Use of NK-1 receptor antagonist serlopitant in pruritus
View Patent ↗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.
1. A method of treating pruritus associated with prurigo nodularis, 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 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.
3. The method of claim 2 , wherein the therapeutically effective amount of serlopitant comprises a dosage of 1 mg, 3 mg or 5 mg once a day.
4. 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.
5. 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.
6. The method of claim 1 , wherein serlopitant is administered over a period of at least 1 month, 1.5 months or 2 months.
7. The method of claim 1 , wherein serlopitant is administered at bedtime.
8. The method of claim 1 , wherein serlopitant is administered orally.
9. The method of claim 1 , wherein serlopitant is administered topically.
10. The method of claim 9 , wherein serlopitant is administered dermally or transdermally.
11. The method of claim 1 , wherein the pruritus is chronic pruritus.
12. The method of claim 1 , further comprising administering one or more additional antipruritic agents.
13. The method of claim 12 , 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.
14. A method of treating pruritus associated with epidermolysis bullosa, 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.
15. The method of claim 14 , 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.
16. The method of claim 15 , wherein the therapeutically effective amount of serlopitant comprises a dosage of 1 mg, 3 mg or 5 mg once a day.
17. The method of claim 14 , 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.
18. The method of claim 14 , wherein serlopitant is administered once a day, once every other day, once every third day, once every fourth day, or once a week.
19. The method of claim 14 , wherein serlopitant is administered over a period of at least 1 month, 1.5 months or 2 months.
20. The method of claim 14 , wherein serlopitant is administered at bedtime.
21. The method of claim 14 , wherein serlopitant is administered orally.
22. The method of claim 14 , wherein serlopitant is administered topically.
23. The method of claim 22 , wherein serlopitant is administered dermally or transdermally.
24. The method of claim 14 , wherein the pruritus is chronic pruritus.
25. The method of claim 14 , further comprising administering one or more additional antipruritic agents.
26. The method of claim 25 , 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.
27. 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.
28. The method of claim 27 , 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.
29. The method of claim 14 , wherein at least one loading dose of serlopitant is first administered, and at least one therapeutically effective maintenance dose of serlopitant is subsequently administered.
30. The method of claim 29 , 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.