Use of NK-1 receptor antagonist serlopitant in pruritus
Inventors
Zhang, Xiaoming • Schnipper, Edward F. • Perlman, Andrew J. • Larrick, James W.
Assignees
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Publication Number
US-9737507-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 methods of treating pruritus by administering serlopitant or a pharmaceutically acceptable salt, solvate or polymorph thereof to a patient in need of treatment. The disclosed treated pruritus includes pruritus associated with atopic dermatitis and pruritus associated with urticaria, and the background problem is pruritus as an acute or chronic condition where treatment is needed.
The therapeutic concept includes administering therapeutically effective amounts of serlopitant with NK-1 receptor antagonism and substance P mediation, with NK-1 selectivity described. The invention further includes serlopitant pharmaceutical compositions suitable for the described treatment, including carriers and serlopitant forms such as salts, solvates, and polymorphs.
The disclosure also includes topical formulation concepts and transdermal delivery concepts, including permeation enhancers and topical or transdermal delivery approaches. It includes evaluation and study approaches using clinical endpoints and model-based evaluation, as well as oral dosage form compositions, a described Phase II clinical study design, and topical skin permeation experiments using Franz diffusion cells to compare release, penetration, and retention.
The disclosure also includes an additional independent application for treating sleep disorders as a sleep aid with sedative/hypnotic effects by administering serlopitant, with optional combination with sleep-aiding agents. The document describes sleep disorders such as insomnia, circadian rhythm disorders, parasomnias, and sleep apnea, and lists classes of additional sleep-aiding agents for combination.
Claims Coverage
The partial content provides two independent claims, directed to a method for pruritus associated with atopic dermatitis and a method for pruritus associated with urticaria. Across the dependent claim sets, the coverage includes multiple dosing and regimen-related refinements in addition to the base serlopitant administration.
Treating pruritus associated with atopic dermatitis with serlopitant
Administering a therapeutically effective amount of serlopitant or a pharmaceutically acceptable salt, solvate or polymorph thereof to a patient in need of treatment, for pruritus associated with atopic dermatitis.
Treating pruritus associated with urticaria with serlopitant
Administering a therapeutically effective amount of serlopitant or a pharmaceutically acceptable salt, solvate or polymorph thereof to a patient in need of treatment, for pruritus associated with urticaria.
Dosage range and administered dose amount
Administering serlopitant as a therapeutically effective dosage in the range of about 0.1 mg to about 30 mg or about 1 mg to about 7.5 mg.
Discrete administered dosage amounts with daily frequency
Administering serlopitant as a dosage selected from listed milligram amounts, given one or more times per day.
Topical administration for pruritus treatment
Administering serlopitant topically.
Loading dose followed by maintenance dose
First administering at least one loading dose of serlopitant and then subsequently administering at least one therapeutically effective maintenance dose of serlopitant.
Additional antipruritic agent selection for combination therapy
When additional antipruritic agents are used, selecting the additional antipruritic agents from antihistamines, corticosteroids, immunomodulators, immunosuppressants, opioid receptor antagonists, antidepressants, and anticonvulsants.
Dosing schedules including alternate-day and weekly patterns
Administering serlopitant on a dosing schedule selected from once a day, once every other day, once every third day, once every fourth day, or once per week.
Bedtime administration
Administering serlopitant at bedtime.
The claim coverage centers on administering serlopitant or pharmaceutically acceptable salts, solvates, or polymorphs to treat pruritus in specific patient-condition contexts, namely atopic dermatitis and urticaria. Dependent claim refinements further specify dosage ranges and discrete dose amounts, administration schedules including alternate-day and weekly patterns, topical administration, loading-dose and maintenance-dose structure, bedtime timing, and optional co-therapy with specified classes of additional antipruritic agents.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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