Vilanterol: A Comprehensive Pharmacological and Clinical Review

1. Introduction to Vilanterol

1.1. Background and Development

Vilanterol is a selective long-acting β2​-adrenergic agonist (LABA) distinguished by its inherent 24-hour activity, permitting once-daily administration for the management of Chronic Obstructive Pulmonary Disease (COPD) and asthma.[1] The impetus for its development stemmed from a clinical need to enhance patient compliance, which is often suboptimal with regimens requiring more frequent dosing or complex administration techniques.[1] This focus on simplifying treatment regimens addresses a significant barrier in chronic respiratory disease management, potentially leading to improved disease control and patient outcomes. This approach is further supported by pharmacoeconomic analyses suggesting adherence benefits for once-daily therapies.[2]

The molecular design of Vilanterol is rooted in the salmeterol scaffold. It was specifically engineered as an antedrug analog of salmeterol, involving modifications to produce homochiral compounds with the (R)-configuration at the chiral benzylic alcohol carbon.[1] This targeted chemical modification aimed to optimize the pharmacological profile, particularly to achieve a duration of action suitable for once-daily dosing, a characteristic that differentiates it from some earlier LABAs like salmeterol, which typically requires twice-daily administration.[1] The development of Vilanterol, particularly the active substance, involved a collaboration between Innoviva (formerly Theravance) and GlaxoSmithKline (GSK). GSK is the primary manufacturer of Vilanterol-containing products, and Innoviva receives royalties from their sales.[3]

1.2. Drug Class and Therapeutic Significance