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用于慢性阻塞性肺疾病(COPD)和哮喘的新型长效支气管扩张剂。

Novel long-acting bronchodilators for COPD and asthma.

作者信息

Cazzola M, Matera M G

机构信息

Unit of Respiratory Diseases, Department of Internal Medicine, University of Rome Tor Vergata, Rome, Italy.

出版信息

Br J Pharmacol. 2008 Oct;155(3):291-9. doi: 10.1038/bjp.2008.284. Epub 2008 Jul 7.

Abstract

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.

摘要

简化哮喘和慢性阻塞性肺疾病(COPD)管理并提高对规定治疗的依从性的一个重要步骤是将给药频率降至维持疾病控制所需的最低限度。因此,采用每日一次给药是提高依从性的重要策略,也是大多数患者偏爱的给药方案,这可能还会提高顺应性,并可能具有改善整体临床结局的优势。每日一次的β2激动剂或超长效β2激动剂(LABA),如卡莫特罗、茚达特罗、GSK-159797、GSK-597901、GSK-159802、GSK-642444和GSK-678007正在研发用于治疗哮喘和COPD。还有一些新型长效抗毒蕈碱药物(LAMA),如阿地溴铵、LAS-35201、GSK656398、GSK233705、NVA-237(格隆溴铵)和OrM3也在研发中。无论如何,目前的观点是,研发含有几类长效支气管扩张剂药物组合的吸入器,尽可能简化治疗方案将是有益的。因此,目前正在评估几种每日一次的双作用超长效LABA+LAMA组合产品的选择。另一种方法是拥有一种同时具备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)。一种成功的MABA产品的出现将彻底改变该领域,并为一系列新的组合产品打开大门。

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