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Claims for Patent: 9,233,117

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Claims for Patent: 9,233,117

Title:Treatment of inflammatory lesions of rosacea with ivermectin
Abstract: Methods for safe and effective treatment of inflammatory lesions of rosacea in a subject are described. The methods involve once daily topically applying to an affected skin area a topical composition containing ivermectin and a pharmaceutically acceptable carrier. It has been demonstrated that once daily topical treatment with ivermectin is significantly superior than twice-daily topical treatment with metronidazole in reducing inflammatory lesion counts.
Inventor(s): Jacovella; Jean (Antibes, FR), Chappuis; Jean-Paul (Valbonne, FR), Sordello Wagner; Nathalie (Pegomas, FR), Graeber; Michael (Lawrenceville, NJ), Kaoukhov; Alexandre (Newport Beach, CA), Salin; Laurence (La Roquette sur Siagne, FR), Poncet; Michel (Mougins, FR), Briantais; Philippe (Antibes, FR), Benkali; Khaled (Antibes, FR)
Assignee: Galderma S. A. (Cham, CH)
Application Number:14/209,927
Patent Claims: 1. A method of treating inflammatory lesions of rosacea in a subject in need thereof, comprising topically administering, once daily, to a skin area affected by the inflammatory lesions of rosacea a pharmaceutical composition comprising 1% by weight ivermectin and a pharmaceutically acceptable carrier, wherein as early as 2 weeks after the initial administration of the pharmaceutical composition, a significant reduction in inflammatory lesion count is observed.

2. The method of claim 1, wherein the treatment results in more reduction in inflammatory lesion count in the subject in comparison to that achieved by topically administering to the subject, twice daily, a second pharmaceutical composition comprising 0.75% by weight metronidazole.

3. The method of claim 1, wherein the treatment results in longer relapse-free time of the inflammatory lesions of rosacea in the subject in comparison to that achieved by twice daily topically administering to the subject a second pharmaceutical composition comprising 0.75% by weight metronidazole.

4. The method of claim 1, wherein the treatment has a median time to first relapse of 110 days or longer.

5. The method of claim 1, wherein the subject has moderate to severe papulopustular rosacea before the treatment.

6. The method of claim 5, wherein the subject has 15 or more of the inflammatory lesions before the treatment.

7. The method of claim 1, wherein a steady state of plasma concentration of ivermectin is reached in the subject as early as 2 weeks after the initial administration of the pharmaceutical composition to the subject, wherein the steady state has a C.sub.max of ivermectin of 0.5-10 ng/mL, and an AUC.sub.0-24 hr of 10-100 nghr/mL in the subject.

8. The method of claim 1, wherein the pharmaceutical composition further comprises one or more ingredients selected from the group consisting of: an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, the oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, cetostearyl alcohol, stearyl alcohol, palmitostearic acid, stearic acid and self-emulsifiable wax; at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20; a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate; one or more gelling agents selected from the group consisting of carbomers, cellulose gelling agents, xanthan gums, aluminum magnesium silicates but excluding aluminum magnesium silicate/titanium dioxide/silica, guar gums, polyacrylamides and modified starches; and water.

9. The method of claim 1, wherein the topical administration of the pharmaceutical composition to the subject results in a mean terminal half-life of ivermectin of about 145 hours in the subject.

10. A method of treating inflammatory lesions of rosacea in a subject in need thereof, comprising topically administering, once daily, to a skin area affected by the inflammatory lesions a pharmaceutical composition comprising 1% by weight ivermectin and a pharmaceutically acceptable carrier, wherein as early as 2 weeks after the initial administration of the pharmaceutical composition to the subject, a significant reduction in inflammatory lesion count is observed and a steady state of plasma concentration of ivermectin is reached in the subject, and the steady state has a mean C.sub.max of ivermectin of 2.10.+-.1.04 ng/mL with a range of 0.69-4.02 ng/mL, and a mean AUC.sub.0-24 hr of 36.14.+-.15.56 nghr/mL with a range of 13.69-75.16 nghr/mL.

11. The method of claim 10, wherein the treatment results in more reduction in inflammatory lesion count in the subject in comparison to that achieved by topically administering to the subject, twice daily, a second pharmaceutical composition comprising 0.75% by weight metronidazole.

12. The method of claim 10, wherein the treatment results in longer relapse-free time of the inflammatory lesions of rosacea in the subject in comparison to that achieved by twice daily topically administering to the subject a second pharmaceutical composition comprising 0.75% by weight metronidazole.

13. The method of claim 10, wherein the treatment has a median time to first relapse of 110 days or longer.

14. The method of claim 10, wherein the subject has moderate to severe papulopustular rosacea before the treatment.

15. The method of claim 14, wherein the subject has 15 or more of the inflammatory lesions before the treatment.

16. The method of claim 10, wherein the pharmaceutical composition further comprises one or more ingredients selected from the group consisting of: an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, the oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, cetostearyl alcohol, stearyl alcohol, palmitostearic acid, stearic acid and self-emulsifiable wax; at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG 100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20; a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate; one or more gelling agents selected from the group consisting of carbomers, cellulose gelling agents, xanthan gums, aluminum magnesium silicates but excluding aluminum magnesium silicate/titanium dioxide/silica, guar gums, polyacrylamides and modified starches; and water.

17. The method of claim 10, wherein the pharmaceutical composition further comprises carbomer copolymer type B; cetyl alcohol; citric acid monohydrate; dimethicone 20 Cst; edetate disodium; glycerin; isopropyl palmitate; methyl paraben; oleyl alcohol; phenoxyethanol; polyoxyl 20 cetostearyl ether; propylene glycol; propyl paraben; purified water; sodium hydroxide; sorbitan monostearate and stearyl alcohol.

18. The method of claim 10, wherein the topical administration of the pharmaceutical composition to the subject results in a mean terminal half-life of ivermectin of about 145 hours in the subject.

19. The method of claim 10, wherein the treatment results in about 27% or more median reduction of the inflammatory lesion counts.
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