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- Nachgewiesen in: USPTO Patent Applications
- Sprachen: English
- Document Number: 20190231743
- Publication Date: August 1, 2019
- Appl. No: 16/341027
- Application Filed: October 10, 2017
- Claim: 1. A method of treating vulvovaginal atrophy (VVA) in women who have previously been diagnosed with primary or metastatic breast cancer, comprising: a) selecting for treatment a patient with VVA who has previously been diagnosed with either i) estrogen receptor positive (ER+) breast cancer or ii) estrogen receptor negative (ER−) breast cancer; and b) administering to the selected patient lasofoxifene, a pharmaceutically acceptable salt thereof, or a prodrug thereof, in an amount effective to treat VVA.
- Claim: 2. The method of claim 1, wherein lasofoxifene is administered as lasofoxifene tartrate.
- Claim: 3. The method of claim 1 or 2, wherein lasofoxifene is administered by oral, intravenous, transdermal, vaginal topical, or vaginal ring administration.
- Claim: 4. The method of claim 3, wherein lasofoxifene is administered by oral administration.
- Claim: 5. The method of claim 4, wherein lasofoxifene is administered at about 0.5 mg/day per os to about 10 mg/day per os.
- Claim: 6. The method of claim 3, wherein lasofoxifene is administered by vaginal topical administration.
- Claim: 7. The method of claim 3, wherein lasofoxifene is administered by vaginal ring administration.
- Claim: 8. The method of any one of claims 1 to 7, wherein lasofoxifene is administered once every day, once every two days, once every three days, once every four days, once every five days, once every six days, once every week, once every two weeks, once every three weeks, or once every month.
- Claim: 9. The method of any one of claims 1 to 8, further comprising treating said patient with at least one additional endocrine therapy.
- Claim: 10. The method of claim 9, wherein the additional endocrine therapy is treatment with a second selective ER modulator (SERM).
- Claim: 11. The method of claim 9, wherein the additional endocrine therapy is treatment with a selective ER degrader (SERD).
- Claim: 12. The method of claim 9, wherein the additional endocrine therapy is treatment with an aromatase inhibitor.
- Claim: 13. The method of any one of claims 1 to 8, further comprising administering to said patient an effective amount of cyclin-dependent kinase 4/6 (CDK4/6) inhibitor.
- Claim: 14. The method of claim 13, wherein said CDK4/6 inhibitor is palbociclib, abemaciclib, or ribociclib.
- Claim: 15. The method of any one of claims 1 to 8, further comprising administering to said patient an effective amount of mammalian target of rapamycin (mTOR) inhibitor, phosphoinositide 3-kinase (PI3K) inhibitor, or heat shock protein 90 (HSP90) inhibitor.
- Claim: 16. The method of any one of claims 1 to 8, further comprising administering to said patient an effective amount of human epidermal growth factor receptor 2 (HER2) inhibitor.
- Claim: 17. The method of claim 16, wherein said HER2 inhibitor is trastuzumab (Herceptin®) or ado-trastuzumab emtansine (Kadcyla®).
- Claim: 18. The method of any one of claims 1 to 8, further comprising administering to said patient an effective amount of a checkpoint inhibitor.
- Claim: 19. The method of claim 18, wherein said checkpoint inhibitor is an antibody specific for programmed cell death protein 1 (PD-1), programmed death-ligand 1 (PD-L1), or cytotoxic T-lymphocyte-associated protein 4 (CTLA-4).
- Claim: 20. The method of claim 19, wherein said PD-1 antibody is pembrolizumab (Keytruda®) or nivolumab (Opdivo®).
- Claim: 21. The method of claim 19, wherein said CTLA-4 antibody is ipilimumab (Yervoy®).
- Claim: 22. The method of any one of claims 1 to 8, further comprising administering to said patient an effective amount of cancer vaccine.
- Claim: 23. The method of any one of claims 1 to 22, comprising administering an amount of lasofoxifene sufficient to decrease vaginal pH, increase vaginal lubrication, and/or improve vaginal cell maturation index in women who are concurrently being treated with one or more drugs causing or predisposing to VVA.
- Claim: 24. The method of any one of claims 1 to 23, comprising administering an amount of lasofoxifene sufficient to reduce one or more symptoms of sexual dysfunction in women who are concurrently being treated with one or more drugs causing or predisposing to sexual dysfunction.
- Claim: 25. The method of any one of claims 1 to 24, comprising administering an amount of lasofoxifene sufficient to reduce one or more symptoms of hot flashes in women who are concurrently being treated with one or more drugs causing or predisposing to hot flashes.
- Claim: 26. The method of any one of claims 1 to 25, comprising administering an amount of lasofoxifene sufficient to reduce recurrence of breast cancer, increase time to recurrence of breast cancer, reduce metastasis of breast cancer to bone, and/or increase duration of breast cancer progression-free survival.
- Claim: 27. The method of any one of claims 1 to 26, comprising administering an amount of lasofoxifene sufficient to increase one or more quality of life measures selected from: joint ache, urogenital symptoms, bone loss, and bone fractures.
- Claim: 28. The method of any one of claims 1 to 27, wherein the patient's breast cancer is in remission.
- Claim: 29. A method of treating vulvovaginal atrophy (VVA) in women who have previously been diagnosed with a malignancy other than breast cancer, comprising: a) selecting for treatment a patient with VVA who has previously been diagnosed with either i) estrogen receptor positive (ER+) malignancy other than breast cancer or ii) estrogen receptor negative (ER−) malignancy other than breast cancer; and b) administering to the selected patient lasofoxifene, a pharmaceutically acceptable salt thereof, or a prodrug thereof, in an amount effective to treat VVA.
- Claim: 30. The method of claim 29, wherein lasofoxifene is administered as lasofoxifene tartrate.
- Claim: 31. The method of claim 29 or 30, wherein lasofoxifene is administered by oral, intravenous, transdermal, vaginal topical, or vaginal ring administration.
- Claim: 32. The method of claim 31, wherein lasofoxifene is administered by oral administration
- Claim: 33. The method of claim 32, wherein lasofoxifene is administered at about 0.5 mg/day per os to about 10 mg/day per os.
- Claim: 34. The method of claim 31, wherein lasofoxifene is administered by vaginal topical administration.
- Claim: 35. The method of claim 31, wherein lasofoxifene is administered by vaginal ring administration.
- Claim: 36. The method of any one of claims 29 to 35, wherein lasofoxifene is administered once every day, once every two days, once every three days, once every four days, once every five days, once every six days, once every week, once every two weeks, once every three weeks, or once every month.
- Claim: 37. The method of any one of claims 29 to 36, further comprising treating said patient with at least one additional endocrine therapy.
- Claim: 38. The method of claim 37, wherein the additional endocrine therapy is treatment with a second selective ER modulator (SERM).
- Claim: 39. The method of claim 37, wherein the additional endocrine therapy is treatment with a selective ER degrader (SERD).
- Claim: 40. The method of claim 37, wherein the additional endocrine therapy is treatment with an aromatase inhibitor.
- Claim: 41. The method of any one of claims 29 to 36, further comprising administering to said patient an effective amount of cyclin-dependent kinase 4/6 (CDK4/6) inhibitor.
- Claim: 42. The method of claim 41, wherein said CDK4/6 inhibitor is palbociclib, abemaciclib, or ribociclib.
- Claim: 43. The method of any one of claims 29 to 36, further comprising administering to said patient an effective amount of mammalian target of rapamycin (mTOR) inhibitor, phosphoinositide 3-kinase (PI3K) inhibitor, or heat shock protein 90 (HSP90) inhibitor.
- Claim: 44. The method of any one of claims 29 to 36, further comprising administering to said patient an effective amount of human epidermal growth factor receptor 2 (HER2) inhibitor.
- Claim: 45. The method of claim 44, wherein said HER2 inhibitor is trastuzumab (Herceptin®) or ado-trastuzumab emtansine (Kadcyla®).
- Claim: 46. The method of any one of claims 29 to 36, further comprising administering to said patient an effective amount of a checkpoint inhibitor.
- Claim: 47. The method of claim 46, wherein said checkpoint inhibitor is an antibody specific for programmed cell death protein 1 (PD-1), programmed death-ligand 1 (PD-L1), or cytotoxic T-lymphocyte-associated protein 4 (CTLA-4).
- Claim: 48. The method of claim 47, wherein said PD-1 antibody is pembrolizumab (Keytruda®) or nivolumab (Opdivo®).
- Claim: 49. The method of claim 47, wherein said CTLA-4 antibody is ipilimumab (Yervoy®).
- Claim: 50. The method of any one of claims 29 to 36, further comprising administering to said patient an effective amount of cancer vaccine.
- Claim: 51. The method of any one of claims 29 to 50, comprising administering an amount of lasofoxifene sufficient to decrease vaginal pH, increase vaginal lubrication, and/or improve vaginal cell maturation index in women who are concurrently being treated with one or more drugs causing or predisposing to VVA.
- Claim: 52. The method of any one of claims 29 to 51, comprising administering an amount of lasofoxifene sufficient to reduce one or more symptoms of sexual dysfunction in women who are concurrently being treated with one or more drugs causing or predisposing to sexual dysfunction.
- Claim: 53. The method of any one of claims 29 to 52, comprising administering an amount of lasofoxifene sufficient to reduce one or more symptoms of hot flashes in women who are concurrently being treated with one or more drugs causing or predisposing to hot flashes.
- Claim: 54. The method of any one of claims 29 to 53, comprising administering an amount of lasofoxifene sufficient to reduce cancer recurrence, increase time to cancer recurrence, reduce metastasis of cancer to bone, and/or increase duration of cancer progression-free survival.
- Claim: 55. The method of any one of claims 29 to 54, comprising administering an amount of lasofoxifene sufficient to increase one or more quality of life measures selected from: joint ache, urogenital symptoms, bone loss, and bone fractures.
- Claim: 56. The method of any one of claims 29 to 55, wherein the patient's malignancy is in remission.
- Claim: 57. A method of treating osteoporosis in women who have previously been diagnosed with primary or metastatic breast cancer, comprising: a) selecting for treatment a patient with osteoporosis who has previously been diagnosed with either i) estrogen receptor positive (ER+) breast cancer or ii) estrogen receptor negative (ER−) breast cancer; and b) administering to the selected patient lasofoxifene, a pharmaceutically acceptable salt thereof, or a prodrug thereof, in an amount effective to treat osteoporosis.
- Claim: 58. The method of claim 57, wherein lasofoxifene is administered as lasofoxifene tartrate.
- Claim: 59. The method of claim 57 or 58, wherein lasofoxifene is administered by oral, intravenous, transdermal, vaginal topical, or vaginal ring administration.
- Claim: 60. The method of claim 59, wherein lasofoxifene is administered by oral administration.
- Claim: 61. The method of claim 60, wherein lasofoxifene is administered at about 0.5 mg/day per os to about 10 mg/day per os.
- Claim: 62. The method of any one of claims 57 to 61, wherein lasofoxifene is administered once every day, once every two days, once every three days, once every four days, once every five days, once every six days, once every week, once every two weeks, once every three weeks, or once every month.
- Claim: 63. The method of any one of claims 57 to 62, further comprising treating said patient with at least one additional endocrine therapy.
- Claim: 64. The method of claim 63, wherein the additional endocrine therapy is treatment with a second selective ER modulator (SERM).
- Claim: 65. The method of claim 63, wherein the additional endocrine therapy is treatment with a selective ER degrader (SERD).
- Claim: 66. The method of claim 63, wherein the additional endocrine therapy is treatment with an aromatase inhibitor.
- Claim: 67. The method of any one of claims 57 to 62, further comprising administering to said patient an effective amount of cyclin-dependent kinase 4/6 (CDK4/6) inhibitor.
- Claim: 68. The method of claim 67, wherein said CDK4/6 inhibitor is palbociclib, abemaciclib, or ribociclib.
- Claim: 69. The method of any one of claims 57 to 62, further comprising administering to said patient an effective amount of mammalian target of rapamycin (mTOR) inhibitor, phosphoinositide 3-kinase (PI3K) inhibitor, or heat shock protein 90 (HSP90) inhibitor.
- Claim: 70. The method of any one of claims 57 to 62, further comprising administering to said patient an effective amount of human epidermal growth factor receptor 2 (HER2) inhibitor.
- Claim: 71. The method of claim 70, wherein said HER2 inhibitor is trastuzumab (Herceptin®) or ado-trastuzumab emtansine (Kadcyla®).
- Claim: 72. The method of any one of claims 57 to 62, further comprising administering to said patient an effective amount of a checkpoint inhibitor.
- Claim: 73. The method of claim 72, wherein said checkpoint inhibitor is an antibody specific for programmed cell death protein 1 (PD-1), programmed death-ligand 1 (PD-L1), or cytotoxic T-lymphocyte-associated protein 4 (CTLA-4).
- Claim: 74. The method of claim 73, wherein said PD-1 antibody is pembrolizumab (Keytruda®) or nivolumab (Opdivo®).
- Claim: 75. The method of claim 73, wherein said CTLA-4 antibody is ipilimumab (Yervoy®).
- Claim: 76. The method of any one of claims 57 to 62, further comprising administering to said patient an effective amount of cancer vaccine.
- Claim: 77. The method of any one of claims 57 to 62, further comprising administering to said patient an effective amount of bisphosphonate.
- Claim: 78. The method of claim 77, wherein said bisphosphonate is selected from etidronate (Didronel®), clodronate (Bonefos®, Loron®), tiludronate (Skelid®), pamidronate (Aredia®), neridronate (Nerixia®), olpadronate, alendronate (Fosamax®), ibandronate (Boniva®), risedronate (Actonel®, Atelvia®), and zoledronate (Zometa®, Aclasta®).
- Claim: 79. The method of any one of claims 57 to 62, further comprising administering to said patient an effective amount of receptor activator of nuclear factor kappa-B ligand (RANKL) inhibitor.
- Claim: 80. The method of claim 79, wherein said RANKL inhibitor is denosumab (Prolia®, Xgeva®).
- Claim: 81. The method of any one of claims 57 to 62, further comprising administering to said patient an effective amount of calcitonin (Miacalcin®, Fortical®).
- Claim: 82. The method of any one of claims 57 to 81, comprising administering an amount of lasofoxifene sufficient to prevent fractures and bone loss in women who are concurrently being treated with one or more drugs causing or predisposing to osteoporosis.
- Claim: 83. The method of any one of claims 57 to 82, comprising administering an amount of lasofoxifene sufficient to reduce recurrence of breast cancer, increase time to recurrence of breast cancer, reduce metastasis of breast cancer to bone, and/or increase duration of breast cancer progression-free survival.
- Claim: 84. The method of any one of claims 57 to 83, comprising administering an amount of lasofoxifene sufficient to increase one or more quality of life measures selected from: joint ache, urogenital symptoms, bone loss, and bone fractures.
- Claim: 85. The method of any one of claims 57 to 84, wherein the patient's breast cancer is in remission.
- Claim: 86. A method of treating osteoporosis in women who have previously been diagnosed with a malignancy other than breast cancer, comprising: a) selecting for treatment a patient with osteoporosis who has previously been diagnosed with either i) estrogen receptor positive (ER+) malignancy other than breast cancer or ii) estrogen receptor negative (ER−) malignancy other than breast cancer; and b) administering to the selected patient lasofoxifene, a pharmaceutically acceptable salt thereof, or a prodrug thereof, in an amount effective to treat osteoporosis.
- Claim: 87. The method of claim 86, wherein lasofoxifene is administered as lasofoxifene tartrate.
- Claim: 88. The method of claim 86 or 87, wherein lasofoxifene is administered by oral, intravenous, transdermal, vaginal topical, or vaginal ring administration.
- Claim: 89. The method of claim 88, wherein lasofoxifene is administered by oral administration.
- Claim: 90. The method of claim 89, wherein lasofoxifene is administered at about 0.5 mg/day per os to about 10 mg/day per os.
- Claim: 91. The method of any one of claims 86 to 90, wherein lasofoxifene is administered once every day, once every two days, once every three days, once every four days, once every five days, once every six days, once every week, once every two weeks, once every three weeks, or once every month.
- Claim: 92. The method of any one of claims 86 to 91, further comprising treating said patient with at least one additional endocrine therapy.
- Claim: 93. The method of claim 92, wherein the additional endocrine therapy is treatment with a second selective ER modulator (SERM).
- Claim: 94. The method of claim 92, wherein the additional endocrine therapy is treatment with a selective ER degrader (SERD).
- Claim: 95. The method of claim 92, wherein the additional endocrine therapy is treatment with an aromatase inhibitor.
- Claim: 96. The method of any one of claims 86 to 91, further comprising administering to said patient an effective amount of cyclin-dependent kinase 4/6 (CDK4/6) inhibitor.
- Claim: 97. The method of claim 96, wherein said CDK4/6 inhibitor is palbociclib, abemaciclib, or ribociclib.
- Claim: 98. The method of any one of claims 86 to 91, further comprising administering to said patient an effective amount of mammalian target of rapamycin (mTOR) inhibitor, phosphoinositide 3-kinase (PI3K) inhibitor, or heat shock protein 90 (HSP90) inhibitor.
- Claim: 99. The method of any one of claims 86 to 91, further comprising administering to said patient an effective amount of human epidermal growth factor receptor 2 (HER2) inhibitor.
- Claim: 100. The method of claim 99, wherein said HER2 inhibitor is trastuzumab (Herceptin®) or ado-trastuzumab emtansine (Kadcyla®).
- Claim: 101. The method of any one of claims 86 to 91, further comprising administering to said patient an effective amount of a checkpoint inhibitor.
- Claim: 102. The method of claim 101, wherein said checkpoint inhibitor is an antibody specific for programmed cell death protein 1 (PD-1), programmed death-ligand 1 (PD-L1), or cytotoxic T-lymphocyte-associated protein 4 (CTLA-4).
- Claim: 103. The method of claim 102, wherein said PD-1 antibody is pembrolizumab (Keytruda®) or nivolumab (Opdivo®).
- Claim: 104. The method of claim 102, wherein said CTLA-4 antibody is ipilimumab (Yervoy®).
- Claim: 105. The method of any one of claims 86 to 91, further comprising administering to said patient an effective amount of cancer vaccine.
- Claim: 106. The method of any one of claims 86 to 91, further comprising administering to said patient an effective amount of bisphosphonate.
- Claim: 107. The method of claim 106, wherein said bisphosphonate is selected from etidronate (Didronel®), clodronate (Bonefos®, Loron®), tiludronate (Skelid®), pamidronate (Aredia®), neridronate (Nerixia®), olpadronate, alendronate (Fosamax®), ibandronate (Boniva®), risedronate (Actonel®, Atelvia®), and zoledronate (Zometa®, Aclasta®).
- Claim: 108. The method of any one of claims 86 to 91, further comprising administering to said patient an effective amount of receptor activator of nuclear factor kappa-B ligand (RANKL) inhibitor.
- Claim: 109. The method of claim 108, wherein said RANKL inhibitor is denosumab (Prolia®, Xgeva®).
- Claim: 110. The method of any one of claims 86 to 91, further comprising administering to said patient an effective amount of calcitonin (Miacalcin®, Fortical®).
- Claim: 111. The method of any one of claims 86 to 110, comprising administering an amount of lasofoxifene sufficient to prevent fractures and bone loss in women who are concurrently being treated with one or more drugs causing or predisposing to osteoporosis.
- Claim: 112. The method of any one of claims 86 to 111, comprising administering an amount of lasofoxifene sufficient to reduce cancer recurrence, increase time to cancer recurrence, reduce metastasis of cancer to bone, and/or increase duration of cancer progression-free survival.
- Claim: 113. The method of any one of claims 86 to 112, comprising administering an amount of lasofoxifene sufficient to increase one or more quality of life measures selected from: joint ache, urogenital symptoms, bone loss, and bone fractures.
- Claim: 114. The method of any one of claims 86 to 113, wherein the patient's malignancy is in remission.
- Current International Class: 61; 61; 61; 61; 07; 07; 61; 61
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