University of Rome Tor Vergata, Department of System Medicine, Rome, Italy.
Expert Opin Investig Drugs. 2012 Oct;21(10):1489-501. doi: 10.1517/13543784.2012.710602. Epub 2012 Aug 23.
Inhaled bronchodilators are the mainstay of the current management of COPD at all stages of the disease, and are critical in the symptomatic management of asthma. Therefore, there is still considerable interest in finding novel classes of broncholytic drugs or, at least, in improving the existing classes of bronchodilator.
This review paper mainly focuses on bronchodilators that are in Phase I and II clinical trials.
To date, finding new classes of bronchodilators has proved difficult. Consequently, many research groups have sought to improve the existing classes of bronchodytic drugs. The majority of programs in development for novel bronchodilators are focused on developing new ligands that interact with β(2)-adrenoceptors and/or muscarinic acetylcholine receptors in a manner that enhances their bronchodilator effectiveness and duration of action, which allows only one administration per day, although the twice-daily dosing of bronchodilators is still considered a useful approach to the symptomatic treatment of COPD, and improving their safety profiles. Moreover, the current opinion is that it is advantageous to develop inhalers containing combinations of long-acting bronchodilator drugs in an attempt to simplify treatment regimes as much as possible. Another goal is to develop novel combinations of one or two classes of long-acting bronchodilators along with inhaled corticosteroids.
吸入性支气管扩张剂是当前 COPD 各阶段疾病管理的主要手段，也是哮喘症状管理的关键。因此，人们仍然非常关注寻找新型支气管扩张药物，或者至少改善现有的支气管扩张药物。
本文主要关注处于 I 期和 II 期临床试验的支气管扩张剂。
迄今为止，发现新的支气管扩张剂类药物一直很困难。因此，许多研究小组试图改进现有的支气管扩张药物。目前，大多数新型支气管扩张剂的研发项目都集中在开发与β(2)-肾上腺素能受体和/或毒蕈碱乙酰胆碱受体相互作用的新型配体，以提高其支气管扩张作用和作用持续时间，从而允许每天只需给药一次，尽管每天两次给药仍被认为是 COPD 症状治疗的一种有效方法，并且可以提高其安全性。此外，目前的观点是，开发含有长效支气管扩张药物组合的吸入器以尽可能简化治疗方案是有利的。另一个目标是开发一种或两种长效支气管扩张剂与吸入性皮质类固醇的新型组合。
