Use of NK-1 receptor antagonists in pruritus
Inventors
Zhang, Xiaoming • Schnipper, Edward F. • Perlman, Andrew J. • Larrick, James W.
Assignees
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Publication Number
US-9737508-B2
Publication Date
2017-08-22
Expiration Date
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.
Core Innovation
The invention relates to treating pruritus using 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. The described treatment covers pruritus associated with a burn and pruritus associated with cutaneous T-cell lymphoma (CTCL).
The document addresses the need for treating acute or chronic pruritus, including pruritus associated with burn-related conditions and pruritus associated with CTCL. The approach is tied to NK-1 receptor antagonist activity of serlopitant and to mediation by substance P/tachykinin signaling.
The document further provides pharmaceutical compositions for serlopitant and related forms, including pharmaceutically acceptable salts, solvates, hydrates, and polymorphs, as well as oral tablets/capsules and topical or transdermal formulations. It also describes serlopitant in combination with an additional antipruritic agent class selected from a listed set.
Claims Coverage
The partial content provides two independent claims. Each independent claim centers on administering serlopitant, or a pharmaceutically acceptable salt, solvate or polymorph, as a therapeutically effective amount to treat a specified pruritus association, with dependent claims covering route, dosing regimen, treatment timing, and optional combinations with other antipruritic agent classes.
Serlopitant for burn-associated pruritus treatment
A method of treating pruritus associated with a burn by administering a therapeutically effective amount of serlopitant or a pharmaceutically acceptable salt, solvate or polymorph thereof to a patient in need of treatment.
Serlopitant for CTCL-associated pruritus treatment
A method of treating pruritus associated with cutaneous T-cell lymphoma (CTCL) by administering a therapeutically effective amount of serlopitant or a pharmaceutically acceptable salt, solvate or polymorph thereof to a patient in need of treatment.
Across the independent claims, the core inventive coverage is serlopitant administration for pruritus associated with either a burn or CTCL. Dependent claims further narrow coverage by specifying administration route options, quantitative dose ranges, dosing frequencies or intervals, an optional loading-dose followed by maintenance-dose scheme, and optional co-administration of selected additional antipruritic agent classes.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treatment of pruritus associated with a burn.
Treatment of pruritus associated with cutaneous T-cell lymphoma (CTCL), including mycosis fungoides and Sézary syndrome.
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