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Jutta Beier, Helena Pujol, Beatriz Seoane, Eulalia Jimenez, Carol Astbury, Eric Massana, Sandrine Ruiz, Gonzalo de Miquel
BACKGROUND: Abediterol is a novel, once-daily long-acting β2-agonist in development for the treatment of chronic obstructive pulmonary disease (COPD) and asthma in combination with an anti-inflammatory agent. This Phase IIa, randomised, double-blind, crossover study investigated the bronchodilation, safety, tolerability and pharmacokinetics of abediterol in patients with moderate to severe COPD. METHODS: Seventy patients (aged ≥40 years, Global initiative for chronic Obstructive Lung Disease Stage II/III) were randomised (1:1:1:1:1:1) to single doses of abediterol 0...
2016: BMC Pulmonary Medicine
Mònica Aparici, Amadeu Gavaldà, Israel Ramos, Carla Carcasona, Raquel Otal, Joan Antoni Fernández-Blanco, Jose Luís Montero, Vicente Marco García, Rosa López, Jorge De Alba, Christopher Doe, Carlos Puig, Dolors Vilella, Montserrat Miralpeix
Abediterol is a novel long-acting β2-adrenoceptor agonist (LABA) currently in development for once-daily combination maintenance therapy of asthma and COPD. This study investigated the preclinical profile of abediterol in terms of affinity, potency, selectivity, duration of action and cardiac effects in comparison to the marketed once-daily LABAs indacaterol, olodaterol and vilanterol. Abediterol was the compound with the highest in vitro potency for dog, guinea pig and human β2-adrenoceptors. In electrical field stimulated guinea pig trachea, abediterol demonstrated 5-, 44- and 77-fold greater potency than olodaterol, indacaterol and vilanterol, respectively...
January 5, 2016: European Journal of Pharmacology
Paolo Montuschi, Giovanni Ciabattoni
Inhaled bronchodilators, including long-acting muscarinic receptor antagonists (LAMA) and long-acting β2-adrenoreceptor agonists (LABA), are the mainstay of pharmacological treatment of stable chronic obstructive pulmonary disease (COPD). Among approved LAMA, tiotropium bromide, glycopyrronium bromide, and umeclidinium bromide are administered once daily, whereas aclidinium bromide is administered every 12 h. New LAMA are under development for COPD. Among the approved LABA, indacaterol has a 24 h duration of action, whereas salmeterol and formoterol require twice-daily administration...
May 28, 2015: Journal of Medicinal Chemistry
Dave Singh, Helena Pujol, Anna Ribera, Beatriz Seoane, Eric Massana, Carol Astbury, Sandrine Ruiz, Gonzalo de Miquel
BACKGROUND: Long-acting β2-adrenergic agonists (LABAs) are recommended in combination with inhaled corticosteroids (ICSs) for asthma management. Abediterol is a novel, selective, potent, once-daily LABA in development for treatment of asthma and chronic obstructive pulmonary disease. This study aimed to determine abediterol doses with similar peak bronchodilatory effect to salbutamol 400 μg, and duration of action compatible with once-daily dosing in patients with persistent, stable asthma...
2014: BMC Pulmonary Medicine
J Beier, R Fuhr, E Massana, E Jiménez, B Seoane, G de Miquel, S Ruiz
BACKGROUND: Abediterol (LAS100977) is a novel, long-acting β2-agonist, in development for the once-daily treatment of asthma in combination with mometasone. Here we report the results of a Phase IIa trial of single doses of abediterol added to ongoing maintenance therapy (inhaled corticosteroids) in patients with persistent mild-to-moderate asthma. METHODS: This was a randomised, double-blind, placebo- and active-comparator-controlled, five-way crossover study...
October 2014: Respiratory Medicine
Wolfgang Timmer, Eric Massana, Eulalia Jimenez, Beatriz Seoane, Gonzalo de Miquel, Sandrine Ruiz
Here we report the results of a first-in-human study to evaluate the safety, tolerability pharmacokinetics, and pharmacodynamics of abediterol, a new β2 -adrenergic agonist. Forty-eight healthy males aged 18-45 years received abediterol doses of 5, 10, 25, or 50 µg, or placebo. Safety and tolerability assessments included adverse event reporting, pulse and blood pressure monitoring, 12-lead electrocardiograms, laboratory tests, and physical examination. Pharmacodynamic assessments included whole body plethysmography to determine the bronchodilatory effect by means of airway conductance and resistance...
December 2014: Journal of Clinical Pharmacology
L Fuso, N Mores, S Valente, M Malerba, P Montuschi
Inhaled bronchodilators, including beta(2)-agonists and antimuscaric receptor antagonists, are the mainstay of pharmacotherapy in chronic obstructive pulmonary disease (COPD). The short-acting beta(2)-agonists, including salbutamol, and fenoterol, have a rapid onset of action, a bronchodilating effect for 3-6 h and are used on demand. The long-acting beta(2)-agonists (LABAs), including salmeterol and formoterol, have 12-hour duration of action and are used with a twice-daily dosing regimen for long-term COPD treatment...
2013: Current Medicinal Chemistry
Mario Cazzola, Clive P Page, Paola Rogliani, M Gabriella Matera
β2-Agonists are effective bronchodilators due primarily to their ability to relax airway smooth muscle (ASM). They exert their effects via their binding to the active site of β2-adrenoceptors on ASM, which triggers a signaling cascade that results in a number of events, all of which contribute to relaxation of ASM. There are some differences between β2-agonists. Traditional inhaled short-acting β2-agonists albuterol, fenoterol, and terbutaline provide rapid as-needed symptom relief and short-term prophylactic protection against bronchoconstriction induced by exercise or other stimuli...
April 1, 2013: American Journal of Respiratory and Critical Care Medicine
Mònica Aparici, Mireia Gómez-Angelats, Dolors Vilella, Raquel Otal, Carla Carcasona, Marisa Viñals, Israel Ramos, Amadeu Gavaldà, Jorge De Alba, Jordi Gras, Julio Cortijo, Esteban Morcillo, Carlos Puig, Hamish Ryder, Jorge Beleta, Montserrat Miralpeix
Abediterol is a novel potent, long-acting inhaled β(2)-adrenoceptor agonist in development for the treatment of asthma and chronic obstructive pulmonary disease. Abediterol shows subnanomolar affinity for the human β(2)-adrenoceptor and a functional selectivity over β(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 β(2)-adrenoceptor (E(max) = 91 ± 5% of the maximal effect of isoprenaline)...
August 2012: Journal of Pharmacology and Experimental Therapeutics
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