Abstract
Background and Objective
Tazarotene, a retinoid pro-drug, is available in gel, cream and foam for the topical treatment of acne vulgaris. This single-centre, randomized, open-label study assessed relative bioavailability of its active metabolite tazarotenic acid after dosing of tazarotene foam or gel.
Study Design and Methods
Subjects with moderate-to-severe acne received a mean, once-daily dose of 3.7 g tazarotene foam or gel applied to face, chest, upper back and shoulders. Blood samples were collected pre-dose on multiple days and multiple time points over a 72-h period to measure plasma tazarotenic acid and tazarotene.
Results
Mean tazarotenic acid area under the plasma concentration–time curve (AUC) and maximum measured plasma concentration (Cmax) values were significantly higher for gel versus foam. Cmax occurred within 5–6 h after dosing, with an apparent terminal elimination half-life (t½) of 18–22 h. Accumulation was observed upon repeated dosing with steady-state conditions achieved at day 20. Mean tazarotene concentrations were also higher following gel application versus foam. Both foam and gel demonstrated an acceptable safety profile.
Conclusion
Tazarotene foam, 0.1 % is an alternative to gel with less systemic exposure.
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Acknowledgements
This study was sponsored by Stiefel, a GSK company. Dr Jarratt is an employee of DermResearch, Inc., Clinical Research. Dr Alió Saenz is an employee of Stiefel, a GSK company. We thank Leandro Santos, BSc, for assistance with analytical methods and Elizabeth Hussey, PharmD, for scientific review. Assistance with editorial preparation of this manuscript was provided by Andy Kerr, PhD, and Joelle Suchy, PhD, and assistance with copy editing and fact checking was provided by Sue Landry of MediTech Media; editorial assistance was funded by Stiefel, a GSK company.
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Clinical Trial Registry Number: NCT01019603.
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Jarratt, M., Werner, C.P. & Alió Saenz, A.B. Tazarotene Foam versus Tazarotene Gel: A Randomized Relative Bioavailability Study in Acne Vulgaris. Clin Drug Investig 33, 283–289 (2013). https://doi.org/10.1007/s40261-013-0065-1
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DOI: https://doi.org/10.1007/s40261-013-0065-1