# US 2025/0144009 A1 · Topical formulations comprising tofacitinib

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- Number: US 2025/0144009 A1
- Document ID: US20250144009A1
- Status: Published application
- Kind: A1
- Application number: 18/949,611
- Filed: 2024-11-15
- Published: 2025-05-08
- Earliest claimed: 2018-01-31
- Assignees: TWi Biotechnology, Inc.
- Applicants: TWi Biotechnology, Inc.
- Inventors: Chih-Ming Chen; Guang-Wei Lu; Ling-Ying Liaw; Fan-Lun Liu; Shih-Fen Liao; Chou-Hsiung Chen; Yu-Han Kao; Yu-Yin Chen
- Web page: https://patentgrep.com/patent/US20250144009A1

## CPC

- 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 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 17/06: Antipsoriatics
- A61P 37/02: Immunomodulators
- 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

A topical formulation comprising (a) a therapeutically effective amount of tofacitinib; (b) at least one solvent; and (c) optionally one or more other pharmaceutically acceptable excipients is provided. Also provided is a method for treating and/or preventing autoimmune diseases in a subject administering said topical formulation.

## Claims

### Claim 1

A topical formulation comprising:
(a) a therapeutically effective amount of tofacitinib;
(b) at least one solvent; and
(c) optionally one or more other pharmaceutically acceptable excipients.

### Claim 2 (depends on 1)

The topical formulation of claim 1, wherein the topical formulation is in the form selected from the group consisting of a solution, a suspension, a cream, an ointment, a lotion and a gel.

### Claim 3 (depends on 1)

The topical formulation of claim 1, wherein the topical formulation is in the form selected from a solution and a gel.

### Claim 4 (depends on 1)

The topical formulation of claim 1, wherein said tofacitinib is in the form of a pharmaceutically acceptable salt selected from citrate salt, hydrochloride salt, hydrobromide salt, oxalate salt, nitrate salt, sulfate salt, phosphate salt, fumarate salt, succinate salt, maleate salt, besylate salt, tosylate salt, palmitate salt and tartrate salt.

### Claim 5 (depends on 4)

The topical formulation of claim 4, wherein said pharmaceutically acceptable salt is citrate salt.

### Claim 6 (depends on 1)

The topical formulation of claim 1, wherein said solvent is selected from the group consisting of dimethyl sulfoxide, propylene glycol, glycerin, poly ethylene glycol, isopropyl alcohol, methanol, sodium pyrrolidone carboxylate, 2-hydroxypropyl-γ-cyclodextrin, acetone, purified water, ethanol, 1-propanol, butanediol, 2-(2-ethoxyethoxy)ethanol (transcutol) and mixtures thereof.

### Claim 7 (depends on 1)

The topical formulation of claim 1, wherein said solvent is dimethyl sulfoxide.

### Claim 8 (depends on 1)

The topical formulation of claim 1, wherein said solvent is a combination of dimethyl sulfoxide with at least one of propylene glycol, ethanol, and water.

### Claim 9 (depends on 1)

The topical formulation of claim 1, wherein said pharmaceutically acceptable excipient is selected from the group consisting of a thickening agent, a stabilizer, an antioxidant, a chelating agent, an oily material, an emulsifier, a penetration enhancer, a pH adjusting agent, a preservative, an antimicrobial agent, an opacifier, a fragrance, a colorant, a gelling agent, a moisturizer, a surfactant, and a combination thereof.

### Claim 10 (depends on 1)

The topical formulation of claim 1, wherein said pharmaceutically acceptable excipient is a thickening agent.

### Claim 11 (depends on 10)

The topical formulation of claim 10, wherein said thickening agent is selected from the group consisting of a cellulose derivative, polyvinylpyrrolidone, a carbomer polymer, carbomer derivative, maltodextrin, polydextrose, dextrates, carboxypolymethylene, polyvinyl alcohol, poloxamers, polyethylene glycols and mixtures thereof.

### Claim 12 (depends on 1)

The topical formulation of claim 1, wherein when the formulation is applied to the skin of a subject, the amount of tofacitinib retained in the skin is more than that penetrating through the skin into the blood or systemic circulation, for 4 hours after the application.

### Claim 13 (depends on 1)

The topical formulation of claim 1, wherein when the formulation is applied to the skin of a subject, the amount of tofacitinib retained in the skin is at least about 4.7 times more than that penetrating through the skin into the blood or systemic circulation, for 8 hours after the application.

### Claim 14 (depends on 1)

The topical formulation of claim 1, wherein less than 2% of total degradation products are observed after stored at room temperature for at least 1 month.

### Claim 15

A topical formulation, comprising:
(a) a therapeutically effective amount of tofacitinib citrate;
(b) dimethyl sulfoxide;
(c) optionally, propylene glycol;
(d) optionally, a thickening agent;
(e) optionally, an antioxidant; and
(f) optionally, one or more other pharmaceutically acceptable excipients.

### Claim 16 (depends on 15)

The topical formulation of claim 15, comprising:
(a) about 0.1% w/w to about 5% w/w of tofacitinib citrate;
(b) about 1% w/w to about 80% w/w of dimethyl sulfoxide;
(c) optionally, about 10% w/w to about 80% w/w of propylene glycol;
(d) optionally, about 0.05% w/w to about 5% w/w of hydroxypropyl cellulose;
(e) optionally, about 0.05% w/w to about 5% w/w of butylated hydroxyanisole; and
(f) optionally, one or more other pharmaceutically acceptable excipients, based on the total weight of the topical formulation.

### Claim 17 (depends on 1)

A method for treating and/or preventing an autoimmune disease in a subject, comprising administering the topical formulation as claimed in claim 1 to said subject.

### Claim 18 (depends on 17)

The method of claim 17, wherein said autoimmune disease is selected from vitiligo, atopic dermatitis, psoriasis, epidermolysis bullosa acquista, pemphigus vulgaris, IgA-mediated bullous dermatoses, systemic lupus erythematosus, alopecia areata, porphyria, scleroderma, rheumatoid arthritis, multiple sclerosis and skin complication of Type I diabetes, Palmoplantar pustulosis, Lichen planus, Discoid lupus erythematosus, granuloma annulare and Ofuji disease.

### Claim 19 (depends on 17)

The method of claim 17, wherein tofacitinib is administered to the skin at a daily therapeutically effective dose of about 0.5 mg/cm2 to about 60 mg/cm2.

### Claim 20 (depends on 17)

The method of claim 17, wherein a daily dose of the topical formulation is applied to skin of the subject in an amount sufficient for the tofacitinib to reach the bloodstream of the subject so as to achieve a plasma concentration within a range between about 3 ng/ml tofacitinib to about 40 ng/ml tofacitinib within about 24 hours of daily dosing of the formulation.

### Claim 21 (depends on 17)

The method of claim 17, wherein a daily dose of the topical formulation is applied to skin of the subject in an amount sufficient for the tofacitinib to reach the bloodstream of the subject so as to achieve a plasma concentration within a range between about 6 ng/ml tofacitinib to about 20 ng/ml tofacitinib within about 24 hours of daily dosing of the formulation.