Topical Tacrolimus: A Review of Its Uses in Dermatology

Denise K. Woo; William D. James


Dermatitis. 2005;16(1):6-21. 

In This Article

Abstract and Introduction

Tacrolimus is one of the newer immunosuppressants that act by inhibiting T-cell activation and cytokine release. It is approved for the treatment of atopic dermatitis, and its safety and efficacy have been extensively studied in large-scale randomized controlled trials and open-label studies worldwide involving over 12,000 patients and up to 3 years of follow-up. Since its introduction, anecdotal reports and case series have found topical tacrolimus also to be effective and well tolerated in patients with a variety of other skin disorders, including other types of eczema, papulosquamous disorders, disorders of cornification, rosacea, other inflammatory skin conditions, vesiculobullous diseases, vitiligo, connective-tissue diseases, graft-versus-host disease, and follicular disorders. This paper reviews the currently available evidence on the use of topical tacrolimus for these conditions, as well as its safety profile and cost-effectiveness. Tacrolimus does appear to offer a safe and efficacious alternative that minimizes the need for topical glucocorticoids and does not cause skin atrophy. However, the risk of systemic absorption is increased with generalized disruption of the skin barrier. Further large-scale studies are needed to clarify the efficacy of topical tacrolimus in a variety of conditions for which anecdotal reports of success exist, especially in regard to different racial groups and in comparison to (as well as in combination with) other existing therapies. Long-term safety data should continue to be monitored and reported.

Topical glucocorticoids represent the mainstay of therapy for a variety of skin disorders. However, their clinical use is limited by local and potential systemic side effects, including skin atrophy, telangiectasia, striae, diabetes mellitus, and osteoporosis. Thus, there is a large demand for alternatives, and considerable emphasis has recently been placed on the macrolide lactones, particularly tacrolimus.

Tacrolimus is an immunomodulator macrolide that was isolated from the soil microbe Streptomyces tsukubaensis in 1984 in Japan. The name "tacrolimus" is derived from a combination of the words "Tsukuba" (the name of the mountain from which the soil sample was extracted), "macrolide" (the chemical class), and "immunosuppressant."[1]


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