Page last updated: 2024-11-12

vilanterol

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID10184665
CHEMBL ID1198857
CHEBI ID75037
SCHEMBL ID142630
MeSH IDM0547788

Synonyms (48)

Synonym
vilanterol ,
D09696
503068-34-6
vilanterol (usan)
gw 642444
gw642444x
vilanterol [usan:inn]
gw-642444x
unii-028lzy775b
4-(2-((6-((2-(((2,6-dichlorophenyl)methyl)oxy)ethyl)oxy)hexyl)amino)-1-hydroxyethyl)-2-(hydroxymethyl)phenol
1,3-benzenedimethanol, alpha1-(((6-(2-((2,6-dichlorophenyl)methoxy)ethoxy)hexyl)amino)methyl)-4-hydroxy-, (alpha1r)-
4-((1r)-2-((6-(2-((2,6-dichlorophenyl)methoxy)ethoxy)hexyl)amino)-1-hydroxyethyl)-2-(hydroxymethyl)phenol
028lzy775b ,
4-{(1r)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyethyl}-2-(hydroxymethyl)phenol
vilanterolum
bdbm50416060
gw642444
chebi:75037 ,
CHEMBL1198857
gw-642444
gtpl7353
4-[(1r)-2-[(6-{2-[(2,6-dichlorophenyl)methoxy]ethoxy}hexyl)amino]-1-hydroxyethyl]-2-(hydroxymethyl)phenol
4-{(1r)-2-[(6-{2-[(2,6-dichlorophenyl)methoxy]ethoxy}hexyl)amino]-1-hydroxyethyl}-2-(hydroxymethyl)phenol
vilanterol [inn]
vilanterol [who-dd]
vilanterol [vandf]
vilanterol [usan]
1,3-benzenedimethanol, .alpha.1-(((6-(2-((2,6-dichlorophenyl)methoxy)ethoxy)hexyl)amino)methyl)-4-hydroxy-, (.alpha.1r)-
HY-14300
CS-1680
SCHEMBL142630
4-((r)-2-{6-[2-(2,6-dichlorobenzyloxy)-ethoxy]-hexylamino}-1-hydroxyethyl)-2-hydroxymethylphenol
4-((r)-2-{6-[2-(2,6-dichlorobenzyloxy)-ethoxy]-hexylamino}-1-hydroxyethyl)-2-hydroxymethyl-phenol
DAFYYTQWSAWIGS-DEOSSOPVSA-N
AC-33108
DTXSID80198318
mfcd18782703
DB09082
AKOS032950047
BCP25897
vilanterol; gw642444x; gw642444
EX-A2177
4-[(1r)-2-[6-[2-[(2,6-dichlorophenyl)methoxy]ethoxy]hexylamino]-1-hydroxyethyl]-2-(hydroxymethyl)phenol
AS-35120
Q15053666
vilanterol (gw642444; gw 642444x)
AMY6916
EN300-20321625

Research Excerpts

Overview

Vilanterol (VI) is an inhaled long-acting beta-2 agonist. In combination with the ICS fluticasone furoate, is being explored as a once-daily treatment for asthma in children.

ExcerptReferenceRelevance
"Vilanterol (VI) is a novel long-acting beta2 agonist, under development in combination with fluticasone furoate, a new inhaled corticosteroid (ICS)."( Comparison of vilanterol, a novel long-acting beta2 agonist, with placebo and a salmeterol reference arm in asthma uncontrolled by inhaled corticosteroids.
Bateman, ED; Bleecker, ER; Busse, WW; Goldfrad, C; Jacques, L; Lötvall, J; O'Byrne, PM; Toler, WT; Woodcock, A, 2014
)
1.48
"Vilanterol (VI) is an inhaled long-acting beta-2 agonist which, in combination with the ICS fluticasone furoate, is being explored as a once-daily treatment for asthma in children."( Randomised trial of once-daily vilanterol in children with asthma on inhaled corticosteroid therapy.
Covar, RA; Goldfrad, CH; Grigg, J; Klein, RM; Oliver, AJ; Pedersen, SE; Sorkness, CA; Tomkins, SA; Villarán, C, 2016
)
1.44
"Vilanterol trifenate is a new once-daily highly selective β2-agonist available in USA and Europe in association with umeclidinium bromide (a long-acting anti-muscarnic agent) and fluticasone furoate (an inhaled corticosteroid) for the once-daily maintenance treatment of COPD. "( Vilanterol trifenatate for the treatment of COPD.
Malerba, M; Montuschi, P; Morjaria, JB; Radaeli, A, 2016
)
3.32
"Vilanterol (VI) is a novel once-daily long-acting beta₂ agonist with inherent 24-h activity. "( Efficacy and optimal dosing interval of the long-acting beta₂ agonist, vilanterol, in persistent asthma: a randomised trial.
Frith, L; Haumann, B; Jacques, L; Lim, J; Snowise, NG; Sterling, R, 2012
)
2.05

Toxicity

ExcerptReferenceRelevance
" Safety assessments included adverse events, vital signs, ECG assessment, and clinical laboratory tests."( The efficacy and safety of the novel long-acting β2 agonist vilanterol in patients with COPD: a randomized placebo-controlled trial.
Barnhart, F; Crim, C; Feldman, G; Hanania, NA; Haumann, B; Lettis, S; Sanford, L; Shim, JJ; Zachgo, W, 2012
)
0.62
" All doses of VI were associated with a low incidence of treatment-related adverse events/serious adverse events, with no suggestion of effects on BP, pulse rate, QT intervals corrected for heart rate calculated by Fridericia formula, or blood glucose and potassium levels."( The efficacy and safety of the novel long-acting β2 agonist vilanterol in patients with COPD: a randomized placebo-controlled trial.
Barnhart, F; Crim, C; Feldman, G; Hanania, NA; Haumann, B; Lettis, S; Sanford, L; Shim, JJ; Zachgo, W, 2012
)
0.62
" Adverse events (AEs) were reported by 11 (26%) patients in the UMEC/VI group and one (11%) patient in the placebo group."( 28-Day safety and tolerability of umeclidinium in combination with vilanterol in COPD: a randomized placebo-controlled trial.
Brooks, J; Crater, G; Feldman, G; Mehta, R; Walker, RR, 2012
)
0.62
" Safety evaluations included adverse events (AEs), non-fasting glucose, potassium, 24-h urinary cortisol excretion, ophthalmic assessments, heart rate and pulse rate."( Safety and tolerability of the novel inhaled corticosteroid fluticasone furoate in combination with the β2 agonist vilanterol administered once daily for 52 weeks in patients >=12 years old with asthma: a randomised trial.
Andersen, L; Apoux, L; Bateman, ED; Bleecker, ER; Busse, WW; Crawford, J; Hicks, W; Jacques, L; Lötvall, J; O'Byrne, PM; Woodcock, A, 2013
)
0.6
"Repeat doses of UMEC and UMEC/VI in combination with and without verapamil were safe and well tolerated."( Effect of verapamil on systemic exposure and safety of umeclidinium and vilanterol: a randomized and open-label study.
Crater, G; Hughes, S; Kelleher, D; Mehta, R; Preece, A, 2013
)
0.62
"Overall, there were no safety concerns and no major differences were found in treatment-related adverse events when FF and VI were administered alone or in combination."( The safety, pharmacokinetics and pharmacodynamics of a combination of fluticasone furoate and vilanterol in healthy Japanese subjects.
Allen, A; Hirama, T; Kempsford, R; Nakahara, N; Nohda, S; Wakamatsu, A; Yamada, M, 2013
)
0.61
" Safety evaluations included adverse events (AEs), vital signs, 12-lead/24-h Holter electrocardiography parameters and clinical laboratory/haematology measurements."( Efficacy and safety of once-daily umeclidinium/vilanterol 62.5/25 mcg in COPD.
Church, A; Donohue, JF; Kalberg, C; Kilbride, S; Maleki-Yazdi, MR; Mehta, R, 2013
)
0.65
" Both treatments were well tolerated, with no clinically relevant effect on urinary cortisol excretion or vital signs and no treatment-related serious adverse events."( Efficacy and safety of fluticasone furoate/vilanterol compared with fluticasone propionate/salmeterol combination in adult and adolescent patients with persistent asthma: a randomized trial.
Bateman, ED; Bleecker, ER; Busse, WW; Ellsworth, A; Jacques, L; Lötvall, J; Medley, H; O'Byrne, PM; Woodcock, A, 2013
)
0.65
" Six patients in the FF/VI (2%) and three in the FP/SAL (1%) arm experienced serious adverse events, none of which were considered to be drug related."( A comparison of the efficacy and safety of once-daily fluticasone furoate/vilanterol with twice-daily fluticasone propionate/salmeterol in moderate to very severe COPD.
Agustí, A; Barnes, N; Bourbeau, J; Crim, C; De Backer, W; de Teresa, L; Locantore, N; Zvarich, MT, 2014
)
0.63
" The most common on-treatment, severe-intensity adverse event in both studies was acute exacerbation of COPD (1-4 [<1-2%] patients across treatment groups in study 1 and 1-6 [<1-3%] patients in study 2)."( Efficacy and safety of umeclidinium plus vilanterol versus tiotropium, vilanterol, or umeclidinium monotherapies over 24 weeks in patients with chronic obstructive pulmonary disease: results from two multicentre, blinded, randomised controlled trials.
Anzueto, A; Church, A; Crater, G; Decramer, M; Harris, S; Kaelin, T; Kerwin, E; Richard, N; Tabberer, M, 2014
)
0.67
" Pooled adverse events (FF/VI 27%; FP/SAL 28%) and serious adverse events (FF/VI 2%; FP/SAL 3%) were similar between treatments."( Efficacy and safety of once-daily fluticasone furoate/vilanterol (100/25 mcg) versus twice-daily fluticasone propionate/salmeterol (250/50 mcg) in COPD patients.
Crim, C; Dransfield, MT; Feldman, G; Korenblat, P; LaForce, CF; Locantore, N; Martinez, FJ; Pistolesi, M; Watkins, ML, 2014
)
0.65
" Study endpoints included adverse events (AEs), clinical chemistry and hematology parameters, vital signs, 12-lead, and 24-hour Holter electrocardiograms."( Safety and tolerability of once-daily umeclidinium/vilanterol 125/25 mcg and umeclidinium 125 mcg in patients with chronic obstructive pulmonary disease: results from a 52-week, randomized, double-blind, placebo-controlled study.
Brooks, J; Church, A; Donohue, JF; Niewoehner, D; O'Dell, D, 2014
)
0.65
" The incidence of adverse events was similar between treatment groups."( Efficacy and safety of umeclidinium/vilanterol 62.5/25 mcg and tiotropium 18 mcg in chronic obstructive pulmonary disease: results of a 24-week, randomized, controlled trial.
Church, A; Kaelin, T; Maleki-Yazdi, MR; Richard, N; Zvarich, M, 2014
)
0.68
" This systematic review tested the hypothesis that the bronchodilator effect of the LABA/LAMA combination, umeclidinium (UMEC)/vilanterol (VIL), would translate into better outcomes without incurring increased adverse events (AEs)."( A Systematic Review of the Efficacy and Safety of a Fixed-Dose Combination of Umeclidinium and Vilanterol for the Treatment of COPD.
Neffen, H; Rodrigo, GJ, 2015
)
0.84
" Primary outcomes were trough FEV1, serious adverse events (SAEs), and serious cardiovascular events (SCVEs)."( A Systematic Review of the Efficacy and Safety of a Fixed-Dose Combination of Umeclidinium and Vilanterol for the Treatment of COPD.
Neffen, H; Rodrigo, GJ, 2015
)
0.64
" The incidence of on-treatment adverse events (AEs) was 48% with FF/VI 200/25 mcg and 37-40% with other treatments."( Efficacy and safety of fluticasone furoate/vilanterol (50/25 mcg; 100/25 mcg; 200/25 mcg) in Asian patients with chronic obstructive pulmonary disease: a randomized placebo-controlled trial.
Crim, C; de Guia, T; Newlands, AH; Wang, C; Wang-Jairaj, J; Zheng, J; Zhong, N, 2015
)
0.68
" Adverse events (AEs) were also assessed."( Efficacy and safety of umeclidinium added to fluticasone furoate/vilanterol in chronic obstructive pulmonary disease: Results of two randomized studies.
Ali, R; Church, A; Donald, A; Kerwin, E; Siler, TM; Sousa, AR, 2015
)
0.65
" The incidence of adverse events was similar across groups."( Efficacy and safety of once-daily inhaled umeclidinium/vilanterol in Asian patients with COPD: results from a randomized, placebo-controlled study.
Church, A; Goh, AH; Newlands, A; Zheng, J; Zhong, N, 2015
)
0.66
" Safety endpoints included cardiovascular monitoring, cortisol excretion, COPD exacerbations, and adverse events, including prespecified drug effects."( Efficacy and safety of fluticasone furoate/vilanterol or tiotropium in subjects with COPD at cardiovascular risk.
Covelli, H; Crim, C; Emmett, A; Pek, B; Schenkenberger, I; Scott-Wilson, C, 2016
)
0.7
" Secondary end points were the mean change from baseline in percentage rescue-free 24-hour periods, daily morning peak expiratory flow, percentage symptom-free 24-hour periods, Asthma Quality of Life Questionnaire score, adverse events, and severe exacerbations."( Efficacy and safety evaluation of once-daily fluticasone furoate/vilanterol in Asian patients with asthma uncontrolled on a low- to mid-strength inhaled corticosteroid or low-dose inhaled corticosteroid/long-acting beta2-agonist.
Chen, P; Crawford, J; Jacques, L; Kim, MK; Lin, J; Stone, S; Tang, H; Wang, H, 2016
)
0.67
" On-treatment adverse events were 35% with FF/VI (n = 2 [serious]), 31% with placebo; severe exacerbations were FF/VI (n = 1), placebo (n = 7)."( Efficacy and safety evaluation of once-daily fluticasone furoate/vilanterol in Asian patients with asthma uncontrolled on a low- to mid-strength inhaled corticosteroid or low-dose inhaled corticosteroid/long-acting beta2-agonist.
Chen, P; Crawford, J; Jacques, L; Kim, MK; Lin, J; Stone, S; Tang, H; Wang, H, 2016
)
0.67
" Annual rates of moderate/severe exacerbations (primary outcome), selected secondary outcomes, and incidence of pneumonia serious adverse events of special interest (SAESI) were compared between randomisation groups across various patient subgroups/baseline treatment strata."( Benefit and safety of fluticasone furoate/vilanterol in the Salford Lung Study in chronic obstructive pulmonary disease (SLS COPD) according to baseline patient characteristics and treatment subgroups.
Bakerly, ND; Boucot, I; Collier, S; Crawford, J; Harvey, C; Leather, DA; New, JP; Vestbo, J; Woodcock, A, 2019
)
0.78
" CV safety assessments included proportion of patients with and exposure-adjusted rates of on-treatment CV adverse events of special interest (CVAESI) and major adverse cardiac events (MACE), as well as time-to-first (TTF) CVAESI, and TTF CVAESI resulting in hospitalization/prolonged hospitalization or death."( Single-inhaler triple therapy fluticasone furoate/umeclidinium/vilanterol versus fluticasone furoate/vilanterol and umeclidinium/vilanterol in patients with COPD: results on cardiovascular safety from the IMPACT trial.
Criner, G; Day, NC; Dransfield, M; Halpin, DMG; Han, MK; Jones, CE; Kaisermann, MC; Kilbride, S; Kumar, S; Lange, P; Lipson, DA; Lomas, DA; Martin, N; Martinez, FJ; Singh, D; Wise, R, 2020
)
0.8
" The safety endpoint is the occurrence of any adverse events."( Efficacy and safety of once-daily single-inhaler triple therapy for mild-to-moderate chronic obstructive pulmonary disease: a study protocol for a randomised and interventional study.
Inoue, H; Kawaguchi, A; Kawayama, T; Kinoshita, T; Machida, K; Takagi, K; Takahashi, K; Takamori, A; Tashiro, H; Yamasaki, K; Yatera, K, 2023
)
0.91
" Safety endpoints were the incidence of adverse events (AEs), including unexpected AEs/adverse drug reactions (ADRs) and serious AEs/ADRs."( Real-World Safety and Effectiveness of Fluticasone Furoate/Vilanterol in Patients with Asthma and/or Chronic Obstructive Pulmonary Disease: A Post-Marketing Study in Korea.
Cho, EY; Cho, JE; Hwang, KE; Jang, SH, 2023
)
1.15

Pharmacokinetics

A population pharmacokinetic analysis was conducted from a subset of samples obtained from the Lung Function and Quality of Life Assessment in Chronic Obstructive Pulmonary Disease with Closed Triple Therapy trial. There were no apparent pharmacokinetics when umeclidinium and vilanterol were co-administered in patients with COPD.

ExcerptReferenceRelevance
" Pharmacodynamic and PK data were obtained up to 48 h following the VI dose."( The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of inhaled fluticasone furoate and vilanterol trifenatate in healthy subjects.
Allen, A; Bal, J; Kempsford, R; Rubin, D; Tombs, L, 2013
)
0.6
"In study 1, there was no effect of co-administration of ketoconazole and VI on pharmacodynamic or PK parameters."( The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of inhaled fluticasone furoate and vilanterol trifenatate in healthy subjects.
Allen, A; Bal, J; Kempsford, R; Rubin, D; Tombs, L, 2013
)
0.6
" There was no increase in β-agonist systemic pharmacodynamic effects, while serum cortisol was decreased by 27%."( The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of inhaled fluticasone furoate and vilanterol trifenatate in healthy subjects.
Allen, A; Bal, J; Kempsford, R; Rubin, D; Tombs, L, 2013
)
0.6
"To assess the effects of renal and hepatic impairment on the pharmacokinetic and pharmacodynamic properties and tolerability of fluticasone furoate/vilanterol (FF/VI) administered in combination."( Influence of renal and hepatic impairment on the pharmacokinetic and pharmacodynamic properties and tolerability of fluticasone furoate and vilanterol in combination.
Allen, A; Davis, A; Hardes, K; Kempsford, R; Tombs, L, 2012
)
0.78
"Severe renal impairment had no apparent clinically relevant effects on the pharmacokinetic or pharmacodynamic properties or tolerability of FF/VI."( Influence of renal and hepatic impairment on the pharmacokinetic and pharmacodynamic properties and tolerability of fluticasone furoate and vilanterol in combination.
Allen, A; Davis, A; Hardes, K; Kempsford, R; Tombs, L, 2012
)
0.58
" Individual pharmacokinetic parameters of FF and VI differed when co-administered but the differences from monotherapy were not clinically significant."( The safety, pharmacokinetics and pharmacodynamics of a combination of fluticasone furoate and vilanterol in healthy Japanese subjects.
Allen, A; Hirama, T; Kempsford, R; Nakahara, N; Nohda, S; Wakamatsu, A; Yamada, M, 2013
)
0.61
" Umeclidinium and vilanterol population-pharmacokinetic model-based systemic exposure predictions showed no pharmacokinetic interactions between umeclidinium and vilanterol when administered in combination."( Population pharmacokinetics of inhaled umeclidinium and vilanterol in patients with chronic obstructive pulmonary disease.
Beerahee, M; Church, A; Goyal, N; Kalberg, C; Kilbride, S; Mehta, R, 2014
)
0.98
"There were no apparent pharmacokinetic interactions when umeclidinium and vilanterol were co-administered in patients with COPD."( Population pharmacokinetics of inhaled umeclidinium and vilanterol in patients with chronic obstructive pulmonary disease.
Beerahee, M; Church, A; Goyal, N; Kalberg, C; Kilbride, S; Mehta, R, 2014
)
0.88
"The objectives of the study were to evaluate the effects of moderate hepatic impairment on the plasma and urinary pharmacokinetic properties of each drug, and on the tolerability of inhalational UMEC/VI 125/25 µg and UMEC 125 µg."( Effects of moderate hepatic impairment on the pharmacokinetic properties and tolerability of umeclidinium and vilanterol in inhalational umeclidinium monotherapy and umeclidinium/vilanterol combination therapy: an open-label, nonrandomized study.
Brealey, N; Hardes, K; Kelleher, D; Mehta, R; Preece, A; Tombs, L, 2014
)
0.61
" Primary end points were the plasma pharmacokinetic properties of single- and repeat-dose UMEC and VI."( Effects of moderate hepatic impairment on the pharmacokinetic properties and tolerability of umeclidinium and vilanterol in inhalational umeclidinium monotherapy and umeclidinium/vilanterol combination therapy: an open-label, nonrandomized study.
Brealey, N; Hardes, K; Kelleher, D; Mehta, R; Preece, A; Tombs, L, 2014
)
0.61
" UMEC accumulation following repeat dosing was 11–34% based on Cmax and 19–59% based on area under the concentration-time curve from time zero to 2 h (AUC(0-2))."( Pharmacokinetics and tolerability of inhaled umeclidinium and vilanterol alone and in combination in healthy Chinese subjects: a randomized, open-label, crossover trial.
Dong, K; Gross, A; Hu, C; Jia, J; Luo, L; Mehta, R; Peng, J; Ren, Y; Wu, K; Yu, H, 2015
)
0.66
"To investigate the pharmacodynamic and pharmacokinetic profiles of fluticasone furoate (FF)/vilanterol (VI) - a fixed-dose combination of an inhaled corticosteroid (ICS) and a long-acting β2 -agonist for the treatment of asthma and chronic obstructive pulmonary disease - after single and repeat administration in healthy Chinese subjects."( Pharmacodynamics and pharmacokinetics of fluticasone furoate/vilanterol in healthy Chinese subjects.
Allen, A; Chen, X; Du, X; Hu, P; Jiang, J; Kempsford, R; Liu, L; Wu, K; Zheng, X; Zhuang, L, 2015
)
0.88
"The co-primary outcome measures reflected pharmacodynamic responses relating to recognized class effects of the two drug classes: reduced serum cortisol level (ICSs), and increased Fridericia's corrected QT interval (QTcF) and reduced serum potassium level (long-acting β2 -agonists)."( Pharmacodynamics and pharmacokinetics of fluticasone furoate/vilanterol in healthy Chinese subjects.
Allen, A; Chen, X; Du, X; Hu, P; Jiang, J; Kempsford, R; Liu, L; Wu, K; Zheng, X; Zhuang, L, 2015
)
0.66
"In healthy Chinese subjects, minimal and non-clinically relevant β-adrenergic pharmacodynamic effects were observed with FF/VI doses ranging from 50/25 to 200/25 μg."( Pharmacodynamics and pharmacokinetics of fluticasone furoate/vilanterol in healthy Chinese subjects.
Allen, A; Chen, X; Du, X; Hu, P; Jiang, J; Kempsford, R; Liu, L; Wu, K; Zheng, X; Zhuang, L, 2015
)
0.66
" These are the first studies where pharmacokinetic (PK) profile assessment was possible for this inhaled triple fixed-dose combination product."( Pharmacokinetics of fluticasone furoate, umeclidinium, and vilanterol as a triple therapy in healthy volunteers.
Allen, A; Brealey, N; Gupta, A; Henderson, A; Mehta, R; Renaux, J, 2015
)
0.66
"Population pharmacokinetic (PK) methods were used to characterize the PK of fluticasone furoate (FF) and vilanterol (VI) in patients with asthma following once daily inhaled FF/VI and FF and to identify significant covariates that impact the PK."( Population pharmacokinetics of inhaled fluticasone furoate and vilanterol in adult and adolescent patients with asthma.
Allen, A; Siederer, S; Yang, S, 2016
)
0.89
"To investigate the potential for systemic pharmacokinetic (PK) and pharmacodynamic (PD) interactions between inhaled fluticasone furoate (FF) and vilanterol (VI) when delivered simultaneously via the ELLIPTA™ dry powder inhaler (DPI)."( The pharmacodynamics, pharmacokinetics, safety and tolerability of inhaled fluticasone furoate and vilanterol administered alone or simultaneously as fluticasone furoate/vilanterol.
Allen, A; Bareille, P; Cheesbrough, A; Hamilton, M; Kempsford, R, 2015
)
0.83
"A population pharmacokinetic analysis was conducted from a subset of samples obtained from the Lung Function and Quality of Life Assessment in Chronic Obstructive Pulmonary Disease with Closed Triple Therapy trial to characterize the pharmacokinetics of fluticasone furoate, umeclidinium, and vilanterol in patients with symptomatic COPD following treatment with fluticason furoate-umeclidinium-vilanterol combined in a single inhaler."( Population Pharmacokinetic Analysis of Fluticasone Furoate/Umeclidinium/Vilanterol via a Single Inhaler in Patients with COPD.
Barnacle, H; Beerahee, M; Birk, R; Brealey, N; Lipson, DA; Mehta, R; Pefani, E; Zhu, CQ, 2018
)
0.89
"Population pharmacokinetic methods were used to characterize the pharmacokinetics of fluticasone furoate (FF), umeclidinium (UMEC), and vilanterol (VI) in patients with chronic obstructive pulmonary disease (COPD) when administered as a fixed-dose combination via a single closed inhaler."( Population Pharmacokinetic Analysis of Fluticasone Furoate/Umeclidinium Bromide/Vilanterol in Patients with Chronic Obstructive Pulmonary Disease.
Birk, R; Farrell, C; Hayes, S; Lipson, DA; Mehta, R; Okour, M, 2020
)
0.99

Compound-Compound Interactions

Umeclidinium (UMEC; GSK573719) is a new long-acting muscarinic antagonist (LAMA) Currently in development in combination with vilanterol (VI), an inhaled beta₂ agonist for the treatment of chronic obstructive pulmonary disease (COPD)

ExcerptReferenceRelevance
"Umeclidinium (UMEC; GSK573719) is a new long-acting muscarinic antagonist (LAMA) currently in development in combination with vilanterol (VI), an inhaled, long-acting beta₂ agonist for the treatment of chronic obstructive pulmonary disease (COPD)."( 28-Day safety and tolerability of umeclidinium in combination with vilanterol in COPD: a randomized placebo-controlled trial.
Brooks, J; Crater, G; Feldman, G; Mehta, R; Walker, RR, 2012
)
0.82
"Once-daily dosing with UMEC in combination with VI in patients with moderate-to-very-severe COPD was well tolerated over 28 days."( 28-Day safety and tolerability of umeclidinium in combination with vilanterol in COPD: a randomized placebo-controlled trial.
Brooks, J; Crater, G; Feldman, G; Mehta, R; Walker, RR, 2012
)
0.62
"The inhaled corticosteroid fluticasone furoate (FF) in combination with the long-acting β2 agonist vilanterol (VI) is in development for asthma and chronic obstructive pulmonary disease."( Safety and tolerability of the novel inhaled corticosteroid fluticasone furoate in combination with the β2 agonist vilanterol administered once daily for 52 weeks in patients >=12 years old with asthma: a randomised trial.
Andersen, L; Apoux, L; Bateman, ED; Bleecker, ER; Busse, WW; Crawford, J; Hicks, W; Jacques, L; Lötvall, J; O'Byrne, PM; Woodcock, A, 2013
)
0.82

Bioavailability

ExcerptReferenceRelevance
" Compound 13f had high potency, selectivity, fast onset, and long duration of action in vitro and was found to have long duration in vivo, low oral bioavailability in the rat, and to be rapidly metabolized."( Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
Barrett, VJ; Bevan, NJ; Biggadike, K; Box, PC; Butchers, PR; Coe, DM; Conroy, R; Emmons, A; Ford, AJ; Holmes, DS; Horsley, H; Kerr, F; Li-Kwai-Cheung, AM; Looker, BE; Mann, IS; McLay, IM; Morrison, VS; Mutch, PJ; Procopiou, PA; Smith, CE; Tomlin, P, 2010
)
0.36

Dosage Studied

Fluticasone furoate/vilanterol (FF/VI) is a novel inhaled corticosteroid/long-acting β₂-agonist (ICS/LABA) fixed dose combination. It offers several benefits from both drugs, such as a convenient once daily dosing schedule and high lipophilicity.

ExcerptRelevanceReference
" Although our study was not powered to demonstrate non-inferiority of once- versus twice-daily dosing of VI, the data suggest no advantage over a 24-h period of twice-daily over once-daily dosing for the same total daily dose."( Efficacy and optimal dosing interval of the long-acting beta₂ agonist, vilanterol, in persistent asthma: a randomised trial.
Frith, L; Haumann, B; Jacques, L; Lim, J; Snowise, NG; Sterling, R, 2012
)
0.61
" Results from Phase II studies have shown clinically and statistically significant improvements over placebo in trough (24-hour postdose) forced expiratory volume in 1 second (FEV(1)) after once-daily dosing with FF or VI (VI concurrently with an inhaled corticosteroid) in asthma and VI in COPD."( Effect of once-daily fluticasone furoate/vilanterol on 24-hour pulmonary function in patients with chronic obstructive pulmonary disease: a randomized, three-way, incomplete block, crossover study.
Boscia, JA; Crim, C; Pudi, KK; Sanford, L; Siederer, SK; Zvarich, MT, 2012
)
0.64
"Patients (aged ≥40 years) who completed a 2-week placebo run-in period were randomized to 1 of 18 three-course sequences of placebo and 2 of 3 dose combinations of FF/VI (50/25 μg, 100/25 μg, and 200/25 μg), dosed once daily in the morning."( Effect of once-daily fluticasone furoate/vilanterol on 24-hour pulmonary function in patients with chronic obstructive pulmonary disease: a randomized, three-way, incomplete block, crossover study.
Boscia, JA; Crim, C; Pudi, KK; Sanford, L; Siederer, SK; Zvarich, MT, 2012
)
0.64
" The primary aim of this study was to evaluate the safety and tolerability of repeat dosing of UMEC and VI in combination once daily for 28 days in patients with COPD."( 28-Day safety and tolerability of umeclidinium in combination with vilanterol in COPD: a randomized placebo-controlled trial.
Brooks, J; Crater, G; Feldman, G; Mehta, R; Walker, RR, 2012
)
0.62
"Once-daily dosing with UMEC in combination with VI in patients with moderate-to-very-severe COPD was well tolerated over 28 days."( 28-Day safety and tolerability of umeclidinium in combination with vilanterol in COPD: a randomized placebo-controlled trial.
Brooks, J; Crater, G; Feldman, G; Mehta, R; Walker, RR, 2012
)
0.62
" This pharmacological profile combined with clinical data is consistent with once a day dosing of vilanterol in the treatment of both asthma and chronic obstructive pulmonary disease (COPD)."( In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action.
Barrett, VJ; Emmons, AJ; Ford, AJ; Knowles, RG; Morrison, VS; Slack, RJ; Sturton, RG, 2013
)
0.87
" All VI doses produced increases in FEV(1) from as early as 5 min after dosing which were maintained up to 24 h post-dose in subjects with asthma and COPD."( Vilanterol trifenatate, a novel inhaled long-acting beta2 adrenoceptor agonist, is well tolerated in healthy subjects and demonstrates prolonged bronchodilation in subjects with asthma and COPD.
Kempsford, R; Norris, V; Siederer, S, 2013
)
1.83
" Peak plasma concentration of FF and VI following repeat dosing was up to two times higher compared with the single dose."( The safety, pharmacokinetics and pharmacodynamics of a combination of fluticasone furoate and vilanterol in healthy Japanese subjects.
Allen, A; Hirama, T; Kempsford, R; Nakahara, N; Nohda, S; Wakamatsu, A; Yamada, M, 2013
)
0.61
"In healthy Japanese subjects, no safety concerns were found following repeat dosing of FF and VI or single dosing of FF, VI and FF/VI."( The safety, pharmacokinetics and pharmacodynamics of a combination of fluticasone furoate and vilanterol in healthy Japanese subjects.
Allen, A; Hirama, T; Kempsford, R; Nakahara, N; Nohda, S; Wakamatsu, A; Yamada, M, 2013
)
0.61
"Repeat once-daily dosing of FF/VI (200/25 μg), which is the highest therapeutic strength used in phase III studies, is not associated with QTc prolongation in healthy subjects."( A repeat-dose thorough QT study of inhaled fluticasone furoate/vilanterol combination in healthy subjects.
Allen, A; Crim, C; Kelly, K; Kempsford, R; Saggu, P, 2014
)
0.64
"To investigate the effect of time of day of dosing (morning or evening) on lung function following administration of fluticasone furoate (FF)/vilanterol (VI) 100/25 mcg."( The efficacy of once-daily fluticasone furoate/vilanterol in asthma is comparable with morning or evening dosing.
Bal, J; Kempsford, RD; Oliver, A; Quinn, D; Tombs, L, 2013
)
0.85
"FF/VI 100/25 administered morning or evening produced clinically significant increases in weighted mean FEV1: the differences [95% confidence interval (CI)] from placebo were 377 mL [293, 462] and 422 mL [337, 507], respectively; the difference between morning and evening dosing was -44 mL [-125, 36]."( The efficacy of once-daily fluticasone furoate/vilanterol in asthma is comparable with morning or evening dosing.
Bal, J; Kempsford, RD; Oliver, A; Quinn, D; Tombs, L, 2013
)
0.65
"FF/VI 100/25 produces comparable improvements in lung function whether dosed in the morning or evening in subjects with persistent asthma."( The efficacy of once-daily fluticasone furoate/vilanterol in asthma is comparable with morning or evening dosing.
Bal, J; Kempsford, RD; Oliver, A; Quinn, D; Tombs, L, 2013
)
0.65
" The once-daily dosing might improve adherence in select patients."( Combination of fluticasone furoate and vilanterol for the treatment of chronic obstructive pulmonary disease.
Bollmeier, SG; Prosser, TR, 2014
)
0.67
"Once-daily repeated dosing of FF/VI, 100/25 µg, using the ELLIPTA dry powder inhaler was as well tolerated as FF, 100 µg, in this small, selected population of 5- to 11-year-old, mostly white/caucasian children with persistent asthma."( Tolerability of fluticasone furoate/vilanterol combination therapy in children aged 5 to 11 years with persistent asthma.
Allen, A; Hamilton, M; Inamdar, A; Kempsford, R; Oliver, A; Tombs, L; VanBuren, S, 2014
)
0.68
" UMEC accumulations with 7-day dosing of UMEC were similar between patients with moderate hepatic impairment and healthy volunteers."( Effects of moderate hepatic impairment on the pharmacokinetic properties and tolerability of umeclidinium and vilanterol in inhalational umeclidinium monotherapy and umeclidinium/vilanterol combination therapy: an open-label, nonrandomized study.
Brealey, N; Hardes, K; Kelleher, D; Mehta, R; Preece, A; Tombs, L, 2014
)
0.61
"Fluticasone furoate/vilanterol (FF/VI) is a novel inhaled corticosteroid/long-acting β₂-agonist (ICS/LABA) fixed dose combination that, by simplifying the dosing schedule, allows, for the first time in a member of the ICS/LABA class, a shift from twice-daily to once-daily treatment."( Fluticasone furoate and vilanterol inhalation powder for the treatment of chronic obstructive pulmonary disease.
Capuano, A; Cazzola, M; Matera, MG, 2015
)
1.05
" This allows lower dosing of individual medications, which may limit adverse effects."( Umeclidinium/vilanterol combination inhaler efficacy and potential impact on current chronic obstructive pulmonary disease management guidelines.
Davidson, JF; Donohue, JF; Ohar, JA, 2015
)
0.79
" UMEC and VI were rapidly absorbed following single and repeat dosing (time to maximum plasma concentration [tmax]: UMEC = 5 min; VI = 5 min)."( Pharmacokinetics and tolerability of inhaled umeclidinium and vilanterol alone and in combination in healthy Chinese subjects: a randomized, open-label, crossover trial.
Dong, K; Gross, A; Hu, C; Jia, J; Luo, L; Mehta, R; Peng, J; Ren, Y; Wu, K; Yu, H, 2015
)
0.66
" FF/VI, by simplifying the dosing schedule, allows, for the first time, a shift from twice-daily to once-daily treatment, with an acceptable safety and tolerability profile that is consistent with the ICS/LABA class."( Fluticasone furoate/vilanterol combination for the treatment of COPD and asthma.
Cazzola, M; Matera, MG; Rogliani, P, 2015
)
0.74
" The once-daily dosing is well tolerated, with limited clinically significant adverse events; the once-daily inhaled dosing regimen should also improve medication adherence."( The combination of fluticasone furoate and vilanterol trifenatate in the management of asthma: clinical trial evidence and experience.
Albertson, TE; Richards, JR; Zeki, AA, 2016
)
0.7
" The effect of race on PK of FF or VI does not have impact on dosage adjustments for FF/VI in East Asian patients with asthma."( Population pharmacokinetics of inhaled fluticasone furoate and vilanterol in adult and adolescent patients with asthma.
Allen, A; Siederer, S; Yang, S, 2016
)
0.67
" It is hoped that OD dosage of FF/VI can improve adherence and hence asthma control in these patients, however evidence to support this has yet to become available."( Fluticasone furoate and vilanterol trifenatate combination therapy for the treatment of asthma.
Chang, V; Gray, EL; Thomas, PS, 2016
)
0.74
" The advantage of them are related with higher adherence and better acceptability by the patients as compared to both components dosed with individual inhalers."( Triple fixed inhaled therapy in frequent chronic obstructive pulmonary disease exacerbators: potential advantages for various degrees of airways obstruction.
Antohe, I; Antoniu, SA; Gavrilovici, C, 2018
)
0.48
" To encourage patient adherence, two classes of medication are often combined in a single medication device; it seems that once-daily dosing offers greatest convenience to patients and may markedly influence adherence."( Once-daily long-acting beta₂-agonists/inhaled corticosteroids combined inhalers versus inhaled long-acting muscarinic antagonists for people with chronic obstructive pulmonary disease.
Bala, MM; Gross-Sondej, I; Jankowski, M; Nowobilski, R; Sliwka, A; Storman, M, 2018
)
0.48
" It offers several benefits from both drugs, such as a convenient once daily dosing schedule; high lipophilicity; high receptor affinity of fluticasone furoate along with high functional selectivity and a quick onset of action of vilanterol."( ICS/Ultra LABA in the Treatment of Obstructive Airway Diseases: A Consensus of Indian Experts.
Barkate, H; Bhagat, S; Dhar, R; James, P; Khatri, N; Mishra, A; Patil, S; Talwar, D; Vachaparambil, J, 2022
)
0.9
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
beta-adrenergic agonistAn agent that selectively binds to and activates beta-adrenergic receptors.
bronchodilator agentAn agent that causes an increase in the expansion of a bronchus or bronchial tubes.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
etherAn organooxygen compound with formula ROR, where R is not hydrogen.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
benzyl alcoholsCompounds containing a phenylmethanol skeleton.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
dichlorobenzeneAny member of the class of chlorobenzenes carrying two chloro groups at unspecified positions.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1346250Human beta2-adrenoceptor (Adrenoceptors)2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID1760549Inhibition of acetylcholine-induced bronchoconstriction in guinea pig assessed as duration of action by measuring half life2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Recent Advances in β
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (236)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's180 (76.27)24.3611
2020's56 (23.73)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 79.33

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index79.33 (24.57)
Research Supply Index5.88 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index137.74 (26.88)
Search Engine Supply Index2.04 (0.95)

This Compound (79.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials111 (45.31%)5.53%
Reviews44 (17.96%)6.00%
Case Studies2 (0.82%)4.05%
Observational6 (2.45%)0.25%
Other82 (33.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]