Igarashi Atsuyuki, Tsuji Gaku, Murata Ryusei, Fukasawa Shuichi, Yamane Satoshi
Igarashi Dermatology Higashigotanda, Tokyo, Japan.
Research and Clinical Center for Yusho and Dioxin, Kyushu University, Fukuoka, Japan.
J Dermatol. 2025 Feb;52(2):247-255. doi: 10.1111/1346-8138.17587. Epub 2024 Dec 15.
Tapinarof is a nonsteroidal, topical, aryl hydrocarbon receptor agonist approved for the treatment of atopic dermatitis (AD) in Japanese patients aged ≥12 years. We evaluated the efficacy and safety of tapinarof in Japanese pediatric patients aged 2 to 11 years with AD in a phase 2, multicenter, randomized, double-blind, vehicle-controlled trial. Eligible patients (N = 121) were randomized 1:1:1 to receive tapinarof cream 0.5%, tapinarof cream 1%, or vehicle cream once daily for 8 weeks. At week 8, the least-squares mean percent change from baseline in Eczema Area and Severity Index (EASI) score (the primary endpoint) was -81.29% in the tapinarof 0.5% group, -77.62% in the tapinarof 1% group, and - 18.56% in the vehicle group. Reductions in EASI score at week 8 were significantly greater in the tapinarof groups than in the vehicle group (p < 0.0001 for both comparisons). The proportion of patients with ≥75% improvement from baseline in EASI score at week 8 was 77.5% in the tapinarof 0.5% group, 70.7% in the tapinarof 1% group, and 15.0% in the vehicle group. The proportion of patients who achieved an Investigator's Global Assessment score of 0 (clear) or 1 (almost clear) with ≥2-grade improvement from baseline at week 8 was 32.5% in the tapinarof 0.5% group, 43.9% in the tapinarof 1% group, and 17.5% in the vehicle group. No treatment-related serious adverse events (AEs) were reported; all of the AEs were mild or moderate. Common AEs in tapinarof-treated patients included gastroenteritis, application site irritation, and nasopharyngitis. The incidence of trial discontinuations due to AEs was low in tapinarof-treated patients (one patient for each strength). In summary, both strengths of tapinarof cream demonstrated greater efficacy than vehicle cream and were well tolerated in Japanese pediatric patients with AD.
他扎罗汀是一种非甾体类局部用芳烃受体激动剂,已被批准用于治疗年龄≥12岁的日本特应性皮炎(AD)患者。我们在一项2期、多中心、随机、双盲、赋形剂对照试验中评估了他扎罗汀在2至11岁日本AD儿科患者中的疗效和安全性。符合条件的患者(N = 121)按1:1:1随机分组,分别接受0.5%他扎罗汀乳膏、1%他扎罗汀乳膏或赋形剂乳膏,每日一次,共8周。在第8周时,0.5%他扎罗汀组湿疹面积和严重程度指数(EASI)评分(主要终点)相对于基线的最小二乘平均变化百分比为-81.29%,1%他扎罗汀组为-77.62%,赋形剂组为-18.56%。他扎罗汀组在第8周时EASI评分的降低幅度显著大于赋形剂组(两项比较的p均<0.0001)。在第8周时,EASI评分较基线改善≥75%的患者比例,0.5%他扎罗汀组为77.5%,1%他扎罗汀组为70.7%,赋形剂组为15.0%。在第8周时,达到研究者整体评估评分为0(清除)或1(几乎清除)且较基线改善≥2级的患者比例,0.5%他扎罗汀组为32.5%,1%他扎罗汀组为43.9%,赋形剂组为17.5%。未报告与治疗相关的严重不良事件(AE);所有AE均为轻度或中度。接受他扎罗汀治疗的患者常见AE包括肠胃炎、用药部位刺激和鼻咽炎。因AE导致试验中断的发生率在接受他扎罗汀治疗的患者中较低(每种强度各有1例患者)。总之,两种强度的他扎罗汀乳膏均显示出比赋形剂乳膏更高的疗效,并且在日本AD儿科患者中耐受性良好。