (Richwood, TX), Volkert; Wynn A. (Columbia, MO), Troutner; David E. (Columbia, MO), Goeckeler; William F. (Midland, MI)
Assignee: The Dow Chemical Company (Midland, MI)
Filing Date:Jan 30, 1990
Application Number:07/472,506
Claims:1. A therapeutically effective composition comprising an aminophosphonic acid which is ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and at least one radionuclide selected from Gd-159, Ho-166, Lu-177 and Yb-175.

2. The composition of claim 1 wherein the radionuclide is Gd-159.

3. The composition of claim 1 wherein the radionuclide is Yb-175.

4. The composition of claim 1 wherein the radionuclide is Lu-177.

5. The composition of claim 1 wherein the radionuclide is Ho-166.

6. A therapeutically effective composition comprising an aminophosphonic acid which is hydroxyethylethylenediaminetrimethylenephosphonic acid or a physiologically acceptable salt thereof and at least one radionuclide selected from Gd-159, Ho-166, Lu-177 and Yb-175.

7. The composition of claim 6 wherein the radionuclide is Gd-159.

8. The composition of claim 6 wherein the radionuclide is Yb-175.

9. The composition of claim 6 wherein the radionuclide is Lu-177.

10. The composition of claim 6 wherein the radionuclide is Ho-166.

11. A therapeutically effective composition comprising an aminophosphonic acid which is diethylenetriaminepentamethylenephosphonic acid or a physiologically acceptable salt thereof and the radionuclide Yb-175.

12. A therapeutically effective composition comprising an aminophosphonic acid which is nitrilotrimethylenephosphonic acid or a physiologically acceptable salt thereof and the radionuclide Yb-175.

13. A therapeutically effective composition comprising Yb-175 and at least one of nitrilotrimethylenephosphonic acid, ethylenediaminetetramethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid, and diethylenetriaminepentamethylenephosphonic acid, or a physiologically acceptable salt thereof.

14. A therapeutically effective composition comprising Ho-166 and at least one of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid or a physiologically acceptable salt thereof.

15. A therapeutically effective composition comprising Lu-177 and at least one of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid or a physiologically acceptable salt thereof.

16. A therapeutically effective composition comprising Gd-159 and at least one of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid or a physiologically acceptable salt thereof.

17. A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of at least one composition comprising an aminophosphonic acid which is ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and at least one radionuclide selected from Gd-159, Ho-166, Lu-177 and Yb-175.

18. The method of claim 17 wherein the radionuclide is Gd-159.

19. The method of claim 17 wherein the radionuclide is Yb-175.

20. The method of claim 17 wherein the radionuclide is Lu-177.

21. The method of claim 17 wherein the radionuclide is Ho-166.

22. A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of at least one composition comprising an aminophosphonic acid which is diethylenetriaminepentamethylenephosphonic acid or a physiologically acceptable salt thereof and the radionuclide Yb-175.

23. A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of at least one composition comprising an aminophosphonic acid which is nitrilotrimethylenephosphonic acid or a physiologically acceptable salt thereof and the radionuclide is Yb-175.

24. A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising Yb-175 and at least one of nitrilotrimethylenephosphonic acid-, ethylenediaminetetramethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid, and diethylenetriaminepentamethylenephosphonic acid, or a physiologically acceptable salt thereof.

25. A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising Ho-166 and at least one of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid or a physiologically acceptable salt thereof.

26. A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising Lu-177 and at least one of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid or a physiologically acceptable salt thereof.

27. A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising Gd-159 and at least one of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid or a physiologically acceptable salt thereof.

28. A composition comprising 1) a complex which comprises at least one radionuclide selected from Gd-159, Ho-166, Lu-177 and Yb-175 and at least one of aminophosphonic acid, or a physiologically acceptable salt thereof, wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid and nitrilotrimethylenephosphonic acid, and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex, and wherein the resulting composition is therapeutically effective.

29. The composition of claim 28 wherein a physiologically acceptable liquid carrier is present.

30. The composition of claim 29 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

31. The composition of claim 28 wherein the radionuclide is Gd-159.

32. The composition of claim 31 wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid, or a physiologically acceptable salt thereof.

33. The composition of claim 28 wherein the radionuclide is Ho-166.

34. The composition of claim 33 wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid, or a physiologically acceptable salt thereof.

35. The composition of claim 28 wherein the radionuclide is Lu-177.

36. The composition of claim 35 wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid, or a physiologically acceptable salt thereof.

37. The composition of claim 28 wherein the radionuclide is Yb-175.

38. A sterile composition suitable for administration to a mammal comprising 1) a complex which comprises at least one radionuclide selected from Gd-159, Ho-166, Lu-177 and Yb-175 and at least one of an aminophosphonic acid, or a physiologically acceptable salt thereof, wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid and nitrilotrimethylenephosphonic acid and nitrilotrimethylenephosphonic acid, and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex, and wherein the resulting composition is therapeutically effective and wherein the radionuclide in dosage form is present in an amount containing at least 0.02 mCi per kilogram of body weight of said mammal.

39. The composition of claim 38 wherein a physiologically acceptable liquid carrier is present.

40. The composition of claim 39 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

41. The composition of claim 38 wherein the radionuclide is Gd-159.

42. The composition of claim 41 wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid, or a physiologically acceptable salt thereof.

43. The composition of claim 38 wherein the radionuclide is Ho-166.

44. The composition of claim 43 wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid, or a physiologically acceptable salt thereof.

45. The composition of claim 38 wherein the radionuclide is Lu-177.

46. The composition of claim 45 wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid, or a physiologically acceptable salt thereof.

47. The composition of claim 38 wherein the radionuclide is Yb-175.

48. A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising 1) a complex which comprises at least one radionuclide selected from Gd-159, Ho-166, Lu-177 and Yb-175 and at least one of an aminophosphonic acid, or a physiologically acceptable salt thereof, wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid and nitrilotrimethylenephosphonic acid, and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

49. The method of claim 48 wherein the animal is a human.

50. The method of claim 48 wherein a physiologically acceptable liquid carrier is present.

51. The method of claim 50 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

52. A method of claim 48 wherein the complex comprises as the radionuclide Gd-159 and as the aminophosphonic acid, or a physiologically acceptable salt thereof, an aminophosphonic acid selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

53. The method of claim 52 wherein the animal is a human.

54. The method of claim 52 wherein a physiologically acceptable liquid carrier is present.

55. The method of claim 54 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

56. A method of claim 48 wherein the complex comprises as the radionuclide Ho-166 and as the aminophosphonic acid, or a physiologically acceptable salt thereof, an aminophosphonic acid selected from the grouping consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

57. The method of claim 56 wherein the animal is a human.

58. The method of claim 56 wherein a physiologically acceptable liquid carrier is present.

59. The method of claim 58 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

60. A method of claim 48 wherein the complex comprises as the radionuclide Lu-177 and as the aminophosphonic acid, or a physiologically acceptable salt thereof, an aminophosphonic acid selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

61. The method of claim 60 wherein the animal is a human.

62. The method of claim 60 wherein a physiologically acceptable liquid carrier is present.

63. The method of claim 62 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

64. A method of claim 48 wherein the complex comprises as the radionuclide Yb-175 and as the aminophosphonic acid, or a physiologically acceptable salt thereof, an aminophosphonic acid selected from the group consisting of diethylenetriaminepentamethylenephosphonic acid, nitrilotrimethylenephosphonic acid, ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

65. The method of claim 64 wherein the animal is a human.

66. The method of claim 64 wherein a physiologically acceptable liquid carrier is present.

67. The method of claim 66 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

68. A method for the therapeutic treatment of an animal having bone pain which comprises administering to said animal a therapeutically effective amount of a composition comprising 1) a complex which comprises at least one radionuclide selected from Gd-159, Ho-166, Lu-17 and Yb-175 and at least one of an aminophosphonic acid, or a physiologically acceptable salt thereof, wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid and nitrilotrimethylenephosphonic acid, and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

69. The method of claim 68 wherein the animal is a human.

70. The method of claim 68 wherein a physiologically acceptable liquid carrier is present.

71. The method of claim 70 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

72. A method of claim 68 wherein the complex comprises as the radionuclide Gd-159 and as the aminophosphonic acid, or a physiologically acceptable salt thereof, an aminophosphonic acid selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

73. The method of claim 72 wherein the animal is a human.

74. The method of claim 72 wherein a physiologically acceptable liquid carrier is present.

75. The method of claim 74 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

76. A method of claim 68 wherein the complex comprises as the radionuclide Ho-166 and as the aminophosphonic acid, or a physiologically acceptable salt thereof, an aminophosphonic acid selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

77. The method of claim 76 wherein the animal is a human.

78. The method of claim 76 wherein a physiologically acceptable liquid carrier is present.

79. The method of claim 78 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

80. A method of claim 68 wherein the complex comprises as the radionuclide Lu-177 and as the aminophosphonic acid, or a physiologically acceptable salt thereof, an aminophosphonic acid selected from the group consisting of ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

81. The method of claim 81 wherein the animal is a human.

82. The method of claim 81 wherein a physiologically acceptable liquid carrier is present.

83. The method of claim 82 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.

84. A method of claim 68 wherein the complex comprises as the radionuclide Yb-175 and as the aminophosphonic acid, or a physiologically acceptable salt thereof, an aminophosphonic acid selected from the group consisting of diethylenetriaminepentamethylenephosphonic acid, nitrilotrimethylenephosphonic acid, ethylenediaminetetramethylenephosphonic acid and hydroxyethylethylenediaminetrimethylenephosphonic acid and 2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.

85. The method of claim 84 wherein the animal is a human.

86. The method of claim 84 wherein a physiologically acceptable liquid carrier is present.

87. The method of claim 86 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
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