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Effect of indacaterol, a novel long-acting ß₂-agonist, on isolated human bronchi

¹ Research Unit EA220, Faculty of Medicine, Versailles University, Hospital Foch, Suresnes, and ³ Dept of Pharmacology, University Victor Segalen Bordeaux 2, Bordeaux, France. ² Novartis Institute for BioMedical Research, Horsham, UK.

CORRESPONDENCE: M. Molimard, Département de Pharmacologie, CHU de Bordeaux, Université Victor Segalen-INSERM U657, 33076 Bordeaux cedex, France. Fax: 33 557574671. E-mail: mathieu.molimard{at}pharmaco.u-bordeaux2.fr

Keywords: Airways smooth muscle, ß₂-adrenoceptor agonists, formoterol, indacaterol, isolated human bronchus, salmeterol

Received: March 7, 2006
Accepted November 21, 2006

Indacaterol is a novel ß₂-adrenoceptor agonist in development for the once-daily treatment of asthma and chronic obstructive pulmonary disease. The present study evaluated the relaxant effect of indacaterol on isolated human bronchi obtained from lungs of patients undergoing surgery for lung carcinoma.

Potency (-logEC₅₀), maximal relaxant effect (E_max) and onset of action were determined at resting tone. Duration of action was determined against cholinergic neural contraction induced by electrical field stimulation (EFS).

At resting tone, -logEC₅₀ and E_max values were 8.82±0.41 and 77±5% for indacaterol, 9.84±0.22 and 94±1% for formoterol, 8.36±0.16 and 74±4% for salmeterol, and 8.43±0.22 and 84±4% for salbutamol, respectively.

In contrast to salmeterol, indacaterol did not antagonise the isoprenaline response. Indacaterol's onset of action (7.8±0.7 min) was not significantly different from that of formoterol (5.8±0.7 min) or salbutamol (11.0±4.0 min), but it was significantly faster than that of salmeterol (19.4±4.3 min). EFS-induced contractions were inhibited with -logIC₅₀ values of 6.96±0.13 (indacaterol), 8.96±0.18 (formoterol), 7.18±0.34 (salmeterol) and 6.39±0.26 (salbutamol). Duration of action was >12 h for indacaterol and salmeterol, and 35.3±8.8 and 14.6±3.7 min for formoterol and salbutamol, respectively.

In isolated human bronchi, indacaterol behaved as a long-acting ß₂-adrenoceptor agonist with high intrinsic efficacy and fast onset of action.

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