gsk573719 profile

GSK573719: Muscarinic Antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

umeclidinium : A quaternary ammonium ion that is quinuclidine substituted at positions 1 and 4 by 2-(benzyloxy)ethyl and hydroxy(diphenyl)methyl groups respectively. [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]

ID Source	ID
PubMed CID	11519070
CHEMBL ID	1187833
CHEBI ID	79041
SCHEMBL ID	2033192
MeSH ID	M0575815

Synonym
bdbm50267614
869185-19-3
umeclidinium (usan)
D10180
gsk573719
1-(2-(benzyloxy)ethyl)-4-(hydroxydiphenylmethyl)-1-azoniabicyclo(2.2.2)octane
unii-ge2t1418sv
1-azoniabicyclo(2.2.2)octane, 4-(hydroxydiphenylmethyl)-1-(2-(phenylmethoxy)ethyl)-
umeclidinium [usan]
umeclidinium
ge2t1418sv ,
umeclidinium cation
umeclidinium ion
CHEMBL1187833
di(phenyl)-[1-[2-(phenylmethoxy)ethyl]-1-azoniabicyclo[2.2.2]octan-4-yl]methanol
gtpl7354
umeclidinium [who-dd]
1-(2-(benzyloxy)ethyl)-4-(hydroxy(diphenyl)methyl)-1-azoniabicyclo(2.2.2)octane
umeclidinium [vandf]
1-[2-(benzyloxy)ethyl]-4-[hydroxy(diphenyl)methyl]-1-azoniabicyclo[2.2.2]octane
CHEBI:79041 ,
DTXSID00235971 ,
SCHEMBL2033192
DB09076
Q21011235
NCGC00379061-01
dtxcid30158462

Excerpt	Reference	Relevance
" 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)	0.38
"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)	0.39
" 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)	0.39
"Thirteen subjects in each population reported adverse events (AEs); none were considered serious."	( Safety, tolerability and pharmacokinetics and pharmacodynamics of inhaled once-daily umeclidinium in healthy adults deficient in CYP2D6 activity: a double-blind, randomized clinical trial. Blowers, J; Cahn, A; Donald, A; Mehta, R; Preece, A, 2013)	0.39
" 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)	0.4
" 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)	0.4
" 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)	0.4
" 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)	0.42
" 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)	0.42
" 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)	0.42
" 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)	0.42
" In most clinical trials the incidence of cardiovascular adverse events was similar in active treatment and placebo groups, especially in patients with previous cardiovascular diseases."	( [Are there cardiovascular adverse effects of inhaled anticholinergics?]. Nagy, LB, 2015)	0.42
" 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)	0.42
" The primary endpoint was the incidence and severity of all adverse events (AEs) throughout the 52 week treatment period."	( Long-term (52 weeks) safety and tolerability of umeclidinium in Japanese patients with chronic obstructive pulmonary disease. Hashimoto, K; Mihara, K; Soutome, T; Tohda, Y; Yamagata, E, 2016)	0.43
" LAMAs are considered to be safe drugs at recommended dosages."	( Safety of long acting muscarinic antagonists: are all these drugs always and equally safe? Melani, AS; Sestini, P, 2016)	0.43
" Adverse events were also assessed."	( A randomized, blinded study to evaluate the efficacy and safety of umeclidinium 62.5 μg compared with tiotropium 18 μg in patients with COPD. Church, A; Fahy, WA; Feldman, G; Khindri, S; Maltais, F; Trivedi, R; Vahdati-Bolouri, M, 2016)	0.43
" Overall incidences of adverse events were similar for UMEC and TIO."	( A randomized, blinded study to evaluate the efficacy and safety of umeclidinium 62.5 μg compared with tiotropium 18 μg in patients with COPD. Church, A; Fahy, WA; Feldman, G; Khindri, S; Maltais, F; Trivedi, R; Vahdati-Bolouri, M, 2016)	0.43
" 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)	0.56

Excerpt	Reference	Relevance
"Umeclidinium has favourable safety and pharmacokinetic profiles in both HVT-NM and HVT-PM populations."	( Safety, tolerability and pharmacokinetics and pharmacodynamics of inhaled once-daily umeclidinium in healthy adults deficient in CYP2D6 activity: a double-blind, randomized clinical trial. Blowers, J; Cahn, A; Donald, A; Mehta, R; Preece, A, 2013)	0.39
" 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)	0.4
"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)	0.4
"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)	0.4
" 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)	0.4
" 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)	0.42
" 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)	0.42
"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)	0.48
"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)	0.56

Excerpt	Reference	Relevance
"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)	0.7
"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)	0.38

Excerpt	Relevance	Reference
"This study evaluated the dose-response and dosing interval of the novel long-acting muscarinic receptor antagonist (LAMA) GSK573719 in patients with COPD."	( A randomized, double-blind dose-ranging study of the novel LAMA GSK573719 in patients with COPD. Anzueto, A; Brooks, J; Crater, G; Donohue, JF; Kalberg, C; Mehta, R, 2012)	0.83
"Once-daily dosing with GSK573719 in COPD provides clinically significant and sustained improvement in lung function over 24 h with similar efficacy to twice-daily dosing."	( A randomized, double-blind dose-ranging study of the novel LAMA GSK573719 in patients with COPD. Anzueto, A; Brooks, J; Crater, G; Donohue, JF; Kalberg, C; Mehta, R, 2012)	0.93
" 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)	0.38
"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)	0.38
"This study evaluated the dose-response of the new long-acting muscarinic antagonist umeclidinium (GSK573719) in patients with COPD."	( Bronchodilation of umeclidinium, a new long-acting muscarinic antagonist, in COPD patients. Brooks, J; Crater, G; Decramer, M; Feldman, G; Harris, S; Maltais, F; Mehta, R, 2013)	0.61
" In the single-dose study, subjects (n = 20) received umeclidinium (10-350 μg), tiotropium bromide 18 μg and placebo in a crossover dosing schedule."	( Safety, tolerability, pharmacokinetics and pharmacodynamics of single and repeat inhaled doses of umeclidinium in healthy subjects: two randomized studies. Cahn, A; Crater, G; Deans, A; Hardes, K; Mehta, R; Pouliquen, IJ; Preece, A; Tal-Singer, R, 2013)	0.39
" To fully characterize the dose-response relationship of UMEC in patients with COPD, a pooled analysis of data from two randomized, placebo-controlled, cross-over, dose-ranging studies was performed, evaluating UMEC at doses of 15."	( Dose response of umeclidinium administered once or twice daily in patients with COPD: a pooled analysis of two randomized, double-blind, placebo-controlled studies. Beerahee, M; Church, A; Donohue, JF; Gunawan, R; Kalberg, C; Mehta, R; Shah, P, 2014)	0.4
" 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)	0.4
" 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)	0.42
" 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)	0.42
" 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)	0.42
"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)	0.42
" 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

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	22.3872	0.0096	10.5250	35.4813	AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID1345286	Human M1 receptor (Acetylcholine receptors (muscarinic))	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.
AID1345343	Human M3 receptor (Acetylcholine receptors (muscarinic))	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.
AID1345326	Human M2 receptor (Acetylcholine receptors (muscarinic))	2013	The Journal of pharmacology and experimental therapeutics, May, Volume: 345, Issue:2	Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases.
AID1345543	Human M5 receptor (Acetylcholine receptors (muscarinic))	2013	The Journal of pharmacology and experimental therapeutics, May, Volume: 345, Issue:2	Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases.
AID1345343	Human M3 receptor (Acetylcholine receptors (muscarinic))	2013	The Journal of pharmacology and experimental therapeutics, May, Volume: 345, Issue:2	Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases.
AID1345326	Human M2 receptor (Acetylcholine receptors (muscarinic))	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.
AID1345465	Human M4 receptor (Acetylcholine receptors (muscarinic))	2013	The Journal of pharmacology and experimental therapeutics, May, Volume: 345, Issue:2	Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases.
AID1345286	Human M1 receptor (Acetylcholine receptors (muscarinic))	2013	The Journal of pharmacology and experimental therapeutics, May, Volume: 345, Issue:2	Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	1 (0.69)	29.6817
2010's	112 (77.78)	24.3611
2020's	31 (21.53)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	63 (42.00%)	5.53%
Reviews	34 (22.67%)	6.00%
Case Studies	1 (0.67%)	4.05%
Observational	5 (3.33%)	0.25%
Other	47 (31.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
bromide Bromides: Salts of hydrobromic acid, HBr, with the bromine atom in the 1- oxidation state. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)	9.57	6	4	halide anion; monoatomic bromine
albuterol Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).	10.57	9	6	phenols; phenylethanolamines; secondary amino compound	beta-adrenergic agonist; bronchodilator agent; environmental contaminant; xenobiotic
verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.	4.39	1	1	aromatic ether; nitrile; polyether; tertiary amino compound
thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.	2.51	2	0	phthalimides; piperidones
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	2.08	1	0	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
carbostyril Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.	10.35	10	4	monohydroxyquinoline; quinolone	bacterial xenobiotic metabolite
quinuclidines Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group.	20.53	153	73	quinuclidines; saturated organic heterobicyclic parent
potassium carbonate potassium carbonate : A potassium salt that is the dipotassium salt of carbonic acid.	2.17	1	0	carbonate salt; potassium salt	catalyst; fertilizer; flame retardant
glycopyrrolate Glycopyrrolate: A muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.. glycopyrronium bromide : A quaternary ammonium salt composed of 3-{[cyclopentyl(hydroxy)phenylacetyl]oxy}-1,1-dimethylpyrrolidin-1-ium and bromide ions in a 1:1 ratio.	10.73	14	3	organic bromide salt; quaternary ammonium salt
carbonates Carbonates: Salts or ions of the theoretical carbonic acid, containing the radical CO2(3-). Carbonates are readily decomposed by acids. The carbonates of the alkali metals are water-soluble; all others are insoluble. (From Grant & Hackh's Chemical Dictionary, 5th ed). carbonates : Organooxygen compounds that are salts or esters of carbonic acid, H2CO3.	2.17	1	0	carbon oxoanion
salmeterol xinafoate Salmeterol Xinafoate: A selective ADRENERGIC BETA-2 RECEPTOR agonist that functions as a BRONCHODILATOR when administered by inhalation. It is used to manage the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE.	7.04	4	1	naphthoic acid
glucose, (beta-d)-isomer beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.	2.8	3	0	D-glucopyranose	epitope; mouse metabolite
moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.	4.46	2	2	aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone	antibacterial drug
bazedoxifene [no description available]	2.52	2	0	phenylindole
eslicarbazepine acetate eslicarbazepine acetate : The acetate ester, with S configuration, of licarbazepine. An anticonvulsant, it is approved for use in Europe and the United States as an adjunctive therapy for epilepsy.	2.11	1	0	acetate ester; carboxamide; dibenzoazepine; ureas	anticonvulsant; drug allergen
pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.	5.89	2	2	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone	anti-inflammatory drug; bronchodilator agent; drug allergen
fluticasone Fluticasone: A STEROID with GLUCOCORTICOID RECEPTOR activity that is used to manage the symptoms of ASTHMA; ALLERGIC RHINITIS, and ATOPIC DERMATITIS.. fluticasone : A trifluorinated corticosteroid used in the form of its propionate ester for treatment of allergic rhinitis.	10.48	12	5	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 3-oxo-Delta(4) steroid; corticosteroid; fluorinated steroid; thioester	anti-allergic agent; anti-asthmatic drug
tiotropium bromide Tiotropium Bromide: A scopolamine derivative and CHOLINERGIC ANTAGONIST that functions as a BRONCHODILATOR AGENT. It is used in the treatment of CHRONIC OBSTRUCTIVE PULMONARY DISEASE.. tiotropium bromide : An organic bromide salt having (1alpha,2beta,4beta,5alpha,7beta)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0(2,4)]nonane as the counterion. Used (in the form of the hydrate) for maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease.	13.16	29	8
tiotropium tiotropium : A quaternary ammonium ion obtained by methylation of the tertiary amino group of (1alpha,2beta,4beta,5alpha,7beta)-7-[(hydroxydi-2-thienylacetyl)oxy]-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.0(2,4)]nonane. Used (in the form of the bromide hydrate) for maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease.	2.08	1	0
indacaterol indacaterol: a beta2 adrenoceptor agonist; indacaterol is the (R)-isomer; structure in first source. indacaterol : A monohydroxyquinoline that consists of 5-[(1R)-2-amino-1-hydroxyethyl]-8-hydroxyquinolin-2-one having a 5,6-diethylindan-2-yl group attached to the amino function. Used as the maleate salt for treatment of chronic obstructive pulmonary disease.	7.91	6	2	indanes; monohydroxyquinoline; quinolone; secondary alcohol; secondary amino compound	beta-adrenergic agonist; bronchodilator agent
fluticasone furoate fluticasone furoate: a glucocorticoid; structure in first source. 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.	15.03	43	21	11beta-hydroxy steroid; 2-furoate ester; 3-oxo-Delta(1),Delta(4)-steroid; corticosteroid; fluorinated steroid; steroid ester; thioester	anti-allergic agent; anti-asthmatic drug; prodrug
avanafil [no description available]	2.52	2	0	aromatic amide; monocarboxylic acid amide; organochlorine compound; prolinols; pyrimidines	EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent
dapagliflozin [no description available]	2.51	2	0	aromatic ether; C-glycosyl compound; monochlorobenzenes	hypoglycemic agent; sodium-glucose transport protein subtype 2 inhibitor
perampanel perampanel : A member of the class of bipyridines that is 2,3'-bipyridin-6'-one substituted at positions 1' and 5' by phenyl and 2-cyanophenyl groups respectively. Used as an adjunctive therapy for the treatment of partial-onset seizures in patients with epilepsy.	2.11	1	0	bipyridines; nitrile; pyridone	AMPA receptor antagonist; anticonvulsant
vortioxetine Vortioxetine: A piperazine derivative that acts as a serotonin reuptake inhibitor, as a 5-HT3 receptor antagonist, and 5-HT1A receptor agonist. It is used for the treatment of anxiety and depression.. vortioxetine : An N-arylpiperazine in which the aryl group is specified as 2-[(2,4-dimethylphenyl)sulfanyl]phenyl. Used (as its hydrobromide salt) for treatment of major depressive disorder.	2.11	1	0	aryl sulfide; N-arylpiperazine	antidepressant; anxiolytic drug; serotonergic agonist; serotonergic antagonist
vorapaxar vorapaxar: has antiplatelet activity; structure in first source. vorapaxar : A carbamate ester that is the ethyl ester of [(1R,3aR,4aR,6R,8aR,9S,9aS)-9-{(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethynyl}-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl]carbamic acid. A protease-activated receptor-1 antagonist used (as its sulfate salt) for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease. It has been shown to reduce the rate of a combined endpoint of cardiovascular death, MI, stroke and urgent coronary revascularisation.	2.1	1	0	carbamate ester; lactone; naphthofuran; organofluorine compound; pyridines	cardiovascular drug; platelet aggregation inhibitor; protease-activated receptor-1 antagonist
vilanterol [no description available]	19.05	114	49	benzyl alcohols; dichlorobenzene; ether; phenols; secondary amino compound	beta-adrenergic agonist; bronchodilator agent
bay 63-2521 riociguat: guanylate cyclase stimulator; structure in first source. riociguat : A carbamate ester that is the methyl ester of {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamic acid. It is used for treatment of chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension	2.1	1	0	aminopyrimidine; carbamate ester; organofluorine compound; pyrazolopyridine	antihypertensive agent; soluble guanylate cyclase activator
olodaterol [no description available]	4.33	4	0	aromatic ether; benzoxazine; phenols; secondary alcohol; secondary amino compound	beta-adrenergic agonist; bronchodilator agent
aclidinium bromide aclidinium bromide: a long-acting, inhaled antimuscarinic; in phase I trial 8/2008. aclidinium bromide : A quaternary ammonium salt that is the bromide salt of aclidinium. A muscarinic acetylcholine M3 receptor antagonist, for the long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD).	4.8	3	0	organic bromide salt; quaternary ammonium salt	bronchodilator agent; muscarinic antagonist
apremilast [no description available]	2.51	2	0	aromatic ether; N-acetylarylamine; phthalimides; sulfone	non-steroidal anti-inflammatory drug; phosphodiesterase IV inhibitor
empagliflozin [no description available]	2.11	1	0	aromatic ether; C-glycosyl compound; monochlorobenzenes; tetrahydrofuryl ether	hypoglycemic agent; sodium-glucose transport protein subtype 2 inhibitor
glucagon-like peptide 1 Glucagon-Like Peptide 1: A peptide of 36 or 37 amino acids that is derived from PROGLUCAGON and mainly produced by the INTESTINAL L CELLS. GLP-1(1-37 or 1-36) is further N-terminally truncated resulting in GLP-1(7-37) or GLP-1-(7-36) which can be amidated. These GLP-1 peptides are known to enhance glucose-dependent INSULIN release, suppress GLUCAGON release and gastric emptying, lower BLOOD GLUCOSE, and reduce food intake.	2.51	2	0
(9R)-9-chloro-11,17-dihydroxy-17-(2-hydroxy-1-oxoethyl)-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one Beclomethasone: An anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of ASTHMA.. beclomethasone : A 17alpha-hydroxy steroid that is prednisolone in which the hydrogens at the 9alpha and 16beta positions are substituted by a chlorine and a methyl group, respectively.	2.31	1	0	21-hydroxy steroid
budesonide, formoterol fumarate drug combination Budesonide, Formoterol Fumarate Drug Combination: A pharmaceutical preparation of budesonide and formoterol fumarate that is used as an ANTI-ASTHMATIC AGENT and for the treatment of CHRONIC OBSTRUCTIVE PULMONARY DISEASE.	4.94	2	1
fluticasone propionate, salmeterol xinafoate drug combination Fluticasone-Salmeterol Drug Combination: A drug combination of fluticasone and salmeterol that is used as an inhaler formulation to manage the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE.	9.26	8	4

Condition	Indicated	Relationship Strength	Studies	Trials
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	0	2.05	1	0
Disease, Pulmonary [description not available]	0	2.08	1	0
Lung Diseases Pathological processes involving any part of the LUNG.	0	2.08	1	0
Airflow Obstruction, Chronic [description not available]	0	20.6	159	81
Pulmonary Disease, Chronic Obstructive A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.	1	22.6	159	81
Breathlessness [description not available]	0	9.58	7	6
Dyspnea Difficult or labored breathing.	0	9.58	7	6
Experimental Lung Inflammation Inflammation of any part, segment or lobe, of the lung parenchyma.	0	2.82	2	0
Pneumonia Infection of the lung often accompanied by inflammation.	0	2.82	2	0
Disease Exacerbation [description not available]	0	9.7	12	4
Asthma, Bronchial [description not available]	0	12.89	23	9
Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).	1	14.89	23	9
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	6.06	3	1
Acute Symptom Flare [description not available]	0	4.62	1	1
Hyperidrosis [description not available]	0	3.56	1	1
Hyperhidrosis Excessive sweating. In the localized type, the most frequent sites are the palms, soles, axillae, inguinal folds, and the perineal area. Its chief cause is thought to be emotional. Generalized hyperhidrosis may be induced by a hot, humid environment, by fever, or by vigorous exercise.	1	5.56	1	1
Catarrh Inflammation of a mucous membrane with increased flow of mucous in humans or animals. Catarrh is used mostly in a historical context.	0	3.09	1	0
Haemophilus Infections Infections with bacteria of the genus HAEMOPHILUS.	0	3.09	1	0
Moraxella Infections [description not available]	0	3.09	1	0
Common Cold A catarrhal disorder of the upper respiratory tract, which may be viral or a mixed infection. It generally involves a runny nose, nasal congestion, and sneezing.	0	3.09	1	0
Biliary Cirrhosis [description not available]	0	4.48	1	1
Itching [description not available]	0	4.48	1	1
Liver Cirrhosis, Biliary FIBROSIS of the hepatic parenchyma due to obstruction of BILE flow (CHOLESTASIS) in the intrahepatic or extrahepatic bile ducts (BILE DUCTS, INTRAHEPATIC; BILE DUCTS, EXTRAHEPATIC). Primary biliary cholangitis involves the destruction of small intra-hepatic bile ducts and decreased bile secretion. Secondary biliary cholangitis is produced by prolonged obstruction of large intrahepatic or extrahepatic bile ducts from a variety of causes.	0	4.48	1	1
Pruritus An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.	0	4.48	1	1
Liver Dysfunction [description not available]	0	3.48	1	1
Liver Diseases Pathological processes of the LIVER.	0	3.48	1	1
Electrocardiogram QT Prolonged [description not available]	0	3.48	1	1
Long QT Syndrome A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.	0	3.48	1	1
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	0	4.41	1	1

gsk573719

Description

Cross-References

Synonyms (27)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Dosage Studied

Protein Targets (1)

Potency Measurements

Ceullar Components (1)

Bioassays (8)

Research

Studies (144)

Market Indicators

Research Demand Index: 16.73

Study Types