Bornhövd Elke C, Burgdorf Walter H C, Wollenberg Andreas
Ludwig-Maximillians-University, Department of Dermatology and Allergology, Munich, Germany.
Curr Opin Investig Drugs. 2002 May;3(5):708-12.
Tacrolimus (FK-506; Fujisawa Pharmaceutical Co Ltd) and pimecrolimus (SDZ-ASM-981; Novartis AG) are topical immunomodulators, which provide an alternative to glucocorticosteroids for the topical treatment of atopic dermatitis and other inflammatory dermatoses. Both substances form a complex with cytosolic immunophilins. The complex blocks calcineurin and inhibits the transcription of NF-AT-dependent pro-inflammatory cytokine genes. Multicenter, randomized, double-blind clinical trials have shown the efficacy of both substances in atopic dermatitis. We review the physicochemical characteristics, mode of action, pharmacokinetic data, side effects, results of the clincal trials and further indications for tacrolimus and pimecrolimus.
他克莫司（FK - 506；藤泽制药有限公司）和吡美莫司（SDZ - ASM - 981；诺华公司）是局部免疫调节剂，它们为特应性皮炎和其他炎症性皮肤病的局部治疗提供了糖皮质激素的替代药物。这两种物质均与胞质亲免蛋白形成复合物。该复合物可阻断钙调神经磷酸酶并抑制NF - AT依赖性促炎细胞因子基因的转录。多中心、随机、双盲临床试验已证明这两种物质在特应性皮炎治疗中的有效性。我们综述了他克莫司和吡美莫司的物理化学特性、作用方式、药代动力学数据、副作用、临床试验结果及其他适应证。
