Cazzola Mario, Matera Maria Gabriella, Lötvall Jan
Department of Respiratory Medicine, A. Cardarelli Hospital, Via del Parco Margherita 24, 80121 Naples, Italy.
Expert Opin Investig Drugs. 2005 Jul;14(7):775-83. doi: 10.1517/13543784.14.7.775.
After the discovery of formoterol and salmeterol, new candidates for long-acting beta2-adrenoceptor agonists (LABAs) have emerged from various companies. In particular, once-daily beta2-adrenoceptor agonists such as arformoterol, carmoterol, indacaterol, GSK-159797, GSK-597901, 159802, 642444 and 678007 are under development for the treatment of asthma and chronic obstructive pulmonary disease. The majority of these compounds are (R,R)-isomers in order to control desensitisation and accumulation. Several options for combination products are currently being evaluated in parallel with the development of these ultra LABAs. Once-daily dosing of an ultra LABA would be a significant convenience and probably a compliance-enhancing advantage leading to improved overall clinical outcomes in patients with asthma and chronic obstructive pulmonary disease. The only limits set for the development of a LABA with a new product profile are medical needs and marketing opportunities.
在福莫特罗和沙美特罗被发现后，各公司推出了长效β2肾上腺素受体激动剂（LABA）的新候选药物。特别是，诸如阿福特罗、卡莫特罗、茚达特罗、GSK-159797、GSK-597901、159802、642444和678007等每日一次的β2肾上腺素受体激动剂正在开发中，用于治疗哮喘和慢性阻塞性肺疾病。这些化合物中的大多数是（R,R）-异构体，以控制脱敏和蓄积。目前正在对几种联合产品选项与这些超长效LABA的开发同时进行评估。每日一次服用超长效LABA将带来极大便利，并且可能具有提高依从性的优势，从而改善哮喘和慢性阻塞性肺疾病患者的整体临床疗效。针对具有新产品特性的LABA开发所设定的唯一限制是医疗需求和市场机会。
