IP Library Granted Patent US 10,702,499
Granted Patent B2
US 10,702,499 · App. 16/364,078 · Granted Jul 7, 2020

Use of NK-1 receptor antagonists in pruritus

Inventors: Xiaoming Zhang (Sunnyvale, CA); Edward F. Schnipper (Redwood City, CA); Andrew J. Perlman (Stanford, CA); James W. Larrick (Sunnyvale, CA)
Assignee: MENLO THERAPEUTICS INC.
A61K31/403A61K9/0014A61K9/0053A61K9/06A61K9/2009A61K9/2013A61K9/2018A61K9/2054A61K9/4808A61K9/4858A61K31/4035A61K45/06A61K47/10Y02A50/463
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Quick Facts
Patent No.
US 10,702,499
App. No.
16/364,078
Granted
Jul 7, 2020
Kind
B2
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 (20)

1. A method for treating pruritus associated with a psychiatric disorder or psychogenic disorder 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.

2. The method of claim 1 , wherein the psychiatric disorder or psychogenic disorder is selected from the group consisting of stress, an anxiety disorder, delusional parasitosis, depression, obsessive-compulsive disorder, schizophrenia and tactile hallucinations.

3. The method of claim 1 , wherein the psychiatric disorder or psychogenic disorder is neurotic excoriation.

4. The method of claim 1 , wherein the therapeutically effective amount of serlopitant comprises a dosage of 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.

5. The method of claim 4 , wherein the therapeutically effective amount of serlopitant comprises a dosage of 0.25 mg, 1 mg or 5 mg once a day.

6. 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.

7. 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.

8. The method of claim 1 , wherein serlopitant is administered over a period of at least 2 weeks, 1 month, 1.5 months or 2 months.

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

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

11. The method of claim 1 , wherein serlopitant is administered topically.

12. The method of claim 11 , wherein serlopitant is administered dermally or transdermally.

13. The method of claim 1 , wherein the pruritus is chronic pruritus.

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

15. The method of claim 14 , wherein the one or more additional antipruritic agents are selected from the group consisting of antihistamines, corticosteroids, immunomodulators, immunosuppressants, opioid receptor antagonists, antidepressants and anticonvulsants.

16. The method of claim 1 , further comprising administering an antidepressant, an antipsychotic, or a combination thereof.

17. 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.

18. 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.

19. The method of claim 18 , wherein the loading dose is three times the at least one therapeutically effective maintenance dose.

20. The method of claim 19 , 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.

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded Sep 20, 2021
From: PERCEPTIVE CREDIT HOLDINGS II, LP
To: VYNE THERAPEUTICS INC. (F/K/A MENLO THERAPEUTICS INC. AND SUCCESSOR-IN-INTEREST TO VYNE PHARMACEUTICALS LTD., F/K/A FOAMIX PHARMACEUTICALS LTD.)
Reel/Frame 057531/0986 →
CHANGE OF NAME Recorded Dec 1, 2020
From: MENLO THERAPEUTICS INC.
To: VYNE THERAPEUTICS INC.
Reel/Frame 054558/0437 →
PATENT SECURITY AGREEMENT Recorded Mar 9, 2020
From: MENLO THERAPEUTICS INC.
To: PERCEPTIVE CREDIT HOLDINGS II, LP
Reel/Frame 052130/0980 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 3, 2019
From: ZHANG, XIAOMING; SCHNIPPER, EDWARD F.; PERLMAN, ANDREW J.; LARRICK, JAMES W.
To: TIGERCAT PHARMA, INC.
Reel/Frame 049077/0009 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 3, 2019
From: ZHANG, XIAOMING; SCHNIPPER, EDWARD F.; PERLMAN, ANDREW J.; LARRICK, JAMES W.
To: TIGERCAT PHARMA, INC.
Reel/Frame 049077/0021 →
CHANGE OF NAME Recorded May 3, 2019
From: TIGERCAT PHARMA, INC.
To: MENLO THERAPEUTICS INC.
Reel/Frame 049085/0793 →