Gallo et al. patent Mast Cell Stabilizers

nasalcrom

A 2014 patent application has surfaced that points to a potential new family of topical rosacea treatments. Drs. Gallo, Nardo and Muto have filed for a patent covering the role of mast cell stabilizers in treating rosacea. The patent also covers the inhibition and stimulation of vitamin D3, cathelicidin and serine protease, and how the resultant pathways can lead to rosacea treatments.

Dr. Di Nardo was awarded a 2012 NRS Grant to study the role of “mast cells as a possible link between an overabundance of the antimicrobial peptides called cathelicidins in individuals with rosacea and the inflammation that appears on rosacea”.

After demonstrating the Mast Cells were key mediators of cathelicidin in mice, erythematotelangiectatic rosacea sufferers also showed a decrease in the expression of MMP activity after 8 weeks of topical cromolyn treatment.

Dr. Di Nardo’s trial used mice and discovered that cromolyn sodium ophthalmic solution 4% is able to reduce skin redness.

The active ingredient in the topical cromolyn treatment – cromolyn sodium, forms the basis of the eye drops known as Crolom and Opticrom and the nasal allergy spray NasalCrom.  The operation of this chemical is known as a mast cell stablizer.

Mast Cell Stabilizer Patent

PREVENTION OF ROSACEA INFLAMMATION

United States Patent Application 20160030386

The disclosure demonstrates the role of mast cell stabilizers in treating rosacea. The disclosure also shows the role of mast cells, cathelicidin, serine protease and/or vitamin D3 in rosacea pathology and the use of antagonists and inhibitors thereof to treat rosacea.

Gallo, Richard L. (San Diego, CA, US)
Di Nardo, Anna (La Jolla, CA, US)
Muto, Yumiko (La Jolla, CA, US)

Some further extracts

the mast cell stabilizer is selected from the group consisting of lodoxamide, nedocromil, cromolyn, pemirolast and pharmaceutical salts of any of the foregoing .

 

the neuropeptide is selected from the group consisting of substance P (SP) , calcitonin gene- related peptide (CGRP) , vasoactive intestinal peptide (VIP) , and neurokinin A (NKA) .

 

A composition comprising a mast cell stabilizer and a second agent selected from the group consisting of: (a) a vitamin D3 antagonist, (b) a serine protease inhibitor, (c) an inhibitor of neuropeptide, and (d) any combination of (a) – (c)

 

Drugs that stabilize mast cells have been studied extensively in connection with the treatment of allergies and several of these drugs are available commercially. The most common mast cell stabilizers are cromolyn, nedocromil, ketotifen and lodoxamide and may either be purchased or synthesized using methods well known in the art.

 

.. composition and method useful for treatment of skin inflammation such as rosacea can include a mast cell stabilizer and further comprise any number of serine protease inhibitors such as those disclosed in, for example, U.S. Pat. No. 5,786,328, U.S. Pat. No. 5,770,568, or U.S. Pat. No. 5,464,820, the disclosures of which are incorporated herein by reference.

 

In another embodiment, the method results in a reduction of inhibition in the amount of activated LL-37 in the skin. The method can be carried out by topically contacting a subject at a site of rosacea. The disclosure also provides a method of treating rosacea comprising contacting a subject having rosacea with an agent that inhibits a neuropeptide. In one embodiment, the the neuropeptide is selected from the group consisting of substance P (SP) , calcitonin gene-related peptide (CGRP) , vasoactive intestinal peptide (VIP) , and neurokinin A (NKA) . In any of these embodiments, the method results in a reduction or inhibition of matrix metalloprotease activity or expression

A Totally New Rosacea Topical?

The possibility of a totally new type of rosacea treating topical is one that rosacea sufferers will be glad to read about. It is still a long way from a patent and preliminary trials to a viable product though, so don’t expect to see anything much more concrete product-wise from this research for a few years yet.

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About the Author: David Pascoe started the Rosacea Support Group in October 1998. .

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3 Reader Comments

  1. John Betts says:

    Mast cell inhibitors have been yo-yo’d around for a number of years (pre-dating this patent application). There are 37 hits dating back to 2008 on Rosacea Support Groups on the use of Cromolyn Sodium for rosacea. This plus other published work seem to make this application somewhat redundant.

  2. Celia says:

    Looking forward to hearing more about this. I’ve found that patting some drops of Nasalchrome on my cheeks reliefs burning/itching. Seems to also help inhibit flushing, though this might off course be a placebo effect.

  3. Billie7 says:

    Can you buy this over the counter?

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