"目錄號(hào): HY-14299A
Indacaterol(Onbrez; Arcapta)馬來(lái)酸鹽是超長(zhǎng)效β-腎上腺素受體激動(dòng)劑芥被。
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生物活性
Description
Indacaterol Maleate is an ultra-long-acting β-adrenoceptor agonist.Target: β-adrenoceptorIndacaterol inhibits cAMP production in Chinese hamster ovary cells stably transfected with human β2 adrenoceptors with pEC50 of 8.06. Indacaterol inhibits electrically induced contraction on the electrically stimulated guinea pig trachea in a concentration-dependent manner with pEC50 of 8.23. Indacaterol induces a concentration-dependent inotropic effect with maximal efficacy of 75% in the isolated guinea pig left atrium [1]. Indacaterol reverses the carbachol-induced contraction in a concentration-dependent manner with IC50 of 37 nM in human small airways. Indacaterol concentration dependently reverses the serotonin-induced contraction with IC50 of 10.5 nM in rat small airways. Indacaterol has the highest intrinsic efficacy of 53% in rat small airways and 73% in human small airways [2]. Indacaterol (6.7 μg/kg) inhibits 5-HT-induced bronchoconstriction with a maximal effect of 85% in the conscious guinea pig. Indacaterol (12.5 μg/kg) dose-dependently inhibits methacholine-induced bronchoconstriction with a maximal effect of 85% in the anesthetized rhesus monkey [1].
Clinical Trial
Novartis Pharmaceuticals-Novartis
Asthma
April 18, 2017
Phase 2
Novartis
Chronic Obstructive Pulmonary Disease
February 2008
Phase 2
Novartis
Chronic Obstructive Pulmonary Disease
January 2010
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease
April 28, 2015
Phase 4
National Institute of Respiratory Diseases, Mexico
COPD
April 2013
Phase 4
Hospital Clinic of Barcelona
Chronic Obstructive Pulmonary Disease
October 2015
Phase 4
Novartis
Chronic Obstructive Pulmonary Disease
February 2008
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
November 2012
Phase 4
Novartis-Merck Sharp & Dohme Corp.
Asthma
October 2007
Phase 2
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
March 2009
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
April 2010
Phase 4
Novartis
Chronic Obstructive Pulmonary Disease
January 2010
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
September 2011
Phase 4
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
March 2011
Phase 3
Novartis
Healthy
December 2006
Phase 1
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease
February 2012
Phase 4
Novartis
COPD
May 2008
Phase 3
Irmandade Santa Casa de Misericórdia de Porto Alegre-Novartis
Chronic Obstructive Pulmonary Disease
March 2013
Phase 4
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease
April 2012
Novartis Pharmaceuticals-Novartis
Persistent Asthma
March 2010
Phase 2
Novartis
Chronic Obstructive Pulmonary Disease
April 2008
Phase 3
Novartis
Chronic Obstructive Pulmonary Disease (COPD)
January 2008
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
November 2008
Phase 3
Novartis Pharmaceuticals-Novartis
Patients With Moderate-to-severe COPD With Destroyed Lung by Tuberculosis
February 2013
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
November 2008
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
May 2012
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease
October 2009
Phase 3
Novartis
Chronic Obstructive Pulmonary Disease (COPD)
February 2008
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
March 2009
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
April 2009
Phase 3
Novartis Pharmaceuticals-Novartis
Asthma
September 2007
Phase 3
Novartis
Chronic Obstructive Pulmonary Disease (COPD)
November 2007
Phase 3
Novartis Pharmaceuticals-Novartis
Asthma
November 2006
Phase 2
Novartis Pharmaceuticals-Novartis
Asthma
June 2009
Phase 2
Novartis Pharmaceuticals-Novartis
Asthma
October 2009
Phase 2
University of Milan-Fondazione Salvatore Maugeri
COPD-Lung Diseases-Dyspnea-Hypoxemia-Tachycardia
May 2011
Phase 4
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease
June 2009
Phase 3
Novartis
Chronic Obstructive Pulmonary Disease
December 2006
Phase 2
Novartis Pharmaceuticals-Novartis
COPD
January 2012
Phase 4
Novartis
Pulmonary Disease, Chronic Obstructive-COPD-Lung Diseases, Obstructive
October 2006
Phase 2-Phase 3
Novartis
Asthma
November 2006
Phase 2-Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease
January 2008
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease (COPD)
January 2009
Phase 3
Novartis Pharmaceuticals-Novartis
Asthma
August 2012
Phase 2
Novartis
Chronic Obstructive Pulmonary Disease
October 2006
Phase 3
Novartis Pharmaceuticals-Novartis
Chronic Obstructive Pulmonary Disease
November 2009
Phase 3
Novartis Pharmaceuticals-Novartis
Healthy Volunteers-Chronic Obstructive Pulmonary Disease
April 2008
Phase 1
Novartis Pharmaceuticals-Novartis
Asthma
November 2013
Phase 2
Novartis Pharmaceuticals-Novartis
