治疗中至重度斑块型银屑病的新药——氘可来昔替尼

Deucravacitinib,a new drug in treatment of moderate-to-severe plaque psoriasis

氘可来昔替尼是一种口服的、选择性变构酪氨酸激酶2(TYK2)抑制药,其通过选择性地与TYK2的调控结构域结合,从而抑制TYK2及其下游的功能而发挥作用。氘可来昔替尼于2022-09-09获美国食品和药物管理局批准,用于治疗适合系统治疗或光疗的中至重度斑块型银屑病成人患者,其是全球唯一获批的TYK2抑制药,也是近10年来口服治疗中至重度斑块型银屑病的首个创新药。氘可来昔替尼在改善皮损清除方面疗效显著,其安全性和耐受性良好,最常见的药物不良反应包括上呼吸道感染、血液磷酸肌酸激酶升高等。本文对其作用机制、药效学、药代动力学、临床研究及安全性做一介绍。

Deucravacitinib is a first-in-class,oral,selective,allosteric tyrosine kinase 2(TYK2)inhibitor,which can bind to the regulatory domain of TYK2,stabilizing an inhibitory interaction between the regulatory and the catalytic domains of the enzyme.It was approved for the treatment of adults with moderate-to-severe plaque psoriasis who are candidates for systemic therapy or phototherapy by U.S.Food and Drug Administration on September 9,2022.Deucravacitinib is the only approved TYK2 inhibitor worldwide and the first innovation in oral treatment for moderate-to-severe plaque psoriasis in nearly 10 years.Deucravacitinib is effective in improving the clearance of skin lesions,which has a well-demonstrated safety and tolerability profile.Most common adverse drug reactions include upper respiratory infections and increased blood creatine phosphokinase.This article reviewed the mechanism,pharmacodynamics,pharmacokinetics,clinical evaluation,and safety of Deucravacitinib in order to provide a reference for clinical application.