Use of levocetirizine and montelukast in the treatment of vasculitis

Inventors

May, Bruce Chandler

Assignees

Irr IncInflammatory Response Research Inc

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Publication Number

US-9669025-B2

Patent

Publication Date

2017-06-06

Expiration Date


Abstract

The embodiments described herein include methods and formulations for treating vasculitis. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and/or modified-release elements, providing for drug delivery to the patient.

Core Innovation

The patent discloses a method of treating vasculitis in a patient in need thereof by administering an effective amount of a combination of levocetirizine and montelukast. In particular, the vasculitis comprises Henoch Schonlein Purpura. The document indicates treatment across vasculitis types including small, medium, and large vessel forms.

The invention addresses an asserted anti-inflammatory problem in vasculitis and relates the observed activity to H1 receptor and leukotriene pathways involving CysLT1 and LTD4. The disclosure further links the combination to reducing eosinophil migration and reducing inflammatory mediators, including pathways referenced as NF-kB and cytokine involvement such as IL-4, IL-6, and IL-8 and ICAM-1.

The combination is described as providing unexpectedly superior or synergistic anti-inflammatory effects compared with baseline approaches described in the document context, including potential add-on use with an additional active agent such as glucocorticoids. Administration timing concepts include onset and sequential or substantially simultaneous dosing, and administration may be via one or more specified routes, including oral and various non-oral routes described in the claims.

Claims Coverage

The independent claim covers a treatment method for vasculitis (including Henoch Schonlein Purpura) using a levocetirizine plus montelukast combination, with dependent claim sets refining administration timing, route selections, same-route constraints, and optional addition of a glucocorticoid active agent. The inventive features are centered on the combination composition and specific treatment context for vasculitis comprising Henoch Schonlein Purpura.

Levocetirizine and montelukast combination for vasculitis

Administering to a patient in need thereof an effective amount of a combination of levocetirizine and montelukast, wherein vasculitis comprises Henoch Schonlein Purpura.

Sequential administration of the combination

Administering the combination sequentially.

Substantially simultaneous administration of the combination

Administering the combination in a substantially simultaneous manner.

Selected administration routes for the combination

Administering the combination via one or more administration routes selected from enteral, intravenous, intraperitoneal, inhalation, intramuscular, subcutaneous, and oral routes.

Same route for levocetirizine and montelukast

Administering levocetirizine and montelukast via the same route.

Addition of a glucocorticoid active agent

Using an additional active agent that is a glucocorticoid.

Overall claim coverage is directed to treating vasculitis (comprising Henoch Schonlein Purpura) with an effective amount of a levocetirizine and montelukast combination, while dependent claims specify whether dosing is sequential or substantially simultaneous, constrain the route(s) of administration (including same-route for both components), and optionally require an added glucocorticoid active agent.

Stated Advantages

Unexpectedly superior or synergistic anti-inflammatory effects.

Reduction of eosinophil migration.

Potential reduction of inflammatory mediators.

Anti-inflammatory activity associated with H1 receptor and leukotriene (CysLT1/LTD4) pathways.

Documented Applications

Treatment of vasculitis including Henoch Schonlein Purpura (HSP), with a documented case of recurrent HSP resolution after a levocetirizine plus montelukast regimen.

Treatment of vasculitis including Churg-Strauss syndrome (eosinophilic vasculitis), with documented improvements and steroid tapering in a 78-year-old patient.

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