Pharmacokinetics of topical calcineurin inhibitors in adult atopic dermatitis: a randomized, investigator-blind comparison.
OBJECTIVE
We sought to compare pharmacokinetics of pimecrolimus cream 1% and tacrolimus ointment 0.1% in adults with extensive, moderate to severe atopic dermatitis. Secondary end points included efficacy and safety.


METHODS
Patients received twice-daily treatment for 13 days. Blood concentrations of pimecrolimus and tacrolimus were measured at days 1, 5, and 13. Treatment success was defined as an Investigators' Global Assessment score of 0 (clear) or 1 (almost clear).


RESULTS
Tacrolimus was detectable in 36% of blood samples and pimecrolimus was detectable in 12%. In patients with measurable blood drug concentrations, systemic exposure to tacrolimus (mean area under the curve(0-10h) < 9.7 ng.h/mL; n = 7) was higher than to pimecrolimus (mean area under the curve(0-10h) < 2.5 ng.h/mL; n = 2). Whole-body treatment success (day 13) was achieved in 1 of 18 (5.6%) and 2 of 19 (10.5%) patients treated with pimecrolimus and tacrolimus, respectively, and face/neck treatment success in 5 of 18 (27.8%) and 5 of 19 (26.3%) patients, respectively. Patients included in the study were adult patients with severe atopic dermatitis. The results and conclusions drawn from this study population may not be applicable for the majority of patients with atopic dermatitis who have mild to moderate disease.


CONCLUSIONS
Pimecrolimus appears to be associated with lower systemic drug exposure than tacrolimus.
Draelos
Zoe
Z
Dermatology Consulting Services, High Point, North Carolina, USA. zdraelos@northstate.net
Nayak
Anjuli
A
Pariser
David
D
Shupack
Jerome L
JL
Chon
Katie
K
Abrams
Beatrice
B
Paul
Carle F
CF
D000328:Adult; D019540:Area Under Curve; D065095:Calcineurin Inhibitors; D003876:Dermatitis, Atopic / Q000188:drug therapy*; D003879:Dermatologic Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D016037:Single-Blind Method; D016559:Tacrolimus / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics*
D065095:Calcineurin Inhibitors; D003879:Dermatologic Agents; D007166:Immunosuppressive Agents; C117268:pimecrolimus; D016559:Tacrolimus