Topical Pimecrolimus

Abstract

Topical pimecrolimus 1% cream (Elidel) [hereafter referred to as topical pimecrolimus] is a nonsteroidal alternative in the treatment of pediatric atopic dermatitis. In vehicle-controlled, short-term, continuous-use trials in pediatric patients with mild to moderate atopic dermatitis, topical pimecrolimus was effective in treating disease symptoms. Topical pimecrolimus was effective in preventing disease flares and reducing the need for topical corticosteroids in longer term, intermittent-use trials. In addition, topical pimecrolimus was associated with improvements in the health-related quality of life (HR-QOL) of pediatric patients with atopic dermatitis and their parents. In vehicle-controlled trials, topical pimecrolimus was generally as well tolerated as vehicle. Topical pimecrolimus showed similar efficacy to topical tacrolimus 0.03% ointment (hereafter topical tacrolimus) in a short-term, continuous-use trial and the two agents had a generally similar tolerability profile. Although comparative data between topical pimecrolimus and topical corticosteroids are lacking in pediatric patients, and the long-term tolerability (beyond 1-2 years) of topical pimecrolimus is yet to be established, topical pimecrolimus is a useful agent in the management of pediatric patients with mild to moderate atopic dermatitis who do not achieve satisfactory treatment with other topical pharmacologic treatments, including topical corticosteroids.

Contemporary Role of Topical Calcineurin Inhibitors: A Pediatric Dermatology Perspective

“…Both tacrolimus ointment and pimecrolimus cream have demonstrated efficacy for the short-term treatment of acute eczema in pivotal clinical trials. 8,9 The primary efficacy outcomes of the vehicle-controlled trials are summarized in Table 1.…”

“…Several short-term active-comparator trials of TCIs vs topical corticosteroids (TCS) have also been published (reviewed in McCollum et al 9 and in Yang and Curran 8 ). Briefly, 3 weeks of treatment with tacrolimus 0.03% 15,16 or 0.1% 15 has been shown to be significantly more effective than hydrocortisone acetate 1% in pediatric patients with moderate to severe AD, and 0.03% tacrolimus has been shown to be as effective as methylprednisolone aceponate 0.1% in children and adolescents with severe or very severe AD.…”

Synthesis and Characterization of an Epimer of Tacrolimus, an Immunosuppressive Drug

“…Tacrolimus ( 1 ), a macrolide lactone also known as FK-506, fugimycin, or tsukubaenolide, is a marketed drug (Prograf, Advagraf, Protopic) used as an immunosuppressive agent to prevent rejection of transplanted organs and also topically in a number of conditions . Tacrolimus is produced by the bacterium Streptomyces tsukubaensis , and its name is an acronym reportedly derived from “ t sukuba m acrol ide im m u no s uppressant”.…”