24-h bronchodilator efficacy of single doses of indacaterol in Japanese patients with asthma: A comparison with placebo and salmeterol

Sugihara, Naruhiko; Kanada, Shigeto; Haida, Michiko; Ichinose, Masakazu; Adachi, Mitsuru; Hosoe, Motoi; Emery, Charlotte; Higgins, Mark; Krämer, Benjamin

doi:10.1016/j.rmed.2010.06.011

Cited by 18 publications

(10 citation statements)

References 27 publications

(25 reference statements)

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“…Accordingly, abediterol showed a fast onset of action relaxing human bronchi, not significantly different from that of formoterol. The results obtained with the reference compounds were consistent with the rates of onset of action in humans; formoterol was an effective bronchodilator within 5 min, salmeterol took 15 to 30 min to achieve significant bronchodilation over baseline, and indacaterol showed an onset of action faster than salmeterol (Kottakis et al, 2002;Sugihara et al, 2010). The onset of action of abediterol in preclinical models was in line with the first results in humans, where abediterol (5, 10, and 25 g), at 5 min postdose, significantly improved lung function compared with placebo (p Ͻ 0.0001) and salmeterol (p Ͻ 0.05) in patients with persistent asthma, suggesting a rapid onset of action .…”

Section: Discussionsupporting

confidence: 73%

Pharmacological Characterization of Abediterol, a Novel Inhaled β₂-Adrenoceptor Agonist with Long Duration of Action and a Favorable Safety Profile in Preclinical Models

Aparici¹,

Gómez‐Angelats²,

Vilella³

et al. 2012

J Pharmacol Exp Ther

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Abediterol is a novel potent, long-acting inhaled ␤ 2 -adrenoceptor agonist in development for the treatment of asthma and chronic obstructive pulmonary disease. Abediterol shows subnanomolar affinity for the human ␤ 2 -adrenoceptor and a functional selectivity over ␤ 1 -adrenoceptors higher than that of formoterol and indacaterol in both a cellular model with overexpressed human receptors and isolated guinea pig tissue. Abediterol is a full agonist at the human ␤ 2 -adrenoceptor (E max ϭ 91 Ϯ 5% of the maximal effect of isoprenaline). The potency and onset of action that abediterol shows in isolated human bronchi (EC 50 ϭ 1.9 Ϯ 0.4 nM; t 1 ⁄2 onset ϭ 7-10 min) is not significantly different from that of formoterol, but its duration of action (t 1 ⁄2 ϳ 690 min) is similar to that of indacaterol. Nebulized abediterol inhibits acetylcholine-induced bronchoconstriction in guinea pigs in a concentration-dependent manner, with higher potency and longer duration of action (t 1 ⁄2 ϭ 36 h) than salmeterol (t 1 ⁄2 ϭ 6 h) and formoterol (t 1 ⁄2 ϭ 4 h) and similar duration of action to indacaterol up to 48 h. In dogs, the bronchoprotective effect of abediterol is more sustained than that of salmeterol and indacaterol at doses without effects on heart rate, thus showing a greater safety margin (defined as the ratio of dose increasing heart rate by 5% and dose inhibiting bronchospasm by 50%) than salmeterol, formoterol, and indacaterol (5.6 versus 3.3, 2.2, and 0.3, respectively). In conclusion, our results suggest that abediterol has a preclinical profile for once-daily dosing in humans together with a fast onset of action and a favorable cardiovascular safety profile.

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Section: Discussionsupporting

confidence: 73%

Pharmacological Characterization of Abediterol, a Novel Inhaled β₂-Adrenoceptor Agonist with Long Duration of Action and a Favorable Safety Profile in Preclinical Models

Aparici¹,

Gómez‐Angelats²,

Vilella³

et al. 2012

J Pharmacol Exp Ther

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“…Novel ultra LABA agents with a 24 h duration of action are available, e.g., indacaterol, vilanterol, and olodaterol. [ 418 419 420 421 422 423 424 ] The ultra LABA has a compliance-enhancing advantage. Due to lack of anti-inflammatory effect, this category should not be used alone as monotherapy in asthma as it leads to increased mortality.…”

Section: Methodsmentioning

confidence: 99%

The Saudi Initiative for Asthma - 2016 update: Guidelines for the diagnosis and management of asthma in adults and children

et al. 2016

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This is an updated guideline for the diagnosis and management of asthma, developed by the Saudi Initiative for Asthma (SINA) group, a subsidiary of the Saudi Thoracic Society. The main objective of SINA is to have guidelines that are up to date, simple to understand and easy to use by nonasthma specialists, including primary care and general practice physicians. SINA approach is mainly based on symptom control and assessment of risk as it is the ultimate goal of treatment. The new SINA guidelines include updates of acute and chronic asthma management, with more emphasis on the use of asthma control in the management of asthma in adults and children, inclusion of a new medication appendix, and keeping consistency on the management at different age groups. The section on asthma in children is rewritten and expanded where the approach is stratified based on the age. The guidelines are constructed based on the available evidence, local literature, and the current situation in Saudi Arabia. There is also an emphasis on patient–doctor partnership in the management that also includes a self-management plan.

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“…Two studies evaluated the clinical efficacy of indacaterol compared with placebo, one each in patients with asthma and COPD (Table ) …”

Section: Clinical Efficacy Trialsmentioning

confidence: 99%

“…Eight trials compared the efficacy of indacaterol to twice‐daily LABAs or anticholinergic therapy (Table ) . Three trials evaluated treatment in patients with asthma and are summarized briefly here.…”

Section: Comparative Clinical Trialsmentioning

confidence: 99%

“…A similar randomized, double‐blind, placebo‐controlled, crossover study of single‐dose indacaterol or placebo by SDDPI, followed by a single day of open‐label twice‐daily salmeterol, was conducted in 41 Japanese patients with stable asthma who were receiving treatment with inhaled corticosteroids for at least 4 weeks . The average age was 48 years, and 70% reported never smoking.…”

Section: Comparative Clinical Trialsmentioning

confidence: 99%

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Indacaterol: A Novel Long‐Acting β₂‐Agonist

Ray¹,

McMillen

Treadway³

et al. 2012

Pharmacotherapy

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Bronchodilator drugs are the foundation for the treatment of chronic obstructive pulmonary disease. The principal inhaled bronchodilator treatments used are β(2) -agonists and anticholinergics, either alone or in combination. Currently available β(2) -agonists are of either short duration and used multiple times/day, or of long duration, which requires twice-daily administration. Indacaterol is considered an ultra-long-acting β(2) -agonist and was recently approved for use in the United States. Its duration of action is approximately 24 hours, allowing for once-daily administration. Cough was the most commonly reported adverse effect with use of indacaterol. Cough usually occurred within 15 seconds of inhalation of the drug, lasted around 6 seconds, was not associated with bronchospasm, and did not cause discontinuation of the drug. Otherwise, the drug's safety profile was similar to that of other bronchodilators. Based on similar improvement in spirometric measurements compared with other bronchodilator drugs and the convenience of its once-daily dosing, indacaterol may be beneficial in the management of mild-to-moderate chronic obstructive pulmonary disease, either alone or in combination with anticholinergic drugs administered once/day.

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24-h bronchodilator efficacy of single doses of indacaterol in Japanese patients with asthma: A comparison with placebo and salmeterol

Abstract: Single dose indacaterol provided sustained 24-h bronchodilation with a faster onset of action than salmeterol and a good overall safety and tolerability profile in Japanese patients with asthma. These results are consistent with data from Caucasian populations.

Cited by 18 publications

References 27 publications

Pharmacological Characterization of Abediterol, a Novel Inhaled β₂-Adrenoceptor Agonist with Long Duration of Action and a Favorable Safety Profile in Preclinical Models

Pharmacological Characterization of Abediterol, a Novel Inhaled β₂-Adrenoceptor Agonist with Long Duration of Action and a Favorable Safety Profile in Preclinical Models

The Saudi Initiative for Asthma - 2016 update: Guidelines for the diagnosis and management of asthma in adults and children

Indacaterol: A Novel Long‐Acting β₂‐Agonist

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24-h bronchodilator efficacy of single doses of indacaterol in Japanese patients with asthma: A comparison with placebo and salmeterol

Abstract: Single dose indacaterol provided sustained 24-h bronchodilation with a faster onset of action than salmeterol and a good overall safety and tolerability profile in Japanese patients with asthma. These results are consistent with data from Caucasian populations.

Cited by 18 publications

References 27 publications

Pharmacological Characterization of Abediterol, a Novel Inhaled β2-Adrenoceptor Agonist with Long Duration of Action and a Favorable Safety Profile in Preclinical Models

Pharmacological Characterization of Abediterol, a Novel Inhaled β2-Adrenoceptor Agonist with Long Duration of Action and a Favorable Safety Profile in Preclinical Models

The Saudi Initiative for Asthma - 2016 update: Guidelines for the diagnosis and management of asthma in adults and children

Indacaterol: A Novel Long‐Acting β2‐Agonist

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Pharmacological Characterization of Abediterol, a Novel Inhaled β₂-Adrenoceptor Agonist with Long Duration of Action and a Favorable Safety Profile in Preclinical Models

Pharmacological Characterization of Abediterol, a Novel Inhaled β₂-Adrenoceptor Agonist with Long Duration of Action and a Favorable Safety Profile in Preclinical Models

Indacaterol: A Novel Long‐Acting β₂‐Agonist