Claims for Patent: 12,005,051

Summary for Patent: 12,005,051

Title:	Topical roflumilast formulation having improved delivery and plasma half life
Abstract:	The present invention is directed to methods for improving the therapeutic outcome of treatment with roflumilast. The therapeutic outcome is improved by consistent delivery and/or a longer plasma half-life of a topically administered roflumilast composition. The roflumilast composition preferably includes dicetyl phosphate, ceteth-10 phosphate, diethylene glycol monoethyl ether, and/or hexylene glycol.
Inventor(s):	David W. Osborne
Assignee:	Arcutis Biotherapeutics Inc
Application Number:	US17/402,051
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,005,051
Patent Claims:	1. A method for improving the therapeutic outcome of treatment with roflumilast, comprising topically administering once daily a composition comprising diethylene glycol monoethyl ether, cetearyl alcohol, dicetyl phosphate, ceteth-10 phosphate and roflumilast to a patient in need of such treatment, wherein said patient misses at least one dose but no more than two consecutive doses, and the plasma concentration of roflumilast decreases by less than 50%. 2. The method according to claim 1, wherein said patient is suffering from atopic dermatitis. 3. The method according to claim 1, wherein after three days of missed dosing, the plasma concentration of roflumilast decreases by less than 50%. 4. The method according to claim 1, wherein the composition comprises: roflumilast 0.3% w/w white petrolatum 10.0% w/w isopropyl palmitate 5.0% w/w cetearyl alcohol, dicetyl phosphate 10.0% w/w and ceteth-10 phosphate diethylene glycol monoethyl ether 25.0% w/w methylparaben 0.2% w/w propylparaben 0.05% w/w, and purified water q.s. ad 100, wherein the pH is adjusted to 5.5. 5. The method according to claim 1, wherein said patient misses two consecutive doses and the plasma concentration of roflumilast decreases by less than 50%. 6. The method according to claim 1, wherein said roflumilast has a half-life of about 81-89 hours. 7. The method according to claim 1, wherein said patient is a human. 8. The method according to claim 1, further comprising an additional active agent selected from the group consisting of Anthralin (dithranol), Azathioprine, Tacrolimus, Coal tar, Methotrexate, Methoxsalen, Salicylic acid, Ammonium lactate, Urea, Hydroxyurea, 5-fluorouracil, Propylthouracil, 6-thioguanine, Sulfasalazine, Mycophenolate mofetil, Fumaric acid esters, Corticosteroids, Corticotropin, Vitamin D analogues, Acitretin, Tazarotene, Cyclosporine, Resorcinol, Colchicine, Adalimumab, Ustekinumab, Infliximab, and antibiotics. 9. The method according to claim 8, wherein said Corticosteroids are selected from the group consisting of Aclometasone, Amcinonide, Betamethasone, Clobetasol, Clocotolone, Mometasone, Triamcinolone, Fluocinolone, Fluocinonide, Flurandrenolide, Diflorasone, Desonide, Desoximetasone, Dexamethasone, Halcinonide, Halobetasol, Hydrocortisone, Methylprednisolone, Prednicarbate, and Prednisone; and/or said vitamin D analogue is selected from the group consisting of calcipotriene and calcitriol. 10. The method according to claim 1, wherein said composition is selected from the group consisting of an oil in water emulsion and a foam. 11. The method according to claim 1, wherein said roflumilast is in an amount of 0.05-1% w/w. 12. The method according to claim 1, wherein said roflumilast is in an amount of 0.1-0.5% w/w. 13. The method according to claim 1, wherein said patient is suffering from psoriasis. 14. The method according to claim 1, wherein said diethylene glycol monoethyl ether is in an amount of 10-30% w/w. 15. A method for improving the therapeutic outcome of treatment with roflumilast, comprising topically administering once daily a composition comprising diethylene glycol monoethyl ether, a phosphate ester surfactant blend comprising dicetyl phosphate, ceteth-10 phosphate and cetearyl alcohol, and roflumilast to a patient in need of such treatment once daily, wherein when said patient misses at least one dose but no more than two consecutive doses, the plasma concentration of roflumilast decreases by less than 50%. 16. The method according to claim 15, wherein said phosphate ester surfactant blend is in an amount of 1-25% w/w. 17. The method according to claim 16, wherein said phosphate ester surfactant blend is in an amount of 2.5-20% w/w. 18. The method according to claim 17, wherein said phosphate ester surfactant blend is in an amount of 5-15% w/w. 19. The method according to claim 15, wherein said diethylene glycol monoethyl ether is in an amount of 10-30% w/w. 20. The method according to claim 4, wherein the purified water is in an amount of 49.45%.