Use of NK-1 receptor antagonist serlopitant in pruritus

A dosage and cream technology, applied in the direction of medical preparations containing active ingredients, pill delivery, drug combination, etc., can solve problems such as lack of clinical experience

Inactive Publication Date: 2016-04-06
MENLO THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tyrosine kinase inhibitors do not induce frequent nausea and vomiting; therefore, clin

Method used

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  • Use of NK-1 receptor antagonist serlopitant in pruritus
  • Use of NK-1 receptor antagonist serlopitant in pruritus
  • Use of NK-1 receptor antagonist serlopitant in pruritus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0175] Example 1. Preparation of Serlopitant Tablets

[0176] 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) can be formulated In the form of tablets for oral use. Table 1 shows the qualitative / quantitative composition of exemplary doses. The amount of excipients can vary slightly (+ / - 10%) during drug development.

[0177] Table 1

[0178]

[0179]Tablet strengths of 0.25, 1 and 5 mg were prepared as compressed tablet formulations. The tablet manufacturing method was the same for all proposed potencies. The method consists of the following steps: 1) mixing compound 1, mannitol and sodium lauryl sulfate; 2) adding the remaining mannitol into a blender and mixing; 3) mixing microcrystalline cellulose, croscarmellose Sodium and colloidal silicon dioxide are added to the mixer containing the above mixture to complete the mixing and de-agglom...

Embodiment 2

[0180] Example 2. Preparation of Serlopitant Capsules

[0181] Serlopitant (Compound 1) is also supplied to clinics as liquid-filled capsules. Table 2 shows the qualitative / quantitative composition of exemplary doses. The amount of excipients can vary slightly (+ / - 10%) during drug development.

[0182] Table 2

[0183]

[0184] *Capsules are supplied by Capsugel (Morristown, NJ) and contain gelatin and titanium dioxide

[0185] ** Approximate weight of empty capsule shell

[0186] ***Required to seal the capsule shell

[0187] The formulations are prepared by dissolving the drug in mono- and diglycerides. In addition, 0.1% by weight of butylated hydroxyanisole was added as an antioxidant. The initial capsule strength was dispensed into hard gelatin capsules and sealed by spraying with a 1:1 (w / w) water:ethanol solution. Subsequent potencies (including 0.25, 1 and 4 mg) were dispensed into hard gelatin capsules and sealed with gelatin / polysorbate 80 strips. Corres...

Embodiment 3

[0189] Example 3. Clinical Study of Serlopitant in Chronic Pruritus

[0190] The good feasibility of testing the efficacy of three doses of serlopitant in the treatment of chronic pruritus was performed according to the ICH's guidelines for good clinical practice, US federal regulations, the Health Insurance Portability and Accountability Act (HIPAA), and any local regulatory requirements. controlled human clinical trials. 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 relative to placebo in patients with chronic pruritus sex. The patient population for the study included adults, male or female, 18 to 72 years old. The patient must have been previously diagnosed with chronic pruritus defined as pruritus greater than 6 weeks and a VAS score greater than 7 due to any etiology (except uremia, liver failure, cancer or cancer treatment).

[0191] Pa...

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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.

Description

[0001] Cross References to Related Applications [0002] This application claims priority and the benefit of US Patent Application No. 13 / 925,509 and US Provisional Patent Application No. 61 / 838,784, both filed June 24, 2013. technical field [0003] The present invention relates to methods of treating acute or chronic pruritus using NK-1 receptor antagonists. The invention also relates to pharmaceutical compositions comprising NK-1 receptor antagonists. Background of the invention [0004] Pruritus, or itch, is an uncomfortable skin sensation that evokes the desire to scratch. Although itching can be acute, for example, due to insect bites, chronic itching can be caused by many different causes. This is a severely debilitating condition comparable to chronic pain that negatively affects quality of life. [0005] Chronic pruritus afflicts millions of people worldwide, yet conclusive epidemiological data are very limited. For example, a study reported that 8-10% of the Os...

Claims

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Application Information

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IPC IPC(8): A61K31/403A61P17/04A61P25/20
CPCA61K45/06A61K31/4035A61K9/0014A61K9/2054A61K9/4858A61P1/16A61P17/00A61P17/04A61P25/20A61P43/00A61K2300/00A61K31/403
Inventor X·张E·F·施尼佩尔A·J·佩尔曼J·W·拉里克
Owner MENLO THERAPEUTICS INC
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