Pharmacokinetics of Minocycline Foam FMX103 in Subjects With Moderate-to-Severe Facial Papulopustular Rosacea Under Maximum-Use Conditions: Results of a Phase 1 Study

Abstract

not available. Disclosures: Study sponsored by Foamix Pharmaceuticals.

Rosacea Topical Treatment and Care: From Traditional to New Drug Delivery Systems

“…132 This formulation was developed for the treatment of moderate to severe PPR rosacea to increase therapeutic efficacy 132 because of the better penetration into the skin of micronized minocycline, 133 which reduces systemic exposure and its adverse effects. 132 Jones et al conducted a phase I, nonrandomized, open-label study to describe the pharmacokinetics (PK) of minocycline and to assess the safety of this formulation with a dosage of 2 g once daily for 14 days. 132 PK determinations were performed by chromatographic separation using gradient conditions with tandem mass chromatography (LC−MS/MS) using plasma samples, and the safety assessment consisted of the treatment-emergent adverse effects (TEAE), the results of clinical laboratory tests, physical exams, and vital signs.…”

“…132 Jones et al conducted a phase I, nonrandomized, open-label study to describe the pharmacokinetics (PK) of minocycline and to assess the safety of this formulation with a dosage of 2 g once daily for 14 days. 132 PK determinations were performed by chromatographic separation using gradient conditions with tandem mass chromatography (LC−MS/MS) using plasma samples, and the safety assessment consisted of the treatment-emergent adverse effects (TEAE), the results of clinical laboratory tests, physical exams, and vital signs. 132 Furthermore, IGA was used to assess erythema.…”

“…132 PK determinations were performed by chromatographic separation using gradient conditions with tandem mass chromatography (LC−MS/MS) using plasma samples, and the safety assessment consisted of the treatment-emergent adverse effects (TEAE), the results of clinical laboratory tests, physical exams, and vital signs. 132 Furthermore, IGA was used to assess erythema. Pharmacokinetic studies have demonstrated minimal systemic absorption of minocycline, with no evidence of drug accumulation, and a steady-state was achieved after the first application.…”

“…Minocycline is a semisynthetic tetracycline derivative with anti-inflammatory, bacteriostatic, and antioxidant effects . FMX103 is a topical formulation in foam consisting of a minocycline micronized suspension , whose excipients consist of soybean oil, coconut oil, light mineral oil, and cyclomethicone due to its compatibility with minocycline and the moisturizing effects of these ingredients . This formulation was developed for the treatment of moderate to severe PPR rosacea to increase therapeutic efficacy because of the better penetration into the skin of micronized minocycline, which reduces systemic exposure and its adverse effects .…”

New medications for the treatment of acne

“…44 In a phase 1, single-center, nonrandomized open-label active-controlled, crossover study, systemic exposure to minocycline was 730-765 times lower with minocycline 4% foam compared to once daily oral formulation (approximately 1 mg/kg dosing); similar results were observed in patients treated with minocycline 1.5% foam for moderate-to-severe papulopustular rosacea. 45,46 In examining the effect of minocycline foam on C. acnes isolates, minocycline foam was found to be fourfold more active than bacitracin and tetracycline, eightfold more active than clindamycin, and ≥32-fold more active than erythromycin or neomycin. 42 In addition, minocycline foam had a lower resistance rate to C. acnes than the other antibiotics.…”