Drug – bio-affecting and body treating compositions – Immunoglobulin – antiserum – antibody – or antibody fragment,...
Reexamination Certificate
1999-05-25
2003-01-21
Ungar, Susan (Department: 1642)
Drug, bio-affecting and body treating compositions
Immunoglobulin, antiserum, antibody, or antibody fragment,...
C530S350000, C530S300000, C530S387100, C514S002600
Reexamination Certificate
active
06509014
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Technical Field of the Invention
The present invention relates to the formulation of an antagonist of CGRP (peptide derived from the calcitonin gene: Calcitonin Gene Related Peptide, or “CGRP”) into cosmetic/pharmaceutical/dermatological compositions, in particular for topical application, for treating rosacea and/or discreet erythema.
More especially, this invention relates to the topical, ingestible or injectable treatment of rosacea or discreet erythema.
2. Description of the Prior Art
It is known to this art that rosacea is a skin affliction characterized by erythema of the face, predominantly on the cheeks, the forehead and the nose, hyperseborrhoea of the face on the forehead, the nose and the cheeks, and an infectious component manifesting acneiform pustules.
Moreover, these indications are associated with a neurogenic component, namely, a cutaneous hyperreactivity of the skin of the face and of the neck, characterized by the appearance of redness and subjective sensations of the itching or pruritus type, sensations of burning or of heating, sensations of stinging, tingling, discomfort, tightness, etc.
These signs of hyperreactivity may be triggered by very varied factors such as the intake of food or of hot or alcoholic drinks, by rapid temperature variations, by heat and in particular exposure to ultraviolet or to infrared irradiation, by a low relative humidity, by exposure of the skin to strong winds or to currents of air (conditioned air, fans and blowing machines), by the application of surfactants, irritant dermatological topical agents (retinoids, benzoyl peroxide, alpha-hydroxy acids, etc.), or the use of certain cosmetics, even when these are themselves not recognized as being particularly irritating.
Hitherto, the mechanism for triggering these indications was very poorly understood and rosacea was treated with active agents such as anti-seborrhoeic agents and anti-infection agents, for example benzoyl peroxide, retinoic acid, metronidazole or cyclins, which act on infection and hyperseborrhoea but do not permit the neurogenic component of this affliction, and in particular hyperreactivity of the skin and redness, to be treated.
Similarly, hitherto no treatment existed for the redness which develops in discreet erythema. This latter affliction occurs at times of emotion and is characterized by redness of the face and neckline, which possibly may be accompanied by pruritus (itching). This condition is very irritating for individuals suffering therefrom, and to date it could only be treated by beta-blockers, powerful drugs used for treating hypertension and exhibiting many contraindications.
Thus, serious need continues to exist in this art for an effective treatment of skin redness and of the state of hyperreactivity of skin affected by rosacea or discreet erythema.
SUMMARY OF THE INVENTION
A major object of the present invention is the administration of one or more CGRP antagonists to a mammalian, notably human patient, for treating the disease states indicated above.
CGRP is a polypeptide chemical species produced and released by a nerve ending. CGRP is involved, in particular, in respiratory and inflammatory diseases, in allergic diseases and in certain dermatological diseases such as eczema and prurigo.
However, to date it was not envisaged to use CGRP antagonists for treating skin redness of neurogenous origin.
It is now unexpectedly been determined that CGRP antagonists are useful for eliciting a preventive and/or curative effect on skin redness.
Thus, the present invention features the formulation of at least one CGRP antagonist into a cosmetic, pharmaceutical or dermatological composition, for treating skin redness of neurogenic origin, in particular due to the release of neuropeptides.
DETAILED DESCRIPTION OF BEST MODE AND SPECIFIC/PREFERRED EMBODIMENTS OF THE INVENTION
More particularly according to the present invention, at least one CGRP antagonist is formulated into a cosmetic, pharmaceutical or dermatological composition for treating rosacea and/or discreet erythema.
The administration of compositions containing one or more CGRP antagonists permits eliciting a marked decrease or even complete disappearance of skin redness, which is manifested both in rosacea and in discreet erythema.
The CGRP antagonist thus acts on the neurogenic component of these disease states, for which no treatment hitherto existed, and thereby reinforces the effectiveness of the known active agents for treating their infectious component, in particular in the case of rosacea.
The compositions of the invention may be administered either via a local route, namely, topically or by subcutaneous and/or intradermal injection, or via a systemic or general route, namely, orally and/or by intramuscular injection. Preferably, they are topically administered.
The present invention accordingly features a regimen for the cosmetic, pharmaceutical and/or dermatological treatment of skin redness of neurogenic origin, comprising topically applying a composition containing at least one CGRP antagonist, in a cosmetically, pharmaceutically and/or dermatologically acceptable medium (vehicle, diluent or carrier), to the skin, to the scalp and/or to the mucous membranes.
This invention also features a regimen for the cosmetic, pharmaceutical and/or dermatological treatment of rosacea and/or discreet erythema, comprising topically applying a composition containing at least one CGRP antagonist, in a cosmetically, pharmaceutically and/or dermatologically acceptable medium, to the skin, to the scalp and/or to the mucous membranes.
The subject compositions for topical application comprise a cosmetically, pharmaceutically or dermatologically acceptable medium (vehicle, diluent or carrier), namely, a medium which is compatible with the skin, the nails, the mucous membranes, tissues and the hair. The compositions containing the CGRP antagonist or antagonists are advantageously applied topically to the face, the neck, the hair, the mucous membranes and the nails, major folds, or any other body skin region.
By “CGRP antagonist” is intended any molecule, whether organic or inorganic, effecting inhibition of the receptor binding of CGRP or of effecting inhibition of the synthesis and/or release of CGRP by sensitive nerve fibers.
In order for a chemical species to be recognized as a CGRP antagonist, it must in particular satisfy the following characteristic: it must have a CGRP antagonist pharmacological activity, i.e., induce a coherent pharmacological response, in particular in one of the following tests:
(a) the antagonist species must reduce the vasodilation induced by capsaicin and/or
(b) the antagonist species must induce an inhibition of the release of CGRP by sensitive nerve fibers and/or
(c) the antagonist species must reduce an inhibition of the contraction of vas deferens smooth muscle induced by CGRP.
In addition, the antagonist must have an affinity for the CGRP receptors.
CGRP 8-37, and anti-CGRP antibodies, are suitable for use according to the invention, for example, as a CGRP antagonist.
In the compositions according to the invention, the CGRP antagonist is preferably employed in an amount ranging from 0.000001% to 10% by weight relative to the total weight of the composition, and in particular in an amount ranging from 0.0001% to 5% by weight relative to the total weight of the composition.
The CGRP antagonist may advantageously be combined with one or more antagonists of another neuropeptide such as substance P antagonists and/or one or more inflammation mediator antagonists such as histamine antagonists, interleukin 1 (IL1) antagonists and Tumor Necrosis Factor alpha (TNF&agr;) antagonists.
Thus, the present invention also features cosmetic/pharmaceutical/dermatological compositions for treating skin redness, comprising, in a cosmetically, pharmaceutically and/or dermatologically acceptable medium (vehicle, diluent or carrier), at. least one CGRP antagonist and at least one antagonist of another neuropeptide and/or at least one inflammation mediator antagon
Breton Lionel
De Lacharriere Olivier
Burns Doane Swecker & Mathis L.L.P.
Davis Minyh-Tam
Societe L'Oreal S.A.
Ungar Susan
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