Cutaneous tolerability of a novel topical minocycline gel for the treatment of rosacea
Cutaneous tolerability of a novel topical minocycline gel for the treatment of rosacea
Presenters: Bhatia N1, Ahmadyar M1, Hansra H2, Del Rosso J3, Baldwin H4, Daniels AM5
Affiliations: 1Therapeutics Clinical Research, San Diego, CA; 2BioPharmX, Inc., Menlo Park, CA; 3JDR Dermatology Research, LLC, Las Vegas, NV; 4The Acne Treatment and Research Center, Morristown, NJ
Background/Objective: Rosacea is a chronic and relapsing skin disorder that primarily involves the central face. Affecting at least 16 million people in the United States alone, rosacea can develop via genetic, immunologic, inflammatory, vascular, or environmental pathways. The papulopustular subtype resembles acne vulgaris in its formation of inflammatory papules, pustules, and plaques.
Minocycline is effective as a first-line systemic therapy for rosacea. It is thought that, like other tetracyclines, its anti-inflammatory properties are responsible. Unfortunately, oral and/or long-term use, as required in a chronic condition such as rosacea, might contribute to antibiotic resistance. Additionally, significant side effects such as gastrointestinal distress and vertigo might make oral minocycline intolerable. Therefore, another form of delivery is needed.
Methods: This was a Phase II feasibility study of 1% and 2% formulations of a novel topical minocycline gel. Nineteen adults with moderate-to-severe papulopustular rosacea participated. Skin diseases, prohibited comorbidities and treatments, and pregnancy were exclusionary.
Treatment was open-label and nonrandomized. Subjects applied the assigned gel to the face once per day for 12 weeks. Numbers of facial lesions and their severity were assessed throughout the study. Safety endpoints were also recorded, as were ratings of the cutaneous tolerability (4-point severity scales, investigator- and subject-reported).
Results: The treatment was well tolerated. According to ratings for erythema, scaling/peeling, and edema, none of the subjects experienced worsening of rosacea. Ratings for burning, stinging, tightness, and itching showed that the majority of the subjects improved or were unchanged. Only a single subject reported severe cutaneous irritation at Week 12 (burning, stinging, and itching). Additionally, there were no study-related adverse events or clinically significant changes in laboratory values. Additionally, for both formulations, lesion count and severity were reduced with rapid onset. Clinically meaningful improvements were reported after just four weeks of treatment. The majority of subjects stated they would use the minocycline gel again.
Conclusion: Both formulations of the novel topical minocycline gel demonstrated improvement in treating rosacea and had good cutaneous tolerability profiles. Because cutaneous symptoms such as erythema, edema, burning, and stinging are commonly reported symptoms of rosacea itself, it is to be expected that these were reported with some frequency at baseline. Improvements, which were observed for the majority of subjects in most measures, might therefore be indicative of an improvement in the underlying condition as well as a lack of treatment reaction. Additionally, safety endpoints were met and there was evidence for the effectiveness of treatment in the rapid reduction in number and severity of facial lesions. Although generalizability is limited by the study’s small size and open-label, single-center design, this new therapy shows promise as a new treatment option for rosacea. An important advantage of the topical minocycline formulation might be in reduction of risks associated with systemic exposure to this antibiotic. Next-phase clinical studies are planned.