Tacrolimus is a topical ointment originally produced by Astellas Pharma under the brand name Protopic and approved by the U.S. Food and Drug Administration to treat atopic dermatitis, or eczema. Tacrolimus can also be used to treat morphea.
This topical treatment is not to be confused with the oral preparation of tacrolimus, which is prescribed under the brand name Astagraf to prevent organ rejection.
How tacrolimus works
Tacrolimus is an antibiotic with immunosuppressive effects. It works by binding to a protein called FKBP. The complex of tacrolimus and FKBP together inhibit calcineurin phosphatase, an enzyme that normally activates immune cells called T-cells. Inhibiting this enzyme blocks the activation of T-cells, which, in turn, prevents the activation and proliferation of antibody-producing B-cells. When applied topically, tacrolimus reduces the inflammatory immune response.
Tacrolimus in clinical trials
A study, published in the Journal of Drugs in Dermatitis, showed that tacrolimus can be used to treat morphea. One patient was treated with 0.1 percent tacrolimus ointment twice a day for eight weeks. Some lesions on the same patient were left untreated as a control. After eight weeks, the treated lesions had softened, and the inflammation had disappeared. Five months later, the site of the treated lesions was almost normal in appearance.
Another randomized, double-blind, placebo-controlled pilot study, published in the American Journal of Clinical Dermatology, showed that 0.1 percent tacrolimus can be used to treat active plaque morphea. In each of the 10 patients, one lesion was treated with tacrolimus ointment, and one with a placebo ointment twice daily for 12 weeks. At the end of the study, significant improvements were observed in lesions treated with tacrolimus compared with lesions treated with placebo, based on both lesion size and clinical feature scores such as color and skin thickness.
Additional information
Tacrolimus is used as an alternative to treating morphea lesions with steroid creams or ointments, such as hydrocortisone. However, once the scleroderma lesions have “burned out” or passed the stage of active inflammation, the color change and skin thickening in the affected region appears to be permanent. The medication is, therefore, not recommended for the treatment of burnt-out lesions.
Side effects associated with tacrolimus include itching and burning, headaches, and flu-like symptoms. Tacrolimus should not be used while drinking alcohol because it may make some of the side effects worse.
Many other medications may interact with tacrolimus, and its use should be discussed with the prescribing physician.
Some patients using tacrolimus have later developed skin cancer or lymphoma; the FDA has updated product information for tacrolimus ointments to include this warning.
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