A Randomized Controlled Tolerability Study to Evaluate Reformulated Benzoyl Peroxide Face Washes for Acne Vulgaris

Introduction: This randomized, evaluator-blind, single-center, parallel-group study sought to evaluate the tolerability of two reformulated face washes containing benzoyl peroxide (BPO) in adults with mild to moderate acne vulgaris. Methods: Healthy adults with mild to moderate acne vulgaris were randomly allocated (1:1:1) to one of two reformulated test products (containing BPO at a concentration of either 4% or 10%) or an older formulation containing 10% BPO (reference product), which they applied twice daily for 21±2 days. The primary tolerability assessment was clinical assessment of signs and symptoms of cutaneous irritation by a dermatologist. The primary outcome was the total dermatologist assessment score (maximum total assessment score=12, indicating the most severe skin irritation). Secondary assessments were ophthalmologist assessments, subject self-assessments, and adverse events. Results: 133 adults were randomized and treated. The total dermatologist score changed by a mean of -0.08 (95% confidence interval [CI] -0.192, 0.038) from baseline to day 21 in the 4% BPO cleanser group, by 0.05 (95% CI -0.021, 0.121) in the 10% BPO cleanser group, and by -0.02 (95% CI -0.105, 0.059) in the reference product group. There was no clinically significant difference between the reference product and the 4% BPO cleanser or 10% BPO cleanser in the mean change from baseline. Mean changes from baseline in ophthalmologist assessment scores and subject self-assessment scores for the 4% and 10% BPO test products were also comparable to those of the reference product. Dermal responses were consistent with the known effects of topical BPO application and no serious safety issues were reported. Discussion: There was no difference in the local tolerance profile of the reformulated BPO-containing face washes when compared with an older formulation. Study registration: www.gsk-clinicalstudyregister.com (study 206239). J Drugs Dermatol. 2019;18(4):350-356

Palladium-catalyzed C-F activation of polyfluoronitrobenzene derivatives in Suzuki-Miyaura coupling reactions.

Highly fluorinated nitrobenzene derivatives are suitable substrates for palladium-catalyzed C-F bond arylation using readily available palladium catalysts under both conventional heating and microwave conditions. Arylation occurs ortho to the nitro group offering a synthetic route to polyfluorinated 2-arylnitrobenzene systems. The regiochemistry of the arylation reactions suggests that there is a significant directing interaction between the nitro group and the incoming nucleophilic palladium catalyst which is facilitated by the presence of several fluorine atoms attached the ring. Investigations into the regioselectivity and reactivity of several tetrafluoro- and trifluoronitrobenzene derivatives provides further evidence for the highly nucleophilic character of the oxidative addition step in contrast to the concerted mechanism of more conventional Suzuki-Miyaura coupling reactions involving aryl iodides and bromides.