JPWO2020136650A5 - - Google Patents

Claims (22)

at least one EGFR inhibitor selected from the group consisting of erlotinib, gefitinib, lapatinib, cetuximab, panitumumab, vandetanib, necitumumab, osimertinib, and combinations thereof, from 0.01% to 1%, from 1% to 3% by weight; Psoriasis, palmoplantar psoriasis, acquired palmoplantar keratosis, eczema, ichthyosis vulgaris at a concentration of 3% to 5%, 5% to 10%, or 10% to 20% by weight. treatment, prophylaxis, or treatment of a skin or mucosal disorder selected from the group consisting of scabies, non-melanoma skin cancer, actinic keratosis, keratinized skin disorder, keratomucosal disorder, Gorlin's syndrome, prurigo nodularis, and prurigo pigmentosa Or topical compositions for relief. 2. The topical composition according to claim 1, wherein said keratinized skin disorder is hyperkeratosis disorder. 3. The topical composition of claim 1 or claim 2, further comprising at least one penetration enhancer. 4. The topical composition of claim 3, wherein said penetration enhancer is at a concentration of 10% to 98% by weight of the composition. 4. The at least one penetration enhancer is selected from dimethylsulfoxide (DMSO), ethanol, isopropyl alcohol, dimethylisosorbide, isopropyl myristate, oleic acid, polyethylene glycol, hexylene glycol, glycofurol, and combinations thereof. 5. The topical composition of claim 3 or claim 4. 4. The topical composition of Claim 3, further comprising at least one solvent. The at least one solvent is selected from dimethylsulfoxide (DMSO), ethanol, isopropyl alcohol, propylene glycol, dimethylisosorbide, isopropyl myristate, oleic acid, polyethylene glycol, hexylene glycol, glycerin, glycofurol, and combinations thereof. 7. The topical composition of claim 6, wherein A topical composition according to any one of claims 3 to 7, wherein said at least one penetration enhancer has dual functionality and can also act as a solvent. at least one additional first active agent selected from corticosteroids, calcipotriene, tapinalof, Janus kinase inhibitors (JAK inhibitors), phosphodiesterase-4 inhibitors (PDE4 inhibitors), and combinations thereof , in a concentration of 0.01% to 1%, 1% to 3%, 3% to 5% by weight. at least one selected from menadione, ketoconazole, dapsone, cevimeline, spironolactone, tretinoin, pimecrolimus, tetracycline, sunscreen, doxycycline, epidermal growth factor (EGF), lycopene, threolone, synthomycin, erythromycin, vitamin K3, and combinations thereof 10. Any of claims 1-9, further comprising one additional second active agent at a concentration of 0.01% to 1%, 1% to 3%, or 3% to 5% by weight. A topical composition according to claim 1. Claim 9 or claim, wherein said at least one additional first active agent is tapinalof at a concentration of 0.01% to 1%, 1% to 3%, 3% to 5% by weight. Item 11. The topical composition according to Item 10. 0.01% to 1%, 1% to 3%, or 3% to 5% by weight of at least one ingredient selected from moisturizers, skin barriers, urea, ammonium lactate, and combinations thereof 12. The topical composition according to any one of claims 1 to 11, further comprising at a concentration of %. 13. The topical product of any one of claims 1-12, wherein said at least one EGFR inhibitor is selected from erlotinib, gefitinib, lapatinib, salts, hydrates or solvates thereof, and combinations thereof. Composition. 14. The topical composition according to claim 13, wherein said at least one EGFR inhibitor is erlotinib hydrochloride. A topical composition according to any preceding claim, wherein the composition is a cream, ointment, gel, lotion, spray, shampoo, patch or foam. 16. The topical composition according to any one of the preceding claims, wherein said at least one EGFR inhibitor is partially or completely solubilized. 17. The topical composition of any one of claims 1-16, wherein the at least one EGFR inhibitor is erlotinib hydrochloride and the composition is formulated as a topical gel. Treatment, prevention, or alleviation of hyperkeratosis disorders comprising erlotinib hydrochloride at a concentration of 0.75% by weight and at least one penetration enhancer at a concentration of 10% to 98% by weight, formulated as a gel. A topical composition for the treatment, prevention or alleviation of hyperkeratosis disorders in a patient in need thereof. erlotinib hydrochloride at a concentration of 0.75% by weight, DMSO at a concentration of 70% by weight, propylene glycol at a concentration of 25% by weight, 2-phenoxyethanol at a concentration of 0.5% by weight, methylparaben at a concentration of 0.25% by weight , and Carbopol 980 at a concentration of 3% by weight, formulated as a gel. Erlotinib hydrochloride at a concentration of 0.1% to 1%, 1% to 3%, 3% to 5%, or 5% to 10% by weight, 0.01% to 1% by weight , tapinalof at a concentration of 1% to 3%, or 3% to 5% by weight, and at least one penetration enhancer at a concentration of 10% to 98% by weight. , or topical compositions for the treatment, prevention, or alleviation of hyperkeratosis disorders in patients in need thereof. Erlotinib hydrochloride at a concentration of 0.1% to 1%, 1% to 3%, 3% to 5%, or 5% to 10% by weight, 0.01% to 1% by weight , tofacitinib citrate at a concentration of 1% to 3%, or 3% to 5% by weight, and at least one penetration enhancer at a concentration of 10% to 98% by weight. A topical composition for treating, preventing, or ameliorating a hyperkeratosis disorder in a patient in need thereof. Erlotinib hydrochloride at a concentration of 0.1% to 1%, 1% to 3%, 3% to 5%, or 5% to 10% by weight, 0.01% to 1% by weight , apremilast at a concentration of 1% to 3%, or 3% to 5% by weight, and at least one penetration enhancer at a concentration of 10% to 98% by weight. , or topical compositions for the treatment, prevention, or alleviation of hyperkeratosis disorders in patients in need thereof.