Rosacea: Update on Management and Emerging Therapies

Robyn S. Fallen MD; Melinda Gooderham MD, MSc, FRCPC


Skin Therapy Letter. 2012;17(10) 

In This Article

Emerging Therapies

Ivermectin Cream (CD5024)

An agent currently under investigation is CD5024 1% cream, which is a new topical formulation of the acaricidal compound, ivermectin.[32] Although the exact pathophysiology is yet to be elucidated, one well-known hypothesis for the etiology of rosacea is the presence of Demodex mites in the pilosebaceous unit of affected individuals.[33] Reports have been published on cutaneous demodicidosis responding to oral ivermectin and topical permethrin, but data is lacking on the topical application of ivermectin alone.[34]

There are currently three Phase III studies ongoing, one comparing CD5024 1% cream to metronidazole cream 0.75% ( identifier NCT01493947) and two similar studies comparing CD5024 1% cream to azelaic acid 15% gel with an initial randomized controlled phase for 12 weeks, and a comparator extension phase for 40 weeks ( identifiers NCT01494467 and NCT01493687).[35–37] The projected trial completion date is August 2013.

Adrenergic Receptor Antagonists: Brimonidine and Oxymetazoline

Novel therapies to treat the erythema associated with rosacea are under development and have the potential to fill a void in the arsenal of rosacea therapeutics. The adrenergic receptor antagonists brimonidine tartrate and oxymetazoline, which have potent vasoconstrictive activity and anti-redness capabilities, are currently found in eye drops for glaucoma and a nasal decongestant spray, respectively.[38]

Brimonidine tartrate, an alpha-2 agonist also known as CD07805/47, has been shown in a two part dose-finding Phase II study to be safe and efficacious in reducing the erythema of rosacea. A single application of the 0.5% gel reduced erythema between 30 minutes to 12 hours, as measured with an objective chromameter.[39] In part B of the study, two dosages (0.18% and 0.5%) of the gel was compared to vehicle over a 4 week period in 269 subjects. No tachyphylaxis, aggravation of symptoms or rebound erythema was observed. The majority of adverse effects were skin-related and mild and transient in nature. The 0.5% gel once daily was significantly more effective according to both patient and clinician assessments (≥ two-grade improvement) and is the dose that has gone forward in Phase III clinical development to confirm safety and efficacy.[38] Results of the Phase III randomized controlled trials are anticipated to be released in the fourth quarter of 2012.

Oxymetazoline or AGN-199201, a potent alpha-1 and partial alpha-2 receptor agonist, has been shown in case reports to be an effective agent for reducing facial erythema.[40] It has been formulated into a cream and is currently in clinical development for the treatment of erythematotelangiectatic rosacea ( identifier NCT 01579084).[41]