MAUI, HAWAII – Within the next year or two, two promising new topical medications may join the roster of products for managing rosacea, according to Dr. Joseph F. Fowler Jr.

The two coming attractions are brimonidine tartrate 0.5% gel and oxymetazoline cream. Brimonidine is further along in development; Galderma has submitted an application for Food and Drug Administration marketing approval of the product. Phase II studies of oxymetazoline cream are ongoing.

"Having seen both of these drugs in studies, I think both are going to be effective," said Dr. Fowler, of the University of Louisville (Ky.). "I have no idea if one will be more effective than the other, but I can tell you that both of them are probably going to be a lot better than anything else we have now for the erythema of rosacea," he noted.

"It usually takes around a year after that for a drug to reach the market, assuming no problems arise," Dr. Fowler said at the Hawaii Dermatology Seminar sponsored by Global Academy for Medical Education/Skin Disease Education Foundation.

Both drugs are vasoconstrictors; they are already marketed in other formulations for indications other than rosacea. Oxymetazoline is used as a decongestant in some versions of Afrin nasal spray. Brimonidine is an alpha-2 agonist formulated as a prescription eye drop for the treatment of glaucoma, said Dr. Fowler, who was codirector of the seminar.

The only two topical therapies currently approved for treatment of rosacea – metronidazole and azelaic acid – don’t do much at all to improve the erythematous component of rosacea, in Dr. Fowler’s view. They do reduce inflammatory lesion counts, but not the background redness, he said.

In a separate presentation during the seminar, Dr. Guy W. Webster described his off-label experience in treating rosacea using oxymetazoline and brimonidine in their current formulations.

"These are two off-label products that really work," he said. "I have rosacea patients who are such spectacular flushers that they can’t go outside in the wintertime, but many of them do great with one of these two off-label medicines. It’s something to think about" when other efforts to improve erythema and flushing fail, said Dr. Webster of Thomas Jefferson University, Philadelphia.

Of the two products, the brimonidine eye drops work better when applied to the skin, said Dr. Webster. In fact, the eye drops are so effective that patients require careful instruction in off-label use or they will end up with white streaking on a background of untreated redness that may last for 4-8 hours, he said. Dr. Webster also recommends a preemptive phone call to a patient’s pharmacist to confirm that the "apply to cheeks" instruction on the prescription for the glaucoma medication is in fact correct.

Alternatively, the version of Afrin that contains oxymetazoline can be sprayed on the cheeks for temporary relief of rosacea. However, the investigational cream formulation works better, Dr. Webster said.

Dr. Webster also discussed the use of the two approved topical agents for rosacea and several other drugs with well-established off-label use.

Topical metronidazole 0.75% was the first the original concentration approved for rosacea, but the more recently approved 1% concentration is "vastly superior," in Dr. Webster’s view.

"Unfortunately, a lot of our insurers make patients get the old generic form, which I find is like a placebo," he noted.

Dr. Webster said that some of his patients respond to azelaic acid – the other FDA-approved topical drug – but not to metronidazole, and vice versa.

Topical benzoyl peroxide/clindamycin products often improve papular inflammatory rosacea, although the mechanism of action is unclear, he added.

Dr. Webster said he is unimpressed with the efficacy of sodium sulfacetamide/sulfur for rosacea. "For the amount of activity it gives, it’s almost not worth the expense," he said.

In Dr. Webster’s experience, tacrolimus and pimecrolimus are not useful in uncomplicated rosacea, but he said he finds the topical calcineurin inhibitors invaluable in patients whose rosacea is exacerbated by comorbid atopic dermatitis or seborrheic dermatitis.

"I find I can’t get the rosacea better when it’s being tweaked by a coexisting inflammatory disease unless I get the atopic dermatitis or seborrheic dermatitis better. These two drugs, off label, are critical to getting the rosacea to be able to respond because rosacea is provoked by other inflammation," he explained.

Dr. Webster serves as a consultant to half a dozen pharmaceutical companies, including Galderma and Allergan, which are developing brimonidine gel and oxymetazoline cream, respectively, as rosacea drugs.

Dr. Fowler is a consultant to multiple pharmaceutical companies, including Galderma, and is a research investigator for multiple companies including Galderma and Allergan.

SDEF and this news organization are owned by the same parent company.

bjancin@frontlinemedcom.com

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