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Aclidinium Bromide
CAS NO.: 320345-99-1
Chemical Formula: C26H30BrNO4S2
Molecular Weight: 564.5550
DMF&GMP status:
Aclidinium bromide (INN, marketed under the brand name Tudorza Pressair in the US, Eklira Genuair in the UK, and Tudorza Genuair in Canada; licensed to Menarini under the brand name Bretaris Genuair for majority of EU member states) is a long-acting, inhaled muscarinic antagonist approved in the US on July 24, 2012 as a maintenance treatment for chronic obstructive pulmonary disease (COPD). 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. Aclidinium is rapidly hydrolysed in human plasma, unlike other currently available antimuscarinics including tiotropium. This results in very low and transient systemic exposure, suggesting a reduced potential for class-related systemic side effects in the clinical setting.
Early clinical studies in healthy subjects have confirmed the low systemic bioavailability and favourable safety profile of single and multiple doses of aclidinium. 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.
Aclidinium is delivered via a novel, multidose dry powder inhaler, the Genuair inhaler.
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