Unit of Respiratory Medicine, Department of Experimental Medicine, University of Rome "Tor Vergata", Rome, Italy.
Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, London, UK.
Drugs. 2020 Nov;80(17):1799-1809. doi: 10.1007/s40265-020-01412-x.
Erdosteine is a drug approved for the treatment of acute and chronic pulmonary diseases, originally developed as a mucolytic agent. It belongs to the thiol-based family of drugs that are known to also possess potentially important antioxidant and anti-inflammatory properties, and exhibit antibacterial activity against a variety of medically important bacterial species. Erdosteine is a prodrug that is metabolized to the ring-opening compound metabolite M1 (MET 1), which has mucolytic properties. Experimental studies have documented that erdosteine prevents or reduces lung tissue damage induced by oxidative stress and, in particular, that Met 1 also regulates reactive oxygen species production. The RESTORE study, which has been the only trial that investigated the effects of a thiol-based drug in chronic obstructive pulmonary disease (COPD) frequent exacerbators, documented that erdosteine significantly reduces the risk of acute exacerbations of COPD (AECOPDs), shortens their course, and also decreases the risk of hospitalization from COPD. The preventive action of erdosteine on AECOPDs was not affected by the presence or absence of inhaled corticosteroids (ICSs) or blood eosinophil count. These findings clearly contrast with the Global Initiative for Chronic Obstructive Lung Disease strategy's approach to use erdosteine only in those COPD patients not treated simultaneously with an ICS. Furthermore, they support the possibility of using erdosteine in a step-down approach that in COPD is characterized by the withdrawal of the ICS.
厄多司坦是一种用于治疗急性和慢性肺部疾病的药物，最初被开发为黏液溶解剂。它属于基于巯基的药物家族，已知具有潜在重要的抗氧化和抗炎特性，并对多种重要的医学细菌具有抗菌活性。厄多司坦是一种前药，可代谢为具有黏液溶解特性的开环化合物代谢物 M1（MET 1）。实验研究表明，厄多司坦可预防或减轻氧化应激引起的肺组织损伤，特别是 MET 1 还可调节活性氧的产生。RESTORE 研究是唯一一项研究基于巯基药物在慢性阻塞性肺疾病（COPD）频繁加重者中的作用的试验，该研究表明厄多司坦可显著降低 COPD 急性加重（AECOPD）的风险，缩短其病程，并降低因 COPD 住院的风险。厄多司坦对 AECOPD 的预防作用不受吸入性皮质类固醇（ICS）或血嗜酸性粒细胞计数的影响。这些发现与全球慢性阻塞性肺疾病倡议策略的方法形成鲜明对比，即仅在未同时使用 ICS 的 COPD 患者中使用厄多司坦。此外，它们支持在 COPD 中以降级方法使用厄多司坦的可能性，该方法的特征是停用 ICS。
