Ultra-Long-Acting β2-Adrenoceptor Agonists
@article{Matera2012UltraLongActingA, title={Ultra-Long-Acting $\beta$2-Adrenoceptor Agonists}, author={Maria Gabriella Matera and Mario Cazzola}, journal={Drugs}, year={2012}, volume={67}, pages={503-515} }
There has been a real interest recently in developing once-daily β2-adrenoceptor agonists (ultra-long-acting β2-adrenoceptor agonists [ultra-LABAs]) for treating asthma and chronic obstructive pulmonary disease (COPD) in an attempt to simplify their management, although an increasing amount of convincing data show an association of LABAs with a rise in asthma-related deaths and life-threatening experiences. This paper reviews the effects of different ultra-LABAs that are at varying stages of…
24 Citations
The Design of the Indacaterol Molecule
- Chemistry, Biology
- 2014
Indacaterol is the first of these agents to be approved for the treatment of COPD, having been designed by a rationale approach to deliver the optimal ultra-long-acting inhaled β2-adrenoceptor agonist profile.
Ultra Long-Acting β-Agonists in Chronic Obstructive Pulmonary Disease
- Medicine, BiologyJournal of experimental pharmacology
- 2020
This article reviews both clinically approved ULABA’s and ULABAs in development and describes how these agents are being combined with antimuscarinic agents and corticosteroids as dual and triple agent treatments that are being tested for clinical use and efficacy.
Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.
- Biology, MedicineACS medicinal chemistry letters
- 2014
A series of dibasic des-hydroxy β2 receptor agonists has been prepared and evaluated for potential as inhaled ultralong acting bronchodilators and AZD3199 was shown to have an excellent over all profile and was progressed into clinical evaluation as a new ultralongs acting inhaled β2 receptors agonist with rapid onset of action.
Novel bronchodilators in asthma
- MedicineCurrent opinion in pulmonary medicine
- 2010
It is likely that the once-daily dosing of a bronchodilator would be a significant convenience and probably a compliance-enhancing advantage, leading to improved overall clinical outcomes in patients with asthma.
Indacaterol: A Novel Long‐Acting β2‐Agonist
- Medicine, BiologyPharmacotherapy
- 2012
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, based on similar improvement in spirometric measurements compared with other bronchodilator drugs.
-AGONISTS IN THE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
- Medicine
- 2017
Aim. The treatment of chronic obstructive pulmonary disease (COPD) is generally based on the assumption of drug combinations in which β2-agonists are commonly included. Ultra-LABAs were developed to…
Sports doping: emerging designer and therapeutic β2-agonists.
- BiologyClinica chimica acta; international journal of clinical chemistry
- 2013
Indacaterol: in chronic obstructive pulmonary disease.
- MedicineDrugs
- 2010
Patients with COPD who received indacaterol 150 or 300 μg once daily had a significantly higher mean trough forced expiratory volume in 1 second (FEV₁) than placebo recipients after 12 weeks, and COPD exacerbations and symptoms, and health-related quality of life were also significantly improved for indACaterol versus placebo recipients in some studies.
Pharmacology and Therapeutics of Bronchodilators
- MedicinePharmacological Reviews
- 2012
An important step in simplifying asthma and COPD management and improving adherence with prescribed therapy is to reduce the dose frequency to the minimum necessary to maintain disease control, so the incorporation of once-daily dose administration is an important strategy to improve adherence.
References
SHOWING 1-10 OF 60 REFERENCES
Ultra long-acting β2-agonists in development for asthma and chronic obstructive pulmonary disease
- MedicineExpert opinion on investigational drugs
- 2005
Once-daily dosing of an ultra LABA would be a significant convenience and probably a compliance-enhancing advantage leading to improved overall clinical outcomes in patients with asthma and chronic obstructive pulmonary disease.
Long-acting beta-agonists role in asthma management.
- MedicineThe Journal of family practice
- 2006
Convincing data now exist that show an association of salmeterol with an increase in asthma-related deaths and life-threatening experiences, while formoterol is associated with more frequent serious asthma exacerbations, Nonetheless, LABAs remain an important component of asthma therapy.
Long-term effects of a long-acting beta 2-adrenoceptor agonist, salmeterol, on airway hyperresponsiveness in patients with mild asthma.
- Medicine, BiologyThe New England journal of medicine
- 1992
Regular treatment of patients with mild asthma with salmeterol leads to tolerance to its protective effects against a bronchoconstrictor stimulus, in this case inhaled methacholine, despite well-maintained bronchodilation, which raises concern about the effectiveness of prolonged therapy with long-acting beta 2-adrenoceptor agonists in asthma.
Beta-adrenoceptor agonists and asthma--100 years of development.
- Medicine, BiologyEuropean journal of pharmacology
- 2002
Association between β2-adrenoceptor polymorphism and susceptibility to bronchodilator desensitisation in moderately severe stable asthmatics
- MedicineThe Lancet
- 1997
β-Adrenergic Receptor Polymorphisms and Response to Salmeterol
- Medicine, Biology
- 2006
B16Arg/Arg patients with asthma may have an impaired therapeutic response to salmeterol in either the absence or presence of concurrent ICS use.
Regular formoterol treatment in mild asthma. Effect on bronchial responsiveness during and after treatment.
- MedicineAmerican journal of respiratory and critical care medicine
- 1995
Examination of the effect of an inhaled long-acting beta 2-adrenoceptor agonist, formoterol for 2 wk on airway function and responsiveness in 17 subjects with mild asthma found it to be effective in single doses in the prevention of methacholine-induced bronchoconstriction.
Effects of genetic polymorphism on ex vivo and in vivo function of beta2-adrenoceptors in asthmatic patients.
- Biology, MedicineChest
- 1999
The results show that genetic polymorphism at codon 16 or 27 does not influence stimulated coupling of lymphocyte beta2-adrenoceptors and similarly did not influence the degree of functional antagonism exhibited by formoterol, demonstrating equal protection against bronchoprotection regardless of genetic polymorphisms.