Long-Term Safety and Efficacy of Once-Daily Topical Brimonidine Tartrate Gel 0.5% for the Treatment of Moderate to Severe Facial Erythema of Rosacea: Results of a 1-Year Open-Label Study

January 2014 | Volume 13 | Issue 1 | Original Article | 56 | Copyright © January 2014


Angela Moore MD,a Steven Kempers MD,b George Murakawa MD,c Jonathan Weiss MD,d Amanda Tauscher MD,e Leonard Swinyer MD,f Hong Liu MSc,g and Matthew Leoni MDg on behalf of the Brimonidine LTS Study Group

aArlington Center for Dermatology, Arlington, TX
bMinnesota Clinical Study Center, Fridley, MN
cDermcenter PC, Troy, MI
dGwinnett Clinical Research, Snellville, GA
eCompliant Clinical Research, Olathe, KS
fDermatology Research Center, Salt Lake City, UT
gGalderma R&D, Princeton, NJ

Abstract
Once-daily topical brimonidine tartrate (BT) gel 0.5% was shown to be efficacious and safe for the treatment of erythema of rosacea in previous studies including a 4-week treatment phase. In the present 1-year study, we aimed to assess the long-term safety and efficacy of the treatment. Subjects with moderate to severe erythema of rosacea were instructed to apply topical BT gel 0.5% once daily for 12 months. Severity of erythema and adverse events (AEs) were evaluated. Approximately 345 subject years of exposure to BT gel 0.5% was achieved in the study. The incidence of AEs and AEs judged to be related to the study drug was higher at the beginning and decreased over the course of the study. Similar safety profiles were observed between the subjects who had received or not received concomitant therapies for the inflammatory lesions of rosacea. Effect of topical BT gel 0.5% on erythema severity was observed after the first application and the durability of the effect was maintained until the end of the study at month 12, with no tachyphylaxis observed. In conclusion, once-daily topical BT gel 0.5% is safe and consistently effective for the long-term treatment of moderate to severe erythema of rosacea, even in the presence of concomitant therapies for the inflammatory lesions of rosacea.

J Drugs Dermatol. 2014;13(1):56-61.

INTRODUCTION

Rosacea is a common inflammatory skin disorder estimated to affect 16 million Americans.1 Although it is usually observed in patients with light skin phototype, rosacea has also been diagnosed in patients with darker skins.2-4 Persistent erythema is the primary feature of rosacea and presents ubiquitously among rosacea patients.3 In addition, other cutaneous signs such as telangiectasia, papules, and pustules may also be present.5,6 Several topical and oral medications are currently approved for the treatment of papules and pustules of rosacea, including metronidazole, azelaic acid and anti-inflammatory dose doxycycline.7,8 However, there is currently no approved medication for the treatment of erythema of rosacea, making it a key unmet medical need.9
Brimonidine tartrate (BT), a highly selective α2-adrenergic receptor agonist, was recently shown to reduce erythema of rosacea when applied topically.10,11 BT possibly acts through its vasoconstrictive activity,12-15 leading to a constriction of the abnormal dilation of facial blood vessels in patients presenting with erythema.16-18 BT ophthalmic solution has been approved for the treatment of open-angle glaucoma, with a well-documented good safety profile.12,19,20 The efficacy and safety of topical BT gel 0.5% were assessed in previous randomized, double-blind and controlled Phase II and pivotal Phase III studies, in which BT gel 0.5% was applied once daily for 4 weeks.10, 11 The results demonstrated that topical BT gel 0.5% provided significantly greater efficacy and a faster onset of action compared to the vehicle gel, with a good overall safety profile. In the present long-term study, we aimed to evaluate the safety and efficacy of topical BT gel 0.5% when the medication is applied once daily for up to 12 months.

MATERIALS AND METHODS

The long-term safety and efficacy of the once daily BT gel 0.5% were evaluated in this open-label study carried out in 27 centers in the United States. This study was conducted in accordance with the ethical principles originating from the Declaration of Helsinki and Good Clinical Practices and in compliance with lo-
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