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New data on the pharmacokinetics of tacrolimus in atopic dermatitis

An open-label, phase II study evaluated the distribution of tacrolimus in the skin and its systemic pharmacokinetics in adults with moderate to severe atopic dermatitis after first and repeated twice-daily applications of tacrolimus 0.1% ointment for 2 weeks. The analysis of skin biopsy samples revealed mean tacrolimus concentrations of 94 ± 20 and 595 ± 98 ng cm-3 at 24 h after the first application and after repeated applications of the ointment, respectively. However, drug concentrations decreased after cessation of treatment. When evaluating the systemic exposure to tacrolimus, the investigators observed that the diffusion into systemic circulation was minimal and variable; hence, levels were 750 and 1800 times lower at 24 ...