Allergan Developing Oxymetazoline (AGN-199201/V-101) Cream Formulations

allergan

A recently surfaced patent application shows that Allergan are continuing to protect their intellectual property around their proposed Oxymetazoline based facial redness treatment.

This patent application relates to the technology and inventions used to create a suitable cream formulation of oxymetazoline. It covers how to make the cream so that it is effective, tolerated, is cosmetically acceptible, and is stable when left on the shelf.

Another patent, U.S. Pat. No. 7,812,049 also assigned to Shanler et.al. describes the use of oxymetazoline to treat erythema resulting from rosacea.

Pharmaceutical cream compositions and methods of use

United States Patent Application 2012/0149748

Inventors: Stuart D. Shanler, Christopher Powala, Luis Rios

Assignee: Allergan, INC, Irvine, CA

Filed: Dec 1, 2011

Pub Date: Jun 14, 2012

Abstract: The present invention is directed to cream compositions and methods in which these cream compositions are administered to patients for the treatment of one or more dermatological conditions.

There exists a need in the art for a topical pharmaceutical composition comprising oxymetazoline which is physically stable (i.e. without phase separation) and chemically stable with the active pharmaceutical agent and which optimizes the delivery of the oxymetazoline to the skin in such a manner as to effectively treat the pathologic condition.

The patent lists some 50 trials and 10 examples of formulations of oxymetazoline that Allergan detail as their intellectual property around the development of their rosacea treatment.

Oxymetazoline Cream vs Afrin Nasal Spray

One example trial compared the use of oxymetazoline nasal spray 0.05% (Afrin) with with 0.5% Oxymetazoline Cream. The facial cream was statistically significantly better at reducing facial redness than the spray alone.

Other trials considered the systemic absorption of oxymetazoline via the topical facial cream vs. the nasal spray.

The final paragraph has the conclusion:

[0164] A single topical facial administration of V-101 cream 0.50% under maximum use conditions in subjects with moderate to severe erythematous rosacea resulted in minimal systemic exposure when compared with a single administration of Afrin Nasal Spray 0.05%.

Topical facial application of V-101 cream 0.50% was well tolerated and significantly reduced erythema from 2 to 12 hours post-dose.

Remember: Just a Patent

It is worth pausing to remember that this is just a patent application. It is not subject to the same rigour as official clinical trials. One can make almost any claim in a Patent Application. Only via FDA accepted clinical trials will the broader applicability of Oxymetazoline be tested.

Some History

We learnt a year ago that Allergan bought Vicept Therapuetics to get access to their Oxymetazoline based V-101 invention.

In April this year Allergan listed a clinical trial for Oxymetazoline for the redness of rosacea. That clinical trial is for a product that Allergan are now calling AGN-199201, which is V-101 from Vicept.

Allergan CEO Speaks

More recently, in March this year we heard from the CEO of Allergan that they are optimising the technology that they purchased via the acquisition of Vicept Therapeutics ;

Allergan’s CEO Hosts 2012 R&D Technology Review Conference Call

And then, you may be aware that last summer we acquired a startup, Vicept, and this was a startup who was developing Oxymetazoline for the treatment of the redness or erythema of rosacea.

Now rosacea, as I’m sure you’re aware, is a very big market and the biggest unmet medical need within rosacea is really the redness.

So there are many products out there right now for the treatment of rosacea, but they primarily treat the papules, the bumps, the pustules that patients get. They really don’t treat the redness effectively.

If you want the redness treated right now, you go to your dermatologist and you get a pulsed dye laser or an intense pulsed light treatment, your insurance doesn’t reimburse that, and it costs you between $800 and $2,000. So there’s a big unmet medical need in the treatment of redness.

So what is Oxymetazoline? Well, you’re all actually familiar with it. This is the active ingredient in Afrin and Visine. “Visine gets the red out”, right? So that’s what we’re trying to do here with the skin.

We have positive Phase II data that was successful from an efficacy and safety standpoint. And we’re now — having met with the FDA, had a successful meeting on endpoints and the pathway forward, we’re now optimizing that formulation and moving into late-stage clinical development.

Here, you see a patient in our Phase II program that was — had this erythematous rosacea, and you can see there’s really — this patient isn’t bothered by bumps and papules and pustules, it’s really the redness that bothers this patient. And after 4 hours after treatment, you can see significant improvement in the redness. So very exciting indeed, and we will be moving into late-stage clinical development.

Who are Allergan?

The owners of this new patent are Allergan who are perhaps better known for making the dry eye treatment Restasis, Refresh artificial tears, and the product that was the genesis of Sansrosa – Alphagan P. Allergan are also the makers of Aczone.

What is Oxymetazoline

Oxymetazoline is the active ingredient in decongestant products like Afrin, Sudafed OM and Vicks Sinex as well as in eye drops like Visine LR.

A well known side effect of Visine is rebound redness, where continued use leads to the redness that you were originally treating. Extended usage of Afrin can also lead to rebound nasal congestion.

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About the Author

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

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2 Reader Comments

  1. Johnabetts says:

    I’ve not looked at the patent yet but I am struck by the statement:

    “One example trial compared the use of oxymetazoline nasal spray 0.05% (Afrin) with with 0.5% Oxymetazoline Cream.”

    How can a valid comparison be made here when there is a ten-fold difference in the concentration of the active material?

  2. David Pascoe says:

    The comparison was done, I imagine because they were familiar with how the nasal spray led to some reduction in redness, and wanted to see how the topical application fared. Also they wanted to compare how much was absorbed into the blood via both application methods.

    So the trial, as part of the description of why they want to patent the discovery, wasn’t proving which way was best, but starting with something known, like Afrin which has been around a long time, and adding in a topical comparison.

    dp.

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