DDInter915 DDInter1934
Indacaterol is a novel, ultra-long-acting, rapid onset β(2)-adrenoceptor agonist developed for Novartis for the once-daily management of asthma and chronic obstructive pulmonary disease. It was approved by the European Medicines Agency (EMA) on 30 November 2009 and by the FDA on 1 July 2011. It is marketed in Europe as Onbrez and in America as Arcapta Neohaler. Indacaterol is provided as its maleate salt form. Indacaterol is also a chiral molecule but only the pure R-enantiomer is dispensed.
Vilanterol is a selective long-acting β2-adrenergic agonist (LABA) with inherent 24-hour activity for the once-daily treatment of COPD and asthma. This is in response to the need for longer-acting β2-adrenergic agonists to overcome poor patient compliance (due to the frequency of dosing regimens or complexities of drug administration). Vilanterol was designed based on the salmeterol molecular scaffold, particularly as a antedrug analog of salmeterol modification by modifying the salmeterol molecule to create homochiral compounds with the (R)-configuration. Vilanterol is 1000 and 400 fold more selective for β2 than β1 and β3 adrenoceptors, respectively, with a faster onset of action than salmeterol. Additionally, vilanterol demonstrated a significantly longer duration of action than salmeterol, with the bronchodilator effect still apparent at 22h. Vilanterol's pharmacological effect is attributable to stimulation of intracellular adenylyl cyclase which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increases in cyclic AMP are associated with the relaxation of bronchial smooth muscle and inhibition of the release of hypersensitivity mediators from mast cells in the lungs.[A7738,A259961] Vilanterol is approved for use in several combination products such as with [fluticasone furoate] under the tradename BREO ELLIPTA, with [umeclidinium bromide] as ANORO ELLIPTA, and with both [fluticasone furoate] and [umeclidinium bromide] under the trade name TRELEGY ELLIPTA.[L46481,L44461,L44456] BREO ELLIPTA is the first vilanterol-containing product to be approved by the FDA in May 2013, followed by ANORO ELLIPTA in December 2013 and TRELEGY ELLIPTA in September 2020.[L46876,L46881,L46886] Although all 3 products are approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD), only TRELEGY ELLIPTA and BREO ELLIPTA are approved for maintenance treatments of asthma in patients aged 18 years and older and 5 years and older respectively.[L46481,L44461,L44456]
Indacaterol {u} (Compound) treats {v} (Disease) asthma
asthma {u} (Disease) is treated by {v} (Compound) Hydrocortisone
Hydrocortisone {u} may cause a minor interaction that can limit clinical effects when taken with {v} Vilanterol
Indacaterol {u} (Compound) binds {v} (Gene) ADRB1
ADRB1 {u} (Gene) is bound by {v} (Compound) Formoterol
Formoterol {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Vilanterol
Indacaterol {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Betamethasone
Betamethasone {u} may cause a minor interaction that can limit clinical effects when taken with {v} Vilanterol
Indacaterol {u} (Compound) is included by {v} (Pharmacologic Class) Adrenergic beta2-Agonists
Adrenergic beta2-Agonists {u} (Pharmacologic Class) includes {v} (Compound) Salbutamol
Salbutamol {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Vilanterol
Indacaterol {u} (Compound) causes {v} (Side Effect) Cardiac disorder
Cardiac disorder {u} (Side Effect) is caused by {v} (Compound) Bosutinib
Bosutinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Vilanterol
Indacaterol {u} (Compound) causes {v} (Side Effect) Cardiac disorder
Cardiac disorder {u} (Side Effect) is caused by {v} (Compound) Budesonide
Budesonide {u} may cause a minor interaction that can limit clinical effects when taken with {v} Vilanterol
Indacaterol {u} (Compound) treats {v} (Disease) asthma
asthma {u} (Disease) is treated by {v} (Compound) Orciprenaline
Orciprenaline {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Vilanterol
Indacaterol {u} (Compound) treats {v} (Disease) asthma
asthma {u} (Disease) is palliated by {v} (Compound) Ephedrine
Ephedrine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Vilanterol
Indacaterol {u} (Compound) binds {v} (Gene) ADRB2
ADRB2 {u} (Gene) is downregulated by {v} (Compound) Dasatinib
Dasatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Vilanterol
Indacaterol {u} (Compound) binds {v} (Gene) ADRB2
ADRB2 {u} (Gene) is upregulated by {v} (Compound) Nilotinib
Nilotinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Vilanterol
Indacaterol (Compound) treats asthma (Disease) and asthma (Disease) is treated by Hydrocortisone (Compound) and Hydrocortisone may cause a minor interaction that can limit clinical effects when taken with Vilanterol
Indacaterol (Compound) binds ADRB1 (Gene) and ADRB1 (Gene) is bound by Formoterol (Compound) and Formoterol may cause a moderate interaction that could exacerbate diseases when taken with Vilanterol
Indacaterol (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Betamethasone (Compound) and Betamethasone may cause a minor interaction that can limit clinical effects when taken with Vilanterol
Indacaterol (Compound) is included by Adrenergic beta2-Agonists (Pharmacologic Class) and Adrenergic beta2-Agonists (Pharmacologic Class) includes Salbutamol (Compound) and Salbutamol may cause a moderate interaction that could exacerbate diseases when taken with Vilanterol
Indacaterol (Compound) causes Cardiac disorder (Side Effect) and Cardiac disorder (Side Effect) is caused by Bosutinib (Compound) and Bosutinib may cause a moderate interaction that could exacerbate diseases when taken with Vilanterol
Indacaterol (Compound) causes Cardiac disorder (Side Effect) and Cardiac disorder (Side Effect) is caused by Budesonide (Compound) and Budesonide may cause a minor interaction that can limit clinical effects when taken with Vilanterol
Indacaterol (Compound) treats asthma (Disease) and asthma (Disease) is treated by Orciprenaline (Compound) and Orciprenaline may cause a moderate interaction that could exacerbate diseases when taken with Vilanterol
Indacaterol (Compound) treats asthma (Disease) and asthma (Disease) is palliated by Ephedrine (Compound) and Ephedrine may cause a moderate interaction that could exacerbate diseases when taken with Vilanterol
Indacaterol (Compound) binds ADRB2 (Gene) and ADRB2 (Gene) is downregulated by Dasatinib (Compound) and Dasatinib may cause a moderate interaction that could exacerbate diseases when taken with Vilanterol
Indacaterol (Compound) binds ADRB2 (Gene) and ADRB2 (Gene) is upregulated by Nilotinib (Compound) and Nilotinib may cause a moderate interaction that could exacerbate diseases when taken with Vilanterol