In vitro and in vivo preclinical profile of abediterol (LAS100977), an inhaled long-acting β2-adrenoceptor agonist, compared with indacaterol, olodaterol and vilanterol

Aparici, Mònica; Gavaldà, Amadeu; Ramos, Israel; Carcasona, Carla; Otal, Raquel; Fernández-Blanco, Joan Antoni; Montero, J.L.; García, Vicente Marco; López, Rosa; Alba, Jorge De; Doe, Christopher P.; Puig, Carlos; Vilella, Dolors; Miralpeix, Montserrat

doi:10.1016/j.ejphar.2015.11.053

Cited by 23 publications

(15 citation statements)

References 33 publications

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“…The affinity of VI for the human β 2 -AR is higher than formoterol, indacaterol and olodaterol but comparable with that of salmeterol and slightly lower than that of abediterol [48,63,64]. VI is a highly In functional activity studies, VI has similar selectivity profile as salmeterol for β 2 -AR over β 1 -AR and β 3 -AR with over 1000-fold selectivity over both these receptors, but it has a significantly improved selectivity profile than albuterol (salbutamol), formoterol and indacaterol decreasing the risk of untoward effects due to the stimulation of the other β-ARs [48,63].…”

Section: Vilanterolmentioning

confidence: 86%

Fluticasone furoate and vilanterol for the treatment of chronic obstructive pulmonary disease

Caramori

Ruggeri

Casolari³

et al. 2017

Expert Review of Respiratory Medicine

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Current national and international guidelines for the management of patients with stable chronic obstructive pulmonary disease (COPD) recommend the use of inhaled long-acting bronchodilators, inhaled glucocorticoids and their combinations for maintenance treatment of moderate to severe stable COPD. Areas covered: The role of fluticasone furoate (FF) and vilanterol (VI) once daily combination therapy for the regular treatment of patients with stable COPD is discussed in this review. Expert commentary: The regular treatment of moderate to severe stable COPD with once daily FF/VI combination therapy is effective, as seen in in several large placebo-controlled clinical trials involving many thousands of patients. FF/VI improved lung function, decreased respiratory symptoms and decreased the number of COPD exacerbations, including COPD-related hospitalizations. FF/VI combination therapy has also been approved for this indication in most countries. The use of this combination therapy may significantly decrease the economic costs for some National Health Services.

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Section: Vilanterolmentioning

confidence: 86%

Fluticasone furoate and vilanterol for the treatment of chronic obstructive pulmonary disease

Caramori

Ruggeri

Casolari³

et al. 2017

Expert Review of Respiratory Medicine

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“…Новые ультра-ДДБА, находящиеся в состояния разработки Абедитерол (AZD0548) является новым ультра-ДДБА, который в предклинических исследованиях показал высокий бронхолитический потенциал и сходную (или превышающую) селективность в отношении β 2 -адренорецепторов по сравнению с β 1 -адренорецепторами, при меньшем влиянии на частоту сердечных сокращений по сравнению с формотеролом, индакатеролом, сальметеролом, вилантеролом и олодатеролом [47,48]. Более то-го, этот новый ультра-ДДБА продемонстрировал длительное время пребывания на человеческих β 2 -адренорецепторах, при значительно более мед-ленной полужизни диссоциации по сравнению с индакатеролом, олодатеролом и вилантеролом [49].…”

Section: обзорыunclassified

Progress and Prospects for Long-Acting Β 2 -Agonists in the Treatment of Chronic Obstructive Pulmonary Disease

Mario¹,

Ermanno²,

Ora³

et al. 2018

BCCM

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Статья итальянских авторов дает полное пред-ставление о развитии адреномиметиков ультрадли-тельного действия при ХОБЛ. Ценность статьи -во всесторонней оценке проблемы, отсутствии ангажированности и тенденциозности в изложении проблемы. Мы надеемся, что знакомство с русской версией статьи обогатит наших читателей новыми знаниями и расширит их мировоззрение. Реферат. Лечение хронической обструктивной болезни легких (ХОБЛ), как правило, предполагает назначение комбинации лекарственных препаратов, одним из которых зачастую является агонист β 2 -адренорецепторов. Цель данной статьи -представить информацию об агонистах β 2 -адренорецепторов длительного действия (ультра-ДДВА) -современную форму препаратов, обеспечивающую высокую приверженность пациентов к лечению, благодаря упрощенной схеме приема 1 раз в сут. Материал и методы. Проанализированы совре-менные литературные данные об агонистах β 2 -адренорецепторов. В частности, новейшие данные о применении ультра-ДДВА в лечении ХОБЛ, а также вопросы безопасности препарата для сердечно-сосудистой системы. Результаты и их обсуждение. Рассматривается инновационный метод назначения фиксированных доз ДДБА в комбинации с антихолинергическими препаратами длительного действия (ДДАХ) и/или с ингаляционными кор-тикостероидами, а также новейших препаратов ультра-ДДВА, находящихся на этапах клинического исследования и доклинической разработки. Выводы. Огромный интерес к разработке новых агонистов β 2 -адренорецепторов длительного действия значительно снизился за последние годы. Тем не менее ультра-ДДВА считаются одним из основных компонентов лечения ХОБЛ в комбинации с другими классами препаратов (ДДАХ и ингаляционные кортикостероиды), которые в настоящее время находятся на этапе внедрения для регулярного использования. Vergata, Via Montpellier,1, Italy, 00133, Rome, Abstract. Aim. The treatment of chronic obstructive pulmonary disease (COPD) is generally based on the assumption of drug combinations in which β 2 -agonists are commonly included. Ultra-LABAs were developed to induce a greater adherence to the treatment as a result of the simplification of treatment with the reduction of the daily dose to be taken. Material and methods. We analyzed the current literature data on β 2 -adrenergic agonists. The potential positioning of ultra-LABAs in the treatment of COPD and their cardiovascular safety is discussed according to the new information on the topics. Results and discussion. The novel fixed-dose combinations of ultra-LABAs with LAMAs and/or ICSs are examined, as well as the novel ultra-LABAs under clinical development and the ultra-LABAs in preclinical development. PROGRESS AND PROSPECTS FOR LONG-ACTING β 2 -AGONISTS IN THE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE

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“…Several new LABA agents designed for once-daily dosing are available or under study including indacaterol, olodaterol, abediterol and VI 16. Appropriate concern for the use of LABA agents alone as maintenance therapy has mandated that asthmatic subjects in most clinical studies evaluating the use of the inhaled LABA VI be currently on an ICS (Table 4).…”

Section: The Use Of VI In Asthmamentioning

confidence: 99%

Spotlight on fluticasone furoate/vilanterol trifenatate for the once-daily treatment of asthma: design, development and place in therapy

Albertson

Bullick

Schivo

et al. 2016

DDDT

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The use of inhaled corticosteroids (ICSs) plays a key role in the treatment of asthmatic patients, and international guidelines have designated ICSs as an early maintenance therapy in controlling asthma symptoms. When asthmatic patients remain symptomatic on ICSs, one common option is to add a long-acting beta2 agonist (LABA) to the maintenance treatment. Fixed combination inhalers that contain both an ICS and a LABA have been popular for both chronic obstructive pulmonary disease (COPD) and asthma. Historically, these inhalers have been dosed twice daily. However, currently, there is a once-daily combination therapy with the ICS fluticasone furoate (FF) and the LABA vilanterol trifenatate (VI) with indications for use in both COPD and asthma. This dry powder inhaler (DPI) comes in two doses of FF (100 or 200 μg) both combined with VI (25 μg). This article reviews the clinical trial data for FF, VI and FF/VI combination inhalers and documents the efficacy and safety of once-daily inhaled maintenance therapy by DPI in asthmatic patients.

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In vitro and in vivo preclinical profile of abediterol (LAS100977), an inhaled long-acting β2-adrenoceptor agonist, compared with indacaterol, olodaterol and vilanterol

Cited by 23 publications

References 33 publications

Fluticasone furoate and vilanterol for the treatment of chronic obstructive pulmonary disease

Fluticasone furoate and vilanterol for the treatment of chronic obstructive pulmonary disease

Progress and Prospects for Long-Acting Β 2 -Agonists in the Treatment of Chronic Obstructive Pulmonary Disease

Spotlight on fluticasone furoate/vilanterol trifenatate for the once-daily treatment of asthma: design, development and place in therapy

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