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Aclidinium bromide  

2012-07-26 09:13:22|  分类: 药物化学 |  标签: |举报 |字号 订阅

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Aclidinium bromide - zliming2004 - zliming2004的博客

Aclidinium bromide (INN) is a long-acting, inhaled muscarinic antagonist currently being developed as a maintenance treatment for chronic obstructive pulmonary disease (COPD).[1] Preclinically, aclidinium showed potent antagonism of human muscarinic receptors, with a long residence time at M3 receptors and a shorter residence time at M2 receptors, indicating the potential to provide sustained bronchodilation.[2] Aclidinium is rapidly hydrolysed in human plasma, unlike other currently available antimuscarinics including tiotropium.[2][3] This results in very low and transient systemic exposure, suggesting a reduced potential for class-related systemic side effects in the clinical setting.[2][3]

Early clinical studies in healthy subjects have confirmed the low systemic bioavailability and favourable safety profile of single and multiple doses of aclidinium.[4][5] In a subsequent Phase IIb study, which included 464 patients with moderate to severe COPD, aclidinium displayed long-lasting bronchodilatory activity and was well tolerated.[6]

Aclidinium is delivered via a novel, multidose dry powder inhaler, the Genuair inhaler.

References

  1. ^ Gavaldà A, Miralpeix M, Ramos I, et al (2009). "Characterization of aclidinium bromide, a novel inhaled muscarinic antagonist, with long duration of action and a favorable pharmacological profile". J Pharmacol Exp Ther. Epub ahead of print. 
  2. ^ a b c Gavaldà A, Miralpeix M, Ramos I (2007). "Aclidinium bromide, a novel muscarinic receptor antagonist combining long residence at M3 receptors and rapid plasma clearance". Eur Respir J 30 (suppl 51): 209S–210S. 
  3. ^ a b Gavaldà A, Sentellas S, Alberti J, et al (2008). "Aclidinium bromide, a novel long-acting anticholinergic, is rapidly inactivated in plasma". Am J Respir Crit Care Med 177: A–654. 
  4. ^ Janset JM, Lamarca R, Garcia Gil E, Ferrer P. (2009). "Safety and pharmacokinetics of single doses of aclidinium bromide, a novel long-acting, inhaled antimuscarinic, in healthy subjects". Int J Clin Pharmacol Ther 47 (7): 460–468. PMID 19640353. 
  5. ^ Janset JM, Lamarca R, de Miquel G, Schr?dter A, Miletzki B, Gurniak M. (2009). "Safety and pharmacokinetics of multiple doses of aclidinium bromide, a novel long-acting muscarinic antagonist for the treatment of chronic obstructive pulmonary disease, in healthy participants". J Clin Pharmacol. Epub ahead of print. 
  6. ^ Chanez P, Burge PS, Dahl R, et al (2009). "Aclidinium bromide provides long-acting bronchodilation in patients with COPD". Pulm Pharmacol Ther. Epub ahead of print.
     
     
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