CA2649893A1 - Lower dosage strength imiquimod formulations and short dosing regimens for treating actinic keratosis - Google Patents
Lower dosage strength imiquimod formulations and short dosing regimens for treating actinic keratosis Download PDFInfo
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- CA2649893A1 CA2649893A1 CA002649893A CA2649893A CA2649893A1 CA 2649893 A1 CA2649893 A1 CA 2649893A1 CA 002649893 A CA002649893 A CA 002649893A CA 2649893 A CA2649893 A CA 2649893A CA 2649893 A1 CA2649893 A1 CA 2649893A1
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Abstract
Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H--imidazo [4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration ("FDA"), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration ("FDA") for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described.
Claims (84)
1. Use of a topical composition comprising imiquimod in an amount of from about 1% to about 4.25% by weight, together with a pharmaceutically acceptable vehicle therefor, for the treatment of an area afflicted with actinic keratosis, the use comprising:
(i) application of the composition to the area once a day for up to three weeks to complete a first cycle, (ii) resting for up to three weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for up to three weeks to complete a second cycle.
(i) application of the composition to the area once a day for up to three weeks to complete a first cycle, (ii) resting for up to three weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for up to three weeks to complete a second cycle.
2. Use of imiquimod to manufacture a topical composition comprising imiquimod in an amount of from about 1% to about 4.25% by weight, together with a pharmaceutically acceptable vehicle therefor, for the treatment of an area afflicted actinic keratosis, the composition being formulated for administration of imiquimod by: (i) application of the composition to a treatment area once a day for up to three weeks to complete a first cycle, (ii) resting for up to three weeks during which the composition is not applied, and (iii) application of the composition to a treatment area once a day for up to three weeks to complete a second cycle.
3. The use defined in any one of Claims 1-2, wherein the topical composition comprises an amount of imiquimod selected from about 1.5%, 1.75%, 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75%, 4.0% and 4.25% by weight.
4. The use defined in any one of Claims 1-2, wherein the topical composition comprises an amount of imiquimod selected from about 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75% and 4.0% by weight.
5. The use defined in any one of Claims 1-2, wherein the topical composition comprises an amount of imiquimod selected from about 2.5%, 2.75%, 3.0%, 3.25%, 3.5% and 3.75% by weight.
6. The use defined in any one of Claims 1-2, wherein the topical composition comprises imiquimod in an amount of 2.5% by weight.
7. The use defined in any one of Claims 1-2, wherein the topical composition comprises imiquimod in an amount of 3.75% by weight.
8. The use defined in Claim 6, wherein the use comprises application of a daily dose of up to 12.5 mg imiquimod during the first cycle.
9. The use defined in Claim 6, wherein the use comprises application of a daily dose of up to 12.5 mg imiquimod during the second cycle.
10. The use defined in Claim 6, wherein the use comprises application of a daily dose of up to 12.5 mg imiquimod during the first cycle and the second cycle.
11. The use defined in Claim 7, wherein the use comprises application of a daily dose of up to 18.75 mg imiquimod during the first cycle.
12. The use defined in Claim 7, wherein the use comprises application of a daily dose of up to 18.75 mg imiquimod during the second cycle.
13. The use defined in Claim 7, wherein the use comprises application of a daily dose of up to 18.75 mg imiquimod during the first cycle and the second cycle.
14. The use defined in any one of Claims 1-13, wherein the pharmaceutically acceptable vehicle comprises a fatty acid.
15. The use defined in Claim 14, wherein the fatty acid is selected from the group consisting of isostearic acid, palmitic acid, stearic acid, linoleic acid, unrefined oleic acid, refined oleic acid and combinations thereof.
16. The use defined in any one of Claims 14-15, wherein the topical formulation is in the form of a cream.
17. The use defined in Claim 16, wherein the fatty acid is present in an amount of from about 3 percent to about 45 percent by weight of the topical composition.
18. The use defined in Claim 16, wherein the fatty acid is present in an amount of from about 5 percent to about 30 percent by weight of the topical composition.
19. The use defined in Claim 16, wherein the fatty acid is present in an amount of from about 5 percent to about 25 percent by weight of the topical composition.
20. The use defined in any one of Claims 16-19, wherein the topical composition further comprises at least one of an emollient, an emulsifier, a thickener, a preservative, a solubilizing agent, a humectant, a skin penetration enhancer and combinations thereof.
21. The use defined in any one of Claims 1-20, wherein the use comprises: (i) application of the composition to the area once a day for three weeks to complete a first cycle, (ii) resting for three weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for three weeks to complete a second cycle.
22. The use defined in any one of Claims 1-20, wherein the use comprises: (i) application of the composition to the area once a day for up to two weeks complete a first cycle, (ii) resting for up to two weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for up to two weeks to complete a second cycle.
23. The use defined in any one of Claims 1-20, wherein the use comprises: (i) application of the composition to the area once a day for two weeks to complete a first cycle, (ii) resting for two weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for two weeks to complete a second cycle.
24. The use defined in any one of Claims 1-23, wherein the area has a size of up to about 250 cm2.
25. The use defined in any one of Claims 1-23, wherein the area has a size in the range of from greater than about 25 cm2 to about 250 cm2.
26. The use defined in any one of Claims 1-23, wherein the area has a size in the range of from about 200 cm2 to about 250 cm2.
27. The use defined in any one of Claims 1-26, wherein, during the first cycle, the composition is removed from the area at about 8 hours after each daily application.
28. The use defined in any one of Claims 1-26, wherein, during the second cycle, the composition is removed from the area at about 8 hours after each daily application.
29. The use defined in any one of Claims 1-26, wherein, during the first cycle and the second cycle, the composition is removed from the area at about 8 hours after each daily application.
30. The use defined in any one of Claims 1-29, wherein the topical formulation is for treatment of an area afflicted with from about 5 to about 20 actinic keratosis lesions.
31. A topical composition for the treatment of an area afflicted with actinic keratosis, the composition comprising imiquimod in an amount of from about 1% to about 4.25% by weight, together with a pharmaceutically acceptable vehicle therefor, and formulated for administration of imiquimod by: (i) application of the composition to the area once a day for up to three weeks to complete a first cycle, (ii) resting for up to three weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for up to three weeks to complete a second cycle.
32. The topical composition defined in Claim 31, wherein the topical composition comprises an amount of imiquimod selected from about 1.5%, 1.75%, 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75%, 4.0% and 4.25% by weight.
33. The topical composition defined in Claim 31, wherein the topical composition comprises an amount of imiquimod selected from about 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75% and 4.0% by weight.
34. The topical composition defined in Claim 31, wherein the topical composition comprises an amount of imiquimod selected from about 2.5%, 2.75%, 3.0%, 3.25%, 3.5% and 3.75% by weight.
35. The topical composition defined in Claim 31, wherein the topical composition comprises imiquimod in an amount of 2.5% by weight.
36. The topical composition defined in Claim 31, wherein the topical composition comprises imiquimod in an amount of 3.75% by weight.
37. The topical composition defined in Claim 35, wherein the composition is formulated for application of a daily dose of up to 12.5 mg imiquimod during the first cycle.
38. The topical composition defined in Claim 35, wherein the composition is formulated for application of a daily dose of up to 12.5 mg imiquimod during the second cycle.
39. The topical composition defined in Claim 35, wherein the composition is formulated for application of a daily dose of up to 12.5 mg imiquimod during the first cycle and the second cycle.
40. The topical composition defined in Claim 36, wherein the composition is formulated for application of a daily dose of up to 18.75 mg imiquimod during the first cycle.
41. The topical composition defined in Claim 36, wherein the composition is formulated for application of a daily dose of up to 18.75 mg imiquimod during the second cycle.
42. The topical composition defined in Claim 36, wherein the composition is formulated for application of a daily dose of up to 18.75 mg imiquimod during the first cycle and the second cycle.
43. The topical composition defined in any one of Claims 31-42, wherein the pharmaceutically acceptable vehicle comprises a fatty acid.
44. The topical composition defined in Claim 43, wherein the fatty acid is selected from the group consisting of isostearic acid, palmitic acid, stearic acid, linoleic acid, unrefined oleic acid, refined oleic acid and combinations thereof.
45. The topical composition defined in any one of Claims 43-44, wherein the topical formulation is in the form of a cream.
46. The topical composition defined in Claim 45, wherein the fatty acid is present in an amount of from about 3 percent to about 45 percent by weight of the topical composition.
47. The topical composition defined in Claim 45, wherein the fatty acid is present in an amount of from about 5 percent to about 30 percent by weight of the topical composition.
48. The topical composition defined in Claim 45, wherein the fatty acid is present in an amount of from about 5 percent to about 25 percent by weight of the topical composition.
49. The topical composition defined in any one of Claims 45-48, wherein the topical composition further comprises at least one of an emollient, an emulsifier, a thickener, a preservative, a solubilizing agent, a humectant, a skin penetration enhancer and combinations thereof.
50. The topical composition defined in any one of Claims 31-49, wherein the topical composition is formulated for administration of imiquimod by: (i) application of the composition to the area once a day for three weeks to complete a first cycle, (ii) resting for three weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for three weeks to complete a second cycle.
51. The topical composition defined in any one of Claims 31-49, wherein the topical composition is formulated for administration of imiquimod by: (i) application of the composition to the area once a day for up to two weeks complete a first cycle, (ii) resting for up to two weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for up to two weeks to complete a second cycle.
52. The topical composition defined in any one of Claims 31-49, wherein topical composition is formulated for administration of imiquimod by: (i) application of the composition to the area once a day for two weeks to complete a first cycle, (ii) resting for two weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for two weeks to complete a second cycle.
53. The topical composition defined in any one of Claims 31-52, wherein the area has a size of up to about 250 cm2.
54. The topical composition defined in any one of Claims 31-52, wherein the area has a size in the range of from greater than about 25 cm2 to about 250 cm2.
55. The topical composition defined in any one of Claims 31-52, wherein the area has a size in the range of from about 200 cm2 to about 250 cm2.
56. The topical composition defined in any one of Claims 31-55, wherein, during the first cycle, the composition is removed from the area at about 8 hours after each daily application.
57. The topical composition defined in any one of Claims 31-55, wherein, during the second cycle, the composition is removed from the area at about 8 hours after each daily application.
58. The topical composition defined in any one of Claims 31-55, wherein, during the first cycle and the second cycle, the composition is removed from the area at about 8 hours after each daily application.
59. The topical composition defined in any one of Claims 31-58, wherein the topical formulation is for treatment of an area afflicted with from about 5 to about 20 actinic keratosis lesions.
60. A topical composition for the treatment of an area afflicted with actinic keratosis, the composition comprising about 3.75% by weight imiquimod, together with a pharmaceutically acceptable vehicle comprising a fatty acid, the topical composition formulated for administration of imiquimod by: (i) application of the composition to the area once a day for up to two weeks to complete a first cycle, (ii) resting for up to two weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for up to two weeks to complete a second cycle.
61. The topical composition defined in Claim 60, wherein the composition is formulated for application of a daily dose of up to 18.75 mg imiquimod during the first cycle and the second cycle.
62. The topical composition defined in any one of Claims 60-61, wherein the fatty acid is selected from the group consisting of isostearic acid, palmitic acid, stearic acid, linoleic acid, unrefined oleic acid, refined oleic acid and combinations thereof.
63. The topical composition defined in any one of Claims 60-61, wherein the topical formulation is in the form of a cream.
64. The topical composition defined in Claim 63, wherein the fatty acid is present in an amount of from about 3 percent to about 45 percent by weight of the topical composition.
65. The topical composition defined in Claim 63, wherein the fatty acid is present in an amount of from about 5 percent to about 30 percent by weight of the topical composition.
66. The topical composition defined in Claim 63, wherein the fatty acid is present in an amount of from about 5 percent to about 25 percent by weight of the topical composition.
67. The topical composition defined in any one of Claims 63-66, wherein the topical composition further comprises at least one of an emollient, an emulsifier, a thickener, a preservative, a solubilizing agent, a humectant, a skin penetration enhancer and combinations thereof.
68. The topical composition defined in any one of Claims 60-67, wherein topical composition is formulated for administration of imiquimod by: (i) application of the composition to the area once a day for two weeks to complete a first cycle, (ii) resting for two weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for two weeks to complete a second cycle.
69. The topical composition defined in any one of Claims 60-68, wherein the area has a size of up to about 250 cm2.
70. The topical composition defined in any one of Claims 60-68, wherein the area has a size in the range of from greater than about 25 cm2 to about 250 cm2.
71. The topical composition defined in any one of Claims 60-68, wherein the area has a size in the range of from about 200 cm2 to about 250 cm2.
72. The topical composition defined in any one of Claims 60-71, wherein, during the first cycle and the second cycle, the composition is removed from the area at about 8 hours after each daily application.
73. The topical composition defined in any one of Claims 60-72, wherein the topical formulation is for treatment of an area afflicted with from about 5 to about 20 actinic keratosis lesions.
74. A topical composition for the treatment of actinic keratosis, the composition comprising 3.75% by weight imiquimod, together with a pharmaceutically acceptable vehicle comprising a fatty acid, the composition formulated for topical administration of imiquimod at a daily dosage of up to about 18.8 mg to an area afflicted with actinic keratosis and having a size in the range of from about 25 cm2 to about 250 cm2.
75. The topical composition defined in Claim 74, wherein the fatty acid is selected from the group consisting of isostearic acid, palmitic acid, stearic acid, linoleic acid, unrefined oleic acid, refined oleic acid and combinations thereof.
76. The topical composition defined in any one of Claims 74-75, wherein the topical formulation is in the form of a cream.
77. The topical composition defined in Claim 76, wherein the fatty acid is present in an amount of from about 3 percent to about 45 percent by weight of the topical composition.
78. The topical composition defined in Claim 76, wherein the fatty acid is present in an amount of from about 5 percent to about 30 percent by weight of the topical composition.
79. The topical composition defined in Claim 76, wherein the fatty acid is present in an amount of from about 5 percent to about 25 percent by weight of the topical composition.
80. The topical composition defined in any one of Claims 76-79, wherein the topical composition further comprises at least one of an emollient, an emulsifier, a thickener, a preservative, a solubilizing agent, a humectant, a skin penetration enhancer and combinations thereof.
81. The topical composition defined in any one of Claims 74-80, wherein topical composition is formulated for administration of imiquimod by: (i) application of the composition to the area once a day for two weeks to complete a first cycle, (ii) resting for two weeks during which the composition is not applied, and (iii) application of the composition to the area once a day for two weeks to complete a second cycle.
82. The topical composition defined in any one of Claims 74-81, wherein the area has a size in the range of from about 200 cm2 to about 250 cm2.
83. The topical composition defined in any one of Claims 74-82, wherein the composition is removed from the area at about 8 hours after each daily application.
84. The topical composition defined in any one of Claims 74-83, wherein the topical formulation is for treatment of an area afflicted with from about 5 to about 20 actinic keratosis lesions.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA2709732A CA2709732C (en) | 2009-01-14 | 2009-01-15 | Lower dosage strength imiquimod formulations and short dosing regimens for treating actinic keratosis |
| CA2649893A CA2649893C (en) | 2009-01-14 | 2009-01-15 | Lower dosage strength imiquimod formulations and short dosing regimens for treating actinic keratosis |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14473109P | 2009-01-14 | 2009-01-14 | |
| US61/144,731 | 2009-01-14 | ||
| CA2649893A CA2649893C (en) | 2009-01-14 | 2009-01-15 | Lower dosage strength imiquimod formulations and short dosing regimens for treating actinic keratosis |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2709732A Division CA2709732C (en) | 2009-01-14 | 2009-01-15 | Lower dosage strength imiquimod formulations and short dosing regimens for treating actinic keratosis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2649893A1 true CA2649893A1 (en) | 2009-08-17 |
| CA2649893C CA2649893C (en) | 2010-08-03 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2649893A Active CA2649893C (en) | 2009-01-14 | 2009-01-15 | Lower dosage strength imiquimod formulations and short dosing regimens for treating actinic keratosis |
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| Country | Link |
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| CA (1) | CA2649893C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9072876B2 (en) | 2010-08-05 | 2015-07-07 | Medicis Pharmaceutical Corporation | Pump systems and methods for storing and dispensing a plurality of precisely measured unit-doses of imiquimod cream |
-
2009
- 2009-01-15 CA CA2649893A patent/CA2649893C/en active Active
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9072876B2 (en) | 2010-08-05 | 2015-07-07 | Medicis Pharmaceutical Corporation | Pump systems and methods for storing and dispensing a plurality of precisely measured unit-doses of imiquimod cream |
| US9642998B2 (en) | 2010-08-05 | 2017-05-09 | Medicis Pharmaceutical Corporation | Pump systems and methods for storing and dispensing a plurality of precisely measured unit-doses of imiquimod cream |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2649893C (en) | 2010-08-03 |
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