# US 10,369,147 B2 · Topical formulations for delivery of hedgehog inhibitor compounds and use thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,369,147 B2 - Document ID: US10369147B2 - Status: Granted - Kind: B2 - Application number: 15/173,257 - Filed: 2016-06-03 - Published: 2016-12-08 - Granted: 2019-08-06 - Earliest claimed: 2015-06-04 - Assignees: PellePharm, Inc. - Applicants: PellePharm, Inc. - Inventors: Marc Barry Brown; Cameron Robert Stevenson; Charles Rodney Greenaway Evans - Web page: https://patentgrep.com/patent/US10369147B2 ## CPC - A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin - A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)} - A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} - A61K 9/7084: {Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches} - A61K 31/4355: the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom - A61K 47/02: Inorganic compounds - A61K 47/08: containing oxygen, {e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides} - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61K 47/12: Carboxylic acids; Salts or anhydrides thereof - A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones - A61P 17/00: Drugs for dermatological disorders - A61P 35/00: Antineoplastic agents - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Compositions for topical administration of a hedgehog inhibitor compound are described. In one embodiment, the hedgehog inhibitor compound is patidegib and the topical composition comprises the compound in a solvent system of a monohydric primary alcohol and a polyol in a w/w ratio of between about 0.9-1.8. In another embodiment, the hedgehog inhibitor is itraconazole and the topical composition comprises the compound in a solvent system comprising a monohydric primary alcohol and an optionally lower alkyl end-capped oligomeric alkylene glycol in a w/w ratio of between about 0.8 and 2.6 and a fused bicyclic ether. Method of using the compositions are also described, where in one embodiment, the compositions are topically applied for treating or preventing basal cell carcinoma. ## Claims ### Claim 1 A composition for intradermal delivery, comprising: a hedgehog inhibitor compound and a solvent system comprising (i) a monohydric primary alcohol and a polyol in a w/w ratio of between about 0.9-1.8 and (ii) a buffer or a fatty acid comprising between 13-22 carbon atoms, wherein the hedgehog inhibitor compound is present in the solvent system between about 0.1-10 wt %, wherein the hedgehog inhibitor compound is patidegib or itraconazole. ### Claim 2 A composition for intradermal delivery, comprising: a hedgehog inhibitor compound and a solvent system, the hedgehog inhibitor having a saturation solubility in the solvent system of between about 2.5-8 wt % and the solvent system comprising between about 15-60 wt % of a monohydric primary alcohol and between about 10-50 wt % propylene glycol, wherein the hedgehog inhibitor compound is patidegib or itraconazole. ### Claim 3 A composition for intradermal delivery, comprising: a hedgehog inhibitor compound and a solvent system comprising (i) a monohydric alcohol comprised of at least one of ethanol and benzyl alcohol and propylene glycol, the monohydric alcohol and propylene glycol in a w/w ratio of between about 0.9-1.8 and (ii) a buffer or a fatty acid comprising between 13-22 carbon atoms, wherein a hedgehog inhibitor compound is present in the solvent system between about 0.1-10 wt %, wherein the hedgehog inhibitor compound is patidegib or itraconazole. ### Claim 4 (depends on 1, 2, 3) The composition of any one of claims 1-3, wherein the monohydric alcohol is represented by the structure CnH2n-OH, where n is 1, 2, 3 or 4. ### Claim 5 (depends on 4) The composition of claim 4, wherein the solvent system further comprises diethylene glycol monoethyl ether. ### Claim 6 (depends on 1) A topical delivery system, comprising an intradermal composition according to claim 1. ### Claim 7 (depends on 6) The topical delivery system of claim 6, further comprising a backing member and membrane joined to define a reservoir in which the composition is contained. ### Claim 8 (depends on 7) The topical delivery system of claim 7, wherein the membrane is a non-rate controlling membrane. ### Claim 9 A composition for intradermal delivery, consisting essentially of: patidegib and a solvent system comprising ethanol and propylene glycol in a w/w ratio of between about 0.9-1.8, wherein the patidegib has a saturation solubility in the solvent system of between about 2.5-8 wt % and wherein formulation provides an in vitro concentration of patidegib in each of the dermis and epidermis of greater than about 250 μM 48 hours after topical application. ### Claim 10 (depends on 9) The composition of claim 9, wherein the solvent system further comprises a fatty acid comprising between 13-22 carbon atoms.