Division of Pulmonary, Allergy and Critical Care Medicine, Department of Internal Medicine, Seoul St. Mary's Hospital, College of Medicine, The Catholic University of Korea, Seoul, Korea.
Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Seoul Metropolitan Government Seoul National University Boramae Medical Center, Seoul, Korea.
Korean J Intern Med. 2020 Mar;35(2):276-283. doi: 10.3904/kjim.2020.035. Epub 2020 Feb 28.
Phosphodiesterase-4 inhibitors (PDE4Is) are potent anti-inf lammatory agents and roflumilast has been used to prevent acute exacerbation of chronic obstructive pulmonary disease (COPD). Roflumilast decreases neutrophil migration, restores cystic fibrosis transmembrane conductance regulator activity, and recovers glucocorticoid effects. A forced expiratory volume in 1 second of < 50%, a chronic bronchitis phenotype, high blood eosinophil levels, and a history of hospitalization are biomarkers for predicting responses to roflumilast. Adverse effects are common in clinical practice. An inhaled PDE4I has recently been developed and is under clinical trial. CHF6001 and RPL554 exhibit promise and may be future treatment options for COPD.
磷酸二酯酶-4 抑制剂（PDE4Is）是一种强效的抗炎药物，利奥西呱已被用于预防慢性阻塞性肺疾病（COPD）的急性加重。利奥西呱可减少中性粒细胞迁移，恢复囊性纤维化跨膜电导调节剂的活性，并恢复糖皮质激素的作用。一秒钟用力呼气容积（FEV1）<50%、慢性支气管炎表型、高血嗜酸性粒细胞水平和住院史是预测利奥西呱反应的生物标志物。不良反应在临床实践中很常见。最近开发了一种吸入性 PDE4I，正在临床试验中。CHF6001 和 RPL554 有希望成为 COPD 的未来治疗选择。
