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他卡西醇,一种新型、首创的、局部用芳香烃受体激动剂,用于治疗银屑病。

Tapinarof, a Novel, First-in-Class, Topical Therapeutic Aryl Hydrocarbon Receptor Agonist for the Management of Psoriasis.

出版信息

J Drugs Dermatol. 2023 Aug 1;22(8):779-784. doi: 10.36849/jdd.7317.

DOI:10.36849/jdd.7317
PMID:37556512
Abstract

Topical treatments remain the foundation of psoriasis management. Tapinarof (VTAMA®; Dermavant Sciences, Inc.) is a first-in-class, non-steroidal, topical, aryl hydrocarbon receptor (AhR) agonist approved by the US Food and Drug Administration for the treatment of plaque psoriasis in adults and is under investigation for the treatment of psoriasis in children, and atopic dermatitis in adults and children down to 2 years old. Here, we review the mechanism of action of tapinarof and the PSOARING phase 3 trial program in mild to severe psoriasis. AhR is a ligand-dependent transcription factor involved in maintaining skin homeostasis. Tapinarof specifically binds to AhR to decrease proinflammatory cytokines, decrease oxidative stress, and promote skin barrier normalization. In two identical, randomized, 12-week pivotal phase 3 trials, PSOARING 1 and 2, tapinarof cream 1% once daily (QD) demonstrated significant efficacy versus vehicle and was well tolerated in adults with mild to severe psoriasis. In the PSOARING 3 long-term extension trial of repeated, intermittent tapinarof cream in eligible patients completing the pivotal trials, a high rate of complete disease clearance (40.9%) and a remittive effect of approximately 4 months off therapy were demonstrated over 52 weeks, with no tachyphylaxis. The most common adverse event, folliculitis, was mostly mild or moderate and resulted in a low trial discontinuation rate in PSOARING 1 and 2 (≤1.8%). Tapinarof cream 1% QD provides a novel, non-steroidal, topical treatment option for patients with psoriasis and is highly effective and well tolerated with long-term use including when applied to sensitive and intertriginous skin. Bobonich M, Gorelick J, Aldredge L, et al. Tapinarof, a novel, first-in-class, topical therapeutic aryl hydrocarbon receptor agonist for the management of psoriasis. J Drugs Dermatol. 2023;22(8):779-784. doi:10.36849/JDD.7317.

摘要

局部治疗仍然是银屑病管理的基础。他卡西醇(VTAMA®; Dermavant Sciences,Inc.)是一种首创的、非甾体类、局部、芳香烃受体(AhR)激动剂,已被美国食品和药物管理局批准用于治疗成人斑块状银屑病,目前正在研究用于儿童银屑病和 2 岁以下儿童特应性皮炎的治疗。在这里,我们回顾了他卡西醇的作用机制和 PSOARING 三期临床试验方案在轻度至重度银屑病中的应用。AhR 是一种配体依赖性转录因子,参与维持皮肤内稳态。他卡西醇特异性地与 AhR 结合,以减少促炎细胞因子,减少氧化应激,并促进皮肤屏障正常化。在两项相同的、随机的、为期 12 周的关键 3 期临床试验 PSOARING 1 和 2 中,他卡西醇乳膏 1%每日一次(QD)与载体相比显示出显著的疗效,并且在轻度至重度银屑病成人中具有良好的耐受性。在符合条件的患者完成关键试验后,在 PSOARING 3 长期扩展试验中重复间歇性他卡西醇乳膏治疗,在 52 周内显示出较高的完全疾病清除率(40.9%)和大约 4 个月的缓解作用,且无脱敏作用。最常见的不良事件,毛囊炎,大多为轻度或中度,导致 PSOARING 1 和 2 中的试验停药率较低(≤1.8%)。他卡西醇乳膏 1%QD 为银屑病患者提供了一种新的非甾体类局部治疗选择,长期使用(包括用于敏感和皱褶部位皮肤)具有高度疗效和良好的耐受性。Bobonich M、Gorelick J、Aldredge L、等。他卡西醇,一种新型首创的、局部治疗芳香烃受体激动剂,用于管理银屑病。J 皮肤病药物杂志。2023;22(8):779-784。doi:10.36849/JDD.7317.

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