阿布昔替尼：首个全球获批的选择性 JAK1 抑制剂，用于治疗特应性皮炎。
Abrocitinib: First Globally Approved Selective Janus Kinase-1 Inhibitor for the Treatment of Atopic Dermatitis.
机构信息
Department of Chemistry, Conju-probe, San Diego, CA 92121, California, USA.
Department of Chemistry, Bharath University, Chennai, Tamil Nadu, 600126, India.
出版信息
Curr Med Chem. 2023;30(38):4278-4282. doi: 10.2174/0929867330666230216123419.
Atopic dermatitis is epidermal hyperplasia, skin barrier dysfunction, and the aberrant activation of immune cells. Janus kinase (JAK) is a family of cytoplasmic nonreceptor tyrosine kinases that consists of four members, such as JAK1, JAK2, JAK3, and TYK2. The JAK signaling pathway plays a critical role in a wide range of autoimmune and inflammatory diseases, including atopic dermatitis. Abrocitinib is an orally bioavailable and selective JAK1 inhibitor, and it was approved in January, 2022, for the treatment of atopic dermatitis. The chemical structure and physical properties of abrocitinib, its synthesis, mechanism of action, and pharmacokinetic profile are summarized.
特应性皮炎是表皮过度增生、皮肤屏障功能障碍和免疫细胞异常激活的疾病。Janus 激酶（JAK）是一组细胞质非受体酪氨酸激酶，由四个成员组成，如 JAK1、JAK2、JAK3 和 TYK2。JAK 信号通路在广泛的自身免疫和炎症性疾病中发挥着关键作用，包括特应性皮炎。阿布昔替尼是一种口服生物利用度和选择性 JAK1 抑制剂，于 2022 年 1 月被批准用于治疗特应性皮炎。本文总结了阿布昔替尼的化学结构和物理性质、合成、作用机制和药代动力学特征。
Zotero 插件