Pimecrolimus – an anti‐inflammatory drug targeting the skin

Pimecrolimus – an anti‐inflammatory drug targeting the skin Abstract: Pimecrolimus is the most recent member of calcineurin inhibitors available for the therapy for inflammatory skin diseases. It targets T‐cells and mast cells and inhibits the production and release of cytokines and other inflammatory mediators, as well as the expression of signals essential for the activation of inflammatory T‐lymphocytes. Pimecrolimus has a cell‐selective mode of action. In contrast to corticosteroids, it does not affect, e.g., Langerhans'cells/dendritic cells (LC/DC), as demonstrated in vitro with human monocyte‐derived DC and in vivo with epidermal LC in mice, nor human primary fibroblasts. As shown in vitro with human skin and by comparison of clinical pharmacokinetic data from patients with atopic dermatitis, pimecrolimus permeates less through skin than tacrolimus and much less than corticosteroids. It, thus, has a lower potential for transcutaneous resorption after topical administration, resulting in a lower risk of systemic effects. Pimecrolimus has high anti‐inflammatory activity in animal models of skin inflammation, including a model reflecting neurogenic inflammation, but a more favourable balance of anti‐inflammatory vs. immunosuppressive activity than tacrolimus. Pimecrolimus does not affect sensitization in a murine model of allergic contact dermatitis and has a lower potency in various models of immunosuppression after systemic administration, compared to tacrolimus. In conclusion, the results of preclinical studies show that pimecrolimus has a selective pharmacological profile, suited for effective and safe treatment for inflammatory skin diseases. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Experimental Dermatology Wiley

Pimecrolimus – an anti‐inflammatory drug targeting the skin

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Publisher
Wiley
Copyright
Copyright © 2004 Wiley Subscription Services, Inc., A Wiley Company
ISSN
0906-6705
eISSN
1600-0625
DOI
10.1111/j.0906-6705.2004.00269.x
pmid
15560755
Publisher site
See Article on Publisher Site

Abstract

Abstract: Pimecrolimus is the most recent member of calcineurin inhibitors available for the therapy for inflammatory skin diseases. It targets T‐cells and mast cells and inhibits the production and release of cytokines and other inflammatory mediators, as well as the expression of signals essential for the activation of inflammatory T‐lymphocytes. Pimecrolimus has a cell‐selective mode of action. In contrast to corticosteroids, it does not affect, e.g., Langerhans'cells/dendritic cells (LC/DC), as demonstrated in vitro with human monocyte‐derived DC and in vivo with epidermal LC in mice, nor human primary fibroblasts. As shown in vitro with human skin and by comparison of clinical pharmacokinetic data from patients with atopic dermatitis, pimecrolimus permeates less through skin than tacrolimus and much less than corticosteroids. It, thus, has a lower potential for transcutaneous resorption after topical administration, resulting in a lower risk of systemic effects. Pimecrolimus has high anti‐inflammatory activity in animal models of skin inflammation, including a model reflecting neurogenic inflammation, but a more favourable balance of anti‐inflammatory vs. immunosuppressive activity than tacrolimus. Pimecrolimus does not affect sensitization in a murine model of allergic contact dermatitis and has a lower potency in various models of immunosuppression after systemic administration, compared to tacrolimus. In conclusion, the results of preclinical studies show that pimecrolimus has a selective pharmacological profile, suited for effective and safe treatment for inflammatory skin diseases.

Journal

Experimental DermatologyWiley

Published: Dec 1, 2004

References

  • A novel anti‐inflammatory drug, SDZ ASM 981, for the treatment of skin diseases: in vitro pharmacology
    Grassberger, Grassberger; Baumruker, Baumruker; Enz, Enz
  • Mast cells in allergy and beyond
    Puxeddu, Puxeddu; Piliponsky, Piliponsky; Bachelet, Bachelet; Levi‐Schaffer, Levi‐Schaffer
  • Pimecrolimus does not affect the differentiation, maturation and function of human monocyte‐derived dendritic cells, in contrast to corticosteroids
    Kalthoff, Kalthoff; Chung, Chung; Musser, Musser; Stuetz, Stuetz
  • Effects of pimecrolimus on dendritic cell
    Krummen, Krummen; A Stuetz, A Stuetz; Luger, Luger
  • Effect of percutaneous absorption of hydrocortisone and adrenocortical responsiveness in infants with severe skin disease
    Turpeinen, Turpeinen; Salo, Salo; Leisti, Leisti
  • A novel anti‐inflammatory drug, SDZ ASM 981, for the topical and oral treatment of skin diseases: in vivo pharmacology
    Meingassner, Meingassner; Grassberger, Grassberger; Fahrngruber, Fahrngruber; Moore, Moore; Schuurman, Schuurman; Stütz, Stütz
  • Atopic dermatitis‐like symptoms in hypomagnesaemic hairless rats are prevented and inhibited by systemic or topical SDZ ASM 981
    Neckermann, Neckermann; Bavandi, Bavandi; Meingassner, Meingassner
  • Two distinct action mechanisms of immunophilin‐ligand complexes for the blockade of T‐cell activation
    Matsuda, Matsuda; Shibasaki, Shibasaki; Takehana, Takehana
  • Safety and efficacy of nonsteroid pimecrolimus cream 1% in the treatment of atopic dermatitis in infants
    Ho, Ho; Gupta, Gupta; Kaufmann, Kaufmann

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