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fluticasone furoate

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Description

fluticasone furoate: a glucocorticoid; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

fluticasone furoate : A trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a 2-furoyl substituent at position 17. Used in combination with vilanterol trifenate for treatment of bronchospasm associated with chronic obstructive pulmonary disease. [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]

Cross-References

ID SourceID
PubMed CID9854489
CHEMBL ID1676
CHEBI ID74899
SCHEMBL ID140504
MeSH IDM0514058

Synonyms (86)

Synonym
(6alpha,11alpha,14beta,16alpha,17alpha)-6,9-difluoro-17-{[(fluoromethyl)sulfanyl]carbonyl}-11-hydroxy-16-methyl-3-oxoan drosta-1,4-dien-17-yl furan-2-carboxylate
gw6 ,
veramyst
avamys
fluticasone furoate
allermist
gw-685698x
gw-685698
397864-44-7
veramyst (tn)
fluticasone furoate (jan/usan/inn)
D06315
(6alpha,11beta,16alpha,17alpha)-6,9-difluoro-17-(((fluoromethyl)thio)carbonyl)-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl-2-furancarboxylate
6alpha,9-difluoro-17-(((fluoromethyl)sulfanyl)carbonyl)-11beta-hydroxy-16alpha-methyl-3-oxoandrosta-1,4-dien-17alpha-yl furan-2-carboxylate
gw 685698x
androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-17-((2- furanylcarbonyl)oxy)-11-hydroxy-16-methyl-3-oxo-, s-(fluoromethyl) ester, (6alpha,11beta,16alpha,17alpha)-
gw685698x
gsk 685 698
gsk685968
gsk-685968
CHEMBL1676
furamist
ennhale
chebi:74899 ,
arnuity ellipta
flonase sensimist allergy relief
fluticasone furoate [usan:inn]
androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-17-((2- furanylcarbonyl)oxy)-11-hydroxy-16-methyl-3-oxo-, s-(fluoromethyl) ester, (6alpha,11beta,16alpha,17alpha)-
unii-js86977wnv
flonase sensimist
js86977wnv ,
alisade
gsk 685698
bdbm50354851
fluticasonum furoas
furoato de fluticasona
furoate de fluticasone
6alpha,9-difluoro-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-11beta-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17alpha-yl 2-furoate
fluticasone furoate component of arnuity ellipta
fluticasone furoate [usan]
(6.alpha.,11.beta.,16.alpha.,17.alpha.)-6,9-difluoro-17-(((fluoro-methyl)thio)carbonyl)-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl 2-furancarboxylate
breo ellipta component fluticasone furoate
(6.alpha.,11.beta.,16.alpha.,17.alpha.)-6,9-difluoro-17-(((fluoromethyl)thio)carbonyl)-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl 2-furoate
fluticasone furoate component of trelegy ellipta
trelegy ellipta component fluticasone furoate
fluticasone furoate [vandf]
fluticasone furoate [jan]
fluticasone furoate [who-dd]
fluticasone furoate [ema epar]
6alpha,9-difluoro-17-[[(fluoromethyl)sulfanyl]carbonyl]-11beta-hydroxy-16alpha-methyl-3-oxoandrosta-1,4-dien-17alpha-yl furan-2-carboxylate
(6.alpha.,11.beta.,16.alpha.,17.alpha.)-6,9-difluoro-17-(((fluoromethyl)thio)carbonyl)-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl-2-furancarboxylate
fluticasone furoate [mi]
fluticasone furoate component of breo ellipta
arnuity ellipta component fluticasone furoate
fluticasone furoate [inn]
androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-17-((2-furanylcarbonyl)oxy)-11-hydroxy-16-methyl-3-oxo-, s-(fluoromethyl) ester, (6.alpha.,11.beta.,16.alpha.,17.alpha.)-
fluticasone furoate [mart.]
fluticasone furoate [orange book]
S6487
DB08906
SCHEMBL140504
[(6s,8s,9r,10s,11s,13s,14s,16r,17r)-6,9-difluoro-17-(fluoromethylsulfanylcarbonyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] furan-2-carboxylate
gw685698
(6alpha,11alpha,14beta,16alpha,17alpha)-6,9-difluoro-17-{[(fluoromethyl)sulfanyl]carbonyl}-11-hydroxy-16-methyl-3-oxoan
drosta-1,4-dien-17-yl furan-2-carboxylate
(6alpha,11alpha,14beta,16alpha,17alpha)-6,9-difluoro-17-{[(fluoromethyl)sulfanyl]carbonyl}-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl furan-2-carboxylate
avamys pound>> veramyst pound>> allermist
BCP18136
HY-15234
Q2166700
gtpl10892
CS-0003822
(6s,8s,9r,10s,11s,13s,14s,16r,17r)-6,9-difluoro-17-(((fluoromethyl)thio)carbonyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3h-cyclopenta[a]phenanthren-17-yl furan-2-carboxylate
MS-29934
DTXSID401024827
EN300-19659651
(1r,2r,3as,3bs,5s,9as,9br,10s,11as)-5,9b-difluoro-1-{[(fluoromethyl)sulfanyl]carbonyl}-10-hydroxy-2,9a,11a-trimethyl-7-oxo-1h,2h,3h,3ah,3bh,4h,5h,7h,9ah,9bh,10h,11h,11ah-cyclopenta[a]phenanthren-1-yl furan-2-carboxylate
E86983
AKOS040744839
(6alpha,11beta,16alpha,17alpha)-6,9-difluoro-17-(((fluoromethyl)thio)carbonyl)-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl 2-furoate
fluticasone furoate (mart.)
6alpha,9-difluoro-17beta-((fluoromethylsulfanyl)carbonyl)-11beta-hydroxy-16alpha-methyl-3-oxoandrosta-1,4-dien-17alpha-yl furan-2-carboxylate
(6alpha,11beta,16alpha,17alpha)-6,9-difluoro-17-(((fluoro-methyl)thio)carbonyl)-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl 2-furancarboxylate
6alpha,9-difluoro-17beta-(((fluoromethyl)sulfanyl)carbonyl)-11beta-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17alpha-yl 2-furoate
androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-17-((2-furanylcarbonyl)oxy)-11-hydroxy-16-methyl-3-oxo-, s-(fluoromethyl) ester, (6alpha,11beta,16alpha,17alpha)-
flonase sensimistallergy relief

Research Excerpts

Overview

Fluticasone furoate (FF) is an intranasal corticosteroid indicated for the treatment of allergic rhinitis (AR) It has been shown to improve lung function vs. placebo. Fluticas one furoates is a novel, once-daily ICS asthma therapy.

ExcerptReferenceRelevance
"Fluticasone furoate (FF) is a novel inhaled corticosteroid with 24-h activity. "( Inhaled fluticasone furoate/vilanterol does not affect hypothalamic-pituitary-adrenal axis function in adolescent and adult asthma: randomised, double-blind, placebo-controlled study.
Allen, A; Cole, J; Gul, N; Hicks, W; Jacques, L; Schenkenberger, I; Trivedi, R, 2013
)
2.27
"Fluticasone furoate (FF) is an intranasal corticosteroid indicated for the treatment of allergic rhinitis (AR). "( Fluticasone furoate inhibits cytokine secretion from nasal epithelial cells and reduces eosinophil survival in an in vitro model of eosinophilic inflammation.
Alobid, I; de Borja Callejas, F; Fuentes, M; Mullol, J; Pérez-Gonzalez, M; Picado, C; Pujols, L; Roca-Ferrer, J; Valero, A, 2014
)
3.29
"Fluticasone furoate (FF) is a new inhaled corticosteroid (ICS) suitable for once-daily dosing in asthma."( Efficacy and safety of fluticasone furoate 100 μg and 200 μg once daily in the treatment of moderate-severe asthma in adults and adolescents: a 24-week randomised study.
Bateman, ED; Busse, WW; Ellsworth, A; Jacques, L; Lötvall, J; Stone, S; Woodcock, A, 2014
)
1.43
"Fluticasone furoate (FF) is a novel, once-daily ICS asthma therapy."( Once-daily fluticasone furoate 50 mcg in mild-to-moderate asthma: a 24-week placebo-controlled randomized trial.
Bateman, ED; Busse, WW; Forth, R; Jacques, L; Lötvall, J; Medley, H; O'Byrne, PM; Woodcock, A, 2014
)
1.51
"Fluticasone furoate (FF) is a novel, once-daily inhaled corticosteroid (ICS) that has been shown to improve lung function vs. "( Efficacy and safety of once-daily fluticasone furoate 50 mcg in adults with persistent asthma: a 12-week randomized trial.
Bateman, ED; Bleecker, ER; Busse, WW; Forth, R; Jacques, L; Lötvall, J; Medley, H; O'Byrne, PM; Woodcock, A, 2014
)
2.12
"Fluticasone furoate is an enhanced-affinity glucocorticoid receptor agonist, with potent anti-inflammatory activity."( Fluticasone furoate/vilanterol: a review of its use in patients with asthma.
Syed, YY, 2015
)
2.58
"Fluticasone furoate (FF) is a novel inhaled corticosteroid (ICS). "( Phamacology of fluticasone furoate and vilanterol trifenatate combination therapy for asthma.
Chang, V; Gray, EL; Thomas, PS, 2016
)
2.23
"Fluticasone furoate is a once-daily inhaled corticosteroid. "( Integrated safety and efficacy analysis of once-daily fluticasone furoate for the treatment of asthma.
Busse, WW; Goldfrad, C; Jacques, L; Kwon, N; O'Byrne, PM; Perrio, M; Yates, LJ, 2016
)
2.13
"Fluticasone furoate is a novel enhanced-affinity glucocorticoid for the treatment of allergic rhinitis."( Effect of once-daily fluticasone furoate nasal spray on nasal symptoms in adults and adolescents with perennial allergic rhinitis.
Berger, W; Cheema, A; Nathan, RA; Philpot, E; Silvey, M; Wu, W; Yang, W, 2008
)
1.39
"Fluticasone furoate is a novel glucocorticoid developed for the treatment of allergic rhinitis and other inflammatory diseases. "( Fluticasone furoate nasal spray in allergic rhinitis.
Goyal, N; Hochhaus, G, 2008
)
3.23
"Fluticasone furoate is an enhanced-affinity glucocorticoid with potent anti-inflammatory activity."( Fluticasone furoate nasal spray consistently and significantly improves both the nasal and ocular symptoms of seasonal allergic rhinitis: a review of the clinical data.
Keith, PK; Scadding, GK, 2008
)
2.51
"Fluticasone furoate is a novel enhanced-affinity corticosteroid that has demonstrated favourable safety and tolerability in paediatric patients. "( Safety and tolerability of fluticasone furoate nasal spray once daily in paediatric patients aged 6-11 years with allergic rhinitis: subanalysis of three randomized, double-blind, placebo-controlled, multicentre studies.
Máspero, JF; Meltzer, EO; Philpot, E; Tripathy, I; Wu, W, 2009
)
2.09
"Fluticasone furoate (FF) is a novel enhanced-affinity corticosteroid for the treatment of allergic rhinitis, delivered by a unique side-actuated device. "( Effectiveness of fluticasone furoate 110 microg once daily in the treatment of nasal and ocular symptoms of seasonal allergic rhinitis in adults and adolescents sensitized to mountain cedar pollen.
Ellsworth, A; Hampel, F; Jacobs, R; Martin, B; Philpot, E; Toler, W, 2009
)
2.14
"Fluticasone furoate is a novel glucocorticoid receptor agonist marketed as a treatment for seasonal and perennial allergic rhinitis. "( Structure elucidation and spectroscopic analysis of photodegradants of the anti-rhinitis drug fluticasone furoate.
Bardsley, B; Gibbon, BH; Smith, MS, 2010
)
2.02
"Fluticasone furoate is a promising molecule in the treatment of allergic rhinitis as it fits fully all the official guidelines' criteria. "( A review of the use of fluticasone furoate since its launch.
Canonica, GW; Magnoni, MS; Micheli, D; Villa, E, 2011
)
2.12
"Fluticasone furoate (FF) is a novel inhaled corticosteroid with 24 h activity. "( Fluticasone furoate demonstrates efficacy in patients with asthma symptomatic on medium doses of inhaled corticosteroid therapy: an 8-week, randomised, placebo-controlled trial.
Bateman, ED; Bleecker, ER; Busse, WW; Davis, AM; Forth, R; Haumann, B; Jacques, L; Lötvall, J; Woodcock, A, 2012
)
3.26
"Fluticasone furoate (FF) is a novel long-acting inhaled corticosteroid (ICS). "( Efficacy in asthma of once-daily treatment with fluticasone furoate: a randomized, placebo-controlled trial.
Bateman, ED; Bleecker, ER; Busse, WW; Forth, R; Haumann, B; Jacques, L; Lötvall, J; Snowise, NG; Woodcock, A, 2011
)
2.07
"Fluticasone furoate is a new potent topical glucocorticoid for the treatment of allergic rhinitis."( An open label, active controlled, multicentric clinical trial to assess the efficacy and safety of fluticasone furoate nasal spray in adult Indian patients suffering from allergic rhinitis.
Khippal, N; Kubavat, AH; Mittal, R; Ojha, T; Patel, T; Pawar, P; Shah, UB; Sinha, V, 2011
)
1.31
"Fluticasone furoate is a novel enhanced-affinity glucocorticoid for the treatment of AR approved by the Food and Drug Administration in 2007 and recently introduced in India."( Fluticasone furoate: a new intranasal corticosteroid.
Kumar, D; Kumar, R; Parakh, A,
)
2.3
"Fluticasone furoate (FF) is an inhaled corticosteroid that is structurally and functionally distinct from fluticasone propionate and is under development as a once-daily therapy for asthma."( Efficacy and safety profile of fluticasone furoate administered once daily in the morning or evening: a randomized, double-blind, double-dummy, placebo-controlled trial in adult and adolescent patients with persistent bronchial asthma.
Allen, A; Medley, H; Orozco, S, 2012
)
2.11
"Fluticasone furoate (FF) is an inhaled corticosteroid (ICS) with 24-hour activity in development as a once-daily treatment for the long-term management of asthma."( Once-daily fluticasone furoate is efficacious in patients with symptomatic asthma on low-dose inhaled corticosteroids.
Bateman, ED; Bleecker, ER; Busse, WW; Davis, AM; Frith, L; Haumann, B; House, KW; Jacques, L; Lötvall, J; Woodcock, A, 2012
)
2.21
"Fluticasone furoate (FF) is a novel enhanced-affinity glucocorticoid that has been developed as topical therapy for allergic rhinitis. "( Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease.
Biggadike, K; Farrow, SN; Gray, DW; Haase, MV; Matthews, JL; Salter, M; Uings, IJ; West, MR, 2007
)
2.02
"Fluticasone furoate nasal spray is a new topical intranasal corticosteroid with enhanced affinity for the glucocorticoid receptor and low systemic exposure, which was recently approved in the US for the treatment of seasonal or perennial allergic rhinitis in adults and in children aged >or=2 years. "( Fluticasone furoate: intranasal use in allergic rhinitis.
McCormack, PL; Scott, LJ, 2007
)
3.23
"Fluticasone furoate is a recently approved, enhanced- affinity intranasal corticosteroid with low systemic bioavailability and proven efficacy in treating allergic rhinitis."( A 2-week, crossover study to investigate the effect of fluticasone furoate nasal spray on short-term growth in children with allergic rhinitis.
Caldwell, MF; Gradman, J; Wolthers, OD, 2007
)
1.31

Toxicity

Safety data from 10 parallel-group, randomised, double-blind Phase II and III studies. No dose-response relationship was observed for the overall incidence of adverse events. There were no significant effects of fluticasone furoate on hypothalamic-pituitary-adrenal axis function.

ExcerptReferenceRelevance
" Safety assessments included clinical adverse event (AE) monitoring, clinical laboratory tests, detailed nasal examinations, monitoring of vital signs, and 12-lead ECGs."( Safety and tolerability of fluticasone furoate nasal spray once daily in paediatric patients aged 6-11 years with allergic rhinitis: subanalysis of three randomized, double-blind, placebo-controlled, multicentre studies.
Máspero, JF; Meltzer, EO; Philpot, E; Tripathy, I; Wu, W, 2009
)
0.65
" Recent studies, which evaluated topical and systemic adverse events associated with ciclesonide (CIC), fluticasone furoate (FF), mometasone furoate (MF), triamcinolone acetonide, fluticasone propionate, budesonide, and beclomethasone dipropionate were summarized."( Safety update regarding intranasal corticosteroids for the treatment of allergic rhinitis.
Blaiss, MS,
)
0.35
" Other end points included change from baseline in forced expiratory volume in 1 second, asthma symptom score, adverse events (AEs), 24-hour urinary cortisol excretion, and FF pharmacokinetics."( Efficacy and safety profile of fluticasone furoate administered once daily in the morning or evening: a randomized, double-blind, double-dummy, placebo-controlled trial in adult and adolescent patients with persistent bronchial asthma.
Allen, A; Medley, H; Orozco, S, 2012
)
0.66
" 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
)
0.63
"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
)
0.62
" There were no ophthalmic-related adverse events of LOCS III PSO or IOP that led to early withdrawal."( Ocular safety of fluticasone furoate nasal spray in patients with perennial allergic rhinitis: a 2-year study.
Chylack, LT; Journeay, GE; LaForce, C; Lee, LA; Miller, SD; Silvey, MJ; Wu, W, 2013
)
0.73
" 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
)
0.7
" 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
)
0.65
" Adverse events (AEs) were assessed."( Efficacy and safety of fluticasone furoate 100 μg once-daily in patients with persistent asthma: a 24-week placebo and active-controlled randomised trial.
Bateman, ED; Bleecker, ER; Busse, WW; Forth, R; Jacques, L; Kerwin, EM; Lötvall, J; O'Byrne, PM; Stone, S; Woodcock, A, 2014
)
0.71
" 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
)
0.68
" Safety assessments included adverse events, laboratory and vital sign measurements, and change from baseline in 24-hour urinary cortisol at Week 24."( Efficacy and safety of fluticasone furoate 100 μg and 200 μg once daily in the treatment of moderate-severe asthma in adults and adolescents: a 24-week randomised study.
Bateman, ED; Busse, WW; Ellsworth, A; Jacques, L; Lötvall, J; Stone, S; Woodcock, A, 2014
)
0.71
" FF 100 μg reported adverse events (63% vs."( Efficacy and safety of fluticasone furoate 100 μg and 200 μg once daily in the treatment of moderate-severe asthma in adults and adolescents: a 24-week randomised study.
Bateman, ED; Busse, WW; Ellsworth, A; Jacques, L; Lötvall, J; Stone, S; Woodcock, A, 2014
)
0.71
" As a safety measure, adverse events and clinical chemistry and hematology were evaluated."( Efficacy and safety of fluticasone furoate nasal spray in Japanese children with perennial allergic rhinitis: a multicentre, randomized, double-blind, placebo-controlled trial.
Honma, G; Komatsubara, M; Okamasa, A; Okubo, K, 2014
)
0.71
" The incidence of adverse events was similar between FFNS 55μg(18%) and placebo (19%)."( Efficacy and safety of fluticasone furoate nasal spray in Japanese children with perennial allergic rhinitis: a multicentre, randomized, double-blind, placebo-controlled trial.
Honma, G; Komatsubara, M; Okamasa, A; Okubo, K, 2014
)
0.71
" The incidence of adverse events was lower with FF (31%) than with placebo (38%); few were treatment-related (FF 50 mcg: n = 1, <1%; placebo: n = 4, 3%)."( Efficacy and safety of once-daily fluticasone furoate 50 mcg in adults with persistent asthma: a 12-week randomized trial.
Bateman, ED; Bleecker, ER; Busse, WW; Forth, R; Jacques, L; Lötvall, J; Medley, H; O'Byrne, PM; Woodcock, A, 2014
)
0.68
" As a safety measure, adverse events and clinical laboratory data were evaluated."( Safety and efficacy of fluticasone furoate nasal spray in Japanese children 2 to <15 years of age with perennial allergic rhinitis: a multicentre, open-label trial.
Honma, G; Komatsubara, M; Okamasa, A; Okubo, K, 2015
)
0.73
"An adverse event was reported by 67% of patients during the treatment and follow-up period, all of which were mild in intensity."( Safety and efficacy of fluticasone furoate nasal spray in Japanese children 2 to <15 years of age with perennial allergic rhinitis: a multicentre, open-label trial.
Honma, G; Komatsubara, M; Okamasa, A; Okubo, K, 2015
)
0.73
" Three adverse events were reported; none were severe or led to withdrawal."( A randomized, crossover study to investigate the pharmacokinetics and safety of inhaled fluticasone furoate and umeclidinium, administered separately and in combination via dry powder inhaler in healthy adult volunteers.
Ayer, J; Lee, L; Mallett, S; Pascoe, S; Wolstenholme, A; Yang, S, 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
)
0.73
" 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
)
0.68
" 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
)
0.74
" All treatments were well tolerated, and adverse event incidence was similar across the treatment groups."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.67
" 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
)
0.69
" 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
)
0.69
" Adverse events (AEs) were monitored."( Efficacy and safety comparison: Fluticasone furoate and fluticasone propionate, after step down from fluticasone furoate/vilanterol in Japanese patients with well-controlled asthma, a randomized trial.
Adachi, M; Goldfrad, C; Jacques, L; Nishimura, Y, 2016
)
0.72
" Safety data from 10 parallel-group, randomised, double-blind Phase II and III studies (including 3345 patients who received at least one dose of fluticasone furoate) were integrated to provide information on adverse events, withdrawals, laboratory assessments, vital signs and hypothalamic-pituitary-adrenal axis function."( Integrated safety and efficacy analysis of once-daily fluticasone furoate for the treatment of asthma.
Busse, WW; Goldfrad, C; Jacques, L; Kwon, N; O'Byrne, PM; Perrio, M; Yates, LJ, 2016
)
0.88
" In the integrated analysis, no dose-response relationship was observed for the overall incidence of adverse events and there were no significant effects of fluticasone furoate on hypothalamic-pituitary-adrenal axis function."( Integrated safety and efficacy analysis of once-daily fluticasone furoate for the treatment of asthma.
Busse, WW; Goldfrad, C; Jacques, L; Kwon, N; O'Byrne, PM; Perrio, M; Yates, LJ, 2016
)
0.88
" 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
)
0.83
" 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
)
0.85
" 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
)
1.18

Pharmacokinetics

Population pharmacokinetic (PK) methods were used to characterize the PK of fluticasone furoate (FF) and vilanterol (VI) in patients with asthma following onc.

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
)
0.61
"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
)
0.61
" 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
)
0.61
"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
)
0.79
"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
)
0.59
" 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
)
0.62
"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
)
0.92
"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
)
0.68
"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
)
0.68
" 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
)
0.74
"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
)
0.93
"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
)
0.86
"The purpose of this study was to investigate potential systemic pharmacokinetic interactions between intranasal fluticasone furoate (FF) and levocabastine (LEVO) when delivered simultaneously via a metered atomizing spray pump."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.88
"These results suggest that in healthy subjects, for LEVO, there is no pharmacokinetic interaction with FF when delivered as FF/LEVO FDC."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.67
" Pharmacokinetic data were analyzed using noncompartmental methods."( Open-Label, Randomized, 6-Way Crossover, Single-Dose Study to Determine the Pharmacokinetics of Batefenterol (GSK961081) and Fluticasone Furoate When Administered Alone or in Combination.
Ambery, C; Daley-Yates, P; Riddell, K, 2016
)
0.64
"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
)
0.93
"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
)
1.05

Compound-Compound Interactions

ExcerptReferenceRelevance
"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
)
0.93

Bioavailability

Fluticasone furoate is a recently approved, enhanced- affinity intranasal corticosteroid with low systemic bioavailability. It has proven efficacy in treating allergic rhinitis.

ExcerptReferenceRelevance
" Fluticasone furoate is a recently approved, enhanced- affinity intranasal corticosteroid with low systemic bioavailability and proven efficacy in treating allergic rhinitis."( A 2-week, crossover study to investigate the effect of fluticasone furoate nasal spray on short-term growth in children with allergic rhinitis.
Caldwell, MF; Gradman, J; Wolthers, OD, 2007
)
1.5
" Fluticasone furoate demonstrates high systemic clearance, low oral bioavailability and low absolute bioavailability after intranasal administration (<0."( Fluticasone furoate nasal spray in allergic rhinitis.
Goyal, N; Hochhaus, G, 2008
)
2.7
" Pharmacokinetic properties were tuned with high intrinsic clearance and low oral bioavailability in mind, to minimise systemic exposure and reduce systemically driven adverse events."( Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.
Ballard, SA; Chunn, S; Dybowski, JA; Fulton, CK; Glossop, PA; Guillabert, E; Hewson, CA; Jones, RM; Lamb, DJ; Millan, DS; Napier, CM; Payne-Cook, TA; Renery, ER; Selby, MD; Tutt, MF; Yeadon, M, 2011
)
0.37
" Important attributes of fluticasone furoate include low systemic bioavailability (<0."( Fluticasone furoate: a new intranasal corticosteroid.
Kumar, D; Kumar, R; Parakh, A,
)
1.88
" The bioavailability of both inhaled FF and FP represents absorption from the lung as the oral bioavailability from the swallowed portion of the inhaled dose is negligible (<1."( Fluticasone furoate, a novel inhaled corticosteroid, demonstrates prolonged lung absorption kinetics in man compared with inhaled fluticasone propionate.
Allen, A; Bareille, PJ; Rousell, VM, 2013
)
1.83
" Absolute bioavailability was greater (36%-55%) in all East Asian groups than for Caucasian subjects following inhaled FF 800 μg."( Pharmacokinetics and pharmacodynamics of intravenous and inhaled fluticasone furoate in healthy Caucasian and East Asian subjects.
Allen, A; Bal, J; Cheesbrough, A; Hamilton, M; Kempsford, R, 2014
)
0.64
" As the majority of data were below the assay sensitivity for FF, any potential differences in the bioavailability of FF when delivered alone or as FF/LEVO FDC could not be established."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.67
"Study 1: For intravenous MF and FP, respectively: absolute bioavailability was 11."( Comparative clinical pharmacology of mometasone furoate, fluticasone propionate and fluticasone furoate.
Daley-Yates, PT; Deans, A; Mehta, R; Sousa, AR, 2022
)
0.95
"Single inhaled and intravenous doses of MF and FP (400 μg) resulted in similar bioavailability and reductions in serum cortisol."( Comparative clinical pharmacology of mometasone furoate, fluticasone propionate and fluticasone furoate.
Daley-Yates, PT; Deans, A; Mehta, R; Sousa, AR, 2022
)
0.95

Dosage Studied

Fluticasone furoate (FF) is a new inhaled corticosteroid (ICS) suitable for once-daily dosing in asthma. This article reviews efficacy versus systemic activity profiles for various adherence patterns and dosing regimens.

ExcerptRelevanceReference
" At the end of the crossover dosing and after completion of the attributes questionnaires, preference for individual attributes of FF or FP nasal spray and overall patient preference were evaluated in a third questionnaire that asked "Based on these attributes, which product did you prefer overall?" Additionally, a follow-up phone call was conducted 24 hours after the study to assess any adverse events following study treatment."( Preferences of adult patients with allergic rhinitis for the sensory attributes of fluticasone furoate versus fluticasone propionate nasal sprays: a randomized, multicenter, double-blind, single-dose, crossover study.
Dalal, AA; Leflein, J; Lim, J; Meltzer, EO; Meltzer, S; Philpot, EE; Prillaman, BA; Stahlman, JE, 2008
)
0.57
"2% ophthalmic solution, fluticasone furoate nasal spray, a tear substitute, or saline nasal spray), dosed with study medication, and challenged 15 minutes later, after which ocular allergic signs and symptoms were assessed."( A comparison of olopatadine 0.2% ophthalmic solution versus fluticasone furoate nasal spray for the treatment of allergic conjunctivitis.
Abelson, MB; Gomes, PJ; Kennedy, K; Mahr, T; Rosenwasser, LJ,
)
0.68
" There was no dose-response relationship across the FF doses studied."( Fluticasone furoate demonstrates efficacy in patients with asthma symptomatic on medium doses of inhaled corticosteroid therapy: an 8-week, randomised, placebo-controlled trial.
Bateman, ED; Bleecker, ER; Busse, WW; Davis, AM; Forth, R; Haumann, B; Jacques, L; Lötvall, J; Woodcock, A, 2012
)
1.82
"A dose-response effect was observed for once-daily FF 25-200 μg including (p < 0."( Dose effect of once-daily fluticasone furoate in persistent asthma: a randomized trial.
Bateman, ED; Bleecker, ER; Busse, WW; Davis, AM; Forth, R; Haumann, B; Jacques, L; Lötvall, J; Medley, H; Woodcock, A, 2012
)
0.68
" 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
)
0.7
"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
)
0.7
" However, morning trough values might have been affected by higher placebo response after morning dosing (18."( Efficacy and safety profile of fluticasone furoate administered once daily in the morning or evening: a randomized, double-blind, double-dummy, placebo-controlled trial in adult and adolescent patients with persistent bronchial asthma.
Allen, A; Medley, H; Orozco, S, 2012
)
0.66
" There was no evidence of a dose-response relationship between FF doses."( Once-daily fluticasone furoate is efficacious in patients with symptomatic asthma on low-dose inhaled corticosteroids.
Bateman, ED; Bleecker, ER; Busse, WW; Davis, AM; Frith, L; Haumann, B; House, KW; Jacques, L; Lötvall, J; Woodcock, A, 2012
)
0.77
" This would suggest that FF is exhibiting absorption rate-limited pharmacokinetics following inhaled FF dosing and that the apparent t(½β) is an estimate of absorption rate."( Fluticasone furoate, a novel inhaled corticosteroid, demonstrates prolonged lung absorption kinetics in man compared with inhaled fluticasone propionate.
Allen, A; Bareille, PJ; Rousell, VM, 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
)
0.62
"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
)
0.62
"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
)
0.67
" Higher FF systemic exposure was seen following inhaled dosing in Chinese, Japanese and Korean subjects compared with Caucasian subjects."( Pharmacokinetics and pharmacodynamics of intravenous and inhaled fluticasone furoate in healthy Caucasian and East Asian subjects.
Allen, A; Bal, J; Cheesbrough, A; Hamilton, M; Kempsford, R, 2014
)
0.64
"Modestly higher (<50%) FF systemic exposure seen in East Asian subjects following inhaled dosing was not associated with a clinically significant effect on serum cortisol, suggesting that a clinical dose adjustment in East Asian subjects is not required."( Pharmacokinetics and pharmacodynamics of intravenous and inhaled fluticasone furoate in healthy Caucasian and East Asian subjects.
Allen, A; Bal, J; Cheesbrough, A; Hamilton, M; Kempsford, R, 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
)
0.9
"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
)
0.69
"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
)
0.69
" 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
)
0.76
"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
)
0.75
" Fluticasone furoate (FF) is a new inhaled corticosteroid (ICS) suitable for once-daily dosing in asthma."( Efficacy and safety of fluticasone furoate 100 μg and 200 μg once daily in the treatment of moderate-severe asthma in adults and adolescents: a 24-week randomised study.
Bateman, ED; Busse, WW; Ellsworth, A; Jacques, L; Lötvall, J; Stone, S; Woodcock, A, 2014
)
1.62
" Three hundred and fifty-one patients (aged ≥12 years; uncontrolled by non-ICS therapy) were randomized to treatment (1 : 1 : 1) with once-daily FF 50 mcg dosed in the evening, twice-daily fluticasone propionate (FP) 100 mcg or placebo."( Once-daily fluticasone furoate 50 mcg in mild-to-moderate asthma: a 24-week placebo-controlled randomized trial.
Bateman, ED; Busse, WW; Forth, R; Jacques, L; Lötvall, J; Medley, H; O'Byrne, PM; Woodcock, A, 2014
)
0.79
"We evaluated the dose-response of umeclidinium (UMEC; a long-acting muscarinic antagonist) combined with fluticasone furoate (FF; an inhaled corticosteroid [ICS]) in patients with asthma."( The effect of fluticasone furoate/umeclidinium in adult patients with asthma: a randomized, dose-ranging study.
Edwards, LD; Kerwin, E; Lee, LA; Pascoe, S; Trivedi, R; Yang, S, 2015
)
0.99
"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
)
3.3
" The present study aimed to further characterise the UMEC dose-response relationship with change from baseline trough forced expiratory volume in one second (FEV1) (day 15)."( Dose-response modelling of umeclidinium and fluticasone furoate/umeclidinium in asthma.
Beerahee, M; Goyal, N; Lee, L; Pascoe, S; Trivedi, R; Yang, S, 2015
)
0.68
"Within the Study 1 dose range, no significant dose-response was demonstrated."( Dose-response modelling of umeclidinium and fluticasone furoate/umeclidinium in asthma.
Beerahee, M; Goyal, N; Lee, L; Pascoe, S; Trivedi, R; Yang, S, 2015
)
0.68
" 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
)
1.86
" 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
)
0.76
" One of the newer fluticasone furoate studies overcomes these limitations and also provides an assessment of a range of doses, suggesting that the therapeutic window is quite narrow and that conventional dosing has probably been too high, although the absolute risk may be different compared to other drugs."( Inhaled corticosteroids and the increased risk of pneumonia: what's new? A 2015 updated review.
Iannella, H; Luna, C; Waterer, G, 2016
)
0.77
" 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
)
0.7
" 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
)
1.88
" In the integrated analysis, no dose-response relationship was observed for the overall incidence of adverse events and there were no significant effects of fluticasone furoate on hypothalamic-pituitary-adrenal axis function."( Integrated safety and efficacy analysis of once-daily fluticasone furoate for the treatment of asthma.
Busse, WW; Goldfrad, C; Jacques, L; Kwon, N; O'Byrne, PM; Perrio, M; Yates, LJ, 2016
)
0.88
" 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
" The inhibition in AHR after one week of daily dosing coincided with a significant decrease in FeNO at 7 days."( Short-term effect of once-daily fluticasone furoate on methacholine-induced bronchoconstriction in mild asthmatics.
Blais, CM; Cockcroft, DW; Davis, BE; Okonkwo, CS, 2019
)
0.8
" Low plasma concentrations of 6β-hydroxy mometasone were detected after intravenous dosing (Study 1) and after multiple inhaled dosing (Study 2); mometasone was not detected in any samples."( Comparative clinical pharmacology of mometasone furoate, fluticasone propionate and fluticasone furoate.
Daley-Yates, PT; Deans, A; Mehta, R; Sousa, AR, 2022
)
0.95
" Repeat dosing of inhaled MF and FP in the therapeutic range (800 μg/day) resulted in greater systemic exposure for MF, and a 35% reduction in serum cortisol that was 2-fold greater than for FP."( Comparative clinical pharmacology of mometasone furoate, fluticasone propionate and fluticasone furoate.
Daley-Yates, PT; Deans, A; Mehta, R; Sousa, AR, 2022
)
0.95
" This article reviews efficacy versus systemic activity profiles for various adherence patterns and dosing regimens of fluticasone furoate (FF)-containing and budesonide (BUD)-containing asthma therapies in clinical trials and real-world studies."( Assessing the Effects of Changing Patterns of Inhaled Corticosteroid Dosing and Adherence with Fluticasone Furoate and Budesonide on Asthma Management.
Berend, N; Daley-Yates, P; Igea, JM; Macchia, L; Plank, M; Singh, D; Verma, M, 2023
)
1.34
"We performed a structured literature review (1 January 2000-3 March 2022) and mathematical modelling analysis of FF-containing and BUD-containing regular daily dosing in patients with mild-to-severe asthma, as-needed BUD/formoterol (FOR) in mild asthma, and BUD/FOR maintenance and reliever therapy (MART) dosing in moderate-to-severe asthma, to assess efficacy (bronchoprotection) and systemic activity (cortisol suppression) profiles of dosing patterns of ICS use in multiple adherence scenarios."( Assessing the Effects of Changing Patterns of Inhaled Corticosteroid Dosing and Adherence with Fluticasone Furoate and Budesonide on Asthma Management.
Berend, N; Daley-Yates, P; Igea, JM; Macchia, L; Plank, M; Singh, D; Verma, M, 2023
)
1.13
" Focusing on FF-containing or BUD-containing treatments at comparable adherence rates, regular daily FF or FF/vilanterol (VI) dosing provided more prolonged bronchoprotection and fewer systemic effects than daily BUD, daily BUD/FOR, or BUD/FOR MART dosing, especially in low adherence scenarios."( Assessing the Effects of Changing Patterns of Inhaled Corticosteroid Dosing and Adherence with Fluticasone Furoate and Budesonide on Asthma Management.
Berend, N; Daley-Yates, P; Igea, JM; Macchia, L; Plank, M; Singh, D; Verma, M, 2023
)
1.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
anti-allergic agentA drug used to treat allergic reactions.
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
anti-asthmatic drugA drug used to treat asthma.
[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 (7)

ClassDescription
11beta-hydroxy steroidAny 11-hydroxy steroid in which the hydroxy group at position 11 has beta- configuration.
corticosteroidA natural or synthetic analogue of the hormones secreted by the adrenal gland.
fluorinated steroidA steroid which is substituted with one or more fluorine atoms in any position.
steroid ester
2-furoate esterAny carboxylic ester where the carboxylic acid component is 2-furoic acid.
thioesterA compound of general formula RC(=O)SR'. Compare with thionoester, RC(=S)OR'.
3-oxo-Delta(1),Delta(4)-steroidA 3-oxo-Delta(1) steroid containing an additional double bond between positions 4 and 5.
[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]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)IC50 (µMol)5.00000.00000.723732.7000AID1476014
Glucocorticoid receptorHomo sapiens (human)IC50 (µMol)0.00040.00000.495310.0000AID1476013; AID429130
Glucocorticoid receptorHomo sapiens (human)Ki0.00050.00010.38637.0010AID1375646
Progesterone receptorHomo sapiens (human)IC50 (µMol)0.02100.00000.580710.0000AID1476016
Mineralocorticoid receptor Homo sapiens (human)IC50 (µMol)0.16600.00030.748410.0000AID1476011
Androgen receptorRattus norvegicus (Norway rat)IC50 (µMol)1.88000.00101.979414.1600AID1476012
Estrogen receptor betaHomo sapiens (human)IC50 (µMol)5.00000.00010.529432.7000AID1476015
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glucocorticoid receptorHomo sapiens (human)EC50 (µMol)0.00040.00040.05401.0000AID1375648; AID622345
Mineralocorticoid receptor Homo sapiens (human)EC50 (µMol)3.00000.00000.01260.1000AID1375650
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (81)

Processvia Protein(s)Taxonomy
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
antral ovarian follicle growthEstrogen receptorHomo sapiens (human)
epithelial cell developmentEstrogen receptorHomo sapiens (human)
chromatin remodelingEstrogen receptorHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
signal transductionEstrogen receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEstrogen receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEstrogen receptorHomo sapiens (human)
androgen metabolic processEstrogen receptorHomo sapiens (human)
male gonad developmentEstrogen receptorHomo sapiens (human)
negative regulation of gene expressionEstrogen receptorHomo sapiens (human)
positive regulation of phospholipase C activityEstrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayEstrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptorHomo sapiens (human)
response to estradiolEstrogen receptorHomo sapiens (human)
regulation of toll-like receptor signaling pathwayEstrogen receptorHomo sapiens (human)
negative regulation of smooth muscle cell apoptotic processEstrogen receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionEstrogen receptorHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
response to estrogenEstrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
fibroblast proliferationEstrogen receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEstrogen receptorHomo sapiens (human)
stem cell differentiationEstrogen receptorHomo sapiens (human)
regulation of inflammatory responseEstrogen receptorHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
RNA polymerase II preinitiation complex assemblyEstrogen receptorHomo sapiens (human)
uterus developmentEstrogen receptorHomo sapiens (human)
vagina developmentEstrogen receptorHomo sapiens (human)
prostate epithelial cord elongationEstrogen receptorHomo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesisEstrogen receptorHomo sapiens (human)
regulation of branching involved in prostate gland morphogenesisEstrogen receptorHomo sapiens (human)
mammary gland branching involved in pregnancyEstrogen receptorHomo sapiens (human)
mammary gland alveolus developmentEstrogen receptorHomo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongationEstrogen receptorHomo sapiens (human)
protein localization to chromatinEstrogen receptorHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptorHomo sapiens (human)
negative regulation of miRNA transcriptionEstrogen receptorHomo sapiens (human)
regulation of epithelial cell apoptotic processEstrogen receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
regulation of gluconeogenesisGlucocorticoid receptorHomo sapiens (human)
chromatin organizationGlucocorticoid receptorHomo sapiens (human)
regulation of DNA-templated transcriptionGlucocorticoid receptorHomo sapiens (human)
apoptotic processGlucocorticoid receptorHomo sapiens (human)
chromosome segregationGlucocorticoid receptorHomo sapiens (human)
signal transductionGlucocorticoid receptorHomo sapiens (human)
glucocorticoid metabolic processGlucocorticoid receptorHomo sapiens (human)
gene expressionGlucocorticoid receptorHomo sapiens (human)
microglia differentiationGlucocorticoid receptorHomo sapiens (human)
adrenal gland developmentGlucocorticoid receptorHomo sapiens (human)
regulation of glucocorticoid biosynthetic processGlucocorticoid receptorHomo sapiens (human)
synaptic transmission, glutamatergicGlucocorticoid receptorHomo sapiens (human)
maternal behaviorGlucocorticoid receptorHomo sapiens (human)
intracellular glucocorticoid receptor signaling pathwayGlucocorticoid receptorHomo sapiens (human)
glucocorticoid mediated signaling pathwayGlucocorticoid receptorHomo sapiens (human)
positive regulation of neuron apoptotic processGlucocorticoid receptorHomo sapiens (human)
negative regulation of DNA-templated transcriptionGlucocorticoid receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
astrocyte differentiationGlucocorticoid receptorHomo sapiens (human)
cell divisionGlucocorticoid receptorHomo sapiens (human)
mammary gland duct morphogenesisGlucocorticoid receptorHomo sapiens (human)
motor behaviorGlucocorticoid receptorHomo sapiens (human)
cellular response to steroid hormone stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to glucocorticoid stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to dexamethasone stimulusGlucocorticoid receptorHomo sapiens (human)
cellular response to transforming growth factor beta stimulusGlucocorticoid receptorHomo sapiens (human)
neuroinflammatory responseGlucocorticoid receptorHomo sapiens (human)
positive regulation of miRNA transcriptionGlucocorticoid receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayGlucocorticoid receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIGlucocorticoid receptorHomo sapiens (human)
ovulation from ovarian follicleProgesterone receptorHomo sapiens (human)
glandular epithelial cell maturationProgesterone receptorHomo sapiens (human)
regulation of DNA-templated transcriptionProgesterone receptorHomo sapiens (human)
signal transductionProgesterone receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProgesterone receptorHomo sapiens (human)
cell-cell signalingProgesterone receptorHomo sapiens (human)
positive regulation of gene expressionProgesterone receptorHomo sapiens (human)
negative regulation of gene expressionProgesterone receptorHomo sapiens (human)
paracrine signalingProgesterone receptorHomo sapiens (human)
negative regulation of phosphorylationProgesterone receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIProgesterone receptorHomo sapiens (human)
lung alveolus developmentProgesterone receptorHomo sapiens (human)
regulation of epithelial cell proliferationProgesterone receptorHomo sapiens (human)
progesterone receptor signaling pathwayProgesterone receptorHomo sapiens (human)
maintenance of protein location in nucleusProgesterone receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisProgesterone receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIProgesterone receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayProgesterone receptorHomo sapiens (human)
signal transductionMineralocorticoid receptor Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionMineralocorticoid receptor Homo sapiens (human)
regulation of transcription by RNA polymerase IIMineralocorticoid receptor Homo sapiens (human)
intracellular steroid hormone receptor signaling pathwayMineralocorticoid receptor Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
signal transductionEstrogen receptor betaHomo sapiens (human)
cell-cell signalingEstrogen receptor betaHomo sapiens (human)
negative regulation of cell growthEstrogen receptor betaHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptor betaHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptor betaHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (37)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
TFIIB-class transcription factor bindingEstrogen receptorHomo sapiens (human)
transcription coregulator bindingEstrogen receptorHomo sapiens (human)
transcription corepressor bindingEstrogen receptorHomo sapiens (human)
transcription coactivator bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
chromatin bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
nuclear receptor activityEstrogen receptorHomo sapiens (human)
steroid bindingEstrogen receptorHomo sapiens (human)
protein bindingEstrogen receptorHomo sapiens (human)
calmodulin bindingEstrogen receptorHomo sapiens (human)
beta-catenin bindingEstrogen receptorHomo sapiens (human)
zinc ion bindingEstrogen receptorHomo sapiens (human)
TBP-class protein bindingEstrogen receptorHomo sapiens (human)
enzyme bindingEstrogen receptorHomo sapiens (human)
protein kinase bindingEstrogen receptorHomo sapiens (human)
nitric-oxide synthase regulator activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor bindingEstrogen receptorHomo sapiens (human)
estrogen response element bindingEstrogen receptorHomo sapiens (human)
identical protein bindingEstrogen receptorHomo sapiens (human)
ATPase bindingEstrogen receptorHomo sapiens (human)
14-3-3 protein bindingEstrogen receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingEstrogen receptorHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
core promoter sequence-specific DNA bindingGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificGlucocorticoid receptorHomo sapiens (human)
DNA-binding transcription factor activityGlucocorticoid receptorHomo sapiens (human)
RNA bindingGlucocorticoid receptorHomo sapiens (human)
nuclear receptor activityGlucocorticoid receptorHomo sapiens (human)
nuclear glucocorticoid receptor activityGlucocorticoid receptorHomo sapiens (human)
steroid bindingGlucocorticoid receptorHomo sapiens (human)
protein bindingGlucocorticoid receptorHomo sapiens (human)
zinc ion bindingGlucocorticoid receptorHomo sapiens (human)
TBP-class protein bindingGlucocorticoid receptorHomo sapiens (human)
protein kinase bindingGlucocorticoid receptorHomo sapiens (human)
identical protein bindingGlucocorticoid receptorHomo sapiens (human)
Hsp90 protein bindingGlucocorticoid receptorHomo sapiens (human)
steroid hormone bindingGlucocorticoid receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingGlucocorticoid receptorHomo sapiens (human)
estrogen response element bindingGlucocorticoid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingProgesterone receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificProgesterone receptorHomo sapiens (human)
transcription coactivator bindingProgesterone receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificProgesterone receptorHomo sapiens (human)
DNA bindingProgesterone receptorHomo sapiens (human)
nuclear steroid receptor activityProgesterone receptorHomo sapiens (human)
G protein-coupled receptor activityProgesterone receptorHomo sapiens (human)
steroid bindingProgesterone receptorHomo sapiens (human)
protein bindingProgesterone receptorHomo sapiens (human)
zinc ion bindingProgesterone receptorHomo sapiens (human)
enzyme bindingProgesterone receptorHomo sapiens (human)
identical protein bindingProgesterone receptorHomo sapiens (human)
ATPase bindingProgesterone receptorHomo sapiens (human)
estrogen response element bindingProgesterone receptorHomo sapiens (human)
nuclear receptor activityProgesterone receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificMineralocorticoid receptor Homo sapiens (human)
DNA-binding transcription factor activityMineralocorticoid receptor Homo sapiens (human)
nuclear steroid receptor activityMineralocorticoid receptor Homo sapiens (human)
steroid bindingMineralocorticoid receptor Homo sapiens (human)
protein bindingMineralocorticoid receptor Homo sapiens (human)
zinc ion bindingMineralocorticoid receptor Homo sapiens (human)
TBP-class protein bindingMineralocorticoid receptor Homo sapiens (human)
sequence-specific double-stranded DNA bindingMineralocorticoid receptor Homo sapiens (human)
nuclear receptor activityMineralocorticoid receptor Homo sapiens (human)
estrogen response element bindingMineralocorticoid receptor Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptor betaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptor betaHomo sapiens (human)
DNA bindingEstrogen receptor betaHomo sapiens (human)
nuclear steroid receptor activityEstrogen receptor betaHomo sapiens (human)
nuclear receptor activityEstrogen receptor betaHomo sapiens (human)
steroid bindingEstrogen receptor betaHomo sapiens (human)
protein bindingEstrogen receptor betaHomo sapiens (human)
zinc ion bindingEstrogen receptor betaHomo sapiens (human)
enzyme bindingEstrogen receptor betaHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptor betaHomo sapiens (human)
estrogen response element bindingEstrogen receptor betaHomo sapiens (human)
receptor antagonist activityEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
nucleusEstrogen receptorHomo sapiens (human)
nucleoplasmEstrogen receptorHomo sapiens (human)
transcription regulator complexEstrogen receptorHomo sapiens (human)
cytoplasmEstrogen receptorHomo sapiens (human)
Golgi apparatusEstrogen receptorHomo sapiens (human)
cytosolEstrogen receptorHomo sapiens (human)
plasma membraneEstrogen receptorHomo sapiens (human)
membraneEstrogen receptorHomo sapiens (human)
chromatinEstrogen receptorHomo sapiens (human)
euchromatinEstrogen receptorHomo sapiens (human)
protein-containing complexEstrogen receptorHomo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
nucleusGlucocorticoid receptorHomo sapiens (human)
nucleusGlucocorticoid receptorHomo sapiens (human)
nucleoplasmGlucocorticoid receptorHomo sapiens (human)
cytoplasmGlucocorticoid receptorHomo sapiens (human)
mitochondrial matrixGlucocorticoid receptorHomo sapiens (human)
centrosomeGlucocorticoid receptorHomo sapiens (human)
spindleGlucocorticoid receptorHomo sapiens (human)
cytosolGlucocorticoid receptorHomo sapiens (human)
membraneGlucocorticoid receptorHomo sapiens (human)
nuclear speckGlucocorticoid receptorHomo sapiens (human)
synapseGlucocorticoid receptorHomo sapiens (human)
chromatinGlucocorticoid receptorHomo sapiens (human)
protein-containing complexGlucocorticoid receptorHomo sapiens (human)
plasma membraneProgesterone receptorHomo sapiens (human)
nucleoplasmProgesterone receptorHomo sapiens (human)
mitochondrial outer membraneProgesterone receptorHomo sapiens (human)
cytosolProgesterone receptorHomo sapiens (human)
chromatinProgesterone receptorHomo sapiens (human)
nucleusProgesterone receptorHomo sapiens (human)
nucleoplasmMineralocorticoid receptor Homo sapiens (human)
endoplasmic reticulum membraneMineralocorticoid receptor Homo sapiens (human)
cytosolMineralocorticoid receptor Homo sapiens (human)
chromatinMineralocorticoid receptor Homo sapiens (human)
receptor complexMineralocorticoid receptor Homo sapiens (human)
nucleusMineralocorticoid receptor Homo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
nucleoplasmEstrogen receptor betaHomo sapiens (human)
mitochondrionEstrogen receptor betaHomo sapiens (human)
intracellular membrane-bounded organelleEstrogen receptor betaHomo sapiens (human)
chromatinEstrogen receptor betaHomo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID429130Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
AID1375648Induction of nuclear translocation of human recombinant ProLabel-tagged glucocorticoid receptor expressed in CHO-K1 cells after 3 hrs by luminescence method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1476013Displacement of fluormone labelled GS Red from human recombinant glucocorticoid receptor after 2 hrs by fluorescence polarization assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
AID1375657MRTlast in Sprague-Dawley rat plasma at 1 umol/kg, it by HPLC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1068841n-Octanol-buffer partition coefficient, log D of the compound at pH 7.4 by shake-flask method2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases.
AID1375652Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release preincubated for 15 mins followed by LPS challenge measured after 18 hrs by Griess assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1476016Displacement of fluormone labelled PL Red from human recombinant progesterone receptor after 1 to 6 hrs ligand by fluorescence polarization assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
AID1375654Cmax in Sprague-Dawley rat lung at 1 umol/kg, it by HPLC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1476014Displacement of fluormone labelled EL Red from human recombinant estrogen receptor alpha after 1 to 5 hrs by fluorescence polarization assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
AID1476015Displacement of fluormone labelled EL Red from human recombinant estrogen receptor beta after 1 to 5 hrs by fluorescence polarization assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
AID1375653Cmax in Sprague-Dawley rat plasma at 1 umol/kg, it by HPLC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID622346Inhibition of TNFalpha release in human PBMC by ELISA assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.
AID1375650Induction of nuclear translocation of human recombinant ProLabel-tagged mineralocorticoid receptor expressed in CHO-K1 cells after 3 hrs by luminescence method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1476012Displacement of fluormone labelled AL green from rat recombinant His/GST-tagged androgen receptor LBD after 4 to 6 hrs by fluorescence polarization assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
AID1476011Displacement of [3H]-aldosterone from N terminal maltose binding protein tagged human mineralocorticoid receptor LBD (726 to 984 residues) expressed in baculovirus infected high five cells after 8 hrs by scintillation proximity assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
AID1375651Selectivity ratio of EC50 for human recombinant ProLabel-tagged mineralocorticoid receptor to EC50 for human recombinant ProLabel-tagged glucocorticoid receptor2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1654621Volume of distribution in human at 0.25 mg, iv administered as single dose measured up to 168 hrs2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Metabolic and Pharmaceutical Aspects of Fluorinated Compounds.
AID622347Inhibition of TNFalpha release in LPS-stimulated human whole blood by ELISA assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.
AID1654620Half life in human at 0.25 mg, iv administered as single dose measured up to 168 hrs2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Metabolic and Pharmaceutical Aspects of Fluorinated Compounds.
AID622345Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.
AID1068810Inhibition of ovalbumin-induced lung eosinophilia in Dunkin-Hartley guinea pig at 0.3 umol/kg administered intratracheally 2 hrs before ovalbumin challenge2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases.
AID1375655AUClast in Sprague-Dawley rat plasma at 1 umol/kg, it by HPLC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1375656AUClast in Sprague-Dawley rat lung at 1 umol/kg, it by HPLC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1375646Displacement of [3H]dexamethasone from human recombinant glucocorticoid receptor expressed in insect cells after 24 hrs by scintillation proximity assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID1375658MRTlast in Sprague-Dawley rat lung at 1 umol/kg, it by HPLC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
AID404878Displacement of [3H]Dexamethasone from glucocorticoid receptor in human lung tissue relative to Dexamethasone2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain.
AID1654622Oral bioavailability in human at 2 mg administered as single dose and measured up to 168 hrs2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Metabolic and Pharmaceutical Aspects of Fluorinated Compounds.
AID1375665Antiinflammatory activity in LPS-induced Sprague-Dawley rat neutrophilic lung inflammation model assessed as inhibition of neutrophilic infiltration in bronchoalveolar lavage at ID80, it preincubated for 24 hrs followed by LPS challenge measured after 4 h2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (232)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's25 (10.78)29.6817
2010's169 (72.84)24.3611
2020's38 (16.38)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.98

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 Index53.98 (24.57)
Research Supply Index5.96 (2.92)
Research Growth Index5.39 (4.65)
Search Engine Demand Index125.24 (26.88)
Search Engine Supply Index2.85 (0.95)

This Compound (53.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials134 (53.17%)5.53%
Reviews37 (14.68%)6.00%
Case Studies0 (0.00%)4.05%
Observational2 (0.79%)0.25%
Other79 (31.35%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]