Entstehungsgeschichte und präklinisches Profil von Pimecrolimus

Stütz, Anton; Grassberger, Maximilian A.; Meingassner, Josef G.

doi:10.1007/s00105-003-0519-0

Cited by 4 publications

(1 citation statement)

References 18 publications

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“…For oral tacrolimus (Prograf®), only results from small studies on patients with psoriasis have been published so far and the drug is not registered for the oral treatment for skin diseases (6,7). Whereas cyclosporin A and tacrolimus were originally developed for the prevention of graft organ rejection in transplantation patients, and are widely used in this indication, pimecrolimus was specifically developed for the treatment of inflammatory skin diseases (8). Topical pimecrolimus as cream 1% (Elidel®) proved to be highly effective, safe and well tolerated in patients with atopic dermatitis (9–11).…”

Section: Introductionmentioning

confidence: 99%

Pimecrolimus – an anti‐inflammatory drug targeting the skin

Grassberger

Steinhoff²,

Schneider

et al. 2004

Experimental Dermatology

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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 antiinflammatory 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.

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Section: Introductionmentioning

confidence: 99%

Pimecrolimus – an anti‐inflammatory drug targeting the skin

Grassberger

Steinhoff²,

Schneider

et al. 2004

Experimental Dermatology

Self Cite

111

View full text Add to dashboard Cite

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Natural and Nature‐Inspired Macrocycles

Wessjohann

Bartelt

Brandt

2017

Practical Medicinal Chemistry With Macrocycles

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Novel pharmacological approaches in the treatment of psoriasis

Schleyer

Landthaler

Szeimies

2004

Acad Dermatol Venereol

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Progress in the understanding of psoriasis as a T-cell mediated inflammatory disease has led to the development of new immunomodulatory therapies. Currently the main focus is on the so-called biologics (or biological agents), including fusion proteins, monoclonal antibodies, cytokines and selective receptors. They mainly target single steps in the complex cascade of humoral and cellular inflammatory immuno-mechanisms that finally lead to the accelerated growth of epidermal and vascular cells in the psoriatic lesions. The most promising and advanced biological agents are discussed along with their influence on the critical pathophysiological steps in psoriasis, including depletion of T cells, blockade of initial T-cell activation and T-cell receptor (TCR) stimulation, blockade of costimulatory signals and T-cell proliferative signals as well as restoration of the T helper type 1 (Th1)/Th2 balance by diminishing type 1 cytokines and administration of type 2 cytokines. In addition to the biological agents, further development of 'classical' dermatological therapies, such as retinoids, or the discovery of new indications for non-dermatological agents contribute to the novel pharmacological approaches in the treatment of psoriasis.

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Entstehungsgeschichte und präklinisches Profil von Pimecrolimus

Cited by 4 publications

References 18 publications

Pimecrolimus – an anti‐inflammatory drug targeting the skin

Pimecrolimus – an anti‐inflammatory drug targeting the skin

Natural and Nature‐Inspired Macrocycles

Novel pharmacological approaches in the treatment of psoriasis

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