Long-term efficacy and tolerability of tacrolimus 0.03% ointment in infants:* A two-year open-label study

Skin and Allergy Hospital, University of Helsinki, Helsinki, Finland.
International journal of dermatology (Impact Factor: 1.31). 09/2011; 51(1):104-10. DOI: 10.1111/j.1365-4632.2011.05015.x
Source: PubMed


Tacrolimus ointment is effective for treatment of moderate to severe atopic dermatitis (AD) in children aged ≥2 years (Br J Dermatol, 2004; 150: 554). Here, efficacy and tolerability of tacrolimus 0.03% ointment were evaluated in 50 infants aged <2 years at start of treatment.
Infants with AD previously enrolled in a tacrolimus ointment pharmacokinetics trial were eligible for a 24-month open-label phase II study. Tacrolimus 0.03% ointment was applied to affected areas until clearance. In cases of exacerbation or clinical worsening, patients restarted treatment.
Mean ± SD Eczema Area and Severity Index (EASI) score improved, from 11.2 ± 10.5 baseline to 2.6 ± 4.1 at endpoint (24 months); mean affected body surface area decreased from 25.2 ± 21.1% to 5.1 ± 9.0%, with improvement on all items of the Physicians' Assessment of Individual Signs. The Physicians' Global Evaluation of Clinical Response showed a result of "cleared"/"excellent" for 63.3% of patients; 85.7% of parents/guardians assessed symptoms as "much better." Treatment was well tolerated, with common, nonserious respiratory infections and gastroenteritis the most frequently reported adverse events. The most common application-site events were infections and pruritus. Over 98% of blood samples showed tacrolimus concentrations <1.0 ng/ml; >40% showed concentrations below the lower limit of quantification (0.0250 ng/ml).
Over a period of two years, tacrolimus 0.03% ointment was associated with substantial clinical improvement of AD in infants aged <2 years. Treatment tolerability was similar to that seen in older children.

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    • "Pharmacokinetic studies on pimecrolimus carried out on children with moderate-to-severe AD and whose body surface was affected up to 92%, showed 67% of pimecrolimus blood concentrations below 0.5 ng/ml and 97% of samples did not exceed 2.0 ng/ml [24]. In a recent study carried out on a group of very young children (between 3 and 24 months) given 0.03% tacrolimus 2 times daily for 2 years in exacerbation, the concentration of tacrolimus was < 1.0 ng/ml in 98% of blood samples and in > 40% of blood samples, tacrolimus concentration was below the limit of detection (0.0250 ng/ml) [25]. "
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