Document Detail

Topical calcineurin inhibitors in cutaneous lupus erythematosus.
MedLine Citation:
PMID:  18797893     Owner:  NLM     Status:  MEDLINE    
Calcineurin inhibitors are immunomodulator macrolides that block T cell activation in the skin. These molecules bind to macrophilin 12 to form a complex capable of blocking calcineurin, a protein that dephosphorylates, and thereby activates, the cytoplasmic subunit of nuclear factor of activated T cells (NF-AT). Thus, in the presence of calcineurin inhibitors, NF-AT cannot enter the nucleus and interact with the promoter regions of many cytokine genes. In addition to T cells, calcineurin inhibitors have also been shown to inhibit the activation of a number of other cell types in the skin immune system, including eosinophils, basophils, and Langerhans cells. These drugs are highly effective in treating atopic dermatitis, even in monotherapy, and they result in rapid, progressive, and sustained improvement. Additionally, calcineurin inhibitors are well tolerated for long-term treatment, and there are virtually no contraindications when using these medications on the face, eyelids, flexural skin, or mucous membranes. Although calcineurin inhibitors are immunomodulators, no significantly increased incidence of infections can be detected during therapy. Cutaneous lupus erythematosus is a chronic, autoimmune, inflammatory skin condition with a wide spectrum of skin manifestations, which presents a therapeutic challenge for dermatologists. In this review, the current treatment options for the different clinical subtypes of this disease are discussed. Therapy with topical calcineurin inhibitors is emphasized, and advantages and drawbacks, effects and side effects, treatment protocols, dosage, and expected outcome are described in detail.
Miklós Sárdy; Thomas Ruzicka; Annegret Kuhn
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review     Date:  2008-09-17
Journal Detail:
Title:  Archives of dermatological research     Volume:  301     ISSN:  1432-069X     ISO Abbreviation:  Arch. Dermatol. Res.     Publication Date:  2009 Jan 
Date Detail:
Created Date:  2008-12-24     Completed Date:  2009-02-24     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8000462     Medline TA:  Arch Dermatol Res     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  93-8     Citation Subset:  IM    
Department of Dermatology and Allergology, Ludwig-Maximilians University, Frauenlobstr. 9-11, 80337, Munich Germany.
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MeSH Terms
Administration, Topical
Calcineurin / antagonists & inhibitors*
Clinical Protocols
Immunologic Factors / administration & dosage,  adverse effects,  therapeutic use*
Lupus Erythematosus, Cutaneous / drug therapy*,  metabolism,  pathology,  physiopathology
Lymphocyte Activation / drug effects,  immunology
NFATC Transcription Factors / immunology
Skin / drug effects,  metabolism,  pathology*
T-Lymphocytes / drug effects,  immunology,  metabolism*
Tacrolimus Binding Protein 1A / metabolism
Treatment Outcome
Reg. No./Substance:
0/Immunologic Factors; 0/NFATC Transcription Factors; EC; EC 5.2.1.-/Tacrolimus Binding Protein 1A

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