DiRuggiero Margaret, Mancuso-Stewart Elizabeth, DiRuggiero Douglas, Zirwas Matt
United States Air Force Academy, Colorado Springs, CO.
Ohio University Heritage College of Osteopathic Medicine, Dublin, OH.
Skinmed. 2023 Sep 29;21(4):264-268. eCollection 2023.
Topical corticosteroids have remained the initial and long-term topical treatment option for inflammatory dermatitis conditions since the 1950s. A number of non-steroidal topicals for treatment of inflammatory dermatoses have been developed in the recent decades, such as topical calcineurin inhibitors (tacrolimus ointment and pimecrolimus cream), vitamin D analogues, and phophodiesterase-4 inhibitors (crisaborole), but none had the combination of broad therapeutic range, relatively rapid onset of action, tolerability, and wide-spread clinical success that allowed topical glucocorticosteroids to remain the mainstay of therapy. This situation has shifted dramatically with three non-steroidal new molecular entities, each with completely different mechanisms of action, receiving approval of the Food and Drug Administration (FDA) in the past year. Topical ruxolitinib, a Janus kinase (JAK) inhibitor, was the first to receive FDA approval, specifically for treating atopic dermatitis, and was the subject of the first report in this series. Subsequently, topical tapinarof, an aryl hydrocarbon receptor modulating agent, was approved by the FDA for treating plaque psoriasis in May 2022 and was the focus of the second report in this series. Finally, and most recently in July 2022, topical roflumilast, a highly potent phosphodiesterase-4 inhibitor, has received FDA approval for treating plaque psoriasis, and is the subject of the third and final report in this series. In addition to their unique mechanisms of action and spectra of activity, each of these agents has unique clinical characteristics, including degree of efficacy, rapidity of onset of efficacy, potential remittive effects, and safety and tolerability profiles. In this three-part series, we reviewed and summarized the data surrounding each agent, providing a comprehensive overview that would allow dermatologists to integrate them confidently and appropriately into treatment paradigms. Part three focuses on topical roflumilast, a highly potent phosphodiesterase-4 inhibitor.
自20世纪50年代以来，局部用皮质类固醇一直是炎症性皮肤病的初始和长期局部治疗选择。近几十年来，已经开发出多种用于治疗炎症性皮肤病的非甾体局部用药，如局部用钙调神经磷酸酶抑制剂（他克莫司软膏和吡美莫司乳膏）、维生素D类似物和磷酸二酯酶-4抑制剂（克立硼罗），但没有一种药物具有广泛的治疗范围、相对较快的起效速度、耐受性以及广泛的临床成功性的组合，使得局部用糖皮质激素仍然是治疗的主要手段。随着三种具有完全不同作用机制的非甾体新分子实体在过去一年获得美国食品药品监督管理局（FDA）的批准，这种情况发生了巨大变化。局部用鲁索替尼，一种 Janus激酶（JAK）抑制剂，是第一个获得FDA批准的药物，专门用于治疗特应性皮炎，并且是本系列第一篇报告的主题。随后，局部用他扎罗汀，一种芳烃受体调节剂，于2022年5月获得FDA批准用于治疗斑块状银屑病，并且是本系列第二篇报告的重点。最后，也是最近在2022年7月，局部用罗氟司特，一种高效的磷酸二酯酶-4抑制剂，已获得FDA批准用于治疗斑块状银屑病，并且是本系列第三篇也是最后一篇报告的主题。除了其独特的作用机制和活性谱外，这些药物中的每一种都具有独特的临床特征，包括疗效程度、起效速度、潜在的缓解作用以及安全性和耐受性。在这个三部分系列中，我们回顾并总结了围绕每种药物的数据，提供了一个全面的概述，使皮肤科医生能够自信且适当地将它们纳入治疗方案。第三部分重点介绍局部用罗氟司特，一种高效的磷酸二酯酶-4抑制剂。
