Systemic exposure, tolerability, and efficacy of pimecrolimus cream 1% in atopic dermatitis patients.
OBJECTIVE
To measure pimecrolimus blood concentrations and to evaluate tolerability and efficacy in children and infants treated topically for atopic dermatitis with pimecrolimus cream 1% for three weeks.


METHODS
Three open label, non-controlled, multiple topical dose studies were conducted in children aged 8-14 years (study A, ten patients), and in infants aged 8-30 months (study B, eight patients) and 4-11 months (study C, eight patients). Pimecrolimus blood concentrations were determined on days 4 and 22 of treatment, and at end of study. Efficacy was assessed using the Eczema Area and Severity Index (EASI).


RESULTS
Pimecrolimus blood concentrations were consistently low, typically (81%) below 1 ng/ml, with more than half of the measurements below the assay limit of quantitation (0.5 ng/ml) in studies A and B. The highest blood concentration measured throughout the three studies was 2.6 ng/ml. The cream was well tolerated, locally and systemically. The most common adverse event suspected to be related to study medication was a transient mild to moderate stinging sensation at the application site in 5/26 patients. There was no indication of any systemic adverse effect. The patients responded well to therapy with a rapid onset of action, usually within four days. Median reductions of EASI from baseline at day 22 were 55% (study A), 63% (study B), and 83% (study C).


CONCLUSIONS
Three weeks treatment of children and infants with extensive atopic dermatitis, using pimecrolimus cream 1% twice daily, is well tolerated and results in minimal systemic exposure, at which no systemic effect is expected.
Allen
B R
BR
Department of Dermatology, University Hospital, Nottingham, UK.
Lakhanpaul
M
M
Morris
A
A
Lateo
S
S
Davies
T
T
Scott
G
G
Cardno
M
M
Ebelin
M-E
ME
Burtin
P
P
Stephenson
T J
TJ
D000293:Adolescent; D002648:Child; D002675:Child, Preschool; D003876:Dermatitis, Atopic / Q000097:blood* / Q000188:drug therapy; D003879:Dermatologic Agents / Q000009:adverse effects / Q000097:blood* / Q000627:therapeutic use; D004334:Drug Administration Schedule; D005260:Female; D006801:Humans; D007166:Immunosuppressive Agents / Q000009:adverse effects / Q000097:blood* / Q000627:therapeutic use; D007223:Infant; D008297:Male; D012720:Severity of Illness Index; D016559:Tacrolimus / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000097:blood* / Q000627:therapeutic use; D016896:Treatment Outcome
D003879:Dermatologic Agents; D007166:Immunosuppressive Agents; C117268:pimecrolimus; D016559:Tacrolimus