Chemical Information

Biological Activity of Vilanterol

Description:
IC50 Value:
Vilanterol (GW642444) (VI) is a novel, inhaled, long-acting β(2) agonist with inherent 24-h activity under development as a once-daily combination therapy with an inhaled corticosteroid for COPD and asthma.
in vitro: Vilanterol displayed a subnanomolar affinity for the β(2)-AR that was comparable with that of salmeterol but higher than olodaterol, formoterol, and indacaterol. In cAMP functional activity studies, vilanterol demonstrated similar selectivity as salmeterol for β(2)- over β(1)-AR and β(3)-AR, but a significantly improved selectivity profile than formoterol and indacaterol. Vilanterolalso showed a level of intrinsic efficacy that was comparable to indacaterol but significantly greater than that of salmeterol [1].
in vivo: The combination of FF/VI at a strength of 100/25 μg significantly (p < 0.001) improved wm FEV1 (173 ml) and trough FEV1 (115 ml) vs. placebo. Similar effects were observed with FF/VI 50/25 μg. VI 25 μg over 24 weeks improved lung function vs. placebo significantly for wm FEV1 (103 ml, p < 0.001) and trough FEV1 (67 ml, p = 0.017) [2].
Toxicity: All doses of VI were associated with a low incidence of treatment-related adverse events/serious adverse events, with no suggestion of effects on BP, pulse rate, QT intervals corrected for heart rate calculated by Fridericia formula, or blood glucose and potassium levels [3].
Clinical trial:
 

Clinical Information of Vilanterol

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References on Vilanterol

[1]. Slack RJ, et al. In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action. J Pharmacol Exp Ther. 2013 Jan;344(1):218-30

[2]. Slack RJ, et al. In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action. J Pharmacol Exp Ther. 2013 Jan;344(1):218-30.

[3]. Kerwin EM, et al. A randomised trial of fluticasone furoate/vilanterol (50/25 μg; 100/25 μg) on lung function in COPD. Respir Med. 2013 Apr;107(4):560-9.

[4]. Hanania NA, et al. The efficacy and safety of the novel long-acting β2 agonist vilanterol in patients with COPD: a randomized placebo-controlled trial. Chest. 2012 Jul;142(1):119-27.