# US 11,026,920 B2 · Use of NK-1 receptor antagonist serlopitant in pruritus

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- Number: US 11,026,920 B2
- Document ID: US11026920B2
- Status: Granted
- Kind: B2
- Application number: 16/806,752
- Filed: 2020-03-02
- Published: 2020-10-01
- Granted: 2021-06-08
- Earliest claimed: 2013-06-24
- Assignees: Vyne Therapeutics Inc.
- Applicants: VYNE Therapeutics Inc.
- Inventors: Xiaoming Zhang; Edward F. Schnipper; Andrew J. Perlman; James W. Larrick
- Web page: https://patentgrep.com/patent/US11026920B2

## CPC

- A61K 31/403: condensed with carbocyclic rings, e.g. carbazole
- 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 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/4858: {Organic compounds}
- A61K 9/4883: {Capsule finishing, e.g. dyeing, aromatising, polishing}
- A61K 31/4035: Isoindoles, e.g. phthalimide
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61P 17/00: Drugs for dermatological disorders
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The invention relates to methods for treating pruritus with NK-1 receptor antagonists such as serlopitant. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonists such as serlopitant. In addition, the invention encompasses treatment of a pruritus-associated condition with serlopitant and an additional antipruritic agent, and the use of serlopitant as a sleep aid, optionally in combination with an additional sleep-aiding agent.

## Claims

### Claim 1

A method for ameliorating or treating a pruritus-associated condition comprising administering a therapeutically effective amount of 3-[(3aR,4R,5S,7aS)-5-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-4-(4-fluorophenyl)-1,3,3a,4,5,6,7,7a-octahydroisoindol-2-yl]cyclopent-2-en-1-one (serlopitant) or a pharmaceutically acceptable salt, solvate or polymorph thereof to a patient in need of treatment, wherein the condition is a viral infection.

### Claim 2 (depends on 1)

The method of claim 1, wherein the therapeutically effective amount of serlopitant comprises a dosage of about 0.10 mg, 0.15 mg, 0.20 mg, 0.25 mg, 0.5 mg, 0.75 mg, 1 mg, 2 mg, 2.5 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 9 mg, 10 mg, 15 mg, 20 mg, 25 mg or 30 mg one or more times a day.

### Claim 3 (depends on 1)

The method of claim 1, wherein the therapeutically effective amount of serlopitant comprises a dosage of from about 0.1 mg to about 30 mg, or from about 1 mg to about 7.5 mg.

### Claim 4 (depends on 1)

The method of claim 1, wherein serlopitant is administered once a day, once every other day, once every third day, once every fourth day, or once a week; and wherein serlopitant is administered over a period of at least 2 weeks, 1 month, 1.5 months or 2 months.

### Claim 5 (depends on 1)

The method of claim 1, wherein serlopitant is administered at bedtime.

### Claim 6 (depends on 1)

The method of claim 1, wherein serlopitant is administered orally.

### Claim 7 (depends on 1)

The method of claim 1, wherein serlopitant is administered topically, dermally or transdermally.

### Claim 8 (depends on 1)

The method of claim 1, wherein serlopitant is administered by injection or infusion.

### Claim 9 (depends on 1)

The method of claim 1, further comprising administering one or more additional agents.

### Claim 10 (depends on 9)

The method of claim 9, wherein the one or more additional agents are selected from the group consisting of antihistamines, corticosteroids, NSAIDs, immunomodulators, immunosuppressants, opioid receptor antagonists, antidepressants and anticonvulsants.

### Claim 11 (depends on 10)

The method of claim 10, wherein the corticosteroid comprises one or more of a cortisone, a hydrocortisone, a prednisolone, a methylprednisolone, a prednisone, a tixocortol, a betamethasone, a dexamethasone, a fluocortolone, a halogenated steroid, analclometasone, a beclometasone, a clobetasol, a clobetasone, a desoximetasone, a diflorasone, a diflucortolone, a fluprednidene, a fluticasone, a halobetasol, a ulobetasol, a halometasone, a mometasone, an acetonide, an amcinonide, a budesonide, a ciclesonide, a desonide, a fluocinonide, a fluocinolone acetonide, a flurandrenolide, a flurandrenolone, a fludroxycortide, a halcinonide, a triamcinolone acetonide, a triamcinolone alcohol, and analogs, derivatives and carbonates thereof.

### Claim 12 (depends on 11)

The method of claim 11, wherein the corticosteroid comprises one or more of cortisone acetate, hydrocortisone acetate, hydrocortisone-17-aceponate, hydrocortisone-17-buteprate, hydrocortisone-17-butyrate, hydrocortisone-17-valerate, methylprednisolone aceponate, tixocortol pivalate betamethasone dipropionate, betamethasone sodium phosphate, betamethasone valerate, dexamethasone sodium phosphate, fluocortolone caproate, fluocortolone pivalate, alclometasone dipropionate, beclometasone dipropionate, clobetasol-17-propionate, clobetasone-17-butyrate, desoximetasone acetate, diflorasone diacetate, diflucortolone valerate, fluprednidene acetate, fluticasone propionate, halobetasol proprionate, halometasone acetate, mometasone furoate, and prednicarbate.

### Claim 13 (depends on 11)

The method of claim 11, wherein the corticosteroid comprises a dexamethasone.

### Claim 14 (depends on 12)

The method of claim 12, wherein the corticosteroid is dexamethasone sodium phosphate.

### Claim 15 (depends on 1)

The method of claim 1, further comprising administering an antiviral, or ultraviolet B phototherapy, or any combination thereof.

### Claim 16 (depends on 13)

The method of claim 13, further comprising administering an antiviral, or ultraviolet B phototherapy, or any combination thereof.

### Claim 17 (depends on 1)

The method of claim 1, wherein at least one loading dose of serlopitant is first administered, and at least one therapeutically effective maintenance dose of serlopitant is subsequently administered.

### Claim 18 (depends on 17)

The method of claim 17, wherein the at least one loading dose is five times, four times, three times or two times larger than the at least one therapeutically effective maintenance dose, and/or wherein the loading dose is 0.75 mg, 3 mg, or 15 mg, and the at least one therapeutically effective maintenance dose is 0.25 mg, 1 mg, or 5 mg.

### Claim 19 (depends on 1)

The method of claim 1, wherein the viral infection is selected from the group consisting of HIV/AIDS, herpes, measles, and a parvovirus; or wherein the viral infection is herpes zoster, parvovirus B19, varicella, or yellow fever.

### Claim 20

A method of administering a therapeutically effective amount of 3-[(3aR,4R,5S,7aS)-5-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-4-(4-fluorophenyl)-1,3,3a,4,5,6,7,7a-octahydroisoindol-2-yl]cyclopent-2-en-1-one (serlopitant) or a pharmaceutically acceptable salt, solvate or polymorph thereof and a corticosteroid to a patient with a viral infection in need of treatment;
wherein serlopitant is administered one, two, three or more times per day, orally, by injection or infusion and the corticosteroid is administered one, two, three or more times per day, intranasally, pulmonarily, by injection or infusion;
wherein at least one loading dose of serlopitant is administered, and at least one therapeutically effective maintenance dose of serlopitant is subsequently administered, wherein the at least one loading dose is five times, four times, three times or two times larger than the at least one therapeutically effective maintenance dose or the at least one loading dose is 0.75 mg, 3 mg, or 15 mg, and the at least one therapeutically effective maintenance dose is 0.25 mg, 1 mg, or 5 mg;
wherein about 0.1 mg to about 30 mg, or from about 1 mg to about 7.5 mg of serlopitant is administered daily; and
wherein the corticosteroid is administered concurrently with or sequentially (before or after) administration of serlopitant.