Pharmacological characterization of abediterol, a novel inhaled β(2)-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical models

The Journal of Pharmacology and Experimental Therapeutics
Mònica ApariciMontserrat Miralpeix

Abstract

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). The potency and onset of action that abediterol shows in isolated human bronchi (EC(50) = 1.9 ± 0.4 nM; t½ onset = 7-10 min) is not significantly different from that of formoterol, but its duration of action (t½ ∼ 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 (t½ = 36 h) than salmeterol (t½ = 6 h) and formoterol (t½ = 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,...Continue Reading

References

Oct 1, 1992·Pharmacology & Toxicology·A B JeppssonB Waldeck
Jun 6, 1991·European Journal of Pharmacology·J CortijoE J Morcillo
Nov 1, 1993·British Journal of Pharmacology·A T NialsC J Vardey
Apr 25, 2002·Canadian Respiratory Journal : Journal of the Canadian Thoracic Society·John KottakisNikolaos Siafakas
May 23, 2002·American Journal of Respiratory and Critical Care Medicine·Nicola A HananiaBurton F Dickey
Jun 18, 2002·European Journal of Pharmacology·Bertil Waldeck
Dec 5, 2002·The Journal of Allergy and Clinical Immunology·L H Philipson
Dec 5, 2002·The Journal of Allergy and Clinical Immunology·Malcolm R Sears
Oct 18, 2003·Naunyn-Schmiedeberg's Archives of Pharmacology·Julio CortijoEsteban J Morcillo
Apr 15, 2004·Allergy·Matthew MasoliUNKNOWN Global Initiative for Asthma (GINA) Program
Jan 3, 2006·The Journal of Allergy and Clinical Immunology·Malcolm Johnson
Jun 15, 2006·The European Respiratory Journal·M A Giembycz, R Newton
Dec 1, 2006·The European Respiratory Journal·E NalineM Molimard
May 1, 2007·Trends in Pharmacological Sciences·Brian J Lipworth
May 29, 2007·Drug Discovery Today·Mary F Fitzgerald, J Craig Fox
Sep 20, 2007·Proceedings of the American Thoracic Society·Nicola A Hanania, James F Donohue
Oct 10, 2009·Current Opinion in Pulmonary Medicine·Mario CazzolaMaria G Matera
Aug 10, 2010·Naunyn-Schmiedeberg's Archives of Pharmacology·Elizabeth M RosethorneSteven J Charlton
Sep 16, 2010·The Annals of Pharmacotherapy·Christie A Robinson
Mar 2, 2011·The Journal of Pharmacology and Experimental Therapeutics·Paola CasarosaFlorian Gantner

❮ Previous
Next ❯

Citations

Nov 20, 2013·Current Opinion in Pulmonary Medicine·Domenico Spina
Jan 26, 2013·American Journal of Respiratory and Critical Care Medicine·Mario CazzolaM Gabriella Matera
Aug 21, 2014·Expert Opinion on Investigational Drugs·Muhammad Ahsan ZafarRalph J Panos
Apr 10, 2013·Expert Opinion on Pharmacotherapy·Mario CazzolaMaria Gabriella Matera
Jan 25, 2017·Expert Opinion on Investigational Drugs·Mario MalerbaJaymin B Morjaria
Nov 12, 2015·European Clinical Respiratory Journal·Domenico Spina
Sep 12, 2017·Expert Opinion on Pharmacotherapy·Ernesto CrisafulliAlfredo Chetta
Nov 27, 2019·Pharmacological Reviews·Stacy Gelhaus WendellCheng Zhang
Sep 5, 2017·Expert Opinion on Emerging Drugs·Thomas J Monaco, Nicola A Hanania
Aug 20, 2019·Respiratory Medicine·Mario CazzolaMaria Gabriella Matera
Dec 29, 2020·Journal of Experimental Pharmacology·Robert M Burkes, Ralph J Panos
Sep 4, 2020·Expert Opinion on Emerging Drugs·Federica Lo BelloGaetano Caramori
Nov 21, 2020·Journal of Medicinal Chemistry·Gang XingMao-Sheng Cheng
Jul 18, 2021·European Journal of Medicinal Chemistry·Gang XingMaosheng Cheng
Jan 15, 2015·Journal of Medicinal Chemistry·Paolo Montuschi, Giovanni Ciabattoni
Nov 11, 2021·Expert Opinion on Pharmacotherapy·W Tatiana Garzon-SiatoyaAlexei Gonzalez-Estrada

❮ Previous
Next ❯

Related Concepts

Related Feeds

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.

Asthma

This feed focuses in Asthma in which your airways narrow and swell. This can make breathing difficult and trigger coughing, wheezing and shortness of breath.

Allergy and Asthma

Allergy and asthma are inflammatory disorders that are triggered by the activation of an allergen-specific regulatory t cell. These t cells become activated when allergens are recognized by allergen-presenting cells. Here is the latest research on allergy and asthma.