Paton D M
University of Auckland School of Medical Sciences, Pharmacology & Clinical Pharmacology, Auckland, New Zealand.
Drugs Today (Barc). 2017 Apr;53(4):239-245. doi: 10.1358/dot.2017.53.4.2604174.
Atopic dermatitis (AD) is an extremely common condition affecting as many as 10-20% of children and 2-10% of adults. A particularly distressing symptom of AD is pruritus. One of the important aspects of AD is inflammation associated with increased activity of phosphodiesterase 4 (PDE4), resulting in decreased intracellular levels of cyclic adenosine monophosphate, which in turn causes increased production of inflammatory cytokines. Crisaborole was developed as a small-molecule, boron-based, selective PDE4 inhibitor that can be used topically. Clinical trials have demonstrated its efficacy in treating patients with mild to moderate AD, resulting in significant relief of pruritus. Unlike PDE4 inhibitors that act systemically, crisaborole does not cause significant gastrointestinal adverse effects. The most common adverse effect has been temporary stinging and burning in about 4% of patients upon application of the 2% ointment. To date there is no evidence of atrophy, telangiectasia or hypopigmentation resulting from its use. Crisaborole is the first topically applied PDE4 inhibitor to be approved by the FDA for use in AD.
特应性皮炎（AD）是一种极为常见的病症，影响着多达10%-20%的儿童和2%-10%的成年人。AD一个特别令人苦恼的症状是瘙痒。AD的一个重要方面是与磷酸二酯酶4（PDE4）活性增加相关的炎症，这导致细胞内环磷酸腺苷水平降低，进而导致炎性细胞因子产生增加。克立硼罗是一种开发用于局部使用的小分子、基于硼的选择性PDE4抑制剂。临床试验已证明其在治疗轻至中度AD患者方面的疗效，能显著缓解瘙痒。与全身性作用的PDE4抑制剂不同，克立硼罗不会引起明显的胃肠道不良反应。最常见的不良反应是在约4%的患者使用2%软膏时出现暂时的刺痛和烧灼感。迄今为止，尚无证据表明使用它会导致萎缩、毛细血管扩张或色素减退。克立硼罗是首个获美国食品药品监督管理局（FDA）批准用于AD的局部应用PDE4抑制剂。
