Up to six weeks dosing regimen for treating actinic keratosis with pharmaceutical compositions formulated with 3.75% imiquimod

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.

1 . A method of topically treating a subject diagnosed with actinic keratosis, with a pharmaceutical composition formulated with (a) about 3.75% by weight of imiquimod; and (b) a pharmaceutically acceptable vehicle, said method comprises:
 topically applying the pharmaceutical composition to a treatment area having actinic keratosis once a day for up to 6 weeks, so as deliver an effective amount of imiquimod and to achieve at least partial clearance of the AK lesions.   
     
     
         2 . The method of  claim 1 , wherein the pharmaceutically acceptable vehicle comprises a fatty acid. 
     
     
         3 . The method of  claim 2 , wherein the fatty acid is selected from a group consisting of stearic acid, palmitic acid, unrefined oleic acid, linoleic acid, isostearic acid and super refined oleic acid. 
     
     
         4 . The method of  claim 2 , wherein the fatty acid is oleic acid. 
     
     
         5 . The method of  claim 4 , wherein the oleic acid is refined oleic acid. 
     
     
         6 . The method of  claim 2 , wherein the fatty acid is isostearic acid. 
     
     
         7 . The method of  claim 1 , wherein the treatment area is an area up to about 250 cm 2 . 
     
     
         8 . The method of  claim 2 , wherein the pharmaceutical composition is selected from the group of 3.75% imiquimod formulations listed in Table 9. 
     
     
         9 . A method of topically treating a subject diagnosed with actinic keratosis, with a pharmaceutical composition formulated with (a) about 3.75% by weight of imiquimod; and (b) a pharmaceutically acceptable vehicle, said method comprises:
 topically applying the pharmaceutical composition to a treatment area having actinic keratosis once a day for up to 6 weeks, so as deliver an effective amount of imiquimod and to achieve a reduction in the number of actinic keratosis lesions.   
     
     
         10 . The method of  claim 9 , wherein the pharmaceutically acceptable vehicle comprises a fatty acid. 
     
     
         11 . The method of  claim 10 , wherein the fatty acid is selected from a group consisting of stearic acid, palmitic acid, unrefined oleic acid, linoleic acid, isostearic acid and super refined oleic acid. 
     
     
         12 . The method of  claim 10 , wherein the fatty acid is oleic acid. 
     
     
         13 . The method of  claim 12 , wherein the oleic acid is refined oleic acid. 
     
     
         14 . The method of  claim 10 , wherein the fatty acid is isostearic acid. 
     
     
         15 . The method of  claim 10 , wherein the pharmaceutical composition is selected from the group of 3.75% imiquimod formulations listed in Table 9. 
     
     
         16 . The method of  claim 9 , wherein the number of the number of actinic keratosis lesions in the treatment area is in the range of from about 5 lesions to about 20 lesions. 
     
     
         17 . The method of  claim 9 , wherein the actinic keratosis lesions include at least one of clinical lesions and sub-clinical lesions. 
     
     
         18 . The method of  claim 9 , wherein the treatment area is an area up to about 250 cm 2 . 
     
     
         19 . The method of  claim 1 , wherein the number of the number of actinic keratosis lesions in the treatment area is in the range of from about 5 lesions to about 20 lesions. 
     
     
         20 . The method of  claim 1 , wherein the actinic keratosis lesions include at least one of clinical lesions and sub-clinical lesions.