An important step in simplifying asthma and chronic obstructive pulmonary disease (COPD) management and improving adherence with prescribed therapy is to reduce the dose frequency to the minimum necessary to maintain disease control. Therefore, the incorporation of once-daily dose administration is an important strategy to improve adherence and is a regimen preferred by most patients, which may also lead to enhancement of compliance, and may have advantages leading to improved overall clinical outcomes. Once-daily beta2-agonists or ultra long-acting beta2-agonists (LABAs) such as carmoterol, indacaterol, GSK-159797, GSK-597901, GSK-159802, GSK-642444 and GSK-678007 are under development for the treatment of asthma and COPD. Also some new long-acting antimuscarinic agents (LAMAs) such as aclidinium, LAS-35201, GSK656398, GSK233705, NVA-237 (glycopyrrolate) and OrM3 are under development. In any case, the current opinion is that it will be advantageous to develop inhalers containing combination of several classes of long-acting bronchodilator drugs in an attempt to simplify treatment regimens as much as possible. Consequently, several options for once-daily dual-action ultra LABA+LAMA combination products are currently being evaluated. A different approach is to have a dimer molecule in which both pharmacologies are present (these molecules are known as M3 antagonist-beta2 agonist (MABA) bronchodilators). The advent of a successful MABA product will revolutionize the field and open the door for a new range of combination products.

译文

:简化哮喘和慢性阻塞性肺疾病(COPD)管理并改善对处方疗法的依从性的重要步骤是将剂量频率降低到维持疾病控制所需的最低限度。因此,每天一次剂量的给药是改善依从性的重要策略,并且是大多数患者首选的治疗方案,这也可能导致依从性增强,并且可能具有导致整体临床结果改善的优势。正在开发每天一次的β2激动剂或超长效β2激动剂(LABA),例如卡莫特罗,茚达特罗,GSK-159797,GSK-597901,GSK-159802,GSK-642444和GSK-678007和COPD。另外,一些新的长效抗毒蕈碱剂(LAMAs),例如阿地铵,LAS-35201,GSK656398,GSK233705,NVA-237(甘草酸吡咯烷酸盐)和OrM3也正在开发中。无论如何,当前的观点是,开发包含几种长效支气管扩张药的组合的吸入器,以试图尽可能简化治疗方案将是有利的。因此,目前正在评估每日一次双作用的超LABA LAMA组合产品的几种选择。一种不同的方法是拥有同时存在两种药理作用的二聚体分子(这些分子被称为M3拮抗剂β2激动剂(MABA)支气管扩张剂)。成功的MABA产品的问世将彻底改变该领域,并为新的组合产品系列打开大门。

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