One of the up and coming treatments for the redness of rosacea is the use of oxymetazoline based formulations.

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

Recent publicity from Vicept Therapetics suggests that their product in development V-101 contains the active ingredient oxymetazoline.

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.

Rebound redness with eyedrop use

PEOPLE’S PHARMACY

Oxymetazoline is a long-acting topical drug that constricts, or shrinks, blood vessels. That is how it relieves congestion in the nose. But people who use nasal decongestants for allergies, colds or sinus problems are warned to use such products for only three to five days. After that they may experience rebound congestion as the medicine wears off.

The same thing can happen in the eyes. Rebound redness occurs when the blood vessels dilate after the effects of the medicine fade. It can take several days (or sometimes longer) for this effect to gradually disappear. You may be better off with artificial tears rather than anti-red drops.

For any oxymetazoline based treatment to succeed as a treatment for a chronic condition like rosacea (i.e. rosacea isn’t a condition that goes away after just a couple of days), the promoters will need to prove that their formulations are safe for use in the medium to long term.

A 2007 paper Successful Treatment of the Erythema and Flushing of Rosacea Using a Topically Applied Selective α1-Adrenergic Receptor Agonist, Oxymetazoline attempted to answer this questions thus;

Neither of our patients exhibited either problem with the application of oxymetazoline to the skin. While the laboratory induction of receptor desensitization cannot yet be perfectly correlated with actual physiologic response, recent laboratory studies indicate that agonists that are more selective for α1D-adrenoceptors are less prone to induce receptor desensitization than are α1A- or α1B-agonists. The clinical significance of this may be an important consideration in contemplating any potential future use of these drug classes on the skin because agonists with certain receptor subtype binding profiles may retain their clinically desirable effects while minimizing their adverse effect.

(emphasis mine)

You can download a full copy of this article from the Archives of Dermatology website; Successful Treatment of the Erythema and Flushing of Rosacea Using a Topically Applied Selective α1-Adrenergic Receptor Agonist, Oxymetazoline

So we all wait to see how the trials of V-101 prove performance with extended and intermittent usage of oxymetazoline.

Related Articles

• Sansrosa’s sister to enter redness race
• V-101 (Oxymetazoline) starting Dose-Finding Trials
• Rosacea Support Community: "Afrin" cure? 

Frontage Clinical in Hackensack, NJ is conducting a research study to evaluate the safety of an investigational topical gel medication for moderate to severe facial redness associated with ROSACEA.

All qualified participants will receive at no cost evaluations by a certified physician, investigational gel medication and compensation for participating.

Must be 18 years or older and have been diagnosed with Rosacea.

Must contact Recruiting Department at (201) 678-0288 for further information

A reasonable guess is that this trial is for the Oxymetazoline based V-101 product from Vicept Therapeutics or the Phase II dose finding study for Sansrosa / CD07805/47. Perhaps there is some clue in that Sansrosa is called a gel and V-101 is called a cream, tipping me to guess that this the Sansrosa trial.

Regardless of the topical in question, I would expect that a lab involved in any trial will keep the product and client close to their chests in the interests of keeping blind tests blind.

If anyone is available then please do join the program so that a new treatment for the redness of rosacea can progress closer to possible availability.

We are working on a new cosmetic line of gentle, effective products to conceal rosacea and other skin flaws and create a flawless, natural-looking complexion. We are looking for women who might enjoy panel testing the products. If they qualify, they will be invited to visit our Soho, New York studio, where a professional makeup artist will apply the products and a photographer will take before and after photographs of them to be used in a how-to video and brochure. In return, they will be given a portable on-trend wardrobe of cosmetics to keep.

PLEASE NOTE: WE ARE SEEKING ORDINARY WOMEN OF ANY AGE, NOT PROFESSIONAL MODELS.

We ask that potential testers please email a photo of themselves and a daytime phone number where they can be reached.

Adrienne Penna

apenna AT manaproducts.com

Product Development

Mana Products Inc.
32-02 Queens Blvd.
Long Island City, NY 11101

718-361-2550 x 3326

A formulation of Ketoconazole 2% for treating seborrheic dermatitis called Extina is currently being promoted by Stiefel Laboratories.

Stiefel, which is a part of GSK, is promoting Extina as the “first and only ketoconazole foam for scalp, body, and face” and being “proven for hair, there and everywhere”.

This foam-based formulation is potentially interesting because it is being promoted as approved for use on facial skin.

The formulation is described as a thermoliable hydroethanolic foam (also known as VersaFoam-HF). The prescribing information advises against dispensing the foam in your hands as it will being to `melt’ immediately. Instead, users are told to dispense the foam into the cap or another cold surface and use fingertips to gently massage into the affected area.

Officially, the reason that ketoconazole works when treating seborrheic dermatitis is unknown.

Active ingredients: ketoconazole

Inactive Ingredients: cetyl alcohol, citric acid, ethanol (denatured with tert-butyl alcohol and brucine sulfate) 58%, polysorbate 60, potassium citrate, propylene glycol, purified water, and stearyl alcohol pressurized with a hydrocarbon (propane/butane) pro

See the Extina web site for the prescribing information and safety warnings.

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The trial will study the efficacy of V-101 Cream, applied once per day, at a low dose of 0.01%, 2 lots of mid-dose of 0.06% and 0.1%, as well as a high dose of 0.15%.

The active ingredient in the formulation has not been officially disclosed, but a reasonable guess is that the active is oxymetazoline. The patents held by the company suggest that oxymetazoline is a primary active of interest, and further confirming the active ingredient is an exclusion criteria for this trial that precludes the “use of products containing oxymetazoline within 14 days of baseline”.

Oxymetazoline is the active ingredient in over the counter products such as Afrin, Vicks Sinex and Visine. The potential side effects of oxymetazoline when applied topically include rebound redness, hypertension and palpitation.

It will be interesting to see how well oxymetazoline performs in a double blind trial as well as get an understanding of any rebound redness and also whether any rebound redness occurs when continuing to use oxymetazoline after having a break.

Here is a short extract of the just announced trial;

Dose Response Study of Patients With Erythematous Rosacea

The purpose of this study is to evaluate the dose-response relationship (effect) of four concentrations of V-101 Cream in patients with erythematous (redness) rosacea.

Related Links

• Vicept Therapeutics positive Phase I study of V-101 for redness of Rosacea
• Vicept Therapeutics gets funding for V-101
• Sansrosa’s sister to enter redness race
• oxymetazoline good for 6 hours and safe for 3 months
• oxymetazoline may be good for 2 years
• AAD Poster Sessions: oxymetazoline
• Dermatology Times highlights Afrin and Sansrosa

Some research also points to rosacea being related to oxidative stress, so rosacea sufferers everywhere are likely to benefit from good nutrition.

SPF on Your Plate: Researcher Connects the Mediterranean Diet With Skin Cancer Prevention

ScienceDaily (Aug. 16, 2010) — We all want that summer glow that comes from a day at the beach, but taking in the rays can have long-term implications for our health. Now Dr. Niva Shapira of Tel Aviv University’s School of Health Professions suggests a way to make fun in the sun safer — and it’s all in our food.

In a study recently published in Nutrition Reviews, Dr. Shapira has shown that a diet rich in antioxidants and omega-3 fatty acids, like the diet eaten in Mediterranean regions where melanoma rates are extremely low, can help protect us from skin cancer.

The sun’s rays damage both the skin and the immune system by penetrating the skin and causing photo-oxidation, she explains, affecting both the cells themselves and the body’s ability to repair any damage. Her prescription is to “go Greek” with foods such as olive oil, fish, yogurt and colorful fruits and vegetables to fight the oxidizing effect of the sun, as well as regular applications of sunscreen and appropriate body coverings such as hats, beach coverups, and other sportswear.

I’m heartened to see this paragraph as well as I think we can easily get sucked in to the `supplements are as good a real food’ idea all too easily.

It might be tempting to load up on dietary supplements instead of changing the diet, but according to Dr. Shapira, supplements are simply not as effective. Foods provide nutrient “synergy,” she says. “In foods, many vitamins and various antioxidants and bioactive ingredients work to support one another and the body’s natural protective mechanisms. Synergies between the nutrients in your food, which make a significant contribution to health, may contrast with the relative isolation of a vitamin supplement.”

A further extract from the referenced Abstract;

Nutritional approach to sun protection: a suggested complement to external strategies

Penetrating photo-oxidative ultraviolet A radiation reduces skin and blood antioxidants and damages cell components, including DNA. Dietary antioxidant vitamins, minerals, and phytochemicals in addition to n-3 polyunsaturated fatty acids, n-9 monounsaturated fatty acids, and low pro-inflammatory n-6 polyunsaturated fatty acids, have demonstrated protective properties. The presence of these elements in the traditional Greek-style Mediterranean diet may have contributed to the low rates of melanoma in the Mediterranean region despite high levels of solar radiation.

Related Articles

• RSPR: Role of Inflammation in Rosacea
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Now that a company name has surfaced we can put the pieces together back to 2007 when Rosacea News featured a publication that suggested that a viable alternative to Sansrosa was about to compete in the anti-redness race. The author of that paper, Dr. D. Shanler is a holder of multiple patents relating to alpha adrenoceptor agonists and treating skin conditions.

While it can’t be said for sure that V-101 is oxymetazoline, it is encouraging to see a product of this sort slowly making its way through the drug development cycle.

V-101 was found to offer a benefit to the redness of rosacea, and was not detectable in the blood of users.

Vicept Therapeutics Announces Positive Clinical Study Results of V-101 for the Treatment of the Erythema of Rosacea

MALVERN, Pa., Aug. 5 /PRNewswire/ — Vicept Therapeutics, Inc., a privately held specialty biopharmaceutical company, announced positive results today from a pharmacodynamic and pharmacokinetic clinical trial of the Company’s lead product V-101, a topical cream under investigation for the treatment of erythema in patients with rosacea.

The double-blinded, placebo-controlled, crossover clinical trial of 22 patients with rosacea was designed to evaluate the bioavailability of V-101 and provide preliminary evidence of efficacy as measured by improvement in moderate to severe erythema, the bright redness of the skin associated with rosacea.  V-101 had a side effect profile similar to placebo and V-101′s active ingredient was not detectable in study participants’ plasma, a strong indication of the product’s overall tolerability and safety profile.  Additionally, the study results were positive for all endpoints, demonstrating a clinically and statistically significant improvement in treating the erythema associated with rosacea.

“This important study demonstrated that V-101 has a good safety profile and provides statistically significant evidence of effectiveness in treating the erythema of rosacea,” said Dr. Neal Walker, president and chief executive officer of Vicept. “We look forward to advancing our clinical program into Phase II and continuing our efforts to develop this product for the 16 million people in the United States who live with this common, chronic skin condition every day.”

Related Articles

• Vicept Therapeutics gets funding for V-101
• Sansrosa’s sister to enter redness race
• oxymetazoline good for 6 hours and safe for 3 months
• oxymetazoline may be good for 2 years
• AAD Poster Sessions: oxymetazoline
• patents abound for treating rosacea with alpha agonist

This latest trial will compare Sansrosa, or CD07805/47 as Galderma now calls it, in strengths of 0.5% and 0.18% against a placebo containing just the vehicle gel. A total of 260 patients will be studied with an estimated primary completion date of February 2011.

Efficacy and Safety Study of CD07805/47 Topical Gel in Subjects With Facial Erythema Associated With Rosacea

Estimated Enrollment: 260

Study Start Date: August 2010

Estimated Study Completion Date: March 2011

Estimated Primary Completion Date: February 2011

The purpose of this vehicle controlled study is to evaluate the efficacy and safety of CD07805/47 gel 0.5% applied topically once daily (QD) for 4 weeks, and CD07805/47 gel 0.18% applied topically once daily (QD) or twice daily (BID) for 4 weeks, in subjects with moderate to severe facial erythema associated with rosacea.

This trial is in addition to the September 2009 trial covered by Rosacea News as Sansrosa starts Phase II strength tests, still a long way to go. That earlier dose-finding trial compared topical gel concentrations of 0.07%, 0.18% and 0.50% and involved 112 participants.

One could speculate from this just listed trial that Galderma is not impressed with the efficacy of CD07805/47 Gel at 0.07%.

It is well worth noting that Sansrosa is now firmly fixed back in Phase 2 trials, and the all important much larger Phase III trials cannot even be contemplated until at least the middle of 2011.

Since Galderma acquired Collagenex in February 2008, Sansrosa has only headed backwards in its development cycle. Galderma don’t seem to be in any rush to get this product to market. This is surprising as there is such a dearth of treatments for the redness of rosacea.

In June 2008 Collagenex tested topical Sansrosa 0.18% against Bromidine Ophthalmic 0.2% to compare systemic absorption of the active molecule.

Previous Phase 2 dose-finding trials by Collagenex, for COL-118, as they then called it, were made public as far back as August 2007  (see Sanrosa (COL-118) phase 2 looking promising).

Here we are 3 years later, and yet again this product is undergoing trials to determine the percentage of active ingredient that should be further developed.

Whilst it may be easy for those waiting for this product to become discouraged, it is a positive that we at least know that Galderma have the R&D dollars to see this product through. Of course this is itself predicated on Galderma continuing to believe that Sansrosa will become a viable product and make substantive returns for their shareholders.

Sansrosa; the never ending story.

Related Articles

• Sansrosa starts Phase II strength tests, still a long way to go
• Sansrosa ingredients revealed in patent application

Seeing this abstract published makes me want to let out a loud groan.

So much of what we see as recently published rosacea research is just recycled sameness.  The actual result of most of these self-similar papers is pretty minimal.

It really doesn’t help rosacea sufferers much to know that the many permutations of the popular and already understood treatments all perform the same.

So the wheels on the bus go round and round, but on this route, the bus never seems to actually get anywhere.

Here is just a sample of the published research showing where this research bus is heading;

• Finacea + Oracea vs Metrogel + Oracea
• Finacea once per day vs Finacea twice per day
• Finacea + doxycyline and then just Finacea for maintenance
• Metrogel vs Finacea
• Metrogel vs Finacea 20%
• Metrogel vs. Finacea 15%
• Metrogel 1% once a day vs Finacea twice a day
• Oracea in combination with Metrogel
• Metrogel with and without antibiotics
• Oracea vs. Doxycycline
• Oracea + Metrogel vs. Doxycycline + Metrogel
• Combination Periostat + Metrogel
• Metrogel vs. Metrolotion vs. Metrocream vs. once a day vs. twice a day

This sort of research does provide good pharmaceutical marketing stories I guess and I suppose it justifies researchers’ efforts, but I am left wondering where this effort could be better utilised.

J Drugs Dermatol. 2010 Jun;9(6):607-13.

Efficacy of topical azelaic acid (AzA) gel 15% plus oral doxycycline 40 mg versus metronidazole gel 1% plus oral doxycycline 40 mg in mild-to-moderate papulopustular rosacea.

Del Rosso JQ, Bruce S, Jarratt M, Menter A, Staedtler G.

Rosacea is a leading reason why people seek the care of a dermatologist, accounting for nearly 7 million office visits annually. Pharmacologic treatments include both topical and oral medications, which are increasingly being used in combination, especially at the outset of therapy. This exploratory study assesses the safety, effectiveness and speed of onset of two common topical agents for the treatment of rosacea azelaic acid gel (AzA) 15% and metronidazole gel 1% used in conjunction with anti-inflammatory dose doxycycline (40 mg once daily). Men and women (n = 207) with mild-to-moderate papulopustular rosacea were enrolled and randomized to receive either AzA gel 15% twice daily plus doxycycline 40 mg once daily (AzA group) or metronidazole gel 1% once daily plus doxycycline 40 mg once daily (Metro group) for 12 weeks. Both regimens were safe, efficacious and well tolerated. Efficacy parameters revealed a possible trend toward greater and earlier benefit with the AzA-based regimen than with the metronidazole-based regimen. These findings warrant further investigation in a sufficiently powered study.

I’ll end this note with a comment that why, seriously, would this study encourage the creation of a more detailed study ?

Always quick to generate a press release, Pyratine XR has been seen some recently published research, this time on the long term efficacy when treating mild to moderate rosacea.

This latest research is in addition to the May 2009 JDD article, Topical PRK 124 (0.125%) lotion for improving the signs and symptoms of rosacea, and the 2007 Topical kinetin 0.1% lotion for improving the signs and symptoms of rosacea

So now we have the June 2010 Journal of Drugs in Dermatology article; Long-term Efficacy and Safety of Topical PRK-124 (0.125%) Lotion (PyratineXR™) in the Treatment of Mild-to-Moderate Rosacea.

Although this study only included 14 patients, it did last 48 weeks which seems to be much longer than the usual period for a study of this type. It is potentially good news that Pyratine XR offers sustained benefit over the long term.

At worst the product didn’t seem to induce an irritation and at best offers a measurable benefit for the redness and papules and pustules of rosacea.

Pyratine XR continues to attract only modest attention in the online rosacea forums. For some snippets of user feedback see Pyratine XR user reviews.

Long-term Efficacy and Safety of Topical PRK 124 (0.125%) Lotion (Pyratine-XR) in the Treatment of Mild-to-Moderate Rosacea

J Drugs Dermatol. 2010 June;9(6):647.

Background: Many patients with rosacea cannot tolerate extended treatment periods with topical agents because their skin sensitivity is often increased.

Objective: To determine the long-term efficacy and tolerability of a new moisturizing lotion for improving the signs and symptoms of mild-to-moderate rosacea.

Methods: In a 48-week, open-label study, a moisturizing lotion containing furfuryl tetrahydropyranyladenine as PRK-124 (0.125%, Pyratine-XR™, Senetek PLC, Napa, CA) was applied twice daily by 18 subjects with mild-to-moderate rosacea. Clinical improvements were assessed by the treating physician. Skin barrier function was measured by transepidermal water loss after treatment. Tolerability and cosmetic outcome were evaluated by subjects.

Results: Subjects experienced a mean 44 percent reduction in erythema severity and a mean 89 percent reduction in inflammatory lesion count at week 48. Reductions were significant (P≤0.05) in both erythema and lesions at weeks 24, 36 and 48. Statistically significant (P≤0.05) improvements in telangiectasias, transepidermal water loss and dryness were noted. Overall clinical improvement was observed in 81 percent of subjects and the investigator’s global assessment steadily improved throughout the study. Treatments were well-tolerated and cosmetically acceptable. Treatment-induced skin irritation was not observed.

Conclusion: The new moisturizing lotion containing furfuryl tetrahydropyranyladenine as PRK 124 is efficacious, does not irritate skin, and is well tolerated for at least 48 weeks.

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