Low systemic exposure after repeated topical application of Pimecrolimus (Elidel), SD Z ASM 981) in patients with atopic dermatitis.
BACKGROUND
Pimecrolimus is a cell-selective inhibitor of inflammatory cytokine release developed specifically for the treatment of inflammatory skin diseases.


OBJECTIVE
The objective of this study was to evaluate blood concentrations and tolerability of pimecrolimus during topical treatment.


METHODS
Twelve adult patients with extensive atopic dermatitis were enrolled in an open-label, noncontrolled, pharmacokinetic study. The patients were treated twice daily for 3 weeks with pimecrolimus cream 1% on all lesions. Pimecrolimus blood concentrations were measured at regular time points, and the safety and tolerability were monitored throughout the study.


RESULTS
In 78% of the 444 blood samples evaluated, pimecrolimus concentrations remained below the limit of quantitation (0.5 ng/ml). The highest concentration measured was 1.4 ng/ml. There was no indication of drug accumulation. Pimecrolimus was well tolerated locally and systemically.


CONCLUSIONS
The 3-week twice daily treatment with pimecrolimus cream 1% results in consistently low pimecrolimus blood concentrations with no accumulation. Pimecrolimus cream appears suitable for the long-term management of atopic dermatitis.
Van Leent
Edwin J M
EJ
Department of Dermatology, Academic Medical Center, University of Amsterdam, The Netherlands. e.j.vanleent@amc.uva.nl
Ebelin
Marie Eve
ME
Burtin
Pascale
P
Dorobek
Birgit
B
Spuls
Phyllis I
PI
Bos
Jan D
JD
D000287:Administration, Topical; D000328:Adult; D001682:Biological Availability; D003876:Dermatitis, Atopic / Q000175:diagnosis / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D005260:Female; D005500:Follow-Up Studies; D006801:Humans; D008297:Male; D012720:Severity of Illness Index; D016559:Tacrolimus / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D016896:Treatment Outcome
C117268:pimecrolimus; D016559:Tacrolimus