Topical Calcineurin Inhibitors

Topical calcineurin inhibitors are non-steroidal immunomodulators. By inhibiting the enzyme calcineurin in immune cells, they interfere with the production of a number of inflammatory substances that contribute to skin inflammation in atopic dermatitis. These medicines have also been shown to inhibit the release of histamine, which can cause itching.

Tacrolimus ointment, marketed by Fujisawa Healthcare Inc. as Protopic® 0.03 percent for children 2 to 15 years of age, and 0.03 percent and 0.1 percent for adults, has been approved by the Food and Drug Administration for short-term and intermittent long-term use in moderate-to-severe eczema. Long-term monitoring of patients treated with tacrolimus has created a global database of over 13,000 patients worldwide, and safety and efficacy data are available for up to four years of tacrolimus use.

Pimecrolimus, a newer calcineurin inhibitior, was developed specifically to treat inflammatory skin conditions. Pimecrolimus cream 1 percent has been shown to be effective for atopic dermatitis with little systemic absorption. Pimecrolimus (Elidel®) cream 1 percent, marketed by Novartis Pharmaceutical Corporation, has been approved by the Food and Drug Administration for use in patients 2 years of age or older with mild to moderate atopic dermatitis. It has been studied extensively in children with atopic dermatitis in large multicenter controlled trials with application twice daily for up to 12 months.