Claims for Patent: 10,918,635

Summary for Patent: 10,918,635

Title:	Lower dosage strength imiquimod formulations and short dosing regimens for treating genital and perianal warts
Abstract:	Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-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 genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available for Aldara.RTM. 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 genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration ("FDA") for Aldara.RTM. 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.
Inventor(s):	Nordsiek; Michael T. (Wayne, PA), Gregory; Jefferson J. (Bristol, TN)
Assignee:	MEDICIS PHARMACEUTICAL CORPORATION (Scottsdale, AZ)
Application Number:	16/364,023
Patent Claims:	1. A method for treating an external genital or perianal wart in a patient 12 years old or older in need thereof, the method comprising topically applying up to 250 mg of a 3.75% (w/w) imiquimod cream once a day to the wart, wherein the imiquimod cream is selected from the following: TABLE-US-00164 Excipients % w/w % w/w % w/w % w/w % w/w % w/w Formulation 181 182 183 184 185 186 Fatty acid* 20.00 20.00 25.00 18.75 2000 21.25 Cetyl alcohol 4.00 2.20 2.20 2.20 2.20 2.20 Stearyl alcohol 2.40 3.10 3.10 3.10 3.10 3.10 White petrolatum 2.80 3.00 3.00 5.00 5.00 3.75 Polysorbate 60 3.00 3.40 3.40 3.00 3.40 3.40 Sorbitan 1.00 0.60 0.60 1.00 0.60 0.60 Monostearate Glycerin 1.00 2.00 2.00 5.00 5.00 5.00 Xanthan gum 0.30 0.50 0.50 0.50 0.50 0.50 Purified water 64.53 59.23 54.23 55.48 54.23 54.23 Benzyl alcohol 2.00 2.00 2.00 2.00 2.00 2.00 Methylparaben 0.20 0.20 0.20 0.20 0.20 0.20 Propylparaben 0.02 0.02 0.02 0.02 0.02 0.02 Imiquimod 3.75 3.75 3.75 3.75 3.75 3.75 Total 100.00 100.00 100.00 100.00 100.00 100.00 Formulation 187 188 189 190 191 192 Fatty acid* 20.00 20.00 20.00 25.00 18.75 25.00 Cetyl alcohol 2.20 2.20 2.20 2.20 2.20 2.70 Stearyl alcohol 3.10 3.10 3.10 3.10 3.10 3.80 White petrolatum 3.00 6.00 6.00 3.00 5.00 3.00 Polysorbate 60 3.40 3.40 3.00 3.40 3.00 3.40 Sorbitan 0.60 0.60 1.00 0.50 1.00 0.60 Monostearate Glycerin 2.00 5.00 5.00 2.00 5.00 2.00 Xanthan gum 0.50 0.50 0.50 0.50 0.50 0.50 Purified water 59.23 53.23 53.23 54.33 55.48 53.03 Benzyl alcohol 2.00 2.00 2.00 2.00 2.00 2.00 Methylparaben 0,20 0.20 0.20 0.20 0.20 0.20 Propylparaben 0.02 0.02 0.02 0.02 0.02 0.02 Imiquimod 3.75 3.75 3.75 3.75 3.75 3.75 Total 100.00 100.00 100.00 100.00 100.00 100.00 Formulation 193 194 195 196 197 198 Fatty acid* 25.00 20.00 20.00 20.00 20.00 21.00 Cetyl alcohol 2.20 4.00 2.20 2.20 2.20 2.20 Stearyl alcohol 3.10 2.40 3.10 3.10 3.10 3.10 White petrolatum 3.00 3.40 5.00 3.00 5.00 5.00 Polysorbate 60 3.40 3.80 3.40 3.40 3.40 3.40 Sorbitan 0.60 1.00 0.60 0.60 0.60 0.60 Monostearate Glycerin 2.00 3.00 2.00 5.00 5.00 5.00 Xanthan gum 1.00 0.70 0.50 0.50 0.50 0.50 Purified water 53.73 55.73 57.23 56.23 54.23 53.23 Benzyl alcohol 2.00 2.00 2.00 2.00 2.00 2.00 Methylparaben 0.20 0.20 0.20 0.20 0.20 0.20 Propylparaben 0.02 0.02 0.02 0.02 0.02 0.02 Imiquimod 3.75 3.75 3.75 3.75 3.75 3.75 Total 100.00 100.00 100.00 100.00 100.00 100.00 wherein the fatty acid selected from the group consisting of palmitic acid, linoleic acid, stearic acid, isostearic acid, unrefined oleic acid, super refined oleic acid and mixtures thereof. 2. The method of claim 1, wherein up to 9.375 mg of imiquimod is applied daily. 3. The method of claim 1, wherein up to 65.625 mg of imiquimod is applied weekly. 4. The method of claim 1, wherein up to 525 mg of imiquimod is applied in the eight week treatment period.