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阿普斯特用于治疗银屑病。

Apremilast for the treatment of psoriasis.

作者信息

Chimenti Maria Sole, Gramiccia Talia, Saraceno Rosita, Bianchi Luca, Garofalo Virginia, Buonomo Oreste, Perricone Roberto, Chimenti Sergio, Chiricozzi Andrea

机构信息

University of Rome "Tor Vergata", Rheumatology, Allergology and Clinical Immunology , Rome , Italy.

出版信息

Expert Opin Pharmacother. 2015;16(13):2083-94. doi: 10.1517/14656566.2015.1076794. Epub 2015 Aug 4.

Abstract

INTRODUCTION

Psoriasis is a chronic inflammatory skin disease characterized by dysregulation of the immune system and release of pro-inflammatory mediators. Drugs available for psoriasis show some limits as tolerability and route of administration. Apremilast , Otezla®, is an oral small molecule recently approved for the treatment of patients with moderate-to-severe plaque psoriasis. Compared to biologics that target a single cytokine, apremilast, degrading phosphodiesterase 4 (PDE4), interferes with cyclic anti-microbial peptides, which is involved in the transduction of intracellular signals, controlling the balance of pro-inflammatory and anti-inflammatory signals.

AREAS COVERED

This review reported the latest data available from Phase I, II and III trials on apremilast for the treatment of plaque psoriasis. A focus on the clinical management of apremilast, safety and clinical efficacy based on two pivotal clinical trials (ESTEEM 1 and ESTEEM 2) currently ongoing was described. A systematic search was conducted using the PubMed Medline database for primary articles.

EXPERT OPINION

Apremilast treatment was demonstrated effective and well tolerated in Phase II and III clinical trials. Several drug peculiarities, such as the low frequency of adverse events and the oral route of administration, make apremilast an innovative treatment for moderate-to-severe psoriasis.

摘要

引言

银屑病是一种慢性炎症性皮肤病,其特征为免疫系统失调和促炎介质的释放。现有的银屑病治疗药物在耐受性和给药途径方面存在一些局限性。阿普米司特(Otezla®)是一种口服小分子药物,最近被批准用于治疗中度至重度斑块状银屑病。与靶向单一细胞因子的生物制剂相比,阿普米司特通过降解磷酸二酯酶4(PDE4),干扰环化抗菌肽,而环化抗菌肽参与细胞内信号转导,控制促炎和抗炎信号的平衡。

涵盖领域

本综述报告了阿普米司特治疗斑块状银屑病的I期、II期和III期试验的最新数据。基于目前正在进行的两项关键临床试验(ESTEEM 1和ESTEEM 2),描述了对阿普米司特临床管理、安全性和临床疗效的关注。使用PubMed Medline数据库对原始文章进行了系统检索。

专家意见

在II期和III期临床试验中,阿普米司特治疗被证明有效且耐受性良好。阿普米司特的一些药物特性,如不良事件发生率低和口服给药途径,使其成为中度至重度银屑病的一种创新治疗方法。

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