Vilanterol (GW642444) is a potent, orally active and long-acting β2-AR (β2-adrenergic receptor) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.
β2-AR is a member of the 7-transmembrane family of receptors. And, β2-AR is a subtype of β-adrenergic receptors, distributing in the respiratory tract. In addition, β2-AR plays an important role in the regulation of heart functionand. First, β2-AR can modify in vitro cytokine release upon stimulation. Second, β2-AR can cause the response including bronchiectasis, vasodilation and so on. Third, β2-AR can activate the intracellular signaling, which is largely affected through cyclic adenosine monophosphate and protein kinase A. Therefore, The β2-AR agonist has potential to treat respiratory disease, such as asthma and chronic obstructive pulmonary disease (COPD).
Vilanterol is a potent, orally active, selective and long-acting β2-AR agonist with a long duration of action.
Vilanterol shows highly selective for the β2-AR with at least a 1000-fold selectivity over both β1– and β3-AR subtypes. In addition, Vilanterol shows reassertion activity in both cell and tissue systems. And, the activity was comparable with salmeterol and indacaterol but longer than formoterol. Vilanterol has a faster onset and longer duration of action than salmeterol. In human airways, Vilanterol exhibits a significant level of bronchodilation 22 h after treatment. Vilanterol has potential to treat asthma and COPD. Vilanterol can improve lung function in COPD. And, this compound is well tolerated in subjects with COPD at a single dose (25-100 μg). In addition, Vilanterol also can treat asthma by activating the β2 AR to dilate obstructed airways.
In summary, Vilanterol is a potent, orally active, selective and long-acting β2-AR agonist, and has potential to treat asthma and COPD.
 Slack RJ, et al. J Pharmacol Exp Ther. 2013 Jan;344(1):218-30.
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