Indacaterol, A Novel Once Daily Inhaled β2-Adrenoreceptor Agonist

Roig, Jordi; Hernando, Rosana; Mora, Ramon

doi:10.2174/1874306400903010027

Cited by 14 publications

(9 citation statements)

References 32 publications

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“…In preclinical trials, indacaterol's onset of action was significantly faster than that of salmeterol and similar to those of salbutamol (albuterol) and formoterol . Like other LABAs, indacaterol is lipophilic and, therefore, dissociates slowly from lung tissue . In humans, less than 1% of the dose is eliminated in the urine .…”

Section: Pharmacology and Pharmacokineticsmentioning

confidence: 80%

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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Section: Pharmacology and Pharmacokineticsmentioning

confidence: 80%

Indacaterol: A Novel Long‐Acting β₂‐Agonist

Ray¹,

McMillen

Treadway³

et al. 2012

Pharmacotherapy

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“…It is a partial agonist at the human β 2 -adrenoceptor with a binding affinity similar to that of formoterol, and an intrinsic activity higher than that of salbutamol and salmeterol [2,3]. The efficacy and safety of indacaterol in patients with COPD have been previously evaluated in number of studies, where once-daily indacaterol has demonstrated 24-h bronchodilation with a rapid onset of action [4-8].…”

Section: Introductionmentioning

confidence: 99%

“…Indacaterol is a novel, inhaled, ultra long-acting β 2 -agonist (LABA) [ 1 ] that is approved in a number of countries, including throughout the European Union (EU), at doses of 150 and 300 μg once-daily (OD) for the maintenance bronchodilator treatment of airflow obstruction in adult patients with chronic obstructive pulmonary disease (COPD). It is a partial agonist at the human β 2 -adrenoceptor with a binding affinity similar to that of formoterol, and an intrinsic activity higher than that of salbutamol and salmeterol [ 2 , 3 ]. The efficacy and safety of indacaterol in patients with COPD have been previously evaluated in number of studies, where once-daily indacaterol has demonstrated 24-h bronchodilation with a rapid onset of action [ 4 - 8 ].…”

Section: Introductionmentioning

confidence: 99%

Cardiac safety of indacaterol in healthy subjects: a randomized, multidose, placebo- and positive-controlled, parallel-group thorough QT study

et al. 2011

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BackgroundIndacaterol is a novel once-daily ultra long-acting β2-agonist for the treatment of chronic obstructive pulmonary disease. It is known that β2-agonists, like other adrenergic compounds, can prolong the QT-interval. This thorough QT/QTc study (as per ICH E14 guideline) evaluated the effect of indacaterol on the QT interval in healthy subjects.MethodsIn this randomized, double-blind, parallel-group, placebo- and positive-controlled (open-label moxifloxacin) study, non-smoking healthy subjects (18-55 years, body mass index: 18.5-32.0 kg/m2) were randomized (4:4:2:4:1) to 14-day treatment with once-daily indacaterol (150 μg, 300 μg, or 600 μg), placebo, or placebo/moxifloxacin (double-blind 14-day treatment with placebo and a single open-label dose of 400 mg moxifloxacin on Day 14). The primary endpoint was the change from baseline on Day 14 in QTcF (QT interval corrected for heart rate using Fridericia's formula).ResultsIn total, 404 subjects were randomized to receive indacaterol (150 [n = 108], 300 [n = 108], 600 μg [n = 54]), placebo (n = 107), or placebo/moxifloxacin (n = 27); 388 subjects completed the study. Maximal time-matched mean (90% confidence intervals) treatment differences from placebo in QTcF change from baseline on Day 14 were 2.66 (0.55, 4.77), 2.98 (1.02, 4.93) and 3.34 (0.86, 5.82) ms for indacaterol 150 μg, 300 μg and 600 μg, respectively. Study sensitivity was confirmed with moxifloxacin demonstrating a significant maximal time-matched QTcF prolongation of 13.90 (10.58, 17.22) ms compared to placebo. All indacaterol doses were well tolerated.ConclusionIndacaterol, at doses up to 600 μg once daily (2-4 times the therapeutic dose) does not have any clinically relevant effect on the QT interval.Trial RegistrationClinicalTrials.gov: NCT01263808

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“…In July 2011, the US Food and Drug Administration (FDA) permitted its use in the USA with the same indication (maintenance therapy of airflow obstruction in COPD patients) at a lower recommended dose of 75 μg 11. Indacaterol has a fast onset of action (5 minutes) and a longer duration (24 hours) than the other long-acting β 2 -agonists, properties conferred by its unique biochemical structure,12 and hence is defined as “ultra-long-acting β 2 -agonist.”13 Various clinical studies have assessed the safety and tolerability profile of indacaterol. Additionally, results from multiple studies, investigating indacaterol’s efficacy, demonstrate an increase in lung function indices, amelioration of patients’ symptoms, improvement of health status, reduction of use of rescue medication, and decrease of exacerbation rate in comparison with placebo 14–16.…”

Section: Definition and Management Of Copdmentioning

confidence: 99%

New developments in the management of COPD: clinical utility of indacaterol 75 µg

Steiropoulos

Archontogeorgis

Nena

et al. 2013

COPD

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Chronic obstructive pulmonary disease (COPD) is a global health challenge and a major cause of mortality worldwide. Bronchodilators, particularly long-acting β2-agonists and long-acting antimuscarinic agents, used singly or in combination, aim to improve lung function, reduce symptoms, prevent exacerbations, and enhance quality of life of COPD patients. Indacaterol is a novel, inhaled, long-acting β2-agonist, with rapid onset of action and once-daily dosing providing 24-hour bronchodilation. Currently, the recommended dose differs between Europe (150 μg; maximum 300 μg) and USA (75 μg), the latter is lower than that assessed in the majority of the conducted studies. This review summarises published evidence regarding the efficacy, tolerability, and safety of indacaterol at a dose of 75 μg. Indacaterol 75 μg was found to be superior than placebo regarding lung function, dyspnea, health status, use of rescue medication, and rate of exacerbations. Furthermore, indacaterol 75 μg was well tolerated, while the most frequent adverse effect was deterioration of COPD occurring at a frequency similar to placebo, without major cardiovascular adverse effects. In conclusion, indacaterol 75 μg, administered once daily, is efficacious and has an excellent tolerability and safety profile, and is therefore a valid alternative in the treatment of COPD patients.

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Indacaterol, A Novel Once Daily Inhaled β2-Adrenoreceptor Agonist

Cited by 14 publications

References 32 publications

Indacaterol: A Novel Long‐Acting β₂‐Agonist

Indacaterol: A Novel Long‐Acting β₂‐Agonist

Cardiac safety of indacaterol in healthy subjects: a randomized, multidose, placebo- and positive-controlled, parallel-group thorough QT study

New developments in the management of COPD: clinical utility of indacaterol 75 µg

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Indacaterol, A Novel Once Daily Inhaled β2-Adrenoreceptor Agonist

Cited by 14 publications

References 32 publications

Indacaterol: A Novel Long‐Acting β2‐Agonist

Indacaterol: A Novel Long‐Acting β2‐Agonist

Cardiac safety of indacaterol in healthy subjects: a randomized, multidose, placebo- and positive-controlled, parallel-group thorough QT study

New developments in the management of COPD: clinical utility of indacaterol 75 &micro;g

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Indacaterol: A Novel Long‐Acting β₂‐Agonist

Indacaterol: A Novel Long‐Acting β₂‐Agonist

New developments in the management of COPD: clinical utility of indacaterol 75 µg