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Use of nk-1 receptor antagonists in pruritus

a technology of nk-1 receptor and antagonist, which is applied in the direction of drug compositions, biocide, heterocyclic compound active ingredients, etc., can solve the problems of severe debilitating, adversely affecting the quality of life, and limited solid epidemiological data

Active Publication Date: 2014-12-25
VYNE THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is a seriously debilitating condition, comparable to chronic pain, which negatively impacts quality of life.
Chronic pruritus affects millions of people worldwide, although solid epidemiological data is very limited.
In addition to marginal efficacy, antihistamines can also cause intolerable drowsiness.
Other current therapies possess various limitations.
For example, anticonvulsants such as gabapentin inhibit spinal mechanisms in the perception of itch, but their use is limited due to their slow onset of action (5-6 weeks) (Metz and Ständer, 2008).
Although oral aprepitant is generally well-tolerated, it is extremely expensive, limiting its use in chronic pruritus (Tey, 2011).
Tyrosine-kinase inhibitors do not induce frequent nausea and emesis; therefore, clinical experience with concomitant administration of aprepitant and these drugs is scarce.

Method used

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  • Use of nk-1 receptor antagonists in pruritus
  • Use of nk-1 receptor antagonists in pruritus
  • Use of nk-1 receptor antagonists in pruritus

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Serlopitant Tablets

[0065]Serlopitant, 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, Compound 1, may be formulated as a tablet for oral use. Table 1 shows the qualitative / quantitative composition of exemplary dosages. Minor variations in the excipient quantities (+ / −10%) may occur during the drug development process.

TABLE 1ComponentsFunction% of compositionCompound 1Active agent1-6%Microcrystalline celluloseDiluent50-60% MannitolDiluent20-30% Croscarmellose SodiumDisintegrant1-3%Colloidal silicaDisintegrant0.25-0.5%  Sodium Lauryl SulfateSurfactant5-6%Magnesium StearateLubricant0.25-2%  Total Tablet Composition100% 

[0066]Tablet potencies of 0.25, 1 and 5 mg are prepared as a compressed tablet formulation. The tablet manufacturing process is the same for all proposed potencies. The process consists of the following steps: 1) Compound 1, mannitol and sodium lauryl sul...

example 2

Preparation of Serlopitant Capsules

[0067]Serlopitant (Compound 1) may also be supplied to the clinic as liquid-filled capsules. Table 2 shows the qualitative / quantitative composition of exemplary dosages. Minor variations in the excipient quantities (+ / −10%) may occur during the drug development process.

TABLE 2Unit StrengthComponentsFunction0.25 mg1 mg4 mgCapsule FillCompound 1Active agent0.25 mg  1 mg  4 mgMono- & Di-glyceridesSolubilizer 399 mg398.6 mg 395.6 mg Butylated HydroxyanisoleAntioxidant0.40 mg0.40 mg0.40 mgCapsule Shell#0 White Opaque Hard GelatinCapsule shell   96 mg**   96 mg**   96 mg**Capsule*Gelatin***Banding———componentPolysorbate 80***Banding———component*Capsules are provided by Capsugel (Morristown, NJ) and contain gelatin and titanium dioxide**Approximate weight of empty capsule shell***As needed to seal the capsule shells

[0068]The formulation is prepared by dissolving the drug substance in mono- and di-glycerides. Furthermore, 0.1 wt % butylated hydroxyanisole ...

example 3

Clinical Study of Serlopitant in Chronic Pruritus

[0070]A well-controlled human clinical trial testing the efficacy of three dosages of serlopitant in the treatment of chronic pruritus is conducted in accordance with the ICH Guidelines for Good Clinical Practices, the U.S. Code of Federal Regulations, the Health Insurance Portability and Accountability Act (HIPAA), and any local regulatory requirements. The study is a Phase II randomized, double-blind, parallel group, placebo-controlled, multicenter trial designed to test the efficacy and safety of several doses of serlopitant versus placebo in patients with chronic pruritus. The study patient population includes adult, males or females, 18 to 72 years of age. The patients must be previously diagnosed with chronic pruritus caused by any etiology, except uremia, hepatic failure, cancer or cancer therapy, with chronic pruritus defined as greater than 6 weeks of itching and a VAS score of greater than 7.

[0071]Patients are randomized to ...

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Abstract

The invention relates to methods for treating pruritus with an NK-1 receptor antagonist. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonist.

Description

TECHNICAL FIELD[0001]The invention relates to methods for treating acute or chronic pruritus with an NK-1 receptor antagonist. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonist.BACKGROUND OF THE INVENTION[0002]Pruritus, or itch, is an uncomfortable skin sensation that provokes a desire to scratch. Although itch may be acute, for example, from an insect sting, chronic pruritus originates from many different causes. It is a seriously debilitating condition, comparable to chronic pain, which negatively impacts quality of life.[0003]Chronic pruritus affects millions of people worldwide, although solid epidemiological data is very limited. For example, one study reported that 8-10% of the population of Oslo suffer from chronic pruritus from all causes (F. Dalgard et al., J. Investig. Dermatol. Symp. Proc., 2004, 9(2):120-5). Patients with certain diseases and conditions report high incidences of chronic itch, including those with psoriasis (...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4035
CPCA61K31/4035A61K9/2054A61K9/4858A61K9/4883A61P17/00Y02A50/30A61K9/0014A61K9/0053A61K9/06A61K31/403A61K45/06A61K47/10
Inventor ZHANG, XIAOMINGSCHNIPPER, EDWARD F.PERLMAN, ANDREW J.LARRICK, JAMES W.
Owner VYNE THERAPEUTICS INC
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