Compounds > salmeterol xinafoate
Page last updated: 2024-12-05

salmeterol xinafoate

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

Description

Salmeterol xinafoate is a long-acting beta2-adrenergic receptor agonist (LABA) used for the treatment of asthma and chronic obstructive pulmonary disease (COPD). It works by relaxing the muscles in the airways, making it easier to breathe. Salmeterol xinafoate is typically administered by inhalation, and its effects can last for up to 12 hours. The synthesis of salmeterol xinafoate involves several steps, starting with the reaction of 4-hydroxy-3-methoxybenzaldehyde with 2-chloro-4-methylaniline to form an imine. This imine is then reacted with 2-methyl-1-propanol to form the corresponding alcohol. The alcohol is then reacted with 4-chlorobenzoyl chloride to form the desired product. The xinafoate salt is formed by reacting salmeterol with xinafoic acid. Salmeterol xinafoate is studied because of its potential to improve lung function and reduce symptoms in patients with asthma and COPD. It is also being investigated for its potential to prevent asthma attacks and reduce the need for other medications. Salmeterol xinafoate is an important medication because it can provide long-lasting relief from asthma and COPD symptoms. However, it is important to note that salmeterol xinafoate should not be used as a first-line treatment for asthma. It should only be used in conjunction with other medications, such as inhaled corticosteroids. Salmeterol xinafoate can also cause serious side effects, such as heart problems, high blood pressure, and seizures.'
```

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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

salmeterol : A racemate consisting of equal parts of (R)- and (S)-salmeterol. It is a potent and selective beta2-adrenoceptor agonist (EC50 = 5.3 nM). Unlike other beta2 agonists, it binds to the exo-site domain of beta2 receptors, producing a slow onset of action and prolonged activation. [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]

2-(hydroxymethyl)-4-(1-hydroxy-2-{[6-(4-phenylbutoxy)hexyl]amino}ethyl)phenol : A phenol having a hydroxymethyl group at C-2 and a 1-hydroxy-2-{[6-(4-phenylbutoxy)hexyl]amino}ethyl group at C-4; derivative of phenylethanolamine. [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 CID56801
CHEMBL ID1082607
CHEBI ID9012
SCHEMBL ID18070
MeSH IDM000602359
PubMed CID5152
CHEMBL ID1263
CHEBI ID64064
CHEBI ID9011
SCHEMBL ID4767
MeSH IDM000602359

Synonyms (225)

Synonym
EU-0101100
salmeterol xinafoate, >=98% (hplc), solid
dilamax
betamican
gr 33343 g
beglan
salmeterol xinafoate
inaspir
asmerole
(+-)-4-hydroxy-alpha(sup 1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-m-xylene-alpha,alpha'-diol 1-hydroxy-2-naphthoate (salt)
serevent inhaler and disks
arial
1,3-benzenedimethanol, 4-hydroxy-alpha(sup 1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-, (+-)-, 1-hydroxy-2-naphthalenecarboxylate (salt)
serevent diskus
ultrabeta
salmeterol xinafoate [usan]
salmeterol 1-hydroxy-2-naphthoate
salmetedur
MLS001332578
MLS001332577
smr000875207
NCGC00094372-02
94749-08-3
salmeterol xinafoate (jan/usp)
serevent (tn)
D00687
NCGC00094372-01
NCGC00094372-03
NCGC00094372-04
gr-33343x
gr-33343 g
lipo-202
CHEMBL1082607
HMS3263K22
6ew8q962a5 ,
salmeterol xinafoate [usan:usp]
unii-6ew8q962a5
dtxcid9025798
cas-94749-08-3
tox21_111270
dtxsid1045798 ,
4-(1-hydroxy-2-((6-(4-phenylbutoxy)hexyl)amino)ethyl)-2-(hydroxymethyl)phenol 1-hydroxy-2-naphthoate
HMS2232I16
S4296
AKOS016004957
FT-0642283
BCP0726000003
gr 33343x xinafoate
LP01100
advair hfa component salmeterol xinafoate
salmeterol xinafoate [orange book]
salmeterol 1-hydroxy-2-naphthoate [mi]
salmeterol xinafoate [who-dd]
salmeterol xinafoate [ep impurity]
advair component salmeterol xinafoate
salmeterol xinafoate [usp-rs]
salmeterol xinafoate component of airduo respiclick
salmeterol xinafoate [usp monograph]
1,3-benzenedimethanol, 4-hydroxy-.alpha.(sup 1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-, (+/-)-, 1-hydroxy-2-naphthalenecarboxylate
salmeterol xinafoate [ep monograph]
salmeterol xinafoate [vandf]
lipo-102 component salmeterol xinafoate
airduo respiclick component salmeterol xinafoate
salmeterol xinafoate component of advair hfa
(+/-)-4-hydroxy-.alpha.(sup 1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-m-xylene-.alpha.,.alpha.'-diol 1-hydroxy-2-naphthoate
salmeterol xinafoate [jan]
salmeterol xinafoate [mart.]
salmeterol xinafoate component of advair
CS-1527
HY-17453
salmeterol (xinafoate)
SCHEMBL18070
tox21_111270_1
NCGC00015938-05
KS-1140
NCGC00261785-01
tox21_501100
Q-201697
4-hydroxy-?1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol 1-hydroxy-2-naphthalenecarboxylic acid salt
A3190
salmeterol xinafoate, pharmaceutical secondary standards; certified reference material
HB3282
2-[2-(4-acetylphenyl)diazenyl]-2-(3 ,4-dihydro-3,3-dimethyl-1(2h)-isoquinolinylidene)a cetamide
c21h22n4o2
mfcd00897708
2-(hydroxymethyl)-4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]phenol;1-hydroxynaphthalene-2-carboxylic acid
xinafoate, salmeterol
SR-01000597359-1
sr-01000597359
salmeterol xinafoate, united states pharmacopeia (usp) reference standard
salmeterol, 1-hydroxy-2-naphthoate
salmeterol xinafoate, european pharmacopoeia (ep) reference standard
salmeterol xinafoate for system suitability, european pharmacopoeia (ep) reference standard
salmeterol xinafoate; (1rs)-1-[4-hydroxy-3-(hydroxymethyl)phenyl]-2-[[6-(4-phenylbutoxy)hexyl]amino]ethanol 1-hydroxynaphthalene-2-carboxylate; gr 33343g; gr 33343g
CHEBI:9012
BCP04778
HMS3676P13
4-[1-hydroxy-2-[[6-(4-phenylbutoxy)hexyl]amino]ethyl]-2-(hydroxymethyl)phenol 1-hydroxy-2-naphthoate
AMY23373
4-(1-hydroxy-2-(6-(4-phenylbutoxy)hexylamino)ethyl)-2-(hydroxymethyl)phenol 1-hydroxy-2-naphthoate
HMS3885J19
HMS3749I03
CCG-270203
Q27264747
R10007
salmeterolo
A916443
(+/-)-4-hydroxy-alpha(sup 1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-m-xylene-alpha,alpha'-diol 1-hydroxy-2-naphthoate
salmeterol xinafoate (ep impurity)
salmeterol xinafoate (mart.)
1,3-benzenedimethanol, 4-hydroxy-alpha(sup 1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-, (+/-)-, 1-hydroxy-2-naphthalenecarboxylate
sereventdiskus
salmeterol xinafoate (ep monograph)
salmeterol xinafoate (usan:usp)
salmeterol xinafoate (usp-rs)
salmeterol xinafoate (usp monograph)
AKOS005561914
HMS3268K19
HMS3394H13
BRD-A01320529-001-05-9
gtpl559
2-(hydroxymethyl)-4-[1-hydroxy-2-({6-[(4-phenylbutyl)oxy]hexyl}amino)ethyl]phenol
(+-)-4-hydroxy-alpha1-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-1,3-benzenedimethanol
aeromax
1,3-benzenedimethanol, 4-hydroxy-alpha(sup 1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-, (+-)-
1,3-benzenedimethanol, 4-hydroxy-alpha1-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-, (+-)-
1,3-benzenedimethanol, 4-hydroxy-alpha(sup 1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl-, (+-)-
salmeterolum [latin]
serevent
hsdb 7315
gr 33343x
(+-)-4-hydroxy-alpha'-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-m-xylene-alpha,alpha'-diol
astmerole
BSPBIO_000910
PRESTWICK3_000945
salmeterol (usan/inn)
D05792
BPBIO1_001002
LOPAC0_001100
4-(1-hydroxy-2-{[6-(4-phenylbutoxy)hexyl]amino}ethyl)-2-(hydroxymethyl)phenol
bdbm25771
1-hydroxy-2-naphthoic acid;4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]-2-methylol-phenol
MLS001424322
AB00513972
C07241
salmeterol
89365-50-4
smr000466295
MLS000759000
cpd000466295
DB00938
salmaterol
NCGC00025247-02
HMS2090E17
HMS2052H13
S 2692 ,
( inverted question mark) 4-hydroxy-a1-[[[6-(4-phenylbutoxy)hexyl]amino]m-ethyl]-1,3-benzenedimethanol; gr 33343x
gr-33343-x
gr 33343 x
sn408d
CHEMBL1263
chebi:64064 ,
L000532
salmeterol dimer impurity
2-(hydroxymethyl)-4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]phenol
2-(hydroxymethyl)-4-(1-hydroxy-2-{[6-(4-phenylbutoxy)hexyl]amino}ethyl)phenol
STK629186
HMS2097N12
dtxcid803571
cas-89365-50-4
tox21_113584
dtxsid6023571 ,
CCG-205176
CCG-101194
NCGC00015938-03
salmeterolum
2i4bc502bt ,
unii-2i4bc502bt
salmeterol [usan:inn:ban]
FT-0674509
FT-0674508
S5527
salmeterol [vandf]
salmeterol [mi]
salmeterol [hsdb]
salmeterol [usan]
salmeterol [inn]
salmeterol [who-dd]
HY-14302
NC00444
SCHEMBL4767
2-hydroxymethyl-4-{1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl}phenol
AB00513972-07
Q-101428
1,3-benzenedimethanol, 4-hydroxy-.alpha.1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-
3-benzenedimethanol, 4-hydroxy-?1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-; 1,3-benzenedimethanol, 4-hydroxy-?1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-, (+/-)-; gr 33343x; salmeterol; gr 33343x
SR-01000076139-6
sr-01000076139
SR-01000076139-2
MRF-0000468
HMS3714N12
BCP04199
Q424333
mfcd00867037
HMS3412P13
4-(1-hydroxy-2-(6-(4-phenylbutoxy)hexylamino)ethyl)-2-(hydroxymethyl)phenol
SDCCGSBI-0633788.P001
HMS3886G10
AMY37616
C77008
EX-A4409
AS-56157
gr33343xgr33343x
salmeterol 100 microg/ml in acetonitrile
salmeterol xinafoate impurity 1
EN300-18530979
r03ac12
(rs)-4-hydroxy-alpha(1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-1,3-benzenedimethanol
(+/-)-4-hydroxy-alpha1-
(+-)-salmeterol
(rs)-salmeterol
(+-)-4-hydroxy-alpha(1)-(((6-(4-phenylbutoxy)hexyl)amino)methyl)-m-xylene-alpha,alpha(1)-diol
chebi:9011
salmeterolum (latin)
4-hydroxy-alpha1-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Safety was determined by monitoring adverse events and standard biochemical, haematological and cardiovascular parameters."( Inhaled salmeterol in the treatment of patients with moderate to severe reversible obstructive airways disease--a 3-month comparison of the efficacy and safety of twice-daily salmeterol (100 micrograms) with salmeterol (50 micrograms).
Palmer, JB; Shepherd, GL; Stuart, AM; Viskum, K, 1992)		0.28
"The incidence of potentially drug-related adverse events was similar among the treatment groups (range: 22% to 23%), with headache being the most commonly reported (range: 9% to 10%)."( Safety of salmeterol in the maintenance treatment of asthma.
Alexander, WJ; Chervinsky, P; Kemp, JP; Liddle, R; Mills, R; Nathan, RA; Seltzer, JM, 1995)		0.29
" Extensive cardiovascular monitoring revealed no significant cardiovascular adverse effects or arrhythmogenic effects associated with salmeterol over 12 weeks."( Safety of salmeterol in the maintenance treatment of asthma.
Alexander, WJ; Chervinsky, P; Kemp, JP; Liddle, R; Mills, R; Nathan, RA; Seltzer, JM, 1995)		0.29
" Cough, headache and itchy throat were adverse events possibly related to the use of Salmeterol."( Efficacy and safety of inhaled Salmeterol (Serevent) as maintenance therapy for asthma in Nairobi.
Gikonyo, BM; Nganga, LW; Odhiambo, JA, 1994)		0.29
" Salmeterol was well tolerated as assessed by pulse, blood pressure, haematological and biochemical variables and number of adverse events."( The efficacy and safety of inhaled salmeterol 50 microg bd in older patients with reversible airflow obstruction.
Luce, P; Starke, ID, 1996)		0.29
" Both studies were continued for a further 9 months during which time exacerbation rates, lung function at the clinic and adverse events were monitored."( Efficacy and safety of salmeterol in childhood asthma.
Boner, AL; Ebbutt, A; Jenkins, MM; Lenney, W; Pedersen, S, 1995)		0.29
"Cardiovascular safety was regularly assessed by 12-lead ECG with a 15-s lead II rhythm strip, 24-h continuous ambulatory ECG (Holter) monitoring, serial vital sign measurements, and review of adverse cardiovascular events."( Long-term cardiovascular safety of salmeterol powder pharmacotherapy in adolescent and adult patients with chronic persistent asthma: a randomized clinical trial.
Arledge, T; Chervinsky, P; Galant, S; Goldberg, P; Stahl, E; Wang, Y; Welch, MB, 1999)		0.3
"Long-term, twice-daily pharmacotherapy with salmeterol powder is safe and is not associated with unfavorable clinically significant changes in cardiac function or increases in cardiovascular adverse effects."( Long-term cardiovascular safety of salmeterol powder pharmacotherapy in adolescent and adult patients with chronic persistent asthma: a randomized clinical trial.
Arledge, T; Chervinsky, P; Galant, S; Goldberg, P; Stahl, E; Wang, Y; Welch, MB, 1999)		0.3
"As no cardiac side effects were detected, it could be concluded that salmeterol is quite a safe drug for use in childhood asthma treatment."( Cardiac side effects of long-acting beta-2 agonist salmeterol in asthmatic children.
Demirsoy, S; Olguntürk, R; Tunaoğlu, FS; Türktaş, I, 1999)		0.3
" Safety measurements included vital signs, physical examination, and reports of clinical adverse events at baseline and after 4, 8, and 12 weeks of treatment."( Efficacy, safety, and impact on quality of life of salmeterol in patients with moderate persistent asthma.
Busse, WW; Casale, TB; Cox, F; Murray, JJ; Petrocella, V; Rickard, K, 1998)		0.3
" Pulmonary function, symptom control, frequency of asthma exacerbations, bronchial hyperresponsiveness (BHR) to methacholine challenge, and adverse events were assessed."( A six-month, placebo-controlled comparison of the safety and efficacy of salmeterol or beclomethasone for persistent asthma.
Emmett, AH; Grossman, J; Nathan, RA; Pinnas, JL; Rickard, KA; Schwartz, HJ; Yancey, SW, 1999)		0.3
" Safety assessments included monitoring of adverse events and morning serum cortisol concentrations."( Salmeterol/fluticasone propionate (50/100 microg) in combination in a Diskus inhaler (Seretide) is effective and safe in children with asthma.
Anttila, H; Davies, PI; Hederos, CA; Ossip, MS; Ribeiro, BL; Van den Berg, NJ, 2000)		0.31
" Frequent adverse events were exacerbations of the underlying airway disease (24%) and infections (12%), while typical pharmacological side-effects like tremor or tachycardia where reported in less than 1% of all patients."( [efficacy and safety of salmeterol in long-term therapy in patients with chronic obstructive airway diseases].
Beeh, KM; Buhl, R; Salem, AE; Wiewrodt, R, 2000)		0.31
" Lung function, quality of life and adverse events were evaluated as primary outcome variables."( [Efficacy and safety of salmeterol (50 microgram) and fluticasone (250 microgram) in a single inhaler device (diskus) in patients with mild to moderate asthma].
Beeh, KM; Beier, J; Buhl, R; Kornmann, O; Wiewrodt, R, 2002)		0.31
" Frequent adverse events included symptoms of asthma (5."( [Efficacy and safety of salmeterol (50 microgram) and fluticasone (250 microgram) in a single inhaler device (diskus) in patients with mild to moderate asthma].
Beeh, KM; Beier, J; Buhl, R; Kornmann, O; Wiewrodt, R, 2002)		0.31
" The incidence of adverse effects (except for an increase in oral candidiasis with FSC and FP) were similar among the treatment groups."( The efficacy and safety of fluticasone propionate (250 microg)/salmeterol (50 microg) combined in the Diskus inhaler for the treatment of COPD.
Darken, P; Davis, S; Hanania, NA; Horstman, D; Lee, B; Reisner, C; Shah, T, 2003)		0.32
"Despite concerns in the 1970s and 1980s about the safety of short-acting beta2-agonists, it is now generally accepted that these agents, used at appropriate doses, provide safe and effective treatment for asthma symptoms."( State of the art in beta2-agonist therapy: a safety review of long-acting agents.
Rabe, KF, 2003)		0.32
" Forced expiratory volume in 1 s (FEV1), pulse, blood pressure, electrocardiogram, adverse events and urine formoterol were assessed."( Dose-related efficacy and safety of formoterol (Oxis) Turbuhaler compared with salmeterol Diskhaler in children with asthma.
Honomichlová, H; Kopriva, F; Matulka, M; Pohunek, P; Rybnícek, O; Svobodová, T, 2004)		0.32
" Both treatments were well tolerated, and the adverse reactions showed no significant difference between the two groups."( [Evaluation of the clinical efficacy and the safety of salmeterol/fluticasone propionate accuhaler compared to budesonide turbuhalar in the control of adult asthma].
Cai, BQ; Chen, BY; Chen, XD; Feng, YL; Guo, XJ; Kang, J; Li, Q; Lin, YP; Qiu, C; Shen, HH; Sun, TY; Tao, JJ; Wang, DQ; Xiao, BR; Xie, CM; Xu, YP; Yin, KS; Zhang, DP; Zheng, JP; Zhong, NS; Zhou, JY; Zhou, X, 2005)		0.33
" Safety was assessed according to adverse events recorded."( Efficacy and safety of salmeterol/fluticasone propionate delivered via a hydrofluoroalkane metered dose inhaler in Chinese patients with moderate asthma poorly controlled with inhaled corticosteroids.
Du, X; Humphries, M; Jiang, J; Wang, L; You-Ning, L, 2005)		0.33
"Although large surveys have documented the favourable safety profile of beta(2)-adrenoceptor agonists (beta(2)-agonists) and, above all, that of the long-acting agents, the presence in the literature of reports of adverse cardiovascular events in patients with obstructive airway disease must induce physicians to consider this eventuality."( Inhaled beta2-adrenoceptor agonists: cardiovascular safety in patients with obstructive lung disease.
Cazzola, M; Donner, CF; Matera, MG, 2005)		0.33
" The overall incidence of adverse events was 59% for fluticasone propionate-salmeterol and 57% for fluticasone propionate."( The safety of twice-daily treatment with fluticasone propionate and salmeterol in pediatric patients with persistent asthma.
Dorinsky, P; Ellsworth, A; House, K; LaForce, C; Malone, R; Nimmagadda, S; Schoaf, L, 2005)		0.33
" There is much to suggest that the adverse outcomes associated with LABA monotherapy have been due to "masking of inflammation" rather than a toxic effect of the drugs."( Long-acting beta-agonists in adult asthma: Evidence that these drugs are safe.
Nelson, HS, 2006)		0.33
"Two very large, randomized, double-blind clinical trials performed in the United Kingdom and in the United States have suggested that addition of salmeteräE to usual asthma therapy is associated with a significant increase in the incidence of serious adverse events and asthma-related deaths compared with addition of albuterol or placebo to usual therapy in the same type of patients."( Serious adverse events and death associated with treatment using long-acting beta-agonists.
Martinez, FD, )		0.13
" LABAs are well-tolerated in patients with COPD, with a low incidence of reported adverse events (AEs)."( Clinical safety of long-acting beta2-agonist and inhaled corticosteroid combination therapy in COPD.
Decramer, M; Ferguson, G, 2006)		0.33
" Few adverse events were reported; all were mild or moderate in severity."( Efficacy and safety of single therapeutic and supratherapeutic doses of indacaterol versus salmeterol and salbutamol in patients with asthma.
Barbier, M; Brookman, LJ; Elharrar, B; Fuhr, R; Knowles, LJ; Pascoe, S, 2007)		0.34
" The sustained bronchodilation of indacaterol 1000 microg was not associated with sustained systemic adverse effects."( Efficacy and safety of single therapeutic and supratherapeutic doses of indacaterol versus salmeterol and salbutamol in patients with asthma.
Barbier, M; Brookman, LJ; Elharrar, B; Fuhr, R; Knowles, LJ; Pascoe, S, 2007)		0.34
"To compare the risk of total mortality and certain respiratory and cardiac adverse events among users of the two types of recommended long-acting bronchodilators, we conducted a cohort study."( Comparative safety of long-acting inhaled bronchodilators: a cohort study using the UK THIN primary care database.
Jara, M; Kesten, S; Lanes, SF; May, C; Wentworth, C, 2007)		0.34
"The aim of this review is to assess the risk of fatal and non-fatal serious adverse events in trials that randomised patients with chronic asthma to regular salmeterol versus placebo or regular short-acting beta(2)-agonists."( Regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Cates, MJ, 2008)		0.35
" Unpublished data on mortality and serious adverse events was sought."( Regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Cates, MJ, 2008)		0.35
" In 6 trials (2,766 patients), no serious adverse event data could be obtained."( Regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Cates, MJ, 2008)		0.35
"In comparison with placebo, we have found an increased risk of serious adverse events with regular salmeterol."( Regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Cates, MJ, 2008)		0.35
" This is a non-inferiority study where safety and efficacy outcomes were serially assessed, including adverse events, Baseline (BDI)/Transition Dyspnea Index (TDI), St."( A double-blind crossover study comparing the safety and efficacy of three weeks of Flu/Sal 250/50 bid plus albuterol 180 ug prn q4 hours to Flu/Sal 250/50 bid plus albuterol/Ipratropium bromide 2 puffs prn q4 hours in patients with chronic obstructive pul
Balkissoon, R; Make, B, 2008)		0.35
" Subgroup analysis suggests that children, patients receiving salmeterol, and a duration of treatment>12 weeks are associated with a higher risk of serious adverse effects; also there was a protective effect of concomitant use of ICS."( Safety of regular use of long-acting beta agonists as monotherapy or added to inhaled corticosteroids in asthma. A systematic review.
Castro-Rodriguez, JA; Marcos, LG; Moral, VP; Rodrigo, GJ, 2009)		0.35
" Nevertheless, in spite of the protective effect of the ICS, children and salmeterol use still show an increased risk of non-fatal serious adverse events."( Safety of regular use of long-acting beta agonists as monotherapy or added to inhaled corticosteroids in asthma. A systematic review.
Castro-Rodriguez, JA; Marcos, LG; Moral, VP; Rodrigo, GJ, 2009)		0.35
" The incidence of adverse events was low and similar between the two groups and events were of the type expected in this population."( Comparison of the clinical efficacy and safety of salmeterol/fluticasone propionate versus current care in the management of persistent asthma in Korea.
Chan, R; Jung, KS; Lee, YC; Park, SK; Shim, JJ; Uh, ST; Williams, AE, 2008)		0.35
" Whether this association represents adverse effects of beta -agonist use or is entirely due to disease severity is a matter of ongoing debate."( Safety of long-acting beta2-agonists in the treatment of asthma.
Cazzola, M; Matera, MG, 2007)		0.34
" The frequency of adverse events, COPD exacerbations, and use of short-acting bronchodilator agents were assessed throughout the study period."( Arformoterol and salmeterol in the treatment of chronic obstructive pulmonary disease: a one year evaluation of safety and tolerance.
Baumgartner, RA; Donohue, JF; Goodwin, E; Grogan, DR; Hanania, NA; Hanrahan, JP; Sciarappa, KA, 2008)		0.35
"Among treated subjects, the frequency of adverse events was similar for those taking arformoterol (90."( Arformoterol and salmeterol in the treatment of chronic obstructive pulmonary disease: a one year evaluation of safety and tolerance.
Baumgartner, RA; Donohue, JF; Goodwin, E; Grogan, DR; Hanania, NA; Hanrahan, JP; Sciarappa, KA, 2008)		0.35
"Increased BDNF concentrations may underly the adverse effects of salmeterol monotherapy on airway responsiveness in asthma."( Adverse effects of salmeterol in asthma: a neuronal perspective.
Bratke, K; Edner, A; Kuepper, M; Lindner, Y; Lommatzsch, M; Virchow, JC, 2009)		0.35
"The aim of this review is to assess the risk of fatal and non-fatal serious adverse events in trials that randomised patients with chronic asthma to regular salmeterol with inhaled corticosteroids versus the same dose of inhaled corticosteroids alone."( Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events.
Cates, CJ; Jaeschke, R; Lasserson, TJ, 2009)		0.35
" Unpublished data on mortality and serious adverse events were obtained from the sponsors, and from FDA submissions."( Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events.
Cates, CJ; Jaeschke, R; Lasserson, TJ, 2009)		0.35
" The overall risk of bias was low and data on serious adverse events were obtained from all studies."( Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events.
Cates, CJ; Jaeschke, R; Lasserson, TJ, 2009)		0.35
"No significant differences have been found in fatal or non-fatal serious adverse events in trials in which regular salmeterol has been randomly allocated with inhaled corticosteroids, in comparison to inhaled corticosteroids at the same dose."( Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events.
Cates, CJ; Jaeschke, R; Lasserson, TJ, 2009)		0.35
"An increase in serious adverse events with both regular formoterol and regular salmeterol in chronic asthma has been demonstrated in previous Cochrane reviews."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2009)		0.35
"We set out to compare the risks of mortality and non-fatal serious adverse events in trials which have randomised patients with chronic asthma to regular formoterol versus regular salmeterol."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2009)		0.35
" Unpublished data on mortality and serious adverse events were sought from the sponsors and authors."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2009)		0.35
" All studies were open label and recruited patients who were already taking inhaled corticosteroids for their asthma, and all studies contributed data on serious adverse events."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2009)		0.35
" Asthma-related serious adverse events were rare, and there were no reported asthma-related deaths."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2009)		0.35
"An increase in serious adverse events with both regular formoterol and regular salmeterol in chronic asthma has been demonstrated in comparison with placebo in previous Cochrane reviews."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2010)		0.36
"We set out to compare the risks of mortality and non-fatal serious adverse events in trials which have randomised patients with chronic asthma to regular formoterol versus regular salmeterol, when each are used with an inhaled corticosteroid as part of the randomised treatment."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2010)		0.36
" Unpublished data on mortality and serious adverse events were sought from the sponsors and authors."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2010)		0.36
" Asthma-related serious adverse events were rare, and there were no reported asthma-related deaths."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2010)		0.36
" Food and Drug Administration and featured in the labeling of drugs associated with serious adverse reactions."( FDA boxed warnings: how to prescribe drugs safely.
O'Connor, NR, 2010)		0.36
"an increase in serious adverse events with both regular formoterol and regular salmeterol in chronic asthma has been demonstrated in comparison with placebo in previous Cochrane reviews."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2010)		0.36
" Unpublished data on mortality and serious adverse events were sought from the sponsors and authors."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2010)		0.36
" Asthma-related serious adverse events were rare, and there were no reported asthma-related deaths."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2010)		0.36
" Adverse events (AEs) were analysed overall and according to Anti-Platelet Trialists' Collaboration (APTC) criteria and baseline cardiovascular risk factors."( Cardio- and cerebrovascular safety of indacaterol vs formoterol, salmeterol, tiotropium and placebo in COPD.
Chung, KF; Felser, JM; Hu, H; Rueegg, P; Worth, H, 2011)		0.37
" However, several studies have indicated an increased risk of asthma mortality and asthma-related serious adverse events and the FDA recently mandated restrictions to the use of LABAs in asthma."( Safe use of long-acting β-agonists: what have we learnt?
Sears, MR, 2011)		0.37
" Add-on therapy with LABA is effective and safe if the dose of ICS is adequate to treat airway inflammation."( Safe use of long-acting β-agonists: what have we learnt?
Sears, MR, 2011)		0.37
"An increase in serious adverse events with both regular formoterol and regular salmeterol in chronic asthma has been demonstrated in previous Cochrane reviews."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2012)		0.38
"We set out to compare the risks of mortality and non-fatal serious adverse events in trials which have randomised patients with chronic asthma to regular formoterol versus regular salmeterol."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2012)		0.38
" We sought unpublished data on mortality and serious adverse events from the sponsors and authors."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2012)		0.38
" All studies were open label and recruited patients who were already taking inhaled corticosteroids for their asthma, and all studies contributed data on serious adverse events."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2012)		0.38
" Asthma-related serious adverse events were rare and there were no reported asthma-related deaths."( Regular treatment with formoterol versus regular treatment with salmeterol for chronic asthma: serious adverse events.
Cates, CJ; Lasserson, TJ, 2012)		0.38
" Secondary endpoints included pulmonary function, plethysmography, pharmacokinetics of GSK233705 and salmeterol, adverse events (AEs), electrocardiograms (ECGs), vital signs, and laboratory parameters."( Safety and efficacy of dual therapy with GSK233705 and salmeterol versus monotherapy with salmeterol, tiotropium, or placebo in a crossover pilot study in partially reversible COPD patients.
Baggen, S; Beier, J; Brooks, J; Cahn, A; Deans, A; Maden, C; Mehta, R; van Noord, J, 2012)		0.38
" We extracted the data relating to children from each review and from new trials found in the updated searches (including risks of bias, study characteristics, serious adverse event outcomes, and control arm event rates)."( Safety of regular formoterol or salmeterol in children with asthma: an overview of Cochrane reviews.
Cates, CJ; Oleszczuk, M; Stovold, E; Wieland, LS, 2012)		0.38
" There are probably an additional three children per 1000 who suffer a non-fatal serious adverse event on combination therapy in comparison to ICS over three months."( Safety of regular formoterol or salmeterol in children with asthma: an overview of Cochrane reviews.
Cates, CJ; Oleszczuk, M; Stovold, E; Wieland, LS, 2012)		0.38
" We summarized data relating to exacerbations and adverse events, particularly events related to COPD."( The safety of long-acting β2-agonists in the treatment of stable chronic obstructive pulmonary disease.
Decramer, ML; Hanania, NA; Lötvall, JO; Yawn, BP, 2013)		0.39
"From 20 studies examined (8774 LABA-treated patients), there was no evidence of an association between LABA treatment and increased exacerbations, COPD-related adverse events, or deaths."( The safety of long-acting β2-agonists in the treatment of stable chronic obstructive pulmonary disease.
Decramer, ML; Hanania, NA; Lötvall, JO; Yawn, BP, 2013)		0.39
" Secondary outcome measures included quality of life as measured by the Paediatric Asthma Quality of Life Questionnaire with Standardised Activities [PAQLQ(S)] and the Paediatric Asthma Caregiver's Quality of Life Questionnaire (PACQLQ); time from randomisation to first exacerbation requiring treatment with a short course of oral corticosteroids; school attendance; hospital admissions; amount of rescue beta-2 agonist therapy prescribed; time from randomisation to treatment withdrawal (because of lack of efficacy or side effects); lung function at 48 weeks (as assessed by spirometry); cost-effectiveness; adverse events."( Management of Asthma in School age Children On Therapy (MASCOT): a randomised, double-blind, placebo-controlled, parallel study of efficacy and safety.
James, M; Lenney, W; McKay, AJ; Price, D; Tudur Smith, C; Williamson, PR, 2013)		0.39
" Adverse events were similar between the groups except for nervous system disorders, which were more frequently reported on fluticasone plus montelukast."( Management of Asthma in School age Children On Therapy (MASCOT): a randomised, double-blind, placebo-controlled, parallel study of efficacy and safety.
James, M; Lenney, W; McKay, AJ; Price, D; Tudur Smith, C; Williamson, PR, 2013)		0.39
"To assess the risk of mortality and non-fatal serious adverse events in trials which randomised patients with chronic asthma to regular salmeterol and inhaled corticosteroids in comparison to the same dose of inhaled corticosteroids."( Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events.
Cates, CJ; Ferrer, M; Jaeschke, R; Schmidt, S, 2013)		0.39
" We obtained unpublished data on mortality and serious adverse events from the sponsors, and from FDA submissions."( Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events.
Cates, CJ; Ferrer, M; Jaeschke, R; Schmidt, S, 2013)		0.39
" We judged that the overall risk of bias was low, and we obtained data on serious adverse events from all studies."( Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events.
Cates, CJ; Ferrer, M; Jaeschke, R; Schmidt, S, 2013)		0.39
"We found no statistically significant differences in fatal or non-fatal serious adverse events in trials in which regular salmeterol was randomly allocated with ICS, in comparison to ICS alone at the same dose."( Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events.
Cates, CJ; Ferrer, M; Jaeschke, R; Schmidt, S, 2013)		0.39
"Our findings suggest that BT is safe for 5 years after BT in patients with severe refractory asthma."( Safety of bronchial thermoplasty in patients with severe refractory asthma.
Armstrong, B; Chung, KF; Corris, PA; Cox, G; Laviolette, M; Niven, RM; Pavord, ID; Shargill, NS; Thomson, NC, 2013)		0.39
" Clinical trials record these safety outcomes as non-fatal and fatal serious adverse events (SAEs), respectively."( Safety of regular formoterol or salmeterol in adults with asthma: an overview of Cochrane reviews.
Cates, CJ; Kew, KM; Oleszczuk, M; Wieland, LS, 2014)		0.4
"To assess the risk of serious adverse events in adults with asthma treated with regular maintenance formoterol or salmeterol compared with placebo, or when randomly assigned in combination with regular ICS, compared with the same dose of ICS."( Safety of regular formoterol or salmeterol in adults with asthma: an overview of Cochrane reviews.
Cates, CJ; Kew, KM; Oleszczuk, M; Wieland, LS, 2014)		0.4
"Available evidence from the reviews of randomised trials cannot definitively rule out an increased risk of fatal serious adverse events when regular formoterol or salmeterol was added to an inhaled corticosteroid (as background or as randomly assigned treatment) in adults or adolescents with asthma."( Safety of regular formoterol or salmeterol in adults with asthma: an overview of Cochrane reviews.
Cates, CJ; Kew, KM; Oleszczuk, M; Wieland, LS, 2014)		0.4
" The profile of treatment-emergent adverse events judged as related to abediterol was consistent with that seen after adrenergic stimulation and occurred exclusively in patients who received abediterol 10 μg or 25 μg."( Abediterol (LAS100977), a novel long-acting β2-agonist: efficacy, safety and tolerability in persistent asthma.
Beier, J; de Miquel, G; Fuhr, R; Jiménez, E; Massana, E; Ruiz, S; Seoane, B, 2014)		0.4
" Long-acting β-2 agonists (LABAs) used in combination with inhaled corticosteroids (ICS) don't appear to increase all-cause mortality or serious adverse events in patients with persistent asthma compared with ICS alone."( HelpDesk answers: is it safe to add long-acting β-2 agonists to inhaled corticosteroids in patients with persistent asthma?
Madlon-Kay, DJ; Townsend, L, 2015)		0.42
" The incidence of treatment-emergent adverse events was similar between the tralokinumab and placebo groups."( Efficacy and safety of tralokinumab in patients with severe uncontrolled asthma: a randomised, double-blind, placebo-controlled, phase 2b trial.
Brightling, CE; Chanez, P; Korn, S; Leigh, R; May, RD; O'Byrne, PM; Piper, E; Ranade, K; She, D; Streicher, K, 2015)		0.42
" The fixed-effects model was used to evaluate the effects of LABAs on fatal cardiovascular adverse events."( Inhaled Long-Acting β2-Agonists Do Not Increase Fatal Cardiovascular Adverse Events in COPD: A Meta-Analysis.
Nie, X; Wang, H; Xia, N, 2015)		0.42
" All GP MDI doses were well tolerated with no evidence of a dose-related effect on adverse events."( Efficacy, safety, and dose response of glycopyrronium administered by metered dose inhaler using co-suspension delivery technology in subjects with intermittent or mild-to-moderate persistent asthma: A randomized controlled trial.
Darken, P; Dorinsky, P; Duncan, EA; Kerwin, E; Nyberg, J; Reisner, C; Sher, L; Siddiqui, S; Wachtel, A, 2018)		0.48
"  OBJECTIVES: To assess risks of mortality and non-fatal serious adverse events (SAEs) in trials that randomised participants with chronic asthma to regular salmeterol and ICS versus the same dose of ICS."( Inhaled steroids with and without regular salmeterol for asthma: serious adverse events.
Cates, CJ; Ferrer, M; Sayer, B; Schmidt, S; Waterson, S, 2018)		0.48
"Non-fatal serious adverse eventsA total of 332 adults receiving regular salmeterol with ICS experienced a non-fatal SAE of any cause, compared to 282 adults receiving regular ICS."( Inhaled steroids with and without regular salmeterol for asthma: serious adverse events.
Cates, CJ; Ferrer, M; Sayer, B; Schmidt, S; Waterson, S, 2018)		0.48
"We did not find a difference in the risk of death or serious adverse events in either adults or children."( Inhaled steroids with and without regular salmeterol for asthma: serious adverse events.
Cates, CJ; Ferrer, M; Sayer, B; Schmidt, S; Waterson, S, 2018)		0.48
" However, an increase in serious adverse events with the use of both regular formoterol and regular salmeterol (long-acting beta₂-agonists) compared with placebo for chronic asthma has been demonstrated in previous Cochrane Reviews."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; O'Shea, O; Stovold, E, 2021)		0.62
"To assess risks of mortality and non-fatal serious adverse events in trials that have randomised patients with chronic asthma to regular formoterol and an inhaled corticosteroid versus regular salmeterol and an inhaled corticosteroid."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; O'Shea, O; Stovold, E, 2021)		0.62
" We sought unpublished data on mortality and serious adverse events from study sponsors and authors."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; O'Shea, O; Stovold, E, 2021)		0.62
" In all, 201 adults reported non-fatal serious adverse events."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; O'Shea, O; Stovold, E, 2021)		0.62
" Evidence on all-cause non-fatal serious adverse events indicates that there is probably little to no difference between formoterol/budesonide and salmeterol/fluticasone inhalers."( Regular treatment with formoterol and an inhaled corticosteroid versus regular treatment with salmeterol and an inhaled corticosteroid for chronic asthma: serious adverse events.
Cates, CJ; O'Shea, O; Stovold, E, 2021)		0.62
" Secondary outcomes included risk of hospitalization, pulmonary function, asthma control level, quality of life, and adverse events (AEs)."( Efficacy and safety of salmeterol/fluticasone compared with montelukast alone (or add-on therapy to fluticasone) in the treatment of bronchial asthma in children and adolescents: a systematic review and meta-analysis.
Hong, JG; Lu, J; Qin, Z; Zhou, XJ, 2021)		0.62
" The primary safety outcome was a composite of serious adverse events (SAEs) and/or adverse events leading to discontinuation (DAEs); the primary effectiveness outcome was time-to-first exacerbation."( Safety and Effectiveness of As-Needed Formoterol in Asthma Patients Taking Inhaled Corticosteroid (ICS)-Formoterol or ICS-Salmeterol Maintenance Therapy.
Anderson, GP; Brusselle, G; Gustafson, P; Jorup, C; Lamarca, R; Reddel, HK, 2023)		0.91
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004)		0.32

Pharmacokinetics

ExcerptReferenceRelevance
"The safety, tolerability and systemic pharmacodynamic activity of the salmeterol/HFA134a inhaler, the current salmeterol inhaler, and placebo (HFA134a) were compared in 12 healthy volunteers in a double blind, randomised crossover study using a cumulative dosing design."( Salmeterol inhaler using a non-chlorinated propellant, HFA134a: systemic pharmacodynamic activity in healthy volunteers.
Kirby, SM; Smith, J; Ventresca, GP, 1995)		0.29
"In healthy volunteers the salmeterol/HFA134a inhaler is at least as safe and well tolerated as the current salmeterol inhaler, and has similar systemic pharmacodynamic activity."( Salmeterol inhaler using a non-chlorinated propellant, HFA134a: systemic pharmacodynamic activity in healthy volunteers.
Kirby, SM; Smith, J; Ventresca, GP, 1995)		0.29
"To investigate the potential for systemic pharmacodynamic and pharmacokinetic interactions between inhaled salmeterol and fluticasone propionate when repeat doses of the two drugs are given in combination to healthy subjects."( Salmeterol and fluticasone propionate given as a combination. Lack of systemic pharmacodynamic and pharmacokinetic interactions.
Daniel, MJ; Falcoz, C; Kirby, S; Milleri, S; Squassante, L; Ventresca, GP; Ziviani, L, )		0.13
" The systemic pharmacodynamic effects of inhaled salmeterol were not affected by the co-administration of fluticasone propionate."( Salmeterol and fluticasone propionate given as a combination. Lack of systemic pharmacodynamic and pharmacokinetic interactions.
Daniel, MJ; Falcoz, C; Kirby, S; Milleri, S; Squassante, L; Ventresca, GP; Ziviani, L, )		0.13
"These results in healthy subjects indicate that there is no systemic pharmacodynamic or pharmacokinetic interaction between inhaled salmeterol and fluticasone propionate when given in combination."( Salmeterol and fluticasone propionate given as a combination. Lack of systemic pharmacodynamic and pharmacokinetic interactions.
Daniel, MJ; Falcoz, C; Kirby, S; Milleri, S; Squassante, L; Ventresca, GP; Ziviani, L, )		0.13
"This was a randomised, double-blind, placebo-controlled, cross-over study comparing the systemic pharmacodynamic effects (heart rate and serum potassium) and pharmacokinetics of salmeterol delivered by the non-CFC hydrofluoralkane (HFA) propellant 134a and the CFC propellant (propellant 11/12) metered dose inhalers (MDI) in healthy subjects."( Comparison of the systemic pharmacodynamic effects and pharmacokinetics of salmeterol delivered by CFC propellant and non-CFC propellant metered dose inhalers in healthy subjects.
Daley-Yates, P; De Silva, M; Handel, M; Kempsford, R; Mehta, R, 2005)		0.33
" Pharmacokinetic results showed a greater initial absorption of salmeterol with DPI-C but greater continued absorption and a 40% greater AUC with DPI-A, which we attribute to slower but more extensive oral absorption because of the greater mass of swallowed large particles of salmeterol generated by DPI-A."( Comparative pulmonary function and pharmacokinetics of fluticasone propionate and salmeterol xinafoate delivered by two dry powder inhalers to patients with asthma.
Harrison, LI; Needham, MJ; Novak, CC; Ratner, P, 2011)		0.37
"Prediction of pharmacokinetic (PK) profile for inhaled drugs in humans provides valuable information to aid toxicology safety assessment, evaluate the potential for systemic accumulation on multiple dosing and enable an estimate for the clinical plasma assay requirements."( A new methodology for predicting human pharmacokinetics for inhaled drugs from oratracheal pharmacokinetic data in rats.
Harrison, A; Jones, RM, 2012)		0.38
" No clinically relevant systemic pharmacodynamic effects were observed."( Pharmacodynamics of GSK961081, a bi-functional molecule, in patients with COPD.
Ambery, C; Bateman, ED; Kornmann, O; Norris, V, 2013)		0.39
"Human pharmacokinetic studies of lung-targeted drugs are typically limited to measurements of systemic plasma concentrations, which provide no direct information on lung target-site concentrations."( Lung pharmacokinetics of inhaled and systemic drugs: A clinical evaluation.
Badorrek, P; Ellinghusen, BD; Eriksson, UG; Faulenbach, C; Fridén, M; Hohlfeld, JM; Holz, O; Lundqvist, AJ; Müller, M; Sadiq, MW; Stomilovic, S, 2021)		0.62
" Pharmacokinetic profiles were generated by combining data from multiple individuals, covering all sample timings."( Lung pharmacokinetics of inhaled and systemic drugs: A clinical evaluation.
Badorrek, P; Ellinghusen, BD; Eriksson, UG; Faulenbach, C; Fridén, M; Hohlfeld, JM; Holz, O; Lundqvist, AJ; Müller, M; Sadiq, MW; Stomilovic, S, 2021)		0.62
"Combining pharmacokinetic data derived from several individuals and techniques sampling different lung compartments enabled generation of pharmacokinetic profiles for evaluation of lung targeting after inhaled and oral drug delivery."( Lung pharmacokinetics of inhaled and systemic drugs: A clinical evaluation.
Badorrek, P; Ellinghusen, BD; Eriksson, UG; Faulenbach, C; Fridén, M; Hohlfeld, JM; Holz, O; Lundqvist, AJ; Müller, M; Sadiq, MW; Stomilovic, S, 2021)		0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
"Salmeterol (S) and montelukast (M) individually inhibit the obstructive consequences of thermal stimuli such as exercise and hyperventilation (HV), but there is no information on whether these drugs can interact positively."( Bronchoprotective effects of single doses of salmeterol combined with montelukast in thermally induced bronchospasm.
Coreno, A; El-Ekiaby, A; McFadden, ER; Skowronski, M; West, E, 2005)		0.33
" Whether inhaled corticosteroids by themselves or in combination with a long-acting beta2-adrenoceptor agonist repress systemic inflammation in chronic obstructive pulmonary disease is unknown."( Can inhaled fluticasone alone or in combination with salmeterol reduce systemic inflammation in chronic obstructive pulmonary disease? Study protocol for a randomized controlled trial [NCT00120978].
Cowie, RL; FitzGerald, M; Ford, G; Mainra, RR; Man, SF; Marciniuk, DD; Melenka, LS; Ramesh, W; Rousseau, R; Sin, DD; Wilde, E; Williams, D; Wong, E; York, E, 2006)		0.33
"If inhaled corticosteroids by themselves or in combination with a long-acting beta2-adrenoceptor agonist could repress systemic inflammation, they might greatly improve clinical prognosis by reducing various complications in chronic obstructive pulmonary disease."( Can inhaled fluticasone alone or in combination with salmeterol reduce systemic inflammation in chronic obstructive pulmonary disease? Study protocol for a randomized controlled trial [NCT00120978].
Cowie, RL; FitzGerald, M; Ford, G; Mainra, RR; Man, SF; Marciniuk, DD; Melenka, LS; Ramesh, W; Rousseau, R; Sin, DD; Wilde, E; Williams, D; Wong, E; York, E, 2006)		0.33
" We examined the effect of inhaled salmeterol, alone and in combination with fluticasone propionate, on the management of patients with COPD."( The effect of inhaled salmeterol, alone and in combination with fluticasone propionate, on management of COPD patients.
Boskabady, M; Boskabady, MH; Mansori, F; Nemat Khorasani, A, 2010)		0.36
" Two LABAs (salmeterol and formoterol) are currently licensed for COPD both as monotherapy and in combination with ICS (fluticasone propionate (FP) and budesonide respectively)."( The use of long acting β₂-agonists, alone or in combination with inhaled corticosteroids, in chronic obstructive pulmonary disease (COPD): a risk-benefit analysis.
Cave, AC; Hurst, MM, 2011)		0.37
" The GLISTEN trial compared the efficacy of two long-acting anti-muscarinic antagonists (LAMA), when combined with an inhaled corticosteroid (ICS) and a long-acting β2 agonist (LABA)."( Glycopyrronium once-daily significantly improves lung function and health status when combined with salmeterol/fluticasone in patients with COPD: the GLISTEN study, a randomised controlled trial.
Bremner, P; Chang, CL; Day, P; Frenzel, C; Frith, PA; Kurstjens, N; Ratnavadivel, R; Thompson, PJ, 2015)		0.42
"This randomised, blinded, placebo-controlled trial in moderate/severe COPD patients compared once-daily glycopyrronium (GLY) 50 µg, once-daily tiotropium (TIO) 18 µg or placebo (PLA), when combined with salmeterol/fluticasone propionate (SAL/FP) 50/500 µg twice daily."( Glycopyrronium once-daily significantly improves lung function and health status when combined with salmeterol/fluticasone in patients with COPD: the GLISTEN study, a randomised controlled trial.
Bremner, P; Chang, CL; Day, P; Frenzel, C; Frith, PA; Kurstjens, N; Ratnavadivel, R; Thompson, PJ, 2015)		0.42
"MSC combined with budesonide, almeterol and azithromycin has been confirmed to be generally safe and can reduce the dose of glucocorticoid in treatment of BOS after HSCT."( [Mesenchymal Stem Cells Combined with Budesonide, Almeterol and Azithromycin for the Treatment of Bronchiolitis Obliterans Syndrome after Hematopoietic Stem Cell Transplantation].
Cao, XP; Ding, L; Guo, ZK; Han, DM; Liu, J; Wang, HX; Wang, ZD; Xue, M; Yan, HM; Zheng, XL; Zhu, L, 2016)		0.43
"To systematically review the efficacy and safety of Liujunzi Decoction combined with Western medicine in the treatment of stable chronic obstructive pulmonary disease(COPD)."( [Systematic review and Meta-analysis on efficacy and safety of Liujunzi Decoction combined with Western medicine for stable chronic obstructive pulmonary disease].
Chang-Zheng, F; Mao-Rong, F; Ning, W; Qing, C; Qing, M; Qiu-Xiao, MA; Xing, L; Ya-Ni, H; Yi-Ling, F, 2020)		0.56
"To observe the clinical efficacy of self-made Lifei Dingchuan decoction combined with western medicine in the treatment of cough variant asthma (phlegm-heat accumulation in the lung syndrome)."( Study on the Effect of Self-Made Lifei Dingchuan Decoction Combined with Western Medicine on Cough Variant Asthma.
Huang, Z; Jian, X; Li, J; Li, K; Liang, B, 2022)		0.72

Bioavailability

ExcerptReferenceRelevance
" In dogs, Cmax was higher and reflected the greater oral bioavailability in this species."( Disposition of salmeterol xinafoate in laboratory animals and humans.
Barrow, A; Colthup, PV; Kulkarni, S; Maconochie, JG; Manchee, GR; Oxford, J; Palmer, E; Tarbit, MH, )		0.13
" The systemic effects of salbutamol are limited by its fairly high first-pass metabolism, but the oral bioavailability of salmeterol is unknown."( The contribution of the swallowed fraction of an inhaled dose of salmeterol to it systemic effects.
Bennett, JA; Harrison, TW; Tattersfield, AE, 1999)		0.3
" Furthermore, 29b was found to have low oral bioavailability in rat and dog and also to have long duration of action in an in vivo model of bronchodilation."( Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Barrett, VJ; Bevan, NJ; Biggadike, K; Butchers, PR; Coe, DM; Conroy, R; Edney, DD; Field, RN; Ford, AJ; Guntrip, SB; Looker, BE; McLay, IM; Monteith, MJ; Morrison, VS; Mutch, PJ; Procopiou, PA; Richards, SA; Sasse, R; Smith, CE, 2009)		0.35
" The relative bioavailability to the lung of inhaled fluticasone and salmeterol combination is primarily dependent on respirable dose delivery and can be reliably quantified using adrenal suppression and early fall in serum potassium (marker of systemic beta-2 adrenoreceptor response) as surrogate markers for delivered lung dose."( A novel breath-actuated integrated vortex spacer device increases relative lung bioavailability of fluticasone/salmeterol in combination.
Clearie, K; Lipworth, BJ; McFarlane, L; Meldrum, K; Menzies, D; Nair, A, 2009)		0.35
"To compare the in vivo relative bioavailability to the lung of Hydrofluoroalkane(HFA) Seretide delivered via Synchro-Breathe (SB); an optimally prepared 750 ml large volume plastic spacer, Volumatic (VM); and conventional Evohaler pMDI (EH)."( A novel breath-actuated integrated vortex spacer device increases relative lung bioavailability of fluticasone/salmeterol in combination.
Clearie, K; Lipworth, BJ; McFarlane, L; Meldrum, K; Menzies, D; Nair, A, 2009)		0.35
"The breath-actuated Synchro-Breathe device was comparable to an optimally prepared Volumatic spacer, and resulted in commensurate improvement in relative lung bioavailability for both fluticasone and salmeterol moieties compared to pMDI."( A novel breath-actuated integrated vortex spacer device increases relative lung bioavailability of fluticasone/salmeterol in combination.
Clearie, K; Lipworth, BJ; McFarlane, L; Meldrum, K; Menzies, D; Nair, A, 2009)		0.35
" Compound 13f had high potency, selectivity, fast onset, and long duration of action in vitro and was found to have long duration in vivo, low oral bioavailability in the rat, and to be rapidly metabolized."( Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
Barrett, VJ; Bevan, NJ; Biggadike, K; Box, PC; Butchers, PR; Coe, DM; Conroy, R; Emmons, A; Ford, AJ; Holmes, DS; Horsley, H; Kerr, F; Li-Kwai-Cheung, AM; Looker, BE; Mann, IS; McLay, IM; Morrison, VS; Mutch, PJ; Procopiou, PA; Smith, CE; Tomlin, P, 2010)		0.36
" It had lower oral absorption and bioavailability than salmeterol in both rat and dog."( The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
Barrett, VJ; Ford, AJ; Looker, BE; Lunniss, GE; Needham, D; Procopiou, PA; Smith, CE; Somers, G, 2011)		0.37
" Administering as a dry powder formulation slowed the rat lung absorption rate of the least soluble compound (fluticasone propionate), impacting the prediction of C(max) and MRT."( A new methodology for predicting human pharmacokinetics for inhaled drugs from oratracheal pharmacokinetic data in rats.
Harrison, A; Jones, RM, 2012)		0.38
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
" An optimal pharmacokinetic profile of low oral bioavailability was combined with a strong pharmacology profile when assessed using a guinea pig trachea tissue model."( The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists.
Brown, AD; Bunnage, ME; Glossop, PA; James, K; Jones, R; Lane, CA; Lewthwaite, RA; Mantell, S; Perros-Huguet, C; Price, DA; Trevethick, M; Webster, R, 2008)		0.35
" Furthermore, 29b was found to have low oral bioavailability in rat and dog and also to have long duration of action in an in vivo model of bronchodilation."( Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Barrett, VJ; Bevan, NJ; Biggadike, K; Butchers, PR; Coe, DM; Conroy, R; Edney, DD; Field, RN; Ford, AJ; Guntrip, SB; Looker, BE; McLay, IM; Monteith, MJ; Morrison, VS; Mutch, PJ; Procopiou, PA; Richards, SA; Sasse, R; Smith, CE, 2009)		0.35
" Compound 13f had high potency, selectivity, fast onset, and long duration of action in vitro and was found to have long duration in vivo, low oral bioavailability in the rat, and to be rapidly metabolized."( Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
Barrett, VJ; Bevan, NJ; Biggadike, K; Box, PC; Butchers, PR; Coe, DM; Conroy, R; Emmons, A; Ford, AJ; Holmes, DS; Horsley, H; Kerr, F; Li-Kwai-Cheung, AM; Looker, BE; Mann, IS; McLay, IM; Morrison, VS; Mutch, PJ; Procopiou, PA; Smith, CE; Tomlin, P, 2010)		0.36
" It had lower oral absorption than salmeterol in rats, and lower bioavailability than salmeterol in vivo in both rats and dogs (2% and 5%, respectively)."( The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
Barrett, VJ; Bevan, NJ; Butchers, PR; Conroy, R; Emmons, A; Ford, AJ; Jeulin, S; Looker, BE; Lunniss, GE; Morrison, VS; Mutch, PJ; Perciaccante, R; Procopiou, PA; Ruston, M; Smith, CE; Somers, G, 2011)		0.37
" It had lower oral absorption and bioavailability than salmeterol in both rat and dog."( The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
Barrett, VJ; Ford, AJ; Looker, BE; Lunniss, GE; Needham, D; Procopiou, PA; Smith, CE; Somers, G, 2011)		0.37
" It had lower than salmeterol oral absorption in rat, lower bioavailability in rat and dog, and a high turnover in human hepatocytes."( Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
Barrett, VJ; Biggadike, K; Butchers, PR; Craven, A; Ford, AJ; Guntrip, SB; Holmes, DS; Hughes, SC; Jones, AE; Looker, BE; Mutch, PJ; Needham, D; Procopiou, PA; Ruston, M; Smith, CE, 2014)		0.4
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

ExcerptRelevanceReference
" All changes were dosed related."( Dose-response study with high-dose inhaled salmeterol in healthy subjects.
Forster, JK; Maconochie, JG, 1992)		0.28
" Before salmeterol treatment was initiated and after 3, 6, 9 and 12 months of salmeterol treatment, a cumulative dose-response curve to inhaled salbutamol (100, 300 and 900 micrograms) was performed, and FEV1 measured."( Twelve months, treatment with inhaled salmeterol in asthmatic patients. Effects on beta 2-receptor function and inflammatory cells.
Lötvall, J; Lunde, H; Svedmyr, N; Törnqvist, H; Ullman, A, 1992)		0.28
"To study the dose-response relationship of salmeterol for protection against a naturally occurring stimulus, isocapnic hyperventilation tests of cold air were done in 16 asthmatic patients."( Salmeterol protects against hyperventilation-induced bronchoconstriction over 12 hours.
Jörres, R; Lüthke, M; Magnussen, H; Nowak, D; Rabe, KF; Wiessmann, J, 1992)		0.28
" Dose-response curves to inhaled SB were obtained the day before and the day after each treatment period."( Inhaled salmeterol and salbutamol in asthmatic patients. An evaluation of asthma symptoms and the possible development of tachyphylaxis.
Hedner, J; Svedmyr, N; Ullman, A, 1990)		0.28
" On the last day of each period a cumulative dose-response experiment with terbutaline in the doses 50, 100, 250 and 500 micrograms (cumulative dose 900 micrograms) was performed."( Influence of budesonide on the response to inhaled terbutaline in children with mild asthma.
Agertoft, L; Fuglsang, G; Pedersen, S; Vikre-Jørgensen, J, 1995)		0.29
" A histamine challenge test was done 12 h after the last dose of each treatment period, and dose-response curves to inhaled salbutamol (200-3200 micrograms) were constructed 36 h after the last dose."( Bronchodilator subsensitivity to salbutamol after twice daily salmeterol in asthmatic patients.
Grove, A; Lipworth, BJ, 1995)		0.29
"When testing the response to beta 2-agonist drugs in severe chronic obstructive pulmonary disease (COPD), a dose-response assessment should be undertaken."( Salmeterol and formoterol in partially reversible severe chronic obstructive pulmonary disease: a dose-response study.
Cazzola, M; D'Amato, G; Matera, MG; Rossi, F; Santangelo, G; Vinciguerra, A, 1995)		0.29
"The safety, tolerability and systemic pharmacodynamic activity of the salmeterol/HFA134a inhaler, the current salmeterol inhaler, and placebo (HFA134a) were compared in 12 healthy volunteers in a double blind, randomised crossover study using a cumulative dosing design."( Salmeterol inhaler using a non-chlorinated propellant, HFA134a: systemic pharmacodynamic activity in healthy volunteers.
Kirby, SM; Smith, J; Ventresca, GP, 1995)		0.29
" Maximum plasma concentrations attained at 1 h after dosing ranged between 35."( The determination in human plasma of 1-hydroxy-2-naphthoic acid following administration of salmeterol xinafoate.
Carey, PF; Chilton, AS; Godward, RE, 1995)		0.29
"01), but significant differences between salmeterol doses were no longer evident, despite an apparent dose-response effect."( A 1-week dose-ranging study of inhaled salmeterol in patients with asthma.
Bierman, CW; Bronsky, EA; Kemp, JP; Liddle, RF; Orgel, HA; Tinkelman, DG; van As, A, 1994)		0.29
" Salmeterol, 42 micrograms twice daily, is a safe and effective dosage for patients with mild-to-moderate asthma who are persistently symptomatic and require maintenance bronchodilator therapy."( A 1-week dose-ranging study of inhaled salmeterol in patients with asthma.
Bierman, CW; Bronsky, EA; Kemp, JP; Liddle, RF; Orgel, HA; Tinkelman, DG; van As, A, 1994)		0.29
" Subjects received cumulative doses of up to 400 micrograms (50 + 50 + 100 + 100 + 100 micrograms at 45 min intervals) inhaled salmeterol prior to a 13 day dosing schedule of twice-daily inhaled salmeterol 100 micrograms or placebo."( Does tachyphylaxis occur to the non-pulmonary effects of salmeterol?
Chilton, JE; Keene, ON; Maconochie, JG; Minton, NA, 1994)		0.29
"The purpose of the present study was to assess the degree of protection of inhaled salmeterol against exercise-induced bronchoconstriction (EIB) after chronic compared with single dosing in patients with asthma."( Reduced protection against exercise induced bronchoconstriction after chronic dosing with salmeterol.
Cree, IA; Dhillon, DP; Ingram, CG; Lipworth, BJ; Ramage, L, 1994)		0.29
" In addition, agents that can be dosed as needed (i."( Cost comparison of beta 2-agonist bronchodilators used in the treatment of asthma.
Nightingale, CH, )		0.13
" Hypothetically, twice daily dosing of salmeterol may result in continuous protection."( Airway responsiveness after a single dose of salmeterol and during four months of treatment in children with asthma.
Creyghton, FB; de Jongste, JC; Hop, WC; Kerrebijn, KF; van den Berg, M; van Rooij, RW; Verberne, AA, 1996)		0.29
" One hour after inhaling single doses of placebo, salmeterol 25 micrograms, or formoterol 12 micrograms, dose-response curves to repeated doses of inhaled fenoterol were constructed (cumulative doses of 100-3200 micrograms)."( Effects of prior treatment with salmeterol and formoterol on airway and systemic beta 2 responses to fenoterol.
Grove, A; Lipworth, BJ, 1996)		0.29
" There were no significant differences in the area under the dose-response curve for any of the parameters during the dose-response curve following treatment with salmeterol or formoterol compared with placebo."( Effects of prior treatment with salmeterol and formoterol on airway and systemic beta 2 responses to fenoterol.
Grove, A; Lipworth, BJ, 1996)		0.29
"Prior treatment with low doses of salmeterol or formoterol does not significantly alter bronchodilator dose-response curves to repeated doses of fenoterol in stable asthmatic patients."( Effects of prior treatment with salmeterol and formoterol on airway and systemic beta 2 responses to fenoterol.
Grove, A; Lipworth, BJ, 1996)		0.29
" The longer dosing intervals, which may enhance compliance, encourage its administration in patients with COPD."( A comparison of the bronchodilating effects of salmeterol, salbutamol and ipratropium bromide in patients with chronic obstructive pulmonary disease.
Calderaro, F; Caputi, M; Cazzola, M; Di Perna, F; Matera, MG; Rossi, F; Vinciguerra, A, 1995)		0.29
" Salmeterol and salbutamol produced the same maximal increase in sGAW and had the same area under the dose-response curves."( Airway effects of salmeterol in healthy individuals.
Bake, B; Bergendal, A; Johansson, A; Löfdahl, CG; Lötvall, J; Skoogh, BE, 1995)		0.29
"The aim of this study was to evaluate the effects of single and chronic dosing with salmeterol on exercise capacity and lung function in patients with chronic obstructive pulmonary disease."( Effects of regular salmeterol on lung function and exercise capacity in patients with chronic obstructive airways disease.
Dhillon, DP; Grove, A; Ingram, CG; Jenkins, RJ; Lipworth, BJ; Ramage, L; Reid, P; Smith, RP; Winter, JH, 1996)		0.29
" When selecting a 15-min pretreatment interval with equieffective anti-WFR doses from the first dose-response experiments (i."( Effects of local treatment with salmeterol and terbutaline on anti-IgE-induced wheal, flare, and late induration in human skin.
Grönneberg, R; Raud, J, 1996)		0.29
"This was a 1-week study evaluating the safety and efficacy of two dosage regimens of salmeterol in children with asthma."( A one-week dose-ranging study of inhaled salmeterol in children with asthma.
Bronsky, EA; Chervinsky, P; Howland, WC; Liddle, R; Nathan, RA; Pollard, SJ; Prenner, B; Stahl, E; Weinstein, S, 1997)		0.3
" The aim of this study was to determine the effects of regular treatment with the long-acting beta-agonist, salmeterol, on the methacholine dose-response curve (DRC) in mild-to-moderate asthmatics."( Effects of long-acting and short-acting beta-agonists on methacholine dose-response curves in asthmatics.
O'Shaughnessy, AD; Sears, MR; Walker, CM; Wong, AG, 1997)		0.3
"Short-term salmeterol use within the prescribed dosage was not shown to increase short-term power output in nonasthmatic cyclists."( The effects of salmeterol on power output in nonasthmatic athletes.
Fleck, SJ; McDowell, SL; Storms, WW, 1997)		0.3
"We conclude that a single 50-microg dose of salmeterol has an excellent protective effect against exercise-induced asthma for at least 9 hours, but that this effect may wane during regular once-daily salmeterol treatment, despite the reduced frequency of dosing and despite concomitant use of inhaled glucocorticoids."( Tolerance to the bronchoprotective effect of salmeterol in adolescents with exercise-induced asthma using concurrent inhaled glucocorticoid treatment.
Cheang, MS; Gerstner, TV; Simons, FE, 1997)		0.3
" For secondary end points salmeterol treatment was associated with higher morning and evening peak expiratory flow and forced expiratory volume in one second; a reduction in symptoms, bronchodilator use and airway responsiveness to methacholine; and no effect on serum potassium concentration, 24 hour heart rate, or the final forced expiratory volume in one second achieved during a salbutamol dose-response study."( Effect of long-term treatment with salmeterol on asthma control: a double blind, randomised crossover study.
Bennett, J; Clark, M; Cooper, S; Lewis, S; Oborne, J; Rushton, L; Tattersfield, AE; Thompson Coon, J; Wilding, P, 1997)		0.3
" Interactive mixtures of micronized Salmeterol Xinafoate adhered to irrespirable lactose monohydrate carrier particles were used as model dosage forms."( The development of a cascade impactor simulator based on adhesion force measurements to aid the development of dry powder inhalations.
Podczeck, F, 1997)		0.3
"A group of 20 patients with moderate bronchial asthma aged 18 through 65, previously treated with Becotide inhaler for 4 weeks was given Serevent in regular dosage for 4 weeks."( [Serevent in the treatment of moderate bronchial asthma].
Acasandri, E; Arghir, O; Filip, G; Floca, L; Mihai, D; Panghea, P; Voicu, G, )		0.13
"1 microM), both caused rightward shifts in the dose-response curve for the inhibition of histamine release by isoprenaline."( Salmeterol inhibition of mediator release from human lung mast cells by beta-adrenoceptor-dependent and independent mechanisms.
Chong, LK; Cooper, E; Peachell, PT; Vardey, CJ, 1998)		0.3
" Consistent in vitro fine particle dosing from the Diskus inhaler translates into a consistent clinical effect at low and high flow rates in children."( Clinical effect of Diskus dry-powder inhaler at low and high inspiratory flow-rates in asthmatic children.
Auk, IL; Bisgaard, H; Bojsen, K; Ifversen, M; Klug, B; Nielsen, KG, 1998)		0.3
"The aim of this study was to investigate whether regular treatment with inhaled salmeterol modifies the dose-response curve to the inhaled short-acting beta2-agonist terbutaline or affects the concentration of nitric oxide (NO) in exhaled air of children with asthma."( Effect of salmeterol treatment on nitric oxide level in exhaled air and dose-response to terbutaline in children with mild asthma.
Agertoft, L; Fuglsang, G; Pedersen, S; Vikre-Jørgensen, J, 1998)		0.3
"We examined whether a pretreatment with formoterol, oxitropium bromide, or salmeterol might modify the dose-response curves to inhaled salbutamol in patients with stable and partially reversible chronic obstructive pulmonary disease (COPD)."( Effects of formoterol, salmeterol or oxitropium bromide on airway responses to salbutamol in COPD.
Calderaro, F; Cazzola, M; Di Perna, F; Girbino, G; Matera, MG; Noschese, P; Vinciguerra, A, 1998)		0.3
" The number of rescue medication inhaled, side effects, heart rate, blood pressure, serum potassium dosage and electrocardiograms, did no show significative differences between the groups."( [Efficacy of and tolerance to salmeterol compared to salbutamol in patients with bronchial asthma].
De Oliveira, MA; Faresin, SM; Jardim, JR; Lucas, SR; Nery, LE, )		0.13
"This study showed that in mild to moderate asthmatic patients, salmeterol in the dosage of 100 mg/day raised the FEV1 and the morning PEF and led to pronounced decrease in the nocturnal symptoms as compared to salbutamol."( [Efficacy of and tolerance to salmeterol compared to salbutamol in patients with bronchial asthma].
De Oliveira, MA; Faresin, SM; Jardim, JR; Lucas, SR; Nery, LE, )		0.13
" HFA134a was rapidly absorbed after inhalation with dose-related blood concentrations which declined rapidly after dosing (t1/2 = 31 min)."( Clinical pharmacology of HFA134a.
Ventresca, GP, 1995)		0.29
" Patients on inhaled corticosteroids, cromolyn, and nedocromil were allowed into the study if their dosing remained constant throughout the study."( Salmeterol vs theophylline: sleep and efficacy outcomes in patients with nocturnal asthma.
Mende, CN; Petrocella, VJ; Rickard, KA; Wiegand, L; Yancey, SW; Zaidel, G; Zwillich, CW, 1999)		0.3
" Salmeterol, however, showed a flatter dose-response curve, and a significantly weaker maximal protective effect (2."( Comparison of the relative efficacy of formoterol and salmeterol in asthmatic patients.
Ibsen, T; Lötvall, J; Mellén, A; Palmqvist, M, 1999)		0.3
"Current evidence suggests that addition of the long-acting beta2-agonist salmeterol to an inhaled corticosteroid in patients with persistent asthma symptoms provides greater clinical benefit than doubling the dosage of the inhaled corticosteroid."( Salmeterol/fluticasone propionate combination.
Jarvis, B; Spencer, CM, 1999)		0.3
" Each agent was given in recommended dosage on separate days in a double-blind, crossover format, and the patients' arterial blood gases (ABGs) were measured at baseline and at intervals to 120 min."( Effects of salmeterol on arterial blood gases in patients with stable chronic obstructive pulmonary disease. Comparison with albuterol and ipratropium.
Gross, NJ; Khoukaz, G, 1999)		0.3
" Exercise challenge was repeated at day 3, week 4, and week 8 after randomization near the end of the dosing interval for both drugs."( Montelukast versus salmeterol in patients with asthma and exercise-induced bronchoconstriction. Montelukast/Salmeterol Exercise Study Group.
Chuchalin, AG; Gunawardena, KA; Helbling, A; Jasan, J; Langley, SJ; Laurenzi, M; Lee, TH; Leff, JA; Menten, J; O'Neill, SJ; Suskovic, S; van Noord, JA; Villaran, C, 1999)		0.3
"There were no differences between regular treatment with formoterol and salmeterol in their effects on lymphocyte beta2-adrenoceptor regulation at the end of a 12-h dosing interval, with both drugs exhibiting a residual degree of bronchodilator activity at the same time point."( Comparative trough effects of formoterol and salmeterol on lymphocyte beta2-adrenoceptor--regulation and bronchodilatation.
Aziz, I; Lipworth, BJ; McFarlane, LC, 1999)		0.3
" Long-term administration of montelukast provided consistent inhibition of exercise-induced bronchoconstriction at the end of the 8-week dosing interval without tolerance."( Oral montelukast compared with inhaled salmeterol to prevent exercise-induced bronchoconstriction. A randomized, double-blind trial. Exercise Study Group.
Bronsky, EA; DeLucca, PT; Edelman, JM; Ghannam, AF; Gormley, GJ; Grossman, J; Kemp, JP; Pearlman, DS; Turpin, JA, 2000)		0.31
" Ratios of PCwheeze between treatment and placebo challenges were calculated for each dosage group."( The bronchoprotective effect of inhaled salmeterol in preschool children: a dose-ranging study.
Brown, R; Efthimiou, J; Kurian, M; Primhak, RA; Smith, CM; Wach, R; Yong, SC, 1999)		0.3
" In contrast to benzalkonium chloride, the dose-response curves for secretostatic and celltoxic effects of salmeterol markedly overlapped."( Influence of salmeterol and benzalkonium chloride on G-protein-mediated exocytotic responses of rat peritoneal mast cells.
Krebs, D; Seebeck, J; Ziegler, A, 2000)		0.31
" Mean maximum (or minimum) absolute values were used to construct dose-response curves to calculate the relative dose potency of the two drugs."( Systemic effects of formoterol and salmeterol: a dose-response comparison in healthy subjects.
Bennett, J; Cooper, S; Guhan, AR; Lewis, S; Oborne, J; Tattersfield, AE, 2000)		0.31
"Our results showed no difference between formoterol and salmeterol in the degree of functional antagonism against methacholine-induced bronchoconstriction at the end of a 12-h dosing interval in patients who expressed the homozygous glycine-16 genotype."( Functional antagonism with formoterol and salmeterol in asthmatic patients expressing the homozygous glycine-16 beta(2)-adrenoceptor polymorphism.
Aziz, I; Dempsey, OJ; Lipworth, BJ, 2000)		0.31
"Homozygous Arg-16 patients are susceptible to clinically important increases in asthma exacerbations during chronic dosing with the short acting beta(2) agonist salbutamol."( Asthma exacerbations during long term beta agonist use: influence of beta(2) adrenoceptor polymorphism.
Drazen, JM; Hancox, RJ; Herbison, GP; Taylor, DR; Town, GI; Yandava, CN, 2000)		0.31
" At each visit, a dose-response curve to inhaled salbutamol was constructed using a total cumulative dose of 800 microg."( Additive effects of salmeterol and fluticasone or theophylline in COPD.
Calderaro, F; Cazzola, M; Centanni, S; Di Lorenzo, G; Di Perna, F; Testi, R, 2000)		0.31
" This dosage is also as effective when added to low-dosage inhaled corticosteroid therapy as doubling of corticosteroid dosages."( Zafirlukast: an update of its pharmacology and therapeutic efficacy in asthma.
Dunn, CJ; Goa, KL, 2001)		0.31
" Dosing continued on the evening of day 10 and on day 11, and on day 12 the effect of repeat-dose treatment with salmeterol and salmeterol/fluticasone propionate on the systemic effects of cumulative doses of inhaled salbutamol (up to a total dosage of 3,200 microg) was evaluated."( Salmeterol and fluticasone propionate given as a combination. Lack of systemic pharmacodynamic and pharmacokinetic interactions.
Daniel, MJ; Falcoz, C; Kirby, S; Milleri, S; Squassante, L; Ventresca, GP; Ziviani, L, )		0.13
" For fluticasone propionate, there were no statistically significant differences between salmeterol/fluticasone propionate and fluticasone propionate with respect to Cmax, plasma concentration at the end of the dosing interval (Ct), terminal elimination half-life (t1/2) or time to Cmax (tmax)."( Salmeterol and fluticasone propionate given as a combination. Lack of systemic pharmacodynamic and pharmacokinetic interactions.
Daniel, MJ; Falcoz, C; Kirby, S; Milleri, S; Squassante, L; Ventresca, GP; Ziviani, L, )		0.13
" The long duration of action of salmeterol offers the advantage of twice daily dosing compared with the required four times a day dosing with ipratropium."( Use of a long-acting inhaled beta2-adrenergic agonist, salmeterol xinafoate, in patients with chronic obstructive pulmonary disease.
Anderson, W; Bailey, W; Broughton, J; Friedman, M; Rennard, SI; Rickard, K; Wisniewski, M; ZuWallack, R, 2001)		0.31
" The primary end point was mean morning peak expiratory flow (PEF) measured 5 minutes after dosing and entered in a patient diary each day during the first 4 weeks of treatment."( Comparison of the efficacy of formoterol and salmeterol in patients with reversible obstructive airway disease: a multicenter, randomized, open-label trial.
Condemi, JJ, 2001)		0.31
" These results indicate that the difference in FPM does not warrant a change in the recommended dosage of salmeterol administered when using the VHCs tested."( Evaluation of particle size distribution of salmeterol administered via metered-dose inhaler with and without valved holding chambers.
Ahrens, RC; Garris, T; Holmes, M; Kelly, HW; Reisner, C; Stevens, AL; Vandermeer, AK, 2001)		0.31
" Unfortunately the most effective dosage of beta2-agonists may increase above that recommended during acute exacerbations."( Acute effects of higher than customary doses of salmeterol and salbutamol in patients with acute exacerbation of COPD.
Califano, C; Cazzola, M; D'Amato, G; D'Amato, M; Di Perna, F; Marsico, SA; Matera, MG; Terzano, C, 2002)		0.31
" Significant benefit was gained from adding salmeterol in a group of patients who appeared to have been at the top of their steroid dose-response curve receiving FP250."( Addition of salmeterol to fluticasone propionate treatment in moderate-to-severe asthma.
Browning, D; Colman, NC; Dal Negro, R; Fletcher, CP; Ind, PW; James, MH, 2003)		0.32
"To determine the magnitude of residual bronchoprotection after chronic dosing with long-acting beta(2)-agonists."( Airway-stabilizing effect of long-acting beta2-agonists as add-on therapy to inhaled corticosteroids.
Currie, GP; Jackson, CM; Lipworth, BJ; Ogston, SA, 2003)		0.32
" These findings suggest that ways need to be found: (i) to increase the use of current asthma management guidelines by practitioners; (ii) to improve documentation of prescribed medications and their dosage and; (iii) to improve education of parents in home management measures."( Prescribing for asthmatic children in primary care. Are we following guidelines?
Dashash, NA; Mukhtar, SH, 2003)		0.32
" Dose-response curves showed that Salm, at concentration >1."( Cytokine release and adhesion molecule expression by stimulated human bronchial epithelial cells are downregulated by salmeterol.
Di Blasi, P; Rossi, GA; Sabatini, F; Sale, R; Serpero, L; Silvestri, M, 2003)		0.32
"if patients with asthma remain symptomatic in spite of chronic treatment with inhaled corticosteroids (ICS), increasing the ICS dosage or adding another drug to the treatment regimen are possible therapeutic alternatives."( Salmeterol/fluticasone propionate (50/250 microg) combination is superior to double dose fluticasone (500 microg) for the treatment of symptomatic moderate asthma.
Bergmann, KC; Braun, R; Lindemann, L; Steinkamp, G, 2004)		0.32
"5 microg) according to asthma severity compared with traditional fixed dosing (FD) regimens."( Adjustable maintenance dosing with budesonide/formoterol compared with fixed-dose salmeterol/fluticasone in moderate to severe asthma.
Aalbers, R; Backer, V; Jorup, C; Kava, TT; Omenaas, ER; Sandström, T; Welte, T, 2004)		0.32
"5, mean inhaled corticosteroids 735 microg/day, mean forced expiratory volume in 1 second [FEV(1)] 84% predicted) were randomised after 2 weeks' run-in to either: budesonide/formoterol adjustable maintenance dosing (AMD), budesonide/formoterol FD or salmeterol/fluticasone (Seretide Diskus dagger 50/250 microg) FD."( Adjustable maintenance dosing with budesonide/formoterol compared with fixed-dose salmeterol/fluticasone in moderate to severe asthma.
Aalbers, R; Backer, V; Jorup, C; Kava, TT; Omenaas, ER; Sandström, T; Welte, T, 2004)		0.32
"Adjustable maintenance dosing with budesonide/formoterol provides more effective asthma control by reducing exacerbations and reliever medication usage compared with fixed-dose salmeterol/fluticasone."( Adjustable maintenance dosing with budesonide/formoterol compared with fixed-dose salmeterol/fluticasone in moderate to severe asthma.
Aalbers, R; Backer, V; Jorup, C; Kava, TT; Omenaas, ER; Sandström, T; Welte, T, 2004)		0.32
" IC was recorded before dosing and at 5, 10, 15 and 30 min and 1, 2, 3 and 4 h post-dose."( Effects of formoterol and salmeterol on resting inspiratory capacity in COPD patients with poor FEV(1) reversibility.
Bouros, D; Della Cioppa, G; Kottakis, J; Le Gros, V; Overend, T; Siafakas, N, 2004)		0.32
"The earlier described faster onset-of-action of formoterol as compared to a equipotent dosage of salmeterol was confirmed in this study."( Profiles of measured and perceived bronchodilation. A placebo-controlled cross-over trial comparing formoterol and salmeterol in moderate persistent asthma.
Creemers, JP; Greefhorst, AP; Hoff, WJ; Schermer, TR; Sips, AP; van Herwaarden, CL; Westbroek, J, 2004)		0.32
" The once-a-day dosing and easy-to-use HandiHaler device should improve patient compliance."( Tiotropium: a new, long-acting agent for the management of COPD--a clinical review.
Crutchfield, D, 2004)		0.32
" Fixed dosing with budesonide/formoterol or salmeterol/fluticasone provides effective asthma control in line with guideline goals."( Combination therapy in asthma--fixed or variable dosing in different patients?
Lötvall, J, 2004)		0.32
" In most SFC patients the fluticasone dosage can be reduced by 50 % without losing asthma control."( [Asthma control with the salmeterol-fluticasone-combination disc compared to standard treatment].
Liefring, E; Molitor, S; Trautmann, M, 2005)		0.33
"Greater clinical benefit in controlling the symptoms of asthma is frequently observed through combining moderate doses of inhaled glucocorticoids together with long-acting beta(2)-agonists, as compared with increasing glucocorticoid dosage alone."( Interleukin-10-secreting "regulatory" T cells induced by glucocorticoids and beta2-agonists.
Corrigan, CJ; Faith, A; Hawrylowicz, CM; Lavender, P; Lee, TH; Peek, EJ; Richards, DF, 2005)		0.33
" Drug use in the 6 months before and after step-up in treatment from inhaled corticosteroids [ICs; total daily dosage of < or =1000 microg beclomethasone dipropionate (BDP) or equivalent] to either salmeterol/fluticasone propionate combination (SFC) or concurrent BDP and long-acting beta(2)-agonists (LABAs) given in separate inhalers was compared."( Short-acting beta 2-agonist and oral corticosteroid use in asthma patients prescribed either concurrent beclomethasone and long-acting beta 2-agonist or salmeterol/fluticasone propionate combination.
Angus, R; Cheesbrough, A; Reagon, R, 2005)		0.33
" The addition of a low-dose long-acting beta(2) agonist is superior to the simple increase of the dosage of inhaled corticosteroids."( [Evaluation of the clinical efficacy and the safety of salmeterol/fluticasone propionate accuhaler compared to budesonide turbuhalar in the control of adult asthma].
Cai, BQ; Chen, BY; Chen, XD; Feng, YL; Guo, XJ; Kang, J; Li, Q; Lin, YP; Qiu, C; Shen, HH; Sun, TY; Tao, JJ; Wang, DQ; Xiao, BR; Xie, CM; Xu, YP; Yin, KS; Zhang, DP; Zheng, JP; Zhong, NS; Zhou, JY; Zhou, X, 2005)		0.33
"A patient-driven, adjustable maintenance dosing (AMD) approach to asthma therapy, in which the dose is adjusted by patients according to the severity of their symptoms, has recently been compared with fixed-dose therapy in open-label studies."( The CONCEPT trial: a 1-year, multicenter, randomized,double-blind, double-dummy comparison of a stable dosing regimen of salmeterol/fluticasone propionate with an adjustable maintenance dosing regimen of formoterol/budesonide in adults with persistent ast
Boulet, LP; FitzGerald, JM; Follows, RM, 2005)		0.33
"This study used a double-blind, double-dummy design to compare the efficacy of 2 treatment approaches: stable dosing of salmeterol/fluticasone propionate (SAL/FP) and AMD of formoterol/budesonide (FOR/BUD)."( The CONCEPT trial: a 1-year, multicenter, randomized,double-blind, double-dummy comparison of a stable dosing regimen of salmeterol/fluticasone propionate with an adjustable maintenance dosing regimen of formoterol/budesonide in adults with persistent ast
Boulet, LP; FitzGerald, JM; Follows, RM, 2005)		0.33
" After 4 weeks of stable dosing in both groups, eligible patients continued the study for an additional 48 weeks, receiving either a stable dose of SAL/FP or AMD of FOR/BUD."( The CONCEPT trial: a 1-year, multicenter, randomized,double-blind, double-dummy comparison of a stable dosing regimen of salmeterol/fluticasone propionate with an adjustable maintenance dosing regimen of formoterol/budesonide in adults with persistent ast
Boulet, LP; FitzGerald, JM; Follows, RM, 2005)		0.33
" Over weeks 1 through 52, patients receiving stable dosing of SAL/FP had a significantly greater percentage of symptom-free days compared with those receiving AMD of FOR/BUD (median, 58."( The CONCEPT trial: a 1-year, multicenter, randomized,double-blind, double-dummy comparison of a stable dosing regimen of salmeterol/fluticasone propionate with an adjustable maintenance dosing regimen of formoterol/budesonide in adults with persistent ast
Boulet, LP; FitzGerald, JM; Follows, RM, 2005)		0.33
"In this adult population with persistent asthma, stable dosing of SAL/FP 50/250 microg BID resulted in significantly greater increases in symptom-free days, days free of rescue medication, and morning PEE, as well as almost halving the exacerbation rate, compared with AMD of FOR/BUD 6/200 microg."( The CONCEPT trial: a 1-year, multicenter, randomized,double-blind, double-dummy comparison of a stable dosing regimen of salmeterol/fluticasone propionate with an adjustable maintenance dosing regimen of formoterol/budesonide in adults with persistent ast
Boulet, LP; FitzGerald, JM; Follows, RM, 2005)		0.33
" Dose-response curves were constructed based on skeletal and cardiac muscle hypertrophy."( Systemic administration of beta2-adrenoceptor agonists, formoterol and salmeterol, elicit skeletal muscle hypertrophy in rats at micromolar doses.
Lynch, GS; Ryall, JG; Sillence, MN, 2006)		0.33
"Response to salmeterol does not vary between ADRB2 genotypes after chronic dosing with an inhaled corticosteroid."( Salmeterol response is not affected by beta2-adrenergic receptor genotype in subjects with persistent asthma.
Anderson, WH; Baitinger, LA; Bleecker, ER; Dorinsky, PM; Edwards, LD; Klotsman, M; Yancey, SW, 2006)		0.33
"We conducted a double blind, randomised, placebo-controlled, crossover study evaluating the effects of halving inhaled steroid dosage plus salmeterol, or salmeterol and tiotropium."( A proof of concept study to evaluate stepping down the dose of fluticasone in combination with salmeterol and tiotropium in severe persistent asthma.
Fardon, T; Haggart, K; Lee, DK; Lipworth, BJ, 2007)		0.34
" The aims of this study were to evaluate the long-term efficacy (including symptom-free days and exacerbations) and impact on HRQoL of a stable-dose regimen of salmeterol/fluticasone propionate (SAL/FP) and an adjustable maintenance dosing (AMD) regimen of formoterol/budesonide (FOR/BUD) where treatment is adjusted based on symptoms [SAM40056]."( Salmeterol/fluticasone stable-dose treatment compared with formoterol/budesonide adjustable maintenance dosing: impact on health-related quality of life.
Price, DB; Williams, AE; Yoxall, S, 2007)		0.34
"Transdermal beta 2-agonist tulobuterol showed an improvement in FEV1, FVC and IC after dosing compared with those at baseline."( Comparison of bronchodilatory properties of transdermal and inhaled long-acting beta 2-agonists.
Akamatsu, K; Hirano, T; Ichikawa, T; Ichinose, M; Matsunaga, K; Minakata, Y; Nakanishi, M; Sugiura, H; Ueshima, K; Yamagata, T; Yanagisawa, S, 2008)		0.35
" For patients in group A, a fixed dosage was maintained for 18 months, while those in group B received tailored dosage or withdrawal of therapy according to the clinical control level (well or total control)."( [A clinical study on the significance of airway hyperresponsiveness monitoring in the adjustment of combined therapy for asthmatic patients].
Liu, CT; Pang, YM; Tan, CW; Wang, G; Wang, YM, 2007)		0.34
" The two FSC treatments were similar except that QD dosing did not maintain improvements in lung function for 24h compared with twice daily dosing."( Efficacy and safety of fluticasone propionate/salmeterol 250/50 mcg Diskus administered once daily.
Dorinsky, PM; Kerwin, EM; Meltzer, EO; Nathan, RA; Ortega, HG; Schoaf, L; Yancey, SW, 2008)		0.35
" Traditional press-and-breathe Metered Dose Inhalers (pMDIs) have recently improved their ecological appeal, can be used in every clinical and environmental situation, their dosing is convenient and highly reproducible, but their efficient delivery remains highly technique dependent."( Inhalatory therapy training: a priority challenge for the physician.
Melani, AS, 2007)		0.34
"It is concluded that four puffs of salmeterol delivered with an MDI and a spacer device induces significant bronchodilation in mechanically ventilated patients with COPD exacerbation, the duration of which is highly variable, precluding definite conclusions in regard to optimum dosing schedules."( Duration of salmeterol-induced bronchodilation in mechanically ventilated chronic obstructive pulmonary disease patients: a prospective clinical study.
Gavriilidis, G; Georgopoulos, D; Linardakis, M; Malliotakis, P, 2008)		0.35
"In subjects with persistent asthma, the ADRB2 Arg16Gly polymorphism does not alter lung function responses to SAL or FSC over the 12 hour dosing interval following acute and chronic dosing."( Acute and chronic lung function responses to salmeterol and salmeterol plus fluticasone propionate in relation to Arg16Gly beta(2)-adrenergic polymorphisms.
Anderson, WH; Edwards, LD; Klotsman, M; Ortega, HG; Yancey, SW, 2009)		0.35
"Chronic dosing with fluticasone propionate/salmeterol in a single device provides superior protection compared with an inhaled corticosteroid alone in protecting against exercise-induced asthma in children with persistent asthma."( Fluticasone propionate/salmeterol and exercise-induced asthma in children with persistent asthma.
Matz, J; Ortega, HG; Pearlman, D; Qaqundah, P; Stempel, DA; Yancey, SW, 2009)		0.35
" Two recently completed trials have demonstrated that with respect to asthma control the combination of inhaled steroid (400 - 800 microg/d) plus theophylline is at least as effective as doubling the dose of inhaled steroid in patients who remain symptomatic on a dosage of 400 - 800 microg daily."( [Asthma therapy: combination of topical glucocorticosteroids and theophylline].
Ukena, D, 1997)		0.3
" The CIC showed the least serum cortisol suppression of the tested dosing regimens."( Population pharmacokinetics and pharmacodynamics of inhaled ciclesonide and fluticasone propionate in patients with persistent asthma.
Derendorf, H; Derom, E; Lahu, G; Nave, R; Xu, J, 2010)		0.36
" dosing schedule, formulation, etc."( Adherence to controller therapy for chronic obstructive pulmonary disease: a review.
Blanchette, CM; Charles, MS; Dalal, AA; Lavallee, D; Mapel, D; Silver, H, 2010)		0.36
" Under-treatment with ICS and differential dosing of ICS in many trials are major factors driving the LABA safety concern."( Safe use of long-acting β-agonists: what have we learnt?
Sears, MR, 2011)		0.37
" Determination of the significance of the observed differences in pharmacokinetics from this single-dose study requires further exploration in studies using clinically relevant dosing regimens."( Comparative pulmonary function and pharmacokinetics of fluticasone propionate and salmeterol xinafoate delivered by two dry powder inhalers to patients with asthma.
Harrison, LI; Needham, MJ; Novak, CC; Ratner, P, 2011)		0.37
" The limitations of the analysis are that the results from a single study, TORCH, have a large bearing on the overall findings of the analysis, and that there is heterogeneity in the length and the dosing of the included studies, although it does not appear that heterogeneity affected the reported results."( Budesonide/formoterol vs. salmeterol/fluticasone in COPD: a systematic review and adjusted indirect comparison of pneumonia in randomised controlled trials.
Edwards, SJ; Gray, J; Halpin, DM; Morais, J; Singh, D, 2011)		0.37
"Prediction of pharmacokinetic (PK) profile for inhaled drugs in humans provides valuable information to aid toxicology safety assessment, evaluate the potential for systemic accumulation on multiple dosing and enable an estimate for the clinical plasma assay requirements."( A new methodology for predicting human pharmacokinetics for inhaled drugs from oratracheal pharmacokinetic data in rats.
Harrison, A; Jones, RM, 2012)		0.38
"For the primary outcome there was significant protection after single and long-term dosing with fluticasone alone and fluticasone-salmeterol combination, whereas salmeterol alone only afforded protection after the first dose."( Effects of intranasal salmeterol and fluticasone given alone and in combination in persistent allergic rhinitis.
Burns, P; Lipworth, BJ; Nair, A; Short, P, 2012)		0.38
"Chronic dosing with fluticasone but not salmeterol confers anti-inflammatory activity against nasal AMP challenge, but there was no potentiation of fluticasone when given in combination with salmeterol."( Effects of intranasal salmeterol and fluticasone given alone and in combination in persistent allergic rhinitis.
Burns, P; Lipworth, BJ; Nair, A; Short, P, 2012)		0.38
" In conclusion, our results suggest that abediterol has a preclinical profile for once-daily dosing in humans together with a fast onset of action and a favorable cardiovascular safety profile."( Pharmacological characterization of abediterol, a novel inhaled β(2)-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical models.
Aparici, M; Beleta, J; Carcasona, C; Cortijo, J; De Alba, J; Gavaldà, A; Gómez-Angelats, M; Gras, J; Miralpeix, M; Morcillo, E; Otal, R; Puig, C; Ramos, I; Ryder, H; Vilella, D; Viñals, M, 2012)		0.38
"The objective of this work was to characterize the dose-response relationship between two inhaled long-acting beta agonists (PF-00610355 and salmeterol) and the forced expiratory volume in one second (FEV1) in order to inform dosing recommendations for future clinical trials in patients with chronic obstructive pulmonary disease (COPD)."( Longitudinal FEV1 dose-response model for inhaled PF-00610355 and salmeterol in patients with chronic obstructive pulmonary disease.
Cleton, A; Hutmacher, MM; Martin, SW; Nielsen, JC; Ribbing, J, 2012)		0.38
" This pharmacological profile combined with clinical data is consistent with once a day dosing of vilanterol in the treatment of both asthma and chronic obstructive pulmonary disease (COPD)."( In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action.
Barrett, VJ; Emmons, AJ; Ford, AJ; Knowles, RG; Morrison, VS; Slack, RJ; Sturton, RG, 2013)		0.39
" The secondary outcome was difference in symptom scores among the three treatment groups to determine if one dosing protocol was superior to another."( Early intervention with high-dose inhaled corticosteroids for control of acute asthma exacerbations at home and improved outcomes: a randomized controlled trial.
Hossain, J; Mannan, S; McGeady, S; Skorpinski, E; Yousef, E, )		0.13
" No effects were observed on glucose, potassium, heart rate, blood pressure and no dose-response effect was seen on corrected QT elongation."( A new class of bronchodilator improves lung function in COPD: a trial with GSK961081.
Baggen, S; Chan, R; Locantore, N; Ludwig-Sengpiel, A; Riley, JH; Wielders, PL, 2013)		0.39
" Controlling for FP dosage and baseline characteristics, FSC patients had lower risks of asthma-related exacerbations, fewer SABAs and systemic corticosteroids, higher costs of asthma medications and total asthma-related health care, and lower total asthma-related health-care costs excluding study medication cost."( Health-care utilization and costs with fluticasone propionate and fluticasone propionate/salmeterol in asthma patients at risk for exacerbations.
Delea, TE; Hagiwara, M; Stanford, RH, )		0.13
" In vivo study, SM-loaded PLGA microspheres are thought to have the potential to maintain SM concentration within target ranges for a long time, decreasing side effects caused by concentration fluctuation, ensuring the efficiency of treatment and improving patient compliance by reducing dosing frequency."( Enhanced oral bioavailability of salmeterol by loaded PLGA microspheres: preparation, in vitro, and in vivo evaluation.
Xu, J; Zhang, H, 2016)		0.43
" RESULTS were adjusted for initial prescriber, initial medication, dosing regimen and relevant comorbidities."( Impact of multiple-dose versus single-dose inhaler devices on COPD patients' persistence with long-acting β₂-agonists: a dispensing database analysis.
Dekhuijzen, PN; Postma, MJ; van Boven, JF; van der Galiën, R; van der Molen, T; van Raaij, JJ; Vegter, S, 2014)		0.4
" In contrast, dosage forms containing non-respirable carriers (e."( Quantitative Macro-Raman Spectroscopy on Microparticle-Based Pharmaceutical Dosage Forms.
Hoe, S; Lechuga-Ballesteros, D; Vehring, R; Wang, H; Williams, L, 2015)		0.42
"We used impulse oscillometry (IOS) to compare single and repeated dosing effects of small- and large-particle long-acting β-agonists."( Effects of formoterol or salmeterol on impulse oscillometry in patients with persistent asthma.
Lipworth, BJ; Manoharan, A; Morrison, A; von Wilamowitz-Moellendorff, A, 2016)		0.43
"Significant improvements in IOS outcomes but not spirometry results occurred after chronic dosing with formoterol compared with salmeterol."( Effects of formoterol or salmeterol on impulse oscillometry in patients with persistent asthma.
Lipworth, BJ; Manoharan, A; Morrison, A; von Wilamowitz-Moellendorff, A, 2016)		0.43
" We aimed to assess the efficacy and safety of two dosing regimens of tralokinumab in patients with severe uncontrolled asthma."( Efficacy and safety of tralokinumab in patients with severe uncontrolled asthma: a randomised, double-blind, placebo-controlled, phase 2b trial.
Brightling, CE; Chanez, P; Korn, S; Leigh, R; May, RD; O'Byrne, PM; Piper, E; Ranade, K; She, D; Streicher, K, 2015)		0.42
" Patients aged 18-75 years with severe asthma and two to six exacerbations in the previous year were randomly assigned (1:1), via an interactive voice-response or web-response system, to one of two dosing regimen groups (every 2 weeks, or every 2 weeks for 12 weeks then every 4 weeks) and further randomised (2:1), via computer-generated permuted-block randomisation (block size of six), to receive tralokinumab 300 mg or placebo for 1 year."( Efficacy and safety of tralokinumab in patients with severe uncontrolled asthma: a randomised, double-blind, placebo-controlled, phase 2b trial.
Brightling, CE; Chanez, P; Korn, S; Leigh, R; May, RD; O'Byrne, PM; Piper, E; Ranade, K; She, D; Streicher, K, 2015)		0.42
" For salbutamol and formoterol, urine thresholds have been adopted to limit supratherapeutic dosing and to discriminate between inhaled (permitted) and oral (prohibited) use."( Beta2-Agonist Doping Control and Optical Isomer Challenges.
Fawcett, JP; Jacobson, GA, 2016)		0.43
" Although salmeterol is permitted via inhalation by athletes and supratherapeutic dosing may enhance performance, no urine threshold has been established by the World Anti-Doping Agency (WADA)."( Enantioselective disposition of (R)-salmeterol and (S)-salmeterol in urine following inhaled dosing and application to doping control.
Haydn Walters, E; Hostrup, M; Jacobson, GA; Narkowicz, CK; Nichols, DS, 2017)		0.46
" For this reason, all beta2-agonists are currently on the Prohibited List issued by the World Anti-Doping Agency (WADA), regardless of dosing route with some exemptions for inhaled salbutamol, formoterol, and salmeterol when used at therapeutic inhaled doses."( The salmeterol anomaly and the need for a urine threshold.
Hostrup, M; Jacobson, GA, 2022)		0.72
" MON, or combination of MFC, with no limitation of dosage or duration."( Efficacy and safety of salmeterol/fluticasone compared with montelukast alone (or add-on therapy to fluticasone) in the treatment of bronchial asthma in children and adolescents: a systematic review and meta-analysis.
Hong, JG; Lu, J; Qin, Z; Zhou, XJ, 2021)		0.62
"Beta 2 agonists are well known for their use in the treatment of asthma and COPD however in the last few years new indications of beta 2 agonist appeared like reduction of local fats and treatment of preterm labour which required the formulation of new dosage forms and administration strategies."( Optimization of two charge transfer reactions for colorimetric determination of two beta 2 agonist drugs, salmeterol xinafoate and salbutamol, in pharmaceutical and biological samples.
Abdelkawy, M; Salem, H; Samir, A, 2022)		0.72
" An improved method for measuring the absorbed fraction of analogues dosed to rats, which considers the glucuronidated fraction is presented."( The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
Barrett, VJ; Bevan, NJ; Butchers, PR; Conroy, R; Emmons, A; Ford, AJ; Jeulin, S; Looker, BE; Lunniss, GE; Morrison, VS; Mutch, PJ; Perciaccante, R; Procopiou, PA; Ruston, M; Smith, CE; Somers, G, 2011)		0.37
" Through this process a novel, high potency, full β(2)-agonist with high selectivity and long duration capable of being dosed once daily has been discovered."( Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
Alcaraz, L; Bailey, A; Cadogan, E; Christie, J; Connolly, S; Cook, AR; Fisher, AJ; Hill, S; Humphries, A; Ingall, AH; Kane, Z; Paine, S; Pairaudeau, G; Stocks, MJ; Young, A, 2011)		0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (6)

ClassDescription
naphthoic acidAn aromatic carboxylic acid that consists of a naphthalene skeleton substituted by one or more carboxy groups.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
etherAn organooxygen compound with formula ROR, where R is not hydrogen.
secondary alcoholA secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
primary alcoholA primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
[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 (109)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency32.46480.025120.237639.8107AID886; AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency32.46480.025120.237639.8107AID886; AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.18380.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency14.12545.623417.292931.6228AID2323
LuciferasePhotinus pyralis (common eastern firefly)Potency14.38180.007215.758889.3584AID624030
acetylcholinesteraseHomo sapiens (human)Potency34.67130.002541.796015,848.9004AID1347398
glp-1 receptor, partialHomo sapiens (human)Potency4.10950.01846.806014.1254AID743262
thioredoxin reductaseRattus norvegicus (Norway rat)Potency17.22060.100020.879379.4328AID588453; AID588456
RAR-related orphan receptor gammaMus musculus (house mouse)Potency23.71010.006038.004119,952.5996AID1159521
ATAD5 protein, partialHomo sapiens (human)Potency10.31830.004110.890331.5287AID504466
Fumarate hydrataseHomo sapiens (human)Potency11.22020.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency50.11870.031637.5844354.8130AID504865
NFKB1 protein, partialHomo sapiens (human)Potency5.62340.02827.055915.8489AID895; AID928
GALC proteinHomo sapiens (human)Potency0.631028.183828.183828.1838AID1159614
GLS proteinHomo sapiens (human)Potency14.49130.35487.935539.8107AID624146; AID624170
TDP1 proteinHomo sapiens (human)Potency11.20200.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency5.44940.000714.592883.7951AID1259369; AID1259392
ThrombopoietinHomo sapiens (human)Potency10.00000.02517.304831.6228AID917; AID918
AR proteinHomo sapiens (human)Potency30.05780.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063
Smad3Homo sapiens (human)Potency22.38720.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency25.11890.011212.4002100.0000AID1030
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency16.78550.000657.913322,387.1992AID1259378
progesterone receptorHomo sapiens (human)Potency26.60320.000417.946075.1148AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency37.68580.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.43930.01237.983543.2770AID1346984; AID1645841
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency5.01190.28189.721235.4813AID2326
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency15.99800.000214.376460.0339AID720691; AID720692
retinoid X nuclear receptor alphaHomo sapiens (human)Potency17.04240.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency18.13890.001530.607315,848.9004AID1224819; AID1224820; AID1224848; AID1224849; AID1259401; AID1259403
estrogen nuclear receptor alphaHomo sapiens (human)Potency25.21240.000229.305416,493.5996AID1259248; AID743069; AID743075; AID743079; AID743080; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency2.18760.00108.379861.1304AID1645840
polyproteinZika virusPotency11.22020.00308.794948.0869AID1347053
67.9K proteinVaccinia virusPotency8.91250.00018.4406100.0000AID720579
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency33.48890.001024.504861.6448AID743212
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency13.44810.001019.414170.9645AID743140
IDH1Homo sapiens (human)Potency16.36010.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency35.48130.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency28.22630.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency26.60320.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.08280.001628.015177.1139AID1224843; AID1224895
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency24.07320.057821.109761.2679AID1159526; AID1159528
beta-2 adrenergic receptorHomo sapiens (human)Potency7.85730.00586.026332.6427AID492947; AID588463; AID588790
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00280.540617.639296.1227AID2364; AID2528
hexokinase-4 isoform 1Homo sapiens (human)Potency8.91252.511913.800328.1838AID743205
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency33.807823.934123.934123.9341AID1967
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.58930.316212.443531.6228AID902; AID924
D(1A) dopamine receptorHomo sapiens (human)Potency22.38720.02245.944922.3872AID488981
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency28.18380.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency79.43280.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID488953
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency2.23873.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency4.00750.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.90470.000323.4451159.6830AID743065; AID743067
histone deacetylase 9 isoform 3Homo sapiens (human)Potency26.60320.037617.082361.1927AID1259364
glucokinase regulatory proteinHomo sapiens (human)Potency8.91252.511913.800328.1838AID743205
mitogen-activated protein kinase 1Homo sapiens (human)Potency15.84890.039816.784239.8107AID995
ras-related protein Rab-9AHomo sapiens (human)Potency58.04790.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency14.68920.00378.618923.2809AID2667; AID2668
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency13.33220.000627.21521,122.0200AID743202
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.94330.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency7.94330.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.94330.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency24.15550.004611.374133.4983AID463097; AID624296; AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency4.05330.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency31.62280.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.94330.031610.279239.8107AID884; AID885
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency19.95260.09120.09120.0912AID488979
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency11.22020.00106.000935.4813AID943
lamin isoform A-delta10Homo sapiens (human)Potency14.12540.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency19.95260.316212.765731.6228AID881
Integrin beta-3Homo sapiens (human)Potency12.58930.316211.415731.6228AID924
Integrin alpha-IIbHomo sapiens (human)Potency12.58930.316211.415731.6228AID924
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency19.95260.00638.235039.8107AID881
D(1A) dopamine receptorSus scrofa (pig)Potency14.68920.00378.108123.2809AID2667
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency12.58930.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.94331.000012.224831.6228AID885
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.11890.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency28.18385.623417.292931.6228AID485281
phosphopantetheinyl transferaseBacillus subtilisPotency56.23410.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency14.13930.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency26.80610.000221.22318,912.5098AID743035; AID743042; AID743054; AID743063
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency7.56240.000214.376460.0339AID720691
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.34430.000229.305416,493.5996AID743069; AID743079; AID743080; AID743091
glucocerebrosidaseHomo sapiens (human)Potency39.81070.01268.156944.6684AID2101
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency16.78550.001723.839378.1014AID743083
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency8.57730.000323.4451159.6830AID743065; AID743067
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency18.25630.00798.23321,122.0200AID2546; AID2551
Cellular tumor antigen p53Homo sapiens (human)Potency33.49150.002319.595674.0614AID651631
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
galanin receptor type 3Homo sapiens (human)IC50 (µMol)29.91600.00661.54317.3650AID687013
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Beta-2 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00500.00020.93267.2000AID640201
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.01830.00000.66359.5499AID1152885; AID1185817; AID1224049; AID1298705; AID1598554; AID238673; AID481516; AID501435; AID578408; AID605349; AID605419
Beta-1 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.50120.00021.46819.0000AID609376; AID643244
Beta-1 adrenergic receptorHomo sapiens (human)Ki1.59920.00011.33919.9840AID1152886; AID1185818; AID501436; AID605350
D(2) dopamine receptorHomo sapiens (human)Ki32.00000.00000.651810.0000AID1298708
Beta-1 adrenergic receptorMus musculus (house mouse)Ki0.55000.00010.13100.5500AID1598553
D(3) dopamine receptorHomo sapiens (human)Ki1.04900.00000.602010.0000AID1185819
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00350.00040.16800.9772AID1185820
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)Ki0.83830.00040.59022.5119AID1152885; AID1152886; AID481516
[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)
beta-2 adrenergic receptorHomo sapiens (human)EC50 (µMol)0.00450.00161.87598.4400AID588763
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)EC50 (µMol)0.00030.00030.01160.0398AID414892
Beta-2 adrenergic receptorHomo sapiens (human)EC50 (µMol)0.00030.00000.311110.0000AID1073604; AID1152884; AID1152893; AID1224052; AID1224054; AID1543325; AID1598564; AID1598568; AID1598570; AID1650066; AID1760529; AID1783430; AID290780; AID302101; AID414892; AID481517; AID483557; AID510454; AID578409; AID606103; AID609373; AID611239; AID623252; AID640202; AID640204; AID643219
Beta-2 adrenergic receptorHomo sapiens (human)Kd1.42660.00000.62888.9130AID1626022; AID1626023; AID1798580
Beta-1 adrenergic receptorHomo sapiens (human)EC50 (µMol)0.84770.00010.49146.0000AID1073602; AID1152890; AID1224051; AID1543326; AID1598556; AID1598562; AID1650067; AID1760528; AID1783429; AID414891; AID483559; AID609382; AID611237; AID623254; AID640203
Beta-1 adrenergic receptorHomo sapiens (human)Kd2.01080.00010.803910.0000AID1798580
Beta-3 adrenergic receptorHomo sapiens (human)EC50 (µMol)1.18490.00010.455310.0000AID1073601; AID1152891; AID1224053; AID414894; AID483560; AID611236; AID623255
Beta-3 adrenergic receptorHomo sapiens (human)Kd2.01080.00010.76318.9130AID1798580
Histamine H2 receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.00030.00030.57191.2023AID414892
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.71200.00020.88438.2000AID1152893; AID1543326; AID481517; AID611234; AID623255
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LMP1 [Human herpesvirus 4]human gammaherpesvirus 4 (Epstein-Barr virus)AC5061.43600.068039.9389277.4300AID504861
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (397)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (106)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (87)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (369)

Assay IDTitleYearJournalArticle
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID483565Permeability across MDR1-expressing MDCK2 cells at 3 uM in presence of p-glycoprotein inhibitor2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID524793Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID510458Bronchodilatory activity in itr dosed Beagle dog assessed as inhibition of acetylcholine-induced bronchoconstriction administered 5 doses of compound at cumulative 1 hr intervals2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID1224053Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.
AID1073586Oral bioavailability in rat2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID1598554Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID1650066Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID481513Binding affinity to human serum albumin by UV/HPLC analysis2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID1137786Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal rings assessed as relaxation of methacholine-constricted tracheal rings2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.
AID1224050Selectivity ratio of Ki for human beta1 adrenergic receptor to Ki for human beta2 adrenergic receptor2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1783427Agonist activity at human beta2 adrenoreceptor in HEK293 cells assessed as cAMP accumulation by measuring intrinsic activity relative to control2021European journal of medicinal chemistry, Nov-15, Volume: 2248-Hydroxyquinolin-2(1H)-one analogues as potential β
AID62632Tested in vitro for binding activity to Dopamine receptor D2 in bovine pituitary membranes (D2-LB); nt =not tested1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Dual D2-receptor and beta2-adrenoceptor agonists for the treatment of airway diseases. 1. Discovery and biological evaluation of some 7-(2-aminoethyl)-4-hydroxybenzothiazol-2(3H)-one analogues.
AID611237Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID643231Terminal half life in iv dosed rat2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID609375Octanol-phosphate buffer distribution coefficient, log D of the compound at pH 7.4 by LC/MS analysis2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID623254Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID414895Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1224054Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.
AID1152893Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID414898Ratio of metabolic stability for drug to verapamil in human microsomes2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID415158Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as ratio of EC50 for inhibition of electrical stimulation-induced contraction after 3 hrs of compound washout to EC50 at equilibrium before washout2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1598568Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID1253962Bronchodilator activity in intratracheally dosed conscious dog assessed as inhibition of methacholine-induced bronchoconstriction administered in micelle solution2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
AID414897Passive permeability across MDR1-expressing dog MDCK2 cells membrane at 3 uM in presence of P-glycoprotein inhibitor2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1152891Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID609376Binding affinity to adrenergic beta1 receptor2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID609382Agonist activity at adrenergic beta1 receptor2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID1185819Displacement of [125I]7-HO-PIPAT from human D3R expressed in HEK cells2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
AID643244Binding affinity to beta1 adrenoceptor2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
AID1598569Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID1253964Therapeutic index, ratio of compound activity for heart rate in conscious dog to compound activity for inhibition of methacholine-induced bronchoconstriction in conscious dog2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
AID1458049Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of F protons with lipid acyl CH3 at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID1152883Selectivity ratio EC50 for human beta2 receptor to EC50 for human beta1 receptor2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID302101Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.
AID510459Bronchodilatory activity in itr dosed Beagle dog assessed as duration of blockade of acetylcholine-induced bronchoconstriction at ED50 administered as single dose prior to acetylcholine challenge2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID1152885Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID235924Partition coefficient (logD)2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.
AID510461Cardiotoxicity in itr dosed Beagle dog assessed as increase in heart rate after 7.5 hrs2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID414916Selectivity assessed as difference in pEC50 for human cloned beta2 adrenergic receptor and pEC50 for human cloned beta-1 adrenergic receptor2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID623256Metabolic stability in human liver microsomes assessed as compound turn over ratio relative to verapamil2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID483562Bronchodialatory activity against electrically-stimulated contraction in guinea pig trachea assessed as time taken for inducing 50% maximum relaxant effect2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID481520Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as time required to reach maximal inhibition of electrically-induced bronchoconstriction2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID1650073Agonist activity at beta2 adrenergic receptor in Dunkin-Hartley guinea pig trachea assessed as reduction in histamine-induced muscle contraction by measuring time of action after withdrawal of compound2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β
AID483573Ex vivo bronchodilatory activity in guinea pig assessed as protection against histamine-induced bronchospasm administered via nebulizer2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID623255Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID414896Distribution coefficient, log D at pH 6.42009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID623252Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID1626024Binding affinity to inactive/G protein-uncoupled human beta2-AR by immobilized artificial membrane HPLC analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
AID640204Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
AID318146Distribution coefficient, log D of the compound2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists.
AID1185822Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as time for response to fall to 50% of maximal response during washout phase at IC502014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
AID481519Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID1458050Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of F protons with segment G-3 at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1152890Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID510457Distribution coefficient, log D of the compound2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID1152884Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID290785Agonist potency at beta-2 adrenoceptor in guinea pig trachea model relative to salmeterol2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
The discovery of long acting beta2-adrenoreceptor agonists.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1650072Agonist activity at beta2 adrenergic receptor in Dunkin-Hartley guinea pig trachea assessed as reduction in histamine-induced muscle contraction by measuring onset time2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β
AID611135Bronchodilatory activity against histamine-induced bronchospasm in guinea pig administered via nebulizer2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID1650067Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β
AID1137783Intrinsic activity at beta-2 adrenergic receptor in guinea pig tracheal rings2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.
AID1152896Inhibition of acetylcholine-induced bronchoconstriction in male guinea pig assessed as pulmonary resistance at 300 ug/ml administered via nebulization for 10 mins measured after >= 24 hrs by plethysmograph2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID483560Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID481516Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID1073599Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as time taken for EC50 concentration to achieve 50% maximum relaxant effect2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID1152892Selectivity ratio EC50 for human beta2 receptor to EC50 for human beta3 receptor2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID1224051Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.
AID36429Tested in vitro for binding activity to Alpha-1 adrenergic receptor in field stimulated rabbit ear artery (REA).1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Dual D2-receptor and beta2-adrenoceptor agonists for the treatment of airway diseases. 1. Discovery and biological evaluation of some 7-(2-aminoethyl)-4-hydroxybenzothiazol-2(3H)-one analogues.
AID1073602Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID640208Bronchoprotective activity in Ach-stimulated guinea pig assessed as reduction in pulmonary resistance at 300 ug/mL administered via nebulization measured after 24 hrs by head-out plethysmography2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
AID1298712Selectivity index, ratio of Ki for human D2S receptor to Ki for human beta2 receptor2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID611238Intrinsic activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cyclic AMP accumulation relative to isoprenaline2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID1152887Selectivity ratio Ki for beta2 receptor (unknown origin) to Ki for beta1 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID414915Inhibition of prostaglandin F2alpha-induced contraction in human lung bronchus assessed as onset time of contraction inhibition2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID611236Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID1152886Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID1650071Agonist activity at beta2 adrenergic receptor in Dunkin-Hartley guinea pig trachea assessed as reduction in histamine-induced muscle contraction relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β
AID6432431-Octanol-aqueous buffer distribution coefficient, log D at pH 7.4 by LC/MS analysis2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
AID290781Ratio of EC50 for beta2 adrenoceptor to EC50 for beta-1 adrenoceptor2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
The discovery of long acting beta2-adrenoreceptor agonists.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID606104Intrinsic activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr relative to formoterol2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.
AID290786Volume of distribution in iv dosed rat2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
The discovery of long acting beta2-adrenoreceptor agonists.
AID621921Oral bioavailability in dog2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID510462Therapeutic index, ratio of dose inducing cardiovascular side effects to ED50 for inhibition of acetylcholine-induced bronchoconstriction in itr dosed Beagle dog2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID1185817Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
AID606103Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.
AID1458045Binding affinity to POPC liposome membrane assessed as 31P chemical shift anisotropy at compound to POPC molar ratio of 1:10 by NMR analysis (Rvb = 28.9 ppm)2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID483557Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID1185818Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID621920Oral bioavailability in rat2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID302102Ratio of EC50 for human recombinant adrenergic beta-2 receptor to EC50 for human recombinant adrenergic beta-1 receptor2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.
AID1073587Oral bioavailability in dog2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID621922Bronchodilatory activity against histamine-induced bronchospasm in the guinea pig2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID1073604Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID248534Concentration required to inhibit electrically induced contraction of superfused guinea-pig trachea was determined2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1458051Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of F protons with segment alpha at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID1598564Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID611239Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID302113Activity at beta2 adrenergic receptor in guinea pig trachea assessed as time taken for muscle tone2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1598556Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1760528Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Recent Advances in β
AID606106Bronchodilatory activity against histamine-induced bronchoconstriction in guinea pig at ED80 intratracheally administered 2 hrs before challenge measured up to 12 hrs2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID510455Selectivity ratio of EC50 for human recombinant beta-1 adrenergic receptor to EC50 for human recombinant beta2 adrenergic receptor2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID1137785Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal rings assessed as time required to reach 90% of final relaxation of methacholine-constricted tracheal rings2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.
AID483571Oral bioavailability in rat2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID1073600Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as duration of action expressed as rightward shift in the agonist concentration-effect curve following compound washout after 1 hr relative to control2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID605419Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.
AID1598555Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay relative to i2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1650069Partial agonist activity at human beta2 adrenoreceptor endogenously expressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β
AID1185820Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
AID1783426Myorelaxant effect in guinea pig model of histamine-induced smooth muscle contraction assessed as time of onset of action measured over 12 hrs2021European journal of medicinal chemistry, Nov-15, Volume: 2248-Hydroxyquinolin-2(1H)-one analogues as potential β
AID609377Selectivity ratio of IC50 for adrenergic beta1 receptor over EC50 for human adrenergic beta2 receptor2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID1253961Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
AID1543327Selectivity ratio of compound effect for agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells to compound effect for agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1137782Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as accumulation of intracellular cAMP2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.
AID1598567Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID1073598Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as duration of action expressed as rightward shift in the agonist concentration-effect curve following compound washout after 3 hrs relative to control2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID623258Bronchodilatory activity against electrically-stimulated contraction in guinea pig trachea assessed as onset time for bronchorelaxation activity2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID1253959Activity at beta2 adrenoceptor/muscarinic M3 receptor in guinea pig trachea assessed as time required for inhibited electric fileld-stimulated contraction to recover by 25%2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID605418Selectivity ratio of Ki for human beta1-adrenergic receptor to Ki human beta2-adrenergic receptor2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.
AID640203Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
AID643220Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry relative to formoterol2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
AID1598559Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK2 and coelenterazine 400a by BRET2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID640202Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
AID1783430Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation2021European journal of medicinal chemistry, Nov-15, Volume: 2248-Hydroxyquinolin-2(1H)-one analogues as potential β
AID640209Bronchoprotective activity in Ach-stimulated guinea pig assessed as reduction in pulmonary resistance at 30 ug/mL administered via nebulization measured at 48 hrs post-dosing by head-out plethysmography2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
AID1599372Antiviral activity against DENV2 infected in human Huh7 cells by qRT-PCR analysis2019European journal of medicinal chemistry, Aug-15, Volume: 176Recent update on anti-dengue drug discovery.
AID1224055Intrinsic agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay relative to isoproterenol2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.
AID62630Tested in vitro for binding activity to Dopamine receptor D2 in bovine pituitary membranes (D2-LB); nt =not tested1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Dual D2-receptor and beta2-adrenoceptor agonists for the treatment of airway diseases. 1. Discovery and biological evaluation of some 7-(2-aminoethyl)-4-hydroxybenzothiazol-2(3H)-one analogues.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID290782Distribution coefficient, log D of the compound2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
The discovery of long acting beta2-adrenoreceptor agonists.
AID609374Intrinsic activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins relative to formoterol2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID643246Drug metabolism in rat hepatocytes2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
AID414893Intrinsic activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay relative to isoprenaline2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1298705Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
AID1783428Selectivity ratio of EC50 for agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells to EC50 for agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells2021European journal of medicinal chemistry, Nov-15, Volume: 2248-Hydroxyquinolin-2(1H)-one analogues as potential β
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1626022Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
AID481521Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as duration of maximal inhibitory action against electrically-induced bronchoconstriction2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID483559Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID483564Bronchodialatory activity against electrically-stimulated contraction in guinea pig trachea assessed as inhibition of recovery of contractile effect measured after 3 hrs of drug washout2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID302112Activity at adrenergic beta-2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated muscle contraction relative to salmeterol2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.
AID1598565Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay re2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID414892Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1783429Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation2021European journal of medicinal chemistry, Nov-15, Volume: 2248-Hydroxyquinolin-2(1H)-one analogues as potential β
AID414913Inhibition of histamine-induced bronchospasm in guinea pig trachea assessed as time duration for 50% recovery time administered as nebulized solution2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID414917Selectivity assessed as difference in pEC50 for human cloned beta2 adrenergic receptor and pEC50 for human cloned beta3 adrenergic receptor2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID578408Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.
AID483558Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation at 10 mM after 30 to 45 mins relative to isoprenaline2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID1626023Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
AID1783425Myorelaxant effect in guinea pig model of histamine-induced smooth muscle contraction assessed as time duration of action measured over 12 hrs2021European journal of medicinal chemistry, Nov-15, Volume: 2248-Hydroxyquinolin-2(1H)-one analogues as potential β
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1224049Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.
AID302103Lipophilicity, log D of the compound2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.
AID1543332Agonist activity at beta2 adrenergic receptor in Dunkin-Hartley guinea pig trachea assessed as reduction in histamine-induced muscle contraction by measuring onset time
AID1650068Selectivity index, ratio of pEC50 for human beta1 adrenoreceptor overexpressed in human HEK293 cells subtracted from pEC50 for human beta2 adrenoreceptor overexpressed in human HEK293 cells2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β
AID643219Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
AID414919Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as ratio of EC50 for inhibition of electrical stimulation-induced contraction after 1 hr of compound washout to EC50 at equilibrium before washout2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID501435Displacement of [3H]CGP12177 from human beta2 adrenoceptor2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.
AID1598570Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID621923Bronchodilatory activity against histamine-induced bronchospasm in guinea pig assessed as time taken for 50% recovery of bronchospasm at EC90 administered via nebulizer2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID318147Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as elevation in cAMP levels2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists.
AID640205Intrinsic activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
AID1543326Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
AID1598562Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID1458053Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of F protons with segment gamma at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID414922Inhibition of prostaglandin F2alpha-induced contraction in human lung bronchus2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID510454Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID1760529Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Recent Advances in β
AID1458065Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of E protons with C2/C3 segment at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID510456Ratio of compound EC50 to salmeterol EC50 for inhibition of electrical filed stimulation-induced constriction in Dunkin-Hartley guinea pig trachea after 4 hrs2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1224052Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.
AID1073601Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID1253963Bronchodilator activity in conscious dog assessed as time required to inhibit methacholine-induced bronchoconstriction at 30 ug administered through intratracheally in micelle solution2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
AID485979Inhibition of CETP in rabbit serum at 10 uM after 1 hr by fluorescent cholesteryl esters transfer assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic exploration.
AID609378Half life in iv dosed rat plasma2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID414891Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1458048Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of E proton with C-3/C-2 region of lipid at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID481525Inhibition of serotonin-induced bronchoconstriction in guinea pig assessed as intrinsic duration of bronchodilatory activity at ED802010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID643235Bronchoprotective activity in it dosed guinea pig assessed as inhibition of histamine-induced constriction2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
AID510453Bronchodilatory activity in Dunkin-Hartley guinea pig trachea assessed as time taken for electrical filed stimulation-induced constrictive response to recover by 50%2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID1783423In vivo agonist activity at beta2 adrenergic receptor isolated from guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring maximal relaxant effect relative to control2021European journal of medicinal chemistry, Nov-15, Volume: 2248-Hydroxyquinolin-2(1H)-one analogues as potential β
AID609383Selectivity ratio of EC50 for human adrenergic beta2 receptor to EC50 for adrenergic beta1 receptor2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID623259Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as duration of action expressed as rightward shift in the agonist concentration-effect curve following 1 hr of washout2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID1458057n-octanol/PBS/sodium carbonate partition coefficient, log P of the compound after 4 hrs2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID609373Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID1253957Activity at beta2 adrenoceptor/muscarinic M3 receptor in guinea pig trachea assessed as inhibition of electric fileld-stimulated contraction2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
AID510460Bronchodilatory activity in itr dosed Beagle dog assessed as duration of blockade of acetylcholine-induced bronchoconstriction at 10 times ED50 administered as single dose prior to acetylcholine challenge2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.
AID414900Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced contraction in guinea pig trachea after 3 hrs washout2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID611145Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as duration of action expressed as rightward shift in the agonist concentration-effect curve following 3 hrs of washout2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID1543333Agonist activity at beta2 adrenergic receptor in Dunkin-Hartley guinea pig trachea assessed as reduction in histamine-induced muscle contraction by measuring time of action
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID609372Binding affinity to dopamine 2 receptor2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID290780Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
The discovery of long acting beta2-adrenoreceptor agonists.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1650070Agonist activity at beta2 adrenergic receptor in Dunkin-Hartley guinea pig trachea assessed as reduction in histamine-induced muscle contraction2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β
AID414918Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as onset time for 50% inhibition of electrical stimulation-induced muscle contraction2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1458064Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of E protons with CH2-C= segment at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID483574Ex vivo bronchodilatory activity against histamine-induced bronchospasm in guinea pig assessed as time taken for 50% recovery of bronchospasm at EC90 administered via nebulizer2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID643245Selectivity ratio of pIC50 for beta1 adrenoceptor to pEC50 for human beta2 adrenoceptor2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
AID1458059Lipophilicity of the compound assessed as capacity factor (CHI IAM7.4) at pH 7.4 by chromatographic analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID1152894Intrinsic activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID481518Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay relative to formoterol2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID1458052Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of F protons with segment beta at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID501436Displacement of [3H]CGP12177 from human beta-1 adrenoceptor2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID483563Bronchodialatory activity against electrically-stimulated contraction in guinea pig trachea assessed as inhibition of recovery of contractile effect measured after 1 hr of drug washout2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID1073603Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay relative to isoprenaline2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID640201Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
AID1185821Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as time to maximal effect at IC502014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
AID611234Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID578409Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.
AID623257Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID238673Binding affinity for human beta-2 adrenergic receptor2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.
AID1298708Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
AID611235Metabolic stability in human liver microsomes with 125 pmol/mL P450 assessed as compound turnover ratio at 5 uM after 30 mins by LC-MS method relative to verapamil2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID1598563Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay relative to i2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID1543325Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
AID414894Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID1152889Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.
AID609380Bronchodilatory activity in intratracheally dosed guinea pig assessed as inhibition of histamine-induced bronchoconstriction2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.
AID1458055Binding affinity to POPC liposome membrane in liquid disorder phase assessed as change in cross-relaxation rate of hydrophilic group B protons with G-3 segment at compound to POPC molar ratio of 1:10 to 1:5 by 1D 1H Mass spectra analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID611147Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as time taken for EC50 concentration to achieve 50% maximum relaxant effect2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID623261Lipophilicity, log D of the compound at pH 6.42011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID1137807Bronchoprotective activity in guinea pig assessed as inhibition of histamine-induced bronchoconstriction at ED80 administered intratracheally after 4 to 24 hrs relative to control2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.
AID41024Tested in vitro for binding activity to Beta-2 adrenergic receptor in guinea pig trachea (GPT).1998Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25
Dual D2-receptor and beta2-adrenoceptor agonists for the treatment of airway diseases. 1. Discovery and biological evaluation of some 7-(2-aminoethyl)-4-hydroxybenzothiazol-2(3H)-one analogues.
AID1598557Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay re2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID483561Metabolic stability in human liver microsomes assessed as compound turnover ratio at 5 uM after 30 mins2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID414912Inhibition of histamine-induced bronchospasm in guinea pig trachea by plethysmograph chamber assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID290788Effect on guinea pig trachea model assessed as duration of muscle tone2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
The discovery of long acting beta2-adrenoreceptor agonists.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1783424In vivo agonist activity at beta2 adrenergic receptor isolated from guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction2021European journal of medicinal chemistry, Nov-15, Volume: 2248-Hydroxyquinolin-2(1H)-one analogues as potential β
AID611146Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as duration of action expressed as rightward shift in the agonist concentration-effect curve following 1 hrs of washout2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
AID481517Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1458054Binding affinity to POPC liposome membrane in liquid disorder phase assessed as change in cross-relaxation rate of hydrophilic group B protons with G-1 segment at compound to POPC molar ratio of 1:10 to 1:5 by 1D 1H Mass spectra analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID1458063Binding affinity to POPC liposome membrane assessed as cross-relaxation rate of E protons with (CH2)n segment at compound to POPC molar ratio of 1:10 by NOESY 1H NMR analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Interactions between β2-Adrenoceptor Ligands and Membrane: Atomic-Level Insights from Magic-Angle Spinning NMR.
AID605350Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma counting2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID623260Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as duration of action expressed as rightward shift in the agonist concentration-effect curve following 3 hrs of washout2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID623253Intrinsic activity at at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.
AID1598561Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID1073589Oral absorption in Han Wistar rat at 2 mg/kg up to 7 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
AID605349Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID250135Inhibition of compound against MES-SA/DX5 cell line was determined using P-glycoprotein assay2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
A pharmacophore hypothesis for P-glycoprotein substrate recognition using GRIND-based 3D-QSAR.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID318148Selectivity for human recombinant adrenergic beta2 receptor over human recombinant adrenergic beta-1 receptor2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID481512Chromatographic hydrophobicity index at 2 mg/ml at pH 7.4 by rapid gradient HPLC analysis2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
AID1598553Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
AID414921Therapeutic index, ratio of drug level causing inhibition of histamine-induced bronchospasm in guinea pig to drug level causing decrease in mean arterial pressure in guinea pig2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID17985803H-CGP 12177 Whole Cell Binding Assay from Article 10.1038/sj.bjp.0706048: \\The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.\\2005British journal of pharmacology, Feb, Volume: 144, Issue:3
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
AID1346250Human beta2-adrenoceptor (Adrenoceptors)2010British journal of pharmacology, Jul, Volume: 160, Issue:5
The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,817)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.06)18.7374
1990's522 (28.73)18.2507
2000's792 (43.59)29.6817
2010's449 (24.71)24.3611
2020's53 (2.92)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.90

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index48.90 (24.57)
Research Supply Index3.85 (2.92)
Research Growth Index5.85 (4.65)
Search Engine Demand Index70.61 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (48.90)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials684 (36.54%)5.53%
Trials0 (0.00%)5.53%
Reviews251 (13.41%)6.00%
Reviews2 (4.35%)6.00%
Case Studies47 (2.51%)4.05%
Case Studies0 (0.00%)4.05%
Observational5 (0.27%)0.25%
Observational0 (0.00%)0.25%
Other885 (47.28%)84.16%
Other44 (95.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (313)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A 16-week Randomised, Placebo-controlled, Double-blind, Double-dummy, Parallel-group Study Comparing the Efficacy and Safety of Tiotropium Inhalation Solution Delivered by the Respimat Inhaler (2 Actuations of 2.5 Mcg Once Daily) With That of Salmeterol F [NCT00350207]Phase 2388 participants (Actual)Interventional2006-07-31Completed
A Multicentre, Randomised, Double-blind, Double Dummy, Parallel Group Study to Compare the Salmeterol/Fluticasone Propionate Combination (SeretideTM) at a Dose of 50/100µg Twice Daily and Fluticasone Propionate (FlixotideTM) at a Dose of 200µg Twice Daily [NCT00353873]Phase 4506 participants (Actual)Interventional2005-11-18Completed
Comparing Treatment Efficacy With High and Medium Dose of Fluticasone in Combination With Salmeterol in COPD Patients [NCT01131806]Phase 4124 participants (Anticipated)Interventional2009-12-31Recruiting
"Clinical Evaluation of GW815SF for Chronic Obstructive Pulmonary Disease (Chronic Bronchitis, Emphysema) A Long-term Treatment Study of GW815SF50/500µg in Chronic Obstructive Pulmonary Disease -" [NCT00269087]Phase 3122 participants (Actual)Interventional2005-01-28Completed
A 1-Year Safety Study of Medium and High Doses of Mometasone Furoate/Formoterol Combination Formulation and Medium and High Doses of Fluticasone/Salmeterol in Persistent Asthmatics Previously Treated With Medium to High Doses of Inhaled Glucocorticosteroi [NCT00379288]Phase 3404 participants (Actual)Interventional2006-06-30Completed
Sub-Sensitivity to Long-Acting Bronchodilators (LABA) [NCT01117116]21 participants (Actual)Interventional2010-03-31Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 500 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharm [NCT03751202]Phase 134 participants (Actual)Interventional2018-11-20Completed
A Single Dose, Placebo-controlled, Randomized, Double-blind, Double-dummy, Crossover Efficacy, Pharmacokinetics and Safety Comparison of Salmeterol Inhalation Powder (12.5 μg, 25 μg and 50 Salmeterol), Administered as the Xinafoate Salt From Hard Polyethy [NCT02238106]Phase 2136 participants (Actual)Interventional2005-09-30Completed
1-yr Study Comparing TioSal Combo Regimens Versus Single Agent Therapies (Spiriva HandiHaler and Salmeterol PE Capsule) [NCT00662740]Phase 3220 participants (Actual)Interventional2008-04-15Terminated
Effect of High Dose Inhaled Budesonide and Fluticasone on Adrenal Function in Patients With Moderate to Severe COPD [NCT01186653]Phase 422 participants (Actual)Interventional2007-10-31Completed
A PHASE III, RANDOMIZED, OPEN-LABEL, NON-INFERIORITY COMPARATIVE STUDY BETWEEN SERETIDE® 50/250 µG AND SALMETEROL/FLUTICASONE SINGLE INHALATION CAPSULE 50/250 µG EUROFARMA IN PATIENTS WITH ASTHMA [NCT01202097]Phase 3334 participants (Anticipated)Interventional2011-08-31Completed
A Double-Blind, Randomized Multicenter, 3-Period, Crossover Study to Evaluate the Effects of a Single Dose of Montelukast Compared With Placebo and Salmeterol on Exercise-Induced Bronchoconstriction [NCT00245570]Phase 347 participants (Actual)Interventional2005-12-31Completed
Personalized Treatment Algorithms for Difficult-to-treat Asthma: Bench to Community [NCT04179461]Phase 221 participants (Actual)Interventional2018-03-16Completed
Acute and Chronic Effects of an Anticholinergic Agent or a Long-Acting Beta 2 Agonist on Levels of Exhaled Nitric Oxide and Pulmonary Function in Persons With Tetraplegia [NCT01355991]Phase 140 participants (Anticipated)Interventional2011-08-31Active, not recruiting
A Randomized, Double-blind, Placebo-controlled, Parallel-group, 12-week Proof-of-Concept (PoC) Study to Assess the Efficacy, Safety, and Tolerability of SAR440340 and the Coadministration of SAR440340 and Dupilumab in Patients With Moderate-to-Severe Asth [NCT03387852]Phase 2296 participants (Actual)Interventional2018-03-12Completed
An Exploratory, Double-blind, Placebo-controlled Study of the Effects of Dupilumab on Airway Inflammation of Adults With Persistent Asthma [NCT02573233]Phase 242 participants (Actual)Interventional2016-01-27Completed
Double-Blinded, Placebo-Controlled, Randomized, 2 Period, Crossover Phase 1/2a Study Testing Safety/Efficacy of Advair HFA (Salmeterol, Fluticasone) in Resting & Exercising Healthy & High Altitude Pulmonary Edema (HAPE) Predisposed Subjects [NCT06040268]Phase 1/Phase 260 participants (Anticipated)Interventional2023-12-12Recruiting
A Double-dummy, Double-blind, Randomized, Parallel-group, Active Controlled Study to Evaluate the Efficacy and Safety of QVM149 (Indacaterol Acetate / Glycopyrronium Bromide / Mometasone Furoate) Compared to Salmeterol Xinafoate/Fluticasone Propionate in [NCT05776927]Phase 3304 participants (Anticipated)Interventional2024-12-23Not yet recruiting
A Phase III, Randomized, Double-blind, Active Controlled, Parallel Group Study, Comparing the Efficacy, Safety and Tolerability of the Fixed Dose Combination FF/UMEC/VI With the Fixed Dose Dual Combination of FF/VI, Administered Once-daily Via a Dry Powde [NCT02924688]Phase 32,436 participants (Actual)Interventional2016-10-13Completed
A Randomized, Double-blind, Double-dummy, Active-controlled, Multi-center, Parallel Group Study to Show the Superiority in Lung Function of 12 Weeks Once Daily Treatment With Orally Inhaled Tiotropium+Olodaterol Fixed Dose Combination Delivered by the Res [NCT03240575]Phase 4302 participants (Actual)Interventional2017-08-14Completed
Special Drug Use Investigation for ADOAIR DISKUS COPD (Salmeterol and Fluticasone) [NCT01332409]2,000 participants (Actual)Observational2009-08-31Completed
Phase I Single Blind, Randomised, Cross-over Pharmacodynamic Dose Response Study in Healthy Volunteers of Two Pressurized Metered Dose Inhalers (pMDIs) That Deliver Salmeterol and Fluticasone Propionate [NCT02232087]Phase 152 participants (Actual)Interventional2014-07-31Completed
A 4-week Dose-Ranging, Dose-Interval, Efficacy, Safety and Tolerability Study of GSK961081 in Subjects With Chronic Obstructive Pulmonary Disease (COPD) [NCT01319019]Phase 2437 participants (Actual)Interventional2010-12-31Completed
A Single-dose, Randomised, Crossover, Placebo-controlled, Double-dummy, Pharmacodynamic Clinical Trial Assessing Two Fixed Dose Combinations of Long-acting Beta-agonist (LABA) and Inhaled Corticosteroid (ICS) [NCT02094274]Phase 130 participants (Actual)Interventional2013-11-30Completed
A Multicenter, Partially-Blinded, Randomized, 24-Week, Parallel-Group, Non-Inferiority, Open-Label Active Controlled Study to Compare the Efficacy and Safety of QVM149 With a Free Triple Combination of Salmeterol/Fluticasone + Tiotropium in Patients With [NCT03158311]Phase 31,426 participants (Actual)Interventional2018-02-05Completed
A Single-centre, Double-blind, Double-dummy, Randomised, Crossover Study to Investigate the Effect of Formoterol HFA-pMDI Versus Salmeterol HFA-pMDI on Small Airways Physiological Parameters in COPD Patients [NCT01344655]Phase 416 participants (Actual)Interventional2011-04-30Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 100 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharm [NCT05697003]Phase 134 participants (Anticipated)Interventional2023-02-17Active, not recruiting
A Randomised, Open-label Four-way Crossover Study to Evaluate Pharmacokinetics of Salmeterol (Serevent®) After Inhalation of a 25 μg and 50 μg Single Dose (Metered Dose Inhaler) and a 50 μg and 100 μg Single Dose (Diskus®) in Healthy Male Volunteers [NCT02254226]Phase 126 participants (Actual)Interventional2004-11-30Completed
A Randomised, Double-Blind, Double-Dummy, Placebo-Controlled, Crossover Comparison of the Effect of 6-Week Treatment Periods of Tiotropium Inhalation Capsules (18 μg) and Salmeterol Inhalation Aerosol on Muscular Efficiency and Resting Energy Expenditure [NCT02172794]Phase 348 participants (Actual)Interventional2002-05-31Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study to Examine the Bioequivalence Between Fluticasone Propionate 250 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharmaceuticals vs. SERETIDE D [NCT03894280]Phase 136 participants (Actual)Interventional2019-03-12Completed
A Stratified, Multicenter, Randomized, Double-Blind, Parallel Group, 4-Week Comparison of Fluticasone Propionate/Salmeterol DISKUS Combination Product 100/50mcg BID Versus Fluticasone Propionate DISKUS 100mcg BID in Pediatric and Adolescent Subjects With [NCT00118716]Phase 4248 participants (Actual)Interventional2003-12-23Completed
A Multicenter, Double-Blind, Randomized, Crossover Design Study to Evaluate the Effect of Montelukast Vs. Salmeterol on the Inhibition of Exercise-Induced Bronchoconstriction in Asthmatic Patients Aged 6-14 Years [NCT00127166]Phase 3154 participants (Actual)Interventional2005-12-31Completed
A Single-blind, Randomized, Active-controlled, Multi-center and Phase IV Study to Evaluate the Small Airway Parameters of Fluticasone/Formoterol (Flutiform®) Compared to Fluticasone/Salmeterol in Asthma Patients [NCT02491970]Phase 415 participants (Actual)Interventional2015-08-31Terminated(stopped due to Difficulty of patients enrollments)
Feasibility of a Personalised Medicine Clinic for Children With Asthma Aged 5-11 Years [NCT03269318]Phase 42 participants (Actual)Interventional2017-07-01Terminated(stopped due to Change to Primary Endpoint resulted in development of new protocol)
A Multicenter Randomized 52 Week Treatment Double-blind, Triple Dummy Parallel Group Study to Assess the Efficacy and Safety of QMF149 Compared to Mometasone Furoate in Patients With Asthma [NCT02554786]Phase 32,216 participants (Actual)Interventional2015-12-29Completed
A Phase IIA Randomised, Double-blind, Double Dummy, Placebo and Active Controlled 5-Way Cross-over Trial to Examine the Bronchodilator Effects of PF-610,355 and to Test for Superiority Versus Placebo in Reversible Asthmatic Patients [NCT00468975]Phase 242 participants Interventional2007-05-31Completed
Is Adenosine Monophosphate Superior to Histamine for Bronchial Provocation Test in Evaluation of Asthma? [NCT02318043]84 participants (Actual)Interventional2007-01-31Completed
A 12-Week, Randomized, Double-Blind, Placebo-Controlled, Efficacy and Safety Study of Fluticasone Propionate Multidose Dry Powder Inhaler Compared With Fluticasone Propionate/Salmeterol Multidose Dry Powder Inhaler in Patients Aged 4 Through 11 Years With [NCT02980133]Phase 3841 participants (Actual)Interventional2016-12-28Completed
A Multicenter, Randomized, Parallel-group, Placebo-controlled, 4-week Clinical Endpoint Bioequivalence Study Comparing Fluticasone Propionate/Salmeterol 100/50 µg Inhalation Powder With Advair® Diskus 100/50 µg in Asthma Patients [NCT03394989]Phase 31,366 participants (Actual)Interventional2018-10-17Completed
A Randomised, Open Label, Four-way Crossover Phase I Trial to Investigate the in Vivo Specificity of a Single Oral Dose of 320 mg KUC 7483 CL Co-administered With Bisoprolol (10 mg Daily), Propranolol (160 mg Daily), and Acipimox (500 mg Daily) Over 5 Day [NCT02256722]Phase 112 participants (Actual)Interventional2005-10-31Completed
A Phase III, Randomized, Multicenter, Parallel-group Clinical Trial for Examining the Therapeutic Equivalence Between Fluticasone Propionate 100 mcg and Salmeterol 50 mcg Inhalation Powder/Respirent Pharmaceuticals vs. ADVAIR DISKUS® 100/50 mcg Inhalation [NCT03676413]Phase 3451 participants (Actual)Interventional2018-10-02Completed
Evaluation of the Effect of 2 Weeks Treatment With CHF 4226 pMDI 2µg and 4µg, Given Once Daily in the Morning, on 24-Hour FEV1 in Patients With COPD [NCT00640484]Phase 257 participants (Actual)Interventional2008-04-30Completed
A Randomised, Open-label, 4-way Crossover Study to Characterize the Pharmacokinetics, Safety and Efficacy of FDC Tiotropium/Salmeterol, Tiotropium, Salmeterol and a Free Combination of Tiotropium Plus Salmeterol Following 4-week Treatment Periods in Patie [NCT00673478]Phase 350 participants (Actual)Interventional2008-05-31Completed
A 24-week Treatment, Multi-center, Randomized, Double-blind, Double-dummy, Parallel Group Study to Compare Umeclidinium/Vilanterol, Umeclidinium, and Salmeterol in Subjects With Chronic Obstructive Pulmonary Disease (COPD) [NCT03034915]Phase 42,696 participants (Actual)Interventional2017-06-16Completed
A Randomized, Parallel-Group, Placebo-Controlled, Clinical Endpoint Bioequivalence Study of Generic Fluticasone Propionate 100 μg and Salmeterol Xinafoate 50 μg Inhalation Powder Compared With Advair Diskus® 100/50 in Subjects With Asthma [NCT03535870]1,556 participants (Actual)Interventional2018-04-26Completed
A Phase 2b, Parallel Group, Placebo And Active Comparator Controlled Study To Investigate The Safety, Toleration And Efficacy Of 6-Week Once Daily Administration Of Inhaled PF-00610355 Dry Powder In Patients With Moderate Chronic Obstructive Pulmonary Dis [NCT00808288]Phase 2405 participants (Actual)Interventional2010-03-31Completed
Comparison of Healthcare Utilization and Costs in Patients With Asthma Who Fluticasone/Salmeterol Inhalation Powder Versus Other Inhaled Corticosteroid(s) in Typical Clinical Practice Using Health Insurance Claims Data. [NCT01332344]5,180 participants (Actual)Observational2009-06-30Completed
Special Drug Use Investigation for ADOAIR Metered-dose Inhaler (Pediatric) [NCT01332422]300 participants (Actual)Observational2009-11-30Completed
A Randomised, Phase II, Double-Blind, Double-Dummy, Four-period Crossover Efficacy and Safety Comparison of 4-Week Treatment Periods of Blinded Fluticasone (500 mcg Bid, MDI), Ciclesonide (400 mcg qd, MDI), Ciclesonide (800 mcg qd, MDI) or Placebo in Free [NCT00535366]Phase 2103 participants (Actual)Interventional2007-10-31Completed
Effect of an Inhaled Glucocorticoid-long-acting Beta Adrenergic Agonist on Endothelial Function in COPD [NCT01209715]Phase 20 participants (Actual)Interventional2010-10-31Withdrawn(stopped due to Due to the ubiquitous use of ICS in the treatment of COPD in 2012, it was hard to find the study population.)
Long-term Effects of Inhaled Corticosteroids (ICS) Treatment on Sputum Bacterial and Viral Loads in Chronic Obstructive Pulmonary Disease (COPD) Patients [NCT01213693]60 participants (Actual)Interventional2009-05-31Completed
A Pivotal, Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 250 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respir [NCT04466176]Phase 134 participants (Actual)Interventional2020-07-01Completed
Inspiratory Capacity and HRCT Comparison of Nebulized Arformoterol (Brovana) vs. Dry-powder Inhaler Salmeterol (Serevent) [NCT01361984]Phase 420 participants (Anticipated)Interventional2011-06-30Recruiting
A Pilot Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 250 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent [NCT04462822]Phase 114 participants (Actual)Interventional2020-08-24Completed
A Retrospective Evaluation of the Effectiveness of Fixed-dose Combination Inhaled Corticosteroid /. Long-acting Beta Agonist (ICS/LABA) Therapy in the Management of Asthma in a Representative UK Primary Care Population [NCT01141465]815,377 participants (Actual)Observational2001-01-31Completed
Effects on Small Airways Obstruction of Two Long-term Treatments With Extrafine Beclomethasone/Formoterol vs Fluticasone/Salmeterol in Asthma [NCT01255579]Phase 410 participants (Actual)Interventional2007-07-31Completed
A Randomized, Multiple-Dose, Blinded, Placebo-Controlled, Parallel-Design, Multiple-Center, Clinical Study to Evaluate the Therapeutic Equivalence of Fluticasone Propionate and Salmeterol Inhalation Powder, 100 mcg/50 mcg to ADVAIR DISKUS® 100/50 (Flutica [NCT03756883]Phase 3999 participants (Actual)Interventional2018-12-03Completed
A Multi-centre, Randomized, Double-blind, Placebo-controlled Phase III Study to Evaluate the Efficacy and Safety of Anti-IgE Monoclonal Antibody to Treat Allergic Asthma Patients Not Adequately Controlled Despite Med/High ICS/LABA. [NCT03468790]Phase 3393 participants (Actual)Interventional2018-05-09Completed
Comparison of Bronchodilator Efficacy of Tiotropium/Salmeterol/Fluticasone 9/50/500 mcg Combination Treatment Administered Via Discair® With Original Products Seretide Diskus 500 mcg Inhalation Powder Plus Spiriva 18 mcg Inhalation Powder Treatment in Pat [NCT03395002]Phase 458 participants (Actual)Interventional2018-03-22Completed
A Randomized, Double-blind, Double-dummy, Active-controlled, 3-period Complete Cross-over Study to Assess the Bronchodilator Effect and Safety of Two Doses of QVM149 Compared to a Fixed Dose Combination of Salmeterol/Fluticasone in Patients With Asthma [NCT03063086]Phase 2116 participants (Actual)Interventional2017-01-21Completed
A Multi-center, Open-label, Randomized, Controlled Study to Evaluate the Effectiveness of Yong Chong Cao Capsule on Outcomes in Patients With Mild to Severe COPD [NCT03745261]Phase 3240 participants (Anticipated)Interventional2018-06-20Recruiting
A Randomized, Double-blind, Parallel Group, Multicenter, Stratified Study Evaluating the Efficacy and Safety of Repeat Doses of GSK3772847 Compared With Placebo in Participants With Moderately Severe Asthma [NCT03207243]Phase 2165 participants (Actual)Interventional2017-09-14Completed
An Exploratory, Randomised, Double-blind, Double-dummy, Active-controlled, Two Period Cross-over Study to Investigate the Effect of 6 Weeks Treatment of Orally Inhaled Tiotropium + Olodaterol Fixed Dose Combination (FDC) Delivered by the Respimat® Inhaler [NCT03055988]Phase 476 participants (Actual)Interventional2017-03-29Completed
Randomized, Double-blind, Placebo-controlled, Parallel Group Study to Assess the Efficacy, Safety, and Tolerability of SAR231893/REGN668 Administered Subcutaneously Once Weekly for 12 Weeks in Patients With Persistent Moderate to Severe Eosinophilic Asthm [NCT01312961]Phase 2104 participants (Actual)Interventional2011-03-31Completed
Effect of Salmeterol on Brain-Derived Neurotrophic Factor (BDNF) Concentrations in Asthma [NCT00736801]35 participants (Actual)Interventional2005-09-30Completed
A Phase 2 Randomized, Placebo-Controlled, Double-Blind Study to Evaluate the Safety and Efficacy of LIPO-202 for the Reduction of Central Abdominal Bulging in a Defined Special Population - Obese Subjects (BMI > or Equal to 30 kg/m2) [NCT02568319]Phase 2120 participants (Anticipated)Interventional2015-09-30Completed
A 2-year Observational Study to Evaluate Safety of Seretide 50/500μg Twice Daily Administered by DISKUS, in Patients With COPD [NCT00662805]762 participants (Actual)Observational2004-06-30Completed
Pilot Study to Examine the Post-Dose Changes in Exhaled Nitric Oxide (eNO) Following Treatment With Fluticasone Propionate (FP)/Salmeterol (SAL) Combination Product Advair [NCT00927758]Phase 2105 participants (Actual)Interventional2009-06-30Completed
A Randomised, Open-label Three-way Crossover Study to Evaluate the Pharmacokinetics of Salmeterol After Inhalation of a 25 μg and 50 μg Single Dose (Inhalation Powder, Hard PE Capsule for HandiHaler®2) and a 50 μg Single Dose (Serevent® Diskus®) in Health [NCT02254187]Phase 130 participants (Actual)Interventional2005-09-30Completed
A Multiple Dose Comparison of Tiotropium Inhalation Capsules, Salmeterol Inhalation Aerosol and Placebo in a Six-Month, Double-Blind, Double-Dummy, Safety and Efficacy Study in Patients With Chronic Obstructive Pulmonary Disease (COPD) [NCT02172287]Phase 3623 participants (Actual)Interventional1999-02-28Completed
A Multiple Dose Comparison of Tiotropium Inhalation Capsules, Salmeterol Inhalation Aerosol and Placebo in a Six-Month, Double-Blind, Double-Dummy, Safety and Efficacy Study in Patients With Chronic Obstructive Pulmonary Disease (COPD) [NCT02173691]Phase 3584 participants (Actual)Interventional1999-02-28Completed
An Open-Label, Crossover Study to Determine the Pharmacokinetic Profile and Tolerability of Single Doses of High Strength Fluticasone Propionate Multidose Dry Powder Inhaler and Fluticasone Propionate/Salmeterol Multidose Dry Powder Inhaler Compared to Hi [NCT02437604]Phase 143 participants (Actual)Interventional2015-05-31Completed
Effectiveness of Single Inhaler Maintenance and Reliever Therapy With Spiromax® Budesonide/Formoterol (SMART) Versus Fixed Dose Treatment With Diskus® Fluticasone/Salmeterol in Patients With a Chronic Obstructive Pulmonary Disease (COPD) [NCT02477397]Phase 3201 participants (Actual)Interventional2015-05-01Active, not recruiting
Pharmacokinetic Study Comparing Salmeterol/Fluticasone Easyhaler Products and Seretide Diskus 50/500 µg/Inhalation: A Randomised, Open, Single Centre, Single Dose, Crossover Study in Healthy Subjects [NCT03060044]Phase 164 participants (Actual)Interventional2016-07-31Completed
Phase IV Study; Strategy for Early Treatment of Exacerbations in COPD: Standing Prescriptions of Advair With a Written Action Plan in the Event of an Exacerbation [NCT02136875]Phase 437 participants (Actual)Interventional2008-07-31Completed
Pharmacokinetic Study Comparing Salmeterol/Fluticasone Easyhaler Products and Seretide Diskus 50/500 µG/Inhalation; A Randomised, Open, Single Centre, Single Dose, Crossover Study in Healthy Subjects [NCT02162485]Phase 1129 participants (Actual)Interventional2014-06-30Completed
Seretide 100 DK vs Flixotide 100 DK in IMT in Moderate Asthma in Adults on Static Lung Volumes (Mechanistic Study) [NCT00461500]Phase 481 participants (Actual)Interventional2007-03-31Completed
The Impact of Salmeterol-Fluticasone on Sleep in Patients With COPD (Advair and Quality of Sleep in COPD) [NCT00741767]0 participants (Actual)Interventional2008-08-31Withdrawn(stopped due to Study subject enrollment difficulties)
A Double-blind, Randomised, Cross-over, Multi-centre Study, to Evaluate Onset of Effect in the Morning in Patients With Severe Chronic Obstructive Pulmonary Disease (COPD) Treated With Symbicort®Turbuhaler® 320/9 μg, Compared With Seretide® Diskus® 50/500 [NCT00542880]Phase 4442 participants (Actual)Interventional2007-09-30Completed
A Phase III, Randomized, Double-blind, Triple-dummy, Placebo Controlled, Multicenter, 5-period, Single-dose Complete Block Crossover Study to Determine the Onset of Action of Indacaterol (150 and 300 μg) in Patients With Moderate to Severe COPD Using Salb [NCT00669617]Phase 389 participants (Actual)Interventional2008-04-30Completed
A Randomized, Double-blind, Parallel Group Study Evaluating the Safety of Fluticasone Propionate/Salmeterol 100/50mcg HFA (2 Inhalations of 50/25mcg) Twice Daily Compared With Fluticasone Propionate 100mcg HFA (2 Inhalations of 50mcg) Twice Daily in Subje [NCT00441441]Phase 3351 participants (Actual)Interventional2007-02-28Completed
Blood and Urinary Concentrations of Inhaled Salmeterol in Asthmatic Subjects and Elite Athletes With Asthma. [NCT00914901]Phase 430 participants (Anticipated)Interventional2009-07-31Not yet recruiting
A Randomized, Controlled,14-Treatment Day, Multicenter Study to Determine the Optimal Efficacious and Safe Dose of CHF 4226 in a Metered Dose Inhaler in Treating Patients With Chronic Obstructive Pulmonary Disease [NCT00605891]Phase 2278 participants (Actual)Interventional2006-10-31Completed
Childhood Asthma Research and Education (CARE) Network Trial - Montelukast or Azithromycin for Reduction of Inhaled Corticosteroids in Childhood Asthma (MARS) [NCT00471809]Phase 4210 participants Interventional2006-03-31Terminated(stopped due to The CARE Network DSMB recommended to the NHLBI that the MARS trial be terminated, based on a futility analysis with 55 randomized children.)
A Randomized, Multicenter, Placebo and Active-Controlled, Single-Dose, 4-Period, Crossover Study to Evaluate the Bronchodilating Effect of SYMBICORT pMDI Versus Advair Diskus and Ventolin HFA. [NCT00646620]Phase 348 participants (Actual)Interventional2003-04-30Completed
STUDY NUMBER: PMC-101-APT Usability and Adherence of Spiromax® Inhaler Device, Turbohaler® and Diskus® Inhaler Devices for Fixed Combination of Corticosteroid/Long-acting beta2- Agonist, in Adults With Asthma or COPD [NCT02757209]84 participants (Actual)Interventional2016-04-30Completed
A 12 Month Open-label Randomized Parallel Group Study to Investigate the Influence of Salmeterol Xinafoate/Fluticasone Propionate Either in Fixed Combination or Separately Via Diskus Inhalers on the Course of the Disease and Frequency of Exacerbations in [NCT00527826]Phase 4214 participants (Actual)Interventional2007-11-30Completed
Onset of Action of Advair HFA 115/21 in Comparison to Symbicort pMDI 160/4.5 Measured by Impulse Oscillometry, IOS. [NCT00867737]Phase 430 participants (Anticipated)Interventional2008-09-30Recruiting
A Double-blind, Randomized, Cross-over, Placebo-controlled, 2-part Study to Compare the Effect of Exercise and High-dose Salbutamol on Maximal Heart-rate in Patients With COPD Following Therapeutic Doses of Inhaled QAB149 and Salmeterol [NCT00531050]Phase 227 participants (Actual)Interventional2007-08-31Completed
A Randomized, Double-Blind, Parallel-Group Clinical Trial Evaluating the Effect of the Fluticasone Propionate/Salmeterol Combination Product 250/50mcg Twice Daily Via DISKUS® Inhaler Versus Salmeterol 50mcg Twice Daily Via DISKUS® Inhaler on Bone Mineral [NCT00355342]Phase 4186 participants (Actual)Interventional2004-04-28Completed
Effect of Inhalation of Tiotropium Once Daily 18 Mcg Versus Salmeterol Twice Daily 50 Mcg on Time to First Exacerbation in COPD Patients (a Randomised, Double-blind, Double-dummy, Parallel Group, One-year Study). [NCT00563381]Phase 47,376 participants (Actual)Interventional2008-01-31Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 100 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharm [NCT03975166]Phase 134 participants (Actual)Interventional2019-05-21Completed
Effect of Charcoal on Gastrointestinal Absorption of Salmeterol and Fluticasone Propionate. [NCT01564199]Phase 120 participants (Actual)Interventional2012-04-30Completed
A Randomised, Open-label Four-way Crossover Study to Evaluate Relative Bioavailability of Tiotropium and Salmeterol After Inhalation of a Fixed Combined Single Dose (7.5 μg Tiotropium, 25 μg Salmeterol, Inhalation Powder, Hard Capsule, HandiHaler®2), a Fr [NCT02254174]Phase 136 participants (Actual)Interventional2006-03-31Completed
A 12 Week Treatment, Multi-center, Randomized, Parallel Group, Double Blind, Double Dummy Study to Assess the Superiority of Indacaterol (150 µg o.d.) Via a SDDPI in Patients With Moderate to Severe COPD, Using Salmeterol (50 µg b.i.d.) as an Active Compa [NCT00821093]Phase 31,123 participants (Actual)Interventional2009-01-31Completed
A Double-Blind, Double-Dummy, Randomized, Placebo- and Active-Controlled, Multicenter, Parallel-Group Study of (R,R)-Formoterol in the Treatment of Subjects With Chronic Obstructive Pulmonary Disease [NCT00685841]Phase 3717 participants (Actual)Interventional2002-02-28Completed
A Randomized, Double-Blind, Parallel-Group, 24-Week Study to Evaluate the Efficacy and Safety of ADVAIR DISKUS (Fluticasone Propionate/Salmeterol Combination Product 250/50mcg Inhalation Powder) BID Plus Spiriva HandiHaler (Tiotropium Bromide Inhalation P [NCT00784550]Phase 4342 participants (Actual)Interventional2008-12-31Completed
A Study to Compare GW815SF HFA MDI With Concomitant Treatment With Salmeterol Xinafoate DPI Plus Fluticasone Propionate DPI and to Assess Long-term Safety of GW815SF HFA MDI [NCT00448435]Phase 351 participants (Actual)Interventional2007-04-30Completed
Yiqi Huoxue Huatan Granule for Reducing Mortality in COPD With Chronic Respiratory Failure: A Randomized, Double-blind, Placebo Controlled Trial [NCT04208581]Phase 3372 participants (Anticipated)Interventional2019-10-08Enrolling by invitation
A Randomised, Double-blind, Double-dummy, Parallel-group Multicentre Study to Assess Efficacy and Safety of Fluticasone Furoate/GW642444 Inhalation Powder and Fluticasone Propionate/Salmeterol Inhalation Powder in the Treatment of Persistent Asthma in Adu [NCT01147848]Phase 3810 participants (Actual)Interventional2010-06-30Completed
A Randomised, Double-blind, Active-controlled Study to Evaluate the Impact of Stepwise Withdrawal of Inhaled Corticosteroid Treatment in Patients With Severe to Very Severe Chronic Obstructive Pulmonary Disease (COPD) on Optimized Bronchodilator Therapy [NCT00975195]Phase 42,488 participants (Actual)Interventional2009-02-28Completed
A Randomized, Multicenter, Placebo and Active-controlled, Single-dose, 4-period, Crossover Study to Evaluate the Bronchodilating Effect of SYMBICORT pMDI Versus Advair Diskus and Ventolin HFA. [NCT00646009]Phase 348 participants (Anticipated)Interventional2003-03-31Completed
Investigator Initiated, Placebo Controlled, Randomized Pilot Trial on the Influence of Fluticasone and Salmeterol on Airway Dendritic Cells (DCs) in Smokers With COPD Stage GOLD 0 or 1. [NCT00908362]Phase 145 participants (Anticipated)Interventional2009-05-31Completed
A Randomized, Double-blind, Double-dummy, Placebo-controlled, Parallel-group Study to Assess the Efficacy and Safety of Different Doses of Indacaterol in Adult Patients With Persistent Asthma, Using Salmeterol as an Active Control [NCT01079130]Phase 3511 participants (Actual)Interventional2010-02-28Completed
A Randomized, Double-Blind, Parallel Group Study of ADVAIR™ DISKUS™ 100/50 and FLOVENT™DISKUS™ 100, Both Twice Daily, in a Pediatric Population During the Fall Viral Season. [NCT01192178]Phase 4339 participants (Actual)Interventional2010-08-31Completed
A Phase III, Randomized, Double-blind, Placebo-controlled, Multicenter, 3-period, 14-day Crossover Study to Determine the 24 Hour Lung Function Profile of Indacaterol (300 µg Once Daily [od]) in Patients With Moderate-to-severe COPD, Using Open-label Salm [NCT00622635]Phase 368 participants (Actual)Interventional2008-01-31Completed
A Randomized, Double-Blind, Cross-Over Study to Demonstrate Superiority of Fluticasone/Salmeterol Over Double the Dose of Fluticasone on Methacholine Hyper-Reactivity in Patients With Persistent, Mild to Moderate Asthma [NCT00830505]Phase 438 participants (Actual)Interventional2009-04-30Completed
The Treatment Effect of Inhaled Corticosteroid and Long-acting beta2 Agonist Combination Versus Long-acting Anti-cholinergic Agent on Stratified COPD Patients Based on the Levels of Exhaled Nitric Oxide [NCT02546349]Phase 4143 participants (Anticipated)Interventional2014-07-31Active, not recruiting
Study of Salmeterol (SN408D) for Adult Asthma - Clinical Study of Salmeterol Compared With Hokunalin (Tulobuterol) Tape - [NCT00950794]Phase 4367 participants (Actual)Interventional2003-09-30Completed
A Two Stage Randomized, Open-Label, Parallel Group, Phase III, Multicenter, 7 Month Study to Assess the Efficacy & Safety of SYMBICORT pMDI Adminstered Either as Fixed or as an Adjustable Regimen Versus a Fixed Regimen of Advair in Subjects 12 Yrs of Age [NCT00646594]Phase 31,200 participants (Anticipated)Interventional2003-11-30Completed
A Randomized, Parallel-Group, Placebo-Controlled, Clinical Endpoint Bioequivalence Study of Generic Fluticasone Propionate 100 µg and Salmeterol Xinafoate 50 µg Inhalation Powder Compared With Advair Diskus® 100/50 in Subjects With Asthma [NCT02649478]1,430 participants (Actual)Interventional2014-08-31Completed
Arg/Arg Genotype and Long Acting Beta Agonists in Asthma. Improved Quality of Care for Patients With Asthma. [NCT00521222]90 participants (Actual)Interventional2007-06-30Completed
A Dose Ranging Study of the Safety and Efficacy of LIPO-202 Healthy Patients With Subcutaneous Fat in the Periumbilical Area [NCT01802723]Phase 2472 participants (Actual)Interventional2013-02-28Completed
A Proof of Concept Study to Evaluate Effects of Intranasal Salmeterol and Fluticasone Given Alone and in Combination in Allergic Rhinitis [NCT01388595]Phase 423 participants (Actual)Interventional2006-11-30Completed
Multicenter, Phase III, Randomized, Open Label Study to Evaluate the Efficacy and Safety of a Fixed-dose Combination of Formoterol/Fluticasone and Salmeterol/Fluticasone in Patients With Moderate-to-severe Chronic Obstructive Pulmonary Disease (COPD). [NCT01393145]Phase 30 participants (Actual)Interventional2011-08-31Withdrawn
Drug Use Investigation for ADOAIR (Fluticasone/Salmeterol) [NCT01395849]2,116 participants (Actual)Observational2007-10-31Completed
Outcomes for Chronic Obstructive Pulmonary Disease Moderate Exacerbators Initiating Treatment [NCT01395875]2,849 participants (Actual)Observational2011-03-31Completed
Pharmacological Properties of Inhaled Salmeterol in Healthy Trained Males [NCT02558088]Phase 411 participants (Actual)Interventional2014-09-30Completed
A Randomized, Open Label, Multicenter, Phase 4 Study for the Comparison of Efficacy of Tiotropium Plus Salmeterol/ Fluticasone Propionate Compared With Tiotropium Alone in COPD Patients [NCT00864812]Phase 4509 participants (Actual)Interventional2009-03-31Completed
A Randomized, Double-Blind, Parallel Group, Multicenter Study of the Effects of Fluticasone Propionate/Salmeterol Combination Product 250/50mcg BID (ADVAIR DISKUS™) in Comparison to Salmeterol 50mcg BID (SEREVENT DISKUS™) on the Rate of Exacerbations of C [NCT01110200]Phase 4639 participants (Actual)Interventional2010-04-30Completed
Effect of Inhalation of a Free Combination of Tiotropium Once Daily 18 Mcg and Salmeterol Twice Daily 50 Mcg Versus a Fixed Combination of Fluticasone and Salmeterol Twice Daily (500/50 Mcg) on Static Lung Volumes and Exercise Tolerance in COPD Patients ( [NCT00530842]Phase 4344 participants (Actual)Interventional2007-09-30Completed
A Comparison of Symbicort® Single Inhaler Therapy (Symbicort Turbuhaler® 160/4.5mg, 1 Inhalation Two Times a Day (b.i.d.) Plus as Needed) and Conventional Best Practice for the Treatment of Persistent Asthma in Adults a -26-week, Randomized, Open-label, P [NCT00628758]Phase 3430 participants (Actual)Interventional2005-12-31Completed
A Multicenter, Randomized, Double-Blind, Triple-Dummy, Placebo-Controlled, Parallel Group, Four-Week Study Assessing the Efficacy of Fluticasone Propionate Aqueous Nasal Spray 200mcg QD Versus Montelukast 10mg QD in Adolescent and Adult Subjects With Asth [NCT00296491]Phase 4725 participants (Actual)Interventional2005-09-30Completed
Investigating the Mechanism of Inhaled Corticosteroids Associated Pneumonia by Longitudinal Characterisation of the Airway Microbiome in Patients With Severe COPD [NCT02972476]Phase 4158 participants (Actual)Interventional2016-12-31Completed
A Randomised, Double-blind Clinical Efficacy and Safety Comparison of Tiotropium/Salmeterol 7.5/25 Inhalation Powder in the Morning Via Tiotropium/Salmeterol HandiHaler, Tiotropium 18 Mcg Inhalation Powder in the Morning Via Spiriva HandiHaler, Salmeterol [NCT00662792]Phase 3147 participants (Actual)Interventional2008-04-15Completed
A Randomized, Double-Blind, Parallel Group, 52-Week Study to Compare the Effect of Fluticasone Propionate/Salmeterol DISKUS® Inhaler Combination Product 250/50mcg Twice Daily With Salmeterol DISKUS® Inhaler 50mcg Twice Daily on the Annual Rate of Moderate [NCT00144911]Phase 4740 participants (Actual)Interventional2004-10-31Completed
Comparison of Stepwise Treatment of Asthmatic Children With Salmeterol/Fluticasone Propionate Combination Product (Seretide®) and/or Fluticasone Propionate (Flixotide®) Based on PD20 Methacholine and Symptoms or Based on Symptoms Only (Children Asthma The [NCT00158834]Phase 3200 participants Interventional1999-11-30Completed
A 26-week Treatment, Multi-center, Randomized, Double-blind, Double- Dummy, Placebo-controlled, Parallel-group Study to Assess the Efficacy, and Safety of Indacaterol (150 µg o.d.) in Patients With Chronic Obstructive Pulmonary Disease, Using Salmeterol ( [NCT00567996]Phase 31,002 participants (Actual)Interventional2007-11-30Completed
A 26-week Treatment, Randomized, Multicenter, Double-blind, Double-dummy, Parallel-group Study to Assess the Safety of Indacaterol (300 and 600 µg o.d.) in Patients With Moderate to Severe Persistent Asthma, Using Salmeterol (50 µg b.i.d.) as an Active Co [NCT00529529]Phase 3805 participants (Actual)Interventional2007-09-30Completed
A 52-Week Efficacy and Safety Non-Inferiority Study of Fluticasone Propionate/Salmeterol 250/50mcg BID Delivered by Dry Powder Inhaler (Diskus) Versus Mometasone Furoate/Formoterol Fumarate 200/10mcg BID Delivered by Pressurized Metered-Dose Inhaler in Pe [NCT00424008]Phase 3722 participants (Actual)Interventional2007-04-30Completed
A 52-week, Randomized, Double-Blind, Parallel-Group Study of Fluticasone Propionate/Salmeterol DISKUS Combination Product (FSC) 250/50 mcg BID and Fluticasone Propionate (FP) DISKUS 250 mcg BID in Treatment of Subjects With Asthma [NCT00452348]Phase 4628 participants (Actual)Interventional2007-05-31Completed
A Randomized, Double-blind, Placebo-controlled, 4-period 4-treatment Crossover, Multicenter, Single-dose, Dose-ranging Study Followed by a Single Day's Treatment With Open Label Salmeterol Bid (100 µg/Day), to Assess the Efficacy and Safety of 3 Doses of [NCT00403754]Phase 241 participants (Actual)Interventional2006-11-30Completed
Childhood Asthma Research and Education (CARE) Network Trial - Best Add-On Therapy Giving Effective Response (BADGER) [NCT00395304]Phase 3182 participants (Actual)Interventional2007-03-31Completed
Asthma Control Assessment Via ACT and DRC in Asthmatics Treated With Seretide (50/250) Over 12 Weeks [NCT00363480]Phase 4221 participants (Actual)Interventional2006-05-17Completed
Asthma Clinical Research Network (ACRN) Trial - Long-Acting Beta Agonist Response by Genotype (LARGE) [NCT00200967]Phase 387 participants (Actual)Interventional2004-12-31Completed
An Exploratory Study to Evaluate the Response of Salmeterol Plus Fluticasone vs Fluticasone Alone to Experimental Nasal Inoculation With Rhinovirus [NCT00503009]Phase 416 participants (Actual)Interventional2007-10-31Terminated(stopped due to lack of data)
The Leukotriene Modifier Or Corticosteroid or Corticosteroid-Salmeterol Trial [NCT00156819]Phase 4500 participants (Actual)Interventional2003-06-30Completed
A 52-week, Randomized, Double-Blind, Parallel-Group Study of Fluticasone Propionate/Salmeterol DISKUS Combination Product (FSC) 250/50 mcg BID and Fluticasone Propionate (FP) DISKUS 250 mcg BID in Treatment of Subjects With Asthma [NCT00452699]Phase 4621 participants (Actual)Interventional2007-05-31Completed
A Randomized, Double-blind, Double-dummy, Placebo-controlled, Parallel-group Study to Assess the Efficacy and Safety of Different Doses of Indacaterol in Patients With Moderate to Severe Chronic Obstructive Pulmonary Disease, Using Salmeterol as an Active [NCT01089127]Phase 3552 participants (Actual)Interventional2010-03-31Completed
A Pilot Study to Assess the Incidence of Local Oropharyngeal and Laryngeal Adverse Effects of Advair DISKUS 250/50 Mcg BID as Assessed by the Development of Laryngitis and Oropharyngeal Candidiasis in Adults With Mild Persistent Asthma [NCT00235053]Phase 413 participants Interventional2005-08-31Active, not recruiting
A Randomized, Double-blind, Double-dummy, Parallel-group, Placebo Controlled (on Inhaled Corticosteroid Medication), Multicenter Study to Evaluate the Efficacy and Safety of Vilanterol Inhalation Powder (GW642444) and Salmeterol, Compared With Placebo in [NCT01181895]Phase 3348 participants (Actual)Interventional2010-09-01Completed
Evaluation of the Effects of Varying Doses of Inhaled Corticosteroids on Suppression of Total Exhaled, Bronchial, and Alveolar Nitric Oxide as Markers of Endogenous Inflammation in Patients With Moderate-to-severe COPD [NCT00568347]39 participants (Actual)Observational2006-01-31Completed
A Multicentre, Randomised, Double-blind, Parallel Group Study to Compare the Efficacy and Safety of Salmeterol/Fluticasone Propionate Combination Product (Seretide®) 50/100 mcg With Fluticasone Propionate (Flixotide® ) 200 mcg, Both Delivered Twice Daily [NCT00197106]Phase 4176 participants (Actual)Interventional2005-06-30Completed
A Study of Fluticasone Propionate/Salmeterol DISKUS Combination Product 250/50 mcg Twice Daily Plus Tiotropium 18 mcg Daily Versus Placebo DISKUS Twice Daily Plus Tiotropium 18 mcg Daily on Exercise Time and Physiological Parameters in Subjects With Chron [NCT01124422]Phase 4255 participants (Actual)Interventional2010-07-19Completed
A Pilot, Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 500 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respiren [NCT04546256]Phase 114 participants (Actual)Interventional2020-09-01Completed
WEUSRTP4850: Phase II: Asthma Treatment in Pregnancy and the Frequency of Adverse Pregnancy Outcomes [NCT01681979]1 participants (Actual)Observational2012-07-31Completed
A Multi-center, Randomized, Double-blind, Controlled Study to Evaluate the Effectiveness of on Severe / Very Severe COPD Patients [NCT02270424]Phase 3564 participants (Anticipated)Interventional2014-10-31Not yet recruiting
A Phase III Randomised, Double-blind, Placebo-controlled, Parallel-group Trial to Evaluate Efficacy and Safety of Tiotropium Inhalation Solution Delivered Via Respimat® Inhaler (2.5 and 5 µg Once Daily) Compared With Placebo and Salmeterol HFA MDI (50 µg [NCT01172821]Phase 31,032 participants (Actual)Interventional2010-08-31Completed
A 12-week Study to Evaluate the 24 Hour Pulmonary Function of Fluticasone Furoate (FF)/Vilanterol Inhalation Powder (FF/VI Inhalation Powder) Once Daily Compared With Salmeterol/Fluticasone Propionate (FP) Inhalation Powder Twice Daily in Subjects With Ch [NCT01342913]Phase 3528 participants (Actual)Interventional2011-02-01Completed
A 12-week Study to Evaluate the 24-hour Pulmonary Function Profile of Fluticasone Furoate/Vilanterol (FF/VI) Inhalation Powder 100/25 mcg Once Daily Compared With Fluticasone Propionate/Salmeterol Inhalation Powder 250/50 mcg Twice Daily in Subjects With [NCT01323621]Phase 3512 participants (Actual)Interventional2011-03-18Completed
The Effects of Montelukast on Sputum Cells and Inflammatory Markers in Smokers With Asthma [NCT00712335]Phase 4105 participants (Actual)Interventional2007-02-28Completed
A Phase III Randomized, Double Blind, Double Dummy, Placebo Controlled, Multicenter, 4 Treatments, 3 Period Incomplete Block Crossover Study to Assess the Efficacy and Safety of Indacaterol 300 µg o.d. Dosed in the Evening in Patients With Moderate to Sev [NCT00615030]Phase 396 participants (Actual)Interventional2008-01-31Completed
A Proof-of-concept Study to Evaluate the Benefit From add-on Therapy With Montelukast Versus Salmeterol in Children With Asthma Carrying the Arg/Arg-16 beta2-receptor Genotype [NCT00655616]64 participants (Actual)Interventional2007-08-31Completed
Prescribing Asthma Controller Medication According to Gene Status to Improve Quality of Life in Young People With Asthma [NCT02758873]241 participants (Actual)Interventional2016-02-29Completed
A Phase III Randomised, Double-blind, Placebo-controlled, Parallel-group Trial to Evaluate Efficacy and Safety of Tiotropium Inhalation Solution Delivered Via Respimat® Inhaler (2.5 and 5 µg Once Daily) Compared With Placebo and Salmeterol HFA MDI (50 µg [NCT01172808]Phase 31,071 participants (Actual)Interventional2010-08-31Completed
A 52-week Treatment, Multi-center, Randomized, Open Label, Parallel Group Study to Assess the Long Term Safety and Efficacy of Indacaterol (300 µg o.d.) Using Salmeterol (50 µg b.i.d.) as an Active Control in Japanese Patients With Chronic Obstructive Pul [NCT00876694]Phase 3186 participants (Actual)Interventional2009-03-31Completed
Dose-ranging Study of the Safety and Efficacy of Fluticasone Propionate and Salmeterol Xinafoate in Healthy Patients With Abdominal Contour Defects [NCT01712451]Phase 2200 participants (Actual)Interventional2011-08-31Completed
Multi-centre, DB, R and Stratified Parallel Group Study to Compare the Efficacy and Safety of FP 500mcg Bid vs. SRT 50/250mcg Via Diskus in COPD Pts With Partial Reversible Obstruction [NCT00549146]Phase 3290 participants (Actual)Interventional2003-11-30Completed
"CONNected Electronic Inhalers Asthma Control Trial 2 (CONNECT 2), a 24-Week Treatment, Multicenter, Open-Label, Randomized, Parallel Group Comparison, Feasibility Study of Standard of Care Treatment Versus the eMDPI Digital System, to Optimize Outcomes i [NCT04677959]Phase 4427 participants (Actual)Interventional2021-02-16Completed
Special Drug Use Investigation for ADOAIR (Fluticasone/Salmeterol) [NCT01395862]1,001 participants (Actual)Observational2007-11-30Completed
Randomised, Double-blind, Double-dummy, Parallel-group, Comparative Study of Salmeterol/FP 50/100mcg bd Inhalation Powder Via Diskus With Oral Montelukast (5mg QD) Chewable Tablets in Children 6-14 Years [NCT00328718]Phase 3526 participants Interventional2005-10-31Completed
Observed Outcomes Associated With Fluticasone Propionate/Salmeterol Xinafoate or Inhaled Corticosteroids in Asthma Patients [NCT01431924]7,779 participants (Actual)Observational2010-10-31Completed
A Randomized, Double-blind, Parallel-group Study of Fluticasone Propionate/Salmeterol Combination (FSC 250/50mcg) Twice Daily and Salmeterol (SAL 50mcg) Twice Daily to Validate a New Shortness of Breath Questionnaire in Patients With Chronic Obstructive P [NCT00411372]Phase 30 participants (Actual)Interventional2006-11-30Withdrawn(stopped due to No subjects enrolled. Study was canceled before active)
Modification of Disease Outcome in COPD. Shortterm Versus Longterm Treatment With Inhaled Corticosteroids, Either or Not Combined With a Long-Acting Beta2-Agonist. [NCT00158847]Phase 4200 participants Interventional2000-04-30Terminated
Acute Bronchodilation and Bronchial Inflammation: Nitric Oxyde Concentration in Chronic Obstructive Pulmonary Disease Patients. Stretching of Airways and Nitric Oxide in Bronchodilation, SANOB Study [NCT01853787]Phase 449 participants (Actual)Interventional2014-07-31Completed
A 12-week Treatment, Multi-center, Randomized, Double-blind, Double-dummy, Parallel-group Study to Assess the Efficacy, Safety and Tolerability of QVA149 Compared to Fluticasone/Salmeterol in COPD Patients With Moderate to Severe Airflow Limitation [NCT01860066]Phase 30 participants (Actual)Interventional2013-12-31Withdrawn
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 500 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharm [NCT06025214]Phase 134 participants (Anticipated)Interventional2023-08-22Recruiting
A Randomized, Double-Blind, Double-Dummy, Parallel Group 12-Week Comparison of the Efficacy and Safety of Fluticasone Propionate/Salmeterol Hydrofluoroalkane 134a Metered-Dose-Inhaler 230/42mcg Twice-daily With Fluticasone Propionate/Salmeterol DISKUS 250 [NCT00633217]Phase 4247 participants (Actual)Interventional2008-03-31Completed
A Four Year Observational Study Comparing Two Treatment Regimens: Inhaled Glucocorticosteroid + Salmeterol and Inhaled Glucocorticosteroid + Montelukast. [NCT01488773]132 participants (Actual)Observational1995-04-30Completed
A Multicentre, Randomised, Partially Blinded, Placebo-controlled, Three-way Crossover, Incomplete Block Design Study to Investigate the Safety, Tolerability, Pharmacodynamics/ Efficacy and Pharmacokinetics of Dual Bronchodilator Therapy With Salmeterol 50 [NCT00422604]Phase 260 participants (Actual)Interventional2006-10-31Completed
Salmeterol Improves Fluid Clearance From Alveolar-Capillary Membrane in COPD Patients [NCT01271556]20 participants (Actual)Interventional2008-12-31Completed
A Randomized, Open Label Comparative Study to Determine the Proportion of Asthma Patients on SERETIDE Diskus 50/250 mcg b.i.d. Achieving Total Control When Given Medication and Compliance Enhancement Training Compared to Those Receiving Medication Only [NCT00351143]Phase 4274 participants (Actual)Interventional2005-07-26Completed
Randomised, Double-blind, Double-dummy, 52-week, Parallel Group Study of a Standard Dosing Regimen With Salmeterol/Fluticasone propionate50/250 Twice Daily Diskus Versus a Symptom-driven, Variable Dosing Regimen With Formoterol/Budesonide Combination 4.5/ [NCT00479739]Phase 4700 participants (Actual)Interventional2002-11-30Completed
A 26-week Treatment, Multi-center, Randomized, Doubleblind, Double Dummy, Parallel-group Study to Assess the Efficacy, Safety and Tolerability of QVA149 Compared to Fluticasone/Salmeterol in Patients With Moderate to Severe Chronic Obstructive Pulmonary D [NCT01315249]Phase 3523 participants (Actual)Interventional2011-03-31Completed
Retrospective, Real-life Observational, Matched Cohort Evaluation of the Effectiveness of BDP/FOR (Fostair® 100/6) and FP/SAL (Seretide® 125) in Patients Switching From Seretide to Fostair in UK Primary Care Asthma Management [NCT01242098]137 participants (Actual)Observational2008-01-31Completed
Effects of Salmeterol on Walking Capacity in Patients With COPD [NCT00525564]Phase 428 participants (Actual)Interventional2006-05-31Completed
Obesity, Inflammation and Response to Therapy in Asthma - Ancillary to Asthma Clinical Research Network (ACRN) Trials [NCT00557180]33 participants (Actual)Observational2007-10-31Completed
A Randomized, Double-blind, Two-way Cross-over Study Evaluating Systemic Bioavailability and Airway Clearance of SymbicortTurbuhaler 320/9mcg vs SeretideDiskus 50/500mcg After Single Inhalations in Patients With COPD and Healthy Volunteers [NCT00379028]Phase 454 participants (Actual)Interventional2006-09-30Completed
The Effect of Salmeterol on Eosinophil (EOS) Function [NCT00214019]36 participants (Actual)Interventional2003-11-30Completed
A Single Dose, Placebo-controlled, Randomized, Double-blind, Double-dummy, Crossover Efficacy, Pharmacokinetics and Safety Comparison of Salmeterol Inhalation Powder (25 μg Salmeterol), Administered as the Xinafoate Salt From a Hard Polyethylene Capsule V [NCT02242227]Phase 2111 participants (Actual)Interventional2005-09-30Completed
A Multi-enter, Randomized, Double-blind, Placebo-controlled, Four-way Incomplete Block Crossover Study to Examine Efficacy, Safety, Tolerability, Pharmacodynamics and Pharmacokinetics of Single and Repeat Administration of Three Inhaled Doses (10, 15, and [NCT00358488]Phase 254 participants (Actual)Interventional2006-04-30Completed
A Multicenter, Open-Label, Randomized, Active-Controlled, Parallel Group Chronic Safety Study of (R,R)-Formoterol in the Treatment of Subjects With Chronic Obstructive Pulmonary Disease [NCT00064415]Phase 3799 participants (Actual)Interventional2002-06-30Completed
Randomized, Double-Blind Comparison of Advair 100/50 BID vs Salmeterol BID vs Albuterol QID in Subjects With ARG/ARG Genotype 12 Years of Age and Older With Presistent Asthma on Short-Acting Beta2-Agonists Alone [NCT00102882]Phase 4547 participants (Actual)Interventional2004-10-31Completed
A 13-week, Double-blind, Parallel Group, Multi-centre Study to Compare the Bronchial Anti-inflammatory Activity of the Combination of Salmeterol/Fluticasone Propionate 50/500mcg Twice Daily Compared With Placebo Twice Daily in Patients With Chronic Obstru [NCT00268177]Phase 3130 participants Interventional2002-10-31Completed
A Multicentre, Randomised, Double-blind, Parallel Group, Placebo-controlled Study to Investigate the Long-term Effects of Salmeterol/Fluticasone Propionate (Seretide tm) 50/500mcg BD, Salmeterol 50mcg BD and Fluticasone Propionate 500mcg BD, All Delivered [NCT00268216]Phase 36,228 participants (Actual)Interventional2000-09-30Completed
A Comparison of the Effects of Tiotropium (18 Mcg) Inhalation Capsule q.d. and Salmeterol (50 Mcg) Inhalation Aerosol b.i.d. on Arterial Blood Gases in a Double-blind, Double-dummy, 4-week Crossover Study in Patients With Chronic Obstructive Pulmonary Dis [NCT00274534]Phase 336 participants Interventional2000-12-31Completed
A Multicentre, Stratified, Randomised, Double Blind, Parallel Group Trial to Evaluate Whether a Treatment Strategy Based on Aiming for Total Control Results in Better AHR Than a Treatment Strategy Based on Maintaining Well Control [NCT00291382]Phase 4150 participants (Actual)Interventional2005-11-30Completed
A Multicenter, Randomized, Double-Blind, Parallel Group, 52-Week Comparison of Asthma Control and Measures of Airway Inflammation in Subjects of African Descent Receiving Fluticasone Propionate/Salmeterol 100/50mcg DISKUS® BID or Fluticasone Propionate 10 [NCT00102765]Phase 4479 participants (Actual)Interventional2004-11-30Completed
A Multicenter, Randomized, Double-Blind, Triple-Dummy, Placebo-Controlled, Parallel Group, Four-Week Study Assessing the Efficacy of Fluticasone Propionate Aqueous Nasal Spray 200mcg QD Versus Montelukast 10mg QD in Adolescent and Adult Subjects With Asth [NCT00296530]Phase 4600 participants (Actual)Interventional2005-09-30Completed
A Pilot Study of the Mechanism of Synergism Between Fluticasone (FP) and Salmeterol in Preventing Chronic Obstructive Pulmonary Disease (COPD) Exacerbations [NCT00116402]Phase 115 participants (Actual)Interventional2005-01-31Completed
SUccessful Control and Clinical Effectiveness of SERETIDE Study in aSthma, a Randomised Controlled Study to Investigate the Clinical Effectiveness and Health Outcome of SERETIDE in Patients With Moderate and Severe Persistent Asthma in Korea [NCT00480649]Phase 4424 participants (Actual)Interventional2004-01-31Completed
An Open Label, Multicentre Study to Evaluate Patient Satisfaction With Fluticasone/Salmeterol HFA MDI With Counter in Adult Subjects (18 Years of Age and Older) With Asthma or COPD. [NCT00404261]Phase 4132 participants (Actual)Interventional2007-01-31Completed
Clinical Assessment of GW815SF Salmeterol/Fluticasone Propionate (HFA MDI) in Pediatric Patients With Bronchial Asthma -A Long Term (24-week) Study- [NCT00449046]Phase 340 participants (Actual)Interventional2007-03-31Completed
Asthma Clinical Research Network (ACRN) Trial - Tiotropium Bromide as an Alternative to Increased Inhaled Corticosteroid in Patients Inadequately Controlled on a Lower Dose of Inhaled Corticosteroid (TALC) [NCT00565266]Phase 3210 participants (Actual)Interventional2008-05-31Completed
Genotype Stratified Treatment With Anticholinergic vs. Beta-agonist (Long Acting) and Exacerbations (GABLE) [NCT00706446]255 participants (Actual)Interventional2008-06-30Terminated(stopped due to Funding was terminated)
Interactive Acute Smooth Muscle Effects of Salmeterol and Fluticasone in the Airway [NCT01231230]14 participants (Actual)Interventional2007-05-31Completed
Outcomes and Costs Associated With Initiating Maintenance Treatment With Fluticasone Propionate 250mcg/Salmeterol Xinafoate 50mcg Combination (FSC) Versus Anticholinergics Including Tiotropium (TIO) in Patients With Chronic Obstructive Pulmonary Disease ( [NCT01331694]76,130 participants (Actual)Observational2009-07-31Completed
Outcomes for Medicare Asthma Patients Taking Fluticasone Propionate/Salmeterol Xinafoate Combination Versus Inhaled Corticosteroids or Other Combination Therapy [NCT01347060]17,448 participants (Actual)Observational2009-07-31Completed
A Six-Week, Randomized, Double-Blind, Quadruple-Dummy Parallel Group Multiple Dose Study Comparing the Efficacy and Safety of Tiotropium Inhalation Capsules Plus Formoterol Inhalation Capsules to Salmeterol Inhalation Aerosol Plus Fluticasone Inhalation A [NCT00239421]Phase 4605 participants Interventional2003-11-30Completed
A Six-Week, Randomised, Double-Blind, Triple-Dummy, Parallel Group, Multiple Dose, Pilot Study Comparing Tiotropium Inhalation Capsules to Salmeterol Inhalation Aerosol Combined With Fluticasone Inhalation Aerosol in Patients With Chronic Obstructive Pulm [NCT00239499]Phase 4107 participants Interventional2003-09-30Completed
A 6-week Randomized, Double-blind, Placebo-controlled, Crossover Study to Assess the Effect of Fluticasone 250μg/Salmeterol 50μg Combination (FSC 250/50) on Exertional Dyspnea in Patients With Symptomatic Mild COPD [NCT00559312]18 participants (Actual)Interventional2007-12-31Completed
Efficacy and Safety of Symbicort ®Turbuhaler® 160/4.5 µg/Inhalation, Two Inhalations Twice Daily Plus As-needed Compared With Seretide™ Diskus™ 50/500 µg/Inhalation, One Inhalation Twice Daily Plus Terbutaline Turbuhaler 0.4 mg/Inhalation As-needed - a 6- [NCT00242775]Phase 32,100 participants Interventional2005-05-31Completed
A Multi-Center, Randomized, Double-Blind, Parallel-Group, Dose-Finding Trial to Evaluate the Safety and Efficacy of Fluticasone Propionate Combined With Formoterol Fumarate in Patients With Chronic Obstructive Pulmonary Disease [NCT00403286]Phase 2457 participants (Actual)Interventional2006-11-30Completed
Efficacy and Safety of Salmeterol/Fluticasone Propionate vs Ipratropium/Albuterolin Chinese Patients With Moderate-to-severe COPD. [NCT01243788]Phase 4450 participants (Anticipated)Interventional2009-07-31Recruiting
A 12-week Study to Evaluate the 24-hour Pulmonary Function Profile of Fluticasone Furoate/Vilanterol (FF/VI) Inhalation Powder 100/25 mcg Once Daily Compared With Fluticasone Propionate/Salmeterol Inhalation Powder 250/50 mcg Twice Daily in Subjects With [NCT01323634]Phase 3519 participants (Actual)Interventional2011-03-18Completed
Prospective, Randomised, Open-label, Multicentre, Active Drug Controlled, Parallel Group Design Clinical Trial of the Efficacy and Safety of Beclomethasone Dipropionate 400 mcg + Formoterol 24 mcg pMDI Via HFA-134a (Foster™) vs. Fluticasone Propionate 500 [NCT00497237]Phase 3382 participants (Anticipated)Interventional2007-04-30Completed
Management of Asthma in School-age Children on Therapy [NCT01526161]Phase 4229 participants (Actual)Interventional2009-04-30Completed
A Randomized, Double-Blind, Parallel Group, 52-Week Study to Compare the Effect of Fluticasone Propionate/Salmeterol Diskus Combination Product 250/50mcg BID With Salmeterol Diskus 50mcg BID on the Annual Rate of Moderate/Severe Exacerbations in Subjects [NCT00115492]Phase 4797 participants (Actual)Interventional2004-12-31Completed
A Stratified, Multicenter, Randomized, Double-Blind, Parallel Group, 4-Week Comparison of Fluticasone Propionate/Salmeterol DISKUS Combination Product 100/50mcg BID Versus Fluticasone Propionate DISKUS 100mcg BID in Pediatric and Adolescent Subjects With [NCT00118690]Phase 4227 participants (Actual)Interventional2003-12-31Completed
A Double-Blind, Double-Dummy, Randomized, Placebo- and Active-Controlled, Multicenter, Parallel-Group Study of (R,R)-Formoterol in the Treatment of Subjects With Chronic Obstructive Pulmonary Disease [NCT00064402]Phase 3741 participants (Actual)Interventional2002-04-30Completed
DOUBLE BLIND, MULTINATIONAL, MULTICENTRE, PARALLEL-GROUP DESIGN CLINICAL TRIAL OF THE EFFICACY AND TOLERABILITY OF CHF 1535 (BECLOMETHASONE DIPROPIONATE 100 µg + FORMOTEROL 6 µg) pMDI VIA HFA-134a vs. FLUTICASONE 125 µg + SALMETEROL 25 µg pMDI (SERETIDE®) [NCT00394368]Phase 3180 participants Interventional2004-11-30Completed
Randomised, Double-blind Parallel Group Study to Assess the Bronchodilative and Bronchoprotective Properties of SERETIDE DISKUS ® Inhlaer 50/100mcg Twice Daily vs. FLIXOTIDE® Inhaler 200mcg Twice Daily. [NCT00169546]Phase 464 participants (Actual)Interventional2003-01-31Completed
The Effect of Beta-2 Adrenergic Polymorphisms on the Bronchoprotective Effects of Regular Salmeterol Treatment in Asthma [NCT00595361]30 participants (Actual)Interventional2008-01-31Completed
A 12-week Treatment, Multi-center, Randomized, Double-blind, Double-dummy, Parallel-group Study to Assess the Efficacy, Safety and Tolerability of QVA149 Compared to Fluticasone/Salmeterol in COPD Patients With Moderate to Severe Airflow Limitation [NCT01834885]Phase 30 participants (Actual)Interventional2013-12-31Withdrawn
A Randomised, Placebo-controlled, Double-blind (Double-dummy Technique),Crossover, Multi-centre Study, to Evaluate Onset of Effect in Patients With Chronic Obstructive Pulmonary Disease (COPD) Treated With Formoterol Turbuhaler® 9 μg, Compared With Sereve [NCT01048333]Phase 2109 participants (Actual)Interventional2010-01-31Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 250 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharm [NCT05982990]Phase 134 participants (Actual)Interventional2023-08-01Active, not recruiting
Dose-response of Salmeterol Delivered by Advair Diskus in Children: Bioassay by Methacholine Challenge Using Oscillometry as the Endpoint [NCT01907334]Phase 410 participants (Actual)Interventional2013-08-31Completed
A Pivotal, Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 500 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respir [NCT04564456]Phase 134 participants (Actual)Interventional2020-09-22Completed
Expression of Inflammatory Mediators in Induced Sputum: A Potential Biomarker of Drug Response in COPD [NCT00233051]20 participants (Actual)Interventional2003-04-30Terminated
A Randomised, Two Treatment, Four-Way Cross-Over (Replicate Design), Two Sequence, Repeat Dose Study in Patients With Moderate Asthma to Compare Pharmacokinetics and Pharmacodynamic Effects of Fluticasone Propionate and Salmeterol Delivered Via the Low Ai [NCT02218762]Phase 10 participants (Actual)Interventional2014-10-31Withdrawn(stopped due to It was decided that data from this study are no longer required and therefore it is not necessary to expose patients to the study medication)
A Comparison of Symbicort Single Inhaler Therapy (Symbicort Turbuhaler 160/4.5 µg, 1 Inhalation b.i.d. Plus as Needed) and Conventional Best Practice for the Treatment of Persistent Asthma in Adults - a 26-Week, Randomised, Open-Label, Parallel-Group, Mul [NCT00252863]Phase 31,600 participants Interventional2004-12-31Completed
See Detailed Description [NCT00269126]Phase 3150 participants (Actual)Interventional2005-02-28Completed
An Open-label, Multi-centre, Randomized, Parallel Group Clinical Effectiveness Study to Determine the Level of Asthma Control in Adolescent and Adult Patients With ADVAIR Versus Usual Care for 24 Weeks. [NCT00273026]Phase 4680 participants Interventional2004-11-08Terminated
Steroid-sparing Management of the Salmeterol/Fluticasone 50/100µg b.i.d. Combination Compared to Fluticasone 200µg b.i.d. in Children and Adolescents With Moderate Asthma [NCT00315744]Phase 4285 participants (Actual)Interventional2004-11-04Completed
[NCT01657487]Phase 4120 participants (Anticipated)Interventional2010-04-30Recruiting
Chronic Obstructive Pulmonary Disease (COPD)-Related Healthcare Utilization and Costs After Discharge From a Hospitalization or Emergency Department Visit on a Regimen of Fluticasone Propionate-Salmeterol Combination Versus Other Maintenance Therapies [NCT01332461]5,677 participants (Actual)Observational2009-11-30Completed
WEUSKOP6416: Evaluating Serious Pneumonia in Subjects With Chronic Obstructive Pulmonary Disease (COPD) to Inform Risk Minimization: A Retrospective Observational Study [NCT01763463]1 participants (Actual)Observational2012-07-31Completed
A Randomized, Double-Blind, Chronic-Dosing (14 Days), 5-Period, 7-Treatment, Placebo-Controlled, Incomplete Block, Cross-Over, Multicenter, Dose-ranging Study to Assess the Efficacy and Safety of PT001 Relative to Placebo Metered Dose Inhaler and Open-Lab [NCT02433834]Phase 2248 participants (Actual)Interventional2015-05-27Completed
Chronic Obstructive Pulmonary Disease (COPD)-Related Outcomes and Costs for Patients on Combination Fluticasone Propionate-Salmeterol Xinafoate 250/50mcg Versus Anticholinergics in a Comorbid COPD-Depression/Anxiety Population [NCT01337336]1 participants (Actual)Observational2010-10-31Completed
Outcomes From Initial Maintenance Therapy With Fluticasone Propionate 250/Salmeterol 50 (FSC) or Tiotropium in Chronic Obstructive Pulmonary Disease [NCT01387178]22,223 participants (Actual)Observational2008-07-31Completed
An Exploratory, Multi-centre, Double-blind, Placebocontrolled Crossover Study, to Investigate the Bronchodilatory Efficacy of a Single Dose of Indacaterol in Fixed Combination With Mometasone Furoate Delivered Via a MDDPI (Twisthaler®) in Adult Patients W [NCT00556673]Phase 231 participants (Actual)Interventional2007-10-31Completed
A Multi-Center, Randomized, Double-Blinded, Placebo-Controlled Study Evaluating the Safety and Efficacy of LIPO-202 for the Reduction of Central Abdominal Bulging Due to Subcutaneous Fat in Non-Obese Subjects [NCT02398188]Phase 3793 participants (Actual)Interventional2015-04-09Completed
A Randomised, Open Label, Five-way Crossover Study to Assess the Systemic Exposure of Fluticasone Propionate and Salmeterol From SERETIDE/ADVAIR 250HFA MDI Alone and With AeroChamber-Max Spacer and VOLUMATIC Both in Their Washed and Unwashed States in Adu [NCT00369993]Phase 220 participants (Actual)Interventional2005-03-31Completed
Evaluating the Control of COPD Symptoms in Patients Treated With Tiotropium Bromide 18mcg Once Daily Alone, ADOAIR 50/250mcg Twice Daily Alone or ADOAIR 50/250mcg Plus Tiotropium Bromide 18mcg [NCT01762800]Phase 4407 participants (Actual)Interventional2013-02-28Completed
Replication of the INSPIRE Trial in Healthcare Claims Data [NCT05179512]98,278 participants (Actual)Observational2020-09-22Completed
Replication of the POET-COPD Trial in Healthcare Claims Data [NCT05083429]8,716 participants (Actual)Observational2020-09-22Completed
A Randomised, Double-blind, Double-dummy, Crossover Efficacy and Safety Comparison of 6-week Treatment Periods of the Free Combinations of Tiotropium Inhalation Powder Capsule (18 μg) QD + Salmeterol Metered Dose Inhaler (2 Puffs of 25 μg) QD or BID, Tiot [NCT02242253]Phase 297 participants (Actual)Interventional2003-09-30Completed
Multicentre, Randomised, Double-Blind, Double Dummy, Parallel Group, 104-week Study to Compare the Effect of the Salmeterol/Fluticasone Propionate Combination Product (SERETIDE*) 50/500mcg Delivered Twice Daily Via the DISKUS*/ACCUHALER* Inhaler With Tiot [NCT00361959]Phase 41,270 participants (Actual)Interventional2003-06-30Completed
TITLE: Double-blinded, Double-dummy, Study Comparing Fluticasone-salmeterol to Placebo in Patients With COPD and Associated Poor Sleep or Daytime Somnolence. [NCT00731770]Phase 410 participants (Actual)Interventional2009-01-31Completed
[NCT00005110]0 participants InterventionalSuspended
Fluticasone Propionate-salmeterol Combination Adherence in Patients With Chronic Obstructive Pulmonary Disease (COPD) [NCT01381471]11,060 participants (Actual)Observational2009-08-31Completed
Use of Fluticasone Propionate/Salmeterol Combination Post Emergency Department Visit [NCT01332357]6,139 participants (Actual)Observational2009-06-30Completed
Efficacy of Inhaling Bronchodilator Medications in Patients With Chronic Obstructive Pulmonary Disease Who Have a Low Peak Inspiratory Flow Rate [NCT01391559]20 participants (Actual)Interventional2011-07-31Completed
Validation of a New Shortness of Breath With Daily Activities Questionnaire in Patients With Chronic Obstructive Pulmonary Disease [NCT00984659]Phase 4366 participants (Actual)Interventional2009-10-29Completed
An Open-Label, Randomised, Two Treatment, Four-Way Cross-Over (Replicate Design), Two Sequence, Repeat Dose, Single Centre Study in Healthy Volunteers to Compare the Pharmacokinetics of Fluticasone Propionate/Salmeterol (100/50 mcg) Delivered Via the Low [NCT01890863]Phase 136 participants (Actual)Interventional2013-08-05Completed
Pooled Analysis of Individual Subjects' Data After Combining the Data From the Bioequivalence Studies Conducted for Fluticasone Propionate 250 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharmaceuticals (Test, T) vs ADVAIR DISKUS® 250/ [NCT04790838]82 participants (Actual)Observational2019-06-02Completed
A Randomized, Double-blind, Double-dummy, Parallel Group, Multicenter Study of Once Daily Fluticasone Furoate/Vilanterol 100/25 mcg Inhalation Powder, Twice Daily Fluticasone Propionate/Salmeterol 250/50 mcg Inhalation Powder, and Twice Daily Fluticasone [NCT02301975]Phase 31,526 participants (Actual)Interventional2015-03-01Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study to Examine the Bioequivalence Between Fluticasone Propionate 100 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharmaceuticals vs. SERETIDE D [NCT04124094]Phase 136 participants (Actual)Interventional2019-10-01Completed
A Randomized, Double-Blind, Parallel-Group, 12-Week Study to Evaluate the Anti-Inflammatory Effect of Fluticasone Propionate/Salmeterol DISKUS 250/50mcg BID Compared With Salmeterol DISKUS 50mcg Twice Daily in Subjects With Chronic Obstructive Pulmonary D [NCT00346749]Phase 4180 participants Interventional2006-12-31Terminated(stopped due to The study was terminated due to difficulties with finding sites and subjects willing to participate.)
Multi-centre, Randomised, Double-blind, Placebo-controlled, Four-way Incomplete Block Crossover Study, to Examine Efficacy, Safety, Tolerability, Pharmacodynamics and Pharmacokinetics of Single and Repeat Administration of Three Inhaled Doses (25, 100 and [NCT00347139]Phase 255 participants (Actual)Interventional2006-05-23Completed
Single-Centre Randomised Open Crossover Study to Examine the Influence of Different Internal Resistances of Discus and Turbohaler Respectively on the Effects of Salmeterol and Formoterol in Asthmatic Subjects [NCT00327353]Phase 477 participants Interventional2004-01-31Completed
A Multiple Dose Comparison of Tiotropium Inhalation Capsules and Salmeterol Inhalation Aerosol in a 12 Week, Randomized, Double-Blind, Double-Dummy Parallel Group Study in Patients With Chronic Obstructive Pulmonary Disease (COPD). [NCT00274560]Phase 3653 participants (Actual)Interventional2002-05-01Completed
A Phase III, Randomized, Multicenter, Parallel-group Clinical Trial for Examining the Therapeutic Equivalence Between Fluticasone Propionate 100 mcg and Salmeterol 50 mcg Inhalation Powder/Respirent Pharmaceuticals vs. ADVAIR DISKUS® 100/50 mcg Inhalation [NCT05664061]Phase 3451 participants (Anticipated)Interventional2023-01-30Recruiting
A 26-Week Open-Label Study to Assess the Long-Term Safety of Fluticasone Propionate Multidose Dry Powder Inhaler and Fluticasone Propionate/Salmeterol Multidose Dry Powder Inhaler in Patients 12 Years of Age and Older With Persistent Asthma [NCT02175771]Phase 3758 participants (Actual)Interventional2014-07-31Completed
A Six-Period Crossover, Dose-Ranging Study to Evaluate the Efficacy and Safety of Four Doses of FS Spiromax (Fluticasone Propionate/Salmeterol Xinafoate Inhalation Powder) Administered as Single Doses Compared With Single Doses of Fluticasone Propionate S [NCT01772368]Phase 272 participants (Actual)Interventional2013-01-31Completed
A Multicenter, Randomized, Double-blind, Parallel-group Study to Evaluate the Efficacy and Safety of the Addition of Umeclidinium Bromide (62.5mcg) Once-daily to Fluticasone Propionate/Salmeterol (250/50mcg) Twice-daily, Umeclidinium Bromide (125mcg) Once [NCT01772134]Phase 3617 participants (Actual)Interventional2013-01-01Completed
Blacks and Exacerbations on LABA vs. Tiotropium (BELT) [NCT01290874]Phase 31,070 participants (Actual)Interventional2011-03-30Completed
Uncontrolled Lower Respiratory Symptoms in the World Trade Center Survivor Program [NCT02024204]60 participants (Actual)Interventional2014-04-09Completed
A Randomized, Double-blind Placebo-controlled Study of Treatments With Salmeterol, Fluticasone Propionate and Their Combination to Evaluate Novel Endpoints in Patients With Chronic Obstructive Pulmonary Disease [NCT00358358]Phase 4163 participants (Actual)Interventional2006-03-31Completed
A Repeat Dose, Randomised, Double Blind, 2-way Crossover Study to Assess the Safety and Systemic Exposure of an Investigational Formulation Compared to Concurrent Administration of Individual Fluticasone Propionate 50 and Salmeterol 50 DISKUS Inhalers in [NCT00364442]Phase 112 participants (Actual)Interventional2005-01-28Completed
A Randomised, Double Blind, Placebo Controlled Study to Examine the Safety, Tolerability, Pharmacodynamics and Pharmacokinetic Profile of Single Inhaled Dry Powder Doses of GSK159802 in Healthy Male Subjects [NCT00364273]Phase 143 participants (Actual)Interventional2005-08-24Completed
Randomised, Double Blind, Parallel Group Study to Assess the Bronchodilative and Bronchoprotective Properties of SERETIDE DISKUS® Inhaler 50/100 mcg Twice Daily vs FLIXOTIDE® Inhaler 200 mcg Twice Daily [NCT00370591]Phase 448 participants (Actual)Interventional2002-12-31Completed
Mechanisms of Adverse Effects of Long-Acting Beta-Agonists in Asthma [NCT04503460]Phase 424 participants (Anticipated)Interventional2021-07-23Recruiting
Effects of Bronchodilatation With Salmeterol on the Autonomic Nervous System [NCT01536587]Phase 432 participants (Actual)Interventional2012-07-31Completed
Evaluation of Mechanism(s)Limiting Expiratory Airflow in Chronic, Stable Asthmatics Who Are Non-smokers [NCT01225913]Phase 450 participants (Anticipated)Interventional2007-10-31Recruiting
Evaluation of Mechanism(s)Limiting Expiratory Airflow in Chronic, Stable Asthmatics Who Are Non-smokers [NCT00576069]60 participants (Anticipated)Observational2007-10-25Recruiting
A Single-Dose, Randomized, Open-Label, Crossover, Pivotal, Comparative Bioavailability Study of Synflutide HFA 250/25 Inhaler and SeretideTM 250 EvohalerTM in Healthy Volunteers With Charcoal Block [NCT02466503]Phase 145 participants (Actual)Interventional2014-08-31Completed
A Single-Dose, Randomized, Open-Label, Crossover, Pivotal, Comparative Bioavailability Study of Synflutide HFA 250/25 Inhaler and SeretideTM 250 EvohalerTM in Healthy Volunteers Without Charcoal Block [NCT02466347]Phase 145 participants (Actual)Interventional2014-06-30Completed
A 12-Week, Double-Blind, Placebo-Controlled, Efficacy and Safety Study of Fluticasone Propionate Multidose Dry Powder Inhaler Compared With Fluticasone/Salmeterol Multidose Dry Powder Inhaler in Adolescent and Adult Patients With Persistent Asthma Symptom [NCT02141854]Phase 3882 participants (Actual)Interventional2014-06-30Completed
A Multicenter, Randomized, 52-week, Double-blind, Parallelgroup, Active Controlled Study to Compare the Efficacy and Safety of QVM149 With QMF149 in Patients With Asthma [NCT02571777]Phase 33,092 participants (Actual)Interventional2015-12-08Completed
Effect of Inhaled Mometasone/Formoterol Versus Inhaled Fluticasone/Salmeterol on Peripheral Airway Function in Asthma Patients [NCT02415179]52 participants (Actual)Interventional2015-05-31Completed
Use of Mobile Devices and the Internet to Streamline an Asthma Clinical Trial [NCT02061280]Phase 4108 participants (Actual)Interventional2013-10-31Completed
24-week Study to Evaluate Efficacy and Safety of the Combination Budesonide / Indacaterol vs Fluticasone / Salmeterol in Patients With COPD [NCT02055352]Phase 4222 participants (Actual)Interventional2014-05-30Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Bioequivalence Study With Pharmacokinetic Endpoints Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 250 mcg and Salmeterol Xina [NCT05085587]Phase 118 participants (Anticipated)Interventional2021-10-01Active, not recruiting
A Multi-Center, Randomized, Double-Blinded, Placebo-Controlled Study Evaluating the Safety and Efficacy of LIPO-202 for the Reduction of Central Abdominal Bulging Due to Subcutaneous Fat in Non-Obese Subjects [NCT02397499]Phase 3800 participants (Anticipated)Interventional2015-04-30Completed
1-yr Study Comparing TioSal Combo Regimens Versus Single Agent Therapies (Spiriva HandiHaler and Salmeterol PE Capsule) [NCT00668772]Phase 3207 participants (Actual)Interventional2008-04-15Terminated
A Guideline Approach to Therapy Step-down Utilising Flutiform Change and Step-down [NCT02388373]Phase 4225 participants (Actual)Interventional2014-07-31Completed
Long-acting Beta Agonist Step Down Study [NCT01437995]Phase 4459 participants (Actual)Interventional2012-03-31Completed
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of LIPO-202 (Salmeterol Xinafoate for Injection) for the Reduction of Submental Subcutaneous Fat [NCT03005717]Phase 2162 participants (Actual)Interventional2016-12-22Completed
A 12-week Treatment, Multi-center, Randomized, Double-blind, Double-dummy, Parallel Group Study to Assess the Efficacy and Safety of Switching From Salmeterol/Fluticasone to QVA149 (Indacaterol Maleate/Glycopyrronium Bromide) in Symptomatic COPD Patients [NCT02516592]Phase 4500 participants (Actual)Interventional2015-10-13Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 250 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharm [NCT03820180]Phase 134 participants (Actual)Interventional2019-01-23Completed
A Randomized, Single-dose, Open Label, Two-treatment, Two-sequence, Two-period, Crossover Study Under Fasting Conditions to Examine the Bioequivalence Between Fluticasone Propionate 250 mcg and Salmeterol Xinafoate 50 mcg Inhalation Powder/Respirent Pharm [NCT04746040]Phase 150 participants (Actual)Interventional2021-01-18Active, not recruiting
A Randomised, Double-blind, Double Dummy, 3 Way Cross-over Study Evaluating the Effects of ADOAIR 50/250mcg Twice Daily Plus Tiotropium Bromide 18mcg Once Daily Compared With the Individual Treatments (Tiotropium Bromide 18mcg Alone and ADOAIR 50/250mcg A [NCT01751113]Phase 453 participants (Actual)Interventional2013-02-28Completed
Randomized, Double-blind, Double-dummy, Active-controlled, 4 Period Complete Cross-over Study to Compare the Effect on Lung Function of 6 Weeks Once Daily Treatment With Orally Inhaled Tiotropium+Olodaterol Fixed Dose Combination Delivered by the Respimat [NCT01969721]Phase 3229 participants (Actual)Interventional2013-10-31Completed
Comparison of Conventional Medicine, TCM Treatment and Combination of Both Conventional Medicine and TCM Treatment for Patients With Chronic Obstructive Pulmonary Disease: A Randomized Comparative Effectiveness Research Trial [NCT01836016]Phase 3360 participants (Anticipated)Interventional2013-05-31Not yet recruiting
SAPS:Smoking Asthmatics Pilot Study: [NCT01696214]Phase 420 participants (Actual)Interventional2012-10-31Completed
A Double-Blind (Incorporating an Open Label Comparator), 3-Period, Crossover Study to Determine the Pharmacokinetic Profile and Tolerability of Single Doses of Fluticasone Propionate Multidose Dry Powder Inhaler and Fluticasone Propionate/Salmeterol Multi [NCT02680561]Phase 120 participants (Actual)Interventional2016-04-30Completed
A 26-week, Randomized, Double Blind, Parallel-group Multicenter Study to Assess the Efficacy and Safety of QVA149 (110/50 μg o.d.) vs Tiotropium (18 µg o.d.) + Salmeterol/Fluticasone Propionate FDC (50/500 µg b.i.d.) in Patients With Moderate to Severe CO [NCT02603393]Phase 41,053 participants (Actual)Interventional2015-11-20Completed
A Double Blind, Double Dummy, Randomized, Two Way Cross-over Study to Compare the Effects of Seretide® Evohaler (Supplied by Allen & Hanburys, UK) and a Generic Salmeterol/Fluticasone HFA pMDI (Manufactured by Cipla Ltd, India) on Functional Respiratory I [NCT01795664]Phase 316 participants (Actual)Interventional2013-03-31Completed
A Randomised, Double-blind, Double-dummy, Active-controlled Study Evaluating the Efficacy, Safety and Tolerability of Twice-daily Aclidinium Bromide/Formoterol Fumarate Compared With Twice-daily Salmeterol/Fluticasone Propionate for 24 Weeks Treatment in [NCT01908140]Phase 3933 participants (Actual)Interventional2013-09-30Completed
A Randomized, Double-blind, Double Dummy, Parallel Group Study to Determine the Local Equivalence of Multiple Doses of MGR001 to Advair Diskus Administered Via Oral Inhalation in Adult Asthma Patients [NCT02245672]Phase 31,128 participants (Actual)Interventional2014-10-31Completed
A Multi-center, Randomized, Double-blind, Double Dummy, Placebo and Active Controlled Crossover Study, to Investigate the 24 Hour FEV1 Profile of a Single Dose of QMF TWISTHALER Device in Adult Patients With Persistent Asthma [NCT00557440]Phase 237 participants (Actual)Interventional2007-11-30Completed
A Multicenter, Randomized, Double-blind, Parallelgroup Study to Evaluate the Efficacy and Safety of the Addition of Umeclidinium Bromide Inhalation Powder (62.5mcg) Once-daily to Fluticasone Propionate/Salmeterol (250/50mcg) Twice-daily, Umeclidinium Brom [NCT01772147]Phase 3608 participants (Actual)Interventional2013-01-31Completed
Salmeterol Xinafoate and Fluticasone Propinate Powder for Inhalation for Asthma: A Randomized, Double-blind, Double-dummy, Positive-controlled, Parallel-group Trail [NCT03461627]Phase 3300 participants (Anticipated)Interventional2017-04-01Recruiting
Individualized Dosing Schedule of Inhaled Bronchodilator for Endotracheally Intubated Chronic Obstructive Pulmonary Disease Patients [NCT01933984]51 participants (Actual)Interventional2013-08-31Completed
Randomised Controlled Single and Chronic Dosing Crossover Comparison of Extra Fine Particle Formoterol and Coarse Particle Salmeterol in Asthmatic Patients With Persistent Small Airways Dysfunction [NCT01892787]Phase 417 participants (Actual)Interventional2013-07-31Completed
A 1-year Multi-center, Prospective, Cohort Study in Patients With Chronic Obstructive Pulmonary Disease Treated With Long-acting Bronchodilator [NCT01794780]Phase 42,229 participants (Actual)Interventional2013-02-05Completed
A 12-Week Study to Evaluate the 24-Hour Pulmonary Function Profile of Fluticasone Furoate/Vilanterol (FF/VI) Inhalation Powder 100/25 mcg Once Daily Compared With Fluticasone Propionate/Salmeterol Inhalation Powder 250/50 mcg Twice Daily in Subjects With [NCT01706328]Phase 3828 participants (Actual)Interventional2012-10-15Completed
Clinical Endpoint Study of Salmeterol Xinafoate/Fluticasone Propionate Combination for Comparison of a Test and Reference Product in Patients With Asthma [NCT02260492]Phase 1879 participants (Actual)Interventional2014-09-30Completed
A 6-month, Open Label, Randomised, Efficacy Study to Evaluate Fluticasone Furoate (FF, GW685698)/Vilanterol (VI, GW642444) Inhalation Powder Delivered Once Daily Via the Dry Powder Inhaler ELLIPTA™ Compared With Usual ICS/LABA Maintenance Therapy Delivere [NCT02446418]Phase 3423 participants (Actual)Interventional2015-07-09Completed
A Pilot Study to Investigate Pharmacokinetic Characteristics After Co-administration of HCP0910 and HGP1011 [NCT02441114]Phase 110 participants (Actual)Interventional2015-07-31Completed
A Double Blind, Double Dummy, Randomised, Multicentre, Two Arm Parallel Group Study to Assess the Efficacy and Safety of FLUTIFORM® pMDI (2 Puffs Bid) vs Seretide® pMDI (2 Puffs Bid) in Subjects Aged ≥12 Years With Moderate to Severe Persistent, Reversibl [NCT03387241]Phase 3330 participants (Anticipated)Interventional2017-06-02Recruiting
Generation of Biological Samples Positive to Salmeterol for Anti-Doping Control [NCT04195867]Phase 14 participants (Actual)Interventional2018-11-20Completed
A 12-Week, Double-Blind, Placebo-Controlled, Efficacy and Safety Study of Fluticasone Propionate Multidose Dry Powder Inhaler Compared With Fluticasone/Salmeterol Multidose Dry Powder Inhaler in Adolescent and Adult Patients With Persistent Asthma Symptom [NCT02139644]Phase 3787 participants (Actual)Interventional2014-06-30Completed
DB2116134: A Randomized, Multi-center, Double-blind, Double-dummy, Parallel Group Study to Evaluate the Efficacy and Safety of Umeclidinium Bromide/Vilanterol Compared With Fluticasone Propionate/Salmeterol Over 12 Weeks in Subjects With COPD [NCT01822899]Phase 3717 participants (Actual)Interventional2013-04-04Completed
Randomized, Parallel, Placebo-controlled, Multiple Dose, Multicenter Study to Compare the Efficacy of Fluticasone/Salmeterol (Test) to Advair® Diskus (GSK) in Adult Asthma Patients [NCT02496715]Phase 30 participants (Actual)Interventional2015-09-30Withdrawn(stopped due to Development terminated.)
Comparison of Efficacy and Safety of Salmeterol/Fluticasone 50/500 mcg Inhalation Powder Treatment Administered Via Capsair and Original Product Seretide Diskus 500 mcg Inhalation Powder Treatment in Patients With Moderate-severe Chronic Obstructive Pulmo [NCT03363503]Phase 464 participants (Actual)Interventional2018-04-13Terminated(stopped due to Adequate number of patients could not be reached in the relevant centers.)
Pharmacokinetic Study Comparing Salmeterol/Fluticasone Easyhaler 50/250 µg/Dose Products and Seretide Diskus 50/250 µg/Dose in Healthy Subjects [NCT03238482]Phase 164 participants (Actual)Interventional2017-08-16Completed
A Multi-centre, Randomised, Double-blind, Placebo Controlled, Dose Ascending, Four Way Crossover Study to Examine Efficacy (FEV1), Safety, Tolerability, Pharmacodynamics and Pharmacokinetics of Single and Repeat Doses of GW642444 [NCT00354874]Phase 228 participants (Actual)Interventional2005-01-31Completed
A 26-week Treatment Randomized, Double-blind, Double Dummy, Parallel-group Study to Assess the Efficacy and Safety of QVA149 (Indacaterol / Glycopyrronium Bromide) Compared to Fluticasone/Salmeterol in Patients With Moderate to Severe COPD [NCT01709903]Phase 3744 participants (Actual)Interventional2012-11-30Completed
DB2114930: A Randomized, Multi-center, Double-blind, Double-dummy, Parallel Group Study to Evaluate the Efficacy and Safety of Umeclidinium/Vilanterol Compared With Fluticasone Propionate/Salmeterol Over 12 Weeks in Subjects With COPD [NCT01817764]Phase 3707 participants (Actual)Interventional2013-03-01Completed
A Randomized, Double-blind, 12-week Treatment, Parallel-group Study to Evaluate the Efficacy and Safety of QMF149 (150 µg/160 µg o.d.) Compared With Salmeterol Xinafoate/Fluticasone Propionate (50 µg/500 µg b.i.d.) in Patients With Chronic Obstructive Pul [NCT01636076]Phase 2629 participants (Actual)Interventional2012-11-30Completed
A Randomized, Double-blind, Parallel-group, 26-week Study Comparing the Efficacy and Safety of Indacaterol (Onbrez® Breezhaler® 150 mcg o.d.) With Salmeterol/Fluticasone Propionate (Seretide® Accuhaler® 50 mcg/500 mcg b.i.d.) in Patients With Moderate Chr [NCT01555138]Phase 4581 participants (Actual)Interventional2012-02-29Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00118716 (7) [back to overview]Four-hour Serial Post-dose FEV1 Area Under the Curve (AUC) on Treatment Day 1
NCT00118716 (7) [back to overview]Percent of Rescue-free Days
NCT00118716 (7) [back to overview]Maximal Percent Change in Forced Expiratory Volume in 1 Second (FEV1) Following Exercise Challenge at Week 4
NCT00118716 (7) [back to overview]Change From Baseline in Evening (PM) PEF
NCT00118716 (7) [back to overview]Change From Baseline in Morning Peak Expiratory Flow (AM PEF)
NCT00118716 (7) [back to overview]Change From Baseline in Pediatric Asthma Quality of Life Questionnaire (PAQLQ)
NCT00118716 (7) [back to overview]Percent of Symptom-free Days
NCT00127166 (5) [back to overview]Maximum Post-exercise Percent (%) Fall in FEV1
NCT00127166 (5) [back to overview]Maximum FEV1 % Predicted Following First Beta-agonist Use
NCT00127166 (5) [back to overview]Average (Avg) %-Change in FEV1 After First Beta (β)-Agonist Use and Prior to Second β-agonist Use
NCT00127166 (5) [back to overview]Area Under the Curve for %-Change From Pre-exercise Baseline FEV1 in Liters (L), From 0 to 20 Minutes (AUC(0-20))
NCT00127166 (5) [back to overview]Time to Recovery to Within 5% of Baseline FEV1
NCT00156819 (1) [back to overview]Treatment Failure
NCT00197106 (9) [back to overview]Percent Change From Baseline in RINT Measurements at Week 26
NCT00197106 (9) [back to overview]Number of Asthma Exacerbations Per Treatment Group at Week 26
NCT00197106 (9) [back to overview]Mean Change From Baseline in Provocation Dose (PD20) Causing a 20% Fall in FEV1 at Week 26
NCT00197106 (9) [back to overview]Mean Change From Baseline in Percentage Predicted Forced Expiratory Volume in One Second (FEV1) at Week 26
NCT00197106 (9) [back to overview]Mean Change From Baseline in Midexpiratory Flow (MEF 50) at Week 26
NCT00197106 (9) [back to overview]Mean Change From Baseline in Forced Vital Capacity (FVC) at Week 26
NCT00197106 (9) [back to overview]Geometric Means of Nitric Oxide (NO) at Week 26
NCT00197106 (9) [back to overview]Percentage of Symptom-free Days During the Last 10 Weeks of the Treatment Period
NCT00197106 (9) [back to overview]Percentage of Symptom-free Days During the Entire Treatment Period
NCT00200967 (12) [back to overview]Methacholine Provocative Concentration 20 (PC20)
NCT00200967 (12) [back to overview]Exhaled Breath Condensate (EBC)
NCT00200967 (12) [back to overview]Rescue Medication (Ipratropium and Albuterol) Use
NCT00200967 (12) [back to overview]Spirometry Forced Vital Capacity (FVC), Pre-bronchodilator
NCT00200967 (12) [back to overview]Asthma Control Questionnaire (ACQ)
NCT00200967 (12) [back to overview]Asthma Symptoms
NCT00200967 (12) [back to overview]Evening (PM) Peak Expiratory Flow (PEF) Rate
NCT00200967 (12) [back to overview]Spirometry Peak Expiratory Flow (PEF) Rate, Pre-bronchodilator
NCT00200967 (12) [back to overview]Exhaled Nitric Oxide (eNO)
NCT00200967 (12) [back to overview]Morning (AM) Peak Expiratory Flow (PEF) Rate
NCT00200967 (12) [back to overview]Peak Expiratory Flow (PEF) Variability
NCT00200967 (12) [back to overview]Spirometry Forced Expiratory Volume in One Second (FEV1), Pre-bronchodilator
NCT00214019 (1) [back to overview]Sputum Eosinophils (EOS) 24 Hours Post Antigen Challenge
NCT00245570 (12) [back to overview]Area Under the Curve for FEV1 Percent Change From Preexercise Baseline During the 60 Minutes Following Exercise Challenge (AUC 0-60 Min) at 24 Hours Postdose
NCT00245570 (12) [back to overview]Time to Recovery From Maximum Percentage Decrease in FEV1 After Exercise Challenge at 8.5 Hours Postdose
NCT00245570 (12) [back to overview]Area Under the Curve for FEV1 Percent Change From Preexercise Baseline During the 60 Minutes Following Exercise Challenge (AUC 0-60 Min) at 8.5 Hours Postdose
NCT00245570 (12) [back to overview]Maximum Percent Fall in FEV1 After Exercise Challenge at 24 Hours Post-dose in Patients With EIB
NCT00245570 (12) [back to overview]Area Under the Curve for FEV1 Percent Change From Preexercise Baseline During the 60 Minutes Following Exercise Challenge (AUC 0-60 Min) at 2 Hours Postdose
NCT00245570 (12) [back to overview]Number of Patients Requiring β-Agonist Rescue Medication After Exercise Challenge at 8.5 Hours Postdose
NCT00245570 (12) [back to overview]Number of Patients Requiring β-Agonist Rescue Medication After Exercise Challenge at 24 Hours Postdose
NCT00245570 (12) [back to overview]Number of Patients Requiring β-Agonist Rescue Medication After Exercise Challenge at 2 Hours Postdose
NCT00245570 (12) [back to overview]Time to Recovery From Maximum Percentage Decrease in FEV1 After Exercise Challenge at 24 Hours Postdose
NCT00245570 (12) [back to overview]Time to Recovery From Maximum Percentage Decrease in FEV1 After Exercise Challenge at 2 Hours Postdose
NCT00245570 (12) [back to overview]Maximum Percent Fall in Forced Expiratory Volume in 1 Second (FEV1) After Exercise Challenge at 2 Hours Post-dose in Patients With Exercise-Induced Bronchoconstriction (EIB)
NCT00245570 (12) [back to overview]Maximum Percent Fall in FEV1 After Exercise Challenge at 8.5 Hours Post-dose in Patients With EIB
NCT00269087 (25) [back to overview]Mean Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT00269087 (25) [back to overview]Mean Change From Baseline in Peak Expiratory Flow (PEF)
NCT00269087 (25) [back to overview]Mean Change From Baseline in Maximal Expiratory Flow Rate at 25% (V25) and 50% (V50) of Vital Capacity
NCT00269087 (25) [back to overview]Mean Change From Baseline in Level of Plasma Cortisol 1
NCT00269087 (25) [back to overview]Mean Change From Baseline in Forced Vital Capacity (FVC)
NCT00269087 (25) [back to overview]Change From Baseline in Symptom Score With Respect to Breathlessness, Cough, Sputum and Nighttime Awakenings
NCT00269087 (25) [back to overview]Median Tmax of Salmeterol
NCT00269087 (25) [back to overview]Median Time of Observed Maximum Plasma Concentration (Tmax) of FP
NCT00269087 (25) [back to overview]Mean Observed Maximum Plasma Concentration (Cmax) of Fluticasone Propionate (FP)
NCT00269087 (25) [back to overview]Mean Frequency of Moderate and Severe Chronic Obstructive Pulmonary Disease (COPD) Exacerbations
NCT00269087 (25) [back to overview]Number of Participants With Any Adverse Events (AEs) and Serious AEs (SAEs)
NCT00269087 (25) [back to overview]Number of Participants With Abnormal Oropharyngeal Examination Findings
NCT00269087 (25) [back to overview]Number of Participants With Abnormal (Shift From Baseline) Urinalysis Parameters
NCT00269087 (25) [back to overview]Number of Participants With Abnormal (Outliers From the Normal Range) Hematology Parameters
NCT00269087 (25) [back to overview]Number of Participants With Abnormal (Outliers From the Normal Range) Clinical Chemistry Parameters
NCT00269087 (25) [back to overview]Mean Change From Baseline in Pulse Rate
NCT00269087 (25) [back to overview]Number of Participants With Abnormal (Clinically Significant) Ophthalmological Examinations Findings
NCT00269087 (25) [back to overview]Number of Participants With Abnormal (Clinically Significant) Electrocardiogram (ECG) Findings
NCT00269087 (25) [back to overview]Mean Level of Plasma Cortisol 2
NCT00269087 (25) [back to overview]Mean Change From Baseline in Weight
NCT00269087 (25) [back to overview]Mean Area Under the Plasma Concentration-time Curve From Zero up to the Last Quantifiable Plasma Concentration [AUC (0-t)] of Salmeterol
NCT00269087 (25) [back to overview]Mean Area Under the Plasma Concentration-time Curve Over a Dosing Interval [AUC(0-tau)] of FP
NCT00269087 (25) [back to overview]Mean Change From Baseline in Bone Mineral Density (BMD)
NCT00269087 (25) [back to overview]Mean Change From Baseline in Percent of Days Without Use of Rescue Medication
NCT00269087 (25) [back to overview]Mean Cmax of Salmeterol
NCT00296491 (10) [back to overview]Rhinitis: Mean Change From Baseline at 1-2 Weeks in Nightime Total Nasal Symptom Scores (N-TNSS)
NCT00296491 (10) [back to overview]Rhinitis: Mean Change From Baseline at 1-2 Weeks in Daytime Total Nasal Symptom Scores (D-TNNS).
NCT00296491 (10) [back to overview]Mean Change From Baseline at Endpoint in Morning Peak Expiratory Flow (PEF) for Per Protocol Population
NCT00296491 (10) [back to overview]Mean Change From Baseline at Endpoint in Morning Peak Expiration Flow (PEF) for Intent-to-Treat Population
NCT00296491 (10) [back to overview]Asthma: Mean Change From Baseline at Endpoint in Predose Morning Forced Expiratory Volume (FEV1) for Per Protocol Population
NCT00296491 (10) [back to overview]Asthma: Mean Change From Baseline at Endpoint in Predose Morning Forced Expiratory Volume (FEV1) for Intent-to-Treat Population
NCT00296491 (10) [back to overview]Asthma: Mean Change From Baseline at Endpoint in Percentage of Asthma Symptom-Free Days for Per Protocol Population
NCT00296491 (10) [back to overview]Asthma: Mean Change From Baseline at Endpoint in Percentage of Asthma Symptom-Free Days for Intent-to-Treat Population
NCT00296491 (10) [back to overview]Asthma: Mean Change From Baseline at Endpoint in Percentage of Albuterol/Salbutamol-Free Days for Per Protocol Population
NCT00296491 (10) [back to overview]Asthma: Mean Change From Baseline at Endpoint in Percentage of Albuterol-Salbutamol Free Days for Intent-to-Treat Population
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question Did You Experience Wheeze or Cough During the Day at Week 12"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question Did You Experience Wheeze or Cough During the Day at Week 16"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question Did You Experience Wheeze or Cough During the Day at Week 4"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question Did You Experience Wheeze or Cough During the Day at Week 8"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question Did You Wake up During the Night Due to Asthma at Week 12"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question Did You Wake up During the Night Due to Asthma at Week 16"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question Did You Wake up During the Night Due to Asthma at Week 4"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question Did You Wake up During the Night Due to Asthma at Week 8"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Limited Were You in Your Activities Today Because of Your Asthma at Week 12"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Limited Were You in Your Activities Today Because of Your Asthma at Week 16"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Limited Were You in Your Activities Today Because of Your Asthma at Week 4"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Limited Were You in Your Activities Today Because of Your Asthma at Week 8"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Much Shortness of Breath Did You Experience During the Day at Week 12"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Much Shortness of Breath Did You Experience During the Day at Week 16"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Much Shortness of Breath Did You Experience During the Day at Week 4"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Much Shortness of Breath Did You Experience During the Day at Week 8"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms During the Day at Week 12"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms During the Day at Week 16"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms During the Day at Week 4"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms During the Day at Week 8"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms in the Morning at Week 4"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms This Morning at Week 12"
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms This Morning at Week 16"
NCT00350207 (63) [back to overview]Mean Weekly Morning Peak Expiratory Flow at Week 8
NCT00350207 (63) [back to overview]Mean Weekly Morning Peak Expiratory Flow at Week 16
NCT00350207 (63) [back to overview]Mean Weekly Morning Peak Expiratory Flow at Week 12
NCT00350207 (63) [back to overview]Mean Weekly Morning Forced Expiratory Volume in 1 Second at Week 8
NCT00350207 (63) [back to overview]Mean Weekly Morning Forced Expiratory Volume in 1 Second at Week 4
NCT00350207 (63) [back to overview]Mean Weekly Morning Forced Expiratory Volume in 1 Second at Week 16
NCT00350207 (63) [back to overview]Systolic Blood Pressure in Conjunction With Spirometry at Visit 5
NCT00350207 (63) [back to overview]Mean Weekly Morning Forced Expiratory Volume in 1 Second at Week 12
NCT00350207 (63) [back to overview]Mean Weekly Evening Peak Expiratory Flow at Week 8
NCT00350207 (63) [back to overview]Mean Weekly Evening Peak Expiratory Flow at Week 4
NCT00350207 (63) [back to overview]Pulse Rate in Conjunction With Spirometry at Visit 4
NCT00350207 (63) [back to overview]Mean Weekly Evening Peak Expiratory Flow at Week 16
NCT00350207 (63) [back to overview]Mean Weekly Evening Peak Expiratory Flow at Week 12
NCT00350207 (63) [back to overview]Mean Weekly Evening Forced Expiratory Volume in 1 Second at Week 8
NCT00350207 (63) [back to overview]Mean Weekly Evening Forced Expiratory Volume in 1 Second at Week 4
NCT00350207 (63) [back to overview]Mean Weekly Evening Forced Expiratory Volume in 1 Second at Week 16
NCT00350207 (63) [back to overview]Mean Weekly Evening Forced Expiratory Volume in 1 Second at Week 12
NCT00350207 (63) [back to overview]Mean PEF Variability at Week 8
NCT00350207 (63) [back to overview]Morning Pre-dose Forced Vital Capacity as Measured by Spirometry at Visit 5
NCT00350207 (63) [back to overview]Mean PEF Variability at Week 4
NCT00350207 (63) [back to overview]Mean PEF Variability at Week 16
NCT00350207 (63) [back to overview]"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms This Morning at Week 8"
NCT00350207 (63) [back to overview]Mean PEF Variability at Week 12
NCT00350207 (63) [back to overview]Diastolic Blood Pressure in Conjunction With Spirometry at Visit 5
NCT00350207 (63) [back to overview]Diastolic Blood Pressure in Conjunction With Spirometry at Visit 4
NCT00350207 (63) [back to overview]Diastolic Blood Pressure in Conjunction With Spirometry at Visit 3
NCT00350207 (63) [back to overview]Change in Mean Weekly Morning Peak Expiratory Flow From Baseline to the End of the Trial
NCT00350207 (63) [back to overview]Systolic Blood Pressure in Conjunction With Spirometry at Visit 4
NCT00350207 (63) [back to overview]Systolic Blood Pressure in Conjunction With Spirometry at Visit 3
NCT00350207 (63) [back to overview]Pulse Rate in Conjunction With Spirometry at Visit 5
NCT00350207 (63) [back to overview]Pulse Rate in Conjunction With Spirometry at Visit 3
NCT00350207 (63) [back to overview]Mean Weekly Morning Peak Expiratory Flow at Week 4
NCT00350207 (63) [back to overview]Morning Pre-dose Forced Vital Capacity as Measured by Spirometry at Visit 4
NCT00350207 (63) [back to overview]Morning Pre-dose Forced Vital Capacity as Measured by Spirometry at Visit 3
NCT00350207 (63) [back to overview]Morning Pre-dose Forced Expiratory Volume in 1 Second as Measured by Spirometry at Visit 5
NCT00350207 (63) [back to overview]Morning Pre-dose Forced Expiratory Volume in 1 Second as Measured by Spirometry at Visit 4
NCT00350207 (63) [back to overview]Morning Pre-dose Forced Expiratory Volume in 1 Second as Measured by Spirometry at Visit 3
NCT00350207 (63) [back to overview]Mini-Asthma Quality of Life Questionnaire (Mini-AQLQ) Overall Score at Visit 3
NCT00350207 (63) [back to overview]Mini-AQLQ Overall Score at Visit 5
NCT00350207 (63) [back to overview]Mini-AQLQ Overall Score at Visit 4
NCT00353873 (4) [back to overview]Number of Participants Who Achieved WC Asthma
NCT00353873 (4) [back to overview]Number of Participants Who Achieved 'Totally Controlled' (TC) Asthma
NCT00353873 (4) [back to overview]Mean Change From Baseline in Morning PEF Over 12 Weeks in Per Protocol (PP) Population
NCT00353873 (4) [back to overview]Mean Change From Baseline in Morning Peak Expiratory Flow (PEF) Over 12 Weeks in Intent-to-treat (ITT) Population
NCT00355342 (2) [back to overview]Percent Change From Baseline in Bone Mineral Density (BMD) at the Lumbar Spine L1-L4
NCT00355342 (2) [back to overview]Percent Change From Baseline in BMD at the Total Hip
NCT00363480 (17) [back to overview]Change From Baseline in Mean Morning Percent Predicted Peak Expiratory Flow (PEF) at Week 12
NCT00363480 (17) [back to overview]Change From Baseline in Quality of Life Using the Asthma Quality of Life Questionnaire (AQLQ)
NCT00363480 (17) [back to overview]Change From Baseline in Mean ACT Score at Visit 6
NCT00363480 (17) [back to overview]Change From Baseline in Mean 24-hour Symptom Score at Week 12
NCT00363480 (17) [back to overview]Change From Baseline in Number of Additional Usage of Salbutamol at Week 12
NCT00363480 (17) [back to overview]Correlation of Change in AQLQ Score and Change in ACT Score
NCT00363480 (17) [back to overview]Number of Participants With Adverse Events (AE) Leading to a Change in Asthma Treatment
NCT00363480 (17) [back to overview]Number of Participants With Occurrence of (Near-) Incidents Associated With Peak Flow Measurements
NCT00363480 (17) [back to overview]Percent Change From Baseline in Number of Nights With no Nocturnal Awakening at Week 12
NCT00363480 (17) [back to overview]Assessment of Tolerability by Change From Baseline of Pulse Rate
NCT00363480 (17) [back to overview]Assessment of Tolerability by Change From Baseline of Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT00363480 (17) [back to overview]Assessment of Tolerability by Number of Participants With at Least One Treatment Emergent Serious and, Non-serious AE
NCT00363480 (17) [back to overview]Percentage of Well Controlled Participants as Per Gaining Optimal Asthma Control (GOAL) Criteria After 12 Week Compared to Percentage of Participants With Asthma Control Test (ACT) Score of 20-25 for Week 9 to Week 12
NCT00363480 (17) [back to overview]Change From Baseline in Forced Expiratory Volume (FEV1) to Week 12
NCT00363480 (17) [back to overview]Change From Baseline in Percentage of Participants With ACT Score of 20-25 at Week 12
NCT00363480 (17) [back to overview]Number of Participants With Emergency Visits Due to Asthma
NCT00363480 (17) [back to overview]Number of Participants With Well Controlled and Totally Controlled Asthma at Week 12
NCT00379288 (1) [back to overview]The Number of All Randomized Subjects Reporting Adverse Events (AEs).
NCT00395304 (14) [back to overview]Change From Baseline in the Pre-bronchodilator FEV1/FVC Ratio
NCT00395304 (14) [back to overview]Change From Baseline in the Pre-bronchodilator Forced Expiratory Volume in One Second (FEV1) % Predicted
NCT00395304 (14) [back to overview]Change From Baseline in the Pre-bronchodilator Forced Vital Capacity (FVC) % Predicted
NCT00395304 (14) [back to overview]The Number of Participants With a Differential Response to the Three Step-up Therapies Based on Fixed Threshold Criteria for the Following Three Asthma Control Measures: Use of Oral Prednisone for Acute Asthma Exacerbations, Asthma Control Days and FEV1.
NCT00395304 (14) [back to overview]Change From Baseline in the Post-bronchodilator FEV1 Percent Predicted
NCT00395304 (14) [back to overview]Change From Baseline in the Peak Expiratory Flow Rate (PEFR) Variability
NCT00395304 (14) [back to overview]Change From Baseline in the Natural Logarithm of Exhaled Nitric Oxide (eNO)
NCT00395304 (14) [back to overview]Change From Baseline in the Morning Peak Expiratory Flow Rate (PEFR) % Predicted
NCT00395304 (14) [back to overview]Change From Baseline in the Logarithm Base 2 of the Methacholine PC20
NCT00395304 (14) [back to overview]Change From Baseline in the Evening Peak Expiratory Flow Rate (PEFR) % Predicted
NCT00395304 (14) [back to overview]Change From Baseline in the Asthma Control Test (ACT)
NCT00395304 (14) [back to overview]Change From Baseline in the Impulse Oscillometry Resistance at 5 Hertz
NCT00395304 (14) [back to overview]Change From Baseline in Asthma Quality of Life
NCT00395304 (14) [back to overview]Number of Participants With Asthma Exacerbations
NCT00403754 (4) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) by Time Point From 5 Minutes to 12 Hours Post-dose on Day 1 and From 22 to 24 Hours Post-dose on Day 2
NCT00403754 (4) [back to overview]Peak Forced Expiratory Volume in 1 Second (FEV1) From 5 Minutes to 4 Hours Post-dose on Day 1
NCT00403754 (4) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) Standardized (With Respect to Time) Area Under the Curve (AUC) From 5 Minutes Post-dose on Day 1 to 24 Hours Post-dose on Day 2
NCT00403754 (4) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) Standardized (With Respect to Time) Area Under the Curve (AUC) From 22 to 24 Hours Post-dose on Day 2
NCT00424008 (4) [back to overview]The Proportion of Symptom-free Days and Nights (Combined) Over the 12-week Treatment Period.
NCT00424008 (4) [back to overview]The Area Under the Curve From 0 to 12 Hours [AUC](0-12 hr) of the Change From Baseline to the Week 12 Endpoint in Forced Expiratory Volume in One Second (FEV1)
NCT00424008 (4) [back to overview]Onset-of-action Based on Change From Baseline FEV1 at the 5 Min Pulmonary Function Test (PFT) Assessment on Day 1
NCT00424008 (4) [back to overview]Change From Baseline in Asthma Control Questionnaire (ACQ) Total Score at Week 12 Endpoint
NCT00441441 (24) [back to overview]Geometric Mean Ratio for Baseline:Week12 24-hour Urinary Cortisol Excretion
NCT00441441 (24) [back to overview]Geometric Mean Ratio for Week12:Baseline for 24-hour Urinary Cortisol Excretion
NCT00441441 (24) [back to overview]Albuterol Use
NCT00441441 (24) [back to overview]AM Peak Expiratory Flow
NCT00441441 (24) [back to overview]Asthma Exacerbations: Worsening of Asthma Requiring Emergency Intervention, Hospitalization, or Treatment With Asthma Medications Prohibited by the Protocols
NCT00441441 (24) [back to overview]Asthma Symptom Scores
NCT00441441 (24) [back to overview]Cardiovascular Adverse Events Reported During the Post-Treatment Period
NCT00441441 (24) [back to overview]Cardiovascular Adverse Events Reported During Treatment Period
NCT00441441 (24) [back to overview]Clinic Morning (AM) Forced Expiratory Volume in Participants 6-11 Years
NCT00441441 (24) [back to overview]Clinically Significant Unfavorable ECGs at Week 12
NCT00441441 (24) [back to overview]ECG Measures - Heart Rate
NCT00441441 (24) [back to overview]ECG Measures - QT Interval
NCT00441441 (24) [back to overview]Geometric Mean Values of 24 Hour Urinary Cortisol Excretion by Spacer Use at Baseline and Week 12
NCT00441441 (24) [back to overview]Geometric Mean Values of 24-hour Urinary Cortisol Excretion at Baseline and Week 12
NCT00441441 (24) [back to overview]Geometric Mean Values of 24-hour Urinary Cortisol Excretion at Baseline and Week 12
NCT00441441 (24) [back to overview]Geometric Mean Values of 24-hour Urinary Cortisol Excretion by Spacer Use Excluding Participants With Abnormal Urinary Cortisol Excretion Values at Baseline From the Cortisol Population at Baseline and Week 12
NCT00441441 (24) [back to overview]Investigator Evaluations of Electrocardiogram (ECG) Results
NCT00441441 (24) [back to overview]Number of Participants With the Indicated Levels of 24 Hour Urinary Cortisol Excretion by Spacer Use
NCT00441441 (24) [back to overview]Number of Participants With the Indicated Levels of 24-hour Urinary Cortisol Excretion
NCT00441441 (24) [back to overview]Percent of Albuterol-free Days
NCT00441441 (24) [back to overview]Percentage of Symptom Free Days
NCT00441441 (24) [back to overview]Possible Drug-Related Adverse Events
NCT00441441 (24) [back to overview]Geometric Mean Ratio for Week12: Baseline for 24 Hour Urinary Cortisol Excretion by Spacer Use
NCT00441441 (24) [back to overview]Geometric Mean Ratio for Baseline: Week 12 24-hour Urinary Cortisol Excretion by Spacer Use Excluding Participants With Abnormal Urinary Cortisol Excretion Values at Baseline From the Cortisol Population
NCT00448435 (14) [back to overview]Percentage of Subjects With Symptom-Free Nights & Days
NCT00448435 (14) [back to overview]Percentage of Subjects With Symptom-Free Nights & Days After 20 Weeks of Treatment
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline in Evening PEF During the 20-week Extension Treatment Period
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline in Morning PEF (Peak Expiratory Flow) During the 4-week Treatment Periods
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline in Evening PEF During the 4-week Treatment Periods
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline in Morning PEF During the 20-week Extension Treatment Period
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline in Percent Personal Best Morning PEF(%) During the 20-week Extension Treatment Period
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline in Percent Personal Best Morning PEF(%) During the 4-week Treatment Periods
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline in Percent Predicted Morning PEF(%) During the 20-Week Extension Treatment Period
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline in Percent Predicted Morning PEF(%) During the 4-week Treatment Periods
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline of Circadian Variation in Morning PEF(%) During the 4-week Treatment Periods
NCT00448435 (14) [back to overview]Adjusted Mean Change From Baseline of Circadian Variation in PEF(%) During the 20-Week Extension Treatment Period
NCT00448435 (14) [back to overview]Percentage of Subjects With Rescue Medication-Free Nights & Days After 20 Weeks of Treatment
NCT00448435 (14) [back to overview]Percentage of Subjects With Rescue Medication-Free Nights and Days
NCT00449046 (8) [back to overview]Change From Baseline in Morning Peak Expiratory Flow (PEF) During Weeks 1-24
NCT00449046 (8) [back to overview]Change From Baseline in Circadian Variation in Peak Expiratory Flow (PEF) During Weeks 1-24
NCT00449046 (8) [back to overview]Change From Baseline in Evening Peak Expiratory Flow (PEF) During Weeks 1-24
NCT00449046 (8) [back to overview]Number of Participants With Symptom-Free Nights and Days
NCT00449046 (8) [back to overview]Number of Participants With Rescue Medication-Free Nights and Days
NCT00449046 (8) [back to overview]Change From Baseline in Percent Predicted Morning Peak Expiratory Flow (PEF) During Weeks 1-24
NCT00449046 (8) [back to overview]Most Frequent Adverse Events - On Therapy
NCT00449046 (8) [back to overview]Serious Adverse Events (SAEs) - On Therapy
NCT00452348 (4) [back to overview]Rate of Asthma Attacks Per Participant Per Year
NCT00452348 (4) [back to overview]Mean Change From Baseline in AM PEF Over Weeks 1-52
NCT00452348 (4) [back to overview]Mean Change From Baseline in Pre-dose FEV1 Over Weeks 1-52
NCT00452348 (4) [back to overview]Mean Change From Baseline in the Percentage of Symptom-free Days Over Weeks 1-52
NCT00452699 (4) [back to overview]Mean Change From Baseline in the Percentage of Symptom-free Days Over Weeks 1-52
NCT00452699 (4) [back to overview]Mean Change From Baseline in AM PEF Over Weeks 1-52
NCT00452699 (4) [back to overview]Rate of Asthma Attacks Per Participant Per Year
NCT00452699 (4) [back to overview]Mean Change From Baseline in Pre-dose FEV1 Over Weeks 1-52
NCT00461500 (13) [back to overview]Change From Baseline in Pre-dose FEV1 (Forced Expiratory Volume in One Second) Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)
NCT00461500 (13) [back to overview]Number of Participants With at Least One Exacerbation During 12-Week Treatment Period
NCT00461500 (13) [back to overview]Number of Participants Who Achieved Well-Controlled Asthma During Weeks 5-12
NCT00461500 (13) [back to overview]Number of Participants Who Achieved Total-controlled Asthma During Weeks 5-12
NCT00461500 (13) [back to overview]ACT Score in Classes at Week 12
NCT00461500 (13) [back to overview]Median Number of Weeks to First Achieve Well-Controlled Asthma During Weeks 5-12
NCT00461500 (13) [back to overview]Change From Baseline in Pre-dose Forced Expiratory Vital Capacity (FVC) Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)
NCT00461500 (13) [back to overview]Change From Baseline in Pre-dose (Percent Predicted) FEV1 Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)
NCT00461500 (13) [back to overview]Change From Baseline in Overall Asthma Quality of Life Questionnaire (AQLQ) Score at Week 12
NCT00461500 (13) [back to overview]Change From Baseline in Asthma Control Test (ACT) Score at Week 12
NCT00461500 (13) [back to overview]Change From Baseline (BL) in Pre-dose FEF 25-75% (Forced Expiratory Flow) Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)
NCT00461500 (13) [back to overview]Change From Baseline in Mean Morning Peak Expiratory Flow (PEF) Over Weeks 5-12
NCT00461500 (13) [back to overview]Change From Baseline in FEV1 Reversibility Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)
NCT00521222 (5) [back to overview]Absolute Change in Morning Peak Flow
NCT00521222 (5) [back to overview]Change in Asthma Symptom Score
NCT00521222 (5) [back to overview]Change in Forced Expiratory Volume in 1 Second (FEV1) Percent Predicted Pre-Bronchodilator
NCT00521222 (5) [back to overview]Change in Forced Expiratory Volume in 1 Second (FEV1) Post-Bronchodilator
NCT00521222 (5) [back to overview]Change in Forced Expiratory Volume in 1 Second (FEV1) Pre-Bronchodilator
NCT00527826 (15) [back to overview]Mean Change From Baseline in Forced Expiratory Volume in 1 Second (FEV1) at Week 52
NCT00527826 (15) [back to overview]Mean Total Costs (Related to COPD) Per Participant
NCT00527826 (15) [back to overview]Mean Number of Exacerbations Per Year: Poisson Model
NCT00527826 (15) [back to overview]Mean Number of COPD-related Visits at/by Physician
NCT00527826 (15) [back to overview]Mean Number of Exacerbations Per Year: Negative Binomial Model
NCT00527826 (15) [back to overview]Compliance and Adherence to Study Medication
NCT00527826 (15) [back to overview]Mean Change From Baseline in the Total Score of the St. George's Respiratory Questionnaire (SGRQ) at Week 52
NCT00527826 (15) [back to overview]Number of Participants With the Indicated Number of Hospital Stays
NCT00527826 (15) [back to overview]Number of Participants With the Indicated Number of Days at the Intensive Care Unit (ICU)
NCT00527826 (15) [back to overview]Mean Number of Days Rescue Medication Was Used
NCT00527826 (15) [back to overview]Mean Change From Baseline in the Tiffeaneau Index at Week 52
NCT00527826 (15) [back to overview]Mean Change From Baseline in the Symptom Score of the St. George's Respiratory Questionnaire (SGRQ) at Week 52
NCT00527826 (15) [back to overview]Mean Change From Baseline in the Impact Score of the St. George's Respiratory Questionnaire (SGRQ) at Week 52
NCT00527826 (15) [back to overview]Mean Change From Baseline in the Activity Score of the St. George's Respiratory Questionnaire (SGRQ) at Week 52
NCT00527826 (15) [back to overview]Mean Change From Baseline in Inspiratory Vital Capacity (IVC) at Week 52
NCT00529529 (17) [back to overview]Blood Glucose 1 Hour Post-dose at Day 1
NCT00529529 (17) [back to overview]Blood Glucose 1 Hour Post-dose at Week 12
NCT00529529 (17) [back to overview]Corrected QT (QTc) Interval Using Fridericia's Formula Measured 1 Hour Post-dose at Day 1
NCT00529529 (17) [back to overview]Corrected QT (QTc) Interval Using Fridericia's Formula Measured 1 Hour Post-dose at Week 12
NCT00529529 (17) [back to overview]Corrected QT (QTc) Interval Using Fridericia's Formula Measured 1 Hour Post-dose at Week 21
NCT00529529 (17) [back to overview]Diastolic Blood Pressure 1 Hour Post-dose at Day 1
NCT00529529 (17) [back to overview]Diastolic Blood Pressure 1 Hour Post-dose at Week 12
NCT00529529 (17) [back to overview]Number of Asthma Exacerbations Per Patient (Without Imputation) During the 26 Weeks of the Study
NCT00529529 (17) [back to overview]Percentage of Patients With at Least 1 Adverse Event During the 26 Weeks of the Study
NCT00529529 (17) [back to overview]Serum Potassium 1 Hour Post-dose at Day 1
NCT00529529 (17) [back to overview]Serum Potassium 1 Hour Post-dose at Week 12
NCT00529529 (17) [back to overview]Percentage of Patients With Clinically Significant Asthma Exacerbations During the 26 Weeks of the Study
NCT00529529 (17) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose at Week 12 + 1 Day, Day 85
NCT00529529 (17) [back to overview]Systolic Blood Pressure 1 Hour Post-dose at Day 1
NCT00529529 (17) [back to overview]Systolic Blood Pressure 1 Hour Post-dose at Week 12
NCT00529529 (17) [back to overview]24 Hour Mean Heart Rate Determined From ECG Holter Monitoring at Week 12
NCT00529529 (17) [back to overview]24 Hour Mean Heart Rate Determined From ECG Holter Monitoring at Week 26
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes
NCT00530842 (59) [back to overview]Static Lung Volumes (Percent)
NCT00530842 (59) [back to overview]Static Lung Volumes (Percent)
NCT00530842 (59) [back to overview]Static Lung Volumes (Percent)
NCT00530842 (59) [back to overview]Static Lung Volumes (Percent)
NCT00530842 (59) [back to overview]Static Lung Volumes (Percent)
NCT00530842 (59) [back to overview]Static Lung Volumes (Percent)
NCT00530842 (59) [back to overview]Static Lung Volumes (Percent)
NCT00530842 (59) [back to overview]Symptom Intensity During Exercise
NCT00530842 (59) [back to overview]Symptom Intensity During Exercise
NCT00530842 (59) [back to overview]Symptom Intensity During Exercise
NCT00530842 (59) [back to overview]Symptom Intensity During Exercise
NCT00530842 (59) [back to overview]Forced Vital Capacity (FVC)
NCT00530842 (59) [back to overview]Locus of Symptom Limitation at Peak Exercise During Exercise
NCT00530842 (59) [back to overview]Locus of Symptom Limitation at Peak Exercise During Exercise
NCT00530842 (59) [back to overview]Locus of Symptom Limitation at Peak Exercise During Exercise
NCT00530842 (59) [back to overview]Static Lung Volumes (Percent)
NCT00530842 (59) [back to overview]Forced Vital Capacity (FVC)
NCT00530842 (59) [back to overview]Forced Vital Capacity (FVC)
NCT00530842 (59) [back to overview]Post-dose TGV(FRC) (After 4 Weeks)
NCT00530842 (59) [back to overview]Forced Vital Capacity (FVC)
NCT00530842 (59) [back to overview]Post-dose TGV(FRC) (After 8 Weeks)
NCT00530842 (59) [back to overview]Slow Vital Capacity (SVC)
NCT00530842 (59) [back to overview]Slow Vital Capacity (SVC)
NCT00530842 (59) [back to overview]Slow Vital Capacity (SVC)
NCT00530842 (59) [back to overview]Slow Vital Capacity (SVC)
NCT00530842 (59) [back to overview]Dyspnea and Leg Discomfort
NCT00530842 (59) [back to overview]Dyspnea and Leg Discomfort
NCT00530842 (59) [back to overview]Endurance Time (After 4 Weeks)
NCT00530842 (59) [back to overview]Endurance Time (After 8 Weeks)
NCT00530842 (59) [back to overview]FEV1 Over FVC (Percent)
NCT00530842 (59) [back to overview]FEV1 Over FVC (Percent)
NCT00530842 (59) [back to overview]FEV1 Over FVC (Percent)
NCT00530842 (59) [back to overview]FEV1 Over FVC (Percent)
NCT00530842 (59) [back to overview]Forced Expiratory Volume in 1 Second (FEV1)
NCT00530842 (59) [back to overview]Forced Expiratory Volume in 1 Second (FEV1)
NCT00530842 (59) [back to overview]Forced Expiratory Volume in 1 Second (FEV1)
NCT00530842 (59) [back to overview]Forced Expiratory Volume in 1 Second (FEV1)
NCT00530842 (59) [back to overview]Forced Expiratory Volume in 1 Second (FEV1)
NCT00530842 (59) [back to overview]Forced Expiratory Volume in 1 Second (FEV1)
NCT00530842 (59) [back to overview]Forced Expiratory Volume in 1 Second (FEV1)
NCT00530842 (59) [back to overview]Forced Expiratory Volume in 1 Second (FEV1)
NCT00531050 (6) [back to overview]Percentage of Participants With Maximum Heart Rate Increase During Exercise in Part 1 of the Study
NCT00531050 (6) [back to overview]Change in Heart Rate During Exercise in Part 1
NCT00531050 (6) [back to overview]Maximum Heart Rate During Exercise in Part 1
NCT00531050 (6) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) During Part 1 and Part 2
NCT00531050 (6) [back to overview]Maximum Heart Rate (HR) During Salbutamol Administration in Part 2
NCT00531050 (6) [back to overview]Percentage of Participants With Maximum Heart Rate Increase During Salbutamol Administration in Part 2 of the Study
NCT00542880 (16) [back to overview]Change in Forced Vital Capacity (FVC) From Before Dose to5 Minutes After Dose at the Clinic
NCT00542880 (16) [back to overview]Change in FEV1from Before Dose to 5 Minutes After Dose in the Morning
NCT00542880 (16) [back to overview]Change in FEV1 From Before Dose to 5 Minutes After Dose at the Clinic
NCT00542880 (16) [back to overview]Change in FEV1 From Before Dose to 15 Minutes After Dose in the Morning
NCT00542880 (16) [back to overview]Capacity of Daily Living in the Morning (CDLM) (Change From Pre to End of Treatment)
NCT00542880 (16) [back to overview]FEV1 15 Minutes After Morning Dose
NCT00542880 (16) [back to overview]FEV1 Before Evening Dose
NCT00542880 (16) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) Before Morning Dose
NCT00542880 (16) [back to overview]Change in PEF From Before Dose to 15 Minutes After Dose in the Morning
NCT00542880 (16) [back to overview]Peak Expiratory Flow (PEF) 5 Minutes After Morning Dose
NCT00542880 (16) [back to overview]PEF 15 Minutes After Morning Dose
NCT00542880 (16) [back to overview]PEF Before Evening Dose
NCT00542880 (16) [back to overview]PEF Before Morning Dose
NCT00542880 (16) [back to overview]The Clinical Chronic Obstructive Pulmonary Disease (COPD) Questionnaire (Change From Pre to End of Treatment)
NCT00542880 (16) [back to overview]Change in PEF From Before Dose to 5 Minutes After Dose in the Morning
NCT00542880 (16) [back to overview]Difficulty in Getting Out From Bed (MASQ) (Change From Pre to End of Treatment)
NCT00556673 (15) [back to overview]Change From Period Baseline in Peak Percent Predicted Forced Expiratory Volume in 1 Second (FEV1)
NCT00556673 (15) [back to overview]Change From Period Baseline in Trough FEV1/FVC Ratio
NCT00556673 (15) [back to overview]Change From Period Baseline in Trough Forced Vital Capacity (FVC)
NCT00556673 (15) [back to overview]Change From Period Baseline in Trough Percent Predicted Forced Expiratory Volume in 1 Second (FEV1)
NCT00556673 (15) [back to overview]Change From Period Baseline to 24 Hour Post-dose (Trough) Forced Expiratory Volume in 1 Second (FEV1)
NCT00556673 (15) [back to overview]Maximum (Peak) Plasma Concentration (Cmax) of Indacaterol
NCT00556673 (15) [back to overview]Maximum (Peak) Plasma Concentration (Cmax) of Mometasone Furoate
NCT00556673 (15) [back to overview]Time to Reach Peak or Maximum Concentration Following Drug Administration for Indacaterol
NCT00556673 (15) [back to overview]Time to Reach Peak or Maximum Concentration Following Drug Administration for Mometasone Furoate
NCT00556673 (15) [back to overview]Area Under the Concentration-time Curve From Time 0 to 12 Hours Post-dose for Mometasone Furoate
NCT00556673 (15) [back to overview]Area Under the Concentration-time Curve From Time 0 to 24 Hours Post-dose for Indacaterol
NCT00556673 (15) [back to overview]Area Under the Concentration-time Curve From Time 0 to 24 Hours Post-dose for Mometasone Furoate
NCT00556673 (15) [back to overview]Change From Baseline in Peak Forced Expiratory Volume in One Second (FEV1)
NCT00556673 (15) [back to overview]Change From Period Baseline in Peak FEV1/FVC Ratio
NCT00556673 (15) [back to overview]Change From Period Baseline in Peak Forced Vital Capacity (FVC)
NCT00557440 (5) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) Standardized Area Under the Curve (AUC) Between Baseline (Pre-dose) and 24 Hours Post-dose
NCT00557440 (5) [back to overview]Change From Period Baseline to 24 Hour Post-dose (Trough) Forced Expiratory Volume in 1 Second (FEV1)
NCT00557440 (5) [back to overview]Time to Peak Forced Expiratory Volume in 1 Second (FEV1)
NCT00557440 (5) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) at Single Time Points
NCT00557440 (5) [back to overview]Forced Vital Capacity (FVC) at Single Time Points
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 10
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 11
NCT00563381 (31) [back to overview]First Occurrence of COPD Exacerbations Treated With Systemic Steroids and Antibiotics
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 3
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 4
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 1
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 6
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 7
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 5
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 14
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 15
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 16
NCT00563381 (31) [back to overview]Number of Participants With Premature Discontinuation of Trial Medication
NCT00563381 (31) [back to overview]First Occurrence of COPD Exacerbations Treated With Systemic Steroids
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 2
NCT00563381 (31) [back to overview]Number of Participants With at Least One COPD Exacerbation Leading to Hospitalisation
NCT00563381 (31) [back to overview]Number of Participants With at Least One COPD Exacerbation
NCT00563381 (31) [back to overview]First Occurrence of COPD Exacerbations Treated With Antibiotics
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 9
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 8
NCT00563381 (31) [back to overview]First Occurrence of (Moderate or Severe) COPD Exacerbation
NCT00563381 (31) [back to overview]Occurrence of Premature Discontinuation of Trial Medication
NCT00563381 (31) [back to overview]First Occurrence of COPD Exacerbation or Discontinuation of Trial Medication Because of Worsening of Underlying Disease, Whichever Comes First
NCT00563381 (31) [back to overview]First Occurrence of COPD Exacerbation Leading to Hospitalization
NCT00563381 (31) [back to overview]COPD Exacerbations Treated With Systemic Steroids Per Patient-year
NCT00563381 (31) [back to overview]COPD Exacerbations Treated With Systemic Steroids and Antibiotics Per Patient-year
NCT00563381 (31) [back to overview]COPD Exacerbations Treated With Antibiotics Per Patient-year
NCT00563381 (31) [back to overview]COPD Exacerbations Per Patient-year Leading to Hospitalisation
NCT00563381 (31) [back to overview]COPD Exacerbations Per Patient-year
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 13
NCT00563381 (31) [back to overview]Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 12
NCT00565266 (7) [back to overview]Change Between Week 14 and Week 0 in the Albuterol Rescue Puffs Per Day
NCT00565266 (7) [back to overview]Change Between Week 14 and Week 0 in the Asthma Control Questionnaire Score
NCT00565266 (7) [back to overview]Change Between Week 14 and Week 0 in the Forced Expiratory Volume in One Second (FEV1)
NCT00565266 (7) [back to overview]Change Between Week 14 and Week 0 in the Morning (AM) Peak Expiratory Flow (PEF)
NCT00565266 (7) [back to overview]Change Between Week 14 and Week 0 in the Proportion of Asthma Control Days
NCT00565266 (7) [back to overview]Change Between Week 14 and Week 0 in Asthma Symptoms
NCT00565266 (7) [back to overview]Change Between Week 14 and Week 0 in the Asthma Quality-of-life Questionnaire Score
NCT00567996 (3) [back to overview]St. George's Respiratory Questionnaire (SGRQ) Total Score After 12 Weeks of Treatment
NCT00567996 (3) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) After 12 Weeks of Treatment
NCT00567996 (3) [back to overview]"Percentage of COPD Days of Poor Control During 26 Weeks of Treatment"
NCT00595361 (3) [back to overview]Comparison of the Maximum Percent Fall in FEV1 From Pre-salmeterol Baseline to the End of the 2-week Treatment Period Between Arg/Arg and Gly/Gly Patients
NCT00595361 (3) [back to overview]Comparison of the Maximum Percent Fall in FEV1 After 1st Dose of Salmeterol to the End of the 2-week Treatment Period Between Arg/Arg and Gly/Gly Subjects
NCT00595361 (3) [back to overview]Comparison of the Maximum Percent Fall in FEV1 After Exercise Challenge at the End of the 2-week Treatment Period Between Arg/Arg and Gly/Gly Patients
NCT00615030 (2) [back to overview]Trough FEV1 Assessed After 14 Days of Dosing for All Other Treatment Comparisons
NCT00615030 (2) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) Following 14 Days of Evening Dosing of Indacaterol Versus Placebo
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 10 Hours Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 11 Hours 10 Minutes Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 11 Hours 45 Minutes Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 14 Hours Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 15 Minutes Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 2 Hours Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 20 Hours 10 Minutes Post-dose at the End of Each Treatment Period (Day 15)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 20 Hours 45 Minutes Post-dose at the End of Each Treatment Period (Day 15)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 23 Hours 10 Minutes Post-dose at the End of Each Treatment Period (Day 15)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 23 Hours 45 Minutes Post-dose at the End of Each Treatment Period (Day 15)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 3 Hours Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 30 Minutes Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 4 Hours Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 5 Hours Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 5 Minutes Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 6 Hours Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 8 Hours Post-dose at the End of Each Treatment Period (Day 14)
NCT00622635 (20) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose at the End of Each Treatment Period (Day 15)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 22 Hours Post-dose at the End of Each Treatment Period (Day 15)
NCT00622635 (20) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) 1 Hour Post-dose at the End of Each Treatment Period (Day 14)
NCT00628758 (4) [back to overview]Number of Severe Asthma Exacerbations
NCT00628758 (4) [back to overview]Mean Use of As-needed Medication Per Day During Treatment Period
NCT00628758 (4) [back to overview]Change in Standardised Asthma Quality of Life Questionnaire (AQLQ(S)) Score
NCT00628758 (4) [back to overview]Time to First Severe Asthma Exacerbation
NCT00633217 (3) [back to overview]Mean Change From Baseline in Forced Expiratory Volume in One Second (FEV1) 2 Hours Post-dose of Blinded Study Drug
NCT00633217 (3) [back to overview]Mean Change From Baseline in Peak Expiratory Flow
NCT00633217 (3) [back to overview]Mean Change From Baseline in AM Pre-dose FEV1
NCT00662792 (28) [back to overview]Response in Peak Expiratory Flow Rate (PEF) Area Under the Curve From 12 to 24 Hours (AUC12-24)
NCT00662792 (28) [back to overview]Response in Peak Forced Expiratory Volume in 1 Second (FEV1)
NCT00662792 (28) [back to overview]Response in Morning and Evening Peak Expiratory Flow Rate (PEF), Recorded by Patients at Home
NCT00662792 (28) [back to overview]Response in Morning and Evening Forced Expiratory Volume in 1 Second (FEV1) Recorded by Participants at Home
NCT00662792 (28) [back to overview]Response in Mean Number of Puffs of Rescue Medication
NCT00662792 (28) [back to overview]Response in Mean Number of Days With Rescue Medication Use
NCT00662792 (28) [back to overview]Response in Individual Peak Expiratory Flow (PEF) Over a 24 Hour Observation Period
NCT00662792 (28) [back to overview]Response in Individual Forced Vital Capacity (FVC) Over a 24 Hour Observation Period
NCT00662792 (28) [back to overview]Response in Individual Forced Expiratory Volume in 1 Second (FEV1) Over a 24 Hour Observation Period
NCT00662792 (28) [back to overview]Response in Peak PEF (Peak Expiratory Flow Rate)
NCT00662792 (28) [back to overview]Number of Participants With Drug Related Adverse Events
NCT00662792 (28) [back to overview]Response in Average Shortness of Breath (SOB) Score at Night
NCT00662792 (28) [back to overview]Response in Forced Expiratory Volume in 1 Second (FEV1) Area Under the Curve From 0 - 12 Hours (AUC0-12)
NCT00662792 (28) [back to overview]Response in Forced Expiratory Volume in 1 Second (FEV1) Area Under the Curve From 0-24 Hours (AUC0-24)
NCT00662792 (28) [back to overview]Response in Forced Expiratory Volume in Second (FEV1) Area Under the Curve From 12 - 24 Hours (AUC12 -24)
NCT00662792 (28) [back to overview]Response in Forced Vital Capacity (FVC) Area Under the Curve From 0 - 24 Hours (AUC0-24)
NCT00662792 (28) [back to overview]Response in Mean Number of Days With Night-time Awakenings
NCT00662792 (28) [back to overview]Response in Mean Number of Days With Night-time Awakenings Due to Shortness of Breath (SOB)
NCT00662792 (28) [back to overview]Response in Means Number of Awakenings Due to Shortness of Breath (SOB)
NCT00662792 (28) [back to overview]Response in Peak Expiratory Flow Rate (PEF) Area Under the Curve Form 0 to 12 Hours (AUC0-12)
NCT00662792 (28) [back to overview]Number of Patients With Marked Changes in Vital Signs
NCT00662792 (28) [back to overview]Response in Peak Expiratory Flow Rate (PEF) Area Under the Curve From 0 to 24 Hours (AUC0-24)
NCT00662792 (28) [back to overview]Response in Forced Vital Capacity (FVC) Area Under the Curve From 12 to 24 Hours (AUC12-24)
NCT00662792 (28) [back to overview]Response in Forced Vital Capacity (FVC) Area Under the Curve From 0 to 12 Hours (AUC0-12)
NCT00662792 (28) [back to overview]Response in Peak Forced Vital Capacity (FVC)
NCT00662792 (28) [back to overview]Response in Trough Peak Expiratory Flow Rate (PEF)
NCT00662792 (28) [back to overview]Response in Trough Forced Vital Capacity (FVC)
NCT00662792 (28) [back to overview]Response in Trough Forced Expiratory Volume in 1 Second (FEV1)
NCT00669617 (1) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) at 5 Minutes Post-dose
NCT00706446 (1) [back to overview]Number of Patients With Asthma Exacerbation
NCT00712335 (7) [back to overview]Sputum RANTES Levels
NCT00712335 (7) [back to overview]Sputum Neutrophil Percentages
NCT00712335 (7) [back to overview]Sputum Eotaxin Levels
NCT00712335 (7) [back to overview]Sputum IL-8 Levels
NCT00712335 (7) [back to overview]Sputum GM-CSF Levels
NCT00712335 (7) [back to overview]Sputum Eosinophil Percentages
NCT00712335 (7) [back to overview]Sputum IFN-gamma/IL-5 Ratios
NCT00784550 (6) [back to overview]Mean Change From Baseline in Scores on the Chronic Respiratory Disease Questionnaire-Self-Administered Standardized (CRQ-SAS) at Endpoint
NCT00784550 (6) [back to overview]Mean Change From Baseline in AM (Morning, Approximately 6-9 AM) Pre-dose Forced Expiratory Volume in One Second (FEV1) at Endpoint
NCT00784550 (6) [back to overview]Mean Change From Baseline in 2 Hour Post-dose FVC at Endpoint
NCT00784550 (6) [back to overview]Mean Change From Baseline in 2 Hour Post-dose FEV1 at Endpoint
NCT00784550 (6) [back to overview]Mean Change From Baseline in AM (Morning, Approximately 6-9 AM) Pre-Dose Inspiratory Capacity (IC) at Endpoint
NCT00784550 (6) [back to overview]Mean Change From Baseline in AM (Morning, Approximately 6-9 AM) Pre-dose Forced Vital Capacity (FVC) at Endpoint
NCT00821093 (2) [back to overview]Forced Expiratory Volume in 1 Second (FEV1) Standardized (With Respect to Time) Area Under the Curve (AUC) From 5 Minutes to 11 Hours 45 Minutes Post-dose at the End of the Study (Week 12, Day 84)
NCT00821093 (2) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose at the End of the Study (Week 12 + 1 Day, Day 85)
NCT00876694 (7) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) After 12, 24 and 52 Weeks
NCT00876694 (7) [back to overview]The Number of Participants With a Clinically Notable Systolic Blood Pressure During 52 Weeks of Treatment
NCT00876694 (7) [back to overview]The Number of Participants With a Clinically Notable QTc Interval Value During 52 Weeks of Treatment
NCT00876694 (7) [back to overview]The Number of Participants With a Clinically Notable Pulse Rate During 52 Weeks of Treatment
NCT00876694 (7) [back to overview]The Number of Participants With a Clinically Notable Diastolic Blood Pressure During 52 Weeks of Treatment
NCT00876694 (7) [back to overview]Serum Potassium (mmol/L) at Weeks 4, 8, 12, 24, 36, 44, and 52
NCT00876694 (7) [back to overview]Blood Glucose (mmol/L) 1 Hour Post Dose at Weeks 4, 8, 12, 24, 36, 44, and 52
NCT00927758 (1) [back to overview]Percentage Change From Baseline (for Each Treatment Cycle) in Exhaled Nitric Oxide (eNO)
NCT00975195 (27) [back to overview]Change in On-treatment Cough and Expectoration as Measured by the CASA-Q: Cough Symptoms Domain
NCT00975195 (27) [back to overview]Change in On-treatment Cough and Expectoration as Measured by the CASA-Q: Sputum Impact Domain
NCT00975195 (27) [back to overview]Change in On-treatment Cough and Expectoration as Measured by the CASA-Q: Sputum Symptoms Domain
NCT00975195 (27) [back to overview]Change in On-treatment Exercise Capacity Measured by Six-minute Walk Test (6-MWT)
NCT00975195 (27) [back to overview]Change in On-treatment FEV1 as Measured by Home Based Spirometry
NCT00975195 (27) [back to overview]Change in On-treatment FVC as Measured by Home Based Spirometry
NCT00975195 (27) [back to overview]Change in On-treatment Lung Function as Measured by Trough FEV1
NCT00975195 (27) [back to overview]Change in On-treatment PEFR as Measured by Home Based Spirometry
NCT00975195 (27) [back to overview]Change in On-treatment Physical Health Status as Determined by Body Mass Index (BMI)
NCT00975195 (27) [back to overview]Change in On-treatment Physician Global Evaluation
NCT00975195 (27) [back to overview]Change in On-treatment St Georges Respiratory Questionnaire (SGRQ) Scores: Activity Domain
NCT00975195 (27) [back to overview]Change in On-treatment St Georges Respiratory Questionnaire (SGRQ) Scores: Impact Domain
NCT00975195 (27) [back to overview]Change in On-treatment St Georges Respiratory Questionnaire (SGRQ) Scores: Symptoms Domain
NCT00975195 (27) [back to overview]Change in On-treatment St Georges Respiratory Questionnaire (SGRQ) Scores: Total Score
NCT00975195 (27) [back to overview]Changes in On-treatment Dyspnoea as Measured by the Modified Medical Research Council (MMRC) Dyspnoea Scale
NCT00975195 (27) [back to overview]Severity of On-treatment COPD Exacerbations
NCT00975195 (27) [back to overview]Time to First On-treatment COPD Exacerbation
NCT00975195 (27) [back to overview]Number of Moderate or Severe On-treatment COPD Exacerbations
NCT00975195 (27) [back to overview]Number of On-treatment COPD Exacerbations
NCT00975195 (27) [back to overview]Number of Severe On-treatment COPD Exacerbations
NCT00975195 (27) [back to overview]Proportion of Patients With ≥1 Moderate or Severe On-treatment COPD Exacerbation
NCT00975195 (27) [back to overview]Proportion of Patients With at Least One On-treatment COPD Exacerbation
NCT00975195 (27) [back to overview]Proportion of Patients With at Least One Severe On-treatment COPD Exacerbation.
NCT00975195 (27) [back to overview]Time to First Moderate or Severe On-treatment COPD Exacerbation
NCT00975195 (27) [back to overview]Time to First Severe On-treatment COPD Exacerbation
NCT00975195 (27) [back to overview]Change in On-treatment BODE Index
NCT00975195 (27) [back to overview]Change in On-treatment Cough and Expectoration as Measured by the CASA-Q: Cough Impact Domain
NCT00984659 (20) [back to overview]"SOBDA Threshold for Response Assessed as Mean Change From the Previous Week's SOBDA Score Based on a Participant-completed PGAC Score Rated of Better"
NCT00984659 (20) [back to overview]Known Group Validity for the SOBDA Questionnaire Measured as the Comparison of the Baseline SOBDA Score in the Indicated Categories of the Physician-completed (PyC) mMRC Score at Visit 2
NCT00984659 (20) [back to overview]Change From the Previous Week to the Current Week's SOBDA Score by Participant-completed PGAC Response at Days 8, 15, 22, 29, 36, and 43 and at Visit 3/PD (End of the 6-week Treatment Period or PD)
NCT00984659 (20) [back to overview]Change From Baseline to Last Treatment Week in the SOBDA Score by Physician-completed mMRC and Participant-completed mMRC Responses at Visit 3/PD
NCT00984659 (20) [back to overview]Change From Baseline to Last Treatment Week in the SOBDA Score by CRQ-SAS Dyspnea Domain (DD) Responses at Visit 3/PD
NCT00984659 (20) [back to overview]Change From Baseline to Last Treatment Week in the SOBDA Score by CGI-C Responses at Visit 3/PD
NCT00984659 (20) [back to overview]"SOBDA Threshold for Response as Assessed by Mean Change From Baseline to the Last Treatment Week in the SOBDA Score Based on a CGI-C Response Rated as Better"
NCT00984659 (20) [back to overview]Known Group Validity for the SOBDA Questionnaire Measured as the Comparison of the Baseline SOBDA Score in the Indicated Categories of the Participant-completed (ParC) mMRC Score at Visit 2
NCT00984659 (20) [back to overview]"SOBDA Threshold for Response as Assessed by Mean Change From Baseline to the Last Treatment Week in the SOBDA Score Based on a CRQ-SAS Dyspnea Domain (DD) Response Rated as Better"
NCT00984659 (20) [back to overview]Convergent Validity (CV) for the SOBDA Questionnaire Measured as the Correlation of the Baseline SOBDA Score With the Chronic Respiratory Disease Questionnaire-Self-Administered Standardized (CRQ-SAS) Dyspnea Domain Score at Visit 2
NCT00984659 (20) [back to overview]Convergent Validity for the SOBDA Questionnaire Measured as the Correlation of the Baseline SOBDA Score With the Clinician Global Assessment of Dyspnea Severity (CGI-S) Score at Visit 2
NCT00984659 (20) [back to overview]Internal Consistency (IC) of the Shortness of Breath With Daily Activities (SOBDA) Questionnaire in Participants With Chronic Obstructive Pulmonary Disease (COPD) Assessed as Cronbach's Alpha Value
NCT00984659 (20) [back to overview]SOBDA Threshold for Response Assessed as Mean Change From Baseline to Last Treatment Week in the SOBDA Score Based on Forced Expiratory Volume in One Second (FEV1) Change From Baseline of 50 Milliliters (mL) to <100 mL
NCT00984659 (20) [back to overview]Test-retest Reliability (T-RR) of SOBDA Scores Measured as the Difference in the SOBDA Weekly Score Between Week 1 and Week 2 of the 2-week Run-in Period
NCT00984659 (20) [back to overview]Convergent Validity for the SOBDA Questionnaire Measured as Correlations of the Baseline SOBDA Score With Participant-completed Modified Medical Research Council (mMRC) and Physician-completed mMRC Scores at Visit 2
NCT00984659 (20) [back to overview]Known Group Validity (KGV) for the SOBDA Questionnaire Measured as the Comparison of the Baseline SOBDA Score in the Indicated Categories of CGI-S Scores at Visit 2
NCT00984659 (20) [back to overview]Number of Participants Classified as Responders and Non-responders by Clinician Global Impression of Change Question (CGI-C) Response at Visit 3/PD
NCT00984659 (20) [back to overview]Number of Participants Classified as Responders and Non-responders by CRQ-SAS Dyspnea Domain Response at Visit 3/PD
NCT00984659 (20) [back to overview]Number of Participants Classified as Responders and Non-responders by Physician-completed and Participant-completed mMRC Response at Visit 3/PD
NCT00984659 (20) [back to overview]Participants (Par.) Classified as Responders/Non-responders According to the Patient Global Assessment of Change (PGAC) Response at Days 8, 15, 22, 29, 36, and 43 and at Visit 3/Premature Discontinuation (PD) (the End of the 6-week Treatment Period or PD)
NCT01048333 (5) [back to overview]Average FEV1 During the First 15 Minutes Post Dose
NCT01048333 (5) [back to overview]Average FEV1 During 120 Minutes Post Dose
NCT01048333 (5) [back to overview]Adverse Events
NCT01048333 (5) [back to overview]Percentage of Patients Who Has Achieved at Least 12 % Increase in FEV1
NCT01048333 (5) [back to overview]FEV1(Forced Expiratory Volume in 1 Second) Measured by Spirometry 5 Minutes Post Dose
NCT01079130 (2) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) After 2 Weeks of Treatment
NCT01079130 (2) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) After 1 Day of Treatment
NCT01089127 (2) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose on Day 2
NCT01089127 (2) [back to overview]Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose at the End of the Study (Week 2 + 1 Day, Day 15)
NCT01110200 (5) [back to overview]Number of EXs of COPD Requiring Hospitalization That Occurred More Than 21 Days Post-discharge or Physician's Office Visit for an EX of COPD Requiring Treatment With OCSs or OCSs and ABs
NCT01110200 (5) [back to overview]Number of EXs of COPD Requiring Treatment With OCSs, Treatment With ABs, and/or Hospitalization (Alone and in Combination)
NCT01110200 (5) [back to overview]Number of Participants With an EX of COPD Requiring Treatment With OCSs, Treatment With ABs, and/or Hospitalization
NCT01110200 (5) [back to overview]Number of Par. With Chronic Obstructive Pulmonary Disease (COPD) EXs Requiring Hospitalization That Occurred >21 Days Post-discharge/Physician's Office Visit for a COPD EX Requiring Treatment With Oral Corticosteroids (OCSs) or OCSs and Antibiotics (ABs)
NCT01110200 (5) [back to overview]Number of Participants With the Indicated Number of EXs of COPD Requiring Hospitalization That Occurred More Than 21 Days Post-discharge or Physician's Office Visit for an EX of COPD Requiring Treatment With OCSs or OCSs and ABs
NCT01124422 (19) [back to overview]Mean Change in Respiratory Exchange Ratio (RER) Per Time Slope During the Course of the ESWT From Baseline to Week 8
NCT01124422 (19) [back to overview]Mean Change in Respiratory Rate (RR) at Isotime During the Course of the ESWT From Baseline to Week 8
NCT01124422 (19) [back to overview]Mean Change in Respiratory Rate (RR) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in Scores on the Exercise Dyspnea Scale (EDS) From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in Tidal Volume (VT) at Isotime During the Course of the ESWT From Baseline to Week 8
NCT01124422 (19) [back to overview]Mean Change in Tidal Volume (VT) Per Time Slope During the Course of the ESWT From Baseline to Week 8
NCT01124422 (19) [back to overview]Baseline Dyspnea Index (BDI) at Week 4 and Transition Dyspnea Index (TDI) at Week 8
NCT01124422 (19) [back to overview]Mean Change in Pre-dose and Post-dose Resting Inspiratory Capacity (IC) From Baseline (Week 4) to Week 8
NCT01124422 (19) [back to overview]Mean Change in Scores on the Chronic Respiratory Disease Questionnaire Self-Administered Standardized (CRQ-SAS) Questionnaire From Week 4 to Week 8
NCT01124422 (19) [back to overview]Mean Change in Flow of Oxygen (V'O2) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in Exercise Inspiratory Capacity (EIC) at the End of Exercise From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in EDS at Isotime From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in EIC at 2 to 3.5 Minutes During the Exercise Period From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in Exercise Endurance Time (EET) From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in Flow of Carbon Dioxide (V'CO2) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in Heart Rate (HR) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in HR Per Time Slope During the Course of the ESWT Using Pulse Oximetry From Baseline to Week 8 (Non-OMS Subgroup)
NCT01124422 (19) [back to overview]Mean Change in Minute Ventilation (V'E) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8
NCT01124422 (19) [back to overview]Mean Change in Ratio of Respiratory Rate (RR) to Tidal Volume (VT) or RR/VT at Isotime During the Course of the ESWT From Baseline to Week 8
NCT01147848 (13) [back to overview]Change From Baseline in EQ-5D Visual Analog Scale (VAS) Score at Day 168
NCT01147848 (13) [back to overview]"Percentage of Participants With No Problems in the EQ-5D Descriptive System Dimensions at Day 168/Week 24"
NCT01147848 (13) [back to overview]Change From Baseline in Weighted-mean 24 Hour Serial FEV1 on Day 168/Week 24
NCT01147848 (13) [back to overview]Change From Baseline in Weighted Mean Serial FEV1 Over 0-4 Hours Post First Dose (at Randomization)
NCT01147848 (13) [back to overview]Change From Baseline in Weighted Mean Serial FEV1 Over 0-4 Hours at Day 168
NCT01147848 (13) [back to overview]Change From Baseline in Trough FEV1 at Day 168
NCT01147848 (13) [back to overview]Serial FEV1 (0-24 Hours)
NCT01147848 (13) [back to overview]Number of Participants With the Indicated Time to Onset of Bronchodilator Effect at Day 1
NCT01147848 (13) [back to overview]Number of Participants Obtaining a >=12% and >=200 mL Increase From Baseline in FEV1
NCT01147848 (13) [back to overview]Number of Healthcare Contacts Related to Asthma or the Treatment of Asthma From Baseline to Day 168
NCT01147848 (13) [back to overview]Baseline FEV1 by Completion Status
NCT01147848 (13) [back to overview]Change From Baseline in Asthma Quality of Life Questionnaire (AQLQ) Total Score for Participants 12 Years of Age and Older (AQLQ + 12)
NCT01147848 (13) [back to overview]Change From Baseline in Asthma Control Test (ACT) Scores at Day 168
NCT01172808 (20) [back to overview]Mean Pre-dose Evening FEV1 (FEV1 p.m.) Based on the Weekly Mean Response at Week 24
NCT01172808 (20) [back to overview]Asthma Symptom-free Days Based on the Weekly Mean Response at Week 24
NCT01172808 (20) [back to overview]FEV1 Area Under Curve 0-3 Hours (AUC0-3h) Response
NCT01172808 (20) [back to overview]Mean Number of Puffs of Rescue Medication During the Entire 24-h Day Based on the Weekly Mean Response at Week 24
NCT01172808 (20) [back to overview]Time to First Severe Asthma Exacerbation From the Two Twin Trials 205.419 (NCT01172821) and the Present 205.418 (NCT01172808)
NCT01172808 (20) [back to overview]Trough PEF Response
NCT01172808 (20) [back to overview]FVC Area Under Curve 0-3 Hours (AUC0-3h) Response
NCT01172808 (20) [back to overview]Trough FVC Response
NCT01172808 (20) [back to overview]Trough FEV1 Response
NCT01172808 (20) [back to overview]Total Asthma Quality of Life Questionnaire (AQLQs)) Score
NCT01172808 (20) [back to overview]Total Asthma Control Questionnaire (ACQ) Score at the End of the 24-week Treatment Period
NCT01172808 (20) [back to overview]Time to First Asthma Exacerbation From the Two Twin Trials 205.419 (NCT01172821) and the Present 205.418 (NCT01172808)
NCT01172808 (20) [back to overview]The Responder Rate as Assessed by the ACQ From the Two Twin Trials 205.419 (NCT01172821) and the Present 205.418 (NCT01172808)
NCT01172808 (20) [back to overview]The Responder Rate as Assessed by the ACQ
NCT01172808 (20) [back to overview]PEF Variability
NCT01172808 (20) [back to overview]Peak FVC Within 3 Hours Post-dose Response
NCT01172808 (20) [back to overview]Peak FEV1 Within 3 Hours Post-dose Response
NCT01172808 (20) [back to overview]Mean Pre-dose Morning PEF (PEF a.m.) Based on the Weekly Mean Response at Week 24
NCT01172808 (20) [back to overview]Mean Pre-dose Morning FEV1 (FEV1 a.m.) Based on the Weekly Mean Response at Week 24
NCT01172808 (20) [back to overview]Mean Pre-dose Evening PEF (PEF p.m.) Based on the Weekly Mean Response at Week 24
NCT01172821 (20) [back to overview]The Responder Rate as Assessed by the ACQ From the Two Twin Trials 205.418 (NCT01172808) and the Present 205.419 (NCT01172821)
NCT01172821 (20) [back to overview]Time to First Asthma Exacerbation From the Two Twin Trials 205.418 (NCT01172808) and the Present 205.419 (NCT01172821)
NCT01172821 (20) [back to overview]Time to First Severe Asthma Exacerbation From the Two Twin Trials 205.418 (NCT01172808) and the Present 205.419 (NCT01172821)
NCT01172821 (20) [back to overview]Total Asthma Control Questionnaire (ACQ) Score
NCT01172821 (20) [back to overview]Total Asthma Quality of Life Questionnaire (AQLQs)) Score
NCT01172821 (20) [back to overview]Trough FEV1 Response
NCT01172821 (20) [back to overview]Trough FVC Response
NCT01172821 (20) [back to overview]Trough PEF Response
NCT01172821 (20) [back to overview]Asthma Symptom-free Days Based on the Weekly Mean Response at Week 24
NCT01172821 (20) [back to overview]FEV1 Area Under Curve 0-3 Hours (AUC0-3h) Response
NCT01172821 (20) [back to overview]FVC Area Under Curve 0-3 Hours (AUC0-3h) Response
NCT01172821 (20) [back to overview]Mean Number of Puffs of Rescue Medication During the Entire 24-h Day Based on the Weekly Mean Response at Week 24
NCT01172821 (20) [back to overview]Mean Pre-dose Evening FEV1 (FEV1 p.m.) Based on the Weekly Mean Response at Week 24
NCT01172821 (20) [back to overview]Mean Pre-dose Evening PEF (PEF p.m.) Based on the Weekly Mean Response at Week 24
NCT01172821 (20) [back to overview]Mean Pre-dose Morning FEV1 (FEV1 a.m.) Based on the Weekly Mean Response at Week 24
NCT01172821 (20) [back to overview]Mean Pre-dose Morning PEF (PEF a.m.) Based on the Weekly Mean Response at Week 24
NCT01172821 (20) [back to overview]Peak FEV1 Within 3 Hours Post-dose Response
NCT01172821 (20) [back to overview]Peak FVC Within 3 Hours Post-dose Response
NCT01172821 (20) [back to overview]PEF Variability
NCT01172821 (20) [back to overview]The Responder Rate as Assessed by the ACQ
NCT01181895 (8) [back to overview]Change From Baseline in Weighted-mean 24-hour Serial Forced Expiratory Volume in One Second (FEV1) at Week 12
NCT01181895 (8) [back to overview]Change From Baseline in Individual Serial FEV1 Assessments at the End of the 12-week Treatment Period, Including the 12-hour and 24-hour Time Points
NCT01181895 (8) [back to overview]Number of Participants With the Indicated Global Assessment of Change Questionnaire Responses at the End of Week 4 and Week 12
NCT01181895 (8) [back to overview]Number of Participants With the Indicated Time to an Increase of >=12% and >=200 Milliliters (mL) Above Baseline in FEV1 on Day 1 and Day 84 (0-2 Hours)
NCT01181895 (8) [back to overview]Change From Baseline in Daily AM (Morning) PEF Averaged Over the 12-week Treatment Period
NCT01181895 (8) [back to overview]Change From Baseline in Daily Trough (Pre-dose and Pre-rescue Bronchodilator) PM (Evening) Peak Expiratory Flow (PEF) Averaged Over the 12-week Treatment Period
NCT01181895 (8) [back to overview]Change From Baseline in the Percentage of Rescue-free 24-hour (hr) Periods During the 12-week Treatment Period
NCT01181895 (8) [back to overview]Change From Baseline in the Percentage of Symptom-free 24-hour (hr) Periods During the 12-week Treatment Period
NCT01192178 (8) [back to overview]Mean Duration of Worsening Asthma Symptoms Associated With the Presence of Moderate or Severe URTS or a Confirmed RV Infection
NCT01192178 (8) [back to overview]Number of Asthma Exacerbations Associated With the Presence of Moderate or Severe URTS or a Confirmed RV Infection During the Peak Viral Period
NCT01192178 (8) [back to overview]Mean Percentage of Symptom-free Days
NCT01192178 (8) [back to overview]Mean Percentage of Rescue-free Days
NCT01192178 (8) [back to overview]Mean Percentage of Episode-free (EF) Days
NCT01192178 (8) [back to overview]Mean Percentage of Asthma-control Days
NCT01192178 (8) [back to overview]Mean Asthma Symptom Scores, as an Indicator of Severity, Associated With the Presence of Moderate or Severe Upper Respiratory Tract Symptoms (URTS) or a Confirmed Rhinovirus (RV) Infection at Baseline and During the Peak Viral Period
NCT01192178 (8) [back to overview]Total Number of Asthma Exacerbations Reported During the Treatment Period
NCT01231230 (1) [back to overview]Maximum Change From Baseline in Airway Blood Flow (Qaw)
NCT01290874 (6) [back to overview]Change in Asthma Quality of Life (AQLQ)
NCT01290874 (6) [back to overview]Change in Asthma Control Questionnaire (ACQ)
NCT01290874 (6) [back to overview]Time to Asthma Exacerbation (Mean Number of Exacerbations/Person-year)
NCT01290874 (6) [back to overview]Change in Rescue Medication Use
NCT01290874 (6) [back to overview]Change in FEV1
NCT01290874 (6) [back to overview]Change in Asthma Symptom Utility Index (ASUI)
NCT01312961 (11) [back to overview]Percentage of Participants With Asthma Exacerbation
NCT01312961 (11) [back to overview]Change From Baseline in Peak Expiratory Flow (PEF) to Week 12
NCT01312961 (11) [back to overview]Percentage of Participants With Composite Asthma Events
NCT01312961 (11) [back to overview]Change From Baseline in Number of Nocturnal Awakenings Per Day to Week 12
NCT01312961 (11) [back to overview]Change From Baseline in Number of Inhalations Per Day of Albuterol or Levalbuterol to Week 12
NCT01312961 (11) [back to overview]Change From Baseline in Morning Asthma Symptom Scores to Week 12
NCT01312961 (11) [back to overview]Change From Baseline in Forced Expiratory Flow in One Second (FEV1) to Week 12
NCT01312961 (11) [back to overview]Change From Baseline in Evening Asthma Symptom Scores to Week 12
NCT01312961 (11) [back to overview]Change From Baseline in Asthma Control Questionnaire (5-question Version [ACQ-5]) to Week 12
NCT01312961 (11) [back to overview]Change From Baseline in 22-item Sinonasal Outcome Test (SNOT-22) Score to Week 12
NCT01312961 (11) [back to overview]Time to First Asthma Exacerbation: Kaplan-Meier Estimates at Week 4, Week 8 and Week 12
NCT01315249 (11) [back to overview]Mean Change From Baseline in Daily Number of Puffs of Rescue Medication
NCT01315249 (11) [back to overview]Inspiratory Capacity (IC) at All-time Points (26 Weeks)
NCT01315249 (11) [back to overview]Inspiratory Capacity (IC) at All-time Points (12 Weeks)
NCT01315249 (11) [back to overview]Forced Vital Capacity at All-time Points (Week 26)
NCT01315249 (11) [back to overview]Forced Vital Capacity at All-time Points (Week 12)
NCT01315249 (11) [back to overview]Focal Score of the Transitional Dyspnea Index (TDI)
NCT01315249 (11) [back to overview]Change From Baseline in Symptom Scores Reported Using the Ediary
NCT01315249 (11) [back to overview]Forced Expiratory Volume in 1 Second Area Under the Curve (FEV1 AUC) 0-12
NCT01315249 (11) [back to overview]Standardized Forced Expiratory Volume in 1 Second Area Under the Curve (FEV1 AUC) 0-12 Hours
NCT01315249 (11) [back to overview]Total Score of the St. George's Respiratory Questionnaire (SGRQ-C)
NCT01315249 (11) [back to overview]Number of Participants With Adverse Events
NCT01323621 (2) [back to overview]Time to Onset on Treatment Day 1
NCT01323621 (2) [back to overview]Change From Baseline Trough in 24-Hour Weighted Mean FEV1 on Treatment Day 84
NCT01323634 (2) [back to overview]Time to Onset on Treatment Day 1
NCT01323634 (2) [back to overview]Change From Baseline Trough in 24-hour Weighted-mean FEV1 on Treatment Day 84
NCT01331694 (2) [back to overview]Time to First Chronic Obstructive Pulmonary Disease (COPD) Event
NCT01331694 (2) [back to overview]Average Annual Adjusted Post-Index COPD-Related Costs
NCT01332357 (1) [back to overview]Number of Participants With an Asthma-related Event Occurring Between 1 and 6 Months Following the Index Event
NCT01332461 (3) [back to overview]Mean Monthly COPD-related Costs Per Participant
NCT01332461 (3) [back to overview]Number of Participants Having a Hospitalization or Emergency Room (ER) Visit Related to Chronic Obstructive Pulmonary Disease (COPD) Represented Per 100 Person-years
NCT01332461 (3) [back to overview]Number of Participants Having a COPD-related Event Related to Chronic Obstructive Pulmonary Disease (COPD) Represented Per 100 Person-years
NCT01337336 (4) [back to overview]Number of Participants With the Indicated COPD-related Exacerbations
NCT01337336 (4) [back to overview]Mean Annual COPD-related Costs Per Participant
NCT01337336 (4) [back to overview]Number of Participants With Any Chronic Obstructive Pulmonary Disease (COPD)-Related Exacerbation
NCT01337336 (4) [back to overview]Number of the Indicated COPD-related Exacerbations
NCT01342913 (3) [back to overview]Change From Baseline Trough in 24-hour Weighted-mean FEV1 on Treatment Day 84
NCT01342913 (3) [back to overview]Time to Onset on Treatment Day 1
NCT01342913 (3) [back to overview]Change From Baseline in Trough FEV1 on Treatment Day 85
NCT01347060 (3) [back to overview]Mean Number of Post-index Asthma-related Events Measured Using Medical and Pharmacy Claims
NCT01347060 (3) [back to overview]Mean Asthma-related Costs in the Post-index Period
NCT01347060 (3) [back to overview]Mean Number of Albuterol (Short-acting β-Agonists) Canisters Dispensed Per Pharmacy Claim Per Participant
NCT01381471 (2) [back to overview]Mean Number of Pharmacy Claims by Participants During the Post-Index Period
NCT01381471 (2) [back to overview]Mean Number of Healthcare Encounters Incurred by Participants During the Post-Index Period
NCT01387178 (3) [back to overview]Number of COPD-related Healthcare Encounters
NCT01387178 (3) [back to overview]Mean Number of COPD Exacerbations
NCT01387178 (3) [back to overview]Post-index Period COPD-related, Unadjusted Costs
NCT01391559 (1) [back to overview]Change in Forced Expiratory Volume in 1 Second (FEV1) From Baseline at Two Hours After Inhalation of the Study Medication
NCT01437995 (5) [back to overview]Pulmonary Function- Change in Peak Expiratory Flow
NCT01437995 (5) [back to overview]Pulmonary Function: Change in FEV1/FVC Ratio
NCT01437995 (5) [back to overview]Change in Pulmonary Function: FEV1 and FVC
NCT01437995 (5) [back to overview]Treatment Failure
NCT01437995 (5) [back to overview]Rate of Episodes of Poor Asthma Control
NCT01536587 (34) [back to overview]Change From Baseline in MSNA (Evaluated by Microneurography as Bursts/Minute) at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Normalized Low Frequency (LF) Power at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Absolute Low Frequency (LF) Power at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Arterial Stiffness at Baseline (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in MSNA (Evaluated by Microneurography as Bursts/100 Heart Beats) at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Tidal Volume at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Systolic and Diastolic Blood Pressure (BP) at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Oxygen Saturation Measured Via Pulse Oxymetry (SpO2) at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Absolute Low Frequency (LF) Power at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Standard Deviation of NN Intervals (SDNN) at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Square Root of the Mean Squared Difference of Successive NNs (RMSSD) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Square Root of the Mean Squared Difference of Successive NNs (RMSSD) at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Change From Baseline in Spontaneous Baroreflex Sensitivity (BRS) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Change From Baseline in Spontaneous Baroreflex Sensitivity (BRS) at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Change From Baseline in Respiratory Rate at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Standard Deviation of NN Intervals (SDNN) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Change From Baseline in Respiratory Minute Volume at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Normalized Low Frequency (LF) Power at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Change in Muscle Sympathetic Nerve Activity (MSNA) at 2 Hours (Week 0)
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Heart Rate at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Normalized High Frequency (HF) Power at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Normalized High Frequency Power (HF) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Number of Participants With Diastolic Dysfunction on Echocardiography at Baseline (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Lung Function (Forced Vital Capacity [FVC], Functional Residual Capacity [FRC; Body and Helium], Total Lung Capacity [TLC], and Residual Volume [RV]) at Baseline (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Transcutaneous Carbon Dioxide (tCO2) at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Absolute High Frequency (HF) Power at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Absolute High Frequency (HF) Power at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Change From Baseline in Forced Expiratory Volume in One Second (FEV1) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Change From Baseline in Forced Expiratory Volume in One Second (FEV1) at 2 Hours (Week 0) and at Week 4 (ITT Population)
NCT01536587 (34) [back to overview]Change From Baseline in Catecholamines (Plasma Norepinephrine) at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Catecholamines (Plasma Epinephrine) at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Catecholamines (Brain Natriuretic Peptide [BNP]) at 2 Hours (Week 0) and at Week 4
NCT01536587 (34) [back to overview]Change From Baseline in Heart Rate Variability (HRV): Heart Rate at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)
NCT01536587 (34) [back to overview]Change From Baseline in MSNA (Evaluated by Microneurography as Bursts/Minute) at 2 Hours (Week 0)
NCT01555138 (11) [back to overview]TDI Focal Score at Week 12 and Week 26: Treatment Comparisons
NCT01555138 (11) [back to overview]St Georges Respiratory Questionnaire for COPD
NCT01555138 (11) [back to overview]Number of COPD Exacerbations Per Patient Over 26 Weeks: Treatment Comparisons (Without Imputation; Full Analysis Set)
NCT01555138 (11) [back to overview]Rescue Medication Use Over 26 Weeks: Percentage of 'Days With no Rescue Use'
NCT01555138 (11) [back to overview]Trough FEV1 (L) at Week 26 (Imputed With LOCF): Treatment Comparisons
NCT01555138 (11) [back to overview]Trough Forced Expiratory Volume in One Second (FEV1) at 12 Weeks (Imputed With LOCF): Treatment Comparisons
NCT01555138 (11) [back to overview]Analysis of AUC (5 Min - 4 h) for FEV1 (L) at Week 12 and Week 26: Treatment Comparison
NCT01555138 (11) [back to overview]FEV1 (L) at Individual Time Points After 12 Weeks Treatment: Treatment Comparisons
NCT01555138 (11) [back to overview]FEV1 (L) at Individual Time Points After 26 Weeks Treatment: Treatment Comparisons
NCT01555138 (11) [back to overview]FVC Over 26 Weeks of Treatment
NCT01555138 (11) [back to overview]Mean Daily Number of Puffs of Rescue Medication Used Over 26 Weeks of Treatment
NCT01636076 (28) [back to overview]FEV1 (L) on Day 1 Between-treatment Comparisons of AUC (5min - 4h)
NCT01636076 (28) [back to overview]FEV1 AUC (5 Min-4 h),
NCT01636076 (28) [back to overview]FEV1/FVC at Each Timepoint
NCT01636076 (28) [back to overview]Forced Vital Capacity (FVC) at Each Timepoint
NCT01636076 (28) [back to overview]Analysis of the Proportion of Subjects With a Clinically Important Improvement of >=1 Point in the TDI (Transitional Dyspnoea Index)Focal Score by Visit
NCT01636076 (28) [back to overview]Mixed Model for Repeated Measures (MMRM): Between-treatment Comparisons for FEV1 (L), by Visit and Timepoint
NCT01636076 (28) [back to overview]Mixed Model for Repeated Measures (MMRM): Between-treatment Comparisons for Trough FEV1 (L) on Day 85
NCT01636076 (28) [back to overview]Patient Reported Outcome Measures: COPD Assessment Test
NCT01636076 (28) [back to overview]Patient Reported Outcome Measures: Medical Outcome Study (MOS) Sleep Scale: Sleep Quantity Subscale
NCT01636076 (28) [back to overview]Patient Reported Outcome Measures: SGRQ (St. George's Respiratory Questionnaire)
NCT01636076 (28) [back to overview]Pharmacokinetic Parameter--AUC0-t
NCT01636076 (28) [back to overview]Pharmacokinetic Parameter--Tmax
NCT01636076 (28) [back to overview]The Percentage of Patients Who Permanently Discontinued Due to COPD Exacerbation
NCT01636076 (28) [back to overview]Plasma Cortisol Concentrations at Each Timepoint
NCT01636076 (28) [back to overview]Plasma Drug Concentrations (Pharmacokinetics) at Each Timepoint
NCT01636076 (28) [back to overview]The Usage of Rescue Medication (Short Acting β2-agonist)
NCT01636076 (28) [back to overview]Time to First COPD Exacerbation
NCT01636076 (28) [back to overview]Total Amount (in Doses) of Systemic Corticosteroid Used to Treat COPD Exacerbation During the 12 Week Treatment Period
NCT01636076 (28) [back to overview]Trough FEV1 After First Dose and After 4 Weeks of Treatment
NCT01636076 (28) [back to overview]Patient Reported Outcome Measures: Medical Outcome Study (MOS) Sleep Scale: Without Quantity Subscale
NCT01636076 (28) [back to overview]Duration (in Days) of COPD Exacerbations
NCT01636076 (28) [back to overview]Percentage of Patients With at Least One Exacerbation up to Week 12
NCT01636076 (28) [back to overview]Summary Statistics of COPD Exacerbations over12 Weeks as Defined by Chronic Pulmonary Disease Tool (EXACT)
NCT01636076 (28) [back to overview]The Overall Change in Usage of Rescue Medication (Short Acting β2-agonist) .
NCT01636076 (28) [back to overview]Mixed Model for Repeated Measures (MMRM): Between-treatment Comparisons for AUC (5 Min - 23 h 45 Min) for FEV1 (L) on Day 28 and Day 84 (Full Analysis Set, 24-h Profiling Subgroup)
NCT01636076 (28) [back to overview]Time (in Days) to Permanent Study Discontinuation Due to COPD Exacerbation
NCT01636076 (28) [back to overview]Annual Rate of COPD Exacerbations
NCT01636076 (28) [back to overview]Pharmacokinetic Parameter: Cmax
NCT01696214 (3) [back to overview]Percent (%) Perdicted FEV1 Changes
NCT01696214 (3) [back to overview]The Asthma Symptom Utility Index (ASUI)
NCT01696214 (3) [back to overview]Asthma Control Test
NCT01706328 (3) [back to overview]Change From Baseline in Trough FEV1 on Treatment Day 85
NCT01706328 (3) [back to overview]Change From Baseline Trough in Weighted-mean 24-hour Serial Forced Expiratory Volume in One Second (FEV1) on Treatment Day 84
NCT01706328 (3) [back to overview]Time to Onset on Treatment Day 1
NCT01709903 (9) [back to overview]Rescue Medication Use: Summary of the Mean Daily, Daytime and Nighttime Number of Puffs of Rescue Medication, by 4 Weekly Intervals
NCT01709903 (9) [back to overview]Health Related Quality of Life Analysis of SGRQ Total Score After 26 Weeks of Treatment
NCT01709903 (9) [back to overview]Analysis of Trough FVC (L) Over the Whole Treatment Period
NCT01709903 (9) [back to overview]Analysis of the TDI Focal Score Over the Whole Treatment Period
NCT01709903 (9) [back to overview]Analysis of FEV1 (L) Trough Response (Pre-dose) Over the Whole Treatment Period
NCT01709903 (9) [back to overview]Trough Forced Expiratory Volume in One Second (FEV1) Following 26 Weeks of Treatment to Demonstrate the Superiority of QVA 110/50μg o.d. to Fluticasone/Salmeterol 500/50 μg b.i.d
NCT01709903 (9) [back to overview]Trough Forced Expiratory Volume in One Second (FEV1) Following 26 Weeks of Treatment to Demonstrate the Non-inferiority of QVA149 110/50 μg o.d. to Fluticasone/Salmeterol 500/50 μg b.i.d
NCT01709903 (9) [back to overview]Symptoms Reported Using E-diary Over 12 and 26 Weeks of Treatment
NCT01709903 (9) [back to overview]Standardized Forced Expiratory Volume in One Second (FEV1) Area Under the Curve (AUC) 0-4 Hours
NCT01751113 (11) [back to overview]Post-dose sGaw at 30, 75, 120 and 240 Minutes Post Dose at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Post-dose sRaw at 30, 75, 120 and 240 Minutes Post Dose at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Trough Forced Expiratory Volume in One Second (FEV1), Forced Vital Capacity (FVC), Inspiratory Capacity (IC), RV, TLC, and TGV at Each Clinic Visit Prior to the Morning Dose and Before the Use of Rescue Medication at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Post-dose FEV1/FVC Ratio (Measured at Trough) at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]AUC (0-4hr) Specific Airway Resistance (sRaw) After the Morning Dose of Each Study Medication at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Area Under the Curve Calculated From 0 to 4 Hours (AUC[0-4hr]) Specific Conductance (sGaw) After the Morning Dose of Study Medication at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Use of Rescue Medication (Number of Occasions Per 24-hour Period) as Recorded in the Daily Record Card at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Trough FEV1/FVC Ratio, at Each Clinic Visit Prior to the Morning Dose and Before the Use of Rescue Medication at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Trough sGaw Measured at Each Clinic Visit Prior to the Morning Dose and Before the Use of Rescue Medication at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Trough sRaw Measured at Each Clinic Visit Prior to the Morning Dose and Before the Use of Rescue Medication at Day 28 of Each Treatment Period
NCT01751113 (11) [back to overview]Post-dose FEV1, FVC, IC, RV, TLC and TGV (Measured at Trough) at Day 28 of Each Treatment Period
NCT01762800 (21) [back to overview]Number of Participants in Each Treatment Efficacy Grade Evaluated by Physician
NCT01762800 (21) [back to overview]Number of Participants in Each Treatment Efficacy Grade Evaluated by Participants
NCT01762800 (21) [back to overview]Forced Expiratory Volume in One Second (FEV1)
NCT01762800 (21) [back to overview]Change From Baseline in FEV1
NCT01762800 (21) [back to overview]Percentage of Participants Who Stepped Down From TRIPLE Therapy to Initial Randomized Treatment
NCT01762800 (21) [back to overview]Change From Baseline in CAT Total Score
NCT01762800 (21) [back to overview]Time to First Switching to TRIPLE Therapy
NCT01762800 (21) [back to overview]Time to First Exacerbation by Physician's Diagnosis
NCT01762800 (21) [back to overview]Time to First Exacerbation by EXAcerbations of Chronic Pulmonary Disease Tool (EXACT)
NCT01762800 (21) [back to overview]Percentage of Participants Who Used Relief Medication (Salbutamol)
NCT01762800 (21) [back to overview]EXACT Total Score.
NCT01762800 (21) [back to overview]EXACT Respiratory Symptoms (E-RS) Total Score
NCT01762800 (21) [back to overview]E-RS Subscale Score
NCT01762800 (21) [back to overview]Continuation Percentage of Participants Managed by Randomized Treatment Plus TRIPLE Therapy
NCT01762800 (21) [back to overview]Percentage of Participants Who Switched to TRIPLE Therapy
NCT01762800 (21) [back to overview]Comparison of Number of Exacerbations Between Two Detection Methods: EXACT and Physician Diagnosis
NCT01762800 (21) [back to overview]Percentage of Participants Who Required Additional Treatment to TRIPLE Therapy
NCT01762800 (21) [back to overview]Percentage of Participants Who Dropped Out
NCT01762800 (21) [back to overview]Percentage of Participants Managed by TRIPLE Therapy
NCT01762800 (21) [back to overview]Chronic Obstructive Pulmonary Disease (COPD) Assessment Test (CAT) Total Score
NCT01762800 (21) [back to overview]Percentage of Participants Who Were Able to Remain on the Randomized Treatment
NCT01772134 (4) [back to overview]Change From Baseline in Weighted Mean 0-6 Hour FEV1 Obtained Post-dose at Day 84
NCT01772134 (4) [back to overview]Change From Baseline in the Trough Forced Expiratory Volume in One Second (FEV1) on Day 85
NCT01772134 (4) [back to overview]Change From Baseline in the Mean Percentage of Rescue-free Days Over Weeks 1-12
NCT01772134 (4) [back to overview]Change From Baseline in the Mean Number of Puffs Per Day of Rescue Albuterol/Salbutamol Over Weeks 1-12
NCT01772147 (4) [back to overview]Change From Baseline in the Mean Percentage of Rescue-free Days Over Weeks 1-12
NCT01772147 (4) [back to overview]Change From Baseline in the Mean Number of Puffs Per Day of Rescue Albuterol/Salbutamol Over Weeks 1-12
NCT01772147 (4) [back to overview]Change From Baseline in Weighted Mean 0-6 Hour FEV1 Obtained Post-dose at Day 84
NCT01772147 (4) [back to overview]Change From Baseline in the Trough Forced Expiratory Volume in One Second (FEV1) on Day 85
NCT01772368 (6) [back to overview]Time of Maximum Observed Plasma Concentration (Tmax) of Salmeterol
NCT01772368 (6) [back to overview]Standardized Baseline-Adjusted Area Under the Curve For Forced Expiratory Volume In 1 Second Over 12 Hours Post-dose (FEV1 AUC0-12)
NCT01772368 (6) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Salmeterol
NCT01772368 (6) [back to overview]Patients With Treatment-Emergent Adverse Experiences (TEAE) During the Treatment Period
NCT01772368 (6) [back to overview]Change From Baseline at 12 Hours Post-Dose in Forced Expiratory Volume in One Second (FEV1) By Treatment
NCT01772368 (6) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the Time of the Last Measurable Concentration (AUC0-t) of Salmeterol
NCT01794780 (6) [back to overview]COPD Exacerbation
NCT01794780 (6) [back to overview]Change From Baseline in Forced Expiratory Volume in 1 Second (FEV1)
NCT01794780 (6) [back to overview]Change From Baseline in Forced Expiratory Volume in 1 Second (FEV1)
NCT01794780 (6) [back to overview]Change From Baseline in Questionnaire COPD Assessment Test (CAT) Score
NCT01794780 (6) [back to overview]Change From Baseline Questionnaire Transition Dyspnea Index (TDI) Score
NCT01794780 (6) [back to overview]Change in Health Status Questionnaire MMRC
NCT01817764 (2) [back to overview]Change From Baseline in Trough FEV1 on Day 85
NCT01817764 (2) [back to overview]Change From Baseline in 24-hour Weighted-mean Serial FEV1 on Treatment Day 84
NCT01822899 (2) [back to overview]Change From Baseline (BL) in 0 to 24 Hour Weighted Mean Serial Forced Expiratory Volume in One Second (FEV1) at Day 84
NCT01822899 (2) [back to overview]Change From Baseline (BL) in Trough Forced Expiratory Volume in One Second (FEV1) at Day 85
NCT01907334 (1) [back to overview]Total Airway Resistance Increase
NCT01908140 (2) [back to overview]Peak Forced Expiratory Volume in One Second (FEV1) at Week 24
NCT01908140 (2) [back to overview]Transition Dyspnoea Index (TDI) Focal Score at Week 24
NCT01933984 (8) [back to overview]Rapidity of ∆Raw Change
NCT01933984 (8) [back to overview]The Participants of Breathing Without Assistance by Day 28
NCT01933984 (8) [back to overview]Numbers of Episode of Drug-related Adverse Effect
NCT01933984 (8) [back to overview]Number of Episode of Nosocomial Pneumonia
NCT01933984 (8) [back to overview]Number of Total Puff of Rescue Short-acting Bronchodilator
NCT01933984 (8) [back to overview]Ventilator-free Days From Day 1 to 28
NCT01933984 (8) [back to overview]∆Raw (the Difference Between Measured and Target Airway Resistance)
NCT01933984 (8) [back to overview]Mortality Rate
NCT01969721 (5) [back to overview]FEV1 AUC (0-12h) Change From Patient Baseline After 6 Weeks of Treatment
NCT01969721 (5) [back to overview]FEV1 AUC (12-24h) Change From Patient Baseline After 6 Weeks of Treatment
NCT01969721 (5) [back to overview]FEV1 Peak (0-3h) Change From Patient Baseline After 6 Weeks of Treatment
NCT01969721 (5) [back to overview]Trough FEV1 Change From Patient Baseline After 6 Weeks of Treatment
NCT01969721 (5) [back to overview]FEV1 AUC (0-24h) Change From Patient Baseline After 6 Weeks of Treatment
NCT02024204 (10) [back to overview]Spirometry Measures
NCT02024204 (10) [back to overview]Score on Voice Handicap Index 10 (VHI-10)
NCT02024204 (10) [back to overview]Total EoS (Eosinophil) Counts
NCT02024204 (10) [back to overview]Total IgE (Immunoglobulin E) Levels
NCT02024204 (10) [back to overview]Forced Oscillation Technique (FOT) Measures
NCT02024204 (10) [back to overview]Score on Leicester Cough Questionnaire (LCQ)
NCT02024204 (10) [back to overview]Levels of Fractional Exhaled Nitric Oxide (FeNO)
NCT02024204 (10) [back to overview]Number of Participants With Positive Level of Paradoxical Vocal Fold Movement (PVFM)
NCT02024204 (10) [back to overview]Number of Participants With Positive Level of Bronchial Hyperreactivity (BHR)
NCT02024204 (10) [back to overview]Rhinosinusitis Score on International Classification of Sleep Disorders (ICSD)
NCT02055352 (5) [back to overview]Change From Baseline in Mean Daily Number of Puffs of Rescue Medication Used Over the 24 Week Treatment
NCT02055352 (5) [back to overview]Change From Baseline in Trough Forced Expiratory Volume in 1 Second (Non-inferiority Analysis).
NCT02055352 (5) [back to overview]Change From Baseline in Trough Forced Expiratory Volume in 1 Second at Week 24 (Analysis of Superiority)
NCT02055352 (5) [back to overview]Change in Health Status - mMRC
NCT02055352 (5) [back to overview]Change in Health Status - SGRQ-C
NCT02061280 (7) [back to overview]Asthma Control Test Scores at Screening (Visit 1, Week -8)
NCT02061280 (7) [back to overview]Caregiver Research Participant Assessment Score at Screening (Visit 1, Week -8)
NCT02061280 (7) [back to overview]Spirometry Quality Control Grade
NCT02061280 (7) [back to overview]Caregiver Research Participant Assessment Score at Study End (Visit 6, Week 12)
NCT02061280 (7) [back to overview]Adolescent Research Participant Assessment Score at Screening (Visit 1, Week -8)
NCT02061280 (7) [back to overview]Adolescent Research Participant Assessment Score at Study End (Visit 6, Week 12)
NCT02061280 (7) [back to overview]Asthma Control Test Score at Final Visit (Visit 6, Week12)
NCT02139644 (9) [back to overview]Change From Baseline in the Weekly Average of the Total Daily (24-hour) Use of Albuterol/Salbutamol Inhalation Aerosol Over the 12-Week Treatment Period
NCT02139644 (9) [back to overview]Patients With Treatment-Emergent Adverse Experiences (TEAE) During the Treatment Period
NCT02139644 (9) [back to overview]Kaplan-Meier Estimates for Time to 15% and 12% Improvement From Baseline in FEV1 Postdose on Day 1
NCT02139644 (9) [back to overview]Standardized Baseline-Adjusted Forced Expiratory Volume in 1 Second (FEV1) Area Under the Effect Curve From Time Zero to 12 Hours Postdose (FEV1 AUEC0-12h) at Week 12
NCT02139644 (9) [back to overview]Kaplan-Meier Estimate of Probability of Remaining in Study At Week 12
NCT02139644 (9) [back to overview]Change From Baseline in the Weekly Average of the Total Daily Asthma Symptom Score Over the 12-Week Treatment Period
NCT02139644 (9) [back to overview]Change From Baseline in the Weekly Average of the Daily Morning Trough Peak Expiratory Flow (PEF) Over the 12 Week Treatment
NCT02139644 (9) [back to overview]Change From Baseline in the Asthma Quality of Life Questionnaire With Standardized Activities (AQLQ(S)) Score at Endpoint for Patients >=18 Years Old
NCT02139644 (9) [back to overview]Change From Baseline in Morning Trough Forced Expiratory Volume in 1 Second (FEV1) at Week 12
NCT02141854 (9) [back to overview]Change From Baseline in Morning Trough Forced Expiratory Volume in 1 Second (FEV1) at Week 12
NCT02141854 (9) [back to overview]Change From Baseline in the Asthma Quality of Life Questionnaire With Standardized Activities (AQLQ(S)) Score at Endpoint for Patients >=18 Years Old
NCT02141854 (9) [back to overview]Change From Baseline in the Weekly Average of the Daily Morning Trough Peak Expiratory Flow (PEF) Over the 12 Week Treatment
NCT02141854 (9) [back to overview]Change From Baseline in the Weekly Average of the Total Daily (24-hour) Use of Albuterol/Salbutamol Inhalation Aerosol Over the 12-Week Treatment Period
NCT02141854 (9) [back to overview]Change From Baseline in the Weekly Average of the Total Daily Asthma Symptom Score Over the 12-Week Treatment Period
NCT02141854 (9) [back to overview]Kaplan-Meier Estimate of Probability of Remaining in Study At Week 12
NCT02141854 (9) [back to overview]Standardized Baseline-Adjusted Forced Expiratory Volume in 1 Second (FEV1) Area Under the Effect Curve From Time Zero to 12 Hours PostDose (FEV1 AUEC0-12) at Week 12
NCT02141854 (9) [back to overview]Kaplan-Meier Estimates for Time to 15% and 12% Improvement From Baseline in FEV1 Postdose on Day 1
NCT02141854 (9) [back to overview]Patients With Treatment-Emergent Adverse Experiences (TEAE) During the Treatment Period
NCT02175771 (6) [back to overview]Analysis of 24-Hour Urine Cortisol Free Over the 26-Week Treatment Period
NCT02175771 (6) [back to overview]Shifts From Baseline to Endpoint in Electrocardiogram (ECG) Findings
NCT02175771 (6) [back to overview]Participants With Treatment-Emergent Adverse Experiences (TEAE) During the Treatment Period
NCT02175771 (6) [back to overview]Participants With Potentially Clinically Significant Abnormal Vital Signs During the Treatment Period
NCT02175771 (6) [back to overview]Participants With Positive Swab Test Results for Oral Candidiasis
NCT02175771 (6) [back to overview]Change From Baseline in Trough Forced Expiratory Volume in 1 Minute (FEV1) Over the 26-Week Treatment Period
NCT02232087 (6) [back to overview]Max Heart Rate
NCT02232087 (6) [back to overview]Max Plasma Glucose Level
NCT02232087 (6) [back to overview]Max QTcB
NCT02232087 (6) [back to overview]Plasma Potassium Level
NCT02232087 (6) [back to overview]Relative Potency Max Heart Rate
NCT02232087 (6) [back to overview]Relative Potency QTcB Interval
NCT02245672 (4) [back to overview]FEV1 Trough Value (Assay Sensitivity)
NCT02245672 (4) [back to overview]Forced Exhaled Volume in 1 Sec (FEV1) Area Under the Effect Curve on Day 1 (Bioequivalence)
NCT02245672 (4) [back to overview]Forced Exhaled Volume in 1 Sec (FEV1) Area Under the Effect Curve on Day 1 (Assay Sensitivity)
NCT02245672 (4) [back to overview]FEV1 Trough Value (Bioequivalence)
NCT02260492 (3) [back to overview]Area Under the Serial FEV1-time Curve (AUC 0-12h)
NCT02260492 (3) [back to overview]Number of Participants With Adverse Events
NCT02260492 (3) [back to overview]FEV1 Trough
NCT02301975 (7) [back to overview]Change From Baseline in PM FEV1 Using Per Protocol (PP) Population
NCT02301975 (7) [back to overview]Change From Baseline in Evening (Post Meridiem [PM]) Forced Expiratory Volume in One Second (FEV1) Using Intent-to-Treat (ITT) Population
NCT02301975 (7) [back to overview]Change From Baseline in Morning (Ante Meridiem [AM]) Peak Expiratory Flow (PEF)
NCT02301975 (7) [back to overview]Change From Baseline in PM PEF
NCT02301975 (7) [back to overview]Change From Baseline in the Percentage of Rescue-free 24-hour Periods
NCT02301975 (7) [back to overview]Change From Baseline in the Percentage of Symptom-free 24-hour Periods
NCT02301975 (7) [back to overview]Percentage of Participants With Asthma Control Test (ACT) Score Greater Than or Equal to 20
NCT02398188 (3) [back to overview]Percent Change in Waist Circumference
NCT02398188 (3) [back to overview]Percent Change in the Patient Reported Global Abdominal Perception Score
NCT02398188 (3) [back to overview]Percentage of Subjects Who Achieved a Composite P-GAPS1/CPnS2 Response
NCT02433834 (7) [back to overview]Change From Baseline in Asthma Control Questionnaire (ACQ-5) on Day 15
NCT02433834 (7) [back to overview]Change From Baseline in Average Daily Post-dose PEFR Over 14 Days
NCT02433834 (7) [back to overview]Change From Baseline in Average Daily Pre-dose PEFR Over 14 Days
NCT02433834 (7) [back to overview]Change From Baseline in Average Daily Rescue Medication Use Over 14 Days
NCT02433834 (7) [back to overview]Change From Baseline in Morning Pre-dose Trough FEV1 on Day 15
NCT02433834 (7) [back to overview]FEV1 AUC0-3 on Day 15
NCT02433834 (7) [back to overview]Peak Change From Baseline in FEV1 Within 3 Hours Post-dosing on Day 15
NCT02441114 (3) [back to overview]Area Under the Concentration Versus Time Curve (AUClast)
NCT02441114 (3) [back to overview]Maximum Observed Concentration (Cmax)
NCT02441114 (3) [back to overview]Time to Maximum Concentration (Tmax)
NCT02446418 (3) [back to overview]Change From Baseline in ACT Total Score at Week 24
NCT02446418 (3) [back to overview]Change From Baseline in Asthma Control Test (ACT) Total Score at Week 12
NCT02446418 (3) [back to overview]Percentage of Participants With Correct Use of Device, Defined as Not Making Any Critical or Non-critical Errors, at Week 12, and at Week 24 Independently of the Use at Week 12
NCT02516592 (5) [back to overview]Change From Baseline in FVC (Forced Vital Capacity)
NCT02516592 (5) [back to overview]Change From Baseline in Mean Daily Use of Rescue Medication
NCT02516592 (5) [back to overview]Change From Baseline in Total Symptom Score- CAT (COPD Assessment Test)
NCT02516592 (5) [back to overview]Change From Baseline in Trough Pre-dose FEV1 in Both Arms
NCT02516592 (5) [back to overview]Transitional Dyspnea Index (TDI) Focal Score
NCT02554786 (27) [back to overview]Time in Days to Permanent Discontinuation of Study Medication Due to Asthma Exacerbations
NCT02554786 (27) [back to overview]Pre-dose FEV1 at Weeks 4 and 12
NCT02554786 (27) [back to overview]Percentage of Participants Achieving the Minimal Important Difference (MID) ACQ ≥ 0.5 at Weeks 26 and 52
NCT02554786 (27) [back to overview]Percentage of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT02554786 (27) [back to overview]Trough FEV1 Measured After 26 Weeks of Treatment
NCT02554786 (27) [back to overview]Percentage of Participants With at Least One Asthma Exacerbation by Exacerbation Category
NCT02554786 (27) [back to overview]Trough FEV1 at Week 52
NCT02554786 (27) [back to overview]Total Amounts of Systemic Corticosteroids (in Doses) Used to Treat Asthma Exacerbations
NCT02554786 (27) [back to overview]Time to First Hospitalization for Asthma Exacerbation
NCT02554786 (27) [back to overview]Change Form Baseline in Percentage of Mornings With no Symptoms on Awakening
NCT02554786 (27) [back to overview]Percentage of Participants With Composite Endpoint of Serious Asthma Outcomes
NCT02554786 (27) [back to overview]Post Dose FEV1 (5 Minutes-1 Hour)
NCT02554786 (27) [back to overview]Trough Forced Vital Capacity (FVC)
NCT02554786 (27) [back to overview]Percentage of Participants Who Permanently Discontinued Study Medication Due to Asthma Exacerbations
NCT02554786 (27) [back to overview]Change From Baseline in Percentage of Nights With no Night-time Awakenings
NCT02554786 (27) [back to overview]Change From Baseline in Percentage of Asthma Symptoms Free Days
NCT02554786 (27) [back to overview]Trough Forced Expiratory Volume in One Second (Trough FEV1) at Week 26
NCT02554786 (27) [back to overview]Change Form Baseline in Percentage of Days With no Daytime Symptoms
NCT02554786 (27) [back to overview]Trough Forced Expiratory Flow (FEF)Between 25% and 75% of FVC (FEF25-75)
NCT02554786 (27) [back to overview]Time to First Asthma Exacerbation by Exacerbation Category
NCT02554786 (27) [back to overview]Annual Rate of Asthma Exacerbations by Exacerbation Category
NCT02554786 (27) [back to overview]Asthma Control Questionnaire (ACQ-7) at Weeks 4, 12, 26 and 52
NCT02554786 (27) [back to overview]Asthma Quality of Life Questionnaire (AQLQ)
NCT02554786 (27) [back to overview]Change From Baseline in Morning and Evening Peak Expiratory Flow Rate (PEF) Over 26 and 52 Weeks of Treatment
NCT02554786 (27) [back to overview]Change From Baseline in Percentage of Rescue Medication Free Days
NCT02554786 (27) [back to overview]Rescue Medication Usage
NCT02554786 (27) [back to overview]Duration in Days of Asthma Exacerbations by Exacerbation Category
NCT02571777 (24) [back to overview]Change From Baseline in Percentage of Mornings With no Symptoms on Rising Over 52 Weeks
NCT02571777 (24) [back to overview]Pre-dose Forced Vital Capacity (FVC) at Week 4 and Week 12
NCT02571777 (24) [back to overview]Time to First Asthma Exacerbation by Exacerbation Category
NCT02571777 (24) [back to overview]Percentage of Patients Achieving the Minimal Clinically Important Difference (MCID) ACQ ≥ 0.5 at Week 26 and Week 52
NCT02571777 (24) [back to overview]Pre-dose FEV1 at Weeks 4 and 12
NCT02571777 (24) [back to overview]Asthma Quality of Life Questionnaire (AQLQ) at Week 52
NCT02571777 (24) [back to overview]Change From Baseline in Percentage of Days With no Daytime Symptoms Over 52 Weeks
NCT02571777 (24) [back to overview]Total Amount of Oral Corticosteroid Used (in Prednisone-equivalent mg Doses) to Treat Asthma Exacerbations
NCT02571777 (24) [back to overview]Percentage of Participants With at Least One Asthma Exacerbation by Exacerbation Category
NCT02571777 (24) [back to overview]Trough FEV1 at Week 52
NCT02571777 (24) [back to overview]Change From Baseline in Percentage of Nights With no Night-time Awakenings Over 52 Weeks
NCT02571777 (24) [back to overview]Percentage of Participants With Composite Endpoint of Serious Asthma Outcomes
NCT02571777 (24) [back to overview]Time in Days to Permanent Discontinuation of Study Medication Due to Asthma Exacerbation
NCT02571777 (24) [back to overview]Trough Forced Expiratory Flow (FEF) Between 25% and 75% of FVC (FEF25-75) at 52 Weeks
NCT02571777 (24) [back to overview]Trough Forced Expiratory Volume in 1 Second (Trough FEV1) of QVM149 Versus QMF149 at Week 26
NCT02571777 (24) [back to overview]Trough Forced Expiratory Volume in 1 Second (Trough FEV1) of QVM149 Versus Salmeterol/Fluticasone at Week 26
NCT02571777 (24) [back to overview]Annual Rate of Asthma Exacerbations by Exacerbation Category
NCT02571777 (24) [back to overview]Time to First Hospitalization for Asthma Exacerbation
NCT02571777 (24) [back to overview]Change From Baseline in Percentage of Asthma Symptom-free Days Over 52 Weeks
NCT02571777 (24) [back to overview]Asthma Control Questionnaire (ACQ-7) at Week 26 and Week 52
NCT02571777 (24) [back to overview]Change From Baseline in Morning and Evening Peak Expiratory Flow Rate (PEF) Over 26 and 52 Weeks of Treatment
NCT02571777 (24) [back to overview]Change From Baseline in Percentage of Days Without Rescue Medication Use Over 26 and 52 Weeks
NCT02571777 (24) [back to overview]Change From Baseline in Percentage of Rescue Medication Free Days Over 26 and 52 Weeks
NCT02571777 (24) [back to overview]Duration in Days of Asthma Exacerbations by Exacerbation Category
NCT02573233 (11) [back to overview]Change From Baseline in T-Helper Lymphocytes Count in the Bronchial Submucosa at Week 12
NCT02573233 (11) [back to overview]Change From Baseline in T-Lymphocytes Count in the Bronchial Submucosa at Week 12
NCT02573233 (11) [back to overview]Pharmacokinetics (PK) Assessment: Serum Functional Dupilumab Concentration
NCT02573233 (11) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT02573233 (11) [back to overview]Number of Participants With Antidrug Antibodies (ADA)
NCT02573233 (11) [back to overview]Average Change in Fractional Exhaled Nitric Oxide (FeNO) From Baseline to Week 6 Through Week 12
NCT02573233 (11) [back to overview]Change From Baseline in Eosinophils Cells Count in the Bronchial Submucosa at Week 12
NCT02573233 (11) [back to overview]Change From Baseline in Fractional Exhaled Nitric Oxide (FeNO) at Week 12
NCT02573233 (11) [back to overview]Change From Baseline in Mast Cells Count (Chymase Positive) in the Bronchial Submucosa at Week 12
NCT02573233 (11) [back to overview]Change From Baseline in Mast Cells Count (Tryptase Positive) in the Bronchial Submucosa at Week 12
NCT02573233 (11) [back to overview]Change From Baseline in Mucin-Stained Area in the Bronchial Submucosa at Week 12
NCT02603393 (11) [back to overview]Transition Dyspnea Index (TDI) Score
NCT02603393 (11) [back to overview]Mean Change From Baseline in St. George's Respiratory Questionnaire
NCT02603393 (11) [back to overview]Mean Change From Baseline in St. George's Respiratory Questionnaire
NCT02603393 (11) [back to overview]Mean Change From Baseline in Post-dose Trough FEV1
NCT02603393 (11) [back to overview]Mean Change From Baseline in Pre-dose Trough FEV1
NCT02603393 (11) [back to overview]Mean Change From Baseline in Forced Vital Capacity (FVC)
NCT02603393 (11) [back to overview]Change From Baseline in the Mean Daily Number of Puffs of Rescue Medication
NCT02603393 (11) [back to overview]Annualized Rate of Moderate or Severe COPD Exacerbations
NCT02603393 (11) [back to overview]Annualized Rate of COPD Exacerbations Requiring Treatment With Systemic Glucocorticosteroids and/or Antibiotics, Moderate Exacerbations Only
NCT02603393 (11) [back to overview]Annualized Rate of COPD Exacerbations Requiring Hospitalisation
NCT02603393 (11) [back to overview]Transition Dyspnea Index (TDI) Score
NCT02924688 (12) [back to overview]Mean Change From Baseline in Trough Forced Expiratory Volume in 1 Second (FEV1) at Week 24
NCT02924688 (12) [back to overview]Mean Change From Baseline in Saint George's Respiratory Questionnaire (SGRQ) Total Score at Week 24
NCT02924688 (12) [back to overview]Mean Change From Baseline in Pulse Rate at Week 24
NCT02924688 (12) [back to overview]Mean Change From Baseline in Clinic FEV1 at 3 Hours Post Study Treatment at Week 24
NCT02924688 (12) [back to overview]Mean Change From Baseline in Asthma Control Questionnaire-7 (ACQ-7) Total Score at Week 24
NCT02924688 (12) [back to overview]Annualized Rate of Moderate and Severe Asthma Exacerbations
NCT02924688 (12) [back to overview]Mean Change From Baseline in Evaluating Respiratory Symptoms (E-RS) Total Score Over Weeks 21 to 24 (Inclusive) of the Treatment Period
NCT02924688 (12) [back to overview]Number of Participants With Any Serious Adverse Event (SAE) and Common (>=3%) Non-SAE
NCT02924688 (12) [back to overview]Number of Participants With Abnormal Hematology Values
NCT02924688 (12) [back to overview]Number of Participants With Abnormal Clinical Chemistry Values
NCT02924688 (12) [back to overview]Mean Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Week 24
NCT02924688 (12) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG) Findings
NCT02980133 (8) [back to overview]For Fp MDPI Versus Placebo: Change From Baseline in Weekly Average of the Percent Predicted Trough Morning FEV1 at Week 12
NCT02980133 (8) [back to overview]Change From Baseline in the Weekly Average of Total Daily (24 Hour) Use of Albuterol/Salbutamol Inhalation Aerosol (Number of Inhalations) Over Weeks 1 Through 12
NCT02980133 (8) [back to overview]Change From Baseline in the Weekly Average of the Total Daily Asthma Symptom Score Over Weeks 1 Through 12
NCT02980133 (8) [back to overview]Change From Baseline in Asthma Control (Measured by Childhood Asthma Control Test [C-ACT] Score) Over the 12 Week Treatment Period
NCT02980133 (8) [back to overview]Change From Baseline in the Weekly Average of Daily Trough Morning (Predose and Pre-Rescue Bronchodilator) Peak Expiratory Flow (PEF) Over the 12 Week Treatment Period
NCT02980133 (8) [back to overview]Time to First Onset of Effect
NCT02980133 (8) [back to overview]Percentage of Participants Who Discontinued From Investigational Medicinal Product (IMP) for Asthma Exacerbation During the 12 Week Treatment Period
NCT02980133 (8) [back to overview]For FS MDPI Versus Fp MDPI: Change From Baseline in 1-Hour Postdose Percent Predicted Morning Forced Expiratory Volume in 1 Second (FEV1) at Week 12
NCT03034915 (11) [back to overview]Mean Change From Baseline in Evaluating Respiratory Symptoms (E-RS) Total Score
NCT03034915 (11) [back to overview]Percentage of E-RS Responders According to E-RS Total Score
NCT03034915 (11) [back to overview]Change From Baseline in Trough Forced Expiratory Volume in One Second (FEV1) at Week 24
NCT03034915 (11) [back to overview]Change From Baseline in St George's Respiratory Questionnaire (SGRQ) Total Score
NCT03034915 (11) [back to overview]Change From Baseline in COPD Assessment Test (CAT)
NCT03034915 (11) [back to overview]Number of Participants With on Treatment Adverse Events (AE) and Serious Adverse Events (SAE)
NCT03034915 (11) [back to overview]Percentage of Responders According to CAT
NCT03034915 (11) [back to overview]Percentage of Responders Based on the Saint (St) George Respiratory Questionnaire COPD Specific (SGRQ) Total Score
NCT03034915 (11) [back to overview]Percentage of TDI Responders According to SAC TDI Focal Score
NCT03034915 (11) [back to overview]Self Administered Computerized (SAC) Transient Dyspnea Index (TDI) Focal Score at Week 24
NCT03034915 (11) [back to overview]Mean Change From Baseline in E-RS Subscale Score
NCT03055988 (9) [back to overview]Change From Baseline in Aortic Distensibility After 6 Weeks of Treatment
NCT03055988 (9) [back to overview]Change From Baseline in 1.5 Hour Post Dose Forced Expiratory Volume in 1st Second (FEV1) After 6 Weeks of Treatment
NCT03055988 (9) [back to overview]Change From Baseline in Left Ventricular End Diastolic Volume Index (LVEDVI) in the 6th Week of Treatment
NCT03055988 (9) [back to overview]Change From Baseline in Functional Residual Capacity Body Plethysmography (FRCpleth) % Predicted After 6 Weeks of Treatment
NCT03055988 (9) [back to overview]Change From Baseline in Central Systolic Pressure After 6 Weeks of Treatment
NCT03055988 (9) [back to overview]Change From Baseline in Aortic Augmentation Index After 6 Weeks of Treatment
NCT03055988 (9) [back to overview]Change From Baseline in 1.5 Hour Post Dose Forced Vital Capacity (FVC) After 6 Weeks of Treatment
NCT03055988 (9) [back to overview]Change From Baseline in Pulmonary Artery Pulsatility After 6 Weeks of Treatment
NCT03055988 (9) [back to overview]Change From Baseline in Pulse Pressure After 6 Weeks of Treatment
NCT03063086 (6) [back to overview]Peak FEV1 (L) Defined as the Highest Bronchodilatory Effect on FEV1 During a Period of 5 Min to 4 h After the Last Evening Dose of Each Treatment Period
NCT03063086 (6) [back to overview]FEV1 AUC 5 Min - 1 h (Day 21) FEV1 AUC 5 Min - 4 h (Day 21) and FEV1 AUC 5 Min - 23 h 45 Min (Day 21)
NCT03063086 (6) [back to overview]FEV1 Over 24 h After 21 Days of Treatment in Relation to Evening Dose
NCT03063086 (6) [back to overview]FEV1/FVC Ratio Over 24 h After 21 Days of Treatment in Relation to Evening Dose
NCT03063086 (6) [back to overview]FVC Over 24 h After 21 Days of Treatment in Relation to Evening Dose
NCT03063086 (6) [back to overview]Trough FEV1 After 21 Days of Treatment
NCT03158311 (8) [back to overview]Percentage of Patients Achieving the Minimally Clinically Important Difference (MCID) Change From Baseline AQLQ ≥ 0.5
NCT03158311 (8) [back to overview]Change From Baseline in Forced Expiratory Flow Between 25% and 75% of Forced Vital Capacity (FEF25-75)
NCT03158311 (8) [back to overview]Change From Baseline in Asthma Control Questionnaire (ACQ-7) Total Score
NCT03158311 (8) [back to overview]Percentage of Patients Achieving the Minimally Clinically Important Difference (MCID) Decrease From Baseline ACQ-7 ≥ 0.5
NCT03158311 (8) [back to overview]Change From Baseline in Forced Vital Capacity (FVC)
NCT03158311 (8) [back to overview]Change From Baseline in Trough Forced Expiratory Volume in 1 Second (FEV1)
NCT03158311 (8) [back to overview]Change From Baseline in AQLQ Total Score
NCT03158311 (8) [back to overview]Change From Baseline in Asthma Quality of Life Questionnaire (AQLQ) Total Score
NCT03207243 (52) [back to overview]Change From Baseline in Pulse Rate (PR)
NCT03207243 (52) [back to overview]Change From Baseline Between Post-dose and Pre-dose in Pulse Rate
NCT03207243 (52) [back to overview]Change From Baseline in St George's Respiratory Questionnaire (SGRQ) Total Score
NCT03207243 (52) [back to overview]Change From Baseline Between Post-dose and Pre-dose in DBP and SBP
NCT03207243 (52) [back to overview]Change Between Pre-dose and Post-dose of QRS Axis
NCT03207243 (52) [back to overview]Change Between Pre-dose and Post-dose of PR Interval, QRS Duration, Uncorrected QT Interval, QTcF Interval and RR Interval
NCT03207243 (52) [back to overview]Change Between Pre-dose and Post-dose of Heart Rate
NCT03207243 (52) [back to overview]Time to Loss of Asthma Control
NCT03207243 (52) [back to overview]Rate Per 1000 Person-years of Participants With Hospitalization
NCT03207243 (52) [back to overview]Percentage of Participants With Loss of Asthma Control Over Weeks 0-6
NCT03207243 (52) [back to overview]Change From Baseline in Hematology Parameter: Erythrocytes Distribution Width (%)
NCT03207243 (52) [back to overview]Percentage of Participants With Loss of Asthma Control Over Weeks 0-16
NCT03207243 (52) [back to overview]Percentage of Participants With Inability to Titrate Inhaled Corticosteroids (ICS)
NCT03207243 (52) [back to overview]Percentage of Participants With Clinically Significant Asthma Exacerbation or Inability to Titrate
NCT03207243 (52) [back to overview]Percentage of Participants With Clinically Significant Asthma Exacerbation
NCT03207243 (52) [back to overview]Percentage of Participants With >=0.5 Point Asthma Control Questionnaire (ACQ-5) Score Increase From Baseline
NCT03207243 (52) [back to overview]Percentage of Participants Who Have Pre-bronchodilator FEV1 Decrease From Baseline >7.5 %
NCT03207243 (52) [back to overview]Change From Baseline in Supraventricular Couplets, Supraventricular Ectopics, Supraventricular Runs, Supraventricular Singles, Ventricular Couplets, Ventricular Ectopics, Ventricular Runs, Ventricular Singles
NCT03207243 (52) [back to overview]Serum Concentrations of GSK3772847
NCT03207243 (52) [back to overview]Percentage of Participants With <=-0.5 Point ACQ-5 Score Decrease From Baseline (Responder)
NCT03207243 (52) [back to overview]Number of Hospitalizations or Emergency Room Visits Per Participants
NCT03207243 (52) [back to overview]Change From Baseline in Pre-bronchodilator Forced Expiratory Volume in One Second (FEV1)
NCT03207243 (52) [back to overview]Change From Baseline in QRS Axis
NCT03207243 (52) [back to overview]Change From Baseline in PR Interval, QRS Duration, Uncorrected QT Interval, QT Corrected Interval-Fredericia [QTcF] Interval and RR Interval
NCT03207243 (52) [back to overview]Change From Baseline in Percent Night-time Awakenings Due to Asthma Symptoms Requiring Rescue Medication Use
NCT03207243 (52) [back to overview]Change From Baseline in Mean Morning Peak Expiratory Flow (PEF) and Mean Evening PEF
NCT03207243 (52) [back to overview]Change From Baseline in Mean Daytime Asthma Symptom Score Over Each Four Weeks of the 16 Week Treatment Period
NCT03207243 (52) [back to overview]Change From Baseline in Mean Daily Rescue Medication Use (Albuterol/Salbutamol)
NCT03207243 (52) [back to overview]Change From Baseline in Maximum, Minimum and Average Changes in Heart Rate
NCT03207243 (52) [back to overview]Change From Baseline in Hematology Parameters: Basophil, Eosinophils, Leukocytes, Lymphocytes, Neutrophils, Monocytes, and Platelets
NCT03207243 (52) [back to overview]Change From Baseline in Hematology Parameter: Mean Corpuscular Hemoglobin Concentration
NCT03207243 (52) [back to overview]Change From Baseline in Hematology Parameter: Mean Corpuscular Hemoglobin
NCT03207243 (52) [back to overview]Change From Baseline in Hematology Parameter: Hemoglobin
NCT03207243 (52) [back to overview]Change From Baseline in Hematology Parameter: Hematocrit Level
NCT03207243 (52) [back to overview]Number of Participants Reporting Serious Adverse Events (SAEs) and Non-Serious Adverse Events (Non-SAEs)
NCT03207243 (52) [back to overview]Number of Participants With Incidence and Titres of Anti- GSK3772847 Antibodies
NCT03207243 (52) [back to overview]Percent Change From Baseline in Fractional Exhaled Nitric Oxide (FeNO)
NCT03207243 (52) [back to overview]Percent Change From Baseline in Total Soluble ST2 Concentration
NCT03207243 (52) [back to overview]Percent Change From Baseline in Free Soluble Suppressor of Tumorigenicity 2 (ST2) Concentration
NCT03207243 (52) [back to overview]Number of Participants Experiencing Asthma Related Hospitalization During the Study Period
NCT03207243 (52) [back to overview]Percentage of Participants With at Least a 4 Units Improvement From Baseline of St. George's Respiratory Questionnaire (SGRQ)
NCT03207243 (52) [back to overview]Change From Baseline in Hematology Parameter: Erythrocytes
NCT03207243 (52) [back to overview]Change From Baseline in Hematology Parameter: Erythrocyte Mean Corpuscular Volume
NCT03207243 (52) [back to overview]Change From Baseline in Diastolic Blood Pressure (DBP) and Systolic Blood Pressure (SBP)
NCT03207243 (52) [back to overview]Change From Baseline in ECG Heart Rate
NCT03207243 (52) [back to overview]Change From Baseline in Clinical Chemistry Parameters: Total Protein and Albumin
NCT03207243 (52) [back to overview]Change From Baseline in Clinical Chemistry Parameters: Glucose, Potassium, Sodium, Calcium, Phosphate, Chloride, Urea and Carbon Dioxide (CO2)
NCT03207243 (52) [back to overview]Change From Baseline in Clinical Chemistry Parameters: Creatinine, Total Bilirubin and Direct Bilirubin
NCT03207243 (52) [back to overview]Change From Baseline in Clinical Chemistry Parameter: Aspartate Aminotransferase (AST), Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Gamma- Glutamyl Transferase (GGT) and Creatine Kinase (CK)
NCT03207243 (52) [back to overview]Change From Baseline in Cardiac Marker: N-Terminal ProB-type Natriuretic Peptide
NCT03207243 (52) [back to overview]Change From Baseline in Cardiac Marker: Cardiac Troponin I
NCT03207243 (52) [back to overview]Change From Baseline in Asthma Control Questionnaire (ACQ-5) Total Score
NCT03240575 (4) [back to overview]Peak 0-3 Hours Forced Expiratory Volume in One Second (FEV1) Response (Change From Baseline) [L] After 12 Weeks Treatment
NCT03240575 (4) [back to overview]Forced Expiratory Volume in One Second (FEV1) Area Under the Curve From 0 to 24 Hours (AUC0-24) Response (Change From Baseline) [L] After 12 Weeks of Treatment
NCT03240575 (4) [back to overview]Forced Expiratory Volume in One Second (FEV1) Area Under the Curve From 0 to 12 Hours (AUC0-12) Response (Change From Baseline) [L] After 12 Weeks of Treatment
NCT03240575 (4) [back to overview]Trough Forced Expiratory Volume in One Second (FEV1) Response (Change From Baseline) [L] After 12 Weeks Treatment
NCT03387852 (3) [back to overview]Percentage of Participants With Loss of Asthma Control
NCT03387852 (3) [back to overview]Change From Baseline at Week 12 in Pre-bronchodilator Forced Expiratory Volume in 1 Second (FEV1)
NCT03387852 (3) [back to overview]Change From Baseline at Week 12 in Post-bronchodilator Forced Expiratory Volume in 1 Second
NCT03756883 (4) [back to overview]Baseline-adjusted Pre-dose FEV1 Measured in the Morning Following 28 Days of Treatment.
NCT03756883 (4) [back to overview]Statistical Superiority of Test and Reference Over Placebo Treatment in Baseline-adjusted Area Under the Serial FEV1-time Curve
NCT03756883 (4) [back to overview]Statistical Superiority of Test and Reference Over Placebo Treatment in Baseline-adjusted Pre-dose FEV1 Measured in the Morning Following 28 Days of Treatment
NCT03756883 (4) [back to overview]Baseline-adjusted Area Under the Serial FEV1-time Curve Calculated From Time Zero to 12 Hours (AUC0-12h) on Day 1 of Treatment
NCT04179461 (4) [back to overview]Adherence of Asthma Controller Medication
NCT04179461 (4) [back to overview]Pulmonary Function Measured by Spirometry: Forced Expiratory Volume in 1 Second (FEV1) / Forced Vital Capacity (FVC)
NCT04179461 (4) [back to overview]Change in Composite Asthma Severity Index (CASI)
NCT04179461 (4) [back to overview]Asthma Control Test (ACT)
NCT04677959 (13) [back to overview]Number of Participants With Adverse Events (AEs)
NCT04677959 (13) [back to overview]Change From Baseline in Work Productivity and Activity Impairment (WPAI) Asthma Questionnaire Score at Week 24
NCT04677959 (13) [back to overview]Number of Participants Achieving Well-Controlled Asthma or Reaching Clinically Important Improvement in Asthma Control
NCT04677959 (13) [back to overview]Number of Decreased Doses of Inhaled Medication
NCT04677959 (13) [back to overview]Change From Baseline in the Number of SABA-free Days at Week 24 for the DS Group
NCT04677959 (13) [back to overview]Change From Baseline in Mean Weekly SABA Usage at Week 24 for the DS Group
NCT04677959 (13) [back to overview]Change From Baseline in Brief Illness Perception Questionnaire (BIPQ) Illness Comprehensibility Subscale Score at Week 24
NCT04677959 (13) [back to overview]Change From Baseline in BIPQ Emotional Representations Subscale Score at Week 24
NCT04677959 (13) [back to overview]Change From Baseline in BIPQ Cognitive Subscale Score at Week 24
NCT04677959 (13) [back to overview]Change From Baseline in Adherence to Maintenance Treatment (FS eMDPI) at Week 24 for the DS Group
NCT04677959 (13) [back to overview]Change From Baseline in BMQ Necessity Subscale Score at Week 24
NCT04677959 (13) [back to overview]Change From Baseline in Beliefs About Medicines Questionnaire (BMQ) Concern Subscale Score at Week 24
NCT04677959 (13) [back to overview]System Usability Scale (SUS) Overall Score for DS Group

Four-hour Serial Post-dose FEV1 Area Under the Curve (AUC) on Treatment Day 1

FEV1 AUC is mean AUC compared between treatment groups at Treatment Day 1. Baseline was defined as the pre-dose FEV1 measure from treatment Day 1. FEV1 AUC was calculated as the area of a trapezoid (calculated as the sum of the bases (top + bottom) divided by 2, then multiplied by width) above the baseline FEV1 area. For participants not completing a serial FEV1 measurement, the last observed post-dose FEV1 measurement was carried forward. (NCT00118716)
Timeframe: Immediately prior to dosing (0 time point), 30 minutes post-dose and 1, 2, 3, 4 hour post-dose on Day 1

InterventionLiters*hour (Mean)
FSC 100/50mcg BID0.70
FP 100mcg BID0.30

[back to top]

Percent of Rescue-free Days

A rescue-free day was defined as a day when no supplemental albuterol was taken (i.e., 0 puffs recorded for both AM and PM assessments of albuterol use in the daily diary). Percent of rescue-free days was calculated as the number of rescue-free days, divided by the total number of days in the treatment period, multiplied by 100 for each participant. (NCT00118716)
Timeframe: Up to Week 4

InterventionPercentage of days (Mean)
FSC 100/50mcg BID59.4
FP 100mcg BID54.7

[back to top]

Maximal Percent Change in Forced Expiratory Volume in 1 Second (FEV1) Following Exercise Challenge at Week 4

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. Maximal percent change in FEV1 following exercise challenge was defined as the percent change from pre-exercise baseline FEV1 to the minimum FEV1 collected within one hour following exercise challenge. Maximal percent change in FEV1 following exercise challenge was mean maximal percent change from pre-exercise baseline compared between treatment groups at Treatment Week 4. FEV1 was measured 5, 10, 15, 30, and 60 minutes post-exercise. The minimum FEV1 measured across these time points, regardless of any missing time points, will be used for the calculation of maximal percent change. (NCT00118716)
Timeframe: Baseline and Week 4

InterventionPercent change (Mean)
FSC 100/50mcg BID-9.5
FP 100mcg BID-12.7

[back to top]

Change From Baseline in Evening (PM) PEF

PEF is defined as the maximum airflow during a forced expiration beginning with the lungs fully inflated. PEF was measured by the participants using a hand-held electronic peak flow meter each evening prior to the dose of study medication after the symptom measurement and any rescue albuterol/salbutamol inhalation aerosol use. Each participant was instructed to perform triplicate PEF measurements in the evening. Change from baseline was calculated as the endpoint value minus the baseline value. Baseline was defined as the average of the values from the 7 days preceding Visit 2 (7-14 [+ or -4] days after Visit1) since these measures were derived from data collected in the evening. (NCT00118716)
Timeframe: Baseline and up to Week 4

InterventionL/min (Mean)
FSC 100/50mcg BID10.8
FP 100mcg BID7.6

[back to top]

Change From Baseline in Morning Peak Expiratory Flow (AM PEF)

PEF is defined as the maximum airflow during a forced expiration beginning with the lungs fully inflated. PEF was measured by the participants using a hand-held electronic peak flow meter each morning prior to the dose of study medication and any rescue albuterol/salbutamol inhalation aerosol use. Each participant was instructed to perform triplicate PEF measurements in the morning. Change from baseline was calculated as the endpoint value minus the baseline value. For AM PEF, baseline was defined as the average of the AM PEF values recorded on the day of Visit 2 (7-14 [+ or -4] days after Visit1) plus the 6 preceding days since AM PEF was measured in the morning. (NCT00118716)
Timeframe: Baseline and Up to Week 4

InterventionLiters/minute (L/min) (Mean)
FSC 100/50mcg BID16.3
FP 100mcg BID9.1

[back to top]

Change From Baseline in Pediatric Asthma Quality of Life Questionnaire (PAQLQ)

PAQLQ measures functional problems that are most troublesome to children with asthma. PAQLQ has 23 questions in 3 domains (activity limitation=5, emotional function=8, symptoms=10). Participants responded to each question on a 7-point scale (7= not bothered at all and 1= extremely bothered). The overall PAQLQ score is the mean of all 23 responses (minimum score 1= 5+8+10/23 and maximum score 7= 35+56+70/23) and the individual domain scores are the means of the items in those domains (minimum: 5/5, 8/8, 10/10 and maximum: 35/5, 56/8, 70/10). Minimum possible value is 1 (maximum impairment); maximum possible value is 7 (no impairment). Endpoint was defined from the last questionnaire collected during the double-blind treatment period or discontinuation visit (up to Week 4). (NCT00118716)
Timeframe: Baseline (Week 0) and up to Week 4

,
InterventionScores on a scale (Mean)
Activity limitation week 2Activity limitation week 4Activity limitation endpointEmotional function Week 2Emotional function Week 4Emotional function endpointSymptoms Week 2Symptoms Week 4Symptoms EndpointOverall score Week 2Overall score Week 4Overall score Endpoint
FP 100mcg BID0.630.750.670.480.470.420.490.550.510.520.570.51
FSC 100/50mcg BID0.780.930.890.440.560.530.390.520.480.490.620.59

[back to top]

Percent of Symptom-free Days

A symptom-free day was defined as a day with no symptoms (i.e., a score of 0, indicating no asthma symptoms during the day or previous night, recorded in the daily diary). Percent of symptom-free days was calculated as the number of symptom-free days, divided by the total number of days in the treatment period, multiplied by 100 for each participant. (NCT00118716)
Timeframe: Up to Week 4

InterventionPercentage of days (Mean)
FSC 100/50mcg BID27.3
FP 100mcg BID28.6

[back to top]

Maximum Post-exercise Percent (%) Fall in FEV1

The effect of four weeks of treatment with oral montelukast plus inhaled fluticasone, and inhaled salmeterol plus inhaled fluticasone on EIB as measured by the maximum post-exercise percent fall (relative to pre-exercise baseline) in FEV1. (NCT00127166)
Timeframe: 4 weeks (Weeks 0 to 4 or Weeks 6 to 10)

InterventionPercent change from baseline (Least Squares Mean)
Montelukast10.57
Salmeterol13.82

[back to top]

Maximum FEV1 % Predicted Following First Beta-agonist Use

The effect of a four-week treatment course of oral montelukast plus inhaled fluticasone, compared to inhaled salmeterol plus inhaled fluticasone, on short-acting β-agonist bronchodilation as measured by the maximum FEV1 percent predicted following first β-agonist use. (NCT00127166)
Timeframe: 4 weeks (Weeks 0 to 4 or Weeks 6 to 10)

InterventionPercent of predicted value (Least Squares Mean)
Montelukast104.03
Salmeterol99.92

[back to top]

Average (Avg) %-Change in FEV1 After First Beta (β)-Agonist Use and Prior to Second β-agonist Use

The effect of a four-week treatment course of oral montelukast plus inhaled fluticasone, compared to inhaled salmeterol plus inhaled fluticasone, on the extent and severity of EIB as measured by the average percent change in FEV1 after first β-agonist intake and prior to second β-agonist use. (NCT00127166)
Timeframe: 4 weeks (Weeks 0 to 4 or Weeks 6 to 10)

InterventionPercent change from baseline (Least Squares Mean)
Montelukast6.51
Salmeterol2.72

[back to top]

Area Under the Curve for %-Change From Pre-exercise Baseline FEV1 in Liters (L), From 0 to 20 Minutes (AUC(0-20))

The effect of a four-week treatment course of oral montelukast plus inhaled fluticasone, compared to inhaled salmeterol plus inhaled fluticasone, on the extent and severity of EIB as measured by the area under the curve from 0 to 20 minutes (AUC0-20) for FEV1 percent change from pre-exercise baseline. (NCT00127166)
Timeframe: 4 weeks (Weeks 0 to 4 or Weeks 6 to 10)

InterventionPercent times Minutes (Least Squares Mean)
Montelukast116.04
Salmeterol168.75

[back to top]

Time to Recovery to Within 5% of Baseline FEV1

The effect of a four-week treatment course of oral montelukast plus inhaled fluticasone, compared to inhaled salmeterol plus inhaled fluticasone, on the extent and severity of EIB as measured by the time to recovery (to within 5 percent of the pre-exercise baseline FEV1) following a standardized exercise challenge. (NCT00127166)
Timeframe: 4 weeks (Weeks 0 to 4 or Weeks 6 to 10)

Interventionminutes (Median)
Montelukast5.9
Salmeterol11.1

[back to top]

Treatment Failure

The primary outcome measure was treatment failure, defined as the occurrence of any one of the following events: hospitalization or an urgent medical visit for asthma initiated by the patient or physician; use of systemic corticosteroids for asthma or need for open-label use of inhaled corticosteroids for asthma, as determined by the study physician or an asthma care provider; a decrease in prebronchodilator forced expiratory volume in 1 second (FEV1) to more than 20% below the baseline value measured at randomization; a decrease in the morning peak expiratory flow rate to more than 35% below the baseline value (the mean over the final 2 weeks of the run-in period) on 2 consecutive days; use of 10 puffs or more per day of rescue beta-agonist for 2 consecutive days (except as medication before exercise); refusal of the patient to continue because of lack of satisfaction with treatment; or judgment by a physician that the patient should stop treatment for reasons of safety. (NCT00156819)
Timeframe: 16 weeks

Interventionparticipants (Number)
Fluticasone34
Montelukast50
Fluticasone Plus Salmeterol33

[back to top]

Percent Change From Baseline in RINT Measurements at Week 26

Change from Baseline was calculated as the Week 26 value minus the Baseline value. Interrupter respiratory resistance (RINT) measurements were calculated by a combined analysis for relation between change from baseline and occurrence of the endpoint. RINT is a technique that is used for evaluating lung function in poorly collaborating patients (e.g., small children). The measurement is performed during tidal breathing (normal breathing) instead of during maximal expiration, as is done by a spirometry test. (NCT00197106)
Timeframe: Baseline and Week 26

Interventionpercent (Number)
Salmeterol/FP 50/100 mcg Plus Placebo-9.1
FP 200 mcg-9.9

[back to top]

Number of Asthma Exacerbations Per Treatment Group at Week 26

An exacerbation is defined as a worsening of the asthma complaints (commonly referred to as an asthma attack) and is reported by the participant experiencing the event. An exacerbation was verified by the use of asthma rescue medication. (NCT00197106)
Timeframe: Week 26

Interventionnumber of exacerbations (Number)
Salmeterol/FP 50/100 mcg Plus Placebo10
FP 200 mcg7

[back to top]

Mean Change From Baseline in Provocation Dose (PD20) Causing a 20% Fall in FEV1 at Week 26

PD20 was calculated by using increasing dosages of methacholine. The dosage that caused a 20% fall in FEV1 was used for analysis. The presented data are ratios (month 6/Baseline) of geometric mean PD20 values. (NCT00197106)
Timeframe: Baseline and Week 26

Interventionratio (Log Mean)
Salmeterol/FP 50/100 mcg Plus Placebo2.7
FP 200 mcg1.5

[back to top]

Mean Change From Baseline in Percentage Predicted Forced Expiratory Volume in One Second (FEV1) at Week 26

Change from Baseline was calculated as the Week 26 value minus the Baseline value. The percentage predicted FEV1 is defined as the volume of air that can be forced out in one second after taking a deep breath and is corrected for the FEV1 value corresponding with the same age. (NCT00197106)
Timeframe: Baseline and Week 26

Interventionpercent predicted change (Mean)
Salmeterol/FP 50/100 mcg Plus Placebo102.5
FP 200 mcg103.0

[back to top]

Mean Change From Baseline in Midexpiratory Flow (MEF 50) at Week 26

Change from Baseline was calculated as the Week 26 value minus the Baseline value. MEF 50 is defined as maximum expiratory flow rate at 50% of vital capacity. Vital capacity is the maximum amount of air that a person can expel from the lungs after first filling the lungs to their maximum extent. Midexpiratory flow was calculated by use of spirometry. The test is normally repeated at least three times in order to ensure reproducibility. (NCT00197106)
Timeframe: Baseline and Week 26

Interventionliters/second (Mean)
Salmeterol/FP 50/100 mcg Plus Placebo2.28
FP 200 mcg2.19

[back to top]

Mean Change From Baseline in Forced Vital Capacity (FVC) at Week 26

Change from Baseline was calculated as the Week 26 value minus the Baseline value. Forced vital capacity is defined as the maximum volume of air that can be forcibly expired from the lungs and is calculated by use of spirometry. The spirometry test is performed by using a device called a spirometer, which measures the amount of air one can blow out maximally. Generally, the participant is asked to take the deepest breath they can, and then exhale into the sensor as hard as possible, for as long as possible. The test is normally repeated three times to ensure reproducibility. (NCT00197106)
Timeframe: Baseline and Week 26

Interventionliters (Mean)
Salmeterol/FP 50/100 mcg Plus Placebo2.28
FP 200 mcg2.28

[back to top]

Geometric Means of Nitric Oxide (NO) at Week 26

Geometric mean values of NO at week 26 were compared using ANCOVA with adjustment for baseline value of NO, age, gender and center. Analysis of covariance (ANCOVA) is a general linear model with one continuous outcome variable (quantitative) and one or more factor variables. (NCT00197106)
Timeframe: Baseline and Week 26

Interventionparts per billion (Geometric Mean)
Salmeterol/FP 50/100 mcg Plus Placebo8.6
FP 200 mcg10.0

[back to top]

Percentage of Symptom-free Days During the Last 10 Weeks of the Treatment Period

Asthma symptom-free days are defined as days (24 hour period) with no symptoms, as recorded in the participant's diary. (NCT00197106)
Timeframe: Last 10 weeks of the treatment period (Weeks 16-26)

Interventionpercentage of days (Mean)
Salmeterol/FP 50/100 mcg Plus Placebo50.45
FP 200 mcg49.75

[back to top]

Percentage of Symptom-free Days During the Entire Treatment Period

Asthma symptom-free days are defined as days (24 hour period) with no symptoms, as recorded in the participant's diary (NCT00197106)
Timeframe: Baseline to Week 26

,
Interventionpercentage of days (Mean)
Baseline0-6 weeks6-16 weeks16-26 weeks
FP 200 mcg23.0631.5045.2449.75
Salmeterol/FP 50/100 mcg Plus Placebo22.7831.5844.6050.45

[back to top]

Methacholine Provocative Concentration 20 (PC20)

Change between placebo salmeterol and active salmeterol for methacholine PC20 (NCT00200967)
Timeframe: Clinic visits at weeks 0 and 18 of each treatment period

Interventionmilligrams per milliliter (Geometric Mean)
B16 Arg/Arg0.06
B16 Gly/Gly-1.27

[back to top]

Exhaled Breath Condensate (EBC)

Change between placebo salmeterol and active salmeterol for EBC (NCT00200967)
Timeframe: Clinic visits at weeks 0, 10, and 18 of each treatment period

InterventionpH (Least Squares Mean)
B16 Arg/Arg-0.10
B16 Gly/Gly-0.03

[back to top]

Rescue Medication (Ipratropium and Albuterol) Use

Change between placebo salmeterol and active salmeterol for rescue medication use (NCT00200967)
Timeframe: Recorded daily on a diary card, and then averaged between weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionpuffs per day (Mean)
B16 Arg/Arg0.2
B16 Gly/Gly0.0

[back to top]

Spirometry Forced Vital Capacity (FVC), Pre-bronchodilator

Change between placebo salmeterol and active salmeterol for Spirometry FVC, pre-bronchodilator (NCT00200967)
Timeframe: Clinic visits at weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionliters (Least Squares Mean)
B16 Arg/Arg-0.04
B16 Gly/Gly-0.03

[back to top]

Asthma Control Questionnaire (ACQ)

Change between placebo salmeterol and active salmeterol for ACQ, where ACQ ranges from 0 (best asthma control) to 6 (worst asthma control). (NCT00200967)
Timeframe: Clinic visits at weeks 0 and 18 of each treatment period

Interventionunits on a scale (Least Squares Mean)
B16 Arg/Arg0.13
B16 Gly/Gly0.11

[back to top]

Asthma Symptoms

Change between placebo salmeterol and active salmeterol for asthma symptoms (0=absent, 1=mild, 2=moderate, 3=severe). (NCT00200967)
Timeframe: Recorded daily on a diary card, and then averaged between weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionunits on a scale (Mean)
B16 Arg/Arg0.04
B16 Gly/Gly0.00

[back to top]

Evening (PM) Peak Expiratory Flow (PEF) Rate

Change between placebo salmeterol and active salmeterol for PM PEF rate (NCT00200967)
Timeframe: Measured daily using a hand-held peak flow meter, and then averaged between weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionliters per minute (Least Squares Mean)
B16 Arg/Arg-25
B16 Gly/Gly-24

[back to top]

Spirometry Peak Expiratory Flow (PEF) Rate, Pre-bronchodilator

Change between placebo salmeterol and active salmeterol for Spirometry PEF rate, pre-bronchodilator (NCT00200967)
Timeframe: Clinic visits at weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionliters per minute (Least Squares Mean)
B16 Arg/Arg-17
B16 Gly/Gly-17

[back to top]

Exhaled Nitric Oxide (eNO)

Change between placebo salmeterol and active salmeterol for eNO (NCT00200967)
Timeframe: Clinic visits at weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionparts per billion (Geometric Mean)
B16 Arg/Arg0.12
B16 Gly/Gly-0.02

[back to top]

Morning (AM) Peak Expiratory Flow (PEF) Rate

Change between placebo salmeterol and active salmeterol for AM PEF rate (NCT00200967)
Timeframe: Measured daily using a hand-held peak flow meter, and then averaged between weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionliters per minute (Least Squares Mean)
B16 Arg/Arg-21
B16 Gly/Gly-22

[back to top]

Peak Expiratory Flow (PEF) Variability

Change between placebo salmeterol and active salmeterol for PEF variability, where PEF variability is defined as 100% x (PM PEF - AM PEF)/(PM PEF) (NCT00200967)
Timeframe: Measured daily using a hand-held peak flow meter, and then averaged between weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionpercentage (Least Squares Mean)
B16 Arg/Arg0.2
B16 Gly/Gly0.7

[back to top]

Spirometry Forced Expiratory Volume in One Second (FEV1), Pre-bronchodilator

Change between placebo salmeterol and active salmeterol for Spirometry FEV1, pre-bronchodilator (NCT00200967)
Timeframe: Clinic visits at weeks 0, 2, 6, 10, 14, and 18 of each treatment period

Interventionliters (Least Squares Mean)
B16 Arg/Arg-0.08
B16 Gly/Gly-0.04

[back to top]

Sputum Eosinophils (EOS) 24 Hours Post Antigen Challenge

Sputum samples were collected from the participants. Cell counts were made from these samples after treatment with 0.1% dithiothreitol. Percentage of eosinophils were reported. Time frame measurement was 24 hours after the subject had an antigen challenge. (NCT00214019)
Timeframe: Eosinophils are measured 24 hours after the subject has an antigen challenge

InterventionEosinophil percentage (Mean)
Placebo/Placebo3.5
Placebo/Salmeterol2.4
Placebo/fFuticasone0.54
Salmeterol/Fluticasone2.4

[back to top]

Area Under the Curve for FEV1 Percent Change From Preexercise Baseline During the 60 Minutes Following Exercise Challenge (AUC 0-60 Min) at 24 Hours Postdose

The measure included only the area below the pre-exercise baseline (NCT00245570)
Timeframe: 0-60 minutes after the exercise challenge at 24 hours postdose

InterventionPercent * minutes (Mean)
Montelukast 10 mg231.09
Salmeterol 50-μg554.93
Placebo395.96

[back to top]

Time to Recovery From Maximum Percentage Decrease in FEV1 After Exercise Challenge at 8.5 Hours Postdose

"The time to recovery from maximum percent fall is the~duration between the time at which the maximum percent fall in FEV1 after exercise challenge occurs and the~time when FEV1 returns to within 5% of the preexercise baseline for the first time." (NCT00245570)
Timeframe: Exercise challenge at 8.5 hours postdose

InterventionMinutes (Mean)
Montelukast 10 mg10.70
Salmeterol 50-μg13.82
Placebo32.34

[back to top]

Area Under the Curve for FEV1 Percent Change From Preexercise Baseline During the 60 Minutes Following Exercise Challenge (AUC 0-60 Min) at 8.5 Hours Postdose

The measure included only the area below the pre-exercise baseline (NCT00245570)
Timeframe: 0-60 minutes after the exercise challenge at 8.5 hours postdose

InterventionPercent * minutes (Mean)
Montelukast 10 mg191.01
Salmeterol 50-μg276.26
Placebo511.28

[back to top]

Maximum Percent Fall in FEV1 After Exercise Challenge at 24 Hours Post-dose in Patients With EIB

In patients with EIB, the percent change from pre-exercise baseline FEV, to the lowest FEV1 within 60 minutes after exercise challenge (24 hours post-dose). The FEV1 measurement obtained 5 minutes before the exercise challenge was the baseline, and was specific to each exercise challenge. (NCT00245570)
Timeframe: 0-60 minutes after the exercise challenge performed 24 hours after a single oral dose

InterventionPercent Change from Baseline (Mean)
Montelukast 10 mg10.09
Salmeterol 50-μg16.22
Placebo13.64

[back to top]

Area Under the Curve for FEV1 Percent Change From Preexercise Baseline During the 60 Minutes Following Exercise Challenge (AUC 0-60 Min) at 2 Hours Postdose

"The measure included only the area below the pre-exercise~baseline" (NCT00245570)
Timeframe: 0-60 minutes after the exercise challenge at 2 hours postdose

InterventionPercent * minutes (Mean)
Montelukast 10 mg254.60
Salmeterol 50-μg293.05
Placebo710.43

[back to top]

Number of Patients Requiring β-Agonist Rescue Medication After Exercise Challenge at 8.5 Hours Postdose

(NCT00245570)
Timeframe: 0-90 minutes after the exercise challenge performed at 8.5 hours postdose

,,
InterventionParticipants (Number)
Patients Requiring Rescue MedicationPatients Not Requiring Rescue Medication
Montelukast 10 mg040
Placebo433
Salmeterol 50-μg039

[back to top]

Number of Patients Requiring β-Agonist Rescue Medication After Exercise Challenge at 24 Hours Postdose

(NCT00245570)
Timeframe: 0-90 minutes after the exercise challenge performed at 24 hours postdose

,,
InterventionParticipants (Number)
Patients Requiring Rescue MedicationPatients Not Requiring Rescue Medication
Montelukast 10 mg343
Placebo640
Salmeterol 50-μg640

[back to top]

Number of Patients Requiring β-Agonist Rescue Medication After Exercise Challenge at 2 Hours Postdose

(NCT00245570)
Timeframe: 0-90 minutes after the exercise challenge performed at 2 hours postdose

,,
InterventionParticipants (Number)
Patients Requiring Rescue MedicationPatients Not Requiring Rescue Medication
Montelukast 10 mg344
Placebo938
Salmeterol 50-μg442

[back to top]

Time to Recovery From Maximum Percentage Decrease in FEV1 After Exercise Challenge at 24 Hours Postdose

"The time to recovery from maximum percent fall is the~duration between the time at which the maximum percent fall in FEV1 after exercise challenge occurs and the~time when FEV1 returns to within 5% of the preexercise baseline for the first time." (NCT00245570)
Timeframe: Exercise challenge at 24 hours postdose

InterventionMinutes (Mean)
Montelukast 10 mg11.04
Salmeterol 50-μg29.75
Placebo23.31

[back to top]

Time to Recovery From Maximum Percentage Decrease in FEV1 After Exercise Challenge at 2 Hours Postdose

The time to recovery from maximum percent fall is the duration between the time at which the maximum percent fall in FEV1 after exercise challenge occurs and the time when FEV1 returns to within 5% of the preexercise baseline for the first time. (NCT00245570)
Timeframe: Exercise challenge at 2 hours postdose

InterventionMinutes (Mean)
Montelukast 10 mg16.63
Salmeterol 50-μg17.58
Placebo42.70

[back to top]

Maximum Percent Fall in Forced Expiratory Volume in 1 Second (FEV1) After Exercise Challenge at 2 Hours Post-dose in Patients With Exercise-Induced Bronchoconstriction (EIB)

In patients with EIB, the percent change from pre-exercise baseline FEV1 to the lowest FEV1 within 60 minutes after exercise challenge (2 hours post-dose). The FEV1 measurement obtained 5 minutes before the exercise challenge was the baseline, and was specific to each exercise challenge. (NCT00245570)
Timeframe: 0-60 minutes after the exercise challenge performed 2 hours after a single oral dose

InterventionPercent Change from Baseline (Mean)
Montelukast 10 mg13.15
Salmeterol 50-μg10.46
Placebo21.86

[back to top]

Maximum Percent Fall in FEV1 After Exercise Challenge at 8.5 Hours Post-dose in Patients With EIB

In patients with EIB, the percent change from pre-exercise baseline FEV, to the lowest FEV1 within 60 minutes after exercise challenge (8.5 hours post-dose). The FEV1 measurement obtained 5 minutes before the exercise challenge was the baseline, and was specific to each exercise challenge. (NCT00245570)
Timeframe: 0-60 minutes after the exercise challenge performed 8.5 hours after a single oral dose

InterventionPercent Change from Baseline (Mean)
Montelukast 10 mg11.60
Salmeterol 50-μg11.01
Placebo16.65

[back to top]

Mean Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

Systolic and diastolic BP was measured in sitting position. Baseline value was the measurement taken at the start of run-in or the treatment period. Change from Baseline was any post Baseline value minus value at Baseline. (NCT00269087)
Timeframe: Baseline and up to Week 56

InterventionMillimeter of mercury (mmHg) (Mean)
SBP, Week 4SBP, Week 8SBP, Week 12SBP, Week 16SBP, Week 20SBP, Week 24SBP, Week 28SBP, Week 32SBP, Week 36SBP, Week 40SBP, Week 44SBP, Week 48SBP, Week 52 / withdrawalDBP, Week 4DBP, Week 8DBP, Week 12DBP, Week 16DBP, Week 20DBP, Week 24DBP, Week 28DBP, Week 32DBP, Week 36DBP, Week 40DBP, Week 44DBP, Week 48DBP, Week 52 / withdrawal
GW815SF 50/500 µg0.5-0.10.60.7-0.80.2-0.4-1.81.10.4-3.1-4.10.3-0.7-1.20.30.3-1.40.6-0.6-1.40.0-1.3-2.1-2.9-0.1

[back to top]

Mean Change From Baseline in Peak Expiratory Flow (PEF)

PEF was the maximum speed of expiration measured using spirometer. A participant took rest just before the measurement. At each time of measurement, a participant expired for at least 6 seconds wherever possible. At each time of measurement, at least 3 readings were obtained, and three readings which were obtained in an appropriate manner were stored. Baseline value was the value measured at visit 2. However, when the value at Visit 2 was missing, the value at Visit 1 was used as Baseline. Change from Baseline was any post Baseline value minus Baseline value. (NCT00269087)
Timeframe: Baseline and up to Week 52

InterventionLiters per second (Mean)
Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48Week 52Week 52/ withdrawal
GW815SF 50/500 µg0.3150.4460.3940.3570.3090.3280.3340.2690.3500.2770.3070.3140.2960.229

[back to top]

Mean Change From Baseline in Maximal Expiratory Flow Rate at 25% (V25) and 50% (V50) of Vital Capacity

V25 and V 50 were measured using spirometer. A participant took rest just before the measurement. At each time of measurement, a participant expired for at least 6 seconds wherever possible. At each time of measurement, at least 3 readings were obtained, and three readings which were obtained in an appropriate manner were stored. Baseline value was the value measured at visit 2. However, when the value at Visit 2 was missing, the value at Visit 1 was used as baseline. Change from Baseline was any post Baseline value minus Baseline value. (NCT00269087)
Timeframe: Baseline and up to Week 52

InterventionLiter per second (Mean)
V25, BaselineV25, Week 8V25, Week 12V25, Week 16V25, Week 20V25, Week 24V25, Week 28V25, Week 32V25, Week 36V25, Week 40V25, Week 44V25, Week 48V25, Week 52V25, Week 52/ withdrawalV50, Week 4V50, Week 8V50, Week 12V50, Week 16V50, Week 20V50, Week 24V50, Week 28V50, Week 32V50, Week 36V50, Week 40V50, Week 44V50, Week 48V50, Week 52V50, Week 52/ withdrawal
GW815SF 50/500 µg0.0180.0210.0150.0160.0120.0170.0120.0090.0180.0220.0150.0100.0170.0120.0440.0760.0540.0600.0400.0470.0490.0530.0460.0530.0460.0380.0590.045

[back to top]

Mean Change From Baseline in Level of Plasma Cortisol 1

On each assessment day at Week 24 and 52, adrenal cortical function tests were performed between 8:00-10:00 in the morning. Additional measurements were taken at follow up visit, if the measurements made at Week 52 revealed any abnormalities of clinical significance. Blood samples were taken from participants at rest before undergoing spirometry. Baseline value was the measurement taken at the start of run-in or the treatment period. Change from Baseline was any post Baseline value minus value at Baseline. (NCT00269087)
Timeframe: Baseline and Week 24 and 52

InterventionMicrograms per decilitre (µg/dL) (Mean)
Week 24Week 52/Withdrawal
GW815SF 50/500 µg0.86-0.62

[back to top]

Mean Change From Baseline in Forced Vital Capacity (FVC)

FVC was the amount of air which can be forcibly exhaled from the lungs after taking the deepest breath possible measured using spirometer. A participant took rest just before the measurement. At each time of measurement, a participant expired for at least 6 seconds wherever possible. At each time of measurement, at least 3 readings were obtained, and three readings which were obtained in an appropriate manner were stored. Baseline value was the value measured at visit 2. However, when the value at Visit 2 was missing, the value at Visit 1 was used as Baseline. Change from Baseline was any post Baseline value minus Baseline value. (NCT00269087)
Timeframe: Baseline and up to Week 52

InterventionLiters (Mean)
Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48Week 52Week 52/ withdrawal
GW815SF 50/500 µg0.1280.1560.1420.1400.1060.1270.1490.1420.1470.1480.1560.1470.1700.096

[back to top]

Change From Baseline in Symptom Score With Respect to Breathlessness, Cough, Sputum and Nighttime Awakenings

A participant recorded scores on the scale of 0 to 4 for breathlessness and nighttime awakenings, where 0 indicated no symptoms and 4 indicated severe symptoms; on the scale of 0 to 3 for cough and sputum production, where 0 indicated no symptoms and 3 indicated severe symptoms, in the 24 hours prior to each entry in the COPD diary. Baseline was mean value of the consecutive 7 days just before Visit2. Change from Baseline was any post Baseline value minus Baseline value. (NCT00269087)
Timeframe: Baseline and up to Week 52

InterventionScores on a scale (Mean)
Breathlessness, treatment periodCough, treatment periodSputum, treatment periodNighttime awakenings, treatment period
GW815SF 50/500 µg-0.20.00.0-0.1

[back to top]

Median Tmax of Salmeterol

For analysis of PK parameters for salmeterol, blood samples were taken just before dosing (within one hour prior to dosing), 5, 15, 30, 45 minutes, 1, 2, 3 and 4 hours after dosing to determine plasma drug concentrations. The investigational product was taken in fasting condition just before each blood sampling. Parameters were calculated by a model-independent method with the plasma concentration-time profile data in individual participants. (NCT00269087)
Timeframe: Within one hour prior to dosing, 5, 15, 30, 45 minutes, 1, 2, 3 and 4 hours

Interventionhour (Median)
GW815SF 50/500 µg0.250

[back to top]

Median Time of Observed Maximum Plasma Concentration (Tmax) of FP

For analysis of PK parameters for FP, blood samples were taken just before dosing (within one hour prior to dosing), 30, 45 minutes, 1, 2, 3, 4, 6, 8 and 12 hours after dosing to determine plasma drug concentrations. The investigational product was taken in fasting condition just before each blood sampling. Parameters were calculated by a model-independent method with the plasma concentration-time profile data in individual participants. (NCT00269087)
Timeframe: Within one hour prior to dosing, 30, 45 minutes, 1, 2, 3, 4, 6, 8 and 12 hours

Interventionhours (Median)
GW815SF 50/500 µg0.875

[back to top]

Mean Observed Maximum Plasma Concentration (Cmax) of Fluticasone Propionate (FP)

For analysis of pharmacokinetic (PK) parameters for FP, blood samples were taken just before dosing (within one hour prior to dosing), 30, 45 minutes, 1, 2, 3, 4, 6, 8 and 12 hours after dosing to determine plasma drug concentrations. The investigational product was taken in fasting condition just before each blood sampling. Parameters were calculated by a model-independent method with the plasma concentration-time profile data in individual participants. (NCT00269087)
Timeframe: Within one hour prior to dosing, 30, 45 minutes, 1, 2, 3, 4, 6, 8 and 12 hours

InterventionPicograms per milliliter (pg/mL) (Mean)
GW815SF 50/500 µg124.63

[back to top]

Mean Frequency of Moderate and Severe Chronic Obstructive Pulmonary Disease (COPD) Exacerbations

An exacerbation was defined as worsening of the participant's symptoms of cough, sputum production and breathlessness requiring a change in medication. When a moderate or severe COPD exacerbation was observed, details (date of onset, outcome, date of resolution/death, severity, medications provided for treatment, whether the COPD exacerbation required hospitalization, whether the COPD exacerbation required participant withdrawal from the study) were recorded. (NCT00269087)
Timeframe: Up to Week 56

InterventionNumber of exacerbations (Mean)
GW815SF 50/500 µg0.456

[back to top]

Number of Participants With Any Adverse Events (AEs) and Serious AEs (SAEs)

AE is any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE include adverse events that result in any of the following outcomes: death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, a persistent or significant incapacity or substantial disruption of the ability to conduct normal functions, or a congenital anomaly/birth defect. Important medical events that may not result in death, be life-threatening, or require hospitalization may be considered serious when, based upon appropriate medical judgment, they may jeopardize the participant and may require medical or surgical intervention to prevent one of the outcomes listed in this definition. (NCT00269087)
Timeframe: Up to Week 56

InterventionParticipants (Count of Participants)
Any AEsAny SAEs
GW815SF 50/500 µg12027

[back to top]

Number of Participants With Abnormal Oropharyngeal Examination Findings

Oropharyngeal examination was performed in participants with suspected oral infection (candidiasis). (NCT00269087)
Timeframe: Up to Week 56

InterventionParticipants (Count of Participants)
Week -2Week 0Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48Week52 / withdrawal
GW815SF 50/500 µg113779996777448

[back to top]

Number of Participants With Abnormal (Shift From Baseline) Urinalysis Parameters

Urinalysis parameters: Urine protein, Glucose and Urobilinogen were presented as shift from Baseline. Only number of participants with urinalysis values more than Baseline values were presented. The plus sign increases with a higher level of glucose and proteins in the urine: 1+: slightly positive, 2+: positive, 3+: high positive and 4+: strongly positive. (NCT00269087)
Timeframe: Up to Week 56

InterventionParticipants (Count of Participants)
Urine protein, Week 4, 1+ to 3+Glucose, Week 4, 3+ to 4+Urine protein, Week 12, 1+ to 2+Urine protein, Week 12, 1+ to 3+Glucose, Week 12, 2+ to 4+Glucose, Week 12, 3+ to 4+Urine protein, Week 24, 1+ to 2+Urine protein, Week 24, 1+ to 3+Glucose, Week 24, 1+ to 2+Glucose, Week 24, 1+ to 4+Glucose, Week 24, 2+ to 4+Urine protein, Week 36, 1+ to 2+Urine protein, Week 36, 1+ to 3+Glucose, Week 36, 1+ to 4+Glucose, Week 36, 2+ to 4+Glucose, Week 36, 3+ to 4+Urine protein, Week 52/withdrawal, 1+ to 3+Glucose, Week 52/withdrawal, 1+ to 2+Glucose, Week 52/withdrawal, 1+ to 4+Glucose, Week 52/withdrawal, 2+ to 4+
GW815SF 50/500 µg11111111121111211211

[back to top]

Number of Participants With Abnormal (Outliers From the Normal Range) Hematology Parameters

Hematology parameters: Red blood cells (RBC), Hemoglobin (Hb), Hematocrit, Platelet count (PC), White blood cells (WBC), Basophils, Eosinophils, Neutrophils, Lymphocytes and Monocytes were presented as the outliers from the normal range as > upper limit and < lower limit. Only number of participants with hematology values outside normal range were presented. (NCT00269087)
Timeframe: Up to Week 56

InterventionParticipants (Count of Participants)
RBC, Baseline, < lower limitRBC, Week 4, < lower limitRBC, Week 12, < lower limitRBC, Week 24, > upper limitRBC, Week 24, < lower limitRBC, Week 36, > upper limitRBC, Week 36, < lower limitRBC, Week 52/Withdrawal, > upper limitRBC, Week 52/Withdrawal, < lower limitHb, Baseline, > upper limitHb, Baseline, < lower limitHb, Week 4, < lower limitHb, Week 12, < lower limitHb, Week 24, < lower limitHb, Week 36, < lower limitHb, Week 52/Withdrawal, Hematocrit, Baseline, > upper limitHematocrit, Baseline, < lower limitHematocrit, Week 4, > upper limitHematocrit, Week 4, < lower limitHematocrit, Week 12, > upper limitHematocrit, Week 12, < lower limitHematocrit, Week 24, > upper limitHematocrit, Week 24, < lower limitHematocrit, Week 36, < lower limitHematocrit,Week 52/Withdrawal,< lower limitPC, Baseline, > upper limitPC, Baseline, < lower limitPC, Week 4, > upper limitPC, Week 4, < lower limitPC, Week 12, > upper limitPC, Week 12, < lower limitPC, Week 24, > upper limitPC, Week 24, < lower limitPC, Week 36, > upper limitPC, Week 36, < lower limitPC, Week 52/Withdrawal, > upper limitPC, Week 52/Withdrawal, < lower limitWBC, Baseline, > upper limitWBC, Baseline, < lower limitWBC, Week 4, > upper limitWBC, Week 4, < lower limitWBC, Week 12, > upper limitWBC, Week 24, > upper limitWBC, Week 24, < lower limitWBC, Week 36, > upper limitWBC, Week 36, < lower limitWBC, Week 52/Withdrawal, > upper limitBasophils, Baseline, > upper limitBasophils, Week 4, > upper limitBasophils, Week 12, > upper limitBasophils, Week 36, > upper limitBasophils, Week 52/Withdrawal, > upper limitEosinophils, Baseline, > upper limitEosinophils, Week 4, > upper limitEosinophils, Week 12, > upper limitEosinophils, Week 24, > upper limitEosinophils, Week 36, > upper limitEosinophils,Week 52/Withdrawal,> upper limitNeutrophils, Baseline, > upper limitNeutrophils, Baseline, < lower limitNeutrophils, Week 4, > upper limitNeutrophils, Week 4, < lower limitNeutrophils, Week 12, > upper limitNeutrophils, Week 24, > upper limitNeutrophils, Week 36, > upper limitNeutrophils, Week 36, < lower limitNeutrophils,Week 52/Withdrawal,>upper limitNeutrophils,Week 52/Withdrawal,< lower limitLymphocytes, Baseline, > upper limitLymphocytes, Baseline, < lower limitLymphocytes, Week 4, < lower limitLymphocytes, Week 12, < lower limitLymphocytes, Week 24, < lower limitLymphocytes, Week 36, < lower limitLymphocytes,Week 52/Withdrawal,< lower limitMonocytes, Baseline, > upper limitMonocytes, Week 4, > upper limitMonocytes, Week 12, > upper limitMonocytes, Week 24, > upper limitMonocytes, Week 36, > upper limitMonocytes, wEEK 52/Withdrawal,> upper limit
GW815SF 50/500 µg303636121122133115202013142741011311319121738177654264242332515271141217101088105573615921112101617251619314737252814

[back to top]

Number of Participants With Abnormal (Outliers From the Normal Range) Clinical Chemistry Parameters

Clinical chemistry parameters: Total bilirubin (TB), Alkaline phosphatase (Al-P), Alanine aminotransferase (ALT), Asparate aminotransferase (AST), Gamma-glutamyl transpeptidase (GTP), Lactate dehydrogenase (LDH), Total cholesterol (TC), Glucose, Creatinine, Blood urea nitrogen (BUN), Uric acid (UA), Sodium (Na), Potassium (K), Chloride (Cl) and Calcium (Ca) were presented as the outliers from the normal range as > upper limit and < lower limit. Only number of participants with clinical chemistry values outside normal range were presented. (NCT00269087)
Timeframe: Up to Week 56

InterventionParticipants (Count of Participants)
TB, Baseline, > upper limitTB, Week 4, > upper limitTB, Week 12, > upper limitTB, Week 12, < lower limitTB, Week 24, > upper limitTB, Week 36, > upper limitTB, Week 36, < lower limitTB, Week 52/ withdrawal, > upper limitAL-P, Baseline, > upper limitAL-P, Week 4, > upper limitAL-P, Week 12, > upper limitAL-P, Week 24, > upper limitAL-P, Week 24, < lower limitAL-P, Week 36, > upper limitAL-P, Week 52/ withdrawal, > upper limitALT, Baseline, > upper limitALT, Week 4, > upper limitALT, Week 12, > upper limitALT, Week 24, > upper limitALT, Week 36, > upper limitALT, Week 52/ withdrawal, > upper limitAST, Baseline, > upper limitAST, Week 4, > upper limitAST, Week 12, > upper limitAST, Week 24, > upper limitAST, Week 36, > upper limitAST, Week 52/ withdrawal, > upper limitGamma GTP, Baseline, > upper limitGamma GTP, Baseline, < lower limitGamma GTP, Week 4, > upper limitGamma GTP, Week 4, < lower limitGamma GTP, Week 12, > upper limitGamma GTP, Week 12, < lower limitGamma GTP, Week 24, > upper limitGamma GTP, Week 24, < lower limitGamma GTP, Week 36, > upper limitGamma GTP, Week 36, < lower limitGamma GTP,Week 52/withdrawal, > upper limitGamma GTP,Week 52/withdrawal, < lower limitLDH, Baseline, > upper limitLDH, Week 4, > upper limitLDH, Week 12, > upper limitLDH, Week 24, > upper limitLDH, Week 36, > upper limitLDH, Week 36, < lower limitLDH, Week 52/ withdrawal, > upper limitTC, Baseline, > upper limitTC, Baseline, < lower limitTC, Week 4, > upper limitTC, Week 4, < lower limitTC, Week 12, > upper limitTC, Week 12, < lower limitTC, Week 24, > upper limitTC, Week 24, < lower limitTC, Week 36, > upper limitTC, Week 36, < lower limitTC, Week 52/ withdrawal, > upper limitTC, Week 52/ withdrawal, < lower limitGlucose, Baseline, > upper limitGlucose, Baseline, < lower limitGlucose, Week 4, > upper limitGlucose, Week 4, < lower limitGlucose, Week 12, > upper limitGlucose, Week 12, < lower limitGlucose, Week 24, > upper limitGlucose, Week 24, < lower limitGlucose, Week 36, > upper limitGlucose, Week 36, < lower limitGlucose, Week 52/ withdrawal, > upper limitGlucose, Week 52/ withdrawal, < lower limitCreatinine, Baseline, > upper limitCreatinine, Baseline, < lower limitCreatinine, Week 4, > upper limitCreatinine, Week 4, < lower limitCreatinine, Week 12, > upper limitCreatinine, Week 12, < lower limitCreatinine, Week 24, > upper limitCreatinine, Week 24, < lower limitCreatinine, Week 36, > upper limitCreatinine, Week 36, < lower limitCreatinine,Week 52/withdrawal, >upper limitCreatinine,Week 52/withdrawal, BUN, Baseline, > upper limitBUN, Baseline, < lower limitBUN, Week 4, > upper limitBUN, Week 4, < lower limitBUN, Week 12, > upper limitBUN, Week 12, < lower limitBUN, Week 24, > upper limitBUN, Week 36, > upper limitBUN, Week 52/ withdrawal, > upper limitBUN, Week 52/ withdrawal, < lower limitUA, Baseline, > upper limitUA, Week 4, > upper limitUA, Week 12, > upper limitUA, Week 24, > upper limitUA, Week 36, > upper limitUA, Week 52/ withdrawal, > upper limitNa, Baseline, > upper limitNa, Week 4, > upper limitNa, Week 4, < lower limitNa, Week 12, > upper limitNa, Week 24, > upper limitNa, Week 36, > upper limitNa, Week 52/ withdrawal, < lower limitK, Baseline, > upper limitK, Baseline, < lower limitK, Week 4, > upper limitK, Week 12, > upper limitK, Week 12, < lower limitK, Week 24, > upper limitK, Week 24, < lower limitK, Week 36, > upper limitK, Week 52/ withdrawal, > upper limitK, Week 52/ withdrawal, < lower limitCl, Baseline, > upper limitCl, Baseline, < lower limitCl, Week 4, > upper limitCl, Week 4, < lower limitCl, Week 12, > upper limitCl, Week 12, < lower limitCl, Week 24, > upper limitCl, Week 24, < lower limitCl, Week 36, > upper limitCl, Week 52/ withdrawal, > upper limitCl, Week 52/ withdrawal, < lower limitCa, Baseline, > upper limitCa, Baseline, < lower limitCa, Week 4, > upper limitCa, Week 4, < lower limitCa, Week 12, > upper limitCa, Week 12, < lower limitCa, Week 24, > upper limitCa, Week 36, > upper limitCa, Week 52/ withdrawal, > upper limitCa, Week 52/ withdrawal, < lower limit
GW815SF 50/500 µg123152141815151811213547634966945159171014812812815101011814101917131916218201022102710402424424313345453889881949376311161231182122135312919213222126232124232732114122323133231317431

[back to top]

Mean Change From Baseline in Pulse Rate

Pulse rate was measured in sitting position. Baseline value was the measurement taken at the start of run-in or the treatment period. Change from Baseline was any post Baseline value minus value at Baseline. (NCT00269087)
Timeframe: Baseline and up to Week 56

Interventionbeats per min (Mean)
Week 4Week 8Week 12Week 16Week 20Week 24Week 28Week 32Week 36Week 40Week 44Week 48Week 52 / withdrawal
GW815SF 50/500 µg-1.5-1.6-0.41.01.11.41.20.40.90.70.4-0.20.8

[back to top]

Number of Participants With Abnormal (Clinically Significant) Ophthalmological Examinations Findings

On each assessment day at Week 24, 52 and follow up, ophthalmological examinations (vision, cornea, lens, intraocular pressure, fundus oculi) were performed to determine the presence or absence of glaucoma and cataract. (NCT00269087)
Timeframe: Up to Week 56

InterventionParticipants (Count of Participants)
Cataract, BaselineCataract, Week 24Cataract, WithdrawalGlaucoma, BaselineGlucoma, Week 24Glucoma, Withdrawal
GW815SF 50/500 µg323444

[back to top]

Number of Participants With Abnormal (Clinically Significant) Electrocardiogram (ECG) Findings

On each assessment day at Week 24, 52 and follow up 12-lead ECG was performed. Additional measurements were taken at follow up visit, if the measurements made at Week 52 revealed any abnormalities of clinical significance. (NCT00269087)
Timeframe: Up to Week 56

InterventionParticipants (Count of Participants)
BaselineWeek 24Withdrawal
GW815SF 50/500 µg234

[back to top]

Mean Level of Plasma Cortisol 2

On each assessment day at Week 24, 52 and follow up, adrenal cortical function tests were performed between 8:00-10:00 in the morning. Additional measurements were taken at follow up visit, if the measurements made at Week 52 revealed any abnormalities of clinical significance. Blood samples were taken from participants at rest before undergoing spirometry. (NCT00269087)
Timeframe: Up to Week 56

Interventionµg/dL (Geometric Mean)
BaselineWeek 24Week 52/Withdrawal
GW815SF 50/500 µg9.4110.088.49

[back to top]

Mean Change From Baseline in Weight

Body weight was measured during run-in period, at Week 24 and 52. (NCT00269087)
Timeframe: Baseline and up to Week 56

InterventionKilograms (Mean)
Week 24Withdrawal
GW815SF 50/500 µg0.17-0.51

[back to top]

Mean Area Under the Plasma Concentration-time Curve From Zero up to the Last Quantifiable Plasma Concentration [AUC (0-t)] of Salmeterol

For analysis of PK parameters for salmeterol, blood samples were taken just before dosing (within one hour prior to dosing), 5, 15, 30, 45 minutes, 1, 2, 3 and 4 hours after dosing to determine plasma drug concentrations. The investigational product was taken in fasting condition just before each blood sampling. Parameters were calculated by a model-independent method with the plasma concentration-time profile data in individual participants. (NCT00269087)
Timeframe: Within one hour prior to dosing, 5, 15, 30, 45 minutes, 1, 2, 3 and 4 hours

InterventionHours*picogram per milliliter (Mean)
GW815SF 50/500 µg158.16

[back to top]

Mean Area Under the Plasma Concentration-time Curve Over a Dosing Interval [AUC(0-tau)] of FP

For analysis of PK parameters for FP, blood samples were taken just before dosing (within one hour prior to dosing), 30, 45 minutes, 1, 2, 3, 4, 6, 8 and 12 hours after dosing to determine plasma drug concentrations. The investigational product was taken in fasting condition just before each blood sampling. Parameters were calculated by a model-independent method with the plasma concentration-time profile data in individual participants. (NCT00269087)
Timeframe: Within one hour prior to dosing, 30, 45 minutes, 1, 2, 3, 4, 6, 8 and 12 hours

InterventionHours*picogram per milliliter (Mean)
GW815SF 50/500 µg903.48

[back to top]

Mean Change From Baseline in Bone Mineral Density (BMD)

On each assessment day at Week 52 and follow up, lumber (L1-L4) BMD was determined with a BMD meter by the dual energy X-ray absorption (DEXA) method. Baseline value was the measurement taken during run-in period. Change from Baseline was any value post Baseline minus value at Baseline. (NCT00269087)
Timeframe: Baseline and up to Week 56

InterventionGrams per centimeter square (Mean)
GW815SF 50/500 µg-0.014

[back to top]

Mean Change From Baseline in Percent of Days Without Use of Rescue Medication

Rescue medication (salbutamol sulfate aerosol provided as an investigational product) was issued to a participant and, when necessary, a spacer at the start of the run-in period. At each time of entry in the Chronic Obstructive Pulmonary Disease (COPD) diary, a participant recorded the number of occasions of rescue medication inhaled in the previous 24 hours in the COPD diary. Baseline was mean value of the consecutive 7 days just before Visit 2. Change from Baseline was any post Baseline value minus Baseline value. (NCT00269087)
Timeframe: Baseline and up to Week 52

InterventionPercentage of days (Mean)
GW815SF 50/500 µg15.6

[back to top]

Mean Cmax of Salmeterol

For analysis of PK parameters for salmeterol, blood samples were taken just before dosing (within one hour prior to dosing), 5, 15, 30, 45 minutes, 1, 2, 3 and 4 hours after dosing to determine plasma drug concentrations. The investigational product was taken in fasting condition just before each blood sampling. Parameters were calculated by a model-independent method with the plasma concentration-time profile data in individual participants. (NCT00269087)
Timeframe: Within one hour prior to dosing, 5, 15, 30, 45 minutes, 1, 2, 3 and 4 hours

Interventionpg/mL (Mean)
GW815SF 50/500 µg66.04

[back to top]

Rhinitis: Mean Change From Baseline at 1-2 Weeks in Nightime Total Nasal Symptom Scores (N-TNSS)

The scores of 3 nighttime symptoms (nasal congestion upon awakening, difficulty going to sleep due to nasal symptoms, nighttime awakenings due to nasal symptoms). Scale: 0=not noticeable, 1=noticeable but not bothersome, 2=noticeable and bothersome some of the time, 3=bothersome most of the time and/or very bothersome some of the time. (NCT00296491)
Timeframe: Baseline To 1-2 Weeks

InterventionPoints on a Scale (Mean)
Flut Prop/Salmeterol/Flut Nasal Spray (FSC+FPANS)-2.0
Fluticasone Propionate/Salmeterol/Montelukast (FSC+MON)1.7

[back to top]

Rhinitis: Mean Change From Baseline at 1-2 Weeks in Daytime Total Nasal Symptom Scores (D-TNNS).

The sum of scores of each of the four daytime symptoms (nasal congestion, itching, rhinorrhea, and sneezing). Scale: 0=none (no sign/symptom evident)1=mild (sign/symptom clearly present; easily tolerated)2=moderate (definite awareness of sign/symptom that is bothersome but tolerable)3=severe (sign/symptom is hard to tolerate) (NCT00296491)
Timeframe: Baseline to 1-2 Weeks

InterventionPoints on a Scale (Mean)
Fluticasone Prop/Salmeterol/Montelukast (FSC+MON)-2.3
Fluticasone Prop/Salmeterol/Flut Nasal Spray (FSC+FPANS)-3.0

[back to top]

Mean Change From Baseline at Endpoint in Morning Peak Expiratory Flow (PEF) for Per Protocol Population

Endpoint was defined as the average of the data reported from the last week of treatment. Data collected by patient throughout the treatment period between visits. The peak expiratory flow rate measures how fast a person can breathe out (exhale) air. It is one of many tests that measure how well your airways work. (NCT00296491)
Timeframe: Baseline to Endpoint (weeks 3-4)

InterventionL/min (Mean)
Flut Prop/Salmeterol/Montelukast (FSC+MON)30.9
Fluticasone Propionate/Salmeterol (FSC)35.2

[back to top]

Mean Change From Baseline at Endpoint in Morning Peak Expiration Flow (PEF) for Intent-to-Treat Population

Endpoint was defined as the average of the data reported from the last week of treatment. Data collected by patient throughout the treatment period between visits. The peak expiratory flow rate measures how fast a person can breathe out (exhale) air. It is one of many tests that measure how well your airways work. (NCT00296491)
Timeframe: Baseline to Endpoint (weeks 3-4)

InterventionL/min (Mean)
Fluticasone Prop/Salmeterol (FSC)26.4
Montelukast (MON)3.6

[back to top]

Asthma: Mean Change From Baseline at Endpoint in Predose Morning Forced Expiratory Volume (FEV1) for Per Protocol Population

Endpoint was defined as the average of the last week's worth of evaluable data. The volume of air that can be forced out taking a deep breath, an important measure of pulmonary function. FEV1 is forced expiratory volume in one second. (NCT00296491)
Timeframe: Baseline to Endpoint (weeks 3-4)

InterventionL/sec (Mean)
Fluticasone Propionate/Salmeterol/Montelukast (FSC+MON)0.27
Fluticasone Propionate/Salmeterol (FSC)0.13

[back to top]

Asthma: Mean Change From Baseline at Endpoint in Predose Morning Forced Expiratory Volume (FEV1) for Intent-to-Treat Population

Endpoint was defined as the average of the last week's worth of evaluable data. The volume of air that can be forced out taking a deep breath, an important measure of pulmonary function. FEV1 is forced expiratory volume in one second. (NCT00296491)
Timeframe: Baseline to Endpoint (weeks 3-4)

InterventionL/sec (Mean)
Fluticasone Propionate/Salmeterol (FSC)0.15
Montelukast (MON)0.04

[back to top]

Asthma: Mean Change From Baseline at Endpoint in Percentage of Asthma Symptom-Free Days for Per Protocol Population

Asthma symptom score:0=no symptoms,1=symptoms 1 short period,2=symptoms 2 or more short periods,3=symptoms most of day not affect activities,4=symptoms most of day did affect activities,5=symptoms severe.Overall satisfaction score:0=very dissatisfied,1=dissatisfied,2=slightly dissatisfied,3=neutral,4=slightly satisfied,5=satisfied 6=very satisfied (NCT00296491)
Timeframe: Baseline to Endpoint (weeks 3-4)

InterventionPercentage of asthma symptom-free days (Mean)
Fluticasone Propionate/Salmeterol/Montelukast (FSC+MON)34.8
Fluticasone Propionate/Salmeterol (FSC)37.1

[back to top]

Asthma: Mean Change From Baseline at Endpoint in Percentage of Asthma Symptom-Free Days for Intent-to-Treat Population

Endpoint was defined as the average of the data reported from the last week of treatment.Asthma symptom scores and the subject-rated overall satisfaction with treatment, related to the percentage of asthma symptom-free days. Same scale used as in outcome 8. (NCT00296491)
Timeframe: Baseline to Endpoint (weeks 3-4)

InterventionPercentage of asthma symptom-free days (Mean)
Fluticasone Propionate/Salmeterol (FSC)34.8
Montelukast (MON)26.1

[back to top]

Asthma: Mean Change From Baseline at Endpoint in Percentage of Albuterol/Salbutamol-Free Days for Per Protocol Population

Endpoint was defined as the average of the data reported from the last week of treatment. Albuterol/salbutamol use (related to percentage of asthma rescue-free days). (NCT00296491)
Timeframe: Baseline to Endpoint (weeks 3-4)

InterventionPercentage of rescue-free days (Mean)
Fluticasone Propionate + Salmeterol & Montelukast (FSC+MON)41.2
Fluticasone Propionate/Salmeterol (FSC)42.9

[back to top]

Asthma: Mean Change From Baseline at Endpoint in Percentage of Albuterol-Salbutamol Free Days for Intent-to-Treat Population

Endpoint was defined as the average of the data reported from the last week of treatment. Albuterol/salbutamol use (related to percentage of asthma rescue-free days). (NCT00296491)
Timeframe: Baseline to Endpoint (weeks 3-4)

InterventionPercentage of rescue-free days (Mean)
Fluticasone Propionate/Salmeterol (FSC)37.5
Montelukast (MON)26.7

[back to top]

"Mean Weekly Score for Asthma Control Diary Question Did You Experience Wheeze or Cough During the Day at Week 12"

Unit on a scale 1-5. 1: Not at all, 2: A little of the time, 3: A moderate amount of the time, 4: Most of the time, 5: All the time. 1 is the best value (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.539
Salmeterol1.505
Placebo1.572

[back to top]

"Mean Weekly Score for Asthma Control Diary Question Did You Experience Wheeze or Cough During the Day at Week 16"

Unit on a scale 1-5. 1: Not at all, 2: A little of the time, 3: A moderate amount of the time, 4: Most of the time, 5: All the time. 1 is the best value (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.528
Salmeterol1.515
Placebo1.669

[back to top]

"Mean Weekly Score for Asthma Control Diary Question Did You Experience Wheeze or Cough During the Day at Week 4"

Unit on a scale 1-5. 1: Not at all, 2: A little of the time, 3: A moderate amount of the time, 4: Most of the time, 5: All the time. 1 is the best value (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.679
Salmeterol1.605
Placebo1.652

[back to top]

"Mean Weekly Score for Asthma Control Diary Question Did You Experience Wheeze or Cough During the Day at Week 8"

Unit on a scale 1-5. 1: Not at all, 2: A little of the time, 3: A moderate amount of the time, 4: Most of the time, 5: All the time. 1 is the best value (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.519
Salmeterol1.56
Placebo1.575

[back to top]

"Mean Weekly Score for Asthma Control Diary Question Did You Wake up During the Night Due to Asthma at Week 12"

Unit on a scale 1-5. 1: Did not wake up, 2: Woke up once, 3: Woke up 2-5 times, 4: Woke up more than 5 times, 5: Was awake all night. 1 is the best value (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.203
Salmeterol1.194
Placebo1.224

[back to top]

"Mean Weekly Score for Asthma Control Diary Question Did You Wake up During the Night Due to Asthma at Week 16"

Unit on a scale 1-5. 1: Did not wake up, 2: Woke up once, 3: Woke up 2-5 times, 4: Woke up more than 5 times, 5: Was awake all night. 1 is the best value (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.196
Salmeterol1.135
Placebo1.185

[back to top]

"Mean Weekly Score for Asthma Control Diary Question Did You Wake up During the Night Due to Asthma at Week 4"

Unit on a scale 1-5. 1: Did not wake up, 2: Woke up once, 3: Woke up 2-5 times, 4: Woke up more than 5 times, 5: Was awake all night. 1 is the best value (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.267
Salmeterol1.22
Placebo1.232

[back to top]

"Mean Weekly Score for Asthma Control Diary Question Did You Wake up During the Night Due to Asthma at Week 8"

Unit on a scale 1-5. 1: Did not wake up, 2: Woke up once, 3: Woke up 2-5 times, 4: Woke up more than 5 times, 5: Was awake all night. 1 is the best value (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.182
Salmeterol1.176
Placebo1.21

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Limited Were You in Your Activities Today Because of Your Asthma at Week 12"

Unit on a scale 1-5. 1: Not limited at all, 2: A little limited, 3: Moderately limited, 4: Severely limited, 5: Totally limited. 1 is the best value (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.458
Salmeterol1.436
Placebo1.52

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Limited Were You in Your Activities Today Because of Your Asthma at Week 16"

Unit on a scale 1-5. 1: Not limited at all, 2: A little limited, 3: Moderately limited, 4: Severely limited, 5: Totally limited. 1 is the best value (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.446
Salmeterol1.415
Placebo1.593

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Limited Were You in Your Activities Today Because of Your Asthma at Week 4"

Unit on a scale 1-5. 1: Not limited at all, 2: A little limited, 3: Moderately limited, 4: Severely limited, 5: Totally limited. 1 is the best value (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.549
Salmeterol1.514
Placebo1.583

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Limited Were You in Your Activities Today Because of Your Asthma at Week 8"

Unit on a scale 1-5. 1: Not limited at all, 2: A little limited, 3: Moderately limited, 4: Severely limited, 5: Totally limited. 1 is the best value (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.475
Salmeterol1.478
Placebo1.545

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Much Shortness of Breath Did You Experience During the Day at Week 12"

Unit on a scale 1-5. 1: None, 2: A very little, 3: A moderate amount, 4: Quite a lot, 5: A very great deal. 1 is the best value (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.57
Salmeterol1.482
Placebo1.62

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Much Shortness of Breath Did You Experience During the Day at Week 16"

Unit on a scale 1-5. 1: None, 2: A very little, 3: A moderate amount, 4: Quite a lot, 5: A very great deal. 1 is the best value (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.623
Salmeterol1.482
Placebo1.691

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Much Shortness of Breath Did You Experience During the Day at Week 4"

Unit on a scale 1-5. 1: None, 2: A very little, 3: A moderate amount, 4: Quite a lot, 5: A very great deal. 1 is the best value (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.699
Salmeterol1.627
Placebo1.735

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Much Shortness of Breath Did You Experience During the Day at Week 8"

Unit on a scale 1-5. 1: None, 2: A very little, 3: A moderate amount, 4: Quite a lot, 5: A very great deal. 1 is the best value (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.557
Salmeterol1.571
Placebo1.643

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms During the Day at Week 12"

Unit on a scale 1-5. 1: No asthma symptoms, 2: Mild asthma symptoms, 3: Moderate asthma symptoms, 4: Severe asthma symptoms, 5: Very severe asthma symptoms. 1 is the best value (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.572
Salmeterol1.495
Placebo1.682

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms During the Day at Week 16"

Unit on a scale 1-5. 1: No asthma symptoms, 2: Mild asthma symptoms, 3: Moderate asthma symptoms, 4: Severe asthma symptoms, 5: Very severe asthma symptoms. 1 is the best value (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.609
Salmeterol1.476
Placebo1.711

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms During the Day at Week 4"

Unit on a scale 1-5. 1: No asthma symptoms, 2: Mild asthma symptoms, 3: Moderate asthma symptoms, 4: Severe asthma symptoms, 5: Very severe asthma symptoms. 1 is the best value (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.735
Salmeterol1.637
Placebo1.744

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms During the Day at Week 8"

Unit on a scale 1-5. 1: No asthma symptoms, 2: Mild asthma symptoms, 3: Moderate asthma symptoms, 4: Severe asthma symptoms, 5: Very severe asthma symptoms. 1 is the best value (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.603
Salmeterol1.569
Placebo1.699

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms in the Morning at Week 4"

Unit on a scale 1-5. 1: No asthma symptoms, 2: Mild asthma symptoms, 3: Moderate asthma symptoms, 4: Severe asthma symptoms, 5: Very severe asthma symptoms. 1 is the best value (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.612
Salmeterol1.486
Placebo1.615

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms This Morning at Week 12"

Unit on a scale 1-5. 1: No asthma symptoms, 2: Mild asthma symptoms, 3: Moderate asthma symptoms, 4: Severe asthma symptoms, 5: Very severe asthma symptoms. 1 is the best value (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.519
Salmeterol1.436
Placebo1.542

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms This Morning at Week 16"

Unit on a scale 1-5. 1: No asthma symptoms, 2: Mild asthma symptoms, 3: Moderate asthma symptoms, 4: Severe asthma symptoms, 5: Very severe asthma symptoms. 1 is the best value (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.536
Salmeterol1.461
Placebo1.647

[back to top]

Mean Weekly Morning Peak Expiratory Flow at Week 8

Mean weekly morning peak expiratory flow at week 8, pre-dose (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium355.42
Salmeterol350.53
Placebo330.193

[back to top]

Mean Weekly Morning Peak Expiratory Flow at Week 16

Mean weekly morning peak expiratory flow at week 16, pre-dose (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium355.619
Salmeterol355.799
Placebo334.525

[back to top]

Mean Weekly Morning Peak Expiratory Flow at Week 12

Mean weekly morning peak expiratory flow at week 12, pre-dose (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium359.05
Salmeterol351.3
Placebo332.808

[back to top]

Mean Weekly Morning Forced Expiratory Volume in 1 Second at Week 8

Mean weekly morning forced expiratory volume in 1 second at week 8, pre-dose (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.254
Salmeterol2.287
Placebo2.164

[back to top]

Mean Weekly Morning Forced Expiratory Volume in 1 Second at Week 4

Mean weekly morning forced expiratory volume in 1 second at week 4, pre-dose (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.301
Salmeterol2.316
Placebo2.161

[back to top]

Mean Weekly Morning Forced Expiratory Volume in 1 Second at Week 16

Mean weekly morning forced expiratory volume in 1 second at week 16, pre-dose (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.3
Salmeterol2.278
Placebo2.188

[back to top]

Systolic Blood Pressure in Conjunction With Spirometry at Visit 5

Systolic blood pressure collected in conjunction with spirometry at 16 weeks (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionmmHg (Mean)
Tiotropium124.23
Salmeterol123.83
Placebo124.47

[back to top]

Mean Weekly Morning Forced Expiratory Volume in 1 Second at Week 12

Mean weekly morning forced expiratory volume in 1 second at week 12, pre-dose (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.256
Salmeterol2.254
Placebo2.156

[back to top]

Mean Weekly Evening Peak Expiratory Flow at Week 8

Mean weekly evening peak expiratory flow at week 8, pre-dose (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium368.758
Salmeterol359.586
Placebo345.299

[back to top]

Mean Weekly Evening Peak Expiratory Flow at Week 4

Mean weekly evening peak expiratory flow at week 4, pre-dose (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium374.496
Salmeterol366.219
Placebo348.344

[back to top]

Pulse Rate in Conjunction With Spirometry at Visit 4

Pulse rate collected in conjunction with spirometry at 12 weeks (NCT00350207)
Timeframe: After 12 weeks of treatment

Interventionbpm (Mean)
Tiotropium74.8
Salmeterol74.6
Placebo74.2

[back to top]

Mean Weekly Evening Peak Expiratory Flow at Week 16

Mean weekly evening peak expiratory flow at week 16, pre-dose (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium363.657
Salmeterol360.304
Placebo340.099

[back to top]

Mean Weekly Evening Peak Expiratory Flow at Week 12

Mean weekly evening peak expiratory flow at week 12, pre-dose (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium366.282
Salmeterol362.01
Placebo344.291

[back to top]

Mean Weekly Evening Forced Expiratory Volume in 1 Second at Week 8

Mean weekly evening forced expiratory volume in 1 second at week 8, pre-dose (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.32
Salmeterol2.301
Placebo2.239

[back to top]

Mean Weekly Evening Forced Expiratory Volume in 1 Second at Week 4

Mean weekly evening forced expiratory volume in 1 second at week 4, pre-dose (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.369
Salmeterol2.318
Placebo2.25

[back to top]

Mean Weekly Evening Forced Expiratory Volume in 1 Second at Week 16

Mean weekly evening forced expiratory volume in 1 second at week 16, pre-dose (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.343
Salmeterol2.291
Placebo2.215

[back to top]

Mean Weekly Evening Forced Expiratory Volume in 1 Second at Week 12

Mean weekly evening forced expiratory volume in 1 second at week 12, pre-dose (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.31
Salmeterol2.299
Placebo2.231

[back to top]

Mean PEF Variability at Week 8

PEF (Peak expiratory flow) variability is defined as the difference between the highest morning PEF value and the highest evening PEF value of one day divided by the arithmetic mean of these two PEF values and multiplied by 100% (NCT00350207)
Timeframe: After 8 weeks of treatment

Interventionratio expressed in percent (Least Squares Mean)
Tiotropium13.377
Salmeterol11.252
Placebo12.964

[back to top]

Morning Pre-dose Forced Vital Capacity as Measured by Spirometry at Visit 5

Morning pre-dose forced vital capacity as measured by spirometry after 16 weeks of treatment (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium3.488
Salmeterol3.474
Placebo3.353

[back to top]

Mean PEF Variability at Week 4

PEF (Peak expiratory flow) variability is defined as the difference between the highest morning PEF value and the highest evening PEF value of one day divided by the arithmetic mean of these two PEF values and multiplied by 100% (NCT00350207)
Timeframe: After 4 weeks of treatment

Interventionratio expressed in percent (Least Squares Mean)
Tiotropium12.043
Salmeterol10.547
Placebo12.085

[back to top]

Mean PEF Variability at Week 16

PEF (Peak expiratory flow) variability is defined as the difference between the highest morning PEF value and the highest evening PEF value of one day divided by the arithmetic mean of these two PEF values and multiplied by 100% (NCT00350207)
Timeframe: After 16 weeks of treatment

Interventionratio expressed in percent (Least Squares Mean)
Tiotropium11.742
Salmeterol10.793
Placebo12.305

[back to top]

"Mean Weekly Score for Asthma Control Diary Question How Were Your Asthma Symptoms This Morning at Week 8"

Unit on a scale 1-5. 1: No asthma symptoms, 2: Mild asthma symptoms, 3: Moderate asthma symptoms, 4: Severe asthma symptoms, 5: Very severe asthma symptoms. 1 is the best value (NCT00350207)
Timeframe: After 8 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium1.504
Salmeterol1.481
Placebo1.613

[back to top]

Mean PEF Variability at Week 12

PEF (Peak expiratory flow) variability is defined as the difference between the highest morning PEF value and the highest evening PEF value of one day divided by the arithmetic mean of these two PEF values and multiplied by 100% (NCT00350207)
Timeframe: After 12 weeks of treatment

Interventionratio expressed in percent (Least Squares Mean)
Tiotropium11.735
Salmeterol11.320
Placebo11.257

[back to top]

Diastolic Blood Pressure in Conjunction With Spirometry at Visit 5

Diastolic blood pressure collected in conjunction with spirometry at 16 weeks (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionmmHg (Mean)
Tiotropium79.23
Salmeterol77.61
Placebo78.38

[back to top]

Diastolic Blood Pressure in Conjunction With Spirometry at Visit 4

Diastolic blood pressure collected in conjunction with spirometry at 12 weeks (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionmmHg (Mean)
Tiotropium77.88
Salmeterol77.22
Placebo78.29

[back to top]

Diastolic Blood Pressure in Conjunction With Spirometry at Visit 3

Diastolic blood pressure collected in conjunction with spirometry at 6 weeks (NCT00350207)
Timeframe: After 6 weeks of treatment

InterventionmmHg (Mean)
Tiotropium78.62
Salmeterol77.62
Placebo79.34

[back to top]

Change in Mean Weekly Morning Peak Expiratory Flow From Baseline to the End of the Trial

Change from baseline in mean weekly morning peak expiratory flow at 16 weeks. Baseline is defined as the last week prior to the randomisation visit (NCT00350207)
Timeframe: baseline and after 16 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium-3.93
Salmeterol-3.15
Placebo-24.63

[back to top]

Systolic Blood Pressure in Conjunction With Spirometry at Visit 4

Systolic blood pressure collected in conjunction with spirometry at 12 weeks (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionmmHg (Mean)
Tiotropium124.81
Salmeterol123.92
Placebo125.18

[back to top]

Systolic Blood Pressure in Conjunction With Spirometry at Visit 3

Systolic blood pressure collected in conjunction with spirometry at 6 weeks (NCT00350207)
Timeframe: After 6 weeks of treatment

InterventionmmHg (Mean)
Tiotropium124.68
Salmeterol123.11
Placebo126.41

[back to top]

Pulse Rate in Conjunction With Spirometry at Visit 5

Pulse rate collected in conjunction with spirometry at 16 weeks (NCT00350207)
Timeframe: After 16 weeks of treatment

Interventionbpm (Mean)
Tiotropium74.4
Salmeterol75.3
Placebo74.7

[back to top]

Pulse Rate in Conjunction With Spirometry at Visit 3

Pulse rate collected in conjunction with spirometry at 6 weeks (NCT00350207)
Timeframe: After 6 weeks of treatment

Interventionbpm (Mean)
Tiotropium74.7
Salmeterol74.9
Placebo74.2

[back to top]

Mean Weekly Morning Peak Expiratory Flow at Week 4

Mean weekly morning peak expiratory flow at week 4, pre-dose (NCT00350207)
Timeframe: After 4 weeks of treatment

InterventionL/min (Least Squares Mean)
Tiotropium360.695
Salmeterol359.762
Placebo335.515

[back to top]

Morning Pre-dose Forced Vital Capacity as Measured by Spirometry at Visit 4

Morning pre-dose forced vital capacity as measured by spirometry after 12 weeks of treatment (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium3.509
Salmeterol3.495
Placebo3.307

[back to top]

Morning Pre-dose Forced Vital Capacity as Measured by Spirometry at Visit 3

Morning pre-dose forced vital capacity as measured by spirometry after 6 weeks of treatment (NCT00350207)
Timeframe: After 6 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium3.531
Salmeterol3.441
Placebo3.367

[back to top]

Morning Pre-dose Forced Expiratory Volume in 1 Second as Measured by Spirometry at Visit 5

Morning pre-dose forced expiratory volume in 1 second as measured by spirometry after 16 weeks od treatment (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.439
Salmeterol2.457
Placebo2.29

[back to top]

Morning Pre-dose Forced Expiratory Volume in 1 Second as Measured by Spirometry at Visit 4

Morning pre-dose forced expiratory volume in 1 second as measured by spirometry after 12 weeks of treatment (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.467
Salmeterol2.442
Placebo2.266

[back to top]

Morning Pre-dose Forced Expiratory Volume in 1 Second as Measured by Spirometry at Visit 3

Morning pre-dose forced expiratory volume in 1 second as measured by spirometry after 6 weeks of treatment (NCT00350207)
Timeframe: After 6 weeks of treatment

InterventionL (Least Squares Mean)
Tiotropium2.471
Salmeterol2.401
Placebo2.299

[back to top]

Mini-Asthma Quality of Life Questionnaire (Mini-AQLQ) Overall Score at Visit 3

Mean of the responses to 15 questions from 4 domains: Symptoms (1), Activity Limitations (2), Emotional Function (3), Environmental Stimuli (4). Unit on a scale 1-7. For domain (2): 1: totally limited, 2: extremely limited, 3: very limited, 4: moderate limitation, 5: some limitation, 6: a little limitation, 7: not at all limited. For other domains: 1: all of the time, 2: most of the time, 3: a good bit of the time, 4: some of the time, 5: a little of the time, 6: hardly any of the time, 7: none of the time. 7 is the best value (NCT00350207)
Timeframe: After 6 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium5.050
Salmeterol5.259
Placebo5.097

[back to top]

Mini-AQLQ Overall Score at Visit 5

Mean of the responses to 15 questions from 4 domains: Symptoms (1), Activity Limitations (2), Emotional Function (3), Environmental Stimuli (4). Unit on a scale 1-7. For domain (2): 1: totally limited, 2: extremely limited, 3: very limited, 4: moderate limitation, 5: some limitation, 6: a little limitation, 7: not at all limited. For other domains: 1: all of the time, 2: most of the time, 3: a good bit of the time, 4: some of the time, 5: a little of the time, 6: hardly any of the time, 7: none of the time. 7 is the best value (NCT00350207)
Timeframe: After 16 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium5.305
Salmeterol5.454
Placebo5.214

[back to top]

Mini-AQLQ Overall Score at Visit 4

Mean of the responses to 15 questions from 4 domains: Symptoms (1), Activity Limitations (2), Emotional Function (3), Environmental Stimuli (4). Unit on a scale 1-7. For domain (2): 1: totally limited, 2: extremely limited, 3: very limited, 4: moderate limitation, 5: some limitation, 6: a little limitation, 7: not at all limited. For other domains: 1: all of the time, 2: most of the time, 3: a good bit of the time, 4: some of the time, 5: a little of the time, 6: hardly any of the time, 7: none of the time. 7 is the best value (NCT00350207)
Timeframe: After 12 weeks of treatment

InterventionUnit on a scale (Least Squares Mean)
Tiotropium5.233
Salmeterol5.399
Placebo5.078

[back to top]

Number of Participants Who Achieved WC Asthma

WC asthma is defined as two or more of symptom score >1 only allowed on <=2 days/week, rescue salbutamol/albuterol use on <=2 days/week and up to a maximum of 4 times per week, >=80% predicted morning PEF daily assessed for 7 consecutive days and all the following criteria: no night-time awakening due to asthma, no exacerbations, no emergency visits, no treatment related adverse events enforcing a change in any asthma therapy. Number of participants/group who achieved the status of at least WC during the last 8 wks of treatment was analyzed using logistic regression, including covariates for sex, age, treatment group, country amalgamation and baseline prebronchodilator FEV1. Each week was classified as 'WC', 'Not Controlled' or 'Unevaluable'. A participant was considered to have WC asthma if they achieved 4/4, 5/5, 6/6, 6/7, 7/8 or 8/8 wks that were WC. 'Unevaluable' classification included participants with less than 4 wks of data during the assessment period. (NCT00353873)
Timeframe: Week 5 up to Week 12

InterventionParticipants (Number)
FP 200 mcg BD61
SFC 50/100 mcg BD65

[back to top]

Number of Participants Who Achieved 'Totally Controlled' (TC) Asthma

TC asthma is defined as no daily symptoms, no night-time wakening due to asthma, no exacerbations, no rescue salbutamol/albuterol use, no emergency visits, >=80% predicted morning PEF, and no treatment related adverse events enforcing a change in asthma therapy over 7 consecutive days. Number of participants/group who achieved the status of at least TC during the last 8 weeks (wks) of treatment was analyzed using logistic regression, including covariates for sex, age, treatment group, country amalgamation and baseline pre-bronchodilator Forced Expiratory Volume in one second (FEV1). Asthma control was assessed each week for the last 8 wks of treatment period. Each week was classified as 'TC', 'Well Controlled' (WC), 'Not Controlled' or 'Unevaluable'. A participant was considered to have TC asthma if they achieved 4/4, 5/5, 6/6, 6/7, 7/8 or 8/8 wks that were TC. 'Unevaluable' classification included participants with less than 4 wks of data during the assessment period. (NCT00353873)
Timeframe: Week 5 up to Week 12

InterventionParticipants (Number)
FP 200 mcg BD23
SFC 50/100 mcg BD28

[back to top]

Mean Change From Baseline in Morning PEF Over 12 Weeks in Per Protocol (PP) Population

PEF is the maximum flow generated during expiration, as measured with a peak flow meter and recorded in eDRC, performed with maximal force and started after a full inspiration. The mean morning PEF measurement was constructed by calculating a simple mean for each participant over the interval Weeks 1 to 12. All PEF measurements were converted to the Wright/McKerow peak flow meter scale for the purposes of analyses. The change from Baseline is then calculated by subtracting the Baseline PEF values from the individual on-treatment values. Baseline was calculated as the mean of the values recorded on the seven days preceding randomization. The analysis was done using ANCOVA adjusted for baseline PEF, country amalgamation, age, sex and treatment. (NCT00353873)
Timeframe: Baseline; Week 1 up to Week 12

InterventionL/min (Least Squares Mean)
FP 200 mcg BD18.4
SFC 50/100 mcg BD27.7

[back to top]

Mean Change From Baseline in Morning Peak Expiratory Flow (PEF) Over 12 Weeks in Intent-to-treat (ITT) Population

PEF is the maximum flow generated during expiration, as measured with a peak flow meter and recorded in electronic diary record card (eDRC), performed with maximal force and started after a full inspiration. The mean morning PEF measurement was constructed by calculating a simple mean for each participant over the interval Weeks 1 to 12. All PEF measurements were converted to the Wright/McKerow peak flow meter scale for the purposes of analyses. The change from Baseline is then calculated by subtracting the Baseline PEF values from the individual on-treatment values. Baseline was calculated as the mean of the values recorded on the seven days preceding randomization. The analysis was done using analysis of covariance (ANCOVA) adjusted for baseline PEF, country amalgamation, age, sex and treatment. (NCT00353873)
Timeframe: Baseline; Week 1 up to Week 12

InterventionLiters/Minute (L/min) (Least Squares Mean)
FP 200 mcg BD19.3
SFC 50/100 mcg BD26.9

[back to top]

Percent Change From Baseline in Bone Mineral Density (BMD) at the Lumbar Spine L1-L4

BMD, a measure of bone density, reflecting the strength of bones as represented by calcium content. The BMD test detects osteopenia (mild bone loss) and osteoporosis (more severe bone loss, which may cause symptoms). BMD at the lumber spine (L1-L4) was measured via dual energy x-ray absorptiometry (DEXA) (using DEXA equipment) scans at Baseline and every 26 weeks during the study. Acceptable DEXA measurements must be conducted prior to the first dose of randomized study medication. Baseline was defined as the collections taken on Day 1 of treatment period. Change from Baseline was calculated by subtracting the Baseline value from indicated time point value. (NCT00355342)
Timeframe: Baseline and Week 26, 52, 78, 104, 130, and 156

,
InterventionPercent Change (Mean)
Week 26Week 52Week 78Week 104Week 130Week 156
Fluticasone Propionate/Salmeterol 250/50 mcg BID0.21.31.00.81.01.9
Salmeterol 50 mcg BID0.50.81.30.90.30.3

[back to top]

Percent Change From Baseline in BMD at the Total Hip

BMD, a measure of bone density, reflecting the strength of bones as represented by calcium content. The BMD test detects osteopenia (mild bone loss) and osteoporosis (more severe bone loss, which may cause symptoms).BMD at the total hip was measured via dual energy x-ray absorptiometry (DEXA) (using DEXA equipment) scans at Baseline and every 26 weeks during the study. Acceptable DEXA measurements must be conducted prior to the first dose of randomized study medication. Baseline was defined as the collections taken on day 1 of treatment period. Change from Baseline was calculated by subtracting the Baseline value from indicated time point value. (NCT00355342)
Timeframe: Baseline and Week 26, 52, 78, 104, 130, and 156

,
InterventionPercent Change (Mean)
Week 26Week 52Week 78Week 104Week 130Week 156
Fluticasone Propionate/Salmeterol 250/50 mcg BID-0.4-1.4-2.1-2.6-2.7-2.9
Salmeterol 50 mcg BID-0.3-0.5-0.8-1.1-1.7-1.8

[back to top]

Change From Baseline in Mean Morning Percent Predicted Peak Expiratory Flow (PEF) at Week 12

PEF, a person's maximum speed of expiration, as measured with a peak flow meter, a small, hand-held device used to monitor a person's ability to breathe out air. The mean morning PEF evaluated by means of the data documented in the asthma diaries. Change from baseline value was calculated by subtracting baseline value from week 12 value. The assessments recorded at Visit 3 were considered as Baseline assessments. (NCT00363480)
Timeframe: Baseline (Visit 3) and Week 12

InterventionPercentage (Mean)
SFC 50/250 mcg7.798

[back to top]

Change From Baseline in Quality of Life Using the Asthma Quality of Life Questionnaire (AQLQ)

For the level of asthma control, baseline values were derived taking the last 8 weeks during the pre-treatment period prior to Visit 3 into consideration. Regarding derived variables based on the asthma diary, data from the last week prior to Visit 3 was taken. Visit 3, regarded as baseline. AQLQ has 32 questions regarding activities, emotions, symptoms, and environmental triggers. Each item values range from 1 (maximum impairment) to 7 (no impairment). A positive change from baseline score indicates improvement. (NCT00363480)
Timeframe: Baseline (Visit 3) up to Week 12

InterventionScore on Scale (Mean)
SFC 50/250 mcg0.83

[back to top]

Change From Baseline in Mean ACT Score at Visit 6

The total ACT score is based on a range of 5 to 25. Higher score indicates better asthma control. A score of 19 or less may be a sign that asthma symptoms not under control. In order to derive the total ACT score, all 5 questions had to be answered. Change from baseline value was calculated by subtracting baseline value from week 12 value. The assessments recorded at Visit 3 were considered as Baseline assessments. (NCT00363480)
Timeframe: Baseline (Viait 3) and Week 12

InterventionScore on a scale (Mean)
SFC 50/250 mcg5.0

[back to top]

Change From Baseline in Mean 24-hour Symptom Score at Week 12

The various symptoms like wheezing, shortness of breath, coughing and chest tightness were assessed by the participants every morning using a symptom score scale which ranged from 0 (no symptoms during the past 24 hours) to 5 (symptoms so severe that participant could not go to work or carry out other normal daily activities). Change from baseline value was calculated by subtracting baseline value from week 12 value. The assessments recorded at Visit 3 were considered as Baseline assessments. (NCT00363480)
Timeframe: Baseline (Visit 3) and Week 12

InterventionScore on Scale (Mean)
SFC 50/250 mcg-0.590

[back to top]

Change From Baseline in Number of Additional Usage of Salbutamol at Week 12

Salbutamol was given as a rescue medicine, used on <= 2 days and at most 4 occasions per week. Change from baseline value was calculated by subtracting the baseline value from week 12 value. The assessments recorded at Visit 3 were considered as Baseline assessments. (NCT00363480)
Timeframe: Baseline (Visit 3) and week 12

InterventionNumber of occassions (Mean)
SFC 50/250 mcg-0.933

[back to top]

Correlation of Change in AQLQ Score and Change in ACT Score

Correlation between change in the AQLQ and ACT score was tabulated using the Pearson coefficient of correlation (linear correlation). The AQLQ contained 32 items in 4 domains: activity limitation, symptoms, emotional function and environmental stimuli. Scores for the domains as well as the overall score were scaled within a range of 1 (worst) to 7 (best). (NCT00363480)
Timeframe: Week 12

Interventionparticipants (Number)
SFC 50/250 mcg0.522

[back to top]

Number of Participants With Adverse Events (AE) Leading to a Change in Asthma Treatment

AE was any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which did not necessarily have a causal relationship with the treatment. Number of participants with AE who lead to change in asthma treatment were reported. (NCT00363480)
Timeframe: Up to Week 12

InterventionParticipants (Number)
SFC 50/250 mcg4

[back to top]

Number of Participants With Occurrence of (Near-) Incidents Associated With Peak Flow Measurements

Frequencies of participants with at least one (near-) incident associated with peak flow measurements were recorded. analysis was done on safety population. (NCT00363480)
Timeframe: Up to Week 12

Interventionparticipants (Number)
SFC 50/250 mcg0

[back to top]

Percent Change From Baseline in Number of Nights With no Nocturnal Awakening at Week 12

Number of nights with no night time awakening were recorded at Week 12. Baseline was the last corresponding time period immediately prior to Visit 3. (NCT00363480)
Timeframe: Baseline (Visit 3) and week 12

InterventionPercent Change (Mean)
SFC 50/250 mcg7.228

[back to top]

Assessment of Tolerability by Change From Baseline of Pulse Rate

Pulse rate was recorded over time (Visit 1, 3, 4, 5, and 6). Baseline was the measurement at Visit 3. Change from baseline value was calculated by subtracting baseline value from week 12 value. (NCT00363480)
Timeframe: Baseline (Visit 3) up to Week 12

InterventionBeats per minute (bpm) (Mean)
Week 4Week 8Week 12
SFC 50/250 mcg1.0-0.20.6

[back to top]

Assessment of Tolerability by Change From Baseline of Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

SBP and DBP were recorded over time (Visit 1, 3, 4, 5, and 6). Baseline was the measurement at Visit 3. Change from baseline value was calculated by subtracting baseline value from week 12 value. (NCT00363480)
Timeframe: Baseline (Visit 3) up to Week 12

Interventionmillimeters of mercury (mmHg) (Mean)
SBP, Week 4SBP, Week 8SBP, Week 12DBP, Week 4DBP, Week 8DBP, Week 12
SFC 50/250 mcg0.8-0.70.20.2-0.20.6

[back to top]

Assessment of Tolerability by Number of Participants With at Least One Treatment Emergent Serious and, Non-serious AE

An AE is any untoward medical occurrence in a participant or clinical AE was any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which did not necessarily have a causal relationship with the treatment. Number of participants with at least one treatment emergent serious and, non-serious AE were reported. (NCT00363480)
Timeframe: Up to Week 12

InterventionParticipants (Number)
Any Non-Serious AEAny Serious AE
SFC 50/250 mcg761

[back to top]

Percentage of Well Controlled Participants as Per Gaining Optimal Asthma Control (GOAL) Criteria After 12 Week Compared to Percentage of Participants With Asthma Control Test (ACT) Score of 20-25 for Week 9 to Week 12

A week with well controlled asthma, when two or more of the criteria were fulfilled (diary entries): At most 2 days per week with 24-hour symptom score >1 (Range: 0= None to 5= severe), rescue salbutamol use on <= 2 days and at most 4 occasions per week, and a morning peak flow >= 80% of the predicted value on each day per week. All of the criteria which includes no night-time awakenings due to asthma (diary entry), no emergency visits (diary entry), no exacerbations and no treatment-related adverse events leading to treatment change are fulfilled. The total ACT score is based on a range of 5 to 25. Higher score indicates better asthma control. A score of 19 or less may be a sign that asthma symptoms are not under control. (NCT00363480)
Timeframe: Week 9 to Week 12

InterventionPercentage (Number)
GOALACT
SFC 50/250 mcg33.564.1

[back to top]

Change From Baseline in Forced Expiratory Volume (FEV1) to Week 12

FEV1, an amount of air exhaled by a person during a forced breath in one second. FEV1 assessed at Visit 1 and at Visits 3, 4, 5, 6. Baseline was the measurement at Visit 3. Change from baseline value was calculated by subtracting baseline value from week 12 value. (NCT00363480)
Timeframe: Baseline (Visit 3) up to Week 12

InterventionLitre/second (L/Sec) (Mean)
Week 4Week 8Week 12
SFC 50/250 mcg0.1330.2120.181

[back to top]

Change From Baseline in Percentage of Participants With ACT Score of 20-25 at Week 12

The total ACT score is based on a range of 5 to 25. Higher score indicates better asthma control. A score of 19 or less may be a sign that asthma symptoms are not under control. In order to derive the total ACT score, all 5 questions needed to be answered. Change from baseline value was calculated by subtracting baseline value from week 12 value. The assessments recorded at Visit 3 were considered as Baseline assessments. (NCT00363480)
Timeframe: Baseline (Visit 3) and Week 12

InterventionParticipants (Number)
BaselineWeek 12
SFC 50/250 mcg32139

[back to top]

Number of Participants With Emergency Visits Due to Asthma

Frequencies of emergency visits per participant were recorded during treatment period. Only the participants at risk were considered when calculating the incidence rates. (NCT00363480)
Timeframe: Up to week 12

InterventionParticipants (Number)
At least 1 day1 day2 days3-4 days5-9 days
SFC 50/250 mcg1310210

[back to top]

Number of Participants With Well Controlled and Totally Controlled Asthma at Week 12

Well controlled or totally controlled asthma assessments were done according to the GOAL criteria. A week with well controlled asthma, when two or more of the criteria were fulfilled (diary entries): At most 2 days per week with 24-hour symptom score >1(Range: 0= None to 5= severe), rescue salbutamol use on <= 2 days and at most 4 occasions per week, and morning peak flow >= 80% of the predicted value on each day per week. All of the criteria which included no night-time awakenings due to asthma (diary entry),no emergency visits (diary entry), no exacerbations and no treatment-related adverse events leading to treatment change were fulfilled. The total ACT score was based on a range of 5 to 25. Higher score indicates better asthma control. A score of 19 or less may be a sign that asthma symptoms are not under control. Change from baseline value was calculated by subtracting baseline value from week 12 value. The assessments recorded at Visit 3 were considered as Baseline assessments. (NCT00363480)
Timeframe: Week 12

InterventionParticipants (Number)
Well ControlledTotally Controlled
SFC 50/250 mcg6529

[back to top]

The Number of All Randomized Subjects Reporting Adverse Events (AEs).

AEs that are considered Related, Severe, and Serious, as determined by the investigator and using specific criteria defined in the protocol, are included in the primary results. (NCT00379288)
Timeframe: 1 year

,,,
Interventionparticipants (Number)
Treatment-Emergent Adverse Events (TEAE)Related Adverse EventsSevere Adverse EventsSerious Adverse Events
F/SC 250/50 mcg BID561644
F/SC 500/50 mcg BID501342
MF/F 200/10 mcg BID1094087
MF/F 400/10 mcg BID1033058

[back to top]

Change From Baseline in the Pre-bronchodilator FEV1/FVC Ratio

(NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionratio (Mean)
2xICS0.98
1xICS + LABA2.13
1xICS + LTRA0.55

[back to top]

Change From Baseline in the Pre-bronchodilator Forced Expiratory Volume in One Second (FEV1) % Predicted

(NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionpercentage points (Mean)
2xICS0.26
1xICS + LABA1.07
1xICS + LTRA-0.84

[back to top]

Change From Baseline in the Pre-bronchodilator Forced Vital Capacity (FVC) % Predicted

(NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionpercentage points (Mean)
2xICS-1.00
1xICS + LABA-1.58
1xICS + LTRA-1.56

[back to top]

The Number of Participants With a Differential Response to the Three Step-up Therapies Based on Fixed Threshold Criteria for the Following Three Asthma Control Measures: Use of Oral Prednisone for Acute Asthma Exacerbations, Asthma Control Days and FEV1.

One treatment period was ranked as better than another if the total amount of prednisone received during the period was at least 180 mg less, if the number of annualized asthma-control days during the final 12 weeks of the period was increased by at least 31 days, or if the FEV1 at the end of the period was at least 5% higher. If the prednisone threshold was met, then we ignored the number of asthmacontrol days and the FEV1. If the threshold for asthma-control days was met, then we ignored the FEV1. Otherwise, the order of response was determined by the FEV1. (NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

InterventionParticipants (Number)
All Participants161

[back to top]

Change From Baseline in the Post-bronchodilator FEV1 Percent Predicted

(NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionpercentage points (Mean)
2xICS-0.2
1xICS + LABA-1.2
1xICS + LTRA-0.8

[back to top]

Change From Baseline in the Peak Expiratory Flow Rate (PEFR) Variability

PEFR variability is calculated as 100% times the difference between the evening and morning PEFR values, divided by the average of the evening and morning PEFR values, i.e., PEFR variability = 100% x (morning PEFR - evening PEFR)/((morning PEFR + evening PEFR)/2) (NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionpercentage points (Mean)
2xICS2.09
1xICS + LABA1.61
1xICS + LTRA1.72

[back to top]

Change From Baseline in the Natural Logarithm of Exhaled Nitric Oxide (eNO)

(NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionnatural logarithm of parts per billion (Mean)
2xICS-0.04
1xICS + LABA-0.05
1xICS + LTRA-0.02

[back to top]

Change From Baseline in the Morning Peak Expiratory Flow Rate (PEFR) % Predicted

(NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionpercentage points (Mean)
2xICS4.44
1xICS + LABA6.26
1xICS + LTRA4.04

[back to top]

Change From Baseline in the Logarithm Base 2 of the Methacholine PC20

The methacholine PC20 is the concentration of methacholine that causes a 20% decrease in the pre-bronchodilator FEV1. The logarithm base 2 transformation converts the PC20 into doubling dilutions. (NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventiondoubling dilutions (Mean)
2xICS1.11
1xICS + LABA1.20
1xICS + LTRA1.00

[back to top]

Change From Baseline in the Evening Peak Expiratory Flow Rate (PEFR) % Predicted

(NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionpercentage points (Mean)
2xICS2.84
1xICS + LABA4.87
1xICS + LTRA2.29

[back to top]

Change From Baseline in the Asthma Control Test (ACT)

The ACT consists of five items, each scored as 1 (worst) to 5 (best). The five items are averaged. (NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionunits on a scale (Mean)
2xICS1.49
1xICS + LABA1.87
1xICS + LTRA1.69

[back to top]

Change From Baseline in the Impulse Oscillometry Resistance at 5 Hertz

Change from baseline in the impulse oscillometry resistance at 5 Hertz, measured in kiloPascals per liters per second (NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

InterventionkiloPascals per liters per second (Mean)
2xICS-0.08
1xICS + LABA-0.09
1xICS + LTRA-0.06

[back to top]

Change From Baseline in Asthma Quality of Life

Asthma quality of life is measured as the average of 23 questions, each of which is scored from 1 (worse) to 7 (best) (NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

Interventionunits on a scale (Mean)
2xICS0.2
1xICS + LABA0.3
1xICS + LTRA0.3

[back to top]

Number of Participants With Asthma Exacerbations

An asthma exacerbation was defined as the administration of a course of oral/systemic prednisone for the treatment of asthma. (NCT00395304)
Timeframe: Measured during the last 12 weeks of each 16-week treatment period

InterventionParticipants (Count of Participants)
2xICS49
1xICS + LABA35
1xICS + LTRA37

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) by Time Point From 5 Minutes to 12 Hours Post-dose on Day 1 and From 22 to 24 Hours Post-dose on Day 2

Spirometry was conducted according to internationally accepted standards. FEV1 by time point was calculated using a mixed model with (period) baseline, defined as the value measured prior to the first study drug intake in the period, as a covariate. (NCT00403754)
Timeframe: 5, 15, and 30 minutes; and 1, 2, 4, 8, and 12 hours post-dose on Day 1; and 22, 23, and 24 hours post-dose on Day 2

,,,,
InterventionLiters (Least Squares Mean)
5 minutes15 minutes30 minutes1 hour2 hours4 hours8 hours12 hours22 hours23 hours24 hours
Indacaterol 150 µg2.192.272.302.322.382.352.282.242.202.252.26
Indacaterol 300 µg2.202.282.332.352.392.392.352.302.252.282.29
Indacaterol 600 µg2.252.332.372.412.452.422.372.332.302.322.32
Placebo2.042.052.072.092.132.102.062.002.012.062.09
Salmeterol 100 μg2.132.192.242.292.342.342.252.202.182.232.27

[back to top]

Peak Forced Expiratory Volume in 1 Second (FEV1) From 5 Minutes to 4 Hours Post-dose on Day 1

Spirometry was conducted according to internationally accepted standards. Peak FEV1 is the maximum FEV1 recorded in the period between 5 minutes and 4 hours post dose. Analysis of Covariance was carried out with a mixed model that used (period) baseline, defined as the value of FEV1 measured prior to the first study drug intake in the period, as a covariate. (NCT00403754)
Timeframe: 5 minutes to 4 hours post-dose on Day 1

InterventionLiters (Least Squares Mean)
Indacaterol 600 µg2.49
Indacaterol 300 µg2.44
Indacaterol 150 µg2.41
Placebo2.19
Salmeterol 100 μg2.39

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) Standardized (With Respect to Time) Area Under the Curve (AUC) From 5 Minutes Post-dose on Day 1 to 24 Hours Post-dose on Day 2

Spirometry was conducted according to internationally accepted standards. Standardized area under the curve (AUC0-24h) of FEV1 values taken at pre-dose to 24 hours post dose was calculated based on the trapezoidal rule. Analysis of Covariance was carried out with a mixed model that used (period) baseline, defined as the value of FEV1 measured prior to the first study drug intake in the period, as a covariate. (NCT00403754)
Timeframe: 5 minutes to 12 hours post-dose on Day 1; and 22 to 24 hours post-dose on Day 2

InterventionLiters (Least Squares Mean)
Indacaterol 600 µg2.35
Indacaterol 300 µg2.31
Indacaterol 150 µg2.26
Placebo2.04
Salmeterol 100 μg2.24

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) Standardized (With Respect to Time) Area Under the Curve (AUC) From 22 to 24 Hours Post-dose on Day 2

Spirometry was conducted according to internationally accepted standards. Standardized area under the curve (AUC22-24h) of FEV1 values taken at 22, 23 and 24 hours post dose, was calculated based on the trapezoidal rule. Analysis of Covariance was carried out with a mixed model that used (period) baseline, defined as the value of FEV1 measured prior to the first study drug intake in the period, as a covariate. (NCT00403754)
Timeframe: 22, 23, and 24 hours post-dose on Day 2

InterventionLiters (Least Squares Mean)
Indacaterol 600 µg2.31
Indacaterol 300 µg2.28
Indacaterol 150 µg2.24
Placebo2.06
Salmeterol 100 μg2.23

[back to top]

The Proportion of Symptom-free Days and Nights (Combined) Over the 12-week Treatment Period.

For each day of the evaluation period, symptoms were collected in the morning for the night's evaluation, and in the evening for the day's evaluation. Symptoms included coughing, wheezing, and difficulty breathing, each integer-scaled from 0=none to 3=severe. A symptom-free Day/Night is defined as a combined score of 0 across the morning and evening evaluations. The proportion of 0 scores across the Baseline period, and across the 12-week treatment period, is calculated to determine the overall proportion of symptom-free Days/Nights for each of these periods. (NCT00424008)
Timeframe: Baseline to Week 12

,
InterventionProportion of symptom-free days/nights (Least Squares Mean)
Baseline (over the last week prior to first dose)Actual proportion over the 12-wk treatment periodChange from Baseline to over the 12-wk tx period
F/SC DPI 250/50 mcg BID0.180.430.25
MF/F MDI 200/10 mcg BID0.190.420.24

[back to top]

The Area Under the Curve From 0 to 12 Hours [AUC](0-12 hr) of the Change From Baseline to the Week 12 Endpoint in Forced Expiratory Volume in One Second (FEV1)

(NCT00424008)
Timeframe: Baseline to Week 12

InterventionLiter x hour (Least Squares Mean)
MF/F MDI 200/10 mcg BID3.43
F/SC DPI 250/50 mcg BID3.24

[back to top]

Onset-of-action Based on Change From Baseline FEV1 at the 5 Min Pulmonary Function Test (PFT) Assessment on Day 1

PFTs, including FEV1, were done on Day 1. Evaluations included 30 min before and immediately before the first dose, the mean of which was Baseline, and at intervals from 5 min to 12 hrs postdose. Onset of action was defined as statistically significant improvement of MF/F over F/SC in Change from Baseline FEV1 at the 5-min postdose evaluation on Day 1. The same series of PFTs were done at Week 12. Change from Baseline to Week 12 evaluations were calculated using the same Day 1 predose scores for Baseline. The Week-12 evaluation consisted of AUC FEV1 scores across the 12-hour postdose interval. (NCT00424008)
Timeframe: Baseline to 5 minutes post-dose on Day 1

InterventionLiters (Least Squares Mean)
MF/F MDI 200/10 mcg BID0.20
F/SC DPI 250/50 mcg BID0.09

[back to top]

Change From Baseline in Asthma Control Questionnaire (ACQ) Total Score at Week 12 Endpoint

The Asthma Control Questionnaire (ACQ) by Juniper et al. is a mean of 7 equally weighted composite scores; each scaled from 0=best case scenario to 6=worst case scenario on an integer scale. Composites include the following: How Often Woken by Asthma, How Bad Were Asthma Symptoms When You Woke, Activity Limitations, Shortness of Breath, Wheezing, Average Daily Short-Acting Beta 2-Agonist (SABA) Puffs, and physician-evaluated lung function. With the exception of physician-evaluated lung function collected at the visit, evaluations were over the last week recall period. (NCT00424008)
Timeframe: Baseline to Week 12

InterventionScores on a scale (Least Squares Mean)
MF/F MDI 200/10 mcg BID-0.65
F/SC DPI 250/50 mcg BID-0.65

[back to top]

Geometric Mean Ratio for Baseline:Week12 24-hour Urinary Cortisol Excretion

A post-hoc analysis excluding participants with urine cortisol baseline values of >200 nmol/24 hrs. The data provided are a direct calculation of the Week 12 geometric mean divided by the baseline value, nanomoles per 24 hours (nmol/24 hrs) . (NCT00441441)
Timeframe: Baseline and Week 12

Interventionratio (Number)
Fluticasone Propionate/Salmeterol HFA0.77
Fluticasone Propionate HFA0.80

[back to top]

Geometric Mean Ratio for Week12:Baseline for 24-hour Urinary Cortisol Excretion

Normal range for Cortisol levels vary by age and gender. The data provided are a direct calculation of the Week 12 geometric mean divided by the baseline value, nanomoles per 24 hours (nmol/24 hrs). (NCT00441441)
Timeframe: Baseline and Week 12

Interventionratio (Number)
Fluticasone Propionate/Salmeterol HFA0.77
Fluticasone Propionate HFA0.75

[back to top]

Albuterol Use

Albuterol inhalation aerosol was used as a rescue or prophylactic and recorded daily by subject or caregiver. The number of puffs of albuterol over the previous 24 hour period prior to dosing was recorded. (NCT00441441)
Timeframe: Baseline and 12-Week Treatment Period

,
InterventionNumber of puffs per 24 hours (Mean)
Baseline - Mean number of puffsWeeks 1-12 - Mean number of puffsWeeks 1-12 - Mean change from baselineLast 7 Days on Treatment - Mean number of puffsLast 7 Days on Treat. - Mean change from baseline
Fluticasone Propionate HFA1.80.9-1.00.7-1.2
Fluticasone Propionate/Salmeterol HFA1.51.0-0.60.70.15

[back to top]

AM Peak Expiratory Flow

The peak expiratory flow (PEF) rate measures how fast a person can exhale air. It is used to compare to normal flow rates to predict obstruction and disease. The average PEF for a child or adolescent whose height is 43 inches is 147 Liters/minute (L/min), whose height is 66 inches is 454 L/min. Triplicate measurements taken for the best effort recorded. (NCT00441441)
Timeframe: Baseline and 12-Week Treatment Period

,
InterventionLiters/minute (L/min) (Mean)
Baseline - Mean AM PEFWeeks 1-12 - Mean AM PEFWeeks 1-12 - Mean Change from BaselineLast 7 Days on Treatment - Mean AM PEFLast 7 Days on Treatment-Mean Change from Baseline
Fluticasone Propionate HFA20322017.422623.3
Fluticasone Propionate/Salmeterol HFA21323320.223825.3

[back to top]

Asthma Exacerbations: Worsening of Asthma Requiring Emergency Intervention, Hospitalization, or Treatment With Asthma Medications Prohibited by the Protocols

The Primary Investigator determined the severity of the exacerbation based on the participant's clinical presentation and the investigator's understanding of the disease, the participant, and his or her clinical experiences. The severity of the exacerbation was not defined in the protocol. Mild: Usually treated at home. Prompt relief with inhaled short-acting beta2 agonist. Possible short course of oral systemic corticosteroids. Moderate: Usually requires office or emergency department visit. Relief with frequent inhaled short-acting beta2 agonist. Oral systemic corticosteroids; some symptoms last for 1-2 days after treatment begins. Severe: Usually requires emergency department visit and likely hospitalization. Partial relief with frequent inhaled short-acting beta2 agonist. Oral systemic corticosteroids; some symptoms last for more than 3 days after treatment begins. Adjunctive therapies are helpful. (NCT00441441)
Timeframe: Treatment period (weeks 1-12)

,
Interventionparticipants (Number)
Participants with any asthma exacerbationSeverity - MildSeverity - Moderate/SevereWithdrawal due to Asthma Exacerbation
Fluticasone Propionate HFA3212
Fluticasone Propionate/Salmeterol HFA1101

[back to top]

Asthma Symptom Scores

Each morning prior dosing or PEF, self-scored based on past 24 hours: 0=No symptoms, 1=Symptoms for one short period, 2=Symptoms for two or more short periods, 3=Frequent Symptoms which did not affect activities of daily living (ADL), 4=Frequent. (NCT00441441)
Timeframe: Baseline and 12-Week Treatment Period

,
InterventionScore in scale (Mean)
Baseline - Mean ScoreWeeks 1-12 - Mean ScoreWeeks 1-12 - Mean change from baselineLast 7 Days on Treatment - Mean ScoreLast 7 Days on Treat. - Mean change from baseline
Fluticasone Propionate HFA1.40.8-0.60.8-0.6
Fluticasone Propionate/Salmeterol HFA1.30.9-0.40.8-0.5

[back to top]

Cardiovascular Adverse Events Reported During the Post-Treatment Period

Cardiovascular Adverse Events, as categorized by the Medical Dictionary for Regulatory Activities (MeDRA), reported during Post-treatment period, defined as 1 day after last dose of study drug. The Adverse Events were identified in any ECG interpretation by a central reader (Cardiologist) for any ECG obtained after the first treatment dose and were then reported by the Primary Investigator as an Adverse Event. (NCT00441441)
Timeframe: 5 Days after Week 12

,
Interventionparticipants (Number)
Participants with Any EventECG QTc interval prolongedQT interval prolongedECG QT interval AbnormalDefect Conduction IntraventricularConduction disorderSinus TachycardiaSupraventricular Ectopics
Fluticasone Propionate HFA195207101
Fluticasone Propionate/Salmeterol HFA1911112110

[back to top]

Cardiovascular Adverse Events Reported During Treatment Period

Cardiovascular Adverse Events, as categorized by the Medical Dictionary for Regulatory Activities (MeDRA), reported during Treatment Period. The Adverse Events were identified in any ECG interpretation by a central reader (Cardiologist) for any ECG obtained after the first treatment dose and were then reported by the Primary Investigator as an Adverse Event. Please see the category titles for a list of candidate cardiovascular adverse events. (NCT00441441)
Timeframe: 12-Week Treatment Period

,
Interventionparticipants (Number)
Participants with Any EventElectrocardiogram (ECG) ChangeECG QTc Interval ProlongedECG AbnormalECG QT Borderline ProlongedDefect Conduction IntraventricularCardiac ArrhythmiaPremature Atrial Contraction
Fluticasone Propionate HFA1032110300
Fluticasone Propionate/Salmeterol HFA983211411

[back to top]

Clinic Morning (AM) Forced Expiratory Volume in Participants 6-11 Years

"FEV1 (Forced Expiratory Volume in 1 second) is the volume of air that can be forced out in one second, after taking a deep breath. FEV1 is measured using a spirometer and obtaining best effort from 3 to 8 measurements. Week 12 is the measure taken at Week 12." (NCT00441441)
Timeframe: Baseline and week 12

,
InterventionLiters per second (L/sec) (Mean)
Baseline - Mean FEV1Week 12 - Mean FEV1Week 12 - Mean Change from baselinePremature discontinuation - Mean FEV1Premature discontin. - Mean Change from baseline
Fluticasone Propionate HFA1.641.820.181.70-0.07
Fluticasone Propionate/Salmeterol HFA1.671.910.241.810.03

[back to top]

Clinically Significant Unfavorable ECGs at Week 12

Post-randomization ECGs categorized by the primary investigator as no change, significant change (favorable), significant change (unfavorable) from the ECG performed at Visit 1 (Baseline) are presented. Significant change (favorable) includes any ECG that improved from baseline, whereas significant change (unfavorable) includes any ECG that worsened from baseline. Clinical significance is determined by the primary investigator. (NCT00441441)
Timeframe: Baseline, Week 12

,
Interventionparticipants (Number)
Clinically significant unfavorable changeAEs Reported for ECG findingsClinically significant unfavorable ECGs repeatedRepeated ECGs w/ no change or insignificant change
Fluticasone Propionate HFA1818115
Fluticasone Propionate/Salmeterol HFA2422116

[back to top]

ECG Measures - Heart Rate

The range of heart rates for this study was between 49-144 beats per minute (NCT00441441)
Timeframe: Baseline and Week 12

,
Interventionbeats per minute (Mean)
Mean Heart Rate - BaselineMean Heart Rate - Week 12Mean Heart Rate - Premature Discontinuation
Fluticasone Propionate HFA82.681.992.4
Fluticasone Propionate/Salmeterol HFA8485.573.1

[back to top]

ECG Measures - QT Interval

Fridericia's formula QTc interval=QT interval/cubed root of the R-R interval. The Bazett's formula QTc=QT/squared root of the R-R interval. (NCT00441441)
Timeframe: Baseline and Week 12

,
Interventionmilliseconds (Mean)
Mean QTc Interval (Fridericia)- BaselineMean QTc Interval (Fridericia) - Week 12Premature Discontinuation (Fridericia)Mean QTc Interval (Bazett) - BaselineMean QTc Interval (Bazett) - Week 12Premature Discontinuation (Bazett)
Fluticasone Propionate HFA390.8393.6394.8411.4413.7422.7
Fluticasone Propionate/Salmeterol HFA394.5397.5392416.3420.8403.3

[back to top]

Geometric Mean Values of 24 Hour Urinary Cortisol Excretion by Spacer Use at Baseline and Week 12

AeroChamber Plus spacers were provided for participants who demonstrated the inability to coordinate the use of an Meter Dose Inhaler at Visit 1. AeroChamber Plus spacer delivers 22% more medication than the original AeroChamber and is available in three mask sizes and without a mask. Geometric mean is the product of the values taken to the Nth root, where N is the number of values in the set of values. (NCT00441441)
Timeframe: Baseline and Week 12

,,,
InterventionNanomoles per 24 hours (nmol/24 hrs) (Geometric Mean)
Baseline - Geometric MeanWeek 12 - Geometric Mean
Fluticasone Propionate HFA - No Spacer31.8923.06
Fluticasone Propionate HFA - Spacer30.6123.20
Fluticasone Propionate/Salmeterol HFA - No Spacer35.8432.05
Fluticasone Propionate/Salmeterol HFA - Spacer31.8923.37

[back to top]

Geometric Mean Values of 24-hour Urinary Cortisol Excretion at Baseline and Week 12

A post-hoc analysis excluding participants with urine cortisol baseline values of >200 nanomoles/24 hours. Geometric mean is the product of the values taken to the Nth root, where N is the number of values in the set of values. (NCT00441441)
Timeframe: Baseline and Week 12

,
InterventionNanamoles per 24 hours (nmol/24 hrs) (Geometric Mean)
Baseline - Geometric MeanWeek 12 - Geometric Mean
Fluticasone Propionate HFA28.3922.80
Fluticasone Propionate/Salmeterol HFA32.7125.03

[back to top]

Geometric Mean Values of 24-hour Urinary Cortisol Excretion at Baseline and Week 12

Normal range for Cortisol levels vary by age and gender. Geometric mean is the product of the values taken to the Nth root, where N is the number of values in the set of values. (NCT00441441)
Timeframe: Baseline and Week 12

,
InterventionNanomoles per 24 hours (nmol/24 hrs) (Geometric Mean)
Baseline - Geometric MeanWeek 12 - Geometric Mean
Fluticasone Propionate HFA30.8823.17
Fluticasone Propionate/Salmeterol HFA32.7125.03

[back to top]

Geometric Mean Values of 24-hour Urinary Cortisol Excretion by Spacer Use Excluding Participants With Abnormal Urinary Cortisol Excretion Values at Baseline From the Cortisol Population at Baseline and Week 12

AeroChamber Plus spacers were provided for participants who demonstrated the inability to coordinate the use of an Meter Dose Inhaler at Visit 1. AeroChamber Plus spacer delivers 22% more medication than the original AeroChamber and is available in three mask sizes and without a mask. Geometric mean is the product of the values taken to the Nth root, where N is the number of values in the set of values. (NCT00441441)
Timeframe: Baseline and Week 12

,
InterventionNanomoles per 24 hr (nmoles/24 hr) (Geometric Mean)
Baseline - Geometric MeanWeek 12 - Geometric Mean
No Spacer31.8827.85
Spacer27.0822.38

[back to top]

Investigator Evaluations of Electrocardiogram (ECG) Results

ECGs were transmitted to an independent cardiologist who was responsible for providing interpretation of the ECG as either normal or abnormal (based on personal assessment). The investigator was then responsible for determining the clinical significance of the abnormal ECG in the context of the participants' history and clinical presentation. An abnormal, clinically significant ECG included, but was not limited to: prolonged QT interval, ischemic changes, ventricular hypertrophy, intraventricular conduction abnormalities, and clinically significant arrhythmias. PD, premature discontinuation. (NCT00441441)
Timeframe: Baseline and Week 12

,
Interventionparticipants (Number)
Baseline - NormalBaseline - Abnormal: Not Clinically SignificantBaseline - Abnormal: Clinically SignificantWeek 12-No Change or insignificant ChangeWeek 12-Clinically Significant Change-FavorableWeek 12-Clinically Significant Change-UnfavorablePD-No Change or insignificant ChangePD-Clinically Significant Change-FavorablePD-Clinically Significant Change-Unfavorable
Fluticasone Propionate HFA155210142018911
Fluticasone Propionate/Salmeterol HFA145271136224700

[back to top]

Number of Participants With the Indicated Levels of 24 Hour Urinary Cortisol Excretion by Spacer Use

"AeroChamber Plus spacers were provided for participants who demonstrated the inability to coordinate the use of an Meter Dose Inhaler at Visit 1. AeroChamber Plus spacer delivers 22% more medication than the original AeroChamber and is available in three mask sizes and without a mask. Abnormal high cortisol excretion and Abnormal low cortisol excretion are defined as above the upper limit of normal and below the lower limit of normal, respectively. An abnormality is defined as a value of 24-hour urinary cortisol excretion that is outside the normal range. The normal range for 24-hour urinary cortisol excretion was provided by the central laboratory." (NCT00441441)
Timeframe: Baseline and Week 12

,,,
Interventionparticipants (Number)
Baseline - Abnormal high cortisol excretionBaseline - Abnormal low cortisol excretionWeek 12 - Abnormal high cortisol excretionWeek 12 - Abnormal low cortisol excretion
Fluticasone Propionate HFA - No Spacer3010
Fluticasone Propionate HFA - Spacer14070
Fluticasone Propionate/Salmeterol HFA - No Spacer1130
Fluticasone Propionate/Salmeterol HFA - Spacer120102

[back to top]

Number of Participants With the Indicated Levels of 24-hour Urinary Cortisol Excretion

"Abnormal high cortisol excretion and Abnormal low cortisol excretion are defined as above the upper limit of normal and below the lower limit of normal, respectively. The normal range for cortisol levels vary by age and gender. An abnormality is defined as a value of 24-hour urinary cortisol excretion that is outside the normal range. The normal range for 24-hour urinary cortisol excretion was provided by the central laboratory." (NCT00441441)
Timeframe: Baseline and week 12

,
Interventionparticipants (Number)
Baseline - Abnormal high cortisol excretion, nBaseline - Abnormal low cortisol excretion, nWeek 12 - Abnormal high cortisol excretion, nWeek 12 - Abnormal low cortisol excretion, n
Fluticasone Propionate HFA17080
Fluticasone Propionate/Salmeterol HFA131132

[back to top]

Percent of Albuterol-free Days

Percentage of days when Albuterol use was unnecessary based on daily record and symptom free days. (NCT00441441)
Timeframe: Baseline and 12-Week Treatment Period

,
InterventionPercentage of days (Mean)
Baseline - Mean percent rescue freeWeeks 1-12 - Mean percent rescue freeWeeks 1-12 - Mean change from baselineLast 7 Days on Treat. - Mean percent rescue freeLast 7 Days on Treat. - Mean change from baseline
Fluticasone Propionate HFA42.570.028.375.832.8
Fluticasone Propionate/Salmeterol HFA43.767.123.675.430.4

[back to top]

Percentage of Symptom Free Days

Percentage of number of days without asthma symptoms based on Asthma Symptom Scores. Each morning prior to dosing or PEF, asthma symptoms were self-scored based on the past 24 hours: 0=no symptoms, 1=symptoms for one short period, 2=symptoms for two or more short periods, 3=frequent symptoms that did not affect activities of daily living (ADL), 4=frequent . (NCT00441441)
Timeframe: Baseline and 12-Week Treatment Period

,
InterventionPercentage of days (Mean)
Baseline - Mean PercentWeeks 1-12 - Mean PercentWeeks 1-12 - Mean change from baselineLast 7 Days on Treatment - Mean PercentLast 7 Days on Treat. - Mean change from baseline
Fluticasone Propionate HFA18.448.730.553.434.9
Fluticasone Propionate/Salmeterol HFA20.046.726.851.932.1

[back to top] [back to top]

Geometric Mean Ratio for Week12: Baseline for 24 Hour Urinary Cortisol Excretion by Spacer Use

AeroChamber Plus spacers were provided for participants who demonstrated the inability to coordinate the use of an Meter Dose Inhaler at Visit 1. AeroChamber Plus spacer delivers 22% more medication than the original AeroChamber and is available in three mask sizes and without a mask. The data provided are a direct calculation of the Week 12 geometric mean divided by the baseline value, nanomoles per 24 hours (nmol/24 hrs). (NCT00441441)
Timeframe: Baseline and Week 12

Interventionratio (Number)
Fluticasone Propionate/Salmeterol HFA - Spacer0.73
Fluticasone Propionate/Salmeterol HFA - No Spacer0.89
Fluticasone Propionate HFA - Spacer0.76
Fluticasone Propionate HFA - No Spacer0.72

[back to top]

Geometric Mean Ratio for Baseline: Week 12 24-hour Urinary Cortisol Excretion by Spacer Use Excluding Participants With Abnormal Urinary Cortisol Excretion Values at Baseline From the Cortisol Population

AeroChamber Plus spacers were provided for participants who demonstrated the inability to coordinate the use of an Meter Dose Inhaler at Visit 1. AeroChamber Plus spacer delivers 22% more medication than the original AeroChamber and is available in three mask sizes and without a mask. The data provided are a direct calculation of the Week 12 geometric mean divided by the baseline value,nanomoles per 24 hours (nmol/24 hrs) . (NCT00441441)
Timeframe: Baseline and Week 12

Interventionratio (Number)
Spacer0.87
No Spacer0.83

[back to top]

Percentage of Subjects With Symptom-Free Nights & Days

Percentage of subjects with Symptom Free Nights & Days after 4 weeks of Treatment (NCT00448435)
Timeframe: Crossover Period Week 1-4, 7-10

,
InterventionPercent of participants (Number)
BaselineAfter 4 Weeks of Treatment
SFC 50/100 Mcg/Day72.991.7
SLM 50 Mcg + FP 100 Mcg/Day81.381.3

[back to top]

Percentage of Subjects With Symptom-Free Nights & Days After 20 Weeks of Treatment

Percentage of subjects with Symptom Free Nights & Days after 20 weeks of Treatment (at week 30). (NCT00448435)
Timeframe: Extension Period Weeks 11-30

InterventionPercentage of participants (Number)
BaselineAfter 20 weeks of treatment (at week 30)
SFC 50/100 Mcg/Day84.084.8

[back to top]

Adjusted Mean Change From Baseline in Evening PEF During the 20-week Extension Treatment Period

Mean change from baseline = value at assessment period (mean of the values obtained at assessment period [Weeks 11-30]) minus baseline value. Baseline: Mean of the daily values over the last 7 days prior to the day of starting the Extension period (Weeks 11-30). (NCT00448435)
Timeframe: Extension Period weeks 11-30

InterventionL/Min (Mean)
SFC 50/100 Mcg/Day2.7

[back to top]

Adjusted Mean Change From Baseline in Morning PEF (Peak Expiratory Flow) During the 4-week Treatment Periods

Mean change from baseline = value at each assessment period (mean of the values obtained at each assessment period [Weeks 1-4/Weeks 7-10]) minus baseline value. Baseline: Mean of the daily values over the last 7 days of the 2-week run-in/wash-out (i.e., the last 7 days prior to the day of starting treatment period [Weeks 1-4/Weeks 7-10]). (NCT00448435)
Timeframe: Crossover Period Weeks 1-4, and 7-10

InterventionLiters/minute (Mean)
SFC 50/100 Mcg/Day14.3
SLM 50 Mcg + FP 100 Mcg/Day17.1

[back to top]

Adjusted Mean Change From Baseline in Evening PEF During the 4-week Treatment Periods

Mean change from baseline = value at each assessment period (mean of the values obtained at each assessment period [Weeks 1-4/Weeks 7-10]) minus baseline value. Baseline: Mean of the daily values over the last 7 days of the 2-week run-in/wash-out. (NCT00448435)
Timeframe: Crossover Period weeks 1-4, 7-10

InterventionL/min (Mean)
SFC 50/100 Mcg/Day16.3
SLM 50 Mcg + FP 100 Mcg/Day15.8

[back to top]

Adjusted Mean Change From Baseline in Morning PEF During the 20-week Extension Treatment Period

Mean change from baseline = value at assessment period (mean of the values obtained at assessment period (Weeks 11-30).) minus baseline value. Baseline: Mean of the daily values over the last 7 days prior to the day of starting of the Extension period (Weeks 11-30). (NCT00448435)
Timeframe: Extension Period Weeks 11-30

InterventionL/min (Mean)
SFC 50/100 Mcg/Day3.0

[back to top]

Adjusted Mean Change From Baseline in Percent Personal Best Morning PEF(%) During the 20-week Extension Treatment Period

Mean change from baseline = value at assessment period (mean of the values obtained at assessment period [Weeks 11-30]) minus baseline value. Baseline: Mean of the daily values over the last 7 days prior to the day of starting the Extension period (Weeks 11-30). (NCT00448435)
Timeframe: Extension Period weeks 11-30

InterventionPercentage of personal best value (Mean)
SFC 50/100 Mcg/Day1.29

[back to top]

Adjusted Mean Change From Baseline in Percent Personal Best Morning PEF(%) During the 4-week Treatment Periods

Mean change from baseline = value at each assessment period (mean of the values obtained at each assessment period [Weeks 1-4/Weeks 7-10]) minus baseline value. Baseline: Mean of the daily values over the last 7 days of the 2-week run-in/wash-out. (NCT00448435)
Timeframe: Crossover Period weeks 1-4, 7-10

InterventionPercentage of personal best value (Mean)
SFC 50/100 Mcg/Day5.01
SLM 50mcg + FP 100 Mcg/Day6.46

[back to top]

Adjusted Mean Change From Baseline in Percent Predicted Morning PEF(%) During the 20-Week Extension Treatment Period

Mean change from baseline = value at assessment period (mean of the values obtained at assessment period [Weeks 11-30]) minus baseline value. Baseline: Mean of the daily values over the last 7 days prior to the day of starting the Extension period (Weeks 11-30). (NCT00448435)
Timeframe: Extension Period weeks 11-30

InterventionPercentage of predicted value (Mean)
SFC 50/100 Mcg/Day1.46

[back to top]

Adjusted Mean Change From Baseline in Percent Predicted Morning PEF(%) During the 4-week Treatment Periods

Mean change from baseline = value at each assessment period (mean of the values obtained at each assessment period [Weeks 1-4/Weeks 7-10]) minus baseline value. Baseline: Mean of the daily values over the last 7 days of the 2-week run-in/wash-out. (NCT00448435)
Timeframe: Crossover Period Weeks 1-4, 7-10

InterventionPercentage of predicted value (Mean)
SFC 50/100 Mcg/Day5.38
SLM 50 Mcg + FP 100 Mcg/Day6.73

[back to top]

Adjusted Mean Change From Baseline of Circadian Variation in Morning PEF(%) During the 4-week Treatment Periods

Mean change from baseline = value at each assessment period (mean of the values obtained at each assessment period [Weeks 1-4/Weeks 7-10]) minus baseline value. Baseline: Mean of the daily values over the last 7 days of the 2-week run-in/wash-out. (NCT00448435)
Timeframe: Crossover Period Weeks 1-4, 7-10

InterventionPercentage of circadian variation (Mean)
SFC 50/100 Mcg/Day0.06
SLM 50 Mcg + FP 100 Mcg/Day-0.08

[back to top]

Adjusted Mean Change From Baseline of Circadian Variation in PEF(%) During the 20-Week Extension Treatment Period

Mean change from baseline = value at assessment period (mean of the values obtained at assessment period [Weeks 11-30]) minus baseline value. Baseline: Mean of the daily values over the last 7 days prior to the day of starting the Extension period (Weeks 11-30). (NCT00448435)
Timeframe: Extension Period weeks 11-30

InterventionPercentage of circadian variation (Mean)
SFC 50/100 Mcg/Day-0.37

[back to top]

Percentage of Subjects With Rescue Medication-Free Nights & Days After 20 Weeks of Treatment

Percentage of subjects with Rescue Medication Free Nights & Days after 20 weeks of Treatment (at week 30). (NCT00448435)
Timeframe: Extension Period Weeks 11-30

InterventionPercentage of participants (Number)
BaselineAfter 20 weeks of treatment (at week 30)
SFC 50/100 Mcg/Day90.089.1

[back to top]

Percentage of Subjects With Rescue Medication-Free Nights and Days

Percentage of subjects with Rescue Medication Free Nights & Days after 4 weeks of Treatment (NCT00448435)
Timeframe: Crossover Period Weeks 1-4, 7-10

,
InterventionPercentage of participants (Number)
BaselineAfter 4 Weeks of Treatment
SFC 50/100 Mcg/Day87.593.8
SLM 50 Mcg + FP 100 Mcg/Day87.587.5

[back to top]

Change From Baseline in Morning Peak Expiratory Flow (PEF) During Weeks 1-24

"PEF taken daily and average used for week 1-24 value. The peak expiratory flow rate measures how fast a person can (exhale) air. Then, compares it to normal flow rates to predict obstruction and disease. The average PEF for a child or adolescent whose height is 43 is 147 L/min, whose height is 66 is 454 L/min." (NCT00449046)
Timeframe: Baseline and during Weeks 1-24

InterventionL/min (Mean)
Salmeterol/Fluticasone Propionate32.9

[back to top]

Change From Baseline in Circadian Variation in Peak Expiratory Flow (PEF) During Weeks 1-24

"Circadian Variation means the various changes in a day. The peak expiratory flow rate measures how fast a person can (exhale) air using a mini-Wright peak flow meter. The average PEF for a child or adolescent whose height is 43 is 147 L/min, whose height is 66 is 454 L/min." (NCT00449046)
Timeframe: Baseline and during Weeks 1-24

InterventionPercent Change (Mean)
Salmeterol/Fluticasone Propionate-1.62

[back to top]

Change From Baseline in Evening Peak Expiratory Flow (PEF) During Weeks 1-24

"The peak expiratory flow rate measures how fast a person can (exhale) air. Then compares it to normal flow rates to predict obstruction and disease. The average PEF for a child or adolescent whose height is 43 is 147 L/min, whose height is 66 is 454 L/min." (NCT00449046)
Timeframe: Baseline and during Weeks 1-24

InterventionL/min (Mean)
Salmeterol/Fluticasone Propionate31.2

[back to top]

Number of Participants With Symptom-Free Nights and Days

(NCT00449046)
Timeframe: Baseline and Week 24

InterventionParticipants (Number)
BaselineWeek 24
Salmeterol/Fluticasone Propionate2931

[back to top]

Number of Participants With Rescue Medication-Free Nights and Days

Rescue free means without the use of other medication. (NCT00449046)
Timeframe: Baseline and Week 24

InterventionParticipants (Number)
BaselineWeek 24
Salmeterol/Fluticasone Propionate3332

[back to top]

Change From Baseline in Percent Predicted Morning Peak Expiratory Flow (PEF) During Weeks 1-24

Percent Predicted Morning Peak Expiratory flow were the percent of patients that were predicted to have their Peak expiratory flow in the morning. (NCT00449046)
Timeframe: Baseline and during Weeks 1-24

InterventionPercent Change (Mean)
Salmeterol/Fluticasone Propionate12.50

[back to top]

Most Frequent Adverse Events - On Therapy

Adverse events, Clinical laboratory tests, Adrenocortical function test, Physical examinations, 12-lead electrocardiogram (ECG), Oropharyngeal examination were included. (NCT00449046)
Timeframe: Baseline to Week 24

InterventionParticipants (Number)
LaryngopharyngitisBronchitisNasopharyngitisAsthmaPharyngitisPyrexiaOtitis mediaPharyngotonsillitisLaryngotracheo bronchitisMolluscum contagiosumStomatitis
Salmeterol/Fluticasone Propionate88886543333

[back to top]

Serious Adverse Events (SAEs) - On Therapy

"Number of participants considered by the investigator to be related to study medication.~Adverse events, Clinical laboratory tests, Adrenocortical function test, Physical examinations, 12-lead ECG, Oropharyngeal examination were included. Frequency threshold of reported SAE's is 0%(100% reported)" (NCT00449046)
Timeframe: Baseline to Week 24

InterventionParticipants (Number)
Salmeterol/Fluticasone Propionate1

[back to top]

Rate of Asthma Attacks Per Participant Per Year

The rate of asthma attacks was defined as the mean number of attacks per participant per year. An asthma attack was defined as a >=20% decrease in AM PEF, a >=70% increase in albuterol use, or the occurrence of an asthma exacerbation requiring oral steroids or hospitalization. (NCT00452348)
Timeframe: Week 1 through Week 52

Interventionattacks per participant per year (Mean)
FSC DISKUS 250/50 mcg BID2.63
FP DISKUS 250 mcg BID for 52 Weeks2.73

[back to top]

Mean Change From Baseline in AM PEF Over Weeks 1-52

Morning (AM) peak expiratory flow (PEF) is defined as the maximum volume of air exhaled in liters per minute. Change from baseline was calculated as the average of the Week 1 through Week 52 values minus the baseline value. (NCT00452348)
Timeframe: Baseline and Week 1 through Week 52

InterventionLiters/minute (L/min) (Mean)
FSC DISKUS 250/50 mcg BID27.7
FP DISKUS 250 mcg BID for 52 Weeks14.6

[back to top]

Mean Change From Baseline in Pre-dose FEV1 Over Weeks 1-52

Pulmonary function was measured by forced expiratory volume in one second (FEV1), which is the volume of air exhaled from the lungs in one second. Change from baseline was calculated as the average of the Week 1 through Week 52 values minus the baseline value. (NCT00452348)
Timeframe: Baseline and Week 1 through Week 52

InterventionLiters (Mean)
FSC DISKUS 250/50 mcg BID0.16
FP DISKUS 250 mcg BID for 52 Weeks0.12

[back to top]

Mean Change From Baseline in the Percentage of Symptom-free Days Over Weeks 1-52

A symptom-free day was defined as a day without asthma symptoms, as measured via the daily asthma symptom score (measuring symptoms during the day and previous night) on a 6-point scale (ranging from 0 to 5). A symptom score of 0=no symptoms, 1=symptoms for one short period, 2=symptoms for two or more short periods, 3=symptoms that did not affect normal daily activities, 4=symptoms that did affect normal daily activities, 5=symptoms so severe that daily activities could not be performed. Change from baseline was calculated as the average of the Week 1-Week 52 values minus the baseline value. (NCT00452348)
Timeframe: Baseline and Week 1 through Week 52

InterventionPercentage of symptom-free days (Mean)
FSC DISKUS 250/50 mcg BID37.4
FP DISKUS 250 mcg BID for 52 Weeks28.9

[back to top]

Mean Change From Baseline in the Percentage of Symptom-free Days Over Weeks 1-52

A symptom-free day was defined as a day without asthma symptoms, as measured via the daily asthma symptom score (measuring symptoms during the day and previous night) on a 6-point scale (ranging from 0 to 5). A symptom score of 0=no symptoms, 1=symptoms for one short period, 2=symptoms for two or more short periods, 3=symptoms that did not affect normal daily activities, 4=symptoms that did affect normal daily activities, 5=symptoms so severe that daily activities could not be performed. Change from baseline was calculated as the average of the Week 1-Week 52 values minus the baseline value. (NCT00452699)
Timeframe: Baseline and Week 1 through Week 52

InterventionPercentage of symptom-free days (Mean)
FSC DISKUS 250/50 mcg BID for 52 Weeks37.1
FP DISKUS 250 mcg BID for 52 Weeks28.5

[back to top]

Mean Change From Baseline in AM PEF Over Weeks 1-52

Morning (AM) peak expiratory flow (PEF) is defined as the maximum volume of air exhaled in liters per minute. Change from baseline was calculated as the average of the Week 1 through Week 52 values minus the baseline value. (NCT00452699)
Timeframe: Baseline and Week 1 through Week 52

InterventionLiters/minute (L/min) (Mean)
FSC DISKUS 250/50 mcg BID for 52 Weeks23.6
FP DISKUS 250 mcg BID for 52 Weeks9.8

[back to top]

Rate of Asthma Attacks Per Participant Per Year

The rate of asthma attacks was defined as the mean number of attacks per participant per year. An asthma attack was defined as a 20% decrease in AM PEF, a 70% increase in albuterol use, or the occurrence of an asthma exacerbation requiring oral steroids or hospitalization. (NCT00452699)
Timeframe: Week 1 through Week 52

Interventionattacks per participant per year (Mean)
FSC DISKUS 250/50 mcg BID for 52 Weeks1.87
FP DISKUS 250 mcg BID for 52 Weeks2.14

[back to top]

Mean Change From Baseline in Pre-dose FEV1 Over Weeks 1-52

Pulmonary function was measured by forced expiratory volume in one second (FEV1), which is the volume of air exhaled from the lungs in one second. Change from baseline was calculated as the average of the Week 1 through Week 52 values minus the baseline value. (NCT00452699)
Timeframe: Baseline and Week 1 through Week 52

InterventionLiters (Mean)
FSC DISKUS 250/50 mcg BID for 52 Weeks0.20
FP DISKUS 250 mcg BID for 52 Weeks0.09

[back to top]

Change From Baseline in Pre-dose FEV1 (Forced Expiratory Volume in One Second) Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)

FEV1 is the amount of air (in liters) you can blow out within one second. A spirometer is the device used to measure FEV1. With normal lungs and airways you can normally blow out most of the air from your lungs within one second. Age, height and gender is used to determine what is normal. Change from baseline could have been measured at any time during the study (up to Week 12), using the LOCF. In the LOCF approach, for each individual, missing values are replaced by the last observed value of that variable. (NCT00461500)
Timeframe: Baseline through Week 12

InterventionLiters (Mean)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined0.25
FP 100: Fluticasone Propionate0.11

[back to top]

Number of Participants With at Least One Exacerbation During 12-Week Treatment Period

Subjects will record exacerbations (defined as temporary PEF decrease, increase in salbutamol use) in a Daily Record Card (DRC). The number of events are categorized as those that showed a deterioration in asthma requiring administration of oral corticosteroids and/or a deterioration in asthma requiring emergency room visit and/or hospitalization (hosp.). (NCT00461500)
Timeframe: 12-Week Treatment Period (Week 1 through Week 12)

,
InterventionParticipants (Number)
Any exacerbation (Exac.)Exac. needing oral corticosteroids and/or hosp.
FP 100: Fluticasone Propionate50
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined10

[back to top]

Number of Participants Who Achieved Well-Controlled Asthma During Weeks 5-12

"Well-controlled asthma is defined as 2 or more of the following: symptoms on no more than 2 days with symptom score of >1; no more than 2 days of rescue meds (maximum of 4 per week); >=80% predicted morning PEF. And no night time awakenings, exacerbations, emergency room visits, and treatment related adverse effects requiring a change to therapy. The number of participants who achieved well-controlled asthma at any time during Week 5-12 of the study period will be summarized by treatment groups. The difference between treatment groups will be assessed using logistic regression." (NCT00461500)
Timeframe: Weeks 5 -12

,
InterventionParticipants (Number)
YesNo
FP 100: Fluticasone Propionate1124
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined1316

[back to top]

Number of Participants Who Achieved Total-controlled Asthma During Weeks 5-12

"Totally-controlled asthma is defined as no daily symptoms, no night-time awakenings, no exacerbations, no rescue medication, no emergency visits, no treatment related adverse events resulting in change in asthma therapy, >=80% predicted PEF. The number of subjects who achieved total-controlled asthma at any time during Week 5-12 of the study period will be summarized by treatment groups. The difference between treatment groups will be assessed using logistic regression." (NCT00461500)
Timeframe: Weeks 5 - 12

,
InterventionParticipants (Number)
YesNo
FP 100: Fluticasone Propionate135
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined128

[back to top]

ACT Score in Classes at Week 12

Score is ranged from 5 (poor control) to 25 (complete control). (NCT00461500)
Timeframe: Week 12

,
InterventionParticpants (Number)
< 15 score15-19 score>=20 score
FP 100: Fluticasone Propionate21525
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined51216

[back to top]

Median Number of Weeks to First Achieve Well-Controlled Asthma During Weeks 5-12

"Well-controlled asthma is defined as 2 or more of the following: symptoms on no more than 2 days with symptom score of >1; no more than 2 days of rescue meds (maximum of 4 per week); >=80% predicted morning PEF. And no night time awakenings, exacerbations, emergency room visits, and treatment related adverse effects requiring a change to therapy. The median number of weeks to first achieve well-controlled asthma during Week 5-12 of the study period will be summarized by treatment groups. The difference between treatment groups will be assessed using logistic regression." (NCT00461500)
Timeframe: Weeks 5 - 12

InterventionWeeks (Median)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined3.1
FP 100: Fluticasone Propionate4.1

[back to top]

Change From Baseline in Pre-dose Forced Expiratory Vital Capacity (FVC) Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)

FVC is the total amount of air that can forcibly be blown out after full inspiration, measured in liters. A spirometer is the device used to measure FVC. Age, height and gender is used to determine what is normal. Change from baseline could have been measured at any time during the study (up to Week 12), using the LOCF. In the LOCF approach, for each individual, missing values are replaced by the last observed value of that variable. (NCT00461500)
Timeframe: Baseline through Week 12

InterventionLiters (Mean)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined0.18
FP 100: Fluticasone Propionate0.14

[back to top]

Change From Baseline in Pre-dose (Percent Predicted) FEV1 Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)

Percent predicted is based on tables of normal values that use variables such as age, gender, and weight as a method of standardization. Spirometry results are expressed as a percentage, and are generally considered abnormal if less than 80 percent of the normal predicted value. Change from baseline could have been measured at any time during the study (up to Week 12), using the LOCF. In the LOCF approach, for each individual, missing values are replaced by the last observed value of that variable. (NCT00461500)
Timeframe: Baseline through Week 12

InterventionPercentage predicted of FEV1 (Mean)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined7.46
FP 100: Fluticasone Propionate4.97

[back to top]

Change From Baseline in Overall Asthma Quality of Life Questionnaire (AQLQ) Score at Week 12

7-point scale where 1=total impairment and 7=no impairment. Questions contain 32 items in four domains. Domains include Activity Limitation (11 items), Symptoms (12 items), Emotional Function (5 items), and Environmental Stimuli (4 items). 32 items produce one overall quality of life score. The 7 points scoring are different and depend on the item : they are the translation in French of the original questionnaire from Juniper. Possible AQLQ scores range from 1 to 7 (the mean of all the questions). (NCT00461500)
Timeframe: Baseline, Week 12

InterventionScore on a scale (Mean)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined0.99
FP 100: Fluticasone Propionate1.11

[back to top]

Change From Baseline in Asthma Control Test (ACT) Score at Week 12

5 question test with various responses rating frequency of asthma events over 4-week period. Questions include occurrence of asthma affecting work/school; causing shortness of breath; symptoms (wheezing, coughing, shortness of breath, chest tightness, pain) wake you up at night; causing need for rescue medication; asthma control. Scale: 1=all of time, 2=most of time, 3=some of the time, 4=a little of the time, 5=none of the time. Possible ACT scores range from 5 to 25. (NCT00461500)
Timeframe: Baseline, Week 12

InterventionScore on a scale (Mean)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined5.64
FP 100: Fluticasone Propionate5.90

[back to top]

Change From Baseline (BL) in Pre-dose FEF 25-75% (Forced Expiratory Flow) Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)

Forced Expiratory Flow 25-75% (measured by a spirometer) is the average flow (or speed) of air coming out of the lung during the middle portion of the expiration. Age, height, and gender is used to determine what is normal. Change from BL could have been measured at any time during the study (up to Week 12), using the LOCF (for each individual, missing values are replaced by the last observed value of that variable). Change from BL is measured as percentage of predicted value, with height, gender, age, and race as variables (percentage of predicted value at endpoint minus value at BL). (NCT00461500)
Timeframe: Baseline through Week 12

InterventionPercentage of predicted value (Mean)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined7.24
FP 100: Fluticasone Propionate4.28

[back to top]

Change From Baseline in Mean Morning Peak Expiratory Flow (PEF) Over Weeks 5-12

Mini Wright Peak Flow Meter used to allow patients to monitor their asthma - Peak Flow (or PEF - peak expiratory flow) is a measurement of how fast you can blow out. When someone is well, their PEF is higher - when the airways are narrow (as in asthma), PEF is lower. Readings based on age, height and gender. (NCT00461500)
Timeframe: Baseline, Weeks 5-12

InterventionLiters per minute (L/min) (Mean)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined59.21
FP 100: Fluticasone Propionate50.98

[back to top]

Change From Baseline in FEV1 Reversibility Through Week 12 (Using Last Observation Carried Forward [LOCF] Approach)

Reversibility is calculated as the percentage improvement of FEV1 from baseline. Change from baseline could have been measured at any time during the study (up to Week 12), using the LOCF. In the LOCF approach, for each individual, missing values are replaced by the last observed value of that variable. Percent reversibility of FEV1 was calculated as follows: (Post-bronchodilator FEV1 - pre-bronchodilator FEV1)/pre-bronchodilator FEV1 x 100. A negative difference indicates less reversibility. (NCT00461500)
Timeframe: Baseline through Week 12

InterventionPercent change (Mean)
SFC 100: Salmeterol Xinafoate/Fluticasone Propionate Combined-9.46
FP 100: Fluticasone Propionate-4.05

[back to top]

Absolute Change in Morning Peak Flow

Absolute change in morning peak flow at the end of the 16-week study period compared with baseline (last two weeks of run-in). Peak flow measurement is a test to measure air flowing out of the lung. (NCT00521222)
Timeframe: Up to 16 weeks from baseline

InterventionL/min (Mean)
Arg/Arg Genotype on Advair (Fluticasone With Salmeterol) HFA-15.7
Gly/Gly Genotype on Advair (Fluticasone With Salmeterol) HFA8.4
Arg/Arg Genotype on Fluticasone HFA-5.6
Gly/Gly Genotype on Fluticasone HFA-14.4

[back to top]

Change in Asthma Symptom Score

Asthma symptom score measures asthma symptoms on a scale from 0 to 3. 0 = No asthma symptoms; 1 = 1-3 asthma episodes each lasting 2 hours or less, all mild; 2= 4 or more asthma episodes that interfered with activity, play, school, or sleep for less than 2 hours; 3= 1 or more asthma episodes lasting longer than 2 hours, or resulting in shortening normal activity, or seeing a doctor, or going to a hospital. A higher score indicates a worse outcome. (NCT00521222)
Timeframe: Up to 16 weeks from baseline

Interventionscore on a scale (Mean)
Arg/Arg Genotype on Advair (Fluticasone With Salmeterol) HFA0.3
Gly/Gly Genotype on Advair (Fluticasone With Salmeterol) HFA-1.2
Arg/Arg Genotype on Fluticasone HFA0.4
Gly/Gly Genotype on Fluticasone HFA0.5

[back to top]

Change in Forced Expiratory Volume in 1 Second (FEV1) Percent Predicted Pre-Bronchodilator

Change in Forced Expiratory Volume in 1 Second (FEV1) Percent Predicted Pre-Bronchodilator as measured by spirometry (NCT00521222)
Timeframe: Up to 16 weeks from baseline

InterventionPercent Predicted (Mean)
Arg/Arg Genotype on Advair (Fluticasone With Salmeterol) HFA-1.0
Gly/Gly Genotype on Advair (Fluticasone With Salmeterol) HFA-2.5
Arg/Arg Genotype on Fluticasone HFA-3.8
Gly/Gly Genotype on Fluticasone HFA-3.3

[back to top]

Change in Forced Expiratory Volume in 1 Second (FEV1) Post-Bronchodilator

Change in Forced Expiratory Volume in 1 Second (FEV1) Post-Bronchodilator as measured by spirometry (NCT00521222)
Timeframe: Up to 16 weeks from baseline

InterventionLiter (Mean)
Arg/Arg Genotype on Advair (Fluticasone With Salmeterol) HFA0.02
Gly/Gly Genotype on Advair (Fluticasone With Salmeterol) HFA-0.07
Arg/Arg Genotype on Fluticasone HFA-0.11
Gly/Gly Genotype on Fluticasone HFA-0.07

[back to top]

Change in Forced Expiratory Volume in 1 Second (FEV1) Pre-Bronchodilator

Change in Forced Expiratory Volume in 1 Second (FEV1) Pre-Bronchodilator as measured by spirometry (NCT00521222)
Timeframe: Up to 16 weeks from baseline

InterventionLiter (Mean)
Arg/Arg Genotype on Advair (Fluticasone With Salmeterol) HFA-0.03
Gly/Gly Genotype on Advair (Fluticasone With Salmeterol) HFA-0.08
Arg/Arg Genotype on Fluticasone HFA-0.12
Gly/Gly Genotype on Fluticasone HFA-0.11

[back to top]

Mean Change From Baseline in Forced Expiratory Volume in 1 Second (FEV1) at Week 52

Change from baseline was calculated as the FEV1 percent predicted value at Week 52 minus the percent predicted value at baseline. The post-bronchodilator lung function test was performed to measure FEV1 30 minutes after inhaling salbutamol. The most reliable result of three different consecutive measurements was documented. (NCT00527826)
Timeframe: Baseline and Week 52

,,
Interventionpercent of predicted value (Mean)
BaselineWeek 52Mean change from baseline
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg36.8238.982.17
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg38.1541.223.08
Total37.4740.092.62

[back to top]

Mean Total Costs (Related to COPD) Per Participant

"Total costs include costs for hospitalization, medication, and visits to/by physician. Medications that were used as required were assumed to be used every second day." (NCT00527826)
Timeframe: Baseline through Week 52

InterventionEuros per participant (Mean)
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg1453
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg1166
Total1311

[back to top]

Mean Number of Exacerbations Per Year: Poisson Model

During regular visits, participants were asked whether they experienced any exacerbation since last contact. Between visits, COPD participants were contacted by phone by the staff and asked about exacerbation details. Exacerbations were defined according to Rodriguez-Roisin: moderate (grade II) exacerbations include a worsening of COPD symptoms that require both a change of respiratory medication (increased dose of prescribed or addition of new drugs) and medical assistance; severe (grade III) exacerbations include deterioration in COPD resulting in hospitalization or emergency room treatment. (NCT00527826)
Timeframe: Baseline through Week 52

InterventionNumber of exacerbations per year (Least Squares Mean)
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg0.863
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg0.830

[back to top] [back to top]

Mean Number of Exacerbations Per Year: Negative Binomial Model

During regular visits, participants were asked whether they experienced any exacerbation since last contact. Between visits, COPD participants were contacted by phone by the staff and asked about exacerbation details. Exacerbations were defined according to Rodriguez-Roisin: moderate (grade II) exacerbations include a worsening of COPD symptoms that require both a change of respiratory medication (increased dose of prescribed or addition of new drugs) and medical assistance; severe (grade III) exacerbations include deterioration in COPD resulting in hospitalization or emergency room treatment. (NCT00527826)
Timeframe: Baseline through Week 52

InterventionNumber of exacerbations per year (Least Squares Mean)
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg0.864
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg0.862

[back to top]

Compliance and Adherence to Study Medication

Compliance is calculated as the ratio (in percent) between the number of actual doses taken during the total treatment period divided by the number of doses that should have been taken during the total treatment period. (NCT00527826)
Timeframe: Baseline through Week 52

Interventionpercentage of doses (Mean)
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg97.08
Sal 50 µg98.44
FP 500 µg98.33

[back to top]

Mean Change From Baseline in the Total Score of the St. George's Respiratory Questionnaire (SGRQ) at Week 52

Change from baseline was calculated as the total score at Week 52 minus the score at baseline. The SGRQ (a self-administered questionnaire) total score ranges from 0 to 100% and summarizes the impact of COPD on overall health status (summed weights of 15 questions). A total score of 0 indicates the best possible status. (NCT00527826)
Timeframe: Baseline and Week 52

,,
Interventionpercent (Mean)
BaselineWeek 52Mean change from baseline
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg57.8256.02-1.80
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg55.8953.25-2.64
Total56.8754.65-2.22

[back to top]

Number of Participants With the Indicated Number of Hospital Stays

The number of participants with the indicated number of hospitalizations was recorded. (NCT00527826)
Timeframe: Baseline through Week 52

,,
Interventionparticipants (Number)
0 hospital stays1 hospital stay2 hospital stays3 hospital stays4 hospital stays5 or more hospital stays
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg82119401
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg87133110
Total1692412511

[back to top]

Number of Participants With the Indicated Number of Days at the Intensive Care Unit (ICU)

The number participants with the indicated number of days at the ICU was recorded. (NCT00527826)
Timeframe: Baseline through Week 52

,,
Interventionparticipants (Number)
0 days1-5 days6-10 days11-30 days>30 days
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg194101
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg132100
Total326201

[back to top]

Mean Number of Days Rescue Medication Was Used

Participants were asked for the number of days they used rescue medication within the 7 days before Week 8 and Week 52. (NCT00527826)
Timeframe: The 7 days before baseline (=Visit 2 [Week 8]) and the last 7 days of study (=Visit 6 [Week 52])

,,
Interventionnumber of days (Mean)
Visit 2 (Week 8)Final visit (Week 52)
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg4.735.03
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg4.114.69
Total4.434.86

[back to top]

Mean Change From Baseline in the Tiffeaneau Index at Week 52

The Tiffeneau index is defined as the FEV1 divided by the IVC (i.e., forced expiratory volume in one second relative to the inspiratory capacity) in percent. Change from baseline is calculated as the FEV1/IVC value at Week 52 minus the value at baseline. (NCT00527826)
Timeframe: Baseline and Week 52

,,
Interventionpercent of IVC (Mean)
BaselineWeek 52Mean change from baseline
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg48.9050.821.92
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg49.0552.833.78
Total48.9851.812.84

[back to top]

Mean Change From Baseline in the Symptom Score of the St. George's Respiratory Questionnaire (SGRQ) at Week 52

Change from baseline is calculated as the symptom score at Week 52 minus the symptom score at baseline. The SGRQ (a self-administered questionnaire) subscale symptom score ranges from 0 to 100% and measures the effect of respiratory symptoms, frequency, and severity on quality of life (summed weights of 8 questions). A score of 0 indicates the best possible status. (NCT00527826)
Timeframe: Baseline and Week 52

,,
Interventionpercent (Mean)
BaselineWeek 52Mean change from baseline
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg68.8065.42-3.38
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg68.9563.77-5.18
Total68.8864.61-4.27

[back to top]

Mean Change From Baseline in the Impact Score of the St. George's Respiratory Questionnaire (SGRQ) at Week 52

Change from baseline was calculated as the impact score at Week 52 minus the score at baseline. The SGRQ (a self-administered questionnaire) subscale impact score ranges from 0 to 100% and is concerned with social functioning and psychological disturbances (summed weights of 5 questions). A score of 0 indicates the best possible status. (NCT00527826)
Timeframe: Baseline and Week 52

,,
Interventionpercent (Mean)
BaselineWeek 52Mean change from baseline
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg46.0344.66-1.37
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg43.5841.26-2.32
Total44.8242.98-1.84

[back to top]

Mean Change From Baseline in the Activity Score of the St. George's Respiratory Questionnaire (SGRQ) at Week 52

Change from baseline is calculated as the activity score at Week 52 minus the score at baseline. The SGRQ (a self-administered questionnaire) subscale activity score ranges from 0 to 100% and is concerned with activities that cause or are limited by breathlessness (summed weights of 2 questions). A score of 0 indicates the best possible status. (NCT00527826)
Timeframe: Baseline and Week 52

,,
Interventionpercent (Mean)
BaselineWeek 52Mean change from baseline
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg72.8071.17-1.63
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg70.6468.53-2.11
Total71.7369.86-1.87

[back to top]

Mean Change From Baseline in Inspiratory Vital Capacity (IVC) at Week 52

Change from baseline was measured as the IVC value at Week 52 minus the value at baseline. The post-bronchodilator lung function test was performed to measure IVC 30 minutes after inhaling salbutamol. The most reliable result of three different, consecutive measurements was documented. (NCT00527826)
Timeframe: Baseline and Week 52

,,
Interventionliters (Mean)
BaselineWeek 52Mean change from baseline
Salmeterol Xinafoate/FP in Fixed Combination (SFC) 50/500 µg2.172.14-0.02
Salmeterol Xinafoate/FP Separately (Sal/FP) 50/500 µg2.292.27-0.02
Total2.232.21-0.02

[back to top]

Blood Glucose 1 Hour Post-dose at Day 1

Blood glucose (in millimoles per liter, mmol/L) was measured from venous blood samples. Samples were sent to a central laboratory for analysis. The analysis included baseline blood glucose and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Day 1

Interventionmmol/L (Least Squares Mean)
Indacaterol 300 μg5.24
Indacaterol 600 μg5.45
Salmeterol 50 μg5.21

[back to top]

Blood Glucose 1 Hour Post-dose at Week 12

Blood glucose (in millimoles per liter, mmol/L) was measured from venous blood samples. Samples were sent to a central laboratory for analysis. The analysis included baseline blood glucose and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Week 12

Interventionmmol/L (Least Squares Mean)
Indacaterol 300 μg5.27
Indacaterol 600 μg5.38
Salmeterol 50 μg5.23

[back to top]

Corrected QT (QTc) Interval Using Fridericia's Formula Measured 1 Hour Post-dose at Day 1

The QTc interval (in milliseconds, ms) is calculated from electrocardiogram (ECG) data collected 1 hour post-dose using Fridericia's formula: QTc = QT/RR^0.33. QTc is the interval between the Q and T waves corrected for heart rate and RR is the interval between two R waves. ECGs included all 12 standard leads and a Lead II rhythm strip of at least 10-second duration. All results were sent to a central laboratory for review by a cardiologist. The analysis included baseline QTc interval and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Day 1

Interventionms (Least Squares Mean)
Indacaterol 300 μg404.46
Indacaterol 600 μg404.97
Salmeterol 50 μg405.05

[back to top]

Corrected QT (QTc) Interval Using Fridericia's Formula Measured 1 Hour Post-dose at Week 12

The QTc interval (in milliseconds, ms) is calculated from electrocardiogram (ECG) data collected 1 hour post-dose using Fridericia's formula: QTc = QT/RR^0.33. QTc is the interval between the Q and T waves corrected for heart rate and RR is the interval between two R waves. ECGs included all 12 standard leads and a Lead II rhythm strip of at least 10-second duration. All results were sent to a central laboratory for review by a cardiologist. The analysis included baseline QTc interval and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Week 12

Interventionms (Least Squares Mean)
Indacaterol 300 μg404.93
Indacaterol 600 μg407.78
Salmeterol 50 μg406.98

[back to top]

Corrected QT (QTc) Interval Using Fridericia's Formula Measured 1 Hour Post-dose at Week 21

The QTc interval (in milliseconds, ms) is calculated from electrocardiogram (ECG) data collected 1 hour post-dose using Fridericia's formula: QTc = QT/RR^0.33. QTc is the interval between the Q and T waves corrected for heart rate and RR is the interval between two R waves. ECGs included all 12 standard leads and a Lead II rhythm strip of at least 10-second duration. All results were sent to a central laboratory for review by a cardiologist. The analysis included baseline QTc interval and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Week 21

Interventionms (Least Squares Mean)
Indacaterol 300 μg406.41
Indacaterol 600 μg407.49
Salmeterol 50 μg407.23

[back to top]

Diastolic Blood Pressure 1 Hour Post-dose at Day 1

Diastolic blood pressure measurements (in millimeters of mercury, mmHg) were made 1 hour post-dose after the patient had rested in the sitting position for at least 10 minutes. Measurements were made using an inflatable cuff around the upper arm. Phase V Korotkoff sounds were used for determination of diastolic pressure. The analysis included baseline diastolic blood pressure and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Day 1

InterventionmmHg (Least Squares Mean)
Indacaterol 300 μg76.67
Indacaterol 600 μg76.55
Salmeterol 50 μg77.08

[back to top]

Diastolic Blood Pressure 1 Hour Post-dose at Week 12

Diastolic blood pressure measurements (in millimeters of mercury, mmHg) were made 1 hour post-dose after the patient had rested in the sitting position for at least 10 minutes. Measurements were made using an inflatable cuff around the upper arm. Phase V Korotkoff sounds were used for determination of diastolic pressure. The analysis included baseline diastolic blood pressure and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Week 12

InterventionmmHg (Least Squares Mean)
Indacaterol 300 μg75.38
Indacaterol 600 μg76.11
Salmeterol 50 μg76.96

[back to top]

Number of Asthma Exacerbations Per Patient (Without Imputation) During the 26 Weeks of the Study

"An asthma exacerbation was defined as a worsening of asthma as judged clinically significant by the physician, requiring treatment with rescue oral or intravenous (IV) corticosteroids. The number of asthma exacerbations includes events recorded on the asthma exacerbation clinical report form (CRF) page and events recorded on the adverse events CRF page with asthma as a key word in the preferred term." (NCT00529529)
Timeframe: Baseline (Day 1) to end of study (Week 26)

InterventionAsthma exacerbations (Mean)
Indacaterol 300 μg0.17
Indacaterol 600 μg0.19
Salmeterol 50 μg0.19

[back to top]

Percentage of Patients With at Least 1 Adverse Event During the 26 Weeks of the Study

Adverse events include asthma exacerbations. An asthma exacerbation was defined as a worsening of asthma as judged clinically significant by the physician, requiring treatment with rescue oral or intravenous (IV) corticosteroids. Asthma worsening that required treatment with inhaled or nebulized short-acting β2-agonists or an increase in inhaled corticosteroids only was not considered an asthma exacerbation. (NCT00529529)
Timeframe: Baseline (Day 1) to end of study (Week 26)

InterventionPercentage of patients (Number)
Indacaterol 300 μg54.9
Indacaterol 600 μg66.4
Salmeterol 50 μg67.3

[back to top]

Serum Potassium 1 Hour Post-dose at Day 1

Serum potassium (in millimoles per liter, mmol/L) was measured from venous blood samples. Samples were sent to a central laboratory for analysis. The analysis included baseline serum potassium and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Day 1

Interventionmmol/L (Least Squares Mean)
Indacaterol 300 μg4.30
Indacaterol 600 μg4.24
Salmeterol 50 μg4.32

[back to top]

Serum Potassium 1 Hour Post-dose at Week 12

Serum potassium (in millimoles per liter, mmol/L) was measured from venous blood samples. Samples were sent to a central laboratory for analysis. The analysis included baseline serum potassium and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Week 12

Interventionmmol/L (Least Squares Mean)
Indacaterol 300 μg4.31
Indacaterol 600 μg4.29
Salmeterol 50 μg4.33

[back to top]

Percentage of Patients With Clinically Significant Asthma Exacerbations During the 26 Weeks of the Study

"A clinically significant asthma exacerbation was defined as a worsening of asthma as judged clinically significant by the physician, requiring treatment with systemic corticosteroids. This includes events recorded on the asthma exacerbation clinical report form (CRF) page and events recorded on the adverse events CRF page with asthma as a key word in the preferred term." (NCT00529529)
Timeframe: Baseline (Day 1) to end of study (Week 26)

,,
InterventionPercentage of patients (Number)
0 exacerbations1 exacerbation2 exacerbations3 exacerbations
Indacaterol 300 μg92.95.60.70.7
Indacaterol 600 μg89.99.30.70.0
Salmeterol 50 μg90.08.61.50.0

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose at Week 12 + 1 Day, Day 85

FEV1 (in liters, L) was measured with spirometry conducted according to internationally accepted standards. Trough FEV1 was defined as the average of measurements made 23 hours 10 minutes and 23 hours 45 minutes post-dose at Week 12, Day 85. The analysis included baseline FEV1 and FEV1 pre-dose and 30 minutes post-dose of salbutamol during screening as covariates. (NCT00529529)
Timeframe: 24 hours post-dose at Week 12 + 1 day, Day 85

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg2.61
Indacaterol 600 μg2.62
Salmeterol 50 μg2.54

[back to top]

Systolic Blood Pressure 1 Hour Post-dose at Day 1

Systolic blood pressure measurements (in millimeters of mercury, mmHg) were made 1 hour post-dose after the patient had rested in the sitting position for at least 10 minutes. Measurements were made using an inflatable cuff around the upper arm. The analysis included baseline systolic blood pressure and forced expiratory volume in 1 second (FEV1) pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Day 1

InterventionmmHg (Least Squares Mean)
Indacaterol 300 μg122.79
Indacaterol 600 μg122.60
Salmeterol 50 μg122.56

[back to top]

Systolic Blood Pressure 1 Hour Post-dose at Week 12

Systolic blood pressure measurements (in millimeters of mercury, mmHg) were made 1 hour post-dose after the patient had rested in the sitting position for at least 10 minutes. Measurements were made using an inflatable cuff around the upper arm. The analysis included baseline systolic blood pressure and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Week 12

InterventionmmHg (Least Squares Mean)
Indacaterol 300 μg120.29
Indacaterol 600 μg121.98
Salmeterol 50 μg122.02

[back to top]

24 Hour Mean Heart Rate Determined From ECG Holter Monitoring at Week 12

Continuous 24 hour electrocardiography (Holter monitoring) was conducted in a subset of patients at designated study centers, and was used to calculate the mean heart rate (in beats per minute, bpm). Patients returned the Holter monitor recorder to the clinic the morning after the 24 hour recording was complete. The results of Holter monitoring were processed centrally. The analysis included baseline 24 hour mean heart rate and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Week 12

Interventionbpm (Least Squares Mean)
Indacaterol 300 μg81.0
Indacaterol 600 μg81.7
Salmeterol 50 μg80.4

[back to top]

24 Hour Mean Heart Rate Determined From ECG Holter Monitoring at Week 26

Continuous 24 hour electrocardiography (Holter monitoring) was conducted in a subset of patients at designated study centers, and was used to calculate the mean heart rate (in beats per minute, bpm). Patients returned the Holter monitor recorder to the clinic the morning after the 24 hour recording was complete. The results of Holter monitoring were processed centrally. The analysis included baseline 24 hour mean heart rate and FEV1 pre-dose and 30 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00529529)
Timeframe: Week 26

Interventionbpm (Least Squares Mean)
Indacaterol 300 μg79.4
Indacaterol 600 μg81.0
Salmeterol 50 μg79.2

[back to top]

Static Lung Volumes

Post-dose IC (Inspiratory Capacity) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol2.46
Fluticasone + Salmeterol2.37

[back to top]

Static Lung Volumes

Post-dose IC (Inspiratory Capacity) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol2.47
Fluticasone + Salmeterol2.35

[back to top]

Static Lung Volumes

Post-dose IRV (Inspiratory Reserve Volume) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol1.62
Fluticasone + Salmeterol1.55

[back to top]

Static Lung Volumes

Post-dose IRV (Inspiratory Reserve Volume) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol1.62
Fluticasone + Salmeterol1.55

[back to top]

Static Lung Volumes

Post-dose RV (Residual Volume) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.91
Fluticasone + Salmeterol4.14

[back to top]

Static Lung Volumes

Post-dose RV (Residual Volume) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.92
Fluticasone + Salmeterol4.07

[back to top]

Static Lung Volumes

Post-dose TLC (Total Lung Capacity) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol7.33
Fluticasone + Salmeterol7.47

[back to top]

Static Lung Volumes

Post-dose TLC (Total Lung Capacity) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol7.36
Fluticasone + Salmeterol7.36

[back to top]

Static Lung Volumes

Trough IC (Inspiratory Capacity) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol2.28
Fluticasone + Salmeterol2.23

[back to top]

Static Lung Volumes

Trough IC (Inspiratory Capacity) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol2.33
Fluticasone + Salmeterol2.23

[back to top]

Static Lung Volumes

Trough IRV (Inspiratory Reserve Volume) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol1.47
Fluticasone + Salmeterol1.42

[back to top]

Static Lung Volumes

Trough IRV (Inspiratory Reserve Volume) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol1.48
Fluticasone + Salmeterol1.41

[back to top]

Static Lung Volumes

Trough RV (Residual Volume) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol4.28
Fluticasone + Salmeterol4.35

[back to top]

Static Lung Volumes

Trough RV (Residual Volume) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol4.23
Fluticasone + Salmeterol4.25

[back to top]

Static Lung Volumes

Trough TGV(FRC) (Thoracic Gas Volume) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol5.32
Fluticasone + Salmeterol5.34

[back to top]

Static Lung Volumes

Trough TGV(FRC) (Thoracic Gas Volume) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol5.24
Fluticasone + Salmeterol5.25

[back to top]

Static Lung Volumes

Trough TLC (Total Lung Capacity) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol7.52
Fluticasone + Salmeterol7.51

[back to top]

Static Lung Volumes

Trough TLC (Total Lung Capacity) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol7.47
Fluticasone + Salmeterol7.39

[back to top]

Static Lung Volumes (Percent)

Post-dose RV/TLC (Residual Volume over Total Lung Capacity) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionPercent of RV over TLC (Mean)
Tiotropium + Salmeterol53.09
Fluticasone + Salmeterol55.07

[back to top]

Static Lung Volumes (Percent)

Post-dose RV/TLC (Residual Volume over Total Lung Capacity) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionPercent of RV over TLC (Mean)
Tiotropium + Salmeterol52.79
Fluticasone + Salmeterol55.02

[back to top]

Static Lung Volumes (Percent)

Post-dose TGV/TLC (Thoracic Gas Volume over Total Lung Capacity) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionPercent of TGV over TLC (Mean)
Tiotropium + Salmeterol67.65
Fluticasone + Salmeterol68.85

[back to top]

Static Lung Volumes (Percent)

Trough RV/TLC (Residual Volume over Total Lung Capacity) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionPercent of RV over TLC (Mean)
Tiotropium + Salmeterol56.57
Fluticasone + Salmeterol57.47

[back to top]

Static Lung Volumes (Percent)

Trough RV/TLC (Residual Volume over Total Lung Capacity) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionPercent of RV over TLC (Mean)
Tiotropium + Salmeterol56.10
Fluticasone + Salmeterol57.18

[back to top]

Static Lung Volumes (Percent)

Trough TGV/TLC (Thoracic Gas Volume over Total Lung Capacity) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionPercent of TGV over TLC (Mean)
Tiotropium + Salmeterol70.59
Fluticasone + Salmeterol70.99

[back to top]

Static Lung Volumes (Percent)

Trough TGV/TLC (Thoracic Gas Volume over Total Lung Capacity) after 8 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 8 weeks

InterventionPercent of TGV over TLC (Mean)
Tiotropium + Salmeterol69.87
Fluticasone + Salmeterol70.94

[back to top]

Symptom Intensity During Exercise

Isotime Borg dyspnea scale after 4 weeks, Unit on a Scale (min. 0, max. 10), 0 = no dyspnea, 10 = worst imaginable dyspnea (NCT00530842)
Timeframe: 4 weeks

InterventionUnit on a Scale (Mean)
Tiotropium + Salmeterol4.80
Fluticasone + Salmeterol5.02

[back to top]

Symptom Intensity During Exercise

Isotime Borg dyspnea scale after 8 weeks, Unit on a Scale (min. 0, max 10), 0 = no dyspnea, 10 = worst imaginable dyspnea (NCT00530842)
Timeframe: 8 weeks

InterventionUnit on a Scale (Mean)
Tiotropium + Salmeterol4.77
Fluticasone + Salmeterol4.98

[back to top]

Symptom Intensity During Exercise

Isotime Borg leg discomfort scale after 4 weeks, Unit on a Scale (min. 0, max. 10), 0 = no leg dyscomfort, 10 = worst imaginable leg dyscomfort (NCT00530842)
Timeframe: 4 weeks

InterventionUnit on a Scale (Mean)
Tiotropium + Salmeterol4.63
Fluticasone + Salmeterol4.63

[back to top]

Symptom Intensity During Exercise

Isotime Borg leg discomfort scale after 8 weeks, Unit on a Scale (min. 0, max. 10), 0 = no leg dyscomfort, 10 = worst imaginable leg dyscomfort (NCT00530842)
Timeframe: 8 weeks

InterventionUnit on a Scale (Mean)
Tiotropium + Salmeterol4.64
Fluticasone + Salmeterol4.53

[back to top]

Forced Vital Capacity (FVC)

Trough FVC (Forced Vital Capacity) after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.04
Fluticasone + Salmeterol2.93

[back to top]

Locus of Symptom Limitation at Peak Exercise During Exercise

Reason for stopping exercise after 8 weeks (leg discomfort, breathing discomfort, both or none) (NCT00530842)
Timeframe: 8 weeks

,
InterventionParticipants (Number)
Leg discomfortBreathing discomfortBoth (leg and breathing discomfort)None
Fluticasone + Salmeterol721317828
Tiotropium + Salmeterol881128227

[back to top]

Locus of Symptom Limitation at Peak Exercise During Exercise

Reason for stopping exercise at baseline (leg discomfort, breathing discomfort, both or none) (NCT00530842)
Timeframe: baseline

,
InterventionParticipants (Number)
Leg discomfortBreathing discomfortBoth (leg and breathing discomfort)None
Fluticasone + Salmeterol531329232
Tiotropium + Salmeterol531329232

[back to top]

Locus of Symptom Limitation at Peak Exercise During Exercise

Reason for stopping exercise after 4 weeks (leg discomfort, breathing discomfort, both or none) (NCT00530842)
Timeframe: 4 weeks

,
InterventionParticipants (Number)
Leg discomfortBreathing discomfortBoth (leg and breathing discomfort)None
Fluticasone + Salmeterol721197840
Tiotropium + Salmeterol891047838

[back to top]

Static Lung Volumes (Percent)

Post-dose TGV/TLC (Thoracic Gas Volume over Total Lung Capacity) after 4 weeks (measured by bodyphlethysmography) (NCT00530842)
Timeframe: 4 weeks

InterventionPercent of TGV over TLC (Mean)
Tiotropium + Salmeterol68.43
Fluticasone + Salmeterol69.22

[back to top]

Forced Vital Capacity (FVC)

Post-dose FVC (Forced Vital Capacity) after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.26
Fluticasone + Salmeterol3.11

[back to top]

Forced Vital Capacity (FVC)

Trough FVC (Forced Vital Capacity) after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.06
Fluticasone + Salmeterol2.94

[back to top]

Post-dose TGV(FRC) (After 4 Weeks)

Post-dose TGV(FRC) (Thoracic Gas Volume) after 4 weeks (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol5.00
Fluticasone + Salmeterol5.19

[back to top]

Forced Vital Capacity (FVC)

Post-dose FVC (Forced Vital Capacity) after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.25
Fluticasone + Salmeterol3.11

[back to top]

Post-dose TGV(FRC) (After 8 Weeks)

Post-dose TGV(FRC) (Thoracic Gas Volume; co-primary endpoint) after 8 weeks (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol4.99
Fluticasone + Salmeterol5.07

[back to top]

Slow Vital Capacity (SVC)

Post-dose SVC (Slow Vital Capacity) after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.39
Fluticasone + Salmeterol3.27

[back to top]

Slow Vital Capacity (SVC)

Post-dose SVC (Slow Vital Capacity) after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.42
Fluticasone + Salmeterol3.28

[back to top]

Slow Vital Capacity (SVC)

Trough SVC (Slow Vital Capacity) after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.19
Fluticasone + Salmeterol3.12

[back to top]

Slow Vital Capacity (SVC)

Trough SVC (Slow Vital Capacity) after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol3.22
Fluticasone + Salmeterol3.12

[back to top]

Dyspnea and Leg Discomfort

Peak Borg dyspnea scale after 8 weeks, Unit on a Scale (min. 0, max 10) (NCT00530842)
Timeframe: 8 weeks

InterventionUnit on a Scale (Mean)
Tiotropium + Salmeterol6.52
Fluticasone + Salmeterol6.61

[back to top]

Dyspnea and Leg Discomfort

Peak Borg leg discomfort scale after 8 weeks, Unit on a Scale (min. 0, max 10) (NCT00530842)
Timeframe: 8 weeks

InterventionUnit on a Scale (Mean)
Tiotropium + Salmeterol6.10
Fluticasone + Salmeterol5.86

[back to top]

Endurance Time (After 4 Weeks)

Endurance time to the point of symptom limitation after 4 weeks during a constant work rate exercise test at 75% Wcap (co-primary endpoint) (NCT00530842)
Timeframe: 4 weeks

InterventionSeconds (Median)
Tiotropium + Salmeterol458
Fluticasone + Salmeterol450

[back to top]

Endurance Time (After 8 Weeks)

Endurance time to the point of symptom limitation after 8 weeks during a constant work rate exercise test at 75% Wcap (co-primary endpoint) (NCT00530842)
Timeframe: 8 weeks

InterventionSeconds (Median)
Tiotropium + Salmeterol463
Fluticasone + Salmeterol453

[back to top]

FEV1 Over FVC (Percent)

Post-dose FEV1 (Forced Expiratory Volume in 1 second) over FVC (Forced Vital Capacity) after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionPercent of FEV1 over FVC (Mean)
Tiotropium + Salmeterol50.90
Fluticasone + Salmeterol50.91

[back to top]

FEV1 Over FVC (Percent)

Post-dose FEV1 (Forced Expiratory Volume in 1 second) over FVC (Forced Vital Capacity) after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionPercent of FEV1 over FVC (Mean)
Tiotropium + Salmeterol50.77
Fluticasone + Salmeterol50.66

[back to top]

FEV1 Over FVC (Percent)

Trough FEV1 (Forced Expiratory Volume in 1 second) over FVC (Forced Vital Capacity) after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionPercent of FEV1 over FVC (Mean)
Tiotropium + Salmeterol49.74
Fluticasone + Salmeterol50.62

[back to top]

FEV1 Over FVC (Percent)

Trough FEV1 (Forced Expiratory Volume in 1 second) over FVC (Forced Vital Capacity) after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionPercent of FEV1 over FVC (Mean)
Tiotropium + Salmeterol49.16
Fluticasone + Salmeterol49.67

[back to top]

Forced Expiratory Volume in 1 Second (FEV1)

Post-dose FEV1 (Forced Expiratory Volume in 1 second) after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol1.62
Fluticasone + Salmeterol1.55

[back to top]

Forced Expiratory Volume in 1 Second (FEV1)

Post-dose FEV1 (Forced Expiratory Volume in 1 second) after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol1.62
Fluticasone + Salmeterol1.55

[back to top]

Forced Expiratory Volume in 1 Second (FEV1)

Post-dose percent predicted FEV1 (Forced Expiratory Volume in 1 second) according to ECCS after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionPercent of predicted FEV1 (Mean)
Tiotropium + Salmeterol54.96
Fluticasone + Salmeterol52.64

[back to top]

Forced Expiratory Volume in 1 Second (FEV1)

Post-dose percent predicted FEV1 (Forced Expiratory Volume in 1 second) according to ECCS after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionPercent of predicted FEV1 (Mean)
Tiotropium + Salmeterol54.99
Fluticasone + Salmeterol52.59

[back to top]

Forced Expiratory Volume in 1 Second (FEV1)

Trough FEV1 (Forced Expiratory Volume in 1 second) after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol1.48
Fluticasone + Salmeterol1.45

[back to top]

Forced Expiratory Volume in 1 Second (FEV1)

Trough FEV1 (Forced Expiratory Volume in 1 second) after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionLitres (Mean)
Tiotropium + Salmeterol1.48
Fluticasone + Salmeterol1.44

[back to top]

Forced Expiratory Volume in 1 Second (FEV1)

Trough percent predicted FEV1 (Forced Expiratory Volume in 1 second) according to ECCS after 4 weeks (measured by spirometry) (NCT00530842)
Timeframe: 4 weeks

InterventionPercent of predicted FEV1 (Mean)
Tiotropium + Salmeterol50.40
Fluticasone + Salmeterol49.26

[back to top]

Forced Expiratory Volume in 1 Second (FEV1)

Trough percent predicted FEV1 (Forced Expiratory Volume in 1 second) according to ECCS after 8 weeks (measured by spirometry) (NCT00530842)
Timeframe: 8 weeks

InterventionPercent of predicted FEV1 (Mean)
Tiotropium + Salmeterol50.27
Fluticasone + Salmeterol49.12

[back to top]

Percentage of Participants With Maximum Heart Rate Increase During Exercise in Part 1 of the Study

The percentage of patients with an increase of more than 10 beats per minute (bpm) in their heart rate following treatment with indacaterol and salmeterol compared to treatment with placebo was determined. (NCT00531050)
Timeframe: 24-hours post-dose on Day 1 (of each treatment)

InterventionPercentage of participants (Number)
Part 1: Indacaterol 300μg20.00
Part 1 : Salmeterol 50μg16.0

[back to top]

Change in Heart Rate During Exercise in Part 1

"Change in heart rate is calculated from the 1.5 hour post dose to the maximum heart rate during exercise.~Analysis of covariance included treatment and period as fixed effects, subject as random effect and 1.5 hour pre-exercise/post dose heart rate as a covariate." (NCT00531050)
Timeframe: 1.5 hour post dose to max heart rate during exercise

InterventionBeats per minute (bpm) (Least Squares Mean)
Part 1: Indacaterol 300μg66.246
Part 1 : Salmeterol 50μg64.265
Part 1: Placebo63.058

[back to top]

Maximum Heart Rate During Exercise in Part 1

Maximum heart rate was generally taken from the continuous ECG monitoring. Analysis based on mixed effects analysis using model with treatment and period as fixed effects and subject as random effect. (NCT00531050)
Timeframe: 2 hour post-dose on Day 1

InterventionBeats per minute (bpm) (Least Squares Mean)
Part 1: Indacaterol 300μg133.13
Part 1 : Salmeterol 50μg131.18
Part 1: Placebo129.96

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) During Part 1 and Part 2

FEV1 was measured with spirometry conducted according to internationally accepted standards. Trough FEV1 was defined as the mean of the 23 hours 30 minutes and 24 hours post morning dose FEV1 measurements. Analysis of covariance included pre-dose FEV1 as covariate. (NCT00531050)
Timeframe: 23 hours 30 minutes and 24 hours post-dose at Day 1

InterventionLiters (Least Squares Mean)
Part 1: Indacaterol 300μg1.72
Part 1 : Salmeterol 50μg1.59
Part 1: Placebo1.56
Part 2:Indacaterol 300μg Morning/Placebo Evening1.75
Part 2:Salmeterol 50μg Morning/Salmeterol 50μg Evening1.68
Part 2:Placebo Morning/Placebo Evening1.54

[back to top]

Maximum Heart Rate (HR) During Salbutamol Administration in Part 2

Maximum HR (0-12 hours): maximum (max) of post dose measurement up to second administration. Maximum HR (12-24 hours): max of the post second administration of salbutamol measurements. Maximum HR (0-24 hours): max of all post dose measurements up to and including the 24 hour measurement. Mixed effects analysis model used period baseline HR as the covariate. The maximum HR for 0-24 hours (h) is the maximum of the maximum HR for the two 12h periods and thus the average (LS means) of the maximum HRs for 0-24h will be equal to or greater than the average of the maximum for the two periods. (NCT00531050)
Timeframe: 24 hours post dose on Day 1

,,
InterventionBeats per minute (bpm) (Least Squares Mean)
0 - 12 hours (N= 23, 24, 23)12 - 24 hours (N= 20, 21, 20)0 - 24 hours (N= 23, 24, 23)
Part 2:Indacaterol 300μg Morning/Placebo Evening98.02697.179102.501
Part 2:Placebo Morning/Placebo Evening97.96097.786103.951
Part 2:Salmeterol 50μg Morning/Salmeterol 50μg Evening98.08799.954102.303

[back to top]

Percentage of Participants With Maximum Heart Rate Increase During Salbutamol Administration in Part 2 of the Study

"The percentage of patients with an increase of >= 10 beats per minute (bpm) in their heart rate (HR) following treatment with indacaterol and salmeterol compared to treatment with placebo over 24 hours in Part 2 was determined.~0-12 hours: post first dose measurements up to second dose~12-24 hours: post second dose measurement up to and including the 24 hour measurement~0-24 hours: all post dose measurements up to and including the 24 hour measurement" (NCT00531050)
Timeframe: 24 hours post dose on Day 1

,
InterventionPercentage of participants (Number)
0 - 12 hours (N= 23,23)12 - 24 hours (N= 20, 20)0 - 24 hours (N= 23, 23)
Part 2:Indacaterol 300μg Morning/Placebo Evening17.3910.0013.04
Part 2:Salmeterol 50μg Morning/Salmeterol 50μg Evening17.3925.0017.39

[back to top]

Change in Forced Vital Capacity (FVC) From Before Dose to5 Minutes After Dose at the Clinic

The change from pre-dose was calculated using the pre-dose baseline value (run-in and washout period respectively), and pre-dose value at day 1, with pre-dose run-in/washout as covariate. (NCT00542880)
Timeframe: Baseline (run-in, and washout) and day 1 of treatment period

InterventionLiters (Mean)
Symbicort Turbuhaler0.0950
Seretide Diskus0.0490

[back to top]

Change in FEV1from Before Dose to 5 Minutes After Dose in the Morning

The change from pre-dose was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with mean pre-dose run-in/washout as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters (Mean)
Symbicort Turbuhaler15.8
Seretide Diskus9.6

[back to top]

Change in FEV1 From Before Dose to 5 Minutes After Dose at the Clinic

The change from pre-dose was calculated using the pre-dose baseline value (run-in and washout period respectively), and pre-dose value at day 1, with pre-dose run-in/washout as covariate. (NCT00542880)
Timeframe: Baseline (run-in, and washout) and day 1 of treatment period

InterventionLiters (Mean)
Symbicort Turbuhaler0.1120
Seretide Diskus0.0440

[back to top]

Change in FEV1 From Before Dose to 15 Minutes After Dose in the Morning

The change from pre-dose was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with mean pre-dose run-in/washout as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters (Mean)
Symbicort Turbuhaler0.0930
Seretide Diskus0.0280

[back to top]

Capacity of Daily Living in the Morning (CDLM) (Change From Pre to End of Treatment)

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. Score scale 0 - 5 with 0=worst and 5 = best. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

Interventionunits on a scale (Mean)
Symbicort Turbuhaler0.1920
Seretide Diskus First0.1240

[back to top]

FEV1 15 Minutes After Morning Dose

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters (Mean)
Symbicort Turbuhaler0.1220
Seretide Diskus0.1030

[back to top]

FEV1 Before Evening Dose

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters (Mean)
Symbicort Turbuhaler0.1470
Seretide Diskus0.1060

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) Before Morning Dose

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters (Mean)
Symbicort Turbuhaler0.0310
Seretide Diskus0.0590

[back to top]

Change in PEF From Before Dose to 15 Minutes After Dose in the Morning

The change from pre-dose was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with mean pre-dose run-in/washout as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters/minute (Mean)
Symbicort Turbuhaler11.6
Seretide Diskus6.1

[back to top]

Peak Expiratory Flow (PEF) 5 Minutes After Morning Dose

The change from baseline in PEF was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and all days of treatment, with baseline as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

Interventionliters/minute (Mean)
Symbicort Turbuhaler15.1
Seretide Diskus13.4

[back to top]

PEF 15 Minutes After Morning Dose

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters/minute (Mean)
Symbicort Turbuhaler19.9
Seretide Diskus16.7

[back to top]

PEF Before Evening Dose

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters/minute (Mean)
Symbicort Turbuhaler4
Seretide Diskus1.8

[back to top]

PEF Before Morning Dose

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters/minutes (Mean)
Symbicort Turbuhaler4.8
Seretide Diskus7.9

[back to top]

The Clinical Chronic Obstructive Pulmonary Disease (COPD) Questionnaire (Change From Pre to End of Treatment)

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. Score scale 0 - 6 with 0=worst and 6 = best. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionUnits on a scale (Mean)
Symbicort Turbuhaler0.24
Seretide Diskus0.19

[back to top]

Change in PEF From Before Dose to 5 Minutes After Dose in the Morning

The change from pre-dose was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with pre-dose run-in/washout as covariate. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionLiters/minute (Mean)
Symbicort Turbuhaler0.0160
Seretide Diskus0.0030

[back to top]

Difficulty in Getting Out From Bed (MASQ) (Change From Pre to End of Treatment)

The change from baseline was calculated using the average over baseline (the last 7 days of run-in and washout period respectively), and over all days of treatment, with baseline as covariate. Score scale 0 - 5 with 0=worst and 5 = best. (NCT00542880)
Timeframe: Baseline (daily records during run-in, and washout) and daily records during the treatment period of 7 days

InterventionUnits on a scale (Mean)
Symbicort Turbuhaler0.21
Seretide Diskus0.14

[back to top]

Change From Period Baseline in Peak Percent Predicted Forced Expiratory Volume in 1 Second (FEV1)

"Peak FEV1 was defined as the peak FEV1 up to 4 hours post-dose. The FEV1 percent predicted expresses FEV1 as a percentage of the predicted values for participants of similar characteristics (height, age, sex, and sometimes race and weight). A positive change from baseline in FEV1 % predicted indicates improvement in lung function. Change from baseline in peak FEV1 % predicted was modeled using a linear mixed effect model fitting treatment, sequence and period as fixed factors, patient within sequence as a random factor and pre-dose value as covariate." (NCT00556673)
Timeframe: Days 1, 8 and 15, pre-dose (Baseline) and 5, 15, and 30 minutes, 1, 2, 3, and 4 hours post-dose.

InterventionPercent of predicted (Least Squares Mean)
Indacaterol/Mometasone16.27
Placebo6.85
Fluticasone/Salmeterol16.49

[back to top]

Change From Period Baseline in Trough FEV1/FVC Ratio

The forced expiratory volume in one second (FEV1)/forced vital capacity (FVC) ratio represents the proportion of a person's vital capacity that they are able to expire in the first second of an expiration. Trough FEV1/FVC was calculated from measurements taken 24 hours post-dose. Change from baseline in trough FEV1/FVC ratio was modeled using a linear mixed effect model fitting treatment, sequence and period as fixed factors, patient within sequence as a random factor and pre-dose value as covariate. (NCT00556673)
Timeframe: Pre-dose for each Treatment Period (Days 1, 8 and 15) and 24-hours post-dose for each Treatment Period (Days 2, 9 and 16).

Interventionratio (Least Squares Mean)
Indacaterol/Mometasone2.50
Placebo2.15
Fluticasone/Salmeterol2.65

[back to top]

Change From Period Baseline in Trough Forced Vital Capacity (FVC)

Vital capacity is the amount of air which can be forcibly exhaled from the lungs after taking the deepest breath possible. Trough FVC was measured 24 hours post-dose. Change form baseline in trough FVC was modeled using a linear mixed effect model fitting treatment, sequence and period as fixed factors, patient within sequence as a random factor and pre-dose value as covariate. (NCT00556673)
Timeframe: Pre-dose for each Treatment Period (Days 1, 8 and 15) and 24-hours post-dose for each Treatment Period (Days 2, 9 and 16).

Interventionliters (Least Squares Mean)
Indacaterol/Mometasone0.22
Placebo-0.14
Fluticasone/Salmeterol0.17

[back to top]

Change From Period Baseline in Trough Percent Predicted Forced Expiratory Volume in 1 Second (FEV1)

"Trough FEV1 was measured 24 hours post-dose. The FEV1 percent predicted expresses FEV1 as a percentage of the predicted values for participants of similar characteristics (height, age, sex, and sometimes race and weight). A positive change from baseline in FEV1 % predicted indicates improvement in lung function. Change from baseline in trough FEV1 % predicted was modeled using a linear mixed effect model fitting treatment, sequence and period as fixed factors, patient within sequence as a random factor and pre-dose value as covariate." (NCT00556673)
Timeframe: Pre-dose for each Treatment Period (Days 1, 8 and 15) and 24-hours post-dose for each Treatment Period (Days 2, 9 and 16).

InterventionPercent of predicted (Least Squares Mean)
Indacaterol/Mometasone6.95
Placebo-2.87
Fluticasone/Salmeterol9.85

[back to top]

Change From Period Baseline to 24 Hour Post-dose (Trough) Forced Expiratory Volume in 1 Second (FEV1)

FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation. Change from the period baseline to 24 hour post dose trough FEV1 after 1 day of treatment was modeled using a linear mixed effect model fitting treatment, sequence and period as fixed factors, patient within sequence as a random factor and pre-dose FEV1 as covariate. (NCT00556673)
Timeframe: Pre-dose for each Treatment Period (Days 1, 8 and 15) and 24-hours post-dose for each Treatment Period (Days 2, 9 and 16).

Interventionliters (Least Squares Mean)
Indacaterol/Mometasone0.27
Placebo-0.12
Fluticasone/Salmeterol0.37

[back to top]

Maximum (Peak) Plasma Concentration (Cmax) of Indacaterol

(NCT00556673)
Timeframe: Samples were taken pre-dose and at 15 and 30 minutes and 1, 2, 4, 12 and 24 hours post-dose.

Interventionpg/mL (Mean)
Indacaterol/Mometasone289

[back to top]

Maximum (Peak) Plasma Concentration (Cmax) of Mometasone Furoate

(NCT00556673)
Timeframe: Samples were taken pre-dose and at 15 and 30 minutes and 1, 2, 4, 12 and 24 hours post-dose.

Interventionpg/mL (Mean)
Indacaterol/Mometasone47.3

[back to top]

Time to Reach Peak or Maximum Concentration Following Drug Administration for Indacaterol

(NCT00556673)
Timeframe: Samples were taken pre-dose and at 15 and 30 minutes and 1, 2, 4, 12 and 24 hours post-dose.

Interventionhours (Median)
Indacaterol/Mometasone0.325

[back to top]

Time to Reach Peak or Maximum Concentration Following Drug Administration for Mometasone Furoate

(NCT00556673)
Timeframe: Samples were taken pre-dose and at 15 and 30 minutes and 1, 2, 4, 12 and 24 hours post-dose.

Interventionhours (Median)
Indacaterol/Mometasone1.05

[back to top]

Area Under the Concentration-time Curve From Time 0 to 12 Hours Post-dose for Mometasone Furoate

(NCT00556673)
Timeframe: Samples were taken pre-dose and at 15 and 30 minutes and 1, 2, 4, and 12 hours post-dose.

Interventionpg*h/mL (Mean)
Indacaterol/Mometasone287

[back to top]

Area Under the Concentration-time Curve From Time 0 to 24 Hours Post-dose for Indacaterol

(NCT00556673)
Timeframe: Samples were taken pre-dose and at 15 and 30 minutes and 1, 2, 4, 12 and 24 hours post-dose.

Interventionpg*h/mL (Mean)
Indacaterol/Mometasone1331

[back to top]

Area Under the Concentration-time Curve From Time 0 to 24 Hours Post-dose for Mometasone Furoate

(NCT00556673)
Timeframe: Samples were taken pre-dose and at 15 and 30 minutes and 1, 2, 4, 12 and 24 hours post-dose.

Interventionpg*h/mL (Mean)
Indacaterol/Mometasone389

[back to top]

Change From Baseline in Peak Forced Expiratory Volume in One Second (FEV1)

FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation. Peak FEV1 is defined as the peak FEV1 between 0 and 4 hours post-dose. The change from baseline in peak FEV1 was modeled using a linear mixed effect model fitting treatment, sequence and period as fixed factors, patient within sequence as a random factor and pre-dose FEV1 as covariate. (NCT00556673)
Timeframe: Days 1, 8 and 15, pre-dose (Baseline) and 5, 15, and 30 minutes, 1, 2, 3, and 4 hours post-dose.

Interventionliters (Least Squares Mean)
Indacaterol/Mometasone0.64
Placebo0.26
Fluticasone/Salmeterol0.62

[back to top]

Change From Period Baseline in Peak FEV1/FVC Ratio

The forced expiratory volume in one second (FEV1)/forced vital capacity (FVC) ratio represents the proportion of a person's vital capacity that they are able to expire in the first second of an expiration. Peak FEV1/FVC was calculated from spirometry measurements taken up to 4 hours post-dose. Change from baseline in peak FEV1/FVC ratio was modeled using a linear mixed effect model fitting treatment, sequence and period as fixed factors, patient within sequence as a random factor and pre-dose value as covariate. (NCT00556673)
Timeframe: Days 1, 8 and 15, pre-dose (Baseline) and 5, 15, and 30 minutes, 1, 2, 3, and 4 hours post-dose.

Interventionratio (Least Squares Mean)
Indacaterol/Mometasone2.86
Placebo2.53
Fluticasone/Salmeterol2.90

[back to top]

Change From Period Baseline in Peak Forced Vital Capacity (FVC)

Vital capacity is the amount of air which can be forcibly exhaled from the lungs after taking the deepest breath possible. Peak FVC was measured up to 4 hours post-dose. Change from baseline in peak FVC was modeled using a linear mixed effect model fitting treatment, sequence and period as fixed factors, patient within sequence as a random factor and pre-dose value as covariate. (NCT00556673)
Timeframe: Days 1, 8 and 15, pre-dose (Baseline) and 5, 15, and 30 minutes, 1, 2, 3, and 4 hours post-dose.

Interventionliters (Least Squares Mean)
Indacaterol/Mometasone0.47
Placebo0.20
Fluticasone/Salmeterol0.35

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) Standardized Area Under the Curve (AUC) Between Baseline (Pre-dose) and 24 Hours Post-dose

"FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation. FEV1 was measured pre-dose and up to 24 hours post-dose. The FEV1 standardized area under the curve (AUC) was analyzed for four time intervals:~Baseline (pre-dose) to 4 hours (hr) post-dosing;~Baseline (pre-dose) to 23 hours, 45 minutes (min) post-dosing;~11 hours, 10 minutes to 12 hours, 30 minutes post-dosing;~11 hours, 10 minutes to 23 hours, 45 minutes post-dosing.~AUC for FEV1 was analyzed using Analysis of Covariance adjusting for treatment, period, sequence and center with period baseline as a covariate and patient nested within sequence as a random effect." (NCT00557440)
Timeframe: Pre-dose, 5, 30 minutes, 1, 2, 3, 4 hours, 11 hours 10 minutes, 11 hours 45 minutes, 12 hours 30 minutes, 14, 16, 18, 20, 22 hours, 23 hours 10 minutes, and 23 hours 45 minutes post-dosing.

,,
Interventionliters (Least Squares Mean)
Baseline to 4 hours [N=36, 36, 37]Baseline to 23 hours, 45 minutes [N=36, 36, 37]11 hr, 10 min to 12 hr, 30 min [N=36, 35, 34]11 hr, 10 min to 23 hr, 45min [N=36, 36, 36]
Fluticasone/Salmeterol2.7132.6792.5852.696
Indacaterol/Mometasone2.7302.7182.6672.726
Placebo2.4692.4302.3142.470

[back to top]

Change From Period Baseline to 24 Hour Post-dose (Trough) Forced Expiratory Volume in 1 Second (FEV1)

FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation. Change from the period baseline to 24 hour post dose trough FEV1 after 1 day of treatment was analyzed using Analysis of Covariance (ANCOVA) adjusting for treatment, period, sequence and center with period baseline as a covariate and patient nested within sequence as a random effect. (NCT00557440)
Timeframe: Pre-dose for each Treatment Period (Days 1, 8 and 15) and 24-hours post-dose for each Treatment Period (Days 2, 9 and 16).

Interventionliters (Least Squares Mean)
Indacaterol/Mometasone0.081
Fluticasone/Salmeterol0.049
Placebo-0.083

[back to top]

Time to Peak Forced Expiratory Volume in 1 Second (FEV1)

"FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation. Time to peak FEV1 is calculated in minutes from the time of inhalation of study drug to the time of the peak FEV1 during the first 4 hours post-dose.~Time to peak FEV1 is based on log-transformed analysis of variance adjusted for treatment, period, sequence and center, with patient nested within sequence as a random effect. Geometric Mean was obtained by taking anti-logs of the adjusted means from the model and standard error was calculated using the delta method." (NCT00557440)
Timeframe: Up to 4 hours post-dose

Interventionminutes (Geometric Mean)
Indacaterol/Mometasone87.4
Fluticasone/Salmeterol67.7
Placebo22.3

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) at Single Time Points

FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation. FEV1 was analyzed using Analysis of Covariance (ANCOVA) adjusting for treatment, period, sequence and center with period baseline as a covariate and patient nested within sequence as a random effect. (NCT00557440)
Timeframe: 5, 30 minutes, 1, 2, 3, 4 hours, 11 hours 10 minutes, 11 hours 45 minutes, 12 hours 30 minutes, 14, 16, 18, 20, 22 hours, 23 hours 10 minutes, and 23 hours 45 minutes post-dosing.

,,
Interventionliters (Least Squares Mean)
5 minutes [N=36, 36, 37]30 minutes [N=36, 36, 36]1 hour [N=36, 36, 36]2 hours [N=36, 36, 36]3 hours [N=36, 36, 36]4 hours [N=36, 36, 35]11 hours 10 minutes [N=36, 35, 34]11 hours 45 minutes [N=36, 35, 32]12 hours 30 minutes [N=36, 35, 32]14 hours [N=36, 35, 32]16 hours [N=36, 35, 31]18 hours [N=35, 36, 33]20 hours [N=35, 36, 34]22 hours [N=35, 36, 34]23 hours 10 minutes [N=35, 36, 35]23 hours 45 minutes [N=36, 36, 34]24 hours post-dose trough [N=36, 36, 35]
Fluticasone/Salmeterol2.6322.7192.7712.7342.7242.6692.5702.5182.6592.7792.6812.7172.7072.6952.6762.6402.656
Indacaterol/Mometasone2.7132.7542.7602.7542.7282.7052.6852.6282.6672.7662.7202.7292.7252.6742.6962.6862.689
Placebo2.5542.5272.5252.4832.4252.3762.2952.2762.3592.4852.4542.5132.4792.4872.5302.5232.524

[back to top]

Forced Vital Capacity (FVC) at Single Time Points

"Vital capacity is the amount of air which can be forcibly exhaled from the lungs after taking the deepest breath possible.~FVC was analyzed using ANCOVA adjusting for treatment, period, sequence and center with period baseline as a covariate and patient nested within sequence as a random effect." (NCT00557440)
Timeframe: 5, 30 minutes, 1, 2, 3, 4 hours, 11 hours 10 minutes, 11 hours 45 minutes, 12 hours 30 minutes, 14, 16, 18, 20, 22 hours, 23 hours 10 minutes, and 23 hours 45 minutes post-dosing.

,,
Interventionliters (Least Squares Mean)
5 minutes [N= 36, 36, 37]30 minutes [N= 36, 36, 36]1 hour [N= 36, 36, 36]2 hours [N= 36, 36, 36]3 hours [N= 36, 36, 36]4 hours [N= 36, 36, 35]11 hours 10 minutes [N= 36, 35, 34]11 hours 45 minutes [N= 36, 35, 32]12 hours 30 minutes [N= 36, 35, 32]14 hours [N= 36, 35, 32]16 hours [N= 36, 35, 31]18 hours [N= 35, 36, 33]20 hours [N= 35, 36, 34]22 hours [N= 35, 36, 34]23 hours 10 minutes [N= 35, 36, 35]23 hours 45 minutes [N=36, 36, 34]
Fluticasone/Salmeterol3.8803.9333.9553.8993.9233.8613.8283.7363.8413.8943.7873.8663.8483.9063.8663.825
Indacaterol/Mometasone3.9173.9463.9454.0803.9253.8573.8963.8373.8333.9183.8963.8933.9033.8653.8703.866
Placebo3.8303.8393.8083.7423.7083.6653.6323.6073.6803.7593.7373.7843.7643.7643.8083.817

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 10

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium230.30
Salmeterol231.27

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 11

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium230.61
Salmeterol231.91

[back to top]

First Occurrence of COPD Exacerbations Treated With Systemic Steroids and Antibiotics

First occurrence analysed by Cox regression as time to first exacerbation treated with systemic steroids and antibiotics and reported as hazard ratio. An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionnumber of first occurrences (Number)
Tiotropium562
Salmeterol671

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 3

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium226.31
Salmeterol228.38

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 4

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium227.37
Salmeterol229.25

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 1

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium222.85
Salmeterol224.45

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 6

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium228.80
Salmeterol229.81

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 7

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium229.35
Salmeterol230.13

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 5

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium228.27
Salmeterol229.37

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 14

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium231.19
Salmeterol232.42

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 15

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium231.64
Salmeterol232.75

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 16

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium232.06
Salmeterol232.65

[back to top]

Number of Participants With Premature Discontinuation of Trial Medication

(NCT00563381)
Timeframe: 52 weeks

,
InterventionParticipants (Number)
Participants with (at least one) eventParticipants with no event
Salmeterol6483021
Tiotropium5853122

[back to top]

First Occurrence of COPD Exacerbations Treated With Systemic Steroids

First occurrence analysed by Cox regression as time to first exacerbation treated with systemic steroids and reported as hazard ratio. An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionnumber of first occurrences (Number)
Tiotropium715
Salmeterol852

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 2

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium225.15
Salmeterol227.21

[back to top]

Number of Participants With at Least One COPD Exacerbation Leading to Hospitalisation

An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

,
InterventionParticipants (Number)
Participants with (at least one) eventParticipants with no event
Salmeterol3363333
Tiotropium2623445

[back to top]

Number of Participants With at Least One COPD Exacerbation

An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

,
InterventionParticipants (Number)
Participants with (at least one) eventParticipants with no event
Salmeterol14142255
Tiotropium12772430

[back to top]

First Occurrence of COPD Exacerbations Treated With Antibiotics

First occurrence analysed by Cox regression as time to first exacerbation treated with antibiotics and reported as hazard ratio. An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionnumber of first occurrences (Number)
Tiotropium1154
Salmeterol1259

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 9

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium229.72
Salmeterol230.57

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 8

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium229.95
Salmeterol230.43

[back to top]

First Occurrence of (Moderate or Severe) COPD Exacerbation

First occurrence analysed by Cox regression as time to first exacerbation and reported as hazard ratio. An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionnumber of first occurrences (Number)
Tiotropium1277
Salmeterol1414

[back to top]

Occurrence of Premature Discontinuation of Trial Medication

Occurrence analysed by Cox regression as time to premature discontinuation of trial medication and reported as hazard ratio (NCT00563381)
Timeframe: 52 weeks

Interventionnumber of first occurrences (Number)
Tiotropium585
Salmeterol648

[back to top]

First Occurrence of COPD Exacerbation or Discontinuation of Trial Medication Because of Worsening of Underlying Disease, Whichever Comes First

First occurrence analysed by Cox regression as time to first exacerbation or discontinuation of trial medication because of worsening of underlying disease, whichever comes first and reported as hazard ratio. An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionnumber of first occurrences (Number)
Tiotropium1316
Salmeterol1448

[back to top]

First Occurrence of COPD Exacerbation Leading to Hospitalization

First occurrence analysed by Cox regression as time to first exacerbation leading to hospitalisation and reported as hazard ratio. An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionnumber of first occurrences (Number)
Tiotropium262
Salmeterol336

[back to top]

COPD Exacerbations Treated With Systemic Steroids Per Patient-year

An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionexacerbations per patient-year (Mean)
Tiotropium0.33
Salmeterol0.41

[back to top]

COPD Exacerbations Treated With Systemic Steroids and Antibiotics Per Patient-year

An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionexacerbations per patient-year (Mean)
Tiotropium0.23
Salmeterol0.28

[back to top]

COPD Exacerbations Treated With Antibiotics Per Patient-year

An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

Interventionexacerbations per patient-year (Mean)
Tiotropium0.53
Salmeterol0.59

[back to top]

COPD Exacerbations Per Patient-year Leading to Hospitalisation

An exacerbation was defined as an increase or new onset of more than 1 symptom (cough, sputum, wheezing, dyspnoea, chest tightness), with at least 1 symptom lasting at least 3 days and requiring treatment with systemic steroids and/or antibiotics (moderate exacerbation) or hospitalisation (severe exacerbation). (NCT00563381)
Timeframe: 52 weeks

InterventionHospitalizations per patient-year (Mean)
Tiotropium0.09
Salmeterol0.13

[back to top]

COPD Exacerbations Per Patient-year

(NCT00563381)
Timeframe: 52 weeks

Interventionexacerbations per patient-year (Mean)
Tiotropium0.64
Salmeterol0.72

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 13

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium231.23
Salmeterol231.89

[back to top]

Pre-dose Morning PEFR Measured by Patients at Home During the First Four Months of Randomised Treatment (Weekly Means Will be Calculated), Week 12

PEFR means peak expiratory flow rate and is measured in liter per minute (NCT00563381)
Timeframe: 16 weeks

Interventionliter per minute (L/min) (Mean)
Tiotropium231.04
Salmeterol232.04

[back to top]

Change Between Week 14 and Week 0 in the Albuterol Rescue Puffs Per Day

Total number of puffs from the albuterol (rescue) inhaler during the previous 24 hours (excluding those puffs for preventive use). (NCT00565266)
Timeframe: Albuterol rescue puffs were measured daily during each of the three 14-week treatment periods. The primary analysis constructed the change between week 14 and week 0.

Interventionpuffs per day (Least Squares Mean)
Tio + 1xICS-0.11
LABA + 1xICS-0.16
2xICS-0.07

[back to top]

Change Between Week 14 and Week 0 in the Asthma Control Questionnaire Score

Scores on the Asthma Control Questionnaire range from 0 to 6, with a higher score indicating worse asthma control. (NCT00565266)
Timeframe: The asthma control questionnaire score was measured on four occasions during each of the three 14-week treatment periods. The primary analysis constructed the change between week 14 and week 0.

Interventionunits on a scale (Least Squares Mean)
Tio + 1xICS-0.22
LABA + 1xICS-0.31
2xICS-0.03

[back to top]

Change Between Week 14 and Week 0 in the Forced Expiratory Volume in One Second (FEV1)

(NCT00565266)
Timeframe: FEV1 was measured on four occasions during each of the three 14-week treatment periods. The primary analysis constructed the change between week 14 and week 0.

Interventionliters (Least Squares Mean)
Tio + 1xICS0.12
LABA + 1xICS0.01
2xICS0.02

[back to top]

Change Between Week 14 and Week 0 in the Morning (AM) Peak Expiratory Flow (PEF)

(NCT00565266)
Timeframe: AM PEF was measured daily during each of the three 14-week treatment periods. The primary analysis constructed the change between week 14 and week 0.

InterventionLiters per minute (Least Squares Mean)
Tio + 1xICS24.4
LABA + 1xICS18.0
2xICS-1.4

[back to top]

Change Between Week 14 and Week 0 in the Proportion of Asthma Control Days

An asthma control day was defined as a day in which there were no symptoms and no albuterol (rescue) puffs. (NCT00565266)
Timeframe: An asthma control day was determined daily during each of the three 14-week treatment periods. The primary analysis constructed the change between week 14 and week 0.

Interventionproportion of asthma control days (Least Squares Mean)
Tio + 1xICS0.13
LABA + 1xICS0.14
2xICS0.05

[back to top]

Change Between Week 14 and Week 0 in Asthma Symptoms

"Asthma symptoms were recorded as 0 (absent = no symptom )~(mild = symptom was minimally troublesome, i.e. not sufficient to interfere with normal daily activity or sleep)~(moderate = symptom was sufficiently troublesome to interfere with normal daily activity or sleep)~(severe = symptom was so severe as to prevent normal activity and/or sleep )" (NCT00565266)
Timeframe: Asthma symptoms were measured daily during each of the three 14-week treatment periods. The primary analysis constructed the change between week 14 and week 0.

Interventionunits on a scale (Least Squares Mean)
Tio + 1xICS-0.09
LABA + 1xICS-0.04
2xICS0.03

[back to top]

Change Between Week 14 and Week 0 in the Asthma Quality-of-life Questionnaire Score

Scores on the Asthma Quality-of-Life Questionnaire range from 1 to 7, with a higher score indicating a better quality of life. (NCT00565266)
Timeframe: The asthma quality-of-life questionnaire score was measured on four occasions during each of the three 14-week treatment periods. The primary analysis constructed the change between week 14 and week 0.

Interventionunits on a scale (Least Squares Mean)
Tio + 1xICS0.15
LABA + 1xICS0.28
2xICS0.05

[back to top]

St. George's Respiratory Questionnaire (SGRQ) Total Score After 12 Weeks of Treatment

SGRQ is a health related quality of life questionnaire consisting of 76 items in three sections: symptoms, activity and impacts. The total score is 0 to 100 with a higher score indicating poorer health status. The mixed model used baseline SGRQ total score, FEV1 prior to and 30 minutes post inhalation of salbutamol/albuterol, and FEV1 prior to and one hour post inhalation of ipratropium as covariates. (NCT00567996)
Timeframe: Week 12

InterventionScore on a scale (Least Squares Mean)
Indacaterol 150 μg36.4
Salmeterol 50 μg38.5
Placebo42.6

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) After 12 Weeks of Treatment

Spirometry was conducted according to internationally accepted standards. Trough FEV1 was defined as the average of the 23 hour 10 minute and 23 hour 45 minute post-dose FEV1 readings. Mixed model used baseline FEV1, FEV1 prior to and 10-15 minutes post inhalation of salbutamol/albuterol, and FEV1 prior to and 1 hour post inhalation of ipratropium as covariates. (NCT00567996)
Timeframe: Week 12

InterventionLiters (Least Squares Mean)
Indacaterol 150 μg1.45
Salmeterol 50 μg1.39
Placebo1.28

[back to top]

"Percentage of COPD Days of Poor Control During 26 Weeks of Treatment"

"Participants rated their symptoms on a scale of 0=none to 3=severe. A Chronic Obstructive Pulmonary Disease (COPD) day of poor control was defined as any day in the participants diary with a score >=2 (moderate or severe) for at least 2 of 5 symptoms (cough, wheeze, production of sputum, color of sputum, breathlessness). The mixed model used baseline percentage of days of poor control, FEV1 prior to and 30 minutes post inhalation of salbutamol/albuterol, and FEV1 prior to and one hour post inhalation of ipratropium as covariates." (NCT00567996)
Timeframe: Up to 26 weeks

InterventionPercentage of days (Least Squares Mean)
Indacaterol 150 μg34.1
Salmeterol 50 μg34.1
Placebo38.1

[back to top]

Comparison of the Maximum Percent Fall in FEV1 From Pre-salmeterol Baseline to the End of the 2-week Treatment Period Between Arg/Arg and Gly/Gly Patients

(NCT00595361)
Timeframe: 2 weeks from pre-salmeterol baseline

Intervention% fall FEV1 (Mean)
Arg/Arg5.9
Gly/Gly4.3

[back to top]

Comparison of the Maximum Percent Fall in FEV1 After 1st Dose of Salmeterol to the End of the 2-week Treatment Period Between Arg/Arg and Gly/Gly Subjects

(NCT00595361)
Timeframe: 2 weeks after 1st dose of Salmeterol

Intervention% fall FEV1 (Mean)
Arg/Arg-12.6
Gly/Gly-16.5

[back to top]

Comparison of the Maximum Percent Fall in FEV1 After Exercise Challenge at the End of the 2-week Treatment Period Between Arg/Arg and Gly/Gly Patients

(NCT00595361)
Timeframe: 2 weeks after exercise challenge

Intervention% fall FEV1 (Mean)
Arg/Arg12.6
Gly/Gly16.5

[back to top]

Trough FEV1 Assessed After 14 Days of Dosing for All Other Treatment Comparisons

Trough FEV1 was assessed by performing spirometry measurements in the clinic for each treatment period. On the morning and evening of Day 15 trough FEV1 (i.e. mean of measurements performed 23 h 10 min and 23 h 45 min post-dose) were assessed. An analysis of covariance (ANCOVA) model was used with the (period) baseline FEV1 as covariate. The (period) baseline FEV1 was defined as the value measured before the study drug administration in that treatment period. (NCT00615030)
Timeframe: After 14 days of dosing

InterventionLiters (Least Squares Mean)
Indacaterol Morning1.56
Indacaterol Evening1.57
Salmeterol Morning1.51
Salmeterol Evening1.46
Placebo Morning1.36
Placebo Evening1.37

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) Following 14 Days of Evening Dosing of Indacaterol Versus Placebo

"Trough FEV1 was assessed by performing spirometry measurements in the clinic for each treatment period. For the primary efficacy variable, trough FEV1 is the mean of two measurements taken at 23h 10 min and 23h 45 min post dose. The primary variable was analyzed using an analysis of covariance (ANCOVA) model with the (period) baseline FEV1 as covariate.~The (period) baseline FEV1 was defined as the value measured before the study drug administration in that treatment period." (NCT00615030)
Timeframe: After 14 days of treatment

InterventionLiters (Least Squares Mean)
Indacaterol Evening1.57
Placebo1.37

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 10 Hours Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 10 hours post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.43
Placebo to Indacaterol1.25
Salmeterol 50 μg1.36

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 11 Hours 10 Minutes Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 11 hours 10 minutes post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.45
Placebo to Indacaterol1.25
Salmeterol 50 μg1.35

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 11 Hours 45 Minutes Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 11 hours 45 minutes post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.46
Placebo to Indacaterol1.24
Salmeterol 50 μg1.35

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 14 Hours Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 14 hours post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.45
Placebo to Indacaterol1.24
Salmeterol 50 μg1.39

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 15 Minutes Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 15 minutes post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.47
Placebo to Indacaterol1.27
Salmeterol 50 μg1.41

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 2 Hours Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 2 hours post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.50
Placebo to Indacaterol1.27
Salmeterol 50 μg1.44

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 20 Hours 10 Minutes Post-dose at the End of Each Treatment Period (Day 15)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 20 hours 10 minutes post-dose at the end of each treatment period (Day 15)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.36
Placebo to Indacaterol1.17
Salmeterol 50 μg1.31

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 20 Hours 45 Minutes Post-dose at the End of Each Treatment Period (Day 15)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 20 hours 45 minutes post-dose at the end of each treatment period (Day 15)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.40
Placebo to Indacaterol1.19
Salmeterol 50 μg1.35

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 23 Hours 10 Minutes Post-dose at the End of Each Treatment Period (Day 15)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 23 hours 10 minutes post-dose at the end of each treatment period (Day 15)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.48
Placebo to Indacaterol1.24
Salmeterol 50 μg1.37

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 23 Hours 45 Minutes Post-dose at the End of Each Treatment Period (Day 15)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 23 hours 45 minutes post-dose at the end of each treatment period (Day 15)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.45
Placebo to Indacaterol1.28
Salmeterol 50 μg1.38

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 3 Hours Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 3 hours post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.51
Placebo to Indacaterol1.29
Salmeterol 50 μg1.45

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 30 Minutes Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 30 minutes post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.49
Placebo to Indacaterol1.26
Salmeterol 50 μg1.42

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 4 Hours Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 4 hours post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.49
Placebo to Indacaterol1.29
Salmeterol 50 μg1.44

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 5 Hours Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 5 hours post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.49
Placebo to Indacaterol1.26
Salmeterol 50 μg1.45

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 5 Minutes Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 5 minutes post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.44
Placebo to Indacaterol1.24
Salmeterol 50 μg1.36

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 6 Hours Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 6 hours post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.48
Placebo to Indacaterol1.29
Salmeterol 50 μg1.42

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 8 Hours Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 8 hours post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.44
Placebo to Indacaterol1.27
Salmeterol 50 μg1.40

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose at the End of Each Treatment Period (Day 15)

FEV1 was measured with spirometry conducted according to internationally accepted standards. Trough FEV1 was defined as the average of measurements made 23 hours 10 minutes and 23 hours 45 minutes post-dose at the end of each treatment period. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: After 14 days

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.46
Placebo to Indacaterol1.26
Salmeterol 50 μg1.37

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 22 Hours Post-dose at the End of Each Treatment Period (Day 15)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 22 hours post-dose at the end of each treatment period (Day 15)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.43
Placebo to Indacaterol1.25
Salmeterol 50 μg1.38

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) 1 Hour Post-dose at the End of Each Treatment Period (Day 14)

FEV1 was measured with spirometry conducted according to internationally accepted standards. The analysis included baseline FEV1, defined as the average of the FEV1 values measured at 50 and 15 minutes prior to the first study drug administration in that period, as a covariate. (NCT00622635)
Timeframe: 1 hour post-dose at the end of each treatment period (Day 14)

InterventionLiters (Least Squares Mean)
Indacaterol 300 μg1.49
Placebo to Indacaterol1.26
Salmeterol 50 μg1.42

[back to top]

Number of Severe Asthma Exacerbations

Total number of severe asthma exacerbations per treatment group (NCT00628758)
Timeframe: 26 weeks

InterventionSevere Exacerbations (Number)
Symbicort10
Conventional BP10

[back to top]

Mean Use of As-needed Medication Per Day During Treatment Period

Mean use of as-needed medication per day during treatment period (NCT00628758)
Timeframe: Daily recording during the treatment period of 26 weeks

Interventioninhalations per day (Mean)
Symbicort0.91
Conventional BP0.68

[back to top]

Change in Standardised Asthma Quality of Life Questionnaire (AQLQ(S)) Score

Quality-of-Life assessment; grouped in four domains;activity limitation, symptoms, emotional function and exposure to environmental stimuli, using with a scale from 1 to 7 where 1 represents the greatest possible impairment and 7 represents the least impairment. (NCT00628758)
Timeframe: Baseline and 26 weeks

InterventionUnits on a scale (Mean)
Symbicort3.98
Conventional BP3.97

[back to top]

Time to First Severe Asthma Exacerbation

Time to severe exacerbation among patients (NCT00628758)
Timeframe: 26 weeks

Interventiondays (Mean)
Symbicort120.3
Conventional Best Practice (BP)103.7

[back to top]

Mean Change From Baseline in Forced Expiratory Volume in One Second (FEV1) 2 Hours Post-dose of Blinded Study Drug

The primary efficacy analysis was mean change from baseline in 2-hour post-dose FEV1 compared between the two treatment groups at Endpoint. Change from baseline was calculated as the value at Endpoint minus the baseline value. FEV1, which is assessed using spirometry, is the maximal amount of air you can forcefully exhale in one second. Endpoint was defined as the last scheduled observation for 2 hour post-dose FEV1 during the 12-week treatment period. (NCT00633217)
Timeframe: 2 hours after administration of blinded study drug; Baseline through Week 12

Interventionmilliliters (mL) (Mean)
HFA MDI 230/42 mcg and Matching DISKUS Placebo155
DISKUS 250/50 mcg and Matching HFA MDI Placebo150

[back to top]

Mean Change From Baseline in Peak Expiratory Flow

The peak expiratory flow is a measure of the amount of air that can be pushed through the airways in a single rapid exhalation. This is measured by a peak flow meter which is a hand held device. Change from baseline was calculated as the average value over Weeks 1-12 minus the baseline value. (NCT00633217)
Timeframe: Baseline through Week 12

InterventionLiters/minute (L/min) (Mean)
HFA MDI 230/42 mcg and Matching DISKUS Placebo21.8
DISKUS 250/50 mcg and Matching HFA MDI Placebo18.7

[back to top]

Mean Change From Baseline in AM Pre-dose FEV1

Change from baseline was calculated as the value at Endpoint minus the baseline value. AM pre-dose FEV1, which is assessed using spirometry, is the maximum amount of air you can forcefully exhale in one second prior to taking the morning dose of study drug. Endpoint was defined as the last scheduled observation for AM pre-dose FEV1 during the 12-week treatment period. (NCT00633217)
Timeframe: Measurement of FEV1 prior to study drug administration; Baseline through Week 12

InterventionmL (Mean)
HFA MDI 230/42 mcg and Matching DISKUS Placebo74
DISKUS 250/50 mcg and Matching HFA MDI Placebo77

[back to top]

Response in Peak Expiratory Flow Rate (PEF) Area Under the Curve From 12 to 24 Hours (AUC12-24)

"PEF(L/min) AUC12-24(h) response is defined as the change from baseline. AUC12-24(h) was calculated as the area under the curve from 12 to 24 hours using the trapezoidal rule, divided by the full duration (12 hours) to report in liter/minutes.~PEF AUC12-24h response = PEF AUC12-24h - PEF (Baseline). The PEF baseline value is defined as the pre-dose PEF measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior and 30 min, 60 min, 2, 10, 11 and 12 hours after inhalation of the evening dose after 6 weeks of treatment.

InterventionLiter/minutes (L/min) (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)7.3
18µg Tiotropium (Tio18GEL)-1.3
50 µg Salmeterol MDPI (Salm50DPI)-3.4
18 µg Tiotropium Free Combination (T18GEL+S_DPI)20.0

[back to top]

Response in Peak Forced Expiratory Volume in 1 Second (FEV1)

"Peak FEV1 was defined as the highest FEV1 reading observed within 3 hours after inhalation of the last morning dose of each randomized treatment. Peak FEV1 response is defined as change from baseline:~Peak FEV1 response = Peak FEV1 - FEV1 (Baseline). The FEV1 baseline value is defined as the pre-dose FEV1 measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and within 3 hours post-morning dose after 6 weeks of treatment.

InterventionLiter (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.296
18µg Tiotropium (Tio18GEL)0.229
50 µg Salmeterol MDPI (Salm50DPI)0.161
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.320

[back to top]

Response in Morning and Evening Peak Expiratory Flow Rate (PEF), Recorded by Patients at Home

"The mean PEF is defined as the mean of the values obtained during the weeks after the first three weeks of treatment. Morning and evening mean PEF were calculated and analyzed separately. PEF was measured twice daily (in the morning prior to inhalation of study medication and in the evening prior to inhalation of study medication).~Morning and evening mean PEF response are defined as the change from morning and evening baseline, respectively.~Morning and evening mean PEF baseline are defined as the mean of the morning and evening values, respectively obtained from the last week preceding the randomization visit.~Mean is adjusted for treatment, center, treatment period and patient within center." (NCT00662792)
Timeframe: At baseline and last 3 weeks of 6-week treatment period.

,,,
InterventionLiter / minute (L/min) (Mean)
PEF, morningPEF, evening
18 µg Tiotropium Free Combination (T18GEL+S_DPI)14.815.2
18µg Tiotropium (Tio18GEL)1.25.8
50 µg Salmeterol MDPI (Salm50DPI)0.6-6.4
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)6.816.7

[back to top]

Response in Morning and Evening Forced Expiratory Volume in 1 Second (FEV1) Recorded by Participants at Home

"Per treatment period, the morning mean FEV1 (mean of the pre-dose morning FEV1 measurements) and evening mean FEV1 (mean of the pre-dose evening FEV1 measurement) were calculated. Per treatment period the data obtained after the first 3 weeks were used for calculating these means.~Morning and evening mean FEV1 responses are defined as the change from morning and evening baseline, respectively. The baseline values, morning and evening mean FEV1(Baseline), are defined as the mean of the morning and evening values, respectively obtained from the last week preceding the randomization visit .~Mean is adjusted for treatment, centre, treatment period and patient within centre." (NCT00662792)
Timeframe: At baseline and last 3 weeks of 6-week treatment period.

,,,
InterventionLiter (L) (Mean)
FEV1, morningFEV1, evening
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.0750.075
18µg Tiotropium (Tio18GEL)0.0130.038
50 µg Salmeterol MDPI (Salm50DPI)0.026-0.010
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.0520.094

[back to top]

Response in Mean Number of Puffs of Rescue Medication

"Response in mean number of puffs of rescue medication. Per treatment period, the response in mean number of puffs rescue medication used was calculated, for day-time (from inhalation of morning dose until 12 hours thereafter), night-time (from inhalation of evening dose until 12 hours thereafter) and 24h-total (from inhalation of morning dose until 24 hours thereafter) separately. Per 6-week treatment period the data obtained after the first 3 weeks was used for calculating means. Night-time, day-time and 24h-total mean number of puffs rescue medication used responses are defined as the change from night-time, day-time and 24h-total baseline, respectively.~The baseline values, night-time, day-time and 24h-total mean mean number of puffs rescue medication used (Baseline), are defined as the mean of the night-time, day-time and 24h-total values, respectively obtained from the last week preceding the randomisation visit." (NCT00662792)
Timeframe: At baseline and last 3 weeks of 6-week treatment period.

,,,
InterventionPuffs (Mean)
DaytimeNight-timeOver 24 hours
18 µg Tiotropium (Tio18GEL)-0.270.01-0.23
18 µg Tiotropium Free Combination (T18GEL+S_DPI)-0.65-0.28-0.92
50 µg Salmeterol MDPI (Salm50DPI)-0.25-0.07-0.30
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)-0.61-0.16-0.76

[back to top]

Response in Mean Number of Days With Rescue Medication Use

"Response (change from baseline) in mean number of days with rescue medication use in day-time, night-time and 24-hours. Per treatment period, the response in mean number of days using rescue medication was calculated for day-time (from inhalation of morning dose until 12 hours thereafter), night-time (from inhalation of evening dose until 12 hours thereafter) and 24h-total (from inhalation of morning dose until 24 hours thereafter) separately.~Per 6-week treatment period the data obtained after the first 3 weeks was used for calculating means. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and last 3 weeks of 6-week treatment period.

,,,
InterventionDays (Mean)
DaytimeNight-time24 hours
18 µg Tiotropium (Tio18GEL)-0.01-0.06-0.04
18 µg Tiotropium Free Combination (T18GEL+S_DPI)-0.11-0.14-0.14
50 µg Salmeterol MDPI (Salm50DPI)-0.06-0.07-0.06
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)-0.08-0.15-0.13

[back to top]

Response in Individual Peak Expiratory Flow (PEF) Over a 24 Hour Observation Period

"Response in individual peak expiratory flow (PEF) over a 24 hour observation period. Response is defined as change from baseline.~Means are adjusted for treatment, centre, treatment period and patient within centre." (NCT00662792)
Timeframe: At baseline, pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 12.5, 13, 14, 22, 23, and 24 hours post morning dose after 6 weeks of treatment.

,,,
InterventionLiter/minutes (L/min) (Mean)
0 hour0.5 hour1 hour2 hours3 hours4 hours6 hours8 hours10 hours12 hours12.5 hours13 hours14 hours22 hours23 hours24 hours
18 µg Tiotropium Free Combination (T18GEL+S_DPI)22.934.341.047.049.946.538.935.528.826.826.625.327.910.118.124.0
18µg Tiotropium (Tio18GEL)11.320.122.227.627.926.425.023.319.011.85.55.84.5-11.72.39.6
50 µg Salmeterol MDPI (Salm50DPI)7.113.714.618.517.117.211.18.61.9-0.6-0.72.61.4-9.7-5.72.0
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)14.430.835.542.245.041.937.833.926.923.413.612.015.6-4.29.114.0

[back to top]

Response in Individual Forced Vital Capacity (FVC) Over a 24 Hour Observation Period

Response in forced vital capacity (FVC) over a 24 hour observation period. Response is defined as change from baseline. (NCT00662792)
Timeframe: At baseline, pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 12.5, 13, 14, 22, 23 and 24 hours post morning dose after 6 weeks of treatment.

,,,
InterventionLiter (Mean)
0 hour0.5 hour1 hour2 hours3 hours4 hours6 hours8 hours10 hours12 hours12.5 hours13 hours14 hours22 hours23 hours24 hours
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.2290.3950.4110.4640.4570.4630.3990.3550.3060.2580.2730.2660.2870.1910.2430.280
18µg Tiotropium (Tio18GEL)0.1650.3020.3320.3300.3190.3120.2540.2250.1850.1420.1310.1160.1220.0010.0980.153
50 µg Salmeterol MDPI (Salm50DPI)0.0950.2000.2200.2430.2520.2230.1790.1410.0510.0510.0660.1060.082-0.0140.0430.089
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.1390.3540.3860.4090.4250.3960.3680.3090.2640.2290.2060.1940.2250.0810.1760.208

[back to top]

Response in Individual Forced Expiratory Volume in 1 Second (FEV1) Over a 24 Hour Observation Period

"Response in individual forced expiratory volume in 1 second (FEV1) over a 24 hour observation period. Response is defined as change from baseline.~Means are adjusted for treatment, centre, treatment period and patient within centre." (NCT00662792)
Timeframe: At baseline, pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 12.5, 13, 14, 22, 23, and 24 hours post morning dose after 6 weeks of treatment.

,,,
InterventionLiter (L) (Mean)
0 hour0.5 hour1 hour2 hour3 hour4 hour6 hour8 hour10 hour12 hour12.5 hour13 hour14 hour22 hour23 hour24 hour
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.0970.2040.2360.2770.2770.2620.2180.1850.1660.1370.1470.1530.1720.0680.1160.147
18µg Tiotropium (Tio18GEL)0.0320.1290.1390.1630.1670.1620.1210.0980.0800.0600.0480.0430.040-0.0570.0180.058
50 µg Salmeterol MDPI (Salm50DPI)0.0030.0680.0840.1080.1110.1020.0640.0440.006-0.0070.0210.0350.031-0.0340.0080.024
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.0620.1800.2110.2420.2570.2310.2090.1670.1380.1170.1010.1050.1150.0050.0710.112

[back to top]

Response in Peak PEF (Peak Expiratory Flow Rate)

"Peak PEF was defined as the highest PEF reading observed within 3 hours after inhalation of the last morning dose of randomized treatment.~Peak PEF response is defined as change from baseline:~Peak PEF response = Peak PEF - PEF (Baseline). The PEF baseline value is defined as the pre-dose PEF measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and within 3 hours post-morning dose after 6 weeks of treatment.

InterventionLiter/minutes (L/min) (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)53.9
18µg Tiotropium (Tio18GEL)40.6
50 µg Salmeterol MDPI (Salm50DPI)30.8
18 µg Tiotropium Free Combination (T18GEL+S_DPI)59.0

[back to top] [back to top]

Response in Average Shortness of Breath (SOB) Score at Night

"Response in average shortness of breath (SOB) score at night. The SOB measured the shortness of breath, ranging from 1 to 5, where 1 = not at all, 2 = a little bit, 3 = somewhat, 4 = quite a bit and 5 = very much. A higher score indicates a worse outcome.~Per 6-week treatment period the data obtained after the first 3 weeks was used for calculating the mean." (NCT00662792)
Timeframe: At baseline and last 3 weeks of 6-week treatment period.

InterventionScore on a scale (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)-0.06
18 µg Tiotropium (Tio18GEL)-0.04
50 µg Salmeterol MDPI (Salm50DPI)-0.06
18 µg Tiotropium Free Combination (T18GEL+S_DPI)-0.11

[back to top]

Response in Forced Expiratory Volume in 1 Second (FEV1) Area Under the Curve From 0 - 12 Hours (AUC0-12)

"FEV1 AUC was defined as the area under the FEV1 curve normalized for time. It was calculated from time 0 to 12 h (FEV1 AUC0-12), using the trapezoidal rule divided by the corresponding duration (12 h) to give the results in liter (L). FEV1 AUC0-12h response is defined as the change from baseline:~FEV1 AUC0-12h response = FEV1 AUC0-12h - FEV1 (Baseline). The FEV1 baseline value is defined as the pre-dose FEV1 measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior to inhalation and 30 min, 60 min, 2, 3, 4, 6, 8, 10 and 12 hours after inhalation of the morning dose after 6 weeks of treatment.

InterventionLiter (L) (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.187
18 µg Tiotropium (Tio18GEL)0.117
50 µg Salmeterol MDPI (Salm50DPI)0.057
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.211

[back to top]

Response in Forced Expiratory Volume in 1 Second (FEV1) Area Under the Curve From 0-24 Hours (AUC0-24)

"FEV1 AUC was defined as the area under the FEV1 curve normalized for time. It was calculated from time 0 to 24 h (FEV1 AUC0-24), using the trapezoidal rule divided by the corresponding duration (24 h) to give the results in liter (L). FEV1 AUC0-24h response is defined as the change from baseline:~FEV1 AUC0-24h response = FEV1 AUC0-24h - FEV1 (Baseline). The FEV1 baseline value is defined as the pre-dose FEV1 measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior and 60 min, 2, 3, 4, 6, 8, 10 and 12 hours after inhalation of the morning dose and 30 min, 60 min, 2, 10, 11, and 12 hours after inhalation of the evening dose after 6 weeks of treatment.

InterventionLiter (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.128
18µg Tiotropium (Tio18GEL)0.060
50 µg Salmeterol MDPI (Salm50DPI)0.030
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.167

[back to top]

Response in Forced Expiratory Volume in Second (FEV1) Area Under the Curve From 12 - 24 Hours (AUC12 -24)

"The FEV1 AUC was defined as the area under the FEV1 curve (AUC) normalised for time. It was calculated from time 12 to 24 h (FEV1 AUC12-24), using the trapezoidal rule divided by the corresponding duration (i.e. 12 h) to give the results in L.~AUC12-24h response is defined as the change from baseline:~FEV1 AUC12-24h response = FEV1 AUC12-24h - FEV1 (Baseline). The FEV1 baseline value is defined as the pre-dose FEV1 measurement in the morning at the randomization visit (Visit 2) just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior to inhalation and 30 min, 60 min, 2, 10, 11, and 12 hours after inhalation of the evening dose after 6 weeks of treatment.

InterventionLiter (L) (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.068
18 µg Tiotropium (Tio18GEL)0.003
50 µg Salmeterol MDPI (Salm50DPI)0.003
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.124

[back to top]

Response in Forced Vital Capacity (FVC) Area Under the Curve From 0 - 24 Hours (AUC0-24)

The FVC AUC was defined as the area under the FVC curve (AUC) normalised for time. It was calculated from time 0 to 24 h (FVC AUC0-24), using the trapezoidal rule divided by the corresponding duration (i.e. 24 h) to give the results in L. AUC response was defined as the change from the baseline FVC; baseline was defined as the FVC measured on randomisation visit. Mean is adjusted mean. (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior and 60 min, 2, 3, 4, 6, 8, 10 and 12 hour after inhalation the morning dose and 30 min, 60 min, 2, 10, 11, and 12 hours after inhalation of the evening dose after 6 weeks of treatment.

InterventionLiter (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.250
18µg Tiotropium (Tio18GEL)0.165
50 µg Salmeterol MDPI (Salm50DPI)0.102
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.313

[back to top]

Response in Mean Number of Days With Night-time Awakenings

Response in mean number of days with night-time awakenings. Per treatment period, the mean number days with awakening during the night was calculated. Per 6-week treatment period the data obtained after the first 3 weeks was used for calculating this mean. Mean number of days with night-time awakenings response is defined as the change from baseline. The baseline value, mean number of days with night-time awakenings (Baseline), is defined as the mean of the number of days with night-time awakenings obtained from the last week preceding the randomization visit. (NCT00662792)
Timeframe: At baseline and last 3 weeks of 6-week treatment period.

InterventionDays (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)-0.06
18 µg Tiotropium (Tio18GEL)-0.06
50 µg Salmeterol MDPI (Salm50DPI)-0.05
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.07

[back to top]

Response in Mean Number of Days With Night-time Awakenings Due to Shortness of Breath (SOB)

"Per treatment period, the mean number days with awakening (only chronic obstructive pulmonary disease (COPD) related awakenings) during the night was calculated. Per 6-week treatment period the data obtained after the first 3 weeks was used for calculating the mean.~Mean number of days with COPD related awakenings response is defined as the change from baseline.~The baseline value, mean number of days with COPD related awakenings (Baseline), is defined as the mean of the number of days with COPD related awakenings obtained from the last week preceding the randomization visit." (NCT00662792)
Timeframe: At baseline and last 3 weeks of 6-week treatment period.

InterventionDays (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)-0.05
18 µg Tiotropium (Tio18GEL)-0.04
50 µg Salmeterol MDPI (Salm50DPI)-0.04
18 µg Tiotropium Free Combination (T18GEL+S_DPI)-0.07

[back to top]

Response in Means Number of Awakenings Due to Shortness of Breath (SOB)

Per treatment period, the mean number of awakening (only chronic obstructive pulmonary disease (COPD) related awakenings) during the night was calculated. Per 6-week treatment period the data obtained after the first 3 weeks was used for calculating this mean. Mean number of COPD related awakenings response is defined as the change from baseline. The baseline value, mean number of COPD related awakenings (Baseline), is defined as the mean of the number of days with COPD related awakenings obtained from the last week preceding the randomization visit. (NCT00662792)
Timeframe: At baseline and last 3 weeks of 6-week treatment period.

InterventionAwakenings (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)-0.02
18 µg Tiotropium (Tio18GEL)-0.02
50 µg Salmeterol MDPI (Salm50DPI)-0.04
18 µg Tiotropium Free Combination (T18GEL+S_DPI)-0.08

[back to top]

Response in Peak Expiratory Flow Rate (PEF) Area Under the Curve Form 0 to 12 Hours (AUC0-12)

"PEF(L/min) AUC0-12(h) response is defined as the change from baseline. AUC0-12(h) was calculated as the area under the curve from 0 to 12 hours using the trapezoidal rule, divided by the full duration (12 hours) to report in liter/minutes.~PEF AUC0-12h response = PEF AUC0-12h - PEF (Baseline). The PEF baseline value is defined as the pre-dose PEF measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior and 30 min, 60 min, 2, 3, 4, 6, 8, 10 and 12 hours after inhalation of the morning dose after 6 weeks of treatment.

InterventionLiter/minutes (L/min) (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)34.5
18µg Tiotropium (Tio18GEL)22.5
50 µg Salmeterol MDPI (Salm50DPI)10.2
18 µg Tiotropium Free Combination (T18GEL+S_DPI)37.8

[back to top]

Number of Patients With Marked Changes in Vital Signs

"Marked changes from baseline in vital signs were defined as followed:~Systolic blood pressure~Increase of ≥25 millimetre of mercury (mmHg) above baseline~Decrease below 100 mmHg if not at that level at baseline and a decrease of >10 mmHg below baseline~Diastolic blood pressure~Increase above 90 mmHg and an increase of >10 mmHg above baseline~Decrease below 60 mmHg if not at that level at baseline and a decrease of >10 mmHg below baseline~Pulse~Increase above 100 bpm if not at that level at baseline and an increase of >10 bpm above baseline~Decrease below 60 bpm if not at that level at baseline and a decrease of >10 bpm below baseline~Baseline is defined as the pre-dose measurement at randomisation visit." (NCT00662792)
Timeframe: At baseline and 6 hours following the morning dose of study medication after 6 weeks of treatment.

,,,
InterventionParticipants (Count of Participants)
Increase in systolic blood pressureIncrease in diastolic blood pressureIncrease in pulse rateDecrease in systolic blood pressureDecrease in diastolic blood pressureDecrease in pulse rate
18 µg Tiotropium (Tio18GEL)181610477
18 µg Tiotropium Free Combination (T18GEL+S_DPI)151413452
50 µg Salmeterol MDPI (Salm50DPI)16119337
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)18166356

[back to top]

Response in Peak Expiratory Flow Rate (PEF) Area Under the Curve From 0 to 24 Hours (AUC0-24)

"PEF(L/min) AUC0-24(h) response is defined as the change from baseline. AUC0-24(h) was calculated as the area under the curve from 0 to 24 hours using the trapezoidal rule, divided by the full duration (24 hours) to report in liter/minutes.~PEF AUC0-24h response = PEF AUC0-24h - PEF (Baseline). The PEF baseline value is defined as the pre-dose PEF measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior and 60 min, 2, 3, 4, 6, 8, 10 and 12 hours after inhalation of the morning dose and 30 min, 60 min, 2, 10, 11, and 12 hours after inhalation of the evening dose after 6 weeks of treatment.

InterventionLiter/minutes (L/min) (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)20.8
18µg Tiotropium (Tio18GEL)10.6
50 µg Salmeterol MDPI (Salm50DPI)3.4
18 µg Tiotropium Free Combination (T18GEL+S_DPI)28.9

[back to top]

Response in Forced Vital Capacity (FVC) Area Under the Curve From 12 to 24 Hours (AUC12-24)

"The FVC AUC was defined as the area under the FVC curve (AUC) normalised for time. It was calculated from time 12 to 24 h (FVC AUC12-24), using the trapezoidal rule divided by the corresponding duration (i.e. 12 h) to give the results in L.~AUC12-24h response is defined as the change from baseline:~FVC AUC12-24h response = FVC AUC12-24h - FVC (Baseline). The FVC baseline value is defined as the pre-dose FVC measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior to inhalation and 30 min, 60 min, 2, 10, 11 and 12 hours after inhalation of the evening dose after 6 weeks of treatment.

InterventionLiter (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.163
18µg Tiotropium (Tio18GEL)0.076
50 µg Salmeterol MDPI (Salm50DPI)0.043
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.245

[back to top]

Response in Forced Vital Capacity (FVC) Area Under the Curve From 0 to 12 Hours (AUC0-12)

"FVC AUC was defined as the area under the FVC curve normalized for time. It was calculated from time 0 to 12 h (FVC AUC0-12), using the trapezoidal rule divided by the corresponding duration (12 h) to give the results in liter (L). FVC AUC0-12h response is defined as the change from baseline:~FVC AUC0-12h response = FVC AUC0-12h - FVC (Baseline). The baseline value for FVC based parameters is defined as the pre-dose FVC measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 10 minutes (min) prior to inhalation and 30 min, 60 min, 2, 3, 4, 6, 8, 10 and 12 hours after inhalation of the morning dose after 6 weeks of treatment.

InterventionLiter (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.337
18µg Tiotropium (Tio18GEL)0.253
50 µg Salmeterol MDPI (Salm50DPI)0.160
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.381

[back to top]

Response in Peak Forced Vital Capacity (FVC)

"Peak FEV1 was defined as the highest FEV1 reading observed within 3 hours after inhalation of the last morning dose of each randomized treatment.~Peak FEV1 response is defined as change from baseline:~Peak FEV1 response = Peak FEV1 - FEV1 (Baseline). The FEV1 baseline value is defined as the pre-dose FEV1 measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and within 3 hours post-morning dose after 6 weeks of treatment.

InterventionLiter (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.502
18µg Tiotropium (Tio18GEL)0.449
50 µg Salmeterol MDPI (Salm50DPI)0.359
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.556

[back to top]

Response in Trough Peak Expiratory Flow Rate (PEF)

"Trough PEF is determined at the end of each treatment period and is defined as the pre-dose PEF measured just prior to the last administration of the morning dose of randomized treatment. Trough PEF response is defined as the change from baseline:~Trough PEF response = Trough PEF - PEF (Baseline) The PEF baseline value is defined as the pre-dose PEF measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 5 minutes prior to the last administration of the morning dose after 6 weeks of treatment.

InterventionLiter/minutes (L/min) (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)14.4
18µg Tiotropium (Tio18GEL)11.3
50 µg Salmeterol MDPI (Salm50DPI)7.1
18 µg Tiotropium Free Combination (T18GEL+S_DPI)22.9

[back to top]

Response in Trough Forced Vital Capacity (FVC)

"Trough FVC1 is determined at the end of each 6-week treatment period and is defined as the pre-dose FVC1 measured just prior to the last administration of the morning dose of randomized treatment.~Trough FVC1 response is defined as the change from baseline:~Trough FVC1 response = Trough FVC1 - FVC1 (Baseline) The FVC1 baseline value is defined as the pre-dose FVC1 measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 5 minutes prior to the last administration of the morning dose after 6 weeks of treatment.

InterventionLiter (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.139
18µg Tiotropium (Tio18GEL)0.165
50 µg Salmeterol MDPI (Salm50DPI)0.095
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.229

[back to top]

Response in Trough Forced Expiratory Volume in 1 Second (FEV1)

"Trough FEV1 is determined at the end of each treatment period and is defined as the pre-dose FEV1 measured just prior to the last administration of the morning dose of randomized treatment.~Trough FEV1 response is defined as the change from baseline:~Trough FEV1 response = Trough FEV1 - FEV1 (Baseline) The FEV1 baseline value is defined as the pre-dose FEV1 measurement in the morning at the randomization visit just prior to administration of the first dose of randomized treatment. Mean is adjusted mean." (NCT00662792)
Timeframe: At baseline and 5 minutes prior to the last administration of the morning dose after 6 weeks of treatment.

InterventionLiter (Mean)
7.5 µg /25 µg Tio /Salmeterol (T+S_PE)0.062
18µg Tiotropium (Tio18GEL)0.032
50 µg Salmeterol MDPI (Salm50DPI)0.003
18 µg Tiotropium Free Combination (T18GEL+S_DPI)0.097

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) at 5 Minutes Post-dose

FEV1 was measured at 5 minutes after dosing with spirometry conducted according to internationally accepted standards. The time of dosing was defined as the time corresponding to the use of the first inhaler device. The primary variable was analyzed using a mixed model containing the period baseline FEV1 as covariate. The period baseline FEV1 was the average of the FEV1 value measured in the clinic at 50 and 15 min prior to the study drug administration in that period. (NCT00669617)
Timeframe: Five Minutes Post Dose

InterventionLiters (Least Squares Mean)
Indacaterol 150 µg1.48
Indacaterol 300 µg1.50
Placebo1.38
Salmeterol/Fluticasone1.43
Salbutamol1.47

[back to top]

Number of Patients With Asthma Exacerbation

(NCT00706446)
Timeframe: 1 year

InterventionParticipants (Count of Participants)
1 - Tiotropium Plus ICS in the Arg/Arg Genotype3
2 - Tiotropium Plus ICS in the Arg/Gly Genotype15
3 - Tiotropium Plus ICS in the Gly/Gly Genotype6
4 - Salmeterol or Formoterol Plus ICS in the Arg/Arg Genotype6
5 - Salmeterol or Formoterol Plus ICS in the Arg/Gly Genotype12
6 - Salmeterol or Formoterol Plus ICS in the Gly/Gly Genotype9

[back to top]

Sputum RANTES Levels

Week 24 sputum RANTES levels in active treatment groups were measured. (NCT00712335)
Timeframe: 24 weeks

Interventionpg/ml (Mean)
Asthmatic Smokers Treated With Combination Therapy42.79
Asthmatic Smoker Treated With Montelukast Only44.03
Non-smoking Asthmatic Treated With Combination Therapy41.78
Non-smoking Asthmatic Treated With Montelukast Only36.41

[back to top]

Sputum Neutrophil Percentages

Week 24 sputum neutrophil percentages were measured in active treatment groups. (NCT00712335)
Timeframe: 24 weeks

Interventionpercentage of neutrophils (Mean)
Asthmatic Smokers Treated With Combination Therapy86.00
Asthmatic Smoker Treated With Montelukast Only72.53
Non-smoking Asthmatic Treated With Combination Therapy89.33
Non-smoking Asthmatic Treated With Montelukast Only79.84

[back to top]

Sputum Eotaxin Levels

Week 24 sputum eotaxin levels in active treatment groups were measured. (NCT00712335)
Timeframe: 24 weeks

Interventionpg/ml (Mean)
Asthmatic Smokers Treated With Combination Therapy47.13
Asthmatic Smoker Treated With Montelukast Only87.90
Non-smoking Asthmatic Treated With Combination Therapy65.14
Non-smoking Asthmatic Treated With Montelukast Only64.61

[back to top]

Sputum IL-8 Levels

Week 24 sputum IL-8 levels in active treatment groups (NCT00712335)
Timeframe: 24 weeks

Interventionpg/ml (Mean)
Asthmatic Smokers Treated With Combination Therapy334545
Asthmatic Smoker Treated With Montelukast Only26,300
Non-smoking Asthmatic Treated With Combination Therapy3602
Non-smoking Asthmatic Treated With Montelukast Only317778

[back to top]

Sputum GM-CSF Levels

Week 24 sputum GM-CSF levels in active treatment groups were measured. (NCT00712335)
Timeframe: 24 weeks

Interventionpg/ml (Mean)
Asthmatic Smokers Treated With Combination Therapy17.60
Asthmatic Smoker Treated With Montelukast Only15.18
Non-smoking Asthmatic Treated With Combination Therapy13.92
Non-smoking Asthmatic Treated With Montelukast Only12.16

[back to top]

Sputum Eosinophil Percentages

Secondary endpoints of inflammatory markers (sputum eosinophil percentages at 24 weeks) were measured in active treatment groups (NCT00712335)
Timeframe: 24 weeks

Interventionpercentage of eosinophils (Mean)
Asthmatic Smokers Treated With Combination Therapy2.33
Asthmatic Smoker Treated With Montelukast Only3.60
Non-smoking Asthmatic Treated With Combination Therapy1.60
Non-smoking Asthmatic Treated With Montelukast Only3.26

[back to top]

Sputum IFN-gamma/IL-5 Ratios

Week 24 sputum IFN-gamma/IL-5 ratios were determined in active treatment groups. (NCT00712335)
Timeframe: 24 weeks

Interventionratio (Mean)
Asthmatic Smokers Treated With Combination Therapy627.4
Asthmatic Smoker Treated With Montelukast Only272.4
Non-smoking Asthmatic Treated With Combination Therapy183.8
Non-smoking Asthmatic Treated With Montelukast Only279.0

[back to top]

Mean Change From Baseline in Scores on the Chronic Respiratory Disease Questionnaire-Self-Administered Standardized (CRQ-SAS) at Endpoint

The CRQ-SAS measures 4 domains of functioning of participants with COPD: mastery (amount of control the participant feels he/she has over COPD symptoms); fatigue (how tired the participant feels); emotional function (how anxious/depressed the participant feels); and dyspnea (how short of breath the participant feels during physical activities). Each domain is measured on a scale of 1-7 (1=maximum impairment; 7=no impairment). Each domain score is calculated separately. (NCT00784550)
Timeframe: Baseline and Endpoint (defined as the last recorded score [up to Week 24 or the early withdrawal visit] on each of the questions on this questionnaire)

,
Interventionpoints on a scale (Mean)
MasteryFatigueEmotional FunctionDyspnea
FSC + Tio0.280.230.240.21
Tiotropium0.040.170.160.19

[back to top]

Mean Change From Baseline in AM (Morning, Approximately 6-9 AM) Pre-dose Forced Expiratory Volume in One Second (FEV1) at Endpoint

Change from baseline was calculated as the Endpoint (defined as the last recorded measure of AM pre-dose FEV1 for each participant) value minus the baseline value. FEV1 is defined as the amount of air expelled from the lungs in one second after a full inspiration and is a measure of pulmonary function. (NCT00784550)
Timeframe: Baseline and Endpoint (defined as the last recorded measure [taken up to Week 24] of AM pre-dose FEV1 for each participant)

Interventionmilliliters (ml) (Mean)
FSC + Tio101
Tiotropium-16

[back to top]

Mean Change From Baseline in 2 Hour Post-dose FVC at Endpoint

Change from baseline was calculated as the Endpoint (defined as the last recorded measure of 2 hour post-dose FVC for each participant) value minus the baseline value. FVC is defined as the amount of air that can forcibly be blown out after a full inspiration (FVC). (NCT00784550)
Timeframe: Baseline and Endpoint (defined as the last recorded measure of 2 hour post-dose FVC [up to Week 24] for each participant)

Interventionml (Mean)
FSC + Tio265
Tiotropium87

[back to top]

Mean Change From Baseline in 2 Hour Post-dose FEV1 at Endpoint

Change from baseline was calculated as the Endpoint (defined as the last recorded measure of 2 hour post-dose FEV1 for each participant) value minus the baseline value. FEV1 is defined as the amount of air expelled from the lungs in one second after a full inspiration and is a measure of pulmonary function. (NCT00784550)
Timeframe: Baseline and Endpoint (defined as the last recorded measure [taken up to Week 24] of 2 hour post-dose FEV1 for each participant)

Interventionml (Mean)
FSC + Tio233
Tiotropium77

[back to top]

Mean Change From Baseline in AM (Morning, Approximately 6-9 AM) Pre-Dose Inspiratory Capacity (IC) at Endpoint

Change from baseline was calculated as the Endpoint (defined as the last recorded measure of AM pre-dose IC for each participant) value minus the baseline value. IC is defined as the amount of air that can be inhaled after a normal expiration. IC is a measure of pulmonary function. (NCT00784550)
Timeframe: Baseline and Endpoint (defined as the last recorded measure of AM pre-dose IC [up to Week 24] for each participant)

Interventionml (Mean)
FSC + Tio107
Tiotropium-8

[back to top]

Mean Change From Baseline in AM (Morning, Approximately 6-9 AM) Pre-dose Forced Vital Capacity (FVC) at Endpoint

Change from baseline was calculated as the Endpoint (defined as the last recorded measure of AM pre-dose FVC fore each participant) value minus the baseline value. FVC is defined as the amount of air that can forcibly be blown out after a full inspiration. (NCT00784550)
Timeframe: Baseline and Endpoint (defined as the last recorded measure [up to Week 24] of AM pre-dose FVC for each participant)

Interventionml (Mean)
FSC + Tio95
Tiotropium-28

[back to top]

Forced Expiratory Volume in 1 Second (FEV1) Standardized (With Respect to Time) Area Under the Curve (AUC) From 5 Minutes to 11 Hours 45 Minutes Post-dose at the End of the Study (Week 12, Day 84)

FEV1 was measured with spirometry conducted according to internationally accepted standards. Measurements were made at 5 and 30 minutes; 1, 2, 3, 4, and 8 hours; 11 hours 10 minutes and 11 hours 45 minutes post-dose at the end of the study (Week 12, Day 84). Standardized FEV1 AUC was calculated by the trapezoidal rule. The analysis included baseline FEV1 and FEV1 pre-dose and 10-15 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00821093)
Timeframe: From 5 minutes to 11 hours 45 minutes post-dose at the end of the study (Week 12, Day 84)

InterventionLiters (Least Squares Mean)
Indacaterol 150 μg1.47
Salmeterol 50 μg1.41

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose at the End of the Study (Week 12 + 1 Day, Day 85)

FEV1 was measured with spirometry conducted according to internationally accepted standards. Trough FEV1 was defined as the average of measurements made 23 hours 10 minutes and 23 hours 45 minutes post-dose at the end of treatment. The analysis included baseline FEV1 and FEV1 pre-dose and 10-15 minutes post-dose of salbutamol/albuterol during screening as covariates. (NCT00821093)
Timeframe: 24 hours post-dose at the end of the study (Week 12 + 1 day, Day 85)

InterventionLiters (Least Squares Mean)
Indacaterol 150 μg1.41
Salmeterol 50 μg1.35

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) After 12, 24 and 52 Weeks

Trough FEV1 was defined as the mean of the values at 23 h 10 min and 23 h 45 min after dosing at clinic on the previous day. Trough FEV1 was analyzed after 12, 24 and 52 weeks using a mixed model which contained the baseline FEV1 measurement, FEV1 prior to inhalation and FEV1 30 minutes post inhalation of salbutamol as covariates. (NCT00876694)
Timeframe: After 12, 24 and 52 weeks

,
InterventionLiters (Least Squares Mean)
Week 12 (n= 122, 56)Week 24 (n= 112, 51)Week 52 (n= 105, 49)
Indacaterol 300 μg1.401.401.39
Salmeterol 50 μg1.331.341.31

[back to top]

The Number of Participants With a Clinically Notable Systolic Blood Pressure During 52 Weeks of Treatment

"The number of participants with newly occurring or worsening clinically notable vital sign: Systolic Blood Pressure (mmHg) at anytime post baseline (BL) by treatment.~A Low Systolic Blood Pressure was defined as a systolic blood pressure measurement: <75 mmHg or <= to 90 mmHg and a decrease from baseline >= to 20 mmHg.~A High Systolic Blood Pressure was defined as a systolic blood pressure measurement: >200 mmHg or >= to 180 mmHg and an increase from baseline >= to 20 mmHg." (NCT00876694)
Timeframe: 52 weeks

,
InterventionParticipants (Number)
Low Systolic Blood Pressure:High Systolic Blood Pressure:
Indacaterol 300 μg01
Salmeterol 50 μg00

[back to top]

The Number of Participants With a Clinically Notable QTc Interval Value During 52 Weeks of Treatment

"The number of participants with newly occurring or worsening clinically notable QTc Interval value at anytime post baseline.~The QTc interval is calculated using Fridericia's formula: QTc= QT/cube root RR. QTc is the interval between the Q and T waves corrected for heart rate and RR is the interval between two R waves in milliseconds (ms).~Notable QTc interval >450 ms for males and >470 ms for females. The maximum QTc increase from baseline at any time during the study was also tabulated with absolute and relative frequencies for categories 30- 60 ms and >60 ms." (NCT00876694)
Timeframe: 52 weeks

,
InterventionParticipants (Number)
Notable QTcQTc increase from BL: 30-60 msQTc increase from BL: >60 ms
Indacaterol 300 μg6120
Salmeterol 50 μg331

[back to top]

The Number of Participants With a Clinically Notable Pulse Rate During 52 Weeks of Treatment

The number of participants with newly occurring or worsening clinically notable vital sign: Pulse Rate in beats per minute (bpm) at anytime post baseline (BL) by treatment. Low Pulse Rate was defined as a pulse rate <40 bpm or <= to 50 bpm and a decrease from baseline >= to 15 bpm. High Pulse Rate was defined as a pulse rate >130 bpm or >= to 120 bpm and an increase from baseline >= to 15 bpm. (NCT00876694)
Timeframe: 52 weeks

,
InterventionParticipants (Number)
Low Pulse Rate:High Pulse Rate:
Indacaterol 300 μg10
Salmeterol 50 μg00

[back to top]

The Number of Participants With a Clinically Notable Diastolic Blood Pressure During 52 Weeks of Treatment

"The number of participants with newly occurring or worsening clinically notable vital sign: Diastolic blood pressure (mmHg) at anytime post baseline (BL) by treatment.~A Low Diastolic Blood Pressure was defined as a diastolic blood pressure measurement: <40 mmHg or <= to 50 mmHg and a decrease from baseline >= to 15 mmHg.~A High Diastolic Blood Pressure was defined as a diastolic blood pressure measurement: >115 mmHg or >= to 105 mmHg and an increase from baseline >= to 15 mmHg." (NCT00876694)
Timeframe: 52 weeks

,
InterventionParticipants (Number)
Low Diastolic Blood Pressure:High Diastolic Blood Pressure:
Indacaterol 300 μg00
Salmeterol 50 μg10

[back to top]

Serum Potassium (mmol/L) at Weeks 4, 8, 12, 24, 36, 44, and 52

The least squares mean of the serum potassium in mmol/L at weeks 4, 8, 12, 24, 36, 44 and 52. Mixed model used baseline serum potassium as a covariate. (NCT00876694)
Timeframe: 4, 8, 12, 24, 36, 44, and 52 weeks

,
Interventionmmol/L (Least Squares Mean)
Week 4 (n= 122, 57)Week 8 (n= 121, 56)Week 12 (n= 118, 56)Week 24 (n= 113, 52)Week 36 (n= 106, 50)Week 44 (n= 104, 50)Week 52 (n= 104, 49)
Indacaterol 300 μg4.264.304.284.344.354.314.32
Salmeterol 50 μg4.284.274.354.274.294.274.31

[back to top]

Blood Glucose (mmol/L) 1 Hour Post Dose at Weeks 4, 8, 12, 24, 36, 44, and 52

The least squares mean of the blood glucose in mmol/L at weeks 4, 8, 12, 24, 36, 44 and 52. Mixed model used baseline blood glucose as a covariate. (NCT00876694)
Timeframe: 4, 8, 12, 24, 36, 44, and 52 weeks

,
Interventionmmol/L (Least Squares Mean)
Week 4 (n= 122, 57)Week 8 (n= 121, 56)Week 12 (n= 118, 56)Week 24 (n= 113, 52)Week 36 (n= 106, 50)Week 44 (n= 104, 50)Week 52 (n= 104, 49)
Indacaterol 300 μg6.105.925.976.165.956.095.96
Salmeterol 50 μg5.966.306.596.136.266.426.65

[back to top]

Percentage Change From Baseline (for Each Treatment Cycle) in Exhaled Nitric Oxide (eNO)

Percentage change in eNO was reported following treatment with inhaled Advair in subjects with chronic but stable asthma as defined in Global Initiative for Asthma (GINA) guidelines. eNO was calculated 3 times every day in a treatment cycle for 7 days. The maximum value of all 3 collected value were collected for each seven days of the individual treatment cycle. Out of the maximum values, the minimum was taken and used for calculating the percentage change from baseline. (NCT00927758)
Timeframe: Baseline to Day 7 of each treatment cycle (total duration about 8 - 10 weeks)

InterventionPercentage change in eNO (Mean)
Flu/Sal- 100mcg/50mcg36.65
Flu/Sal- 250mcg/50mcg45.31
Flu/Sal- 500mcg/50mcg54.58

[back to top]

Change in On-treatment Cough and Expectoration as Measured by the CASA-Q: Cough Symptoms Domain

"Change from baseline in on-treatment cough and expectoration as measured by the cough and sputum assessment questionnaire (CASA-Q) (selected sites only): Cough symptoms domain. Change was calculated as week score minus baseline score. Response options for the items in this domain range from not at all/never to a lot/always on a five-point scale. Domain items were reverse scored, summed and transformed to a domain score ranging from 0 to 100 where a higher score is associated with less symptoms due to cough.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 12, 18 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 12 visit (N=309, 318)Week 18 visit (N=305, 312)Week 52 visit (N=270, 268)
Fluticasone Maintenance-0.32-1.47-1.69
Fluticasone Withdrawal-0.85-3.34-3.26

[back to top]

Change in On-treatment Cough and Expectoration as Measured by the CASA-Q: Sputum Impact Domain

"Change from baseline in on-treatment cough and expectoration as measured by the cough and sputum assessment questionnaire (CASA-Q) (selected sites only): Sputum impact domain. Change was calculated as week score minus baseline score. Response options for the items in this domain range from not at all/never to a lot/always on a five-point scale. Domain items were reverse scored, summed and transformed to a domain score ranging from 0 to 100 where a higher score is associated with less impact due to sputum.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 12, 18 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 12 visit (N=308, 317)Week 18 visit (N=303, 310)Week 52 visit (N=267, 267)
Fluticasone Maintenance-2.26-2.38-4.29
Fluticasone Withdrawal-1.63-3.31-4.15

[back to top]

Change in On-treatment Cough and Expectoration as Measured by the CASA-Q: Sputum Symptoms Domain

"Change from baseline in on-treatment cough and expectoration as measured by the cough and sputum assessment questionnaire (CASA-Q) (selected sites only): Sputum symptoms domain. Change was calculated as week score minus baseline score. Response options for the items in this domain range from not at all/never to extremely/always on a five-point scale. Domain items were reverse scored, summed and transformed to a domain score ranging from 0 to 100 where a higher score is associated with less symptoms due to sputum.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 12, 18 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 12 visit (N=308, 317)Week 18 visit (N=302, 311)Week 52 visit (N=269, 268)
Fluticasone Maintenance-1.36-2.71-5.10
Fluticasone Withdrawal-1.24-1.93-2.45

[back to top]

Change in On-treatment Exercise Capacity Measured by Six-minute Walk Test (6-MWT)

Change from baseline in on-treatment exercise capacity measured by six-minute walk test (6-MWT); change was calculated as week score minus baseline score. Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest. (NCT00975195)
Timeframe: Baseline and week 18 and 52 visits

,
Interventionmeters (Least Squares Mean)
Week 18 visit (N=1111, 1110)Week 52 visit (N=1013, 987)
Fluticasone Maintenance3.893.94
Fluticasone Withdrawal1.940.42

[back to top]

Change in On-treatment FEV1 as Measured by Home Based Spirometry

Change from baseline in on-treatment Forced Expiratory Volume in One Second (FEV1) as measured by home based spirometry. Change was calculated as week score minus baseline score. The weekly mean was defined as the mean of the measurements taken during the last 7 days prior to the visit date, and was calculated if ≥4 of the 7 days had non-missing measurements. Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest. (NCT00975195)
Timeframe: Baseline and week 6, 12, 18, 27, 36, 45 and 52 visits

,
InterventionLitres (Least Squares Mean)
Week 6 visit (N=893, 939)Week 12 visit (N=910, 930)Week 18 visit (N=913, 901)Week 27 visit (N=863, 843)Week 36 visit (N=854, 845)Week 45 visit (N=830, 815)Week 52 visit (N=785, 788)
Fluticasone Maintenance-0.049-0.050-0.051-0.056-0.059-0.061-0.067
Fluticasone Withdrawal-0.053-0.056-0.093-0.092-0.099-0.103-0.115

[back to top]

Change in On-treatment FVC as Measured by Home Based Spirometry

Change from baseline in on-treatment forced vital capacity (FVC) as measured by home based spirometry. Change was calculated as week score minus baseline score. The weekly mean was defined as the mean of the measurements taken during the last 7 days prior to the visit date, and was calculated if ≥4 of the 7 days had non-missing measurements. Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest. (NCT00975195)
Timeframe: Baseline and week 6, 12, 18, 27, 36, 45 and 52 visits

,
InterventionLitres (Least Squares Mean)
Week 6 visit (N=893, 939)Week 12 visit (N=910, 930)Week 18 visit (N=913, 901)Week 27 visit (N=863, 843)Week 36 visit (N=854, 845)Week 45 visit (N=830, 815)Week 52 visit (N=785, 788)
Fluticasone Maintenance-0.116-0.113-0.122-0.123-0.135-0.141-0.157
Fluticasone Withdrawal-0.089-0.105-0.124-0.147-0.158-0.168-0.201

[back to top]

Change in On-treatment Lung Function as Measured by Trough FEV1

Change from baseline in on-treatment lung function as measured by trough forced expiratory volume in one second (FEV1); change was calculated as week score minus baseline score. Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest. (NCT00975195)
Timeframe: Baseline and week 6, 12, 18 and 52 visits

,
InterventionLitres (Least Squares Mean)
Week 6 visit (N=1135, 1135)Week 12 visit (N=1114, 1092)Week 18 visit (N=1077, 1058)Week 52 visit (N=970, 935)
Fluticasone Maintenance-0.009-0.011-0.011-0.016
Fluticasone Withdrawal-0.011-0.018-0.050-0.059

[back to top]

Change in On-treatment PEFR as Measured by Home Based Spirometry

Change from baseline in on-treatment peak expiratory flow rate (PEFR) as measured by home based spirometry; change was calculated as week score minus baseline score. Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest. (NCT00975195)
Timeframe: Baseline and week 6, 12, 18, 27, 36, 45 and 52 visits

,
InterventionLitres/sec (Least Squares Mean)
Week 6 visit (N=893, 939)Week 12 visit (N=910, 930)Week 18 visit (N=913, 901)Week 27 visit (N=863, 843)Week 36 visit (N=854, 845)Week 45 visit (N=830, 815)Week 52 visit (N=785, 788)
Fluticasone Maintenance-0.228-0.266-0.295-0.319-0.352-0.368-0.377
Fluticasone Withdrawal-0.230-0.290-0.435-0.430-0.473-0.490-0.538

[back to top]

Change in On-treatment Physical Health Status as Determined by Body Mass Index (BMI)

Change from baseline in on-treatment physical health status as determined by body mass index (BMI); change was calculated as week score minus baseline score. Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest. (NCT00975195)
Timeframe: Baseline and week 18 and 52 visits

,
Interventionkg/m2 (Least Squares Mean)
Week 18 visit (N=1143, 1146)Week 52 visit (N=1047, 1021)
Fluticasone Maintenance0.0300.004
Fluticasone Withdrawal0.040-0.009

[back to top]

Change in On-treatment Physician Global Evaluation

"Change from baseline in on-treatment physician global evaluation. The evaluation reflected the physician's opinion of the patient's overall condition and was based on the need for concomitant medication, the number and severity of exacerbations, the severity of cough, the ability to exercise, the amount of wheezing and any other relevant clinical observations. Patients were graded on a scale of 1 (poor) to 8 (excellent). Change was calculated as week score minus baseline score.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 27 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 27 visit (N=1113, 1093)Week 52 visit (N=1041, 1014)
Fluticasone Maintenance0.100.19
Fluticasone Withdrawal0.040.08

[back to top]

Change in On-treatment St Georges Respiratory Questionnaire (SGRQ) Scores: Activity Domain

"Change from baseline in on-treatment St Georges Respiratory Questionnaire (SGRQ) scores: Activity domain. Scores range from 0 to 100, with higher scores indicating more limitations. Change was calculated as week score minus baseline score.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 27 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 27 visit (N=1002, 988)Week 52 visit (N=942, 916)
Fluticasone Maintenance0.09-0.19
Fluticasone Withdrawal0.850.78

[back to top]

Change in On-treatment St Georges Respiratory Questionnaire (SGRQ) Scores: Impact Domain

"Change from baseline in on-treatment St Georges Respiratory Questionnaire (SGRQ) scores: Impact Domain. Scores range from 0 to 100, with higher scores indicating more limitations. Change was calculated as week score minus baseline score.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 27 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 27 visit (N=1004, 998)Week 52 visit (N=946, 921)
Fluticasone Maintenance-0.78-0.08
Fluticasone Withdrawal0.351.27

[back to top]

Change in On-treatment St Georges Respiratory Questionnaire (SGRQ) Scores: Symptoms Domain

"Change from baseline in on-treatment St Georges Respiratory Questionnaire (SGRQ) scores: Symptoms domain. Scores range from 0 to 100, with higher scores indicating more limitations. Change was calculated as week score minus baseline score.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 27 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 27 visit (N=1010, 998)Week 52 visit (N=955, 921)
Fluticasone Maintenance0.120.51
Fluticasone Withdrawal0.621.11

[back to top]

Change in On-treatment St Georges Respiratory Questionnaire (SGRQ) Scores: Total Score

"Change from baseline in on-treatment St Georges Respiratory Questionnaire (SGRQ) scores: Total score. Scores range from 0 to 100, with higher scores indicating more limitations. Change was calculated as week score minus baseline score.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 27 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 27 visit (N=996, 986)Week 52 visit (N=939, 913)
Fluticasone Maintenance-0.42-0.07
Fluticasone Withdrawal0.551.15

[back to top]

Changes in On-treatment Dyspnoea as Measured by the Modified Medical Research Council (MMRC) Dyspnoea Scale

"Change from baseline in on-treatment dyspnoea as measured by the Modified Medical Research Council (MMRC) dyspnoea scale; change was calculated as week score minus baseline score. Negative changes from baseline indicate an improvement in health.~Scale from 0 to 4:~0 = not troubled by breathlessness, except during strenuous exercise~1 = short of breath when hurrying or walking up a slight hill~2 = walks slower than contemporaries on the same level because of breathlessness, or has to stop for breath when walking at own pace~3 = stops for breath after approximately 100 yards, or after a few minutes on the level~4 = too breathless to leave the house, or breathless when dressing or undressing~No breathlessness was given a score of -1~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 18 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 18 visit (N=1140, 1143)Week 52 visit (N=1043, 1019)
Fluticasone Maintenance-0.030-0.028
Fluticasone Withdrawal-0.0010.035

[back to top]

Severity of On-treatment COPD Exacerbations

Severity of on-treatment COPD exacerbations: for each patient, the worst applicable category was taken (i.e. none, mild, moderate or severe) (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

,
Interventionpercentage of participants (Number)
None and patient completed randomised treatmentNone and patient discontinued randomised treatmentMildModerateSevere
Fluticasone Maintenance42.910.22.730.813.4
Fluticasone Withdrawal41.29.82.331.515.2

[back to top]

Time to First On-treatment COPD Exacerbation

"Time to first on-treatment COPD exacerbation of any severity. The measure type displays the 25th percentile and its 95% confidence interval." (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventiondays (Number)
Fluticasone Maintenance365.0
Fluticasone Withdrawal346.0

[back to top]

Number of Moderate or Severe On-treatment COPD Exacerbations

"Number of moderate or severe on-treatment COPD exacerbations, based on a 7-day gap rule: exacerbations where the onset date of the second exacerbation event was ≤7 days after the end date of the first exacerbation event were combined and counted as moderate or severe if ≥1 of the contributing exacerbation events was moderate or severe. Exacerbations were considered severe if the patient was held and treated for an acute respiratory condition in an urgent care department or an observation unit for >6 hours, the patient was treated at home by a mobile urgent care team or the patient was admitted to hospital. Exacerbations were considered moderate if they required prescription of antibiotics and/or systemic steroids.~Measured values show adjusted mean event rate." (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventionexacerbations per patient-year (Mean)
Fluticasone Maintenance0.91
Fluticasone Withdrawal0.95

[back to top]

Number of On-treatment COPD Exacerbations

"Number of on-treatment COPD exacerbations of any severity, based on a 7-day gap rule: exacerbations where the onset date of the second exacerbation event was ≤7 days after the end date of the first exacerbation event were combined.~Measured values show adjusted event rate." (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventionexacerbations per patient-year (Mean)
Fluticasone Maintenance1.03
Fluticasone Withdrawal1.08

[back to top]

Number of Severe On-treatment COPD Exacerbations

"Number of severe on-treatment COPD exacerbations based on a 7-day gap rule: exacerbations where the onset date of the second exacerbation event was ≤7 days after the end date of the first exacerbation event were combined and counted as severe if ≥1 of the contributing exacerbation events was severe. Exacerbations were considered severe if the patient was held and treated for an acute respiratory condition in an urgent care department or an observation unit for >6 hours, the patient was treated at home by a mobile urgent care team or the patient was admitted to hospital.~Measured values show adjusted event rate." (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventionexacerbations per patient-year (Mean)
Fluticasone Maintenance0.20
Fluticasone Withdrawal0.23

[back to top]

Proportion of Patients With ≥1 Moderate or Severe On-treatment COPD Exacerbation

Presence (yes vs no) of at least one moderate or severe on-treatment COPD exacerbation, displayed as a percentage. Exacerbations were considered severe if the patient was held and treated for an acute respiratory condition in an urgent care department or an observation unit for >6 hours, the patient was treated at home by a mobile urgent care team or the patient was admitted to hospital. Exacerbations were considered moderate if they required prescription of antibiotics and/or systemic steroids. (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventionpercentage of participants (Number)
Fluticasone Maintenance44.2
Fluticasone Withdrawal46.7

[back to top]

Proportion of Patients With at Least One On-treatment COPD Exacerbation

Presence (yes vs no) of at least one on-treatment COPD exacerbation of any severity, displayed as a percentage. (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventionpercentage of participants (Number)
Fluticasone Maintenance46.9
Fluticasone Withdrawal49.0

[back to top]

Proportion of Patients With at Least One Severe On-treatment COPD Exacerbation.

Presence (yes vs no) of at least one severe on-treatment COPD exacerbation, displayed as a percentage. Exacerbations were considered severe if the patient was held and treated for an acute respiratory condition in an urgent care department or an observation unit for >6 hours, the patient was treated at home by a mobile urgent care team or the patient was admitted to hospital. (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventionpercentage of participants (Number)
Fluticasone Maintenance13.4
Fluticasone Withdrawal15.2

[back to top]

Time to First Moderate or Severe On-treatment COPD Exacerbation

"A Chronic Obstructive Pulmonary Disease (COPD) exacerbation was defined as an increase or new onset of ≥2 lower respiratory symptoms related to COPD, with ≥1 symptom lasting ≥3 days, requiring a change in treatment. Lower respiratory symptoms included shortness of breath, sputum production (volume), sputum purulence, cough, wheezing and chest tightness. A change in treatment included: hospitalisation/treatment in an urgent care unit, prescription of antibiotics and/or systemic steroids or a significant change of prescribed respiratory medication such as theophyllines, long-acting beta-agonists or inhaled corticosteroids. Exacerbations were considered severe if the patient was held and treated for an acute respiratory condition in an urgent care department or an observation unit for >6 hours, the patient was treated at home by a mobile urgent care team or the patient was admitted to hospital.The measure type displays the 25th percentile and its 95% confidence interval." (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventiondays (Number)
Fluticasone Maintenance107.0
Fluticasone Withdrawal110.0

[back to top]

Time to First Severe On-treatment COPD Exacerbation

"Time to first severe on-treatment COPD exacerbation. Exacerbations were considered severe if the patient was held and treated for an acute respiratory condition in an urgent care department or an observation unit for >6 hours, the patient was treated at home by a mobile urgent care team or the patient was admitted to hospital.~The measure type displays the 25th percentile and its 95% confidence interval." (NCT00975195)
Timeframe: During randomised treatment, up to 488 days

Interventiondays (Number)
Fluticasone MaintenanceNA
Fluticasone Withdrawal419.0

[back to top]

Change in On-treatment BODE Index

Change from baseline in on-treatment BODE index (Body mass index, airflow Obstruction, Dyspnea and Exercise capacity index), a composite score ranging from 0 (best) to 10 (worst); change was calculated as week score minus baseline score. Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest. (NCT00975195)
Timeframe: Baseline and week 18 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 18 visit (N=1038, 1024)Week 52 visit (N=931, 907)
Fluticasone Maintenance-0.06-0.03
Fluticasone Withdrawal0.060.14

[back to top]

Change in On-treatment Cough and Expectoration as Measured by the CASA-Q: Cough Impact Domain

"Change from baseline in on-treatment cough and expectoration as measured by the cough and sputum assessment questionnaire (CASA-Q) (selected sites only): Cough impact domain. Change was calculated as week score minus baseline score. Response options for the items in this domain range from not at all/never to extremely/always on a five-point scale. Domain items were reverse scored, summed and transformed to a domain score ranging from 0 to 100 where a higher score is associated with less impact due to cough.~Statistical analysis results are presented only for the week 52 visit as this is the primary timepoint of interest." (NCT00975195)
Timeframe: Baseline and week 12, 18 and 52 visits

,
Interventionunits on a scale (Least Squares Mean)
Week 12 visit (N=307, 319)Week 18 visit (N=302, 312)Week 52 visit (N=268, 269)
Fluticasone Maintenance-1.65-2.87-4.51
Fluticasone Withdrawal-1.24-3.71-5.54

[back to top]

"SOBDA Threshold for Response Assessed as Mean Change From the Previous Week's SOBDA Score Based on a Participant-completed PGAC Score Rated of Better"

"Changes from Baseline in the SOBDA score for responders (Rs) and non-responders (NRs) (using the PGAC assessment; 1 [much worse] to 5 [much better]), together with the cumulative proportions of Rs and NRs, was used to establish the threshold for defining SOBDA questionnaire Rs. The threshold of response is a score change in the SOBDA questionnaire that is demonstrated to have a perceivable benefit for the participant. The threshold of response was evaluated as the change from Baseline in the SOBDA score based on PGAC scores pre-specified as better or demonstrating meaningful improvement." (NCT00984659)
Timeframe: Baseline (last week of the 2-week Run-in Period) and Weeks 1, 2, 3, 4, 5, and 6 (6-week Treatment Period)

Interventionscores on a scale (Mean)
Baseline to Week 1, n=97Week 1 to Week 2, n=82Week 2 to Week 3, n=70Week 3 to Week 4, n=49Week 4 to Week 5, n=66Week 5 to Week 6, n=26
MITT Population: 6-Week Treatment Period-0.26-0.08-0.08-0.10-0.08-0.05

[back to top]

Known Group Validity for the SOBDA Questionnaire Measured as the Comparison of the Baseline SOBDA Score in the Indicated Categories of the Physician-completed (PyC) mMRC Score at Visit 2

SOBDA known group validity refers to the extent to which scores from the SOBDA questionnaire should differentiate participants with varying levels of dyspnea severity. It was assessed by comparing summary measures for the SOBDA score for each indicated level (0, 1, 2, 3, and 4) of the PyC mMRC. The physician rated the degree of the participant's dyspnea on the 5-point mMRC scale: 0 (none) to 4 (very severe). Known group validity was confirmed if the SOBDA score increased with increasing values of PyC mMRC, both indicating increased levels of breathlessness. (NCT00984659)
Timeframe: Baseline (last week of the 2-week Run-in Period) and pre-treatment on Visit 2 (Day 1 of the 6-week Treatment Period)

Interventionscores on a scale (Least Squares Mean)
PyC mMRC: 0 to 1, n=12PyC mMRC: 2, n=200PyC mMRC: 3, n=117PyC mMRC: 4, n=10
All Participants: 2-week Run-in Period1.782.082.282.73

[back to top] [back to top]

Change From Baseline to Last Treatment Week in the SOBDA Score by Physician-completed mMRC and Participant-completed mMRC Responses at Visit 3/PD

The responsiveness of the SOBDA questionnaire was assessed by comparing score changes between responders and non-responders. The mMRC ranges from 0 (no breathlessness except with strenous exercise) to 4 (too breathless to leave the house; breathless when dressing/undressing) and is completed by the clinician or the participant as indicated. Changes in mean SOBDA scores during the last week of treatment in responders and non-responders using definitions based on the Physician-completed (Ph-C) and Participant-completed (Pa-C) mMRC conducted at Visit 3/Premature Discontinuation were assessed. (NCT00984659)
Timeframe: Baseline (2-week Run-in Period) and Week Prior to Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

InterventionScores on a scale (Mean)
Ph-C mMRC, responders, n=91Ph-C mMRC, non-responders, n=210Pa-C mMRC, responders, n=92Pa-C mMRC, non-responders, n=209
MITT Population: 6-Week Treatment Period-0.13-0.11-0.18-0.09

[back to top]

Change From Baseline to Last Treatment Week in the SOBDA Score by CRQ-SAS Dyspnea Domain (DD) Responses at Visit 3/PD

The responsiveness of the SOBDA questionnaire was assessed by comparing score changes of responders (Rs) versus non-responders (NRs). The CRQ-SAS DD includes 5 questions (q.) scored 1 (maximum impairment) to 7 (no impairment). Individual q. were equally weighted, and domain scores (DSs) (range=1-7) were calculated as the mean across the non-missing items within each domain (DSs were calculated although an individual item score was missing). Changes in mean SOBDA scores during the last treatment week in Rs and NRs using definitions based on the CRQ-SAS DD conducted at Visit 3/PD were assessed. (NCT00984659)
Timeframe: Baseline (2-week Run-in Period) and Week Prior to Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

InterventionScores on a scale (Mean)
Responders, n=117Non-responders, n=184
MITT Population: 6-Week Treatment Period-0.320.01

[back to top]

Change From Baseline to Last Treatment Week in the SOBDA Score by CGI-C Responses at Visit 3/PD

The responsiveness of the SOBDA questionnaire was assessed by comparing score changes between responders and non-responders. The CGI-C is clinician completed on a 1 to 5 scale: 1, much worse; 2, worse; 3, no change; 4, better; 5, much better. Changes in mean SOBDA scores during the last week of treatment in responders and non-responders using definitions based on the CGI-C conducted at Visit 3/Premature Discontinuation were assessed. (NCT00984659)
Timeframe: Baseline (2-week Run-in Period) and Week Prior to Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

Interventionscores on a scale (Mean)
Responders, n=120Non-responders, n=181
MITT Population: 6-Week Treatment Period-0.25-0.03

[back to top]

"SOBDA Threshold for Response as Assessed by Mean Change From Baseline to the Last Treatment Week in the SOBDA Score Based on a CGI-C Response Rated as Better"

"The threshold of response is a score change in the SOBDA questionnaire that is demonstrated to have a perceivable benefit for the participant. The threshold of response was evaluated as the change from Baseline in the SOBDA score based on CGI-C scores pre-specified as better or demonstrating meaningful improvement. The CGI-C is clinician completed on a 1 to 5 scale: 1, much worse, 2, worse; 3, no change; 4, better; 5, much better." (NCT00984659)
Timeframe: Baseline and Week Prior to Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

InterventionScores on a scale (Mean)
MITT Population: 6-Week Treatment Period-0.25

[back to top]

Known Group Validity for the SOBDA Questionnaire Measured as the Comparison of the Baseline SOBDA Score in the Indicated Categories of the Participant-completed (ParC) mMRC Score at Visit 2

SOBDA known group validity refers to the extent to which scores from the SOBDA questionnaire should differentiate participants with varying levels of dyspnea severity. It was assessed by comparing summary measures for the SOBDA score for each indicated level (0, 1, 2, 3, and 4) of the ParC mMRC. The participant rated the degree of his/her dyspnea on the 5-point mMRC scale: 0 (none) to 4 (very severe). Known group validity was confirmed if the SOBDA score increased with increasing values of ParC mMRC, both indicating increased levels of breathlessness. (NCT00984659)
Timeframe: Baseline (last week of the 2-week Run-in Period) and pre-treatment on Visit 2 (Day 1 of the 6-week Treatment Period)

Interventionscores on a scale (Least Squares Mean)
ParC mMRC: 0, n=12ParC mMRC: 1, n=103ParC mMRC: 2, n=138ParC mMRC: 3, n=65ParC mMRC: 4, n=22
All Participants: 2-week Run-in Period1.921.942.202.262.73

[back to top]

"SOBDA Threshold for Response as Assessed by Mean Change From Baseline to the Last Treatment Week in the SOBDA Score Based on a CRQ-SAS Dyspnea Domain (DD) Response Rated as Better"

"The threshold of response (TOR) is a score change in the SOBDA questionnaire that is demonstrated to have a perceivable benefit. The TOR was evaluated as the change from Baseline in the SOBDA score based on CRQ-SAS scores pre-specified as better or demonstrating meaningful improvement. The CRQ-SAS DD includes 5 questions (q.) scored 1 (maximum impairment) to 7 (no impairment). Individual q. were equally weighted, and domain scores (DSs) (range=1-7) were calculated as the mean across the non-missing items within each domain (DSs were calculated although an individual item score was missing)." (NCT00984659)
Timeframe: Baseline and Week Prior to Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

InterventionScores on a scale (Mean)
MITT Population: 6-Week Treatment Period-0.13

[back to top]

Convergent Validity (CV) for the SOBDA Questionnaire Measured as the Correlation of the Baseline SOBDA Score With the Chronic Respiratory Disease Questionnaire-Self-Administered Standardized (CRQ-SAS) Dyspnea Domain Score at Visit 2

Convergent validity is defined as the ability of the SOBDA questionnaire to measure required information and was assessed by examining the relationship between the SOBDA score and the CRQ-SAS dyspnea domain score. Pearson's correlation coefficient is a measure of the linear dependence between 2 variables. A correlation of +1 or -1 will occur if the data from the 2 variables lie exactly on a line. The CRQ is a 20-item instrument measuring 4 domains (each measured on a scale of 1 [maximum impairment] to 7 [no impairment]) of functioning: mastery, fatigue, emotional function, and dyspnea. (NCT00984659)
Timeframe: Baseline (last week of the 2-week Run-in Period) and pre-treatment on Visit 2 (Day 1 of the 6-week Treatment Period)

InterventionPearson's correlation coefficient (Number)
All Participants: 2-week Run-in Period-0.68

[back to top]

Convergent Validity for the SOBDA Questionnaire Measured as the Correlation of the Baseline SOBDA Score With the Clinician Global Assessment of Dyspnea Severity (CGI-S) Score at Visit 2

Convergent validity is defined as the ability of the SOBDA questionnaire to measure the required information and was assessed by examining the relationship between the SOBDA score with the CGI-S score. Spearman's rank correlation coefficient assesses if the relationship between two variables is monotone. A correlation of +1 or -1 will occur if one variable is a perfect monotone of the other. Clinicians were asked to assess the severity of the participant's dyspnea on the CGI-S scale. This was evaluated on a 1-4 Likert scale: 1 (mild) to 4 (very severe). (NCT00984659)
Timeframe: Baseline (last week of the 2-week Run-in Period) and pre-treatment on Visit 2 (Day 1 of the 6-week Treatment Period)

InterventionSpearman rank correlation coefficient (Number)
All Participants: 2-week Run-in Period0.24

[back to top]

Internal Consistency (IC) of the Shortness of Breath With Daily Activities (SOBDA) Questionnaire in Participants With Chronic Obstructive Pulmonary Disease (COPD) Assessed as Cronbach's Alpha Value

Cronbach's alpha (CA) is a measure of the IC of the 13-item SOBDA questionnaire (completed via electronic diary by a sample of participants). It is the ratio of the variance (var.) of the sum of the individual scores and the var. of the total score. The var. of the sum of a group of independent variables is the sum of their var.; thus, if the variables are positively correlated, the var. of the sum will be increased. If the items making up the score are identical and so perfectly correlated, CA=1. If the items are independent, CA=0. Higher scores indicate a more reliable (precise) instrument. (NCT00984659)
Timeframe: Day 1 of the 2-week Run-in Period

Interventionratio of variance (Number)
All Participants: 2-week Run-in Period0.892

[back to top]

SOBDA Threshold for Response Assessed as Mean Change From Baseline to Last Treatment Week in the SOBDA Score Based on Forced Expiratory Volume in One Second (FEV1) Change From Baseline of 50 Milliliters (mL) to <100 mL

"FEV1 response was rated as 1=No change or worse (i.e., change of <50 mL); 2=Better (i.e., change of 50 to <100 mL); 3=Much better (i.e., change of >=100 mL). The threshold of response is a score change in the SOBDA questionnaire that is demonstrated to have a perceivable benefit for the participant. The threshold of response was evaluated as the change from Baseline in the SOBDA score based on study assessment (FEV1) scores pre-specified as better or demonstrating meaningful improvement." (NCT00984659)
Timeframe: Baseline and Week Prior to Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

InterventionmL (Mean)
MITT Population: 6-Week Treatment Period-0.16

[back to top]

Test-retest Reliability (T-RR) of SOBDA Scores Measured as the Difference in the SOBDA Weekly Score Between Week 1 and Week 2 of the 2-week Run-in Period

T-RR=stability during repeat measures over time in a stable population. SOBDA score was determined by the 13-item (it.) scoring algorithm, assigning a weekly mean score of 1-4 (higher scores=more severe breathlessness with daily activities) based on the mean of 7 days of data (or >=4 days). Daily total score is computed from the mean of the participant's (par.) scores on the 13 it. (>=7 it. must have non-missing responses). Only scores of stable par. (indicating no change [score=3] on the par.-completed Patient Global Assessment of Change [PGAC]; 1 [ much worse] to 5 [much better]) were used. (NCT00984659)
Timeframe: Week 1 and Week 2 of the 2-week Run-in Period

Interventionscores on a scale (Mean)
All Participants: 2-week Run-in Period0.01

[back to top]

Convergent Validity for the SOBDA Questionnaire Measured as Correlations of the Baseline SOBDA Score With Participant-completed Modified Medical Research Council (mMRC) and Physician-completed mMRC Scores at Visit 2

Convergent validity is defined as the ability of the SOBDA questionnaire to measure required information and was assessed by examining the relationship between the SOBDA score and the participant/physician-completed mMRC Dyspnea Scale assessments. The physician/participant rated the degree of the participant's dyspnea (trouble breathing) on the 5-point mMRC scale (0, none; 4, very severe). Spearman's rank correlation coefficient assesses if the relationship between two variables is monotone. A correlation of +1 or -1 will occur if one variable is a perfect monotone of the other. (NCT00984659)
Timeframe: Baseline (last week of the 2-week Run-in Period) and pre-treatment on Visit 2 (Day 1 of the 6-week Treatment Period)

InterventionSpearman rank correlation coefficient (Number)
Physician-completed mMRC, n=339Participant-completed mMRC, n=340
All Participants: 2-week Run-in Period0.240.29

[back to top]

Known Group Validity (KGV) for the SOBDA Questionnaire Measured as the Comparison of the Baseline SOBDA Score in the Indicated Categories of CGI-S Scores at Visit 2

SOBDA KGV refers to the extent to which scores from the SOBDA questionnaire should differentiate participants with varying levels of dyspnea severity. It was assessed by comparing summary measures for the SOBDA score for each indicated level (0, 1, 2, 3, and 4) of the CGI-S score. Clinicians were asked to assess the severity of the participant's dyspnea on the CGI-S scale. This was evaluated on a 1-4 Likert scale: 1 (mild) to 4 (very severe). KGV was confirmed if the SOBDA score increased with increasing values of CGI-S, both indicating increased levels of breathlessness. (NCT00984659)
Timeframe: Baseline (last week of the 2-week Run-in Period) and pre-treatement on Visit 2 (Day 1 of the 6-week Treatment Period)

Interventionscores on a scale (Least Squares Mean)
CGI-S: 1, n=19CGI-S: 2, n=236CGI-S: 3, n=78CGI-S: 4, n=5
All Participants: 2-week Run-in Period1.872.112.332.72

[back to top]

Number of Participants Classified as Responders and Non-responders by Clinician Global Impression of Change Question (CGI-C) Response at Visit 3/PD

"Clinicians were asked to provide their clinical impression regarding change in the participant's shortness of breath by CGI-C. This was evaluated on a 1-5 Likert scale: 1 (much worse) to 5 (much better), with 3 being no change. A CGI-C responder was defined as a participant who had a response of better (4) or much better (5), and a non-responder was defined as a participant who had a response of much worse (1), worse (2), or no change (3)." (NCT00984659)
Timeframe: Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

Interventionparticipants (Number)
RespondersNon-responders
MITT Population: 6-Week Treatment Period120181

[back to top]

Number of Participants Classified as Responders and Non-responders by CRQ-SAS Dyspnea Domain Response at Visit 3/PD

A CRQ-SAS dyspnea domain responder was defined as a participant who had a score increase of 0.5 units or more for the dyspnea domain of the CRQ-SAS between Visit 2 and Visit 3/Premature Discontinuation. A non-responder was defined as a participant who had a decrease in the score, or an increase of less than 0.5 units. (NCT00984659)
Timeframe: Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

Interventionparticipants (Number)
RespondersNon-responders
MITT Population: 6-Week Treatment Period117184

[back to top]

Number of Participants Classified as Responders and Non-responders by Physician-completed and Participant-completed mMRC Response at Visit 3/PD

A Physician-completed and Participant-completed mMRC responder was defined as a participant who had a score decrease of one unit or more between Visit 2 and Visit 3/Premature Discontinuation. A non-responder was defined as a participant who had the same score or an increase in score. (NCT00984659)
Timeframe: Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

Interventionparticipants (Number)
Physician-completed mMRC respondersPhysician-completed mMRC non-respondersParticipant-completed mMRC respondersParticipant-completed mMRC non-responders
MITT Population: 6-Week Treatment Period9121092209

[back to top]

Participants (Par.) Classified as Responders/Non-responders According to the Patient Global Assessment of Change (PGAC) Response at Days 8, 15, 22, 29, 36, and 43 and at Visit 3/Premature Discontinuation (PD) (the End of the 6-week Treatment Period or PD)

"The PGAC is par. completed on a 1-5 scale: 1, much worse; 2, worse; 3, no change; 4, better; 5, much better. Responders were defined as par. with a rating of better or much better (score of 4 or 5) on the PGAC at the relevant week; non-responders were defined as par. with a response of much worse, worse, or no change on the PGAC. As pre-specified in the study protocol, results are presented independent of treatment allocation . The study objectives were to assess the measurement properties and validity of the SOBDA questionnaire independent of specific treatment effect." (NCT00984659)
Timeframe: Days 8, 15, 22, 29, 36, and 43 and Visit 3/PD (end of 6-week Treatment Period or earlier up to Week 8)

Interventionparticipants (Number)
Responders, Day 8 (Baseline to Week 1), n=293Non-responders, Day 8 (Baseline to Week 1), n=293Responders, Day 15 (Week 1 to Week 2), n=303Non-responders, Day 15 (Week 1 to Week 2), n=303Responders, Day 22 (Week 2 to Week 3), n=299Non-responders, Day 22 (Week 2 to Week 3), n=299Responders, Day 29 (Week 3 to Week 4), n=285Non-responders, Day 29 (Week 3 to Week 4), n=285Responders, Day 36 (Week 4 to Week 5), n=277Non-responders, Day 36 (Week 4 to Week 5), n=277Responders, Day 43 (Week 5 to Week 6), n=119Non-responders, Day 43 (Week 5 to Week 6), n=119Responders, Last Treatment Week, n=151Non-responders, Visit 3/PD, n=151
MITT Population: 6-Week Treatment Period10518891212832166222377200318845106

[back to top]

Average FEV1 During the First 15 Minutes Post Dose

Average FEV1 during the first 15 minutes post dose, change versus pre dose FEV1 (NCT01048333)
Timeframe: Pre dose and 15 minutes post dose

Interventionpercentage change (Geometric Mean)
Formoterol1.064
Salmeterol1.041
Placebo1.012

[back to top]

Average FEV1 During 120 Minutes Post Dose

Average FEV1 during 120 minutes post dose, change versus pre dose FEV1 (NCT01048333)
Timeframe: Pre dose and 120 minutes post dose

Interventionpercentage change (Geometric Mean)
Formoterol1.096
Salmeterol1.082
Placebo1.014

[back to top]

Adverse Events

Number of participants with at least 1 AE. (NCT01048333)
Timeframe: At baseline and at each day of treatment

InterventionParticipants (Number)
Formoterol6
Salmeterol6
Placebo2

[back to top]

Percentage of Patients Who Has Achieved at Least 12 % Increase in FEV1

Percentage of patients who has achieved at least 12 % increase in FEV1 at each time point between 5 to 120 minutes post dose, change versus pre dose FEV1 (NCT01048333)
Timeframe: Pre dose, 5, 10, 15, 20, 30, 40, 50, 60 and 120 minutes post dose

,,
InterventionPercentage of Participants (Number)
5 min10 min15 min20 min30 min40 min50 min60 min120 min
Formoterol23.138.039.844.445.449.153.754.655.6
Placebo6.47.39.210.113.815.616.518.320.2
Salmeterol9.217.623.927.532.136.740.443.148.6

[back to top]

FEV1(Forced Expiratory Volume in 1 Second) Measured by Spirometry 5 Minutes Post Dose

FEV1(Forced Expiratory Volume in 1 second) measured by spirometry 5 minutes post dose, percentage change versus pre dose FEV1 (NCT01048333)
Timeframe: Pre-dose and 5 minutes post-dose

Interventionpercentage change (Geometric Mean)
Formoterol1.072
Salmeterol1.041
Placebo1.007

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) After 2 Weeks of Treatment

Spirometry was conducted according to internationally accepted standards. The trough FEV1 was defined as the average of the FEV1 measurements taken at 23 hours 10 minutes and 23 hours 45 minutes post dose. The mixed model used baseline FEV1 and FEV1 prior to and 30 minutes post inhalation of albuterol as covariates. (NCT01079130)
Timeframe: Day 15 (after 2 weeks of treatment)

InterventionLiters (Least Squares Mean)
Indacaterol 18.75 µg2.50
Indacaterol 37.5 µg2.52
Indacaterol 75 µg2.59
Indacaterol 150 µg2.54
Salmeterol2.54
Placebo2.42

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) After 1 Day of Treatment

Spirometry was conducted according to internationally accepted standards. The trough FEV1 was defined as the average of the FEV1 measurements taken at 23 hours 10 minutes and 23 hours 45 minutes post dose on day 2. The mixed model used baseline FEV1 and FEV1 prior to and 30 minutes post inhalation of albuterol as covariates. (NCT01079130)
Timeframe: Day 2 (after 1 day of treatment)

InterventionLiters (Least Squares Mean)
Indacaterol 18.75 µg2.46
Indacaterol 37.5 µg2.52
Indacaterol 75 µg2.54
Indacaterol 150 µg2.60
Salmeterol2.65
Placebo2.45

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose on Day 2

FEV1 was measured with spirometry conducted according to internationally accepted standards. Trough FEV1 was defined as the average of measurements made 23 hours 10 minutes and 23 hours 45 minutes post-dose on Day 2. The analysis included baseline FEV1, FEV1 pre-dose and 10-15 minutes post-dose of salbutamol/albuterol during screening, and FEV1 pre-dose and 1 hour post-dose of ipratropium during screening as covariates. (NCT01089127)
Timeframe: 24 hours post-dose on Day 2

InterventionLiters (Least Squares Mean)
Indacaterol 18.75 μg1.33
Indacaterol 37.5 μg1.34
Indacaterol 75 μg1.38
Indacaterol 150 μg1.40
Salmeterol 50 μg1.41
Placebo1.28

[back to top]

Trough Forced Expiratory Volume in 1 Second (FEV1) 24 Hours Post-dose at the End of the Study (Week 2 + 1 Day, Day 15)

FEV1 was measured with spirometry conducted according to internationally accepted standards. Trough FEV1 was defined as the average of measurements made 23 hours 10 minutes and 23 hours 45 minutes post-dose at the end of treatment. The analysis included baseline FEV1, FEV1 pre-dose and 10-15 minutes post-dose of salbutamol/albuterol during screening, and FEV1 pre-dose and 1 hour post-dose of ipratropium during screening as covariates. (NCT01089127)
Timeframe: 24 hours post-dose at the end of the study (Week 2 + 1 day, Day 15)

InterventionLiters (Least Squares Mean)
Indacaterol 18.75 μg1.35
Indacaterol 37.5 μg1.38
Indacaterol 75 μg1.38
Indacaterol 150 μg1.40
Salmeterol 50 μg1.39
Placebo1.28

[back to top]

Number of EXs of COPD Requiring Hospitalization That Occurred More Than 21 Days Post-discharge or Physician's Office Visit for an EX of COPD Requiring Treatment With OCSs or OCSs and ABs

A COPD EX was defined as the worsening of >=2 major symptoms (dyspnoea, sputum volume, sputum purulence [containing/discharging pus]) or the worsening of any 1 major symptom together with any 1 minor symptom (sore throat, cold [nasal discharge and/or nasal conjestion], fever without other cause, increased cough or wheeze) for at least 2 consecutive days. COPD EXs were identified by symptom review, and/or were based on investigator judgment (via phone contact or at a clinic visit). Hospitalization had to occur more than 21 days post-discharge or physician's office visit for a prior COPD EX. (NCT01110200)
Timeframe: From 21 days post-discharge (hospital or emergency room) or physician's office visit, up to 29 weeks

InterventionExacerbations (Number)
FSC 250/5050
SAL 5051

[back to top]

Number of EXs of COPD Requiring Treatment With OCSs, Treatment With ABs, and/or Hospitalization (Alone and in Combination)

A COPD EX was defined as the worsening of >=2 major symptoms (dyspnoea, sputum volume, sputum purulence [containing/discharging pus]) or the worsening of any 1 major symptom together with any 1 minor symptom (sore throat, cold [nasal discharge and/or nasal conjestion], fever without other cause, increased cough or wheeze) for at least 2 consecutive days. COPD EXs were identified by symptom review, and/or were based on investigator judgment (via phone contact or at a clinic visit). (NCT01110200)
Timeframe: From Baseline up to Week 29, approximately

,
Interventionexacerbations (Number)
Number of EXs, n=314,325Number of EXs requiring hospitalization, n=156,182Number of EXs treated with OCSs, n=156, 182Number of EXs treated with ABs, n=156, 182
FSC 250/5015650140121
SAL 5018251167144

[back to top]

Number of Participants With an EX of COPD Requiring Treatment With OCSs, Treatment With ABs, and/or Hospitalization

A COPD EX was defined as the worsening of >=2 major symptoms (dyspnoea, sputum volume, sputum purulence [containing/discharging pus]) or the worsening of any 1 major symptom together with any 1 minor symptom (sore throat, cold [nasal discharge and/or nasal conjestion], fever without other cause, increased cough or wheeze) for at least 2 consecutive days. COPD EXs were identified by symptom review, and/or were based on investigator judgment (via phone contact or at a clinic visit). (NCT01110200)
Timeframe: From Baseline up to Week 29, approximately

Interventionparticipants (Number)
FSC 250/50102
SAL 50115

[back to top]

Number of Par. With Chronic Obstructive Pulmonary Disease (COPD) EXs Requiring Hospitalization That Occurred >21 Days Post-discharge/Physician's Office Visit for a COPD EX Requiring Treatment With Oral Corticosteroids (OCSs) or OCSs and Antibiotics (ABs)

A COPD exacerbation (EX) was defined as the worsening of >=2 major symptoms (dyspnoea, sputum volume, sputum purulence [containing/discharging pus]) or the worsening of any 1 major symptom together with any 1 minor symptom (sore throat, cold [nasal discharge and/or nasal conjestion], fever without other cause, increased cough or wheeze) for at least 2 consecutive days. COPD EXs were identified by symptom review, and/or were based on investigator judgment (via phone contact or at a clinic visit). Hospitalization had to occur >21 days post-discharge/physician's office visit for a prior COPD EX. (NCT01110200)
Timeframe: From 21 days post-discharge (hospital or emergency room) or physician's office visit, up to 29 weeks

Interventionparticipants (Number)
FSC 250/5043
SAL 5039

[back to top]

Number of Participants With the Indicated Number of EXs of COPD Requiring Hospitalization That Occurred More Than 21 Days Post-discharge or Physician's Office Visit for an EX of COPD Requiring Treatment With OCSs or OCSs and ABs

A COPD EX was defined as the worsening of >=2 major symptoms (dyspnoea, sputum volume, sputum purulence [containing/discharging pus]) or the worsening of any 1 major symptom together with any 1 minor symptom (sore throat, cold [nasal discharge and/or nasal conjestion], fever without other cause, increased cough or wheeze) for at least 2 consecutive days. COPD EXs were identified by symptom review, and/or were based on investigator judgment (via phone contact or at a clinic visit). Hospitalization had to occur more than 21 days post-discharge or physician's office visit for a prior COPD EX. (NCT01110200)
Timeframe: From 21 days post-discharge (hospital or emergency room) or physician's office visit, up to 29 weeks

,
Interventionparticipants (Number)
01234
FSC 250/5027136700
SAL 5028631521

[back to top]

Mean Change in Respiratory Exchange Ratio (RER) Per Time Slope During the Course of the ESWT From Baseline to Week 8

The respiratory exchange ratio was calculated as the ratio of VCO2 and VO2. The ratio of the amount of carbon dioxide and oxygen in the hemoglobin of the participants was measured during the ESWT using the OMS. The system consisted of oxygen and carbon dioxide sensors and allowed breath-by-breath measurement of pulmonary gas exchange parameters. Change from Baseline in RER was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionRatio of VCO2 and VO2 (Mean)
TIO+Placebo-0.01
TIO+FSC0.01

[back to top]

Mean Change in Respiratory Rate (RR) at Isotime During the Course of the ESWT From Baseline to Week 8

RR is defined as the number of breaths taken within a set amount of time (typically within 60 secs). The RR of the participants at isotime was measured during the ESWT using the OMS. Change from Baseline in RR at isotime was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

Interventionbreaths/min (Mean)
TIO+Placebo0.8
TIO+FSC-0.5

[back to top]

Mean Change in Respiratory Rate (RR) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8

RR is defined as the number of breaths taken within a set amount of time (typically within 60 secs). The RR of the participants was measured during the ESWT using the OMS. The system consisted of volume transducer oxygen and carbon dioxide sensors and allowed breath-by-breath measurement of pulmonary gas exchange parameters. The RR per time slope was calculated for each participant by fitting a linear regression line to the RR recorded for each participant during the ESWT. RR per time slope results were compared between treatment groups as means of these regression lines. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

Interventionbreaths/min/min (Mean)
TIO+Placebo-0.1
TIO+FSC-0.5

[back to top]

Mean Change in Scores on the Exercise Dyspnea Scale (EDS) From Baseline (Week 3) to Week 8

EDS is used to measure the level of breathlessness due to exercise, assessed using a 10-point modified Borg scale at 2-minute intervals during the ESWT: 0=no difficulty in breathing at all, 10=maximal breathing difficulty (BD). The participant pointed to the level on the scale correlating with his BD, and the local study coordinator confirmed that level verbally to him. Change from Baseline was calculated as the value at Week 8 minus the value at Baseline. A dyspnea score/time slope was calculated by fitting a linear regression line to the dyspnea scores reported during the exercise tests. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionScores on a scale/minute (Mean)
TIO+Placebo-0.1
TIO+FSC-0.06

[back to top]

Mean Change in Tidal Volume (VT) at Isotime During the Course of the ESWT From Baseline to Week 8

VT is defined as the lung volume representing the normal volume of air displaced between normal inspiration and expiration when extra effort is not applied. The normal value is approximately 500 mL or 7 mL/kg body weight. The VT of the participants at isotime was measured during the ESWT using the OMS. Change from Baseline in VT at isotime was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionL (Mean)
TIO+Placebo-0.10
TIO+FSC0.08

[back to top]

Mean Change in Tidal Volume (VT) Per Time Slope During the Course of the ESWT From Baseline to Week 8

VT is the lung volume representing the normal volume of air displaced between normal inspiration and expiration when extra effort is not applied (normal value is approximately 500 mL or 7 mL/kg body weight). VT was measured during the ESWT using the OMS, consisting of volume transducer O2 and CO2 sensors and allowing breath-by-breath measurement of pulmonary gas exchange parameters. The participant's VT per time slope was calculated by fitting a linear regression line (RL) to their VT during the ESWT. VT per time slope results were compared between treatment groups as means of these RLs. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionL/min (Mean)
TIO+Placebo-0.02
TIO+FSC0

[back to top]

Baseline Dyspnea Index (BDI) at Week 4 and Transition Dyspnea Index (TDI) at Week 8

The BDI-TDI is a multidimensional dyspnea measurement. The BDI, administered at Week 4, consisted of 3 items (functional impairment, magnitude of task in exertional capacity, and magnitude of effort) requiring recall over the previous 4 weeks. BDI scores ranged from 0 (very severe impairment) to 4 (no impairment); the summed total score = 0 to 12. The TDI, administered at Week 8 as a follow-up of the BDI, consisted of the same 3 items requiring recall over the previous 4 weeks. TDI scores ranged from -3 (major deterioration) to +3 (major improvement); the summed total score = -9 to 9. (NCT01124422)
Timeframe: BDI: Week 4; TDI: Week 8

,
InterventionScores on a scale (Mean)
BDI; n=130; 122TDI; n=121, 115
TIO+FSC6.91.4
TIO+Placebo6.71.1

[back to top]

Mean Change in Pre-dose and Post-dose Resting Inspiratory Capacity (IC) From Baseline (Week 4) to Week 8

Resting IC is the volume of gas that can be taken into the lungs in a full inhalation at the resting position. The resting IC was measured before and after dosing. Change from Baseline in pre-dose resting IC was calculated as the pre-dose value at Week 8 minus the pre-dose value at Week 4. Change from Baseline in post-dose resting IC was calculated as the post-dose value at Week 8 minus the pre-dose value at Week 4. (NCT01124422)
Timeframe: Baseline (Week 4) and Week 8

,
InterventionMilliliters (mL) (Mean)
Pre-dosePost-dose
TIO+FSC60167
TIO+Placebo-2973

[back to top]

Mean Change in Scores on the Chronic Respiratory Disease Questionnaire Self-Administered Standardized (CRQ-SAS) Questionnaire From Week 4 to Week 8

The CRQ-SAS, a self-administered tool used to assess health-related quality-of-life (HRQOL), consists of 20 questions (q.) in 4 domains: Dyspnea (5 q.), Fatigue (4 q.), Emotional Function (7 q.), and Mastery (4 q.). Participants rated their experience on a 7-point scale in response to each q.: 1 (maximum impairment) to 7 (no impairment); higher scores indicate better HRQOL. Individual q. were equally weighted, and domain scores (range=1-7) were calculated as the mean across the non-missing items within each domain (domain scores were calculated although an individual item score was missing). (NCT01124422)
Timeframe: Week 4 and Week 8

,
InterventionScores on a scale (Mean)
Mastery ScoreFatigue ScoreEmotional Function ScoreDyspnea Score
TIO+FSC0.090.260.130.32
TIO+Placebo0.070.110.100.21

[back to top]

Mean Change in Flow of Oxygen (V'O2) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8

The V'O2 was measured during the ESWT using the Oxycon Mobile System (OMS), a portable telemetric monitoring system consisting of an oxygen sensor allowing for breath-by-breath measurement of gas exchange parameters in the lungs. The V'O2 was collected in units of mL and then regressed over the conduct of the exercise test measured in minutes. The V'O2 per time slope was calculated for each participant (par.) by fitting a linear regression line to the V'O2 recorded for each par. during the ESWT. V'O2 per time slope results were compared between treatment groups as means of these regression lin (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionmL/minute (min) (Mean)
TIO+Placebo-13.3
TIO+FSC-6.1

[back to top]

Mean Change in Exercise Inspiratory Capacity (EIC) at the End of Exercise From Baseline (Week 3) to Week 8

EIC is the volume of gas that can be taken into the lungs in a full inhalation during exercise. Participants were asked to undergo the IC test every 2 minutes during exercise and at the end of the exercise, to follow changes in operational lung volumes that occured in association with exercise. Change from Baseline in EIC was calculated as the value at the end of exercise at Week 8 minus the value at the end of exercise at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionmL (Mean)
TIO+Placebo-7.4
TIO+FSC46.6

[back to top]

Mean Change in EDS at Isotime From Baseline (Week 3) to Week 8

EDS at isotime (last common time point for an exercise assessment [i.e., last Borg score time point of the shortest exercise test for each participant]) was assessed using a 10-point modified Borg scale. Change from Baseline in EDS at isotime was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionScores on a scale (Mean)
TIO+Placebo-0.3
TIO+FSC-0.5

[back to top]

Mean Change in EIC at 2 to 3.5 Minutes During the Exercise Period From Baseline (Week 3) to Week 8

The EIC was measured at 2 to 3.5 minutes during the exercise period. Change from Baseline in EIC was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionmL (Mean)
TIO+Placebo-148.3
TIO+FSC200

[back to top]

Mean Change in Exercise Endurance Time (EET) From Baseline (Week 3) to Week 8

EET is defined as the time taken by a participant to exert himself during an exercise. EET was calculated based on the Endurance Shuttle Walk test (ESWT). The ESWT is a standardized, externally controlled, constant-paced field test for the assessment of endurance capacity in participants with chronic lung disease. Change from Baseline in EET was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionSeconds (sec) (Mean)
TIO+Placebo23.3
TIO+FSC6.0

[back to top]

Mean Change in Flow of Carbon Dioxide (V'CO2) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8

The amount of CO2 in the hemoglobin of the participants was measured during the ESWT using the OMS. The system consisted of a carbon dioxide sensor and allowed breath-by-breath measurement of pulmonary gas exchange parameters. The V'CO2 per time slope was calculated for each participant by fitting a linear regression line to the V'CO2 recorded for each participant during the ESWT. V'CO2 per time slope results were compared between treatment groups as means of these regression lines. Change from Baseline in V'CO2 per time slope was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionmL/min (Mean)
TIO+Placebo-17.4
TIO+FSC-0.7

[back to top]

Mean Change in Heart Rate (HR) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8

HR is defined as the number of heartbeats per unit of time, typically expressed as beats per minute (bpm). It was measured during the ESWT using the OMS. The HR was collected in units of bpm and then regressed over the conduct of the exercise test measured in minutes. The HR per time slope was calculated for each participant by fitting a linear regression line to the HR recorded for each participant during the exercise test. HR per time slope results were compared between treatment groups as means of these regression lines. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

Interventionbpm/min (Mean)
TIO+Placebo-1.1
TIO+FSC0.7

[back to top]

Mean Change in HR Per Time Slope During the Course of the ESWT Using Pulse Oximetry From Baseline to Week 8 (Non-OMS Subgroup)

HR was measured during the course of the ESWT in the non-OMS subgroup using pulse oximetry. The HR per time slope was calculated for each participant by fitting a linear regression line to the HR recorded for each participant during the ESWT. HR per time slope results were compared between treatment groups as means of these regression lines. Change from Baseline in HR was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

Interventionbpm/min (Mean)
TIO+Placebo-0.8
TIO+FSC-0.6

[back to top]

Mean Change in Minute Ventilation (V'E) Per Time Slope During the Course of the ESWT From Baseline (Week 3) to Week 8

The V'E was measured in the participants during the ESWT using the OMS. The system consisted of a volume transducer, oxygen sensor, and carbon dioxide sensor and allowed breath-by-breath measurement of pulmonary gas exchange parameters. The V'E was collected in liters and then regressed over the conduct of the exercise test measured in minutes. The V'E per time slope was calculated for each participant by fitting a linear regression line to the V'E recorded for each participant during the ESWT. V'E per time slope results were compared between treatment groups as means of the regression lines. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

InterventionLiter (L)/min (Mean)
TIO+Placebo-0.7
TIO+FSC-0.2

[back to top]

Mean Change in Ratio of Respiratory Rate (RR) to Tidal Volume (VT) or RR/VT at Isotime During the Course of the ESWT From Baseline to Week 8

The RR and VT of the participants at isotime were measured during the ESWT using the OMS. The ratio of RR per VT (value of RR divided by value of VT) at isotime was calculated. Change from Baseline in RR/VT at isotime was calculated as the value at Week 8 minus the value at Baseline. (NCT01124422)
Timeframe: Baseline (Week 3) and Week 8

Interventionbreaths/min/L (Mean)
TIO+Placebo2.7
TIO+FSC-2.5

[back to top]

Change From Baseline in EQ-5D Visual Analog Scale (VAS) Score at Day 168

"The EQ-5D is a standardized, 2-part, self-assessment instrument, designed for self-completion, used to measure health outcome. The first part consists of 5 items covering 5 dimensions (mobility, self care, usual activities, pain/discomfort, and anxiety/depression). The second part is a 20 centimeter VAS that has endpoints labelled best imaginable health state and worst imaginable health state anchored at 100 and 0, respectively. Participants were asked to indicate how they rate their own health by drawing a line from an anchor box to that point on the EQ-VAS that best represents their own health on that day. Analysis was performed using ANCOVA with covariates of Baseline VAS score, country, sex, age, and treatment." (NCT01147848)
Timeframe: Baseline and Day 168

Interventionscores on a scale (Least Squares Mean)
Fluticasone Furoate/Vilanterol 100/25 µg OD5.5
Fluticasone Propionate/Salmeterol 250/50 µg BID4.1

[back to top]

"Percentage of Participants With No Problems in the EQ-5D Descriptive System Dimensions at Day 168/Week 24"

"The EQ-5D is a standardized, 2-part, self-assessment instrument, designed for self-completion, used to measure health outcome. The first part consists of 5 items covering 5 dimensions (mobility, self care, usual activities, pain/discomfort, and anxiety/depression). Each dimension is measured by a three-point Likert scale (1=no problems, 2=some problems and 3=severe problems). Respondents are asked to choose one level that reflects their own health state today for each of the five dimensions." (NCT01147848)
Timeframe: Day 168/Week 24

,
Interventionpercentage of participants (Number)
MobilitySelf careUsual activitiesPain/DiscomfortAnxiety/Depression
Fluticasone Furoate/Vilanterol 100/25 µg OD8698867078
Fluticasone Propionate/Salmeterol 250/50 µg BID8498826681

[back to top]

Change From Baseline in Weighted-mean 24 Hour Serial FEV1 on Day 168/Week 24

Pulmonary function was measured by FEV1, defined as the maximal amount of air that can be forcefully exhaled in one second. The weighted mean was calculated from the pre-dose FEV1 and post-dose FEV1 measurements at 5, 15, and 30 minutes (min) and at 1, 2, 3, 4, 11, 12, 12.5, 13, 14, 16, 20, 23, and 24 hours, respectively, on Day 168/Week 24. Change from Baseline was calculated as the weighted mean of the 24-hour serial FEV1 measures on Day 168/Week 24 minus the Baseline value. Baseline was the pre-dose measurement on Day 1. Analysis was performed using analysis of covariance (ANCOVA) with covariates of Baseline FEV1, region, sex, age, and treatment. (NCT01147848)
Timeframe: Baseline and Day 168/Week 24

InterventionLiters (Least Squares Mean)
Fluticasone Furoate/Vilanterol 100/25 µg OD0.341
Fluticasone Propionate/Salmeterol 250/50 µg BID0.377

[back to top]

Change From Baseline in Weighted Mean Serial FEV1 Over 0-4 Hours Post First Dose (at Randomization)

The weighted mean serial FEV1 (the maximal amount of air that can be forcefully exhaled in one second) over 0-4 hours post-dose at Baseline was derived using actual times and using the pre-dose assessment as the 0 hour measurement. Change from Baseline was calculated as the weighted mean of the 4-hour serial FEV1 measures on Day 1 minus the Baseline value. Baseline was the pre-dose measurement on Day 1. Analysis was performed using ANCOVA with covariates of Baseline FEV1, region, sex, age, and treatment. (NCT01147848)
Timeframe: Baseline and Randomization

InterventionLiters (Least Squares Mean)
FFluticasone Furoate/Vilanterol 100/25 µg OD0.316
Fluticasone Propionate/Salmeterol 250/50 µg BID0.346

[back to top]

Change From Baseline in Weighted Mean Serial FEV1 Over 0-4 Hours at Day 168

The weighted mean serial FEV1 (the maximal amount of air that can be forcefully exhaled in one second) over 0-4 hours post-dose at Baseline and Day 168 was derived using actual times and using the pre-dose assessment as the 0 hour measurement. Change from Baseline was calculated as the weighted mean of the 4-hour serial FEV1 measures on Day 168/Week 24 minus the Baseline value. Baseline was the pre-dose measurement on Day 1. Analysis was performed using ANCOVA with covariates of Baseline FEV1, region, sex, age, and treatment. (NCT01147848)
Timeframe: Baseline and Day 168

InterventionLiters (Mean)
Fluticasone Furoate/Vilanterol 100/25 µg OD0.360
Fluticasone Propionate/Salmeterol 250/50 µg BID0.394

[back to top]

Change From Baseline in Trough FEV1 at Day 168

Pulmonary function was measured by FEV1, defined as the maximal amount of air that can be forcefully exhaled in one second . Trough FEV1 is defined as the pre-dose measurement on Day 168/Week 24. Any missing data at Day 168/Week 24 was imputed using the last observation carried forward (LOCF). Baseline was the pre-dose measurement on Day 1. Change from Baseline was calculated as the pre-dose measurement on Day 168/Week 24 minus the Baseline value. (NCT01147848)
Timeframe: Baseline and Day 168

InterventionLiters (Least Squares Mean)
Fluticasone Furoate/Vilanterol 100/25 µg OD0.281
Fluticasone Propionate/Salmeterol 250/50 µg BID0.300

[back to top]

Serial FEV1 (0-24 Hours)

Pulmonary function was measured by FEV1, defined as the maximal amount of air that can be forcefully exhaled in one second . The pre-dose FEV1 assessment and the individual serial FEV1 assessments at Day 168/Week 24 at the indicated time points (pre-dose, 5 minutes, 15 minutes, 30 minutes, 1 hour, 2 hours, 3 hours, 4 hours, 11 hours, 12 hours, 12.5 hours, 13 hours, 14 hours, 16 hours, 20 hours, 23 hours, and 24 hour s) were summarized. (NCT01147848)
Timeframe: Day 168

,
InterventionLiters (Mean)
Pre-dose, n=359,3535 minutes, n=356, 34415 minutes, n=355, 34730 minutes, n=357, 3511 hour, n=358, 3532 hours, n=359, 3533 hours, n=357, 3534 hours, n=357, 35411 hours, n=359, 34712 hours, n=356, 35412.5 hours, n=357, 35213 hours, n=354, 35414 hours, n=356, 35316 hours, n=354, 35020 hours, n=355, 35223 hours, n=354, 35324 hours, n=354, 354
Fluticasone Furoate/Vilanterol 100/25 µg OD0.3040.3200.3230.3390.3440.3620.3730.3560.3050.3300.3300.3430.3570.3510.3210.3100.304
Fluticasone Propionate/Salmeterol 250/50 µg BID0.3230.3390.3540.3660.3900.4090.4190.4170.3190.3380.3800.3960.4260.4190.3760.3440.340

[back to top]

Number of Participants With the Indicated Time to Onset of Bronchodilator Effect at Day 1

Time to onset of bronchodilator effect at Day 1 is defined as the actual time during the 4-hour serial FEV1 (the maximal amount of air that can be forcefully exhaled in one second) measurements that the participant first meets or exceeds a 12% and 200 mL increase over Baseline and was derived at Day 1 only. Time to onset was calculated over 0 to 4 hours (5 minutes, 15 minutes, 30 minutes, 1 hour, 2 hours, 3 hours, and 4 hours) post-dose. Participants who never exceeded a 12% and 200 mL increase over Baseline were censored at the actual time of their last FEV1 measurement. (NCT01147848)
Timeframe: Baseline to Day 1

,
Interventionparticipants (Number)
5 minutes15 minutes30 minutes1 hour2 hours3 hours4 hoursCensored
Fluticasone Furoate/Vilanterol 100/25 µg OD100414032191711140
Fluticasone Propionate/Salmeterol 250/50 µg BID85515539291212118

[back to top]

Number of Participants Obtaining a >=12% and >=200 mL Increase From Baseline in FEV1

The number of participants obtaining a >=12% and >=200 mL increase from Baseline in FEV1 (the maximal amount of air that can be forcefully exhaled in one second) was evaluated at 12-hours post-dose and at 24-hours post-dose on Day 168. (NCT01147848)
Timeframe: Baseline and Day 168

,
Interventionparticipants (Number)
12 hours post-dose, n=356,35424 hours post-dose, n=354, 354
Fluticasone Furoate/Vilanterol 100/25 µg OD199181
Fluticasone Propionate/Salmeterol 250/50 µg BID178176

[back to top] [back to top]

Baseline FEV1 by Completion Status

Pulmonary function was measured by FEV1, defined as the maximal amount of air that can be forcefully exhaled in one second . Baseline is defined as the mean of the two assessments made 30 minutes pre-dose and 5 minutes pre-dose on Treatment Day 1. (NCT01147848)
Timeframe: Baseline

,
InterventionLiters (Mean)
All Participants, n=401, 401Completers, n=359, 355Withdrawals, n=42, 46
Fluticasone Furoate/Vilanterol 100/25 µg OD2.0112.0131.996
Fluticasone Propionate/Salmeterol 250/50 µg BID2.0482.0432.091

[back to top]

Change From Baseline in Asthma Quality of Life Questionnaire (AQLQ) Total Score for Participants 12 Years of Age and Older (AQLQ + 12)

"The AQLQ is a disease-specific, self-administered quality of life (QOL) questionnaire developed to evaluate the impact of asthma treatments on the QOL of asthma sufferers. The AQLQ contains 32 items in four domains: activity limitation (11 items), symptoms (12 items), emotional function (5 items), and environmental stimuli (4 items). The response format consists of a 7-point scale: a value of 1 indicates total impairment; a value of 7 indicates no impairment. The AQLQ total score is defined as the average of the scores from all 32 questions, provided at least 90% of the questions have been answered; thus, the total score ranges from 1 (indicates total impairment) to 7 (indicates no impairment). Change from Baseline was calculated as the Day 168 value minus the Baseline value. Analysis was performed using ANCOVA with covariates of Baseline total AQLQ score, country, sex, age, and treatment." (NCT01147848)
Timeframe: Baseline and Day 168

InterventionScores on a scale (Least Squares Mean)
Fluticasone Furoate/Vilanterol 100/25 µg OD0.46
Fluticasone Propionate/Salmeterol 250/50 µg BID0.37

[back to top]

Change From Baseline in Asthma Control Test (ACT) Scores at Day 168

"The ACT is a 5-item questionnaire developed as a measure of the participant's asthma control. Questions are designed to be self-completed by the participant and include the following: In the past 4 weeks, How much of the time did your asthma keep you from getting as much done at work, school or at home?, How often have you had shortness of breath?, How often did your asthma symptoms wake you up at night or earlier than usual in the morning?, How often have you used your rescue inhaler or nebulizer medication (such as albuterol)? and How would you rate your asthma control? The ACT total score is defined as the sum of the scores from all 5 questions, provided all questions have been answered; thus, the total score ranges from 5 (poor control of asthma) to 25 (complete control of asthma). A score of 20 or higher indicates well-controlled asthma. Change from Baseline was calculated as the Day 168 value minus the Baseline value." (NCT01147848)
Timeframe: Baseline and Day 168

InterventionScores on a scale (Least Squares Mean)
Fluticasone Furoate/Vilanterol 100/25 µg OD2.3
Fluticasone Propionate/Salmeterol 250/50 µg BID2.0

[back to top]

Mean Pre-dose Evening FEV1 (FEV1 p.m.) Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionLitre (Mean)
Placebo-0.000
Tio R2.50.065
Tio R50.039
Salmeterol0.072

[back to top]

Asthma Symptom-free Days Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. An asthma symptom-free day was defined as a day with no reported symptoms and no use of rescue medication. (NCT01172808)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionDays (Mean)
Placebo0.162
Tio R2.50.207
Tio R50.157
Salmeterol0.266

[back to top]

FEV1 Area Under Curve 0-3 Hours (AUC0-3h) Response

Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2) determined at the end of the 24-week treatment. Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. FEV1 AUC 0-3h was calculated from 0-3 hours post-dose using the trapezoidal rule, divided by the observation time (3h) to report in litres. (NCT01172808)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo-0.033
Tio R2.50.192
Tio R50.163
Salmeterol0.182

[back to top]

Mean Number of Puffs of Rescue Medication During the Entire 24-h Day Based on the Weekly Mean Response at Week 24

Daily use of salbutamol (albuterol) rescue medication as needed during the entire study period. Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionNumber of Puffs (Mean)
Placebo-0.962
Tio R2.5-1.124
Tio R5-0.818
Salmeterol-1.416

[back to top]

Time to First Severe Asthma Exacerbation From the Two Twin Trials 205.419 (NCT01172821) and the Present 205.418 (NCT01172808)

Time to first severe asthma exacerbation during the 24-week treatment period on combined data from the two twin trials 205.418 (NCT01172808) and 205.419 (NCT01172821). (NCT01172808)
Timeframe: 24 weeks

Interventionweeks (Median)
PlaceboNA
Tio R2.5NA
Tio R5NA
SalmeterolNA

[back to top]

Trough PEF Response

Trough peak expiratory flow (PEF) response determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: 24 weeks

InterventionLitre/min (Mean)
Placebo2.913
Tio R2.540.819
Tio R536.590
Salmeterol31.317

[back to top]

FVC Area Under Curve 0-3 Hours (AUC0-3h) Response

Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2) determined at the end of the 24-week treatment. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. FVC AUC 0-3h was calculated from 0-3 hours post-dose using the trapezoidal rule, divided by the observation time (3h) to report in litres. (NCT01172808)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo-0.066
Tio R2.50.092
Tio R50.041
Salmeterol0.062

[back to top]

Trough FVC Response

Trough FVC response determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo-0.039
Tio R2.50.086
Tio R50.036
Salmeterol0.028

[back to top]

Trough FEV1 Response

Trough FEV1 response determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo-0.036
Tio R2.50.148
Tio R50.115
Salmeterol0.086

[back to top]

Total Asthma Quality of Life Questionnaire (AQLQs)) Score

Total score from the Standardised Asthma Quality of Life Questionnaire (AQLQ(s)) determined at the end of 24-week treatment. The AQLQ(s) contains 32 questions, each question has a 7 point scale from 1 (highest intensity) till 7 (no symptoms). Total score was defined as the sum of all items divided by the number of items. Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Placebo5.449
Tio R2.55.522
Tio R55.519
Salmeterol5.654

[back to top]

Total Asthma Control Questionnaire (ACQ) Score at the End of the 24-week Treatment Period

Control of asthma as assessed by the ACQ determined at the end of 24-week treatment. The ACQ contains 7 questions, each question has a 7 point scale from 0 (no symptoms) till 6 (highest intensity). Total score was defined as the sum of all items divided by the number of items. Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Placebo1.563
Tio R2.51.362
Tio R51.431
Salmeterol1.302

[back to top]

Time to First Asthma Exacerbation From the Two Twin Trials 205.419 (NCT01172821) and the Present 205.418 (NCT01172808)

Time to first asthma exacerbation (including severe, non-severe; symptomatic, asymptomatic; i.e. any exacerbation) during the 24-week treatment period on combined data from the two twin trials 205.418 (NCT01172808) and 205.419 (NCT01172821) (NCT01172808)
Timeframe: 24 weeks

Interventionweeks (Median)
PlaceboNA
Tio R2.5NA
Tio R5NA
SalmeterolNA

[back to top]

The Responder Rate as Assessed by the ACQ From the Two Twin Trials 205.419 (NCT01172821) and the Present 205.418 (NCT01172808)

"The responder rate as assessed by the Asthma Control Questionnaire (ACQ) determined at the end of the 24-week treatment period (on combined data from the two twin trials 205.418 (NCT01172808) and 205.419 (NCT01172821)). A patient was considered to be a responder if he or she was reported with an improvement (decrease) in the ACQ total score of at least 0.5 points.~The ACQ total score was calculated as the mean of the responses to 7 questions and was analysed as an absolute value. The score ranges from 0 (no impairment) to 6 (maximum impairment)." (NCT01172808)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
Placebo57.7
Tio R2.564.5
Tio R564.3
Salmeterol66.5

[back to top]

The Responder Rate as Assessed by the ACQ

The responder rate as assessed by the Asthma Control Questionnaire (ACQ) determined at the end of the 24-week treatment period. A patient was considered to be a responder if he or she was reported with an improvement (decrease) in ACQ total score of at least 0.5 points. The ACQ total score was calculated as the mean of the responses to 7 questions and was analysed as an absolute value. The score ranges from 0 (no impairment) to 6 (maximum impairment). (NCT01172808)
Timeframe: 24 weeks

InterventionPercentage of Participants (Number)
Placebo53.2
Tio R2.562.5
Tio R566.7
Salmeterol68.6

[back to top]

PEF Variability

PEF daily variability was assesed by patients at home using the AM3 device. PEF variability is the absolute difference between morning and evening PEF value divided by their mean, based on the weekly mean response at week 24. Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: Last 7 days before week 24 visit

InterventionPercentage of mean PEF (Mean)
Placebo-1.400
Tio R2.5-1.958
Tio R50.180
Salmeterol-2.300

[back to top]

Peak FVC Within 3 Hours Post-dose Response

Peak forced vital capacity (FVC) response within 3 hours post-dose determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo0.045
Tio R2.50.219
Tio R50.148
Salmeterol0.168

[back to top]

Peak FEV1 Within 3 Hours Post-dose Response

Peak forced expiratory volume in one second (FEV1) response within 3 hours post-dose determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo0.053
Tio R2.50.289
Tio R50.250
Salmeterol0.266

[back to top]

Mean Pre-dose Morning PEF (PEF a.m.) Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionLitre/min (Mean)
Placebo-10.159
Tio R2.520.432
Tio R513.501
Salmeterol22.467

[back to top]

Mean Pre-dose Morning FEV1 (FEV1 a.m.) Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionLitre (Mean)
Placebo0.021
Tio R2.50.101
Tio R50.073
Salmeterol0.117

[back to top]

Mean Pre-dose Evening PEF (PEF p.m.) Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172808)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionLitre/min (Mean)
Placebo-9.181
Tio R2.518.978
Tio R515.188
Salmeterol19.727

[back to top]

The Responder Rate as Assessed by the ACQ From the Two Twin Trials 205.418 (NCT01172808) and the Present 205.419 (NCT01172821)

The responder rate as assessed by the Asthma Control Questionnaire (ACQ) determined at the end of the 24-week treatment period (on combined data from the two twin trials 205.418 (NCT01172808) and 205.419 (NCT01172821)). A patient was considered to be a responder if he or she was reported with an improvement (decrease) in the ACQ total score of at least 0.5 points. (NCT01172821)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
Placebo57.7
Tio R2.564.5
Tio R564.3
Salmeterol66.5

[back to top]

Time to First Asthma Exacerbation From the Two Twin Trials 205.418 (NCT01172808) and the Present 205.419 (NCT01172821)

Time to first asthma exacerbation (including severe, non-severe; symptomatic, asymptomatic; i.e. any exacerbation) during the 24-week treatment period on combined data from the two twin trials 205.418 (NCT01172808) and 205.419 (NCT01172821) (NCT01172821)
Timeframe: 24 weeks

Interventionweeks (Median)
PlaceboNA
Tio R2.5NA
Tio R5NA
SalmeterolNA

[back to top]

Time to First Severe Asthma Exacerbation From the Two Twin Trials 205.418 (NCT01172808) and the Present 205.419 (NCT01172821)

Time to first severe asthma exacerbation during the 24-week treatment period on combined data from the two twin trials 205.418 (NCT01172808) and 205.419 (NCT01172821) (NCT01172821)
Timeframe: 24 weeks

Interventionweeks (Median)
PlaceboNA
Tio R2.5NA
Tio R5NA
SalmeterolNA

[back to top]

Total Asthma Control Questionnaire (ACQ) Score

Control of asthma as assessed by the ACQ determined at the end of 24-week treatment. The ACQ contains 7 questions, each question has a 7 point scale from 0 (no symptoms) till 6 (highest intensity). Total score was defined as the sum of all items divided by the number of items and ranges from from 0 (no symptoms) till 6 (highest intensity). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Placebo1.442
Tio R2.51.315
Tio R51.359
Salmeterol1.318

[back to top]

Total Asthma Quality of Life Questionnaire (AQLQs)) Score

"Total score from the Standardised Asthma Quality of Life Questionnaire (AQLQ(s)) determined at the end of 24-week treatment.~The AQLQ(s) contains 32 questions, each question has a 7 point scale from 1 (highest intensity) till 7 (no symptoms). Total score was defined as the sum of all items divided by the number of items and ranges from from 1 (highest intensity) till 7 (no symptoms). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week." (NCT01172821)
Timeframe: 24 weeks

Interventionunits on a scale (Mean)
Placebo5.551
Tio R2.55.562
Tio R55.548
Salmeterol5.634

[back to top]

Trough FEV1 Response

Trough FEV1 response determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo-0.012
Tio R2.50.164
Tio R50.121
Salmeterol0.094

[back to top]

Trough FVC Response

Trough FVC response determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo-0.048
Tio R2.50.039
Tio R50.035
Salmeterol0.020

[back to top]

Trough PEF Response

Trough peak expiratory flow (PEF) response determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: 24 weeks

InterventionLitre/min (Mean)
Placebo7.938
Tio R2.536.698
Tio R536.117
Salmeterol29.352

[back to top]

Asthma Symptom-free Days Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. An asthma symptom-free day was defined as a day with no reported symptoms and no use of rescue medication. (NCT01172821)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionDays (Mean)
Placebo0.189
Tio R2.50.164
Tio R50.196
Salmeterol0.195

[back to top]

FEV1 Area Under Curve 0-3 Hours (AUC0-3h) Response

Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2) determined at the end of the 24- week treatment. Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. FEV1 AUC 0-3h was calculated from 0-3 hours post-dose using the trapezoidal rule, divided by the observation time (3h) to report in litres. (NCT01172821)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo-0.005
Tio R2.50.196
Tio R50.158
Salmeterol0.173

[back to top]

FVC Area Under Curve 0-3 Hours (AUC0-3h) Response

Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2) determined at the end of the 24- week treatment. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. FVC AUC 0-3h was calculated from 0-3 hours post-dose using the trapezoidal rule, divided by the observation time (3h) to report in litres. (NCT01172821)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo-0.065
Tio R2.50.043
Tio R50.024
Salmeterol0.066

[back to top]

Mean Number of Puffs of Rescue Medication During the Entire 24-h Day Based on the Weekly Mean Response at Week 24

Daily use of salbutamol (albuterol) rescue medication as needed during the entire study period. Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionNumber of Puffs (Mean)
Placebo-0.952
Tio R2.5-1.123
Tio R5-0.843
Salmeterol-1.078

[back to top]

Mean Pre-dose Evening FEV1 (FEV1 p.m.) Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionLitre (Mean)
Placebo-0.002
Tio R2.50.066
Tio R50.064
Salmeterol0.048

[back to top]

Mean Pre-dose Evening PEF (PEF p.m.) Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionLitre/min (Mean)
Placebo-0.072
Tio R2.515.919
Tio R521.175
Salmeterol11.617

[back to top]

Mean Pre-dose Morning FEV1 (FEV1 a.m.) Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionLitre (Mean)
Placebo0.020
Tio R2.50.099
Tio R50.084
Salmeterol0.103

[back to top]

Mean Pre-dose Morning PEF (PEF a.m.) Based on the Weekly Mean Response at Week 24

Weekly means obtained during the last 7 days before week 24 measured by patients at home using the AM3 device. Response was defined as change from baseline. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week (NCT01172821)
Timeframe: Baseline and last 7 days before week 24 visit

InterventionLitre/min (Mean)
Placebo2.764
Tio R2.523.377
Tio R527.521
Salmeterol19.779

[back to top]

Peak FEV1 Within 3 Hours Post-dose Response

Peak forced expiratory volume in one second (FEV1) response within 3 hours post-dose determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo0.075
Tio R2.50.287
Tio R50.244
Salmeterol0.252

[back to top]

Peak FVC Within 3 Hours Post-dose Response

Peak forced vital capacity (FVC) response within 3 hours post-dose determined at the end of the 24-week treatment. Response was defined as change from baseline (10 minutes before the first dose of trial medication at visit 2). Means are adjusted for treatment, centre, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: 24 weeks

InterventionLitre (Mean)
Placebo0.071
Tio R2.50.181
Tio R50.160
Salmeterol0.188

[back to top]

PEF Variability

PEF daily variability was assesed by patients at home using the AM3 device. PEF variability is the absolute difference between morning and evening PEF value divided by their mean, based on the weekly mean response at week 24. Means are adjusted for treatment, country, week, baseline, treatment by week, and baseline by week. (NCT01172821)
Timeframe: Last 7 days before week 24 visit

InterventionPercentage of Mean PEF (Mean)
Placebo-0.448
Tio R2.5-1.401
Tio R5-0.627
Salmeterol-1.518

[back to top]

The Responder Rate as Assessed by the ACQ

The responder rate as assessed by the Asthma Control Questionnaire (ACQ) determined at the end of the 24-week treatment period. A patient was considered to be a responder if he or she was reported with an improvement (decrease) in ACQ total score of at least 0.5 points.The score ranges from 0 (no impairment) to 6 (maximum impairment). (NCT01172821)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
Placebo62.5
Tio R2.566.4
Tio R561.9
Salmeterol64.4

[back to top]

Change From Baseline in Weighted-mean 24-hour Serial Forced Expiratory Volume in One Second (FEV1) at Week 12

FEV1 is a measure of lung function and is defined as the volume of air that can be forcefully exhaled in one second. The weighted mean is calculated from the pre-dose FEV1 and post-dose FEV1 measurements at 5, 15, and 30 minutes (min) and at 1, 2, 3, 4, 11, 12, 12.5, 13, 14, 16, 20, 23, and 24 hours, respectively, at Week 12. The Baseline value was the Day 1 pre-dose FEV1 measurement. Change from Baseline is calculated as the weighted mean 0-24 hour FEV1 (Liters) at Week 12 minus the Baseline value. Analysis was performed using analysis of covariance (ANCOVA) with covariates of Baseline FEV1, region, sex, age, and treatment. (NCT01181895)
Timeframe: Baseline and Week 12

InterventionLiters (Least Squares Mean)
Placebo0.289
Vilanteral 25 µg OD0.359
Salmeterol 50 µg BID0.283

[back to top]

Change From Baseline in Individual Serial FEV1 Assessments at the End of the 12-week Treatment Period, Including the 12-hour and 24-hour Time Points

FEV1 is a measure of lung function and is defined as the volume of air that can be forcefully exhaled in one second. The individual serial FEV1 is calculated from the pre-dose FEV1 and post-dose FEV1 measurements at 5, 15, 30, and 60 minutes (min) and 2, 3, 5, 11, 12, 12.5, 13, 14, 16, 20, 23, and 24 hours, relatively, on Treatment Day 84 (Week 12). The Baseline value was the Day 1 pre-dose FEV1 measurement. Change from Baseline was calculated as the value of the individual serial FEV1 taken at Week 12 minus the Baseline value. Analysis was performed using ANCOVA with covariates of Baseline FEV1, region, sex, age, and treatment. Analysis was performed separately for each planned time point. (NCT01181895)
Timeframe: Baseline and Week 12

,,
InterventionLiters (Least Squares Mean)
Predose, n=97,104,1015 min, n=95,100,9815 min, n=96, 101, 9930 min, n=,96,101,10060 min, n=96, 101, 1002 hours, n=96, 100, 993 hours, n=96, 101, 1004 hours, n=96, 101, 1005 hours, n=96, 100, 10011 hours, n=94, 99, 9612 hours, n=93,98,9512.5 hours, n=96, 97, 9813 hours, 96, 98, 10014 hours, n=95, 99, 9916 hours, n=95, 98, 9720 hours, n= 94, 101, 9923 hours, 94, 101, 9924 hours, n= 95, 101, 100
Placebo0.3020.3130.3080.3220.3360.3130.3040.3110.2920.1950.2500.2700.3120.3410.3640.3180.3100.301
Salmeterol 50 µg BID0.2330.2140.2570.2720.2960.3350.3160.2930.2790.1790.2170.2820.3040.3590.3570.2960.2710.275
Vilanteral 25 µg OD0.2720.3010.3240.3440.3520.3690.3740.3590.3680.3120.3410.3370.3410.4010.3710.3710.3450.330

[back to top]

Number of Participants With the Indicated Global Assessment of Change Questionnaire Responses at the End of Week 4 and Week 12

At the end of Week 4 and Week 12, the Global Assessment of Change Questionnaire, which assesses changes in asthma symptoms and rescue medication use, was completed by participants using the following scale: asthma symptom (AS) change: much better, somewhat better, a little better, the same, a little worse, somewhat worse, much worse; rescue medication use (RMU): much less often , somewhat less often , a little less often , the same , a little more often , somewhat more often , much more often. (NCT01181895)
Timeframe: Week 4 and Week 12

,,
InterventionParticipants (Number)
Week 4, AS: Much better, n=110, 109, 110Week 4, AS: Somewhat better, n=110, 109, 110Week 4, AS: A little better, n=110, 109, 110Week 4, AS: The same, n=110, 109, 110Week 4, AS: A little worse, n=110, 109, 110Week 4, AS: Somewhat worse, n=110, 109, 110Week 4, AS: Much worse, n=110, 109, 110Week 4, RMU: Much less often, n=110, 109, 110Week 4, RMU: Somewhat less often, n=110, 109, 110Week 4, RMU: A little less often, n=110, 109, 110Week 4, RMU: The same, n=110, 109, 110Week 4, RMU: A little more often, n=110, 109, 110Week 4, RMU: Somewhat more often, n=110, 109, 110Week 4, RMU: Much more often, n=110, 109, 110Week 12, AS: Much better, n=100, 105, 101Week 12, AS: Somewhat better, n=100, 105, 101Week 12, AS: A little better, n=100, 105, 101Week 12, AS: The same, n=100, 105, 101Week 12, AS: A little worse, n=100, 105, 101Week 12, AS: Somewhat worse, n=100, 105, 101Week 12, AS: Much worse, n=100, 105, 101Week 12, RMU: Much less often, n=100, 105, 101Week 12, RMU: Somewhat less often, n=100, 105, 101Week 12, RMU: A little less often, n=100, 105, 101Week 12, RMU: The same, n=100, 105, 101Week 12, RMU: A little more often, n=100, 105, 101Week 12, RMU: Somewhat more often, n=100, 105, 101Week 12, RMU: Much more often, n=100, 105, 101
Placebo25352417621184018264223135131244125311323242
Salmeterol 50 µg BID34342116320283620177203534161141032291321420
Vilanteral 25 µg OD374314131013331231830152319921140321611501

[back to top]

Number of Participants With the Indicated Time to an Increase of >=12% and >=200 Milliliters (mL) Above Baseline in FEV1 on Day 1 and Day 84 (0-2 Hours)

The number of participants with a >=12% and >=200 mL increase from Baseline in FEV1 (the maximal amount of air that can be forcefully exhaled in one second) was evaluated on Day 1 and Week 12 for the time to a >=12% increase from Baseline (at the 5 minutes (min), 15 min, 30 min, 1hour (hr), and 2 hr nominal time points. Participants who did not achieve a >=12% and >=200 mL increase from Baseline in FEV1 over this time period were considered censored. (NCT01181895)
Timeframe: Day 1 and Week 12

,,
InterventionParticipants (Number)
Day 1, 5 min, n=113, 115, 116Day 1, 15 min, n=113, 115, 116Day 1, 30 min, n=113, 115, 1116Day 1, 1 hr, n=113, 115, 116Day 1, 2 hr, n=113, 115, 116Day 1, Censored, n=113, 115, 116Week 12, 5 min, n=96, 101, 100Week 12, 15 min, n=96, 101, 100Week 12, 30 min, n=96, 101, 100Week 12, 1 hr, n=96, 101, 100Week 12, 2 hr, n=96, 101, 100Week 12, Censored, n=96, 101, 100
Placebo2323357739621345
Salmeterol 50 µg BID1811136115730785446
Vilanteral 25 µg OD33118765042224744

[back to top]

Change From Baseline in Daily AM (Morning) PEF Averaged Over the 12-week Treatment Period

PEF is defined as the maximum airflow during a forced expiration beginning with the lungs fully inflated. Trough PEF is the PEF measured approximately 24 hours after the last administration of study drug. The Baseline value is the average value of the last 7 days of daily AM PEF prior to randomization. Change from Baseline in trough AM PEF was calculated as the averaged value of all daily AM PEF for Weeks 1 to Week 12 minus the value at Baseline. Analysis was performed using ANCOVA with covariates of Baseline, region, sex, age, and treatment. (NCT01181895)
Timeframe: Baseline and Weeks 1-12

InterventionLiters per minute (L/min) (Least Squares Mean)
Placebo14.2
Vilanteral 25 µg OD28.0
Salmeterol 50 µg BID23.6

[back to top]

Change From Baseline in Daily Trough (Pre-dose and Pre-rescue Bronchodilator) PM (Evening) Peak Expiratory Flow (PEF) Averaged Over the 12-week Treatment Period

PEF is defined as the maximum airflow during a forced expiration beginning with the lungs fully inflated. Trough PEF is the PEF measured approximately 24 hours after the last administration of study drug. The Baseline value is the average value of the last 7 days of daily PM PEF prior to randomization. Change from Baseline in trough PM PEF was calculated as the averaged value of all daily PM PEF for Week 1 to Week 12 minus the value at Baseline. Analysis was performed using ANCOVA with covariates of Baseline, region, sex, age, and treatment. (NCT01181895)
Timeframe: Baseline and Weeks 1-12

InterventionLiters per minute (L/min) (Least Squares Mean)
Placebo11.0
Vilanteral 25 µg OD24.9
Salmeterol 50 µg BID18.8

[back to top]

Change From Baseline in the Percentage of Rescue-free 24-hour (hr) Periods During the 12-week Treatment Period

The time span during which the participants did not have to take any rescue bronchodilator (medication intended to relieve symptoms immediately) was considered to be a rescue-free period. The Baseline value was derived from the last 7 days of the daily diary prior to the randomization of the participant (including the day of randomization). Change from Baseline is calculated as the value at Weeks 1-12 minus the value at Baseline. Analysis was performed using ANCOVA with covariates of Baseline, region, sex, age, and treatment. (NCT01181895)
Timeframe: Baseline and Weeks 1-12

InterventionPercentage of rescue-free 24-hr periods (Least Squares Mean)
Placebo14.6
Vilanteral 25 µg OD21.7
Salmeterol 50 µg BID22.9

[back to top]

Change From Baseline in the Percentage of Symptom-free 24-hour (hr) Periods During the 12-week Treatment Period

Participants who were symptom free for 24-hour periods during the12-week treatment period were assessed. The Baseline value was derived from the last 7 days of the daily diary prior to the randomization of the participant (including the day of randomization). Change from Baseline is calculated as the value at Weeks 1-12 minus the value at Baseline. Analysis was performed using ANCOVA with covariates of Baseline, region, sex, age, and treatment. (NCT01181895)
Timeframe: Baseline and Weeks 1-12

InterventionPercentage of symptom-free 24-hr periods (Least Squares Mean)
Placebo12.7
Vilanteral 25 µg OD19.4
Salmeterol 50 µg BID19.5

[back to top]

Mean Duration of Worsening Asthma Symptoms Associated With the Presence of Moderate or Severe URTS or a Confirmed RV Infection

A worsening asthma day is one on which any of the following occurred: rescue albuterol use above baseline, use of oral/parenteral corticosteroids for asthma, use of asthma medication other than study medication, asthma symptom scores >=3, nighttime awakenings, unscheduled health care visits, or missed school due to asthma. The duration of worsening asthma is the number of consecutive worsening asthma days after the date of a URTS score of 2 (moderate) or 3 (severe) or collection of a mucus sample containing RV (whichever occurred first). Each span of consecutive days is a participant interval. (NCT01192178)
Timeframe: Peak Viral Period (from 30 August 2010 through the end of treatment [up to Week 16])

InterventionDays per participant interval (Mean)
FSC DISKUS 100/50 mcg BID4.1
FP DISKUS 100 mcg BID4.0

[back to top]

Number of Asthma Exacerbations Associated With the Presence of Moderate or Severe URTS or a Confirmed RV Infection During the Peak Viral Period

Each participant (with assistance from the parent/legal guardian as needed) was instructed to keep an electronic diary (eDiary) with record of daily URTS symptoms that included: runny nose, sneezing, nasal congestion, and sore throat. Based on the best-described aggregate URTS during the previous 24 hours, participants rated symptoms as: 0 = Not present; 1 = Mild, clearly present; 2 = Moderately severe, uncomfortable; and 3 = Severe, interfering with sleep or activity. Mucus samples were collected and analyzed for RVwhen the eDiary alerted for moderate/severe URTS. (NCT01192178)
Timeframe: Peak Viral Period (from 30 August 2010 through the end of treatment [up to Week 16])

InterventionNumber of asthma exacerbations (Number)
FSC DISKUS 100/50 mcg BID5
FP DISKUS 100 mcg BID7

[back to top]

Mean Percentage of Symptom-free Days

A symptom-free day was defined as a day during the Peak Viral Period on which the asthma symptom score was zero. The daily asthma symptom score (measured during the day and the previous night) was reported on a 6-point scale (ranging from 0=no symptoms to 5=severe symptoms). Percentage of symptom-free days was defined as the number of days during the Peak Viral Period on which the asthma symptom score=0, divided by the number of days in that same period on which non-missing values were recorded, multiplied by 100. (NCT01192178)
Timeframe: Peak Viral Period (from 30 August 2010 through the end of treatment [up to Week 16])

InterventionPercentage of days (Mean)
FSC DISKUS 100/50 mcg BID90.1
FP DISKUS 100 mcg BID91.1

[back to top]

Mean Percentage of Rescue-free Days

A rescue-free day was defined as a day during the Peak Viral Period on which no puffs of rescue medication were recorded. Percentage of rescue-free days was defined as the number of days during the Peak Viral Period on which no puffs of rescue medication were recorded, divided by the number of days in that same period on which non-missing values were recorded, multiplied by 100. (NCT01192178)
Timeframe: Peak Viral Period (from 30 August 2010 through the end of treatment [up to Week 16])

InterventionPercentage of days (Mean)
FSC DISKUS 100/50 mcg BID92.1
FP DISKUS 100 mcg BID91.7

[back to top]

Mean Percentage of Episode-free (EF) Days

An EF day was defined as a day without any of the following: rescue albuterol use, use of oral/parenteral corticosteroids for asthma, use of asthma medication other than study treatment, asthma symptom score >0, nighttime awakenings due to asthma, unscheduled health care visits (defined as home visits, office visits, or urgent care visits), ER visits, hospitalizations for asthma, school absenteeism due to asthma, or morning peak expiratory flow (measure of maximum airflow) <80% of baseline. Percentage of EF days=No. of EF days divided by No. of days of treatment exposure, multiplied by 100. (NCT01192178)
Timeframe: Peak Viral Period (from 30 August 2010 through the end of treatment [up to Week 16])

InterventionPercentage of days (Mean)
FSC DISKUS 100/50 mcg BID42.4
FP DISKUS 100 mcg BID44.5

[back to top]

Mean Percentage of Asthma-control Days

An asthma-control day was defined as a day without any of the following: rescue albuterol use, use of oral/parenteral corticosteroids for asthma, use of asthma medication other than double-blind study treatment, asthma symptom score >0, nighttime awakenings due to asthma, unscheduled health care visits (defined as home visits, office visits, or urgent care visits), ER visits, hospitalizations for asthma, or school absenteeism due to asthma. The percentage of asthma-control days = the number (No.) of asthma-control days divided by the No. of days of treatment exposure, multiplied by 100. (NCT01192178)
Timeframe: Peak Viral Period (from 30 August 2010 through the end of treatment [up to Week 16])

InterventionPercentage of days (Mean)
FSC DISKUS 100/50 mcg BID48.3
FP DISKUS 100 mcg BID49.7

[back to top]

Mean Asthma Symptom Scores, as an Indicator of Severity, Associated With the Presence of Moderate or Severe Upper Respiratory Tract Symptoms (URTS) or a Confirmed Rhinovirus (RV) Infection at Baseline and During the Peak Viral Period

Participants recorded their asthma symptom score over the previous 24 hours (during the day and the previous night) using the following 6-point scale: 0=No symptoms; 1=Symptoms for 1 short period; 2=Symptoms for >=2 short periods; 3=Symptoms for most of the day/previous night that did not affect normal daily activities; 4=Symptoms for most of the day/previous night that affected normal daily activities; 5=Symptoms so severe that participant could not perform normal daily activities. The Baseline mean asthma symptom score was calculated as the average score over 7 days prior to Week 1, Visit 2. (NCT01192178)
Timeframe: Baseline (Week 1) and Peak Viral Period ([period during which the greatest number of viral infections is expected] from 30 August 2010 through the end of the treatment period [up to Week 16])

,
InterventionScores on a scale (Mean)
Baseline, n=105, 104Peak Viral Period, n=106, 104
FP DISKUS 100 mcg BID0.20.4
FSC DISKUS 100/50 mcg BID0.20.5

[back to top]

Total Number of Asthma Exacerbations Reported During the Treatment Period

An asthma exacerbation was defined as deterioration of asthma that required the use of outpatient oral/parenteral corticosteroids (tablets, suspensions, or injection) or an urgent care, hospitalization, or emergency room (ER) visit due to asthma that required oral/parenteral corticosteroids. Two exacerbations (out of a total of 51) were excluded: (1) one exacerbation occurred within 7 days of the resolution of an earlier one, and, per protocol, was combined with the previous exacerbation; and (2) one exacerbation occurred post treatment. (NCT01192178)
Timeframe: From Baseline (Week 1) until the end of treatment (up to Week 16)

InterventionNumber of asthma exacerbations (Number)
FSC DISKUS 100/50 mcg BID24
FP DISKUS 100 mcg BID25

[back to top]

Maximum Change From Baseline in Airway Blood Flow (Qaw)

(NCT01231230)
Timeframe: maximum change in Qaw within 240 minutes post drug inhalation

Interventionchange from baseline ( µl/min/ml) (Mean)
Fluticasone-11.0
Placebo14.1
Salmeterol23.9
Fluticasone/Salmeterol25.5

[back to top]

Change in Asthma Quality of Life (AQLQ)

"Average Change in Asthma Quality of Life Score Per Participant Over 12 Months Using the Asthma Quality of Life Questionnaire (AQLQ).~The AQLQ has 32 questions in four domains (symptoms, activity limitation, emotional function, and environmental stimuli) and measures the functional problems that are troublesome to individuals with asthma. Symptoms (11 items), Activity Limitation (12 items, 5 of which are individualized), Emotional Function (5 items), and Environmental Exposure (4 items); 7-point Likert scale (7 = not impaired at all - 1 = severely impaired); scores range 1-7, with higher scores indicating better quality of life." (NCT01290874)
Timeframe: from baseline to 12 months

Interventionunits on a scale (Mean)
Tiotropium1.00
Salmeterol or Formoterol1.02

[back to top]

Change in Asthma Control Questionnaire (ACQ)

"Average Change in Asthma Control Score Per Participant Over 12 Months Using the Asthma Control Questionnaire (ACQ).~The ACQ has six questions regarding symptoms, rescue short-acting β-agonist use and one about FEV1 % predicted. A 7-point scale (0 = no impairment, 6 = maximum impairment) is used for each question and the ACQ score is the mean value of these questions - hence between 0 (totally controlled) and 6 (severely uncontrolled)." (NCT01290874)
Timeframe: from baseline to 12 months

Interventionunits on a scale (Mean)
Tiotropium-0.70
Salmeterol or Formoterol-0.66

[back to top]

Time to Asthma Exacerbation (Mean Number of Exacerbations/Person-year)

We summarize the survival experience using mean number of exacerbations/person-year and compare it using the log-rank test comparing kaplan-meier survival curve. (NCT01290874)
Timeframe: evaluated monthly (on average) via questionnaire for 12 months

Interventionevent per person-year (Mean)
Tiotropium0.37
Salmeterol or Formoterol0.42

[back to top]

Change in Rescue Medication Use

Average Change in Rescue Medication Use Per Participant Over 12 Months. Monthly questionnaires will evaluate the amount of rescue medication subjects have used on average, measured in puffs per day. (NCT01290874)
Timeframe: from baseline to 12 months

Interventionunits on a scale (Mean)
Tiotropium-0.92
Salmeterol or Formoterol-0.97

[back to top]

Change in FEV1

Average change in lung function (FEV1) evaluated by spirometry per participant over 12 months (NCT01290874)
Timeframe: from baseline to 12 months

Interventionliters (Mean)
Tiotropium-0.018
Salmeterol or Formoterol0.003

[back to top]

Change in Asthma Symptom Utility Index (ASUI)

"Average Change in Asthma Symptom Utility Score Per Participant Over 12 Months Using the Asthma Symptom Utility Index (ASUI).~The ASUI is an 11-item preference-based outcome measure used in clinical trials and cost-effectiveness studies for asthma and is designed to assess the frequency and severity of cough, wheeze, dyspnea, nighttime awakenings, and side effects, weighted according to patient preferences.~4-point Likert scale to assess frequency (not at all, 1 to 3 days, 4 to 7 days, and 8 to 14 days) and severity (not applicable, mild, moderate and severe); scores range from 0 (worst possible symptoms) to 1 (no symptoms)." (NCT01290874)
Timeframe: from baseline to 12 months

Interventionunits on a scale (Mean)
Tiotropium0.11
Salmeterol or Formoterol0.10

[back to top]

Percentage of Participants With Asthma Exacerbation

An asthma exacerbation was defined as the occurrence of any of the following: ≥30% reduction from baseline in morning PEF on 2 consecutive days; or ≥6 additional reliever puffs of albuterol or levalbuterol in a 24-hour period (compared to baseline) on 2 consecutive days; or deterioration of asthma, as determined by the investigator, requiring systemic steroid treatment, or an increase in inhaled corticosteroid (ICS) of ≥4 times the last dose received prior to discontinuation from the study, or hospitalization. The occurrence of asthma exacerbations by individual criteria are reported. (NCT01312961)
Timeframe: Baseline up to Week 12

,
Interventionpercentage of participants (Number)
Asthma exacerbation≥30% reduction from baseline in morning PEF≥6additional albuterol/levalbuterol puffsSystemic steroid treatmentIncrease in ICS ≥4 times baseline dose of ICSHospitalization
Dupilumab 300 mg qw5.81.91.91.90.00.0
Placebo (for Dupilumab)44.219.219.29.65.80.0

[back to top]

Change From Baseline in Peak Expiratory Flow (PEF) to Week 12

The PEF is a participant's maximum speed of expiration, as measured with a peak flow meter. Peak flow testing for PEF was performed at home (morning and evening) while sitting or standing prior to using any medication (if needed) for asthma. (NCT01312961)
Timeframe: Baseline, Week 12

,
Interventionliters/minute (Mean)
Change in morning PEFChange in evening PEF
Dupilumab 300 mg qw10.6-3.4
Placebo (for Dupilumab)-11.2-15.6

[back to top]

Percentage of Participants With Composite Asthma Events

Composite asthma event was defined as a 30% or greater reduction from baseline in morning PEF on 2 consecutive days together with 6 or more additional reliever puffs of albuterol or levalbuterol in a 24-hour period (compared to baseline) on 2 consecutive days. (NCT01312961)
Timeframe: Baseline up to Week 12

Interventionpercentage of participants (Number)
Placebo (for Dupilumab)1.9
Dupilumab 300 mg qw0

[back to top]

Change From Baseline in Number of Nocturnal Awakenings Per Day to Week 12

Participants recorded every morning on awakening the number of asthma-related nocturnal awakenings requiring use of rescue medication that occurred during the previous night. (NCT01312961)
Timeframe: Baseline, Week 12

Interventionnumber of awakenings/day (Mean)
Placebo (for Dupilumab)0.1
Dupilumab 300 mg qw-0.3

[back to top]

Change From Baseline in Number of Inhalations Per Day of Albuterol or Levalbuterol to Week 12

Number of Albuterol or Levalbuterol inhalations were recorded daily by the participants in their electronic diary as Albuterol or Levalbuterol was to be used only as needed for symptoms, not on a regular basis or prophylactically. (NCT01312961)
Timeframe: Baseline, Week 12

Interventionnumber of inhalations/day (Mean)
Placebo (for Dupilumab)0.4
Dupilumab 300 mg qw-1.3

[back to top]

Change From Baseline in Morning Asthma Symptom Scores to Week 12

AM (ante meridiem) symptom scoring system rates were participant's overall asthma symptoms experienced during the night. It ranges from 0 to 4 as: 0 = No asthma symptoms, slept through the night, 1= Slept well, but some complaints in the morning. No nighttime awakenings,2= Woke up once because of asthma (including early awakening),3= Woke up several times because of asthma (including early awakening), 4= Bad night, awake most of the night because of asthma. (NCT01312961)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Mean)
Placebo (for Dupilumab)0.3
Dupilumab 300 mg qw-0.4

[back to top]

Change From Baseline in Forced Expiratory Flow in One Second (FEV1) to Week 12

FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation. (NCT01312961)
Timeframe: Baseline, Week 12

InterventionLiters (Mean)
Placebo-0.12
Dupilumab 300 mg qw0.06

[back to top]

Change From Baseline in Evening Asthma Symptom Scores to Week 12

PM (post meridiem) symptom scoring system rates were participant's overall asthma symptoms experienced during the day. It ranges from 0 to 4 as: 0=very well, no asthma symptoms, 1=one episode of wheezing, cough, or breathlessness, 2=more than one episode of wheezing, cough, or breathlessness without interference of normal activities, 3=wheezing, cough, or breathlessness most of the day, which interfered to some extent with normal activities, 4=asthma very bad, unable to carry out daily activities as usual. (NCT01312961)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Mean)
Placebo (for Dupilumab)0.1
Dupilumab 300 mg qw-0.5

[back to top]

Change From Baseline in Asthma Control Questionnaire (5-question Version [ACQ-5]) to Week 12

ACQ-5 questionnaire is a validated questionnaire comprising of 5 questions for asthma symptoms: woken at night by symptoms, wake in the mornings with symptoms, limitation of daily activities, shortness of breath, and wheeze. Participants were asked to rate their asthma symptoms during the previous week on a 7-point scale as 0=no impairment, 6=maximum impairment. ACQ-5 score is the mean of the 5 questions and range between 0 (disease totally controlled) and 6 (disease severely uncontrolled), a higher score indicated lower asthma control. (NCT01312961)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Mean)
Placebo (for Dupilumab)-0.50
Dupilumab 300 mg qw-1.07

[back to top]

Change From Baseline in 22-item Sinonasal Outcome Test (SNOT-22) Score to Week 12

The SNOT-22 is a validated measure of health related quality of life in sinonasal disease. It is a 22 item questionnaire with each item assigned a score ranging from 0-5. The total score may range from 0 (no disease) -110 (worst disease), lower scores represent better health related quality of life. (NCT01312961)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Mean)
Placebo (for Dupilumab)1.27
Dupilumab 300 mg qw-9.17

[back to top]

Time to First Asthma Exacerbation: Kaplan-Meier Estimates at Week 4, Week 8 and Week 12

The time-to-asthma exacerbation was defined as the time from the date of randomization to the date of the first asthma exacerbation event; for participants without asthma exacerbation, it was censored at the end of treatment visit date. The median time to first asthma exacerbation was not estimated because the number of asthma exacerbations was too low in the Dupilumab arm. Therefore, alternative Kaplan-Meier statistics, the probability of asthma exacerbation at Week 4, 8 and 12, are presented as the descriptive measure statistics. (NCT01312961)
Timeframe: Baseline up to Week 12

,
InterventionProbability of asthma exacerbation (Number)
Probability at Week 4Probability at Week 8Probability at Week 12
Dupilumab 300 mg qw0.0380.0580.058
Placebo (for Dupilumab)0.0580.2450.460

[back to top]

Mean Change From Baseline in Daily Number of Puffs of Rescue Medication

Participants maintained a diary to record the daily number of puffs of rescue medication used to treat COPD symptoms. (NCT01315249)
Timeframe: Baseline, 12 weeks and 26 weeks

,
Interventionpuffs (Least Squares Mean)
Weeks 1 to12Weeks 1 to 26
Fluticasone/Salmeterol-1.90-1.93
QVA149-2.18-2.32

[back to top]

Inspiratory Capacity (IC) at All-time Points (26 Weeks)

After 26 weeks of treatment, Inspiratory Capacity (IC) was measured via spirometry, conducted according to internationally accepted standards. The mean of 3 acceptable measurements was calculated and reported in liters. (NCT01315249)
Timeframe: 26 weeks

,
InterventionLiters (Least Squares Mean)
-20 minutes (n=53 QVA149; 63 flut/salm)25 minutes (n=58 QVA149; 63 flut/salm)1 hour (n=53 QVA149; 63 flut/salm)3 hours (n=52 QVA149; 60 flut/salm)7 hours (n=56 QVA149; 61 flut/salm)11 hours (n=57 QVA149; 66 flut/salm)
Fluticasone/Salmeterol2.222.342.352.322.302.27
QVA1492.252.412.382.332.402.37

[back to top]

Inspiratory Capacity (IC) at All-time Points (12 Weeks)

After 12 weeks of treatment, Inspiratory Capacity (IC) was measured via spirometry, conducted according to internationally accepted standards. The mean of 3 acceptable measurements was calculated and reported in liters. (NCT01315249)
Timeframe: 12 weeks

,
InterventionLiters (Least Squares Mean)
-20 minutes (n=51 QVA149; 65 flut/salm)25 minutes (n=56 QVA149; 71 flut/salm)1 hour (n=59 QVA149; 68 flut/salm)3 hours (n=54 QVA149; 67 flut/salm)7 hours (n=58 QVA149; 67 flut/salm)11 hours (n=49 QVA149; 72 flut/salm)
Fluticasone/Salmeterol2.312.422.432.452.412.34
QVA1492.392.552.542.522.422.40

[back to top]

Forced Vital Capacity at All-time Points (Week 26)

"Forced Vital Capacity (FVC) is the amount of air which can be forcibly exhaled from the lungs after taking the deepest breath possible. FVC was assessed via spirometry. A positive change from baseline in FVC indicates improvement in lung function.~This outcome measures absolute values at -45 min, -15 min predose; 5 min, 30 min, 1 hr, 2hr, 4 hr, 8 hr, 12 hr post-dose on week 26. Results are obtained from linear mixed model." (NCT01315249)
Timeframe: -45 min, -15 min predose; 5 min, 30 min, 1 hr, 2hr, 4 hr, 8 hr, 12 hr post-dose on week 26

,
Interventionliters (Least Squares Mean)
-45 minutes (n=213 QVA149; 216 flut/salm)-15 minutes (n=213 QVA149; 215 flut/salm)5 minutes (n=212 QVA149; 215 flut/salm)30 minutes (n=212 QVA149; 214 flut/salm)1 hour (n=212 QVA149; 216 flut/salm)2 hours (n=212 QVA149; 216 flut/salm)4 hours (n=212 QVA149; 215 flut/salm)8 hours (n=212 QVA149; 216 flut/salm)12 hours (n=211 QVA149; 213 flut/salm)
Fluticasone/Salmeterol3.133.123.173.233.233.293.283.213.18
QVA1493.323.333.423.473.503.513.453.403.40

[back to top]

Forced Vital Capacity at All-time Points (Week 12)

"Forced Vital Capacity (FVC) is the amount of air which can be forcibly exhaled from the lungs after taking the deepest breath possible. FVC was assessed via spirometry. A positive change from baseline in FVC indicates improvement in lung function.~This outcome measures absolute values at -45 min, -15 min predose; 5 min, 30 min, 1 hr, 2hr, 4 hr, 8 hr, 12 hr post-dose week 12. Results are obtained from linear mixed model." (NCT01315249)
Timeframe: -45 min, -15 min predose; 5 min, 30 min, 1 hr, 2hr, 4 hr, 8 hr, 12 hr post-dose on week 12

,
Interventionliters (Least Squares Mean)
-45 minutes (n=230 QVA149; 237 flut/salm)-15 minutes (n=228 QVA149; 235 flut/salm)5 minutes (n=229 QVA149; 236 flut/salm)30 minutes (n=229 QVA149; 235 flut/salm)1 hour (n=228 QVA149; 236 flut/salm)2 hours (n=229 QVA149; 237 flut/salm)4 hours (n=228 QVA149; 237 flut/salm)8 hours (n=228 QVA149; 237 flut/salm)12 hours (n=228 QVA149; 236 flut/salm)
Fluticasone/Salmeterol3.163.173.203.233.263.313.333.273.26
QVA1493.373.373.443.483.493.543.493.463.45

[back to top]

Focal Score of the Transitional Dyspnea Index (TDI)

Transition Dyspnea Index (TDI) captures changes from baseline. The TDI score is based on three domains with each domain scored from -3 (major deterioration) to +3 (major improvement), to give an overall score of -9 to +9, a negative score indicating a deterioration from baseline. A TDI focal score of 1 is considered to be a clinically significant improvement. (NCT01315249)
Timeframe: 12 weeks and 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
12 weeks (n=224 QVA149; 236 flut/salm)26 weeks (n=212 QVA149; 213 flut/salm)
Fluticasone/Salmeterol1.451.60
QVA1492.032.36

[back to top]

Change From Baseline in Symptom Scores Reported Using the Ediary

"Participants maintained an ediary to record daily symptom scores (AM and PM) over 12 weeks and 26 weeks of treatment. This analysis compares the mean symptom scores over 12 weeks and 26 weeks compared to baseline. The diary records morning and evening daily clinical symptoms including cough, wheezing, shortness of breath, sputum volume, sputum purulence, night time awakenings and rescue medication use.~Scale ranges: ranges are 0 to 3 with varying scale descriptions that pertain to the question being asked.~0 is the minimum score = none or No symptoms or never or No~= mild, a little~= moderate~= severe For the scale range provided, high values represent a worse outcome." (NCT01315249)
Timeframe: 12 weeks and 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
Weeks 1-12Weeks 1-26
Fluticasone/Salmeterol-1.17-1.24
QVA149-1.08-1.28

[back to top]

Forced Expiratory Volume in 1 Second Area Under the Curve (FEV1 AUC) 0-12

Forced Expiratory Volume in one second (FEV1) was calculated as the volume of air forcibly exhaled in one second as measured by a spirometer. FEV1 was normalized by 12 hours (divided by time). This outcome measures absolute values at week 26. Results are obtained from linear mixed model. (NCT01315249)
Timeframe: Week 26

Interventionliters (Least Squares Mean)
QVA1491.69
Fluticasone/Salmeterol1.56

[back to top]

Standardized Forced Expiratory Volume in 1 Second Area Under the Curve (FEV1 AUC) 0-12 Hours

Standardized Forced Expiratory Volume in 1 Second (FEV1) was measured with spirometry conducted according to internationally accepted standards. Measurements were made between 0 and 12 hours after treatment. FEV1 was normalized by 12 hours (divided by time). This outcome measures absolute values at week 12. Results are obtained from linear mixed model. (NCT01315249)
Timeframe: Week 12

Interventionliters (Least Squares Mean)
QVA1491.71
Fluticasone/Salmeterol1.59

[back to top]

Total Score of the St. George's Respiratory Questionnaire (SGRQ-C)

The total score of the St. George's Respiratory Questionnaire (SGRQ-C) is a health related quality of life questionnaire consisting of 51 items in three components: symptoms, activity, and impacts. The lowest possible value is zero and the highest 100. Higher values correspond to greater impairment in quality of life. (NCT01315249)
Timeframe: 12 weeks and 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
12 weeks (n=230 QVA149; 238 flut/salm)26 weeks (n=211 QVA149; 216 flut/salm)
Fluticasone/Salmeterol36.0336.68
QVA14936.7435.45

[back to top]

Number of Participants With Adverse Events

The assessment of safety was based on Adverse Events. A summary of adverse events is presented with this outcome, additional details are provided in Adverse Events Section. (NCT01315249)
Timeframe: 26 weeks

,
Interventionparticipants (Number)
Any Adverse EventDeathSerious Adverse EventsDiscontinued due to Adverse EventsDiscontinued due to Serious Adverse EventsDiscontinued due to non-Serious Adverse Events
Fluticasone/Salmeterol15911427918
QVA14914301322517

[back to top]

Time to Onset on Treatment Day 1

Time to onset on Treatment Day 1 is defined as the time to an increase of 100 milliliters (mL) from Baseline in FEV1. Time to onset was calculated over 0 to 4 hours (5 min, 15 min, 30 min, 60 min, 120 min, and 240 min) post-dose. (NCT01323621)
Timeframe: Baseline and Day 1

InterventionMinutes (Median)
FSC 250/50 µg BID30
FF/VI 100/25 µg QD16

[back to top]

Change From Baseline Trough in 24-Hour Weighted Mean FEV1 on Treatment Day 84

Pulmonary function was measured by forced expiratory volume in one second (FEV1), defined as the maximal amount of air that can be forcefully exhaled in one second. The weighted mean was calculated from the pre-dose FEV1 and the post-dose FEV1 measurements at 5, 15, 30, and 60 minutes (min) and 2, 4, 6, 8, 12, 13, 14, 16, 20, and 24 hours post-dose on Treatment Day 84. Baseline trough FEV1 was calculated as the mean of the two assessments made 30 and 5 minutes pre-dose on Treatment Day 1. Change from Baseline was calculated as the average of the Day 84 values minus the Baseline value. Analysis of covariance (ANCOVA) was conducted with covariates for country, smoking status, reversibility, and Baseline FEV1. (NCT01323621)
Timeframe: Baseline (Day 1) and Day 84

InterventionLiters (Least Squares Mean)
FSC 250/50 µg BID0.114
FF/VI 100/25 µg QD0.142

[back to top]

Time to Onset on Treatment Day 1

Time to onset on Treatment Day 1 is defined as the time to an increase of 100 milliliters (mL) from Baseline in FEV1. Time of onset was calculated over 0 to 4 hours (5 min, 30 min, 60 min, 120 min, and 240 min) post-dose. (NCT01323634)
Timeframe: Day 1

InterventionMinutes (Median)
FSC 250/50 µg BID30
FF/VI 100/25 µg QD15

[back to top]

Change From Baseline Trough in 24-hour Weighted-mean FEV1 on Treatment Day 84

Pulmonary function was measured by forced expiratory volume in one second (FEV1). The weighted mean was calculated from the pre-dose FEV1 and the post-dose FEV1 measurements at 5, 15, 30, and 60 minutes (min) and 2, 4, 6, 8, 12, 13, 14, 16, 20, and 24 hours on Treatment Day 84. Baseline trough FEV1 was the mean of the two assessments made 30 and 5 minutes pre-dose on Treatment Day 1. Change from Baseline was calculated as the average of the Day 84 values minus the Baseline value. (NCT01323634)
Timeframe: Baseline (Day 1) and Day 84

InterventionLiters (Least Squares Mean)
FSC 250/50 µg BID0.094
FF/VI 100/25 µg QD0.174

[back to top]

Time to First Chronic Obstructive Pulmonary Disease (COPD) Event

The first COPD event occurring after 30 days from initial treatment arm prescription was measured. Four categories of COPD events were analyzed; either a hospitalization or emergency department visit; an emergency department visit; an outpatient visit followed by an oral corticosteroid prescription claim within 10 days; an outpatient visit followed by an oral antibiotic prescription claim within 10 days. (NCT01331694)
Timeframe: Anytime from 30 days to 12 months after initial treatment arm prescription

,,
Interventiondays (Mean)
Hospitalization or emergency department visitEmergency department visitOutpatient visit with oral steroid fillOutpatient visit with antibiotic fill
Risk Population TIO321.59328.48331.23326.70
Risk Population: FSC325.17330.24332.74329.96
Risk Population: IP315.89324.47328.23326.73

[back to top]

Average Annual Adjusted Post-Index COPD-Related Costs

Medical costs are associated with COPD-related medical care (claims submitted with a primary International Classification of Diseases, 9th Revision, Clinical Modification diagnosis of COPD) and pharmaceutical care (treatment arm medications, oral corticosteroids, oral antibiotics, short-acting beta-agonists, long-acting beta-agonists [LABA], inhaled corticosteroids [ICS], ICS/LABA combinations, etc.. Means are adjusted for age, sex, geographic region, pre-initial treatment comorbidities, and COPD-related utilization. Total costs are the sum of medical care and pharmacy costs. (NCT01331694)
Timeframe: Incurred over the 12 month period after initial treatment arm prescription

,,
InterventionUnited States dollars (Mean)
MedicalPharmacyTotal
Cost Population: FSC10769722068
Cost Population: IP24816142841
Cost Population: TIO14199852408

[back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top] [back to top]

Change From Baseline Trough in 24-hour Weighted-mean FEV1 on Treatment Day 84

Pulmonary function was measured by forced expiratory volume in one second (FEV1). The weighted mean was calculated from the pre-dose FEV1 and post-dose FEV1 measurements at 5, 15, 30, and 60 minutes (min) and 2, 4, 6, 8, 12, 13, 14, 16, 20, and 24 hours on Treatment Day 84. Baseline trough FEV1 was the mean of the two assessments made 30 and 5 minutes pre-dose on Treatment Day 1. Change from Baseline was calculated as the average of the Day 84 values minus the Baseline value. (NCT01342913)
Timeframe: Baseline and Day 84

InterventionLiters (Least Squares Mean)
Salmeterol/FP 50/500 µg BID0.108
FF/VI 100/25 µg QD0.130

[back to top]

Time to Onset on Treatment Day 1

Time to onset on Treatment Day 1 is defined as the time to an increase of 100 milliliters (mL) from Baseline in FEV1. Time of onset was calculated over 0 to 4 hours (5 min, 15 min, 30 min, 60 min, 120 min, and 240 min) post-dose. (NCT01342913)
Timeframe: Day 1

InterventionMinutes (Median)
Salmeterol/FP 50/500 µg BID28
FF/VI 100/25 µg QD16

[back to top]

Change From Baseline in Trough FEV1 on Treatment Day 85

Pulmonary function was measured by forced expiratory volume in one second (FEV1). Trough FEV1 was defined as the 24-hour FEV1 assessment, which was obtained on Day 85. Baseline is defined as the mean of the two assessments made 30 minutes pre-dose and 5 minutes pre-dose on Treatment Day 1.Change from Baseline was calculated as the average of the Day 85 values minus the Baseline value. (NCT01342913)
Timeframe: Baseline and Day 85

InterventionLiters (Least Squares Mean)
Salmeterol/FP 50/500 µg BID0.088
FF/VI 100/25 µg QD0.111

[back to top]

Mean Number of Post-index Asthma-related Events Measured Using Medical and Pharmacy Claims

Asthma-related events were defined as events with any primary ICD-9 code of 493.xx for hospitalizations, emergency department visits, and combined hospitalization/emergency department visits. The post-index period is defined as 3-12 months after either the first administration of fluticasone propionate and salmetrol or inhaled corticosteroids. Medical and pharmacy claims are recorded healthcare encounters in a large managed care administrative insurance database. (NCT01347060)
Timeframe: Up to 7 years from July 1, 2001 to June 30, 2008

,
InterventionAsthma-related events (Mean)
Inpatient visitsEmergency department visitsInpatient/emergency department visits
Fluticasone Propionate and Salmeterol0.0330.0220.05
Inhaled Corticosteroids0.0460.0270.07

[back to top]

Mean Asthma-related Costs in the Post-index Period

Asthma-related costs were calculated as pharmacy costs, medical costs, and total asthma (pharmacy plus medical) costs. Medical costs were made up of asthma-related visits, hospitalizations, emergency department visits, and medical office visits. Pharmacy costs were comprised of all asthma-related medications used during the follow-up period. Medical services were identified by place of service and PharMetrics-specific confinement codes. Prescriptions were counted by 30-day fills, with fills less than 30 days rounded up to indicate one fill. (NCT01347060)
Timeframe: Up to 7 years from July 1, 2001 to June 30, 2008

,
InterventionUnited States dollars (Mean)
Medical Services CostsPharmacy CostsTotal Asthma Costs
Fluticasone Propionate and Salmeterol38111281509
Inhaled Corticosteroids4629391401

[back to top]

Mean Number of Albuterol (Short-acting β-Agonists) Canisters Dispensed Per Pharmacy Claim Per Participant

The number of albuterol canisters dispensed was used as a surrogate marker of asthma symptoms. (NCT01347060)
Timeframe: Up to 7 years from July 1, 2001 to June 30, 2008

Interventionalbuterol canisters (Mean)
Fluticasone Propionate and Salmeterol1.01
Inhaled Corticosteroids1.5

[back to top]

Mean Number of Pharmacy Claims by Participants During the Post-Index Period

The mean number of pharmacy claims incurred by participants during the one-year post-index period was measured. (NCT01381471)
Timeframe: One Year

Interventionpharmacy claims (Mean)
Albuterol Pharmacy ClaimsInhaled Corticosteriod Pharmacy ClaimsAnticholinergic Pharmacy ClaimsTheophylline Pharmacy ClaimsOral Corticosteriod Pharmacy ClaimsAntibiotic Pharmacy Claims
Fluticasone Propionate/Salmeterol (FSC)2.9600.2195.4910.5731.5452.181

[back to top]

Mean Number of Healthcare Encounters Incurred by Participants During the Post-Index Period

The mean number of outpatient office visits, inpatient visits, and emergency department visits incurred by participants during the one-year post-index period was measured. (NCT01381471)
Timeframe: One Year

Interventionhealthcare encounters (Mean)
Outpatient Office VisitsEmergency Department VisitsInpatient Visits
Fluticasone Propionate/Salmeterol (FSC)2.0480.1450.078

[back to top] [back to top]

Mean Number of COPD Exacerbations

Moderate COPD exacerbations were defined as the occurrence of a COPD-related emergency department (ED) visit or a COPD-related office visit that is closely followed by a prescription claim for oral steroids or antibiotics. Severe exacerbations were defined as the occurrence of a COPD-related hospital admission. (NCT01387178)
Timeframe: 1 year

,
Interventionnumber of exacerbations (Mean)
Moderate ExacerbationSevere ExacerbationAny Exacerbation
Fluticasone Propionate/Salmeterol 250 Micrograms (µg)/50 µg0.350.050.4
Tiotropium Bromide 18 µg0.290.050.34

[back to top]

Post-index Period COPD-related, Unadjusted Costs

The mean cost per participant for COPD-related healthcare interventions for one year following the index date (first pharmacy claim for fluticasone propionate/salmeterol 250 µg/50 µg [FSC] or tiotropium bromide [TIO]) was calculated. Total medical costs included inpatient, emergency department, and outpatient costs associated with the treatment of COPD. Total pharmacy costs included costs of all COPD-related medications, and total healthcare costs included all medical and pharmacy costs that were related to COPD treatment. These costs were unadjusted and reflect the actual costs. (NCT01387178)
Timeframe: 1 year

,
InterventionUnited States (US) dollars (Mean)
Inpatient servicesEmergency department visitsInpatient and emergency department visitsOffice visitsOther outpatient/ancillary servicesTotal medical costsTotal pharmacy costsTotal healthcare utilization
Fluticasone Propionate/Salmeterol 250 Micrograms (µg)/50 µg68855743231734170912913000
Tiotropium Bromide 18 µg86752919293879209112093299

[back to top]

Change in Forced Expiratory Volume in 1 Second (FEV1) From Baseline at Two Hours After Inhalation of the Study Medication

FEV1 (NCT01391559)
Timeframe: 2 hours

InterventionmL (Mean)
Arformoterol84
Salmeterol52

[back to top]

Pulmonary Function- Change in Peak Expiratory Flow

Change in morning peak expiratory flow rate from the patients' daily diary cards, calculated at 48 weeks minus baseline (randomization) (NCT01437995)
Timeframe: Baseline and 48 weeks

InterventionLiters per minute (Median)
Stable ICS-LABA-0.08
Reduced ICS/LABA4.40
LABA Step Off-14.16

[back to top]

Pulmonary Function: Change in FEV1/FVC Ratio

Change in participant's FEV1/FVC ratio calculated as 48 weeks minus baseline. (NCT01437995)
Timeframe: Baseline and 48 weeks

Interventionratio (Median)
Stable ICS-LABA-0.002
Reduced ICS/LABA-0.009
LABA Step Off-0.02

[back to top]

Change in Pulmonary Function: FEV1 and FVC

Change in participant's pre-bronchodilator pulmonary function tests (FEV1 and FVC) calculated as 48 weeks minus baseline. (NCT01437995)
Timeframe: Baseline and 48 weeks

,,
InterventionLiters (Median)
Pre-bronchodilator FEV1Pre-bronchodilator FVC
LABA Step Off-0.13-0.09
Reduced ICS/LABA-0.07-0.04
Stable ICS-LABA-0.02-0.01

[back to top]

Treatment Failure

Rate of treatment failures assessed by decline in peak flow or FEV1, increased need for beta agonists, requirement for non-scheduled medical care for asthma symptoms, or prednisone taper. (NCT01437995)
Timeframe: 48 weeks

Interventionparticipants (Number)
Stable ICS-LABA38
Reduced ICS/LABA39
LABA Step Off45

[back to top]

Rate of Episodes of Poor Asthma Control

Rate of episodes of poor asthma control (EPAC) defined by unscheduled medical care, hospitalization, use of oral corticosteroids and/or increased use of rescue medications and/or decrease of 30% or more in morning peak expiratory flow rate (NCT01437995)
Timeframe: 48 weeks

InterventionEpisodes of poor asthma control (Number)
Stable ICS-LABA183
Reduced ICS/LABA164
LABA Step Off219

[back to top]

Change From Baseline in MSNA (Evaluated by Microneurography as Bursts/Minute) at Week 4

Human MSNA is composed of vasoconstrictor impulses grouped in pulse synchronous bursts that usually occur in sequences, preferentially during transient reductions of blood pressure. Sympathetic activity was measured using microneurographic recordings of efferent in the peroneal nerve. MSNA reflects sympathetic discharge to the vascular bed of the skeletal muscle. Change in MSNA is expressed in terms of bursts per minute (bursts/minute). Change from Baseline was calculated as the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline and Week 4

InterventionBursts/minute (Mean)
Salmeterol 50 µg BID0.5

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Normalized Low Frequency (LF) Power at 2 Hours (Week 0) and at Week 4 (ITT Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. HRV frequencies can be analyzed with frequency domain methods: the LF component of the HRV spectrum reflects sympathetic activity. Change in HRV (normalized LF) after salmeterol inhalation is expressed in terms of normalized units that represent the relative value of LF power component in proportion to the total power minus the very LF (VLF) component (LF/(Total Power-VLF)*100). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionpercent change (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID8.42.5

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Absolute Low Frequency (LF) Power at 2 Hours (Week 0) and at Week 4 (ITT Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. HRV frequencies can be analyzed with frequency domain methods: the LF component of the HRV spectrum reflects sympathetic activity. Change in HRV (absolute LF) after salmeterol inhalation is expressed in terms of milliseconds squared (ms^2). Change from Baseline were calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms^2 (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-123.8-390.1

[back to top]

Arterial Stiffness at Baseline (Week 0) and at Week 4

Arterial stiffness occurs as a consequence of age and arteriosclerosis. Carotid-femoral pulse wave velocity (PWV), a measure of arterial stiffness, is determined from the time taken for the arterial pulse to propagate from the carotid to the femoral artery. PWV was evaluated in terms of meters per second (m/s). PWV after salmeterol inhalation at Baseline (Week 0, [Visit 1, before any inhalation]) and at Week 4 (Visit 2, after inhalation of salmeterol) was assessed. (NCT01536587)
Timeframe: Baseline and Week 4

Interventionm/s (Mean)
PWV at Baseline, Week 0, n=30PWV at Week 4, n=29
Salmeterol 50 µg BID9.28.8

[back to top]

Change From Baseline in MSNA (Evaluated by Microneurography as Bursts/100 Heart Beats) at Week 4

Human MSNA is composed of vasoconstrictor impulses grouped in pulse synchronous bursts that usually occur in sequences, preferentially during transient reductions of blood pressure. Sympathetic activity was measured using microneurographic recordings of efferent in the peroneal nerve. MSNA reflects sympathetic discharge to the vascular bed of the skeletal muscle. Change in MSNA is expressed in terms of bursts per 100 heart beats (bursts/100 heart beats). Change from Baseline was calculated as the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline and Week 4

InterventionBursts/100 heart beats (Mean)
Salmeterol 50 µg BID-3.1

[back to top]

Change From Baseline in Tidal Volume at 2 Hours (Week 0) and at Week 4

Tidal volume is defined as the lung volume representing the normal volume of air displaced between normal inspiration and expiration when extra effort is not applied (normal value is approximately 500 milliliters or 7 milliliters per kilogram of body weight). Change in tidal volume after salmeterol inhalation is expressed in terms of milliliters (mL). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

InterventionmL (Mean)
Change from Baseline to 2 hours, Week 0, n=30Change from Baseline to Week 4, n=24
Salmeterol 50 µg BID60.455.6

[back to top]

Change From Baseline in Systolic and Diastolic Blood Pressure (BP) at 2 Hours (Week 0) and at Week 4

Systolic and diastolic BP was manually measured. Change in BP after salmeterol inhalation is expressed in terms of millimeters of mercury (mmHg). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

InterventionmmHg (Mean)
Systolic: Change from Baseline to 2 hours, Week 0Systolic: Change from Baseline to Week 4Diastolic: Change from Baseline to 2 hours, Week 0Diastolic: Change from Baseline to Week 4
Salmeterol 50 µg BID3.63.71.90.7

[back to top]

Change From Baseline in Oxygen Saturation Measured Via Pulse Oxymetry (SpO2) at 2 Hours (Week 0) and at Week 4

Oxygen saturation measures the capacity of blood to transport oxygen to other parts of the body. Oxygen binds to hemoglobin in red blood cells when moving through the lungs. A pulse oximeter uses two frequencies of light (red and infrared) to determine the percentage of hemoglobin in the blood that is saturated with oxygen. The percentage is called blood oxygen saturation, or SpO2. Change in SpO2 after salmeterol inhalation is expressed in terms of percent. Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionpercent (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-0.2-0.5

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Absolute Low Frequency (LF) Power at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

HRV refers to the complex beat-to-beat (N-N) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. HRV frequencies can be analyzed with frequency domain methods: The LF component of the HRV spectrum reflects sympathetic activity. Change in HRV (absolute LF) after salmeterol inhalation is expressed in terms of milliseconds squared (ms2). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation), respectively. (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms^2 (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID220.7-248.1

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Standard Deviation of NN Intervals (SDNN) at 2 Hours (Week 0) and at Week 4 (ITT Population)

Heart rate variability (HRV) refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. SDNN reflects all the cyclic components responsible for variability in the period of recording; therefore, it represents total variability. Change in HRV (SDNN) after salmeterol inhalation is expressed in terms of milliseconds (ms). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-1.70.1

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Square Root of the Mean Squared Difference of Successive NNs (RMSSD) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. Compared with SDNN, RMSSD is a short-term variation of heart rate. Change in HRV (RMSSD) after salmeterol inhalation is expressed in terms of milliseconds (ms). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID-10.6-32.5

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Square Root of the Mean Squared Difference of Successive NNs (RMSSD) at 2 Hours (Week 0) and at Week 4 (ITT Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. Compared with SDNN, RMSSD is a short-term variation of heart rate. Change in HRV (RMSSD) after salmeterol inhalation is expressed in terms of milliseconds (ms). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-11.5-5.2

[back to top]

Change From Baseline in Spontaneous Baroreflex Sensitivity (BRS) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

BRS is an important characteristic of baroreflex control and is often noninvasively assessed by relating heart rate (HR) fluctuations to blood pressure (BP) fluctuations. Change in BRS after salmeterol inhalation is expressed in terms of milliseconds per millimeters of mercury (ms/mmHg). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0 before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms/mmHg (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID0.280.44

[back to top]

Change From Baseline in Spontaneous Baroreflex Sensitivity (BRS) at 2 Hours (Week 0) and at Week 4 (ITT Population)

BRS is an important characteristic of baroreflex control and is often noninvasively assessed by relating heart rate (HR) fluctuations to blood pressure (BP) fluctuations. Change in BRS after salmeterol inhalation is expressed in terms of milliseconds per millimeters of mercury (ms/mmHg). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0 before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms/mmHg (Mean)
Change from Baseline to 2 hours, Week 0, n=31Change from Baseline to Week 4, n=29
Salmeterol 50 µg BID0.10.2

[back to top]

Change From Baseline in Respiratory Rate at 2 Hours (Week 0) and at Week 4

Respiratory rate is defined as the number of breaths taken within a set amount of time (typically within 60 seconds). Change in respiratory rate after salmeterol inhalation is expressed in terms of respiratory rate (breaths) per minute (min). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionbreaths per minute (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-0.5-0.1

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Standard Deviation of NN Intervals (SDNN) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. SDNN reflects all the cyclic components responsible for variability in the period of recording; therefore, it represents total variability. Change in HRV (SDNN) after salmeterol inhalation is expressed in terms of milliseconds (ms). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID1.2-12.1

[back to top]

Change From Baseline in Respiratory Minute Volume at 2 Hours (Week 0) and at Week 4

Respiratory minute volume is defined as the volume of gas inhaled (inhaled minute volume) or exhaled (exhaled minute volume) from a person's lungs per minute. Change in respiratory minute volume after salmeterol inhalation is expressed in terms of milliliters per minute (mL/min). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

InterventionmL/min (Mean)
Change from Baseline to 2 hours, Week 0, n=30Change from Baseline to Week 4, n=24
Salmeterol 50 µg BID572.0671.4

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Normalized Low Frequency (LF) Power at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. HRV frequencies can be analyzed with frequency domain methods: The LF component of the HRV spectrum reflects sympathetic activity. Change in HRV (normalized LF) after salmeterol inhalation is expressed in terms of normalized units that represent the relative value of LF power component in proportion to the total power minus the very LF (VLF) component (LF/(Total Power-VLF)*100). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionpercent change (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID10.811.6

[back to top]

Change in Muscle Sympathetic Nerve Activity (MSNA) at 2 Hours (Week 0)

Human MSNA is composed of vasoconstrictor impulses grouped in pulse synchronous bursts that usually occur in sequences, preferentially during transient reductions of blood pressure. Sympathetic activity was measured using microneurographic recordings of efferent in the peroneal nerve. MSNA reflects sympathetic discharge to the vascular bed of the skeletal muscle. The change in MSNA (bursts per 100 heart beats [bursts/100 heart beats]) was calculated as the difference in MSNA change from Baseline to after the inhalation of salmeterol (2 hours, Week 0, Visit 1) minus the MSNA change from Baseline to after the inhalation of placebo (1 hour, Week 0, Visit 1). (NCT01536587)
Timeframe: Baseline and 2 hours (Week 0)

InterventionBursts/100 heart beats (Mean)
Salmeterol 50 µg BID-1.3

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Heart Rate at 2 Hours (Week 0) and at Week 4 (ITT Population)

Heart rate refers to the speed of the heartbeat, specifically the number of heartbeats per unit of time. Change in HRV (heart rate) after salmeterol inhalation is expressed in terms of the heart rate (beats) per minute (heart rate/min). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0 before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionbeats per minute (bpm) (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID3.73.9

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Normalized High Frequency (HF) Power at 2 Hours (Week 0) and at Week 4 (ITT Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. HRV frequencies can be analyzed with frequency domain methods: the HF component of the HRV spectrum reflects parasympathetic activity. Change in HRV (normalized HF) after salmeterol inhalation is expressed in terms of normalized units that represent the relative value of HF power component in proportion to the total power minus the very LF (VLF) component (HF/(Total Power-VLF)*100). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionpercent change (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-8.4-2.5

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Normalized High Frequency Power (HF) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. HRV frequencies can be analyzed with frequency domain methods: the HF component of the HRV spectrum reflects parasympathetic activity. Change in HRV (normalized HF) after salmeterol inhalation is expressed in terms of normalized units that represent the relative value of HF power component in proportion to the total power minus the very LF (VLF) component (HF/(Total Power-VLF)*100). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionpercent change (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID-10.8-11.6

[back to top]

Number of Participants With Diastolic Dysfunction on Echocardiography at Baseline (Week 0) and at Week 4

Diastolic dysfunction refers to the decline in performance of one (usually the left ventricle) or both (left and right) ventricles during diastole. The number of participants with diastolic dysfunction on echocardiography was evaluated at Baseline (Week 0, [Visit 1, before any inhalation]) and at Week 4 (Visit 2, after salmeterol inhalation). (NCT01536587)
Timeframe: Baseline and Week 4

Interventionparticipants (Number)
Baseline: Diastolic dysfunction: Yes, n=32Baseline: Diastolic dysfunction: No, n=32Week 4: Diastolic dysfunction: Yes, n=31Week 4: Diastolic dysfunction: No, n=31
Salmeterol 50 µg BID329526

[back to top]

Lung Function (Forced Vital Capacity [FVC], Functional Residual Capacity [FRC; Body and Helium], Total Lung Capacity [TLC], and Residual Volume [RV]) at Baseline (Week 0) and at Week 4

FVC is defined as the volume of air that can be forcibly blown out from the lungs after a full inspiration. FRC is defined as the volume of air present in the lungs, specifically the parenchyma tissues, at the end of a passive expiration. TLC is defined as the maximum volume to which the lungs can be expanded with the greatest possible inspiratory effort; it is equal to VC plus the RV and is approximately 5800 milliliters. RV is defined as the amount of gas remaining in the lungs at the end of a maximal exhalation. All parameters describing lung function are expressed in terms of liters (L). Lung function (FVC, FRC [body and helium], TLC, and RV) was evaluated at Baseline (Week 0, [Visit 1, before any inhalation]) and at Week 4 (Visit 2, after salmeterol inhalation). (NCT01536587)
Timeframe: Baseline and Week 4

InterventionL (Mean)
FVC at Baseline, Week 0, n=32FVC at Week 4, n=31FRC (body) at Baseline, Week 0, n=32FRC (body) at Week 4, n=27FRC (helium) at Baseline, Week 0, n=24FRC (helium) at Week 4, n=24TLC at Baseline, Week 0, n=32TLC at Week 4, n=27RV at Baseline, Week 0, n=32RV at Week 4, n=27
Salmeterol 50 µg BID2.602.644.653.673.643.386.615.673.902.90

[back to top]

Change From Baseline in Transcutaneous Carbon Dioxide (tCO2) at 2 Hours (Week 0) and at Week 4

Transcutaneous carbon dioxide monitoring is a noninvasive way of continuously measuring the tension of these gases in the skin. This methodology provides a continuous noninvasive estimation of the arterial CO2 value. Change in tCO2 after salmeterol inhalation is expressed in terms of millimeters of mercury (mmHg). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

InterventionmmHg (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-0.94-0.82

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Absolute High Frequency (HF) Power at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. HRV frequencies can be analyzed with frequency domain methods: the HF component of the HRV spectrum reflects parasympathetic activity. Change in HRV (absolute HF) after salmeterol inhalation is expressed in terms of milliseconds squared (ms^2). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms^2 (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID-372.1-840.2

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Absolute High Frequency (HF) Power at 2 Hours (Week 0) and at Week 4 (ITT Population)

HRV refers to the complex beat-to-beat (NN) variation in heart rate produced by the interplay of sympathetic and parasympathetic neural activity at the sinus node of the heart. HRV frequencies can be analyzed with frequency domain methods: the HF component of the HRV spectrum reflects parasympathetic activity. Change in HRV (absolute HF) after salmeterol inhalation is expressed in terms of milliseconds squared (ms^2). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionms^2 (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-457.9817.5

[back to top]

Change From Baseline in Forced Expiratory Volume in One Second (FEV1) at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

Pulmonary function was measured by FEV1, defined as the volume of air that which can be forcibly exhaled from the lungs in the first second of a forced exhalation. Change in FEV1 after salmeterol inhalation is expressed in terms of liters (L). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

InterventionL (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID-0.05-0.08

[back to top]

Change From Baseline in Forced Expiratory Volume in One Second (FEV1) at 2 Hours (Week 0) and at Week 4 (ITT Population)

Pulmonary function was measured by FEV1, defined as the volume of air that which can be forcibly exhaled from the lungs in the first second of a forced exhalation. Change in FEV1 after salmeterol inhalation is expressed in terms of liters (L). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

InterventionL (Mean)
Change from Baseline to 2 hours, Week 0, n=32Change from Baseline to Week 4, n=31
Salmeterol 50 µg BID-0.04-0.04

[back to top]

Change From Baseline in Catecholamines (Plasma Norepinephrine) at 2 Hours (Week 0) and at Week 4

Catecholamines are important neurotransmitters in the central nervous system and play a crucial role in the autonomic regulation of many homeostatic functions. Change in catecholamines (plasma norepinephrine) after salmeterol inhalation is expressed in terms of nanogramms per liter (ng/L). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionng/L (Mean)
Change from Baseline to 2 hours, Week 0, n=26Change from Baseline to Week 4, n=29
Salmeterol 50 µg BID-42.4-5.7

[back to top]

Change From Baseline in Catecholamines (Plasma Epinephrine) at 2 Hours (Week 0) and at Week 4

Catecholamines are important neurotransmitters in the central nervous system and play a crucial role in the autonomic regulation of many homeostatic functions. Change in catecholamines (plasma epinephrine) after salmeterol inhalation is expressed in terms of nanograms per milliliter (ng/mL). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionng/mL (Mean)
Change from Baseline to 2 hours, Week 0, n=26Change from Baseline to Week 4, n=29
Salmeterol 50 µg BID6.7-0.3

[back to top]

Change From Baseline in Catecholamines (Brain Natriuretic Peptide [BNP]) at 2 Hours (Week 0) and at Week 4

Catecholamines are important neurotransmitters in the central nervous system and play a crucial role in the autonomic regulation of many homeostatic functions. Change in catecholamines (BNP) after salmeterol inhalation is expressed in terms of picograms per milliliter (pg/mL). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0, before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionpg/mL (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID2.4-6.1

[back to top]

Change From Baseline in Heart Rate Variability (HRV): Heart Rate at 2 Hours (Week 0) and at Week 4 (ITT-MSNA Population)

Heart rate refers to the speed of the heartbeat, specifically the number of heartbeats per unit of time. Change in HRV (heart rate) after salmeterol inhalation is expressed in terms of the heart rate (beats) per minute (heart rate/min). Change from Baseline was calculated as the value at 2 hours (Week 0 [Visit 1, after salmeterol inhalation]) and the value at Week 4 (Visit 2, after salmeterol inhalation) minus the value at Baseline (Week 0 before any inhalation). (NCT01536587)
Timeframe: Baseline, 2 hours (Week 0), and Week 4

Interventionbeats per minute (bpm) (Mean)
Change from Baseline to 2 hours, Week 0Change from Baseline to Week 4
Salmeterol 50 µg BID4.44.9

[back to top]

Change From Baseline in MSNA (Evaluated by Microneurography as Bursts/Minute) at 2 Hours (Week 0)

Human MSNA is composed of vasoconstrictor impulses grouped in pulse synchronous bursts that usually occur in sequences, preferentially during transient reductions of blood pressure. Sympathetic activity was measured using microneurographic recordings of efferent in the peroneal nerve. MSNA reflects sympathetic discharge to the vascular bed of the skeletal muscle. The change in MSNA (bursts per minute [bursts/minute]) was calculated as the difference in MSNA change from Baseline to after the inhalation of salmeterol (2 hours, Week 0, Visit 1) minus the MSNA change from Baseline to after the inhalation of placebo (1 hour, Week 0, Visit 1). (NCT01536587)
Timeframe: Baseline and 2 hours (Week 0)

InterventionBursts/minute (Mean)
Salmeterol 50 µg BID0.3

[back to top]

TDI Focal Score at Week 12 and Week 26: Treatment Comparisons

The Transition Dyspnea Index (TDI) total score after 12 and 26 weeks of treatment will be analyzed using the same mixed model as specified for the primary analysis with the Baseline Dyspnea Index (BDI) total score as the baseline.Total score ranging - 9 to + 9. The lower the score, the more deterioration in severity of dyspnea. One additional option in each category, which does not contribute to the score, allows for circumstances in which impairment is due to reasons other than dyspnea. (NCT01555138)
Timeframe: 12 and 26 weeks

,
InterventionUnits on a scale (Least Squares Mean)
12 weeks26 weeks
Indacaterol1.892.58
Salmeterol/Fluticasone Propionate1.692.70

[back to top]

St Georges Respiratory Questionnaire for COPD

A Total and three component scores are calculated: Symptoms; Activity; Impacts. Each component of the questionnaire is scored separately:The score for each component is calculated separately by dividing the summed weights by the maximum possible weight for that component and expressing the result as a percentage: Score = 100 x Summed weights from all positive items in that component divided by Sum of weights for all items in that component The Total score is calculated in similar way: Score = 100 x Summed weights from all positive items in the questionnaire divided by Sum of weights for all items in the questionnaire Sum of maximum possible weights for each component and Total: Symptoms 566.2 Activity 982.9 Impacts 1652.8 Total (sum of maximum for all three components) 3201.9 The proportion of patients who achieve a clinically important improvement of at least 4 units in the total SGRQ will be analyzed. The higher the score the more symptoms of disease are present. (NCT01555138)
Timeframe: 12 and 26 weeks

,
Interventionscores on a scale (Least Squares Mean)
Week 12Week 26
Indacaterol32.833.1
Salmeterol/Fluticasone Propionate32.933.5

[back to top]

Number of COPD Exacerbations Per Patient Over 26 Weeks: Treatment Comparisons (Without Imputation; Full Analysis Set)

The number of exacerbations during the 26 week treatment period will be analyzed using a generalized linear model assuming a negative binomial distribution. (NCT01555138)
Timeframe: 26 weeks

,
Interventionparticipants (Number)
noneonetwothreeGreater than or equal to four
Indacaterol233471120
Salmeterol/Fluticasone Propionate215571510

[back to top]

Rescue Medication Use Over 26 Weeks: Percentage of 'Days With no Rescue Use'

A 'day with no rescue use' is defined from diary data as any day where the patient has taken no puffs of rescue medication. The percentage of 'days with no rescue use' will be derived and analyzed as for the percentage of 'nights with no nighttime awakenings'. (NCT01555138)
Timeframe: 26 weeks

Intervention% of Days (Least Squares Mean)
Indacaterol52.8
Salmeterol/Fluticasone Propionate54.6

[back to top]

Trough FEV1 (L) at Week 26 (Imputed With LOCF): Treatment Comparisons

Trough FEV1 is defined as the average of the 23 h 10 min and the 23 h 45 min values taken in the clinic at Visit 11. (NCT01555138)
Timeframe: 26 weeks

InterventionLiters (Least Squares Mean)
Indacaterol1.567
Salmeterol/Fluticasone Propionate1.569

[back to top]

Trough Forced Expiratory Volume in One Second (FEV1) at 12 Weeks (Imputed With LOCF): Treatment Comparisons

Spirometry conducted to internationally accepted standards. Trough FEV1 defined as the mean of the FEV1 measurements at 23 h 10 min and 23 h 45 min post the Day 84 morning dose. The primary variable (imputed with last observation carried forward) will be analysed using a mixed model for the Per Protocol Set (PPS). The model will contain treatment as a fixed effect with the baseline FEV1 measurement, FEV1 prior to inhalation and FEV1 10-15 min post inhalation of salbutamol (components of reversibility at Visit 1) as covariates. (NCT01555138)
Timeframe: 12 weeks

InterventionLiters (Least Squares Mean)
Indacaterol1.591
Salmeterol/Fluticasone Propionate1.604

[back to top]

Analysis of AUC (5 Min - 4 h) for FEV1 (L) at Week 12 and Week 26: Treatment Comparison

The standardized (with respect to the length of time) AUC for FEV1 will be calculated between 5 min and 4 h post morning dose as the sum of trapezoids divided by the length of time at Day 84 (Visit 6) and Day 182 (Visit 10). Scheduled (not actual) time points are to be used. FEV1 measurements taken within 6 h of rescue use will be set to missing before the standardized AUC is calculated. (NCT01555138)
Timeframe: 12 and 26 weeks

,
InterventionLiters (Least Squares Mean)
Week 12Week 26
Indacaterol1.6891.683
Salmeterol/Fluticasone Propionate1.6891.682

[back to top]

FEV1 (L) at Individual Time Points After 12 Weeks Treatment: Treatment Comparisons

FEV1 at each time point, for each visit, will be analyzed using the same mixed model as specified for the primary analysis. Least squares means will be displayed by treatment group. (NCT01555138)
Timeframe: 12 weeks

,
InterventionLiters (Least Squares Mean)
-50 min pre-dose30 min post-dose,1h post-dose,2h post-dose4h post-dose23h 10 min post-dose23h 45 min post-dose-15 min pre-dose5 min post-dose
Indacaterol1.6011.6671.6931.7051.6701.5771.5971.6231.631
Salmeterol/Fluticasone Propionate1.5881.6561.6841.7081.6991.5911.6131.6161.613

[back to top]

FEV1 (L) at Individual Time Points After 26 Weeks Treatment: Treatment Comparisons

FEV1 at each time point, for each visit, will be analyzed using the same mixed model as specified for the primary analysis. Least squares means will be displayed by treatment group . (NCT01555138)
Timeframe: 26 weeks

,
InterventionLiters (Least Squares Mean)
-50 min pre-dose30 min post-dose,1h post-dose,2h post-dose4h post-dose23h 10 min post-dose23h 45 min post-dose-15 min pre-dose5 min post-dose
Indacaterol1.5691.6701.6761.7001.6641.5511.5741.5761.630
Salmeterol/Fluticasone Propionate1.5821.6561.6771.6931.6631.5591.5751.5951.630

[back to top]

FVC Over 26 Weeks of Treatment

FVC at each time point, for each visit, will be analyzed using the same mixed model as specified for the primary analysis. Least squares means will be displayed by treatment group. (NCT01555138)
Timeframe: 12 and 26 weeks

,
InterventionLiters (Least Squares Mean)
12 weeks26 weeks
Indacaterol3.0903.057
Salmeterol/Fluticasone Propionate3.0643.062

[back to top]

Mean Daily Number of Puffs of Rescue Medication Used Over 26 Weeks of Treatment

The mean daily number of puffs of rescue medication taken by the patient will be derived. If the number of puffs is missing for part of the day (either morning or evening) then a half day will be used in the denominator. Rescue medication data recorded during the 14 day run-in period will be used to calculate the baseline. The mean change from baseline in the daily number of puffs of rescue medication will be analyzed using the same mixed model as specified for the primary analysis, with the baseline FEV1 replaced with the baseline daily rescue use. (NCT01555138)
Timeframe: 12 and 26 weeks

,
Interventionnumber of puffs (Mean)
BaselineWeek 12Week 26
Indacaterol1.821.501.37
Salmeterol/Fluticasone Propionate1.831.451.37

[back to top]

FEV1 (L) on Day 1 Between-treatment Comparisons of AUC (5min - 4h)

Spirometry is conducted according to the global standard. FEV1 AUC (5 min-4 h), Scheduled (not actual) time points are to be used. The standardized AUC(5 min - 4 h) for FEV1 will be summarized by treatment. (NCT01636076)
Timeframe: Day 1

,
InterventionLiters * hours (Least Squares Mean)
Day 1 baseline (n=303,311)Day 1 post (n=303,311)
QMF1491.1421.277
Salmeterol Xinafoate/Fluticasone Propionate1.1691.260

[back to top]

FEV1 AUC (5 Min-4 h),

Spirometry is conducted according to the global standard. FEV1 AUC (5 min-4 h), (5 min-24 h) is measured after the first dose on Day 1 and on Day 28 and Day 84 in a subset of approximately 60 patients. Scheduled (not actual) time points are to be used. The interpretation of FEV1 at time 0 is the baseline value at the randomization visit and the latest pre-dose value (-50 min or -15 min) at subsequent visits. The standardized AUC(5 min - 4 h) for FEV1 will be summarized by treatment. The same will be repeated for standardized AUC for FEV1 between 5 min and 24 hours post morning dose. (NCT01636076)
Timeframe: Day 1(Baseline), Day 28, Day 84

,
InterventionLiters*hours (Least Squares Mean)
Day 1 baseline (n=46,47)Day 28 (n=45,46)Day 84 (n=44,46)
QMF1491.3021.4101.387
Salmeterol Xinafoate/Fluticasone Propionate1.3311.3551.372

[back to top]

FEV1/FVC at Each Timepoint

Spirometry is conducted according to the global standard. FEV1/FVC is measured at pre-dose and post dose up to 4 hour on Day 1, Day 28, and Day 84, at post dose 12 hour, 23 hour 10 minute and 23 hour 45 minutes on Day 2 and Day 29, and at pre-dose 50 min and 15 min on Day 2, Day 28, and Day 84. (NCT01636076)
Timeframe: Day 1, Day 2, Day 28, Day , Day 29, Day 84, Day 85

,
InterventionFEV1/ FVC (%) (Mean)
Baseline (n=316, 313)Day 1 / 5 min (n=299, 298) changeDay 1 / 30 min (n=302,306) changeDay 1 / 60 min (n=308,303) changeDay 1 / 4 hr (n=302, 297) changeDay 2 / 23 Hr 10 min (n=297,296) changeDay 2 / 23 Hr 45 min (n=307,306) changeDay 28 / -50 min (n=295,296) changeDay 28 / -15 min (n=300,291) changeDay 28 / 5 min (n=297,290) changeDay 28 / 30 min (n=301,291) changeDay 28 / 60 min (n=299,292) changeDay 28 / 4 hr (n=44,45) changeDay 28 / 11hr 10 min (n=47,44) changeDay 28 / 11hr 45 min (n=43,42) changeDay 28 / 16 hr (n=40,41) changeDay 28 / 20 hr (n=43,44) changeDay 29 / 23 hr 10 min (n=293,293) changeDay 29 / 23 hr 45 min (n=299,296) changeDay 84 / -50 min (n=295,279) changeDay 84 / -15 min (n=291,286) changeDay 84 / 5 min (n=288,280) changeDay 84 / 30 min (n=295,281) changeDay 84 / 60 min (n=296,282) changeDay 84 / 4 hr (n=45,44) changeDay 84 / 11hr 10 min (n=45,43) changeDay 84 / 11 hr 45 min (n=39,39) changeDay 84 / 16 hr (n=41,39) changeDay 84 / 20 hr (n=44,43) changeDay 84 / 23 hr 10 min (n=302,292) changeDay 84 / 23 hr 45 min (n=301,286) change
QMF14946.7860.4880.9551.1121.0450.5030.5831.4631.8371.9512.2962.5254.0342.5532.7912.2502.5351.7712.0001.4492.1552.3322.4202.5712.3891.9442.5381.4152.3641.8562.098
Salmeterol Xinafoate/Fluticasone Propionate46.8590.0470.8791.1821.3971.0421.3191.1401.4951.5811.8732.0602.3221.9092.4762.3052.2501.3191.5661.0681.5841.7962.0622.0672.6822.1052.2951.9621.8371.4141.593

[back to top]

Forced Vital Capacity (FVC) at Each Timepoint

Spirometry is conducted according to the global standard. FVC is measured at pre-dose and post dose up to 4 hour on Day 1, Day 28, and Day 84, at post dose 12 hour, 23 hour 10 minute and 23 hour 45 minutes on Day 2 and Day 29, and at pre-dose 50 min and 15 min on Day 2, Day 28, and Day 84. (NCT01636076)
Timeframe: Day 1, Day 2, Day 28, Day , Day 29, Day 84, Day 85

,
Interventionliters (Mean)
Baseline (n=316,313)Day 1/ 5 min (n=299,298) ChangeDay 1/ 30 min (n=302,306) ChangeDay 1/ 60 min (n=308,303) ChangeDay 1/ 4 hr (n=302,297) ChangeDay 2/ 23hr 10 min (n=297,296) ChangeDay 2/ 23hr 45 min (n=307,306) ChangeDay 28 / -50 min (n=295,296) ChangeDay 28 / -15 min (n=300,291) ChangeDay 28 / 5 min (n=297,290) ChangeDay 28 / 30 min (n=301,291) ChangeDay 28 / 60 min (n=299,292) ChangeDay 29 / 23hr 10 min (n=293,293) ChangeDay 29 /23hr 45 min (n=299,296) ChangeDay 84 / -50min (n=295,279) ChangeDay 84 /-15 min (n=291,286) ChangeDay 84 / 5 min (n=288,290) ChangeDay 84 /30 min (n=295,281) ChangeDay 84 / 60 min (n=296,282) ChangeDay 85 / 23 hr 10 min (n=302,292) ChangeDay 85 / 23 hr 45 min (n=301,286) Change
QMF1492.4600.1790.2070.2220.2170.0890.0830.1320.1610.2380.2630.2790.1210.1330.1250.1440.2290.2550.2720.1130.126
Salmeterol Xinafoate/Fluticasone Propionate2.4810.0600.1290.1520.1830.0920.0920.0680.0720.1220.1680.1890.0840.0970.1440.0490.0760.1200.1590.0220.035

[back to top]

Analysis of the Proportion of Subjects With a Clinically Important Improvement of >=1 Point in the TDI (Transitional Dyspnoea Index)Focal Score by Visit

A TDI focal score of ≥1 is considered to be a clinically important improvement from baseline. Analysis of the proportion of subjects with a clinically important improvement of >=1 point in the TDI focal score, by visit (NCT01636076)
Timeframe: 4 and 12 weeks

,
Intervention(%) showing clinical improvement (Number)
Day 28 Change from baseline (n=291,294)Day 84 Change from baseline (n=287,283)
QMF14943.352.6
Salmeterol Xinafoate/Fluticasone Propionate40.545.9

[back to top]

Mixed Model for Repeated Measures (MMRM): Between-treatment Comparisons for FEV1 (L), by Visit and Timepoint

(NCT01636076)
Timeframe: Day 1 through day 85

,
Interventionliter (Least Squares Mean)
Absolute Value Day 1/5min (n=290,298)Absolute Value Day 1/30 min (n=294,306)Absolute Value Day 1/60min (n=300,303)Absolute Value Day 2/ 23 hr 10 min (n=288,295)Absolute Value Day 2/ 23 hr 45 min (n=297,305)Absolute Value Day 28/ -50min (n=288,295)Absolute Value Day 28/ -15min (n=292,290)Absolute Value Day 28/ 5min (n=290,289)Absolute Value Day 28/ 30min (n=293,290)Absolute Value Day 28/ 60min (n=292,290)Absolute Value Day 29/ 23 hr 10 min (n=285,292)Absolute Value Day 29/ 23 hr 45 min (n=290,295)Absolute Value Day 84/ -50 min (n=286,278)Absolute Value Day 84/ -15 min (n=282,285)Absolute Value Day 84/ 5 min (n=280,279)Absolute Value Day 84/ 30 min (n=286,280)Absolute Value Day 84/ 60 min (n=287,281)Absolute Value Day 84/ 23 hr 10 min (n=292,291)Absolute Value Day 84/ 23 hr 45 min (n=291,285)
QMF1491.2541.2811.2811.2131.2151.2651.2871.3291.3521.3531.2691.2811.2591.2821.3361.3521.3511.2641.273
Salmeterol Xinafoate/Fluticasone Propionate1.1981.2501.2561.2391.2441.2871.2351.2681.2981.2981.2421.2541.1951.2221.2431.2771.2831.2121.221

[back to top]

Mixed Model for Repeated Measures (MMRM): Between-treatment Comparisons for Trough FEV1 (L) on Day 85

Spirometry is conducted according to the global standard. Trough FEV1 is defined as the average of the 23 hour 10 minute and 23 hour 45 minute post dose FEV1 readings. (NCT01636076)
Timeframe: 12 weeks

,
InterventionLiters (Least Squares Mean)
Full analysis set (n=291,282)Per protocol set (n=259,251)
QMF1491.2701.277
Salmeterol Xinafoate/Fluticasone Propionate1.2151.228

[back to top]

Patient Reported Outcome Measures: COPD Assessment Test

It consists of eight items, each presented as a semantic 6-point differential scale, providing a total score out of 40. A higher score indicates a worse health status. Scores of 0 - 10, 11 - 20, 21 - 30 and 31 - 40 represent a mild, moderate, severe or very severe clinical impact of COPD upon the patient. (NCT01636076)
Timeframe: Baseline, 4 and 12 weeks

,
InterventionUnits on a scale (Mean)
Baseline (n= 311,308)Day 28 baseline (n=303,298)Day 28 Post (n=303,298)Day 28 Change (n=303,298)Day 84 Baseline (n=295,285)Day 84 Post (n=295,285)Day 84 change (n=295,285)
QMF14916.316.215.8-0.415.915.5-0.4
Salmeterol Xinafoate/Fluticasone Propionate16.216.216.80.616.116.30.2

[back to top]

Patient Reported Outcome Measures: Medical Outcome Study (MOS) Sleep Scale: Sleep Quantity Subscale

The sleep quantity subscale,which refers to question 2 of the PRO: On average, how many hours did you sleep each night during the past 4 weeks. More hours of sleep indicate better outcome. (NCT01636076)
Timeframe: Baseline, 4 and 12 weeks

,
Interventionhours of sleep (Mean)
Sleep quantity Baseline (n=301,295)Sleep quantity Baseline D28(n=292,285)Sleep quantity Post D28(n=292,285)Sleep quantity Change D28(n=292,285)Sleep quantity Baseline D84(n=285,274)Sleep quantity Post D84(n=285,274)Sleep quantity Change D84(n=285,274)
QMF1496.55656.57026.57170.00156.54566.55610.0105
Salmeterol Xinafoate/Fluticasone Propionate6.62036.63516.6246-0.01056.64966.65690.0073

[back to top]

Patient Reported Outcome Measures: SGRQ (St. George's Respiratory Questionnaire)

A Total and three component scores are calculated: Symptoms; Activity; Impacts. Each component of the questionnaire is scored separately:The score for each component is calculated separately by dividing the summed weights by the maximum possible weight for that component and expressing the result as a percentage: Score = 100 x Summed weights from all positive items in that component divided by Sum of weights for all items in that component The Total score is calculated in similar way: Score = 100 x Summed weights from all positive items in the questionnaire divided by Sum of weights for all items in the questionnaire Sum of maximum possible weights for each component and Total: Symptoms 566.2 Activity 982.9 Impacts 1652.8 Total (sum of maximum for all three components) 3201.9 The proportion of patients who achieve a clinically important improvement of at least 4 units in the total SGRQ will be analyzed. The higher the score the more symptoms of disease are present. (NCT01636076)
Timeframe: 4 and 12 weeks

,
InterventionTotal Score (Mean)
Baseline (n=314, 308)Day 28 Baseline (n=304,295)Day 28 Post (n=304,295)Day 28 Change (n=304,295)Day 84 Baseline (n=297,284)Day 84 Post (n=297,284)Day 84 Change (n=297,284)
QMF14943.0542.8740.95-1.9242.5739.81-2.76
Salmeterol Xinafoate/Fluticasone Propionate42.2842.4742.18-0.2942.0341.01-1.02

[back to top]

Pharmacokinetic Parameter--AUC0-t

"Area under the plasma concentration time curve from time zero to time t post-dose is to be measured in a subset of approximately 60 patients via central laboratory, and will be determined for indacaterol and MF following morning dosing on Days 28 and 84." (NCT01636076)
Timeframe: Day 28, 84

,
Interventionhr*pg/mL (Mean)
28 Days (n=35,36)84 Days (n=31,33)
QMF149 Analyte Mometasone Furoate653693
QMF149 Analyte QAB14924002760

[back to top]

Pharmacokinetic Parameter--Tmax

Time to reach the maximum plasma concentration after drug administration is to be measured in a subset of approximately 60 patients via central laboratory, and will be determined for indacaterol and MF following morning dosing on Days 28 and 84. (NCT01636076)
Timeframe: Day 28, 84

,
InterventionHr (Median)
Day 28 (n= 36 ,35)Day 84 (n= 32 ,35)
QMF 149 Anaylyte: Mometasone Furorate0.2500.250
QMF149 Analyte: Indacaterol Acetate0.9701.00

[back to top]

The Percentage of Patients Who Permanently Discontinued Due to COPD Exacerbation

Time-to-event variables will be analyzed by the Kaplan-Meier estimates and the stratified Cox proportional hazard model by smoking status and COPD severity. The model will include treatment and country as factors, and FEV1 prior to inhalation and FEV1 15 min post inhalation of salbutamol/albuterol as covariates. (NCT01636076)
Timeframe: 12 weeks

InterventionPercentage participants (Number)
QMF1490.6
Salmeterol Xinafoate/Fluticasone Propionate1.6

[back to top]

Plasma Cortisol Concentrations at Each Timepoint

Plasma cortisol to be measured in a subset of approximately 60 patients via central laboratory. Blood sample for Plasma cortisol is collected at pre-dose and post dose up to 4 hour on Day 1, up to 12 hours post-dose on Day 28 and Day 84, and 23 hour 35 minute on Day 2, Day 29, and Day 85, and at pre-dose 25 minute on Day 28, and Day 84. (NCT01636076)
Timeframe: Day 1, Day 28, Day 84

,
Interventionnmol/mL (Mean)
Baseline (n=45,41)Day 1 / 15 min (n=44,41)Day 1 / 1 hr (n=44,41)Day 1/ 4 hr (n=44,38)Day 1 /23 hr 35 min (n=38,37)Day 28/-25min (n=40,39)Day 28 / 15 min (n=40,39)Day 28 / 1 hr (n=40,39)Day 28 / 4hr (n=40,38)Day 28 / 11hr 35 min (n=40,37)Day 28/ 23 hr 35 min (n=33,32)Day 84 /-25 min (n=41,37)Day 84/ 15 min (n=40,36)Day 84/ 60 min (n=41,38)Day 84/ 4 hr (n=41,38)Day 84/ 11 hr 35 min (n=41,35)Day 84 / 23 hr 35 min (n=37,36)
QMF149328.5284.0249.1247.6295.9342.1275.0255.9241.9124.8310.6337.4291.1271.3268.4152.0339.9
Salmeterol Xinafoate/Fluticasone Propionate300.2247.1223.0205.7274.2295.6239.8211.9203.6124.1306.5324.1265.5236.3224.2147.5315.9

[back to top]

Plasma Drug Concentrations (Pharmacokinetics) at Each Timepoint

Plasma indacaterol and mometasone furoate is to be measured in a subset of approximately 60 patients via central laboratory. Blood samples are collected at pre-dose on Day 1, 29, and 84; and post dose up to 4 hour on Day 1, up to 12 hours on Day 28 and 84. For sparse pharmacokinetic testing, blood samples will be collected at 23h 35 min post-dose following morning dose administration on Day 28 and 84, in all patients participating in this study. (NCT01636076)
Timeframe: Day 1, 29, 84

,
Interventionpg/mL (Mean)
Day 1 time 0 (n=34,44)Day 1 / 15 min (n=44,45)Day 1 / 1 hr (n=43,45)Day 1/ 4 hr (n=43,45)Day 1 /23 hr 35 min (n=37, 38)Day 28 0 time (n=41,42)Day 28 / 15 min (n= 42,43)Day 28 / 1 hr (n=41,42)Day 28 / 4hr (n=42,42)Day 28 / 11hr 35 min (n=41,42)Day 28/ 23 hr 35 min (n=45,46)Day 84 0 time (n=39,40)Day 84/ 15 min (n=38,40)Day 84/ 60 min (n=38,40)Day 84/ 4 hr (n=40,40)Day 84/ 11 hr 35 min (n=39,41)Day 84 / 23 hr 35 min (n=44,45)
QMF149 (Analyte Indacaterol Acetate)4.3211189.751.444.882.021319413286.676.510125524116111598.7
QMF149 (Analyte Mometasone Furoate)4.1731.444.626.813.114.557.568.443.719.210.823.168.184.249.925.914.6

[back to top]

The Usage of Rescue Medication (Short Acting β2-agonist)

Participants record the number of puffs of rescue medication taken in the previous 12 hours each morning and evening throughout the 12 week treatment period. (NCT01636076)
Timeframe: 12 weeks

,
InterventionNumber of puffs (Least Squares Mean)
Daily Change Weeks 1-12 (n-281,274)Daytime Change Weeks 1-12 (n=276-272)Nighttime Change Weeks 1-12 (n=281,271)
QMF149-1.064-0.625-0.452
Salmeterol Xinafoate/Fluticasone Propionate-0.593-0.300-0.308

[back to top]

Time to First COPD Exacerbation

Time-to-event variables will be analyzed by the Kaplan-Meier estimates and the stratified Cox proportional hazard model by smoking status and COPD severity. The model will include treatment and country as factors, and FEV1 prior to inhalation and FEV1 15 min post inhalation of salbutamol/albuterol as covariates. The reported measure will detail the percentage of participants that were event free of a specified event. (NCT01636076)
Timeframe: 12 weeks

,
InterventionPercentage of participants event free (Number)
Mild COPD exacerbationModerate COPD exacerbationSevere COPD exacerbationModerate or Severe COPD exacerbationAny( mild, moderate,severe)
QMF14999.394.598.092.992.2
Salmeterol Xinafoate/Fluticasone Propionate98.788.598.386.885.8

[back to top]

Total Amount (in Doses) of Systemic Corticosteroid Used to Treat COPD Exacerbation During the 12 Week Treatment Period

Total amount (in doses) of systemic corticosteroid used to treat COPD exacerbation will be summarized descriptively by treatment group per each systemic corticosteroid. (NCT01636076)
Timeframe: 12 weeks

,
Intervention(Prednisolone dose equivalents) mg (Mean)
IM Hydrocortisone (mg) (n=1,0)IV dexamethasone (mg) (n=0,1)IV Hydrocortisone (mg) (n=0,1)IV Hydrocortisone sodium succinate (mg) (n=2,0)IV methylprenisolone sodium succinate(mg)(n=1,0)IV methylprenisolone sodium succinate(ug)(n=0,1)IV prednisolone (mg) (n=0,1)Oral Budesonide (mg) (n=0,1)Oral methylprenisolone (mg) (n=7,13)Oral prednisolone (mg) (n=8,28)Oral prednisone (mg) (n=8,16)Oral prednisone (ug) (n=0,1)Inhalation budesonide (mL)(n=0,1)
QMF149100NANA400.00250NANANA16.5724.3831.25NANA
Salmeterol Xinafoate/Fluticasone PropionateNA4.00100NANA802502020.3123.9325.31100.50

[back to top]

Trough FEV1 After First Dose and After 4 Weeks of Treatment

Spirometry is conducted according to the global standard. FEV1 is measured at pre-dose and post dose up to 1 hours on Day 1 and Day 28; 24 hours post-dose on Day 29 and 85. In a subset of approximately 60 patients, FEV1 is measured up to 20 hours postdose on Day 28 and Day 84. (NCT01636076)
Timeframe: Day 1 and Day 85

,
InterventionLiters (Mean)
Baseline Day 2 (n=286, 302)Day 2 (n=286, 302)Baseline Day 29 (n=293, 296)Day 29 (n=293,296)Day 84 baseline (n=289,287)Day 84 (n=289,287)
QMF1491.1471.2161.1481.2771.1441.269
Salmeterol Xinafoate/Fluticasone Propionate1.1671.2431.1781.2471.1871.208

[back to top]

Patient Reported Outcome Measures: Medical Outcome Study (MOS) Sleep Scale: Without Quantity Subscale

"Scoring the MOS Sleep Survey is a two-step process:• All items are scored so that a high score reflects more of the attribute implied by the scale name. Each item is converted to a 0 to 100 possible range so that the lowest and highest possible scores are set at 0 and 100, respectively. In this format, scores represent the achieved percentage of the total possible score. For example, a score of 50 represents 50% of the highest possible score.~• Second, items within each scale are averaged together to create the 7 scale scores. Scales with at least one item answered can be used to generate a scale score. Items that are left blank (missing data) are not taken into account when calculating the scale scores. Scores represent the average for all items in the scale that the respondent answered. An additional measure is based on the average number of hours sleep each night during the past 4 weeks and are described in outcome measure 15." (NCT01636076)
Timeframe: Baseline, 4 and 12 weeks

,
InterventionUnits on a scale (Mean)
Sleep disturbance Day 28 Baseline (n=290,285)Sleep disturbance Baseline (n=299,295)Sleep disturbance Day 28 post (n=290,285)Sleep disturbance Day 28 change (n=290,285)Sleep disturbance Day 84 Baseline (n=283,274)Sleep disturbance Day 84 Post (n=283,274)Sleep disturbance Day 84 Change (n=283,274)Sleep snoring Baseline (n=299,295)Sleep snoring Day 28 Baseline (n=290,285)Sleep snoring Day 28 Post (n=290,285)Sleep snoring Day 28 change(n=290,285)Sleep snoring Day 84 Baseline (n=283,274)Sleep snoring Day 84 post (n=283,274)Sleep snoring Day 84 change (n=283,274)Sleep shortness of breath Baseline (n=302,295)Sleep shortness of breath D 28 Bseline(n=293,285)Sleep shortness of breath D 28 post (n=293,285)Sleep shortness of breath D 28 change (n=293,285)Sleep shortness of breath D 84 Bseline (n=287,274)Sleep shortness of breath D 84 post (n=287,274)Sleep shortness of breath D 84 change (n=287,274)Sleep adequacy baseline (n=300,295)Sleep adequacy baseline D 28 (n=291,285)Sleep adequacy Post D 28 (n=291,285)Sleep adequacy Change D 28 (n=291,285)Sleep adequacy baseline D 84 (n=284,274)Sleep adequacy Post D 84 (n=284,274)Sleep adequacy change D 84 (n=284,274)Sleep somnolence baseline (n=302,296)Sleep somnolence baseline D28 (n=290,285)Sleep somnolence post D28 (n=290,285)Sleep somnolence change D28 (n=290,285)Sleep somnolence baseline D84 (n=284,274)Sleep somnolence post D84 (n=284,274)Sleep somnolence change D84 (n=284,274)Sleep Problems Index 1 Baseline (n=300,295)Sleep Problems Index 1 Baseline D28 (n=290,285)Sleep Problems Index 1 Post D28 (n=290,285)Sleep Problems Index 1 Change D28 (n=290,285)Sleep Problems Index 1 Baseline D84 (n=284,274)Sleep Problems Index 1 Post D84 (n=284,274)Sleep Problems Index 1 Change D84 (n=284,274)Sleep Problems Index 2 baseline (n=299,295)Sleep Problems Index 2 baseline D 28 (n=289,285)Sleep Problems Index 2 Post D 28 (n=289,285)Sleep Problems Index 2 Change D 28 (n=289,285)Sleep Problems Index 2 Baseline D 84 (n=283,274)Sleep Problems Index 2 Post D 84 (n=283,274)Sleep Problems Index 2 Change D 84 (n=283,274)
QMF14949.683349.642350.93231.249049.762250.75080.988748.881548.823449.34760.524148.841449.45910.617744.522144.634845.88141.246644.864545.76760.903154.999955.053155.20320.150155.212555.24670.034247.664647.871148.44290.571847.782148.25680.474750.479550.603451.47990.876450.732751.35900.626350.461050.572051.55780.985850.688051.46150.7735
Salmeterol Xinafoate/Fluticasone Propionate49.761649.929250.08580.324249.663450.23800.574549.889549.773349.5067-0.266749.638549.6108-0.027745.425945.329245.57740.248145.318045.70490.387054.972555.067954.8296-0.238355.108454.5424-0.565949.170949.109248.6761-0.433148.933549.04610.112650.838250.791150.7836-0.007450.695150.98880.293851.070150.992351.01160.019350.884851.15110.2663

[back to top]

Duration (in Days) of COPD Exacerbations

Duration and number of the COPD exacerbation will be analyzed by the negative binomial regression model including treatment, country, smoking status, and COPD severity as factors and FEV1 prior to inhalation and FEV1 15 min post inhalation of salbutamol/albuterol as covariates. (NCT01636076)
Timeframe: 12 weeks

InterventionDays (Mean)
QMF1491.4
Salmeterol Xinafoate/Fluticasone Propionate2.0

[back to top]

Percentage of Patients With at Least One Exacerbation up to Week 12

Time-to-event variables will be analyzed by the Kaplan-Meier estimates and the stratified Cox proportional hazard model by smoking status and COPD severity. The model will include treatment and country as factors, and FEV1 prior to inhalation and FEV1 15 min post inhalation of salbutamol/albuterol as covariates. The reported measure will detail the percentage of participants that had an exacerbation up to week 12. Less exacerbations reflect a better outcome. (NCT01636076)
Timeframe: 12 weeks

InterventionPercentage of participants (Number)
QMF1497.6
Salmeterol Xinafoate/Fluticasone Propionate14.1

[back to top]

Summary Statistics of COPD Exacerbations over12 Weeks as Defined by Chronic Pulmonary Disease Tool (EXACT)

The EXACT is a 14-item electronic questionnaire designed to detect the frequency, severity, and duration of exacerbations in patients with COPD. (NCT01636076)
Timeframe: 12 weeks

InterventionCOPD exacerbation per participant (Mean)
QMF1490.2
Salmeterol Xinafoate/Fluticasone Propionate0.3

[back to top]

The Overall Change in Usage of Rescue Medication (Short Acting β2-agonist) .

This value represents the percent of days in the study where no rescue medication was needed. (NCT01636076)
Timeframe: Baseline to 12 weeks

Intervention% of days (Least Squares Mean)
QMF1498.796
Salmeterol Xinafoate/Fluticasone Propionate2.538

[back to top]

Mixed Model for Repeated Measures (MMRM): Between-treatment Comparisons for AUC (5 Min - 23 h 45 Min) for FEV1 (L) on Day 28 and Day 84 (Full Analysis Set, 24-h Profiling Subgroup)

Spirometry is conducted according to the global standard. FEV1 AUC (5 min-4 h), (5 min-24 h) is measured after the first dose on Day 1 and on Day 28 and Day 84 in a subset of approximately 60 patients. Scheduled (not actual) time points are to be used. The interpretation of FEV1 at time 0 is the baseline value at the randomization visit and the latest pre-dose value (-50 min or -15 min) at subsequent visits. The standardized AUC(5 min - 4 h) for FEV1 will be summarized by treatment. The same will be repeated for standardized AUC for FEV1 between 5 min and 24 hours post morning dose. (NCT01636076)
Timeframe: Day 28, Day 84

,
InterventionLiters*hours (Least Squares Mean)
Day 28 (n=45,46)Day 85 (n=47,47)
QMF1491.3521.317
Salmeterol Xinafoate/Fluticasone Propionate1.2981.303

[back to top]

Time (in Days) to Permanent Study Discontinuation Due to COPD Exacerbation

Time-to-event variables will be analyzed by the Kaplan-Meier estimates and the stratified Cox proportional hazard model by smoking status and COPD severity. The model will include treatment and country as factors, and FEV1 prior to inhalation and FEV1 15 min post inhalation of salbutamol/albuterol as covariates. (NCT01636076)
Timeframe: 12 weeks

InterventionDays (Median)
QMF149NA
Salmeterol Xinafoate/Fluticasone PropionateNA

[back to top]

Annual Rate of COPD Exacerbations

Time-to-event variables will be analyzed by the Kaplan-Meier estimates and the stratified Cox proportional hazard model by smoking status and COPD severity. The model will include treatment and country as factors, and FEV1 prior to inhalation and FEV1 15 min post inhalation of salbutamol/albuterol as covariates. (NCT01636076)
Timeframe: 12 weeks

,
InterventionCOPD Exacerbations per year (Number)
Model based estimatesActual rate exacerbations per year
QMF1490.3540.39
Salmeterol Xinafoate/Fluticasone Propionate0.6590.73

[back to top]

Pharmacokinetic Parameter: Cmax

Maximum observed plasma concentration after drug administration is to be measured in a subset of approximately 60 patients via central laboratory, and will be determined for indacaterol and MF following morning dosing on Days 28 and 84. (NCT01636076)
Timeframe: Day 28, 84

,
Interventionpg/mL (Mean)
Day 28 (n=36,35)Day 84 (n=32,35)
QMF149 Analyte: Indacaterol Acetate215263
QMF149 Analyte: Mometasone Furoate73.380.2

[back to top]

Percent (%) Perdicted FEV1 Changes

Physiologic measures of % predicted FEV1 (NCT01696214)
Timeframe: Outcome measure was assessed at the initial visit, at randomization following a wash-in period of 1 month, monthly for 24 weeks. Median scores over the 24 weeks of treatment were compared

Interventionpercent predicted FEV1 (Median)
Ipratropium-1.62
Theophylline4.73
Montelukast0.87
Fluticasone 250 mg/Salmeterol 50mg-5.71

[back to top]

The Asthma Symptom Utility Index (ASUI)

The Asthma Symptom Utility Index (ASUI), an important secondary outcome in the proposed full-scale TOM Trial, has also been shown to be useful in tracking the frequency and severity of asthma-related symptoms in non-smoking asthmatics. ASUI is a brief, interviewer-administered, patient preference-based scale assessing frequency and severity of selected asthma-related symptoms and treatment side effects. 11 items are reviewed, with 2-week recall to assess four symptoms (cough, wheeze, shortness of breath, and awakening at night) and medication side-effects each on two dimensions (frequency and severity). 4-point Likert scale is used to assess frequency (not at all, 1 to 3 days, 4 to 7 days, and 8 to 14 days) and severity (not applicable, mild, moderate and severe). Scores range from 0 (worst possible symptoms) to 1 (no symptoms). The change between two time points, initial visit and after 24 weeks of treatment, is reported. The median value is reported with the standard deviation. (NCT01696214)
Timeframe: Outcome measure was assessed at the initial visit, at randomization following a wash-in period of 1 month, monthly for 24 weeks and a follow-up visit 1 month off study drug. Median scores, change from initial visit and end of treatment, were compared

Interventionunits on a scale (Median)
Ipratropium0.16
Theophylline0.24
Montelukast0.14
Fluticasone 250 mg/Salmeterol 50mg0.13

[back to top]

Asthma Control Test

The primary symptomatic measure, the Asthma Control Test (ACT), has been shown to be valid for measuring poor asthma control in asthmatic children and non-smoking adults. The ACT is a tool developed by Nathan and collaborators a decade ago for evaluating asthma control. It consists of five questions with five possible answers each. A maximum score of 25 points indicates complete asthma control. A score between 20 and 24 represents partially controlled asthma, while a score 19 or below indicates poorly controlled asthma and a score <16 indicates uncontrolled asthma. The minimally important clinical difference has been determined to be 3. (NCT01696214)
Timeframe: Outcome measure was assessed at the initial visit, at randomization following a wash-in period of 1 month, monthly for 24 weeks and at follow-up visit 1 month off study drug. Median scores over the 24 weeks of treatment were compared.

Interventionunits on a scale (Median)
Ipratropium17.5
Theophylline13
Montelukast12
Fluticasone 250 mg/Salmeterol 50mg10

[back to top]

Change From Baseline in Trough FEV1 on Treatment Day 85

FEV1 is a measure of lung function and is defined as the volume of air that can be forcefully exhaled in one second. Trough FEV1 is defined as the 24-hour FEV1 assessment, which was obtained on Day 85. Baseline trough was calculated as the mean of the two assessments made 30 minutes pre-dose and 5 minutes pre-dose on Treatment Day 1. Change from Baseline was calculated as the average of the Day 85 values minus the Baseline value. The analysis used an analysis of covariance (ANCOVA) model with covariates of Baseline FEV1, reversibility stratum, smoking status (at Screening), country, and treatment. (NCT01706328)
Timeframe: Baseline and Day 85

InterventionLiters (Least Squares Mean)
FF/VI 100/25 µg QD0.151
FP/Salmeterol 250/50 µg BID0.121

[back to top]

Change From Baseline Trough in Weighted-mean 24-hour Serial Forced Expiratory Volume in One Second (FEV1) on Treatment Day 84

FEV1 is a measure of lung function and is defined as the volume of air that can be forcefully exhaled in one second. The weighted mean was calculated from the pre-dose FEV1 and the post-dose FEV1 measurements taken at 5, 15, 30, and 60 minutes and 2, 4, 6, 8, 12, 13, 14, 16, 20, and 24 hours on Treatment Day 84. Baseline trough FEV1 was calculated as the mean of the two assessments made 30 minutes pre-dose and 5 minutes pre-dose on Treatment Day 1. The weighted mean was derived by calculating the area under curve, and then dividing by the relevant time interval. The weighted mean change from Baseline was calculated as the weighted mean of the 24-hour serial FEV1 measurements on Day 84 minus the Baseline trough FEV1 value. The analysis used an analysis of covariance (ANCOVA) model with covariates of Baseline FEV1, reversibility stratum, smoking status (at Screening), country, and treatment. (NCT01706328)
Timeframe: Baseline and Day 84

InterventionLiters (Least Squares Mean)
FF/VI 100/25 µg QD0.168
FP/Salmeterol 250/50 µg BID0.142

[back to top]

Time to Onset on Treatment Day 1

Time to onset on Treatment Day 1 is defined as the time to an increase of 100 milliliters (mL) from Baseline in FEV1 during the 0- to 4-hour serial measurements (5, 15, 30, 60, 120, and 240 minutes post-dose). Participants who never met or exceeded a 100 mL increase over the Baseline value during the 4-hour serial measurements were censored at the actual time of their last FEV1 measurement. (NCT01706328)
Timeframe: Baseline and Day 1

InterventionMinutes (Median)
FF/VI 100/25 µg QD15
FP/Salmeterol 250/50 µg BID15

[back to top]

Rescue Medication Use: Summary of the Mean Daily, Daytime and Nighttime Number of Puffs of Rescue Medication, by 4 Weekly Intervals

"The number of puffs of rescue medication taken in the previous 12 hours will be recorded in the Patient Diary in the morning and evening. Baseline 12 weeks and Baseline 26 weeks, were the baseline scores for available participants analyzed for each time point. Less puffs taken is better." (NCT01709903)
Timeframe: 12 and 26 weeks

,
Intervention# of puffs (Mean)
Baseline Daytime 12-16 weeks (n=329,318)Daytime 12-16 weeks (n=329,318)Baseline Nighttime 12-16 weeks (n=322,307)Nighttime 12-16 weeks (n=322,307)Baseline Daytime 24-26 weeks (n=326,315)Daytime 24-26 weeks (n=326,315)Baseline Night time 24-26 weeks (n=320,304)Night time 24-26 weeks (n=320,304)
Fluticasone/Salmeterol1.690.611.240.491.700.621.210.48
QVA1491.570.661.250.521.540.631.230.52

[back to top] [back to top]

Analysis of Trough FVC (L) Over the Whole Treatment Period

Average of Trough Forced Vital Capacity (FVC) at 23 hours 15 min and the 23 hours 45 min post dose (NCT01709903)
Timeframe: 12 and 26 weeks

,
Interventionliter (Least Squares Mean)
Day 1 (n=350,351)Week 12 (n=342,332)week 26 (n= 333,323)
Fluticasone/Salmeterol2.9572.8352.793
QVA1493.0403.0362.966

[back to top]

Analysis of the TDI Focal Score Over the Whole Treatment Period

"The Transition Dyspnea Index (TDI) total score after 12 and 26 weeks of treatment will be analyzed using the same mixed model as specified for the primary analysis with the Baseline Dyspnea Index (BDI) total score as the baseline.Total score ranging - 9 to + 9. The lower the score, the more deterioration in severity of dyspnea. One additional option in each category, which does not contribute to the score, allows for circumstances in which impairment is due to reasons other than dyspnea. .Baseline 12 weeks and Baseline 26 weeks, were the baseline scores for available participants analyzed for each time point." (NCT01709903)
Timeframe: 12 and 26 weeks

,
InterventionNumbers on a scale (Least Squares Mean)
Baseline 12 weeks (n=348,337)12 weeks (n=348,337)Baseline 26 weeks (n=335,326)26 weeks (n=335,326)
Fluticasone/Salmeterol6.362.406.402.86
QVA1496.362.626.383.02

[back to top]

Analysis of FEV1 (L) Trough Response (Pre-dose) Over the Whole Treatment Period

Average of Trough Forced Expiratory Volume in one second (FEV1) (NCT01709903)
Timeframe: 6,12,18 and 26 weeks

,
Interventionliter (Least Squares Mean)
Week 6 (n=356,341)week 12 (n=346,333)week 18 (n=339,332)week 26 (n=338,324)
Fluticasone/Salmeterol1.1841.1911.1741.142
QVA1491.2561.2651.2521.226

[back to top]

Trough Forced Expiratory Volume in One Second (FEV1) Following 26 Weeks of Treatment to Demonstrate the Superiority of QVA 110/50μg o.d. to Fluticasone/Salmeterol 500/50 μg b.i.d

(NCT01709903)
Timeframe: 26 weeks

Interventionliters (Least Squares Mean)
QVA1491.259
Fluticasone/Salmeterol1.183

[back to top]

Trough Forced Expiratory Volume in One Second (FEV1) Following 26 Weeks of Treatment to Demonstrate the Non-inferiority of QVA149 110/50 μg o.d. to Fluticasone/Salmeterol 500/50 μg b.i.d

Measurement of QVA149 110/50 μg o.d. to fluticasone/salmeterol 500/50 μg b.i.d. in terms of trough FEV1 (mean of 23 h 15 min and 23 h 45 min post QVA149 dose) following 26 weeks of treatment in patients with moderate to severe COPD. (NCT01709903)
Timeframe: 26 weeks

Interventionliters (Least Squares Mean)
QVA1491.248
Fluticasone/Salmeterol1.176

[back to top]

Symptoms Reported Using E-diary Over 12 and 26 Weeks of Treatment

Percentage of nights with 'no nighttime awakenings', percentage of days with 'no daytime symptoms', and percentage of 'days able to perform usual daily activities' over 26 weeks (FAS) (NCT01709903)
Timeframe: 26 weeks

,
Intervention% days in study (Least Squares Mean)
% nights 'no nighttime awakenings' (n=336,322)% days with 'no daytime symptoms' (n=341,334)% days able perform daily activities (n=341,334)
Fluticasone/Salmeterol67.8610.2242.16
QVA14967.577.3144.02

[back to top]

Standardized Forced Expiratory Volume in One Second (FEV1) Area Under the Curve (AUC) 0-4 Hours

Forced Expiratory Volume in 1 Second (FEV1) Area Under the Curve (AUC) 0-4h at Day 1 was measured via spirometry conducted according to internationally accepted standards. Measurements were made at 0, 5, 15, and 30 minutes; and 1, 2, 3 and 4 hours post-dose. The standardized AUC FEV1 was calculated as the sum of trapezoids divided by the length of time. Mixed model used: AUC FEV1 = treatment + baseline FEV1 + FEV1 reversibility components + baseline smoking status + baseline ICS use + country + center (country) + error. Center was included as a random effect nested within country. (NCT01709903)
Timeframe: Day 1, 12 and 26 weeks

,
InterventionLiter (Mean)
Day 1 (n=369,364)12 weeks (n=350,338)26 weeks (n=339,323)
Fluticasone/Salmeterol1.2521.2621.229
QVA1491.3171.3881.351

[back to top]

Post-dose sGaw at 30, 75, 120 and 240 Minutes Post Dose at Day 28 of Each Treatment Period

sGaw is a measure of airways conductance and is intimately related to the diameter of the airways and consequently the level of bronchodilation. Plethysmography was performed to assess sGaws. A natural logarithmic transformation was applied and the data was analyzed by a mixed model including treatment, time, period, a treatment by time interaction and Baseline sGaw fitted as fixed effects and participant fitted as a random effect. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

,,
Intervention1/kPa*s (Geometric Mean)
30 min75 min120 min240 min
Ado 50/250 µg BID0.6390.6520.6800.690
Ado 50/250 µg BID+Tio 18 µg QD0.8330.8730.8850.855
Tio 18 µg QD0.7050.7430.7690.750

[back to top]

Post-dose sRaw at 30, 75, 120 and 240 Minutes Post Dose at Day 28 of Each Treatment Period

sRaw is a measure of airways resistance and is intimately related to the diameter of the airways and consequently the level of bronchodilation. Plethysmography was performed to assess sRaw. A natural logarithmic transformation was applied and the data was analysed by a mixed model including treatment, time, period, a treatment by time interaction and Baseline sRaw fitted as fixed effects and participant fitted as a random effect. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

,,
InterventionkPa*s (Geometric Mean)
30 min75 min120 min240 min
Ado 50/250 µg BID1.5671.5351.4681.446
Ado 50/250 µg BID+Tio 18 µg QD1.2011.1461.1291.170
Tio 18 µg QD1.4191.3481.3001.334

[back to top]

Trough Forced Expiratory Volume in One Second (FEV1), Forced Vital Capacity (FVC), Inspiratory Capacity (IC), RV, TLC, and TGV at Each Clinic Visit Prior to the Morning Dose and Before the Use of Rescue Medication at Day 28 of Each Treatment Period

FEV1 is a measure of lung function and the maximal amount of air that can be forcefully exhaled in one second. FVC is defined as the amount of air that can forcibly be blown out after a full inspiration. FEV1 and FVC data was obtained by spirometry measurements. IC is defined as the maximum amount of air that can be inhaled into the lungs from the normal resting position after breathing out normally. Total lung capacity (TLC) is the maximum volume to which the lungs can be expanded with the greatest possible inspiratory effort; it is equal to the vital capacity (VC) plus the residual volume (RV). RV is defined as the volume of air remaining in the lungs. after a maximal exhalation. Thoracic gas volume at functional residual capacity (TGV) is defined as the volume of intrathoracic gas at the time the airway is occluded for the plethysmographic measurement at the end of a normal expiration. Trough values were the values taken pre-dose. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

,,
InterventionLiters (L) (Least Squares Mean)
FEV1FVCICRVTLCTGV
Ado 50/250 µg BID1.7063.4392.3953.1236.5254.129
Ado 50/250 µg BID+Tio 18 µg QD1.8233.5752.4603.0216.5114.053
Tio 18 µg QD1.6663.4932.4063.1296.5244.118

[back to top]

Post-dose FEV1/FVC Ratio (Measured at Trough) at Day 28 of Each Treatment Period

FEV1 is a measure of lung function and the maximal amount of air that can be forcefully exhaled in one second. FVC is defined as the amount of air that can forcibly be blown out after a full inspiration. FEV1 and FVC data was obtained by spirometry measurements. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

InterventionRatio of FEV1/FVC (Least Squares Mean)
Ado 50/250 µg BID+Tio 18 µg QD0.500
Tio 18 µg BID0.472
Ado 50/250 µg BID0.492

[back to top]

AUC (0-4hr) Specific Airway Resistance (sRaw) After the Morning Dose of Each Study Medication at Day 28 of Each Treatment Period

sRaw is a measure of airways resistance and is intimately related to the diameter of the airways and consequently the level of bronchodilation. Plethysmography was performed to assess sRaw. The AUC was determined by using the trapezoidal rule and then dividing by the relevant time interval. A natural logarithmic transformation was applied and the data was analyzed by a mixed model including treatment, period and Baseline sRaw fitted as fixed effects and participants fitted as a random effect. Treatment ratios of all statistical comparisons were calculated by taking the anti-log of the difference between the LS means. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

InterventionkPa*s (Geometric Mean)
Ado 50/250 µg BID+Tio 18 µg QD1.181
Tio 18 µg QD1.380
Ado 50/250 µg BID1.525

[back to top]

Area Under the Curve Calculated From 0 to 4 Hours (AUC[0-4hr]) Specific Conductance (sGaw) After the Morning Dose of Study Medication at Day 28 of Each Treatment Period

sGaw is a measure of airways conductance and is intimately related to the diameter of the airways and consequently the level of bronchodilation. Plethysmography was performed to assess sGaw. The AUC was determined by using the trapezoidal rule and then dividing by the relevant time interval. A natural logarithmic transformation was applied and the data was analyzed by a mixed model including treatment, period and Baseline sGaw fitted as fixed effects and participants fitted as a random effect. Treatment ratios of all statistical comparisons were calculated by taking the anti-log of the difference between the Least Square (LS) means. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

Intervention1/kilopascal*second (1/kPa*s) (Geometric Mean)
Ado 50/250 µg BID+Tio 18 µg QD0.854
Tio 18 µg QD0.737
Ado 50/250 µg BID0.663

[back to top]

Use of Rescue Medication (Number of Occasions Per 24-hour Period) as Recorded in the Daily Record Card at Day 28 of Each Treatment Period

Participants were given daily record cards for daily completion during the run-in, washout and treatment periods. Each morning, participants recorded the number of occasions in the last 24 hours when they had used their rescue medication (salbutamol) for symptomatic relief of COPD symptoms. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

,,
InterventionNumber of occasions (Mean)
Treatment, n=20, 18, 17Washout, n=15, 15, 11
Ado 50/250 µg BID0.20.4
Ado 50/250 µg BID+Tio 18 µg QD0.20.4
Tio 18 µg QD0.30.5

[back to top]

Trough FEV1/FVC Ratio, at Each Clinic Visit Prior to the Morning Dose and Before the Use of Rescue Medication at Day 28 of Each Treatment Period

FEV1 is a measure of lung function and the maximal amount of air that can be forcefully exhaled in one second. FVC is defined as the amount of air that can forcibly be blown out after a full inspiration. FEV1 and FVC data was obtained by spirometry measurements. Trough values were the values taken pre-dose. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

InterventionRatio of FEV1/FVC (Least Squares Mean)
Ado 50/250 µg BID+Tio 18 µg QD0.513
Tio 18 µg QD0.481
Ado 50/250 µg BID0.496

[back to top]

Trough sGaw Measured at Each Clinic Visit Prior to the Morning Dose and Before the Use of Rescue Medication at Day 28 of Each Treatment Period

sGaw is a measure of airways conductance and is intimately related to the diameter of the airways and consequently the level of bronchodilation. Trough values were the values taken pre-dose. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

Intervention1/kPa*s (Geometric Mean)
Ado 50/250 µg BID+Tio 18 µg QD0.720
Tio 18 µg QD0.600
Ado 50/250 µg BID0.577

[back to top]

Trough sRaw Measured at Each Clinic Visit Prior to the Morning Dose and Before the Use of Rescue Medication at Day 28 of Each Treatment Period

sRaw is a measure of airways resistance and is intimately related to the diameter of the airways and consequently the level of bronchodilation. Trough values were the values taken pre-dose. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

InterventionkPa*s (Geometric Mean)
Ado 50/250 µg BID+Tio 18 µg QD1.391
Tio 18 µg QD1.666
Ado 50/250 µg BID1.732

[back to top]

Post-dose FEV1, FVC, IC, RV, TLC and TGV (Measured at Trough) at Day 28 of Each Treatment Period

FEV1 is a measure of lung function and the maximal amount of air that can be forcefully exhaled in one second. FVC is defined as the amount of air that can forcibly be blown out after a full inspiration. FEV1 and FVC data was obtained by spirometry measurements. IC is defined as the maximum amount of air that can be inhaled into the lungs from the normal resting position after breathing out normally. Total lung capacity (TLC) is the maximum volume to which the lungs can be expanded with the greatest possible inspiratory effort; it is equal to the vital capacity (VC) plus the RV. RV is defined as the volume of air remaining in the lungs after a maximal exhalation. Thoracic gas volume at functional residual capacity (TGV) is defined as the volume of intrathoracic gas at the time the airway is occluded for the plethysmographic measurement at the end of a normal expiration. (NCT01751113)
Timeframe: Day 28 of each treatment period (up to 35 days)

,,
InterventionLiters (L) (Least Squares Mean)
FEV1FVCICRVTLCTGV
Ado 50/250 µg BID1.6643.3872.3513.2346.5924.238
Ado 50/250 µg BID+Tio 18 µg QD1.7663.5352.3443.0456.4874.147
Tio 18 µg QD1.6053.4302.3513.2756.5884.239

[back to top]

Number of Participants in Each Treatment Efficacy Grade Evaluated by Physician

Physician evaluated treatment efficacy by using the following grades: significantly improved (SII), moderately improved (MOI), mildly improved (MII), no change (NC), mildly worse (MIW), moderately worse (MOW), and significantly worse (SIW). Treatment efficacy was assessed at Visit 3 (Week 4), Visit 4 (Week 8), Visit 5 (Week 8), Visit 6 (Week 12), Visit 7 (Week 16), and Visit 8 (Week 24). (NCT01762800)
Timeframe: 24 weeks

,,,
InterventionParticipants (Number)
Visit 3; SIIVisit 3; MOIVisit 3; MIIVisit 3; NCVisit 3; MIWVisit 3; MOWVisit 3; SIWVisit 4; SIIVisit 4; MOIVisit 4; MIIVisit 4; NCVisit 4; MIWVisit 4; MOWVisit 4; SIWVisit 5; SIIVisit 5; MOIVisit 5; MIIVisit 5; NCVisit 5; MIWVisit 5; MOWVisit 5; SIWVisit 6; SIIVisit 6; MOIVisit 6; MIIVisit 6; NCVisit 6; MIWVisit 6; MOWVisit 6; SIWVisit 7; SIIVisit 7; MOIVisit 7; MIIVisit 7; NCVisit 7; MIWVisit 7; MOWVisit 8; SIIVisit 8; MOIVisit 8; MIIVisit 8; NCVisit 8; MIWVisit 8; MOW
SAL/FLU 50/250 µg BID-Single611406770131428746111122973701210317430001325793027367011
SAL/FLU 50/250 µg BID-TRIPLE01123116801313331260261435101011183311111218385214193921
TIO 18 µg QD-Single15218373128237940024228350023287210002523775137277141
TIO 18 µg QD-TRIPLE143322312009182712804819291030211173293031212358139134050

[back to top]

Number of Participants in Each Treatment Efficacy Grade Evaluated by Participants

Participants evaluated treatment efficacy by using the following grades: significantly improved (SII), moderately improved (MOI), mildly improved (MII), no change (NC), mildly worse (MIW), moderately worse (MOW), and significantly worse (SIW). Treatment efficacy was assessed at Visit 3 (Week 4), Visit 4 (Week 8), Visit 5 (Week 8), Visit 6 (Week 12), Visit 7 (Week 16), and Visit 8 (Week 24). (NCT01762800)
Timeframe: Up to 24 weeks

,,,
InterventionParticipants (Number)
Visit 3; SIIVisit 3; MOIVisit 3; MIIVisit 3; NCVisit 3; MIWVisit 3; MOWVisit 3; SIWVisit 4; SIIVisit 4; MOIVisit 4; MIIVisit 4; NCVisit 4; MIWVisit 4; MOWVisit 5; SIIVisit 5; MOIVisit 5; MIIVisit 5; NCVisit 5; MIWVisit 5; MOWVisit 5; SIWVisit 6; SIIVisit 6; MOIVisit 6; MIIVisit 6; NCVisit 6; MIWVisit 6; MOWVisit 6; SIWVisit 7; SIIVisit 7; MOIVisit 7; MIIVisit 7; NCVisit 7; MIWVisit 7; MOWVisit 8; SIIVisit 8; MOIVisit 8; MIIVisit 8; NCVisit 8; MIWVisit 8; MOW
SAL/FLU 50/250 µg BID-Single593574711315316710121331661001213356640011327754059395851
SAL/FLU 50/250 µg BID-TRIPLE02103219501612398217173472014163311012417375114193750
TIO 18 µg QD-Single132085930252579502331782002430727002528717028306931
TIO 18 µg QD-TRIPLE137322291162128135462031930413143472041120269149193440

[back to top]

Forced Expiratory Volume in One Second (FEV1)

FEV1 is defined as the volume of air forcefully expelled from the lungs in one second. At Screening (Visit 1) spirometric assessments were conducted before (Visit 1A) and 30 to 60 minutes after a bronchodilator challenge (400 µg of salbutamol) (Visit 1B). FEV1 during each visit are presented. FEV1 was assessed at Visit 1A (Screening), Visit 1B (Screening), Visit 2 (Baseline), Visit 3 (Week 4), Visit 4 (Week 8), Visit 5 (Week 8), Visit 6 (Week 12), Visit 7 (Week 16), and Visit 8 (Week 24). (NCT01762800)
Timeframe: Up to 24 weeks

,,,
InterventionLiters (Mean)
Visit 1A; n=136, 68, 126, 75Visit 1B; n=136, 68, 126, 75Visit 2; n=136, 68, 126, 75Visit 3; n=131, 68, 119, 75Visit 4; n=127, 68, 116, 74Visit 5; n=122, 68, 116, 72Visit 6; n=120, 66, 114, 74Visit 7; n=119, 66, 113, 71Visit 8; n=117, 66, 113, 70
SAL/FLU 50/250 µg BID-Single1.6871.7641.6951.7311.7131.7181.7161.7101.694
SAL/FLU 50/250 µg BID-TRIPLE1.4011.4711.3851.3421.3551.3841.4131.4041.435
TIO 18 µg QD-Single1.6751.7541.6811.7101.7031.7081.7121.6941.688
TIO 18 µg QD-TRIPLE1.3491.4291.3621.2851.3361.3761.4051.4231.390

[back to top]

Change From Baseline in FEV1

FEV1 is defined as the volume of air forcefully expelled from the lungs in one second. Baseline was a value at Visit 2 (randomization). Change from Baseline was calculated as specific timepoint value minus Visit 2 value. FEV1 was assessed at Visit 2 (Baseline), Visit 3 (Week 4), Visit 4 (Week 8), Visit 5 (Week 8), Visit 6 (Week 12), Visit 7 (Week 16), and Visit 8 (Week 24). (NCT01762800)
Timeframe: Baseline (Visit 2) and up to 24 weeks

,,,
InterventionLiters (Mean)
Visit 3; n=131, 68, 119, 75Visit 4; n=127, 68, 116, 74Visit 5; n=122, 68, 116, 72Visit 6; n=120, 66, 114, 74Visit 7; n=119, 66, 113, 71Visit 8; n=117, 66, 113, 70
SAL/FLU 50/250 µg BID-Single0.0240.008-0.010-0.007-0.012-0.019
SAL/FLU 50/250 µg BID-TRIPLE-0.043-0.030-0.0010.0270.0180.049
TIO 18 µg QD-Single0.007-0.011-0.0060.002-0.010-0.017
TIO 18 µg QD-TRIPLE-0.077-0.0320.0050.0370.0500.027

[back to top]

Percentage of Participants Who Stepped Down From TRIPLE Therapy to Initial Randomized Treatment

The percentage of participants who stepped down from TRIPLE therapy to initial randomized treatment was calculated as number of participants who step-down from TRIPLE therapy divided by number of participants who switch to TRIPLE therapy and then multiplied by 100. (NCT01762800)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
TIO 18 µg QD1.33
SAL/FLU 50/250 µg BID2.94

[back to top]

Change From Baseline in CAT Total Score

Participants were assessed for COPD symptoms by means of CAT at each Visit. This assessment was performed prior to the spirometry testing. A CAT total score of less than 10 represents best health status and greater than 15 represents worst health status. Baseline was the value at Visit 2 (randomization). Change from Baseline was calculated as specific timepoint value minus Visit 2 value. Scores were assessed at Visit 2 (Baseline), Visit 3 (Week 4), Visit 4 (Week 8), Visit 5 (Week 8), Visit 6 (Week 12), Visit 7 (Week 16), and Visit 8 (Week 24). Scores range from 0 to 40, high value in score indicate worse outcome. (NCT01762800)
Timeframe: Baseline and up to 24 weeks

,,,
InterventionScores on a scale (Mean)
Visit 3, n=132, 68, 121, 75Visit 4, n=127, 68, 116, 74Visit 5, n=123, 68, 116, 73Visit 6, n=120, 66, 115, 74Visit 7, n=120, 66, 113, 71Visit 8, n=117, 66, 113, 70
SAL/FLU 50/250 µg BID-Single-1.6-1.7-1.6-2.3-2.0-2.4
SAL/FLU 50/250 µg BID-TRIPLE0.1-0.2-0.80.0-0.8-1.0
TIO 18 µg QD-Single0.1-0.3-0.7-0.7-0.8-1.4
TIO 18 µg QD-TRIPLE2.11.60.80.0-0.6-0.5

[back to top]

Time to First Switching to TRIPLE Therapy

The day of first switch to TRIPLE therapy (SAL/FLU 50/250 µg BID+TIO 18 µg QD) for the first switching participant in each arm. (NCT01762800)
Timeframe: 24 weeks

InterventionDays (Number)
TIO 18 µg QD5
SAL/FLU 50/250 µg BID5

[back to top]

Time to First Exacerbation by Physician's Diagnosis

The day of detection of first exacerbation in any participant in each arm as diagnosed by physician. Exacerbation is defined primarily by physician's judgment. Date of randomisation will be start point and timing of exacerbation (first exacerbation if there are more than one) will be event. For subjects without exacerbation, last day of study or follow up period is regarded as censor. (NCT01762800)
Timeframe: 24 weeks

InterventionDays (Number)
SAL/FLU 50/250 µg BID-Single3
SAL/FLU 50/250 µg BID-TRIPLE5
TIO 18 µg QD-Single10
TIO 18 µg QD-TRIPLE2

[back to top]

Time to First Exacerbation by EXAcerbations of Chronic Pulmonary Disease Tool (EXACT)

The EXAcerbations of Chronic pulmonary disease Tool (EXACT) is a 14-item patient-reported outcome (PRO) daily diary used to quantify and measure exacerbations of chronic obstructive pulmonary disease (COPD). Reported as units on a 0 [best health status] to 100 [worst possible status] scale). The day of detection of first exacerbation in any participant in each arm by EXACT. (NCT01762800)
Timeframe: 24 weeks

InterventionDays (Number)
SAL/FLU 50/250 µg BID-Single0
SAL/FLU 50/250 µg BID-TRIPLE0
TIO 18 µg QD-Single0
TIO 18 µg QD-TRIPLE1

[back to top]

Percentage of Participants Who Used Relief Medication (Salbutamol)

Each evening participants recorded the number of occasions in the last 24 hours when they used their salbutamol for symptomatic relief of COPD symptoms. The percentage of participants who used relief medication in the study are presented. (NCT01762800)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
SAL/FLU 50/250 µg BID-Single40.4
SAL/FLU 50/250 µg BID-TRIPLE61.8
TIO 18 µg QD-Single43.7
TIO 18 µg QD-TRIPLE70.7

[back to top]

EXACT Total Score.

"EXACT is a 14-item patient questionnaire used as a measure of respiratory symptoms (reported as units on a 0 [best health status] to 100 [worst possible status] scale). Scores were assessed at Baseline, Week 1-4, Week 5-8, Week 9-12, Week 13-16, Week 17-20 and Week 21-24. Daily EXACT total score is obtained as total score of 14 items from diary. Daily E-RS total score as 11 items and Daily E-RS subscale scores are subset of E-RS total score.~Mean EXACT total score is mean value of daily EXACT total score within subject by every 4 weeks(Week1-4, Week5-8, Week9-12, Week13-16, Week17-20, Week21-24). Same calculation of mean values are applied to E-RS total and E-RS subscale scores." (NCT01762800)
Timeframe: Baseline and up to 24 weeks

,,,
InterventionScores on a scale (Mean)
Baseline; n=125, 66, 111, 71Week 1-4; n=120, 67, 109, 73Week 5-8; n=117, 63, 102, 69Week 9-12; n=109, 67, 101, 72Week 13-16; n=105, 65, 100, 71Week 17-20; n=107, 65, 97, 66Week 21-24; n=79, 51, 77, 46
SAL/FLU 50/250 µg BID-Single28.9927.8327.3527.6327.3326.9826.50
SAL/FLU 50/250 µg BID-TRIPLE36.0036.9237.5836.1635.9234.9232.72
TIO 18 µg QD-Single29.7728.8828.8028.4028.9328.6628.80
TIO 18 µg QD-TRIPLE35.7838.2635.8735.5733.7934.0333.67

[back to top]

EXACT Respiratory Symptoms (E-RS) Total Score

"The E-RS total score is an 11-item patient questionnaire, which provides information specific to respiratory symptoms-severity of respiratory symptoms overall and severity of breathlessness, cough and sputum, and chest symptoms. Scores were assessed at Baseline, Week 1-4, Week 5-8, Week 9-12, Week 13-16, Week 17-20 and at Week 21-24. Daily EXACT total score is obtained as total score of 14 items from diary. Daily E-RS total score as 11 items and Daily E-RS subscale scores are subset of E-RS total score.~Mean EXACT total score is mean value of daily EXACT total score within subject by every 4 weeks(Week1-4, Week5-8, Week9-12, Week13-16, Week17-20, Week21-24). Same calculation of mean values are applied to E-RS total and E-RS subscale scores. Scores range from 0-100, high value in score indicate worse outcome." (NCT01762800)
Timeframe: Baseline and up to 24 weeks

,,,
InterventionScores on a scale (Mean)
Baseline; n=135, 67, 124, 73Week 1-4; n=131, 68, 121, 75Week 5-8; n=126, 68, 115, 73Week 9-12; n=122, 68, 116, 74Week 13-16; n=121, 66, 116, 74Week 17-20; n=118, 66, 114, 72Week 21-24; n=93, 51, 94, 51
SAL/FLU 50/250 µg BID-Single7.426.766.756.696.236.335.99
SAL/FLU 50/250 µg BID-TRIPLE11.4312.3911.8611.7911.6610.809.82
TIO 18 µg QD-Single7.517.186.996.706.826.856.58
TIO 18 µg QD-TRIPLE11.3613.2311.1111.3010.269.899.59

[back to top]

E-RS Subscale Score

The E-RS total score is an 11-item patient questionnaire, which provides information specific to respiratory symptoms-severity of respiratory symptoms overall and severity of breathlessness, cough and sputum, and chest symptoms. The E-RS subscale scores for respiratory symptoms (RS)-breathlessness (RS-BRL), RS-cough and sputum (RS-CSP), and RS-chest symptoms (RS-CSY) are presented. Scores were assessed at Baseline, Week 1-4, Week 5-8, Week 9-12, Week 13-16, Week 17-20 and at Week 21-24. Daily EXACT total score is obtained as total score of 14 items from diary. Daily E-RS total score as 11 items and Daily E-RS subscale scores are subset of E-RS total score. Mean EXACT total score is mean value of daily EXACT total score within subject by every 4 weeks(Week1-4, Week5-8, Week9-12, Week13-16, Week17-20, Week21-24). Same calculation of mean values are applied to E-RS total and E-RS subscale scores. RS total scores range from 0 to 40, high value in score indicate worse outcome. (NCT01762800)
Timeframe: 24 weeks

,,,
InterventionScores on a scale (Mean)
RS-BRL; Baseline; n=135, 68, 125, 73RS-BRL; Week 1-4; n=131, 68, 121, 75RS-BRL; Week 5-8; n=126, 68, 115, 73RS-BRL; Week 9-12; n=122, 68, 116, 74RS-BRL; Week 13-16; n=121, 66, 116, 74RS-BRL; Week 17-20; n=118, 66, 114, 72RS-BRL; Week 21-24; n=93, 51, 94, 51RS-CSP; Baseline; n=135, 68, 124, 73RS-CSP; Week 1-4; n=131, 68, 121, 75RS-CSP; Week 5-8; n=126, 68, 116, 73RS-CSP; Week 9-12; n=122, 68, 116, 74RS-CSP; Week 13-16; n=121, 66, 116, 74RS-CSP; Week 17-20; n=119, 66, 114, 72RS-CSP; Week 21-24; n=93, 51, 94, 51RS-CSY; Baseline; n=135, 67, 125, 73RS-CSY; Week 1-4; n=131, 68, 121, 75RS-CSY; Week 5-8; n=126, 68, 116, 73RS-CSY; Week 9-12; n=122, 68, 116, 74RS-CSY; Week 13-16; n=121, 66, 116, 74RS-CSY; Week 17-20; n=119, 66, 114, 72RS-CSY; Week 21-24; n=93, 51, 94, 51
SAL/FLU 50/250 µg BID-Single3.363.063.083.082.802.822.792.292.122.032.061.982.061.821.771.581.651.541.461.481.38
SAL/FLU 50/250 µg BID-TRIPLE5.816.285.965.875.815.564.942.732.902.832.812.742.432.272.933.213.053.123.112.812.61
TIO 18 µg QD-Single3.413.363.182.983.043.042.952.232.132.132.112.092.091.991.841.691.701.601.701.721.64
TIO 18 µg QD-TRIPLE5.626.595.385.525.114.944.712.813.052.742.772.492.402.342.923.592.993.012.662.552.53

[back to top]

Continuation Percentage of Participants Managed by Randomized Treatment Plus TRIPLE Therapy

The randomized treatment could be switched to TRIPLE therapy in the case that chronic obstructive pulmonary disease (COPD) was not controlled by the randomized treatment. Participants on TRIPLE therapy received SAL/FLU 50/250 µg BID plus TIO 18 µg QD together. Continuation TRIPLE proportion is defined as [(number of subjects who switched to TRIPLE) - (number of subjects who stepped down)/ number of evaluable population]*100. Randomised treatment continuation proportion is calculated by a formula: (100 - switch proportion). (NCT01762800)
Timeframe: 24 weeks

,
InterventionPercentage of participants (Number)
Randomised treatmentTRIPLE therapy
SAL/FLU 50/250 µg BID66.6732.35
TIO 18 µg QD62.6936.82

[back to top]

Percentage of Participants Who Switched to TRIPLE Therapy

Switched to TRIPLE therapy is defined as: 1. Date of switch: when SAL/FLU or TIO was administered additionally to randomised treatment. 2. Date of randomisation was a start point and timing of switching (first switch if there are more than once) to TRIPLE was event. For participants without switching, last day of study or follow up period was regarded as censored. Percentage of participants who switched to TRIPLE therapy was calculated as: number of participants who switched to TRIPLE therapy divided by number of evaluable population and then multiplied by 100. (NCT01762800)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
TIO 18 µg QD37.31
SAL/FLU 50/250 µg BID33.33

[back to top]

Comparison of Number of Exacerbations Between Two Detection Methods: EXACT and Physician Diagnosis

The comparison of number of exacerbation between two detection methods EXACT and physician diagnosis: number of exacerbations detected by EXACT and number of exacerbations judged by physician. (NCT01762800)
Timeframe: 24 weeks

,
InterventionNumber of exacerbations (Mean)
EXACTPhysician's diagnosis
SAL/FLU 50/250 µg BID0.70.1
TIO 18 µg QD0.90.2

[back to top]

Percentage of Participants Who Required Additional Treatment to TRIPLE Therapy

The percentage of participants who required additional treatment to TRIPLE therapy is defined as number of participants who took additional medicine or therapy in TRIPLE therapy divided by number of participants who switch to TRIPLE therapy multiplied by 100. (NCT01762800)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
TIO 18 µg QD77.33
SAL/FLU 50/250 µg BID72.06

[back to top]

Percentage of Participants Who Dropped Out

The percentage of participants who were withdrawn from the study. (NCT01762800)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
TIO 18 µg QD9
SAL/FLU 50/250 µg BID10

[back to top]

Percentage of Participants Managed by TRIPLE Therapy

Percentage of participants managed by TRIPLE therapy was calculated as [(number of participants who switched to TRIPLE therapy) - (number of participants who stepped down)/ number of evaluable population]*100 (NCT01762800)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
TIO 18 µg QD36.82
SAL/FLU 50/250 µg BID32.35

[back to top]

Chronic Obstructive Pulmonary Disease (COPD) Assessment Test (CAT) Total Score

Participants were assessed for COPD symptoms by means of CAT at each Visit. This assessment was performed prior to the spirometry testing. A CAT total score of less than 10 represents best health status and greater than 15 represents worst health status. Scores were assessed at Visit 1 (Screening), Visit 2 (Baseline), Visit 3 (Week 4), Visit 4 (Week 8), Visit 5 (Week 8), Visit 6 (Week 12), Visit 7 (Week 16), and Visit 8 (Week 24). Scores range from 0 to 40, high value in score indicate worse outcome. (NCT01762800)
Timeframe: 24 weeks

,,,
InterventionScores on a scale (Mean)
Visit 1, n=136, 68, 126, 75Visit 2, n=136, 68, 126, 75Visit 3, n=132, 68, 121, 75Visit 4, n=127, 68, 116, 74Visit 5, n=123, 68, 116, 73Visit 6, n=120, 66, 115, 74Visit 7, n=120, 66, 113, 71Visit 8, n=117, 66, 113, 70
SAL/FLU 50/250 µg BID-Single11.39.98.48.38.37.47.77.2
SAL/FLU 50/250 µg BID-TRIPLE13.313.413.513.212.613.312.412.3
TIO 18 µg QD-Single11.29.69.28.88.48.58.37.8
TIO 18 µg QD-TRIPLE13.412.114.313.612.812.011.411.6

[back to top]

Percentage of Participants Who Were Able to Remain on the Randomized Treatment

The randomized treatment could be switched to TRIPLE therapy in the case that chronic obstructive pulmonary disease (COPD) is not controlled by the randomized treatment. Participants on TRIPLE therapy received SAL/FLU 50/250 µg BID plus TIO 18 µg QD together. The percentage of participants who were able to remain on the randomized treatment was calculated by the following formula: 100 minus percentage of participants who switched over to TRIPLE therapy. (NCT01762800)
Timeframe: 24 weeks

InterventionPercentage of participants (Number)
TIO 18 µg QD62.69
SAL/FLU 50/250 µg BID66.67

[back to top]

Change From Baseline in Weighted Mean 0-6 Hour FEV1 Obtained Post-dose at Day 84

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. The weighted mean FEV1 was derived by calculating the area under the curve, and then dividing the value by the relevant time interval. The weighted mean was calculated using the 24-hour serial FEV1 measurements at Day 84, which included pre-dose, and post-dose at 15 min, 30 min, 1 hour, 3 hours, and 6 hours. Baseline trough FEV1 is the mean of the two assessments made at -30 and -5 min pre-dose on Treatment Day 1. Change from Baseline was calculated as the Day 84 value minus the Baseline value. Analysis was performed using a repeated measures model with covariates of treatment, Baseline (mean of the two assessments made at -30and -5 min pre-dose on Treatment Day 1), smoking status, day, day by Baseline and day by treatment interactions. (NCT01772134)
Timeframe: Baseline and Day 84

InterventionLiters (Least Squares Mean)
Placebo QD + FSC 250/50 µg BID0.032
UMEC 62.5 µg QD + FSC 250/50 µg BID0.196
UMEC 125 µg QD + FSC 250/50 µg BID0.192

[back to top]

Change From Baseline in the Trough Forced Expiratory Volume in One Second (FEV1) on Day 85

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. Trough FEV1 on Treatment Day 85 is defined as the mean of the FEV1 values obtained 23 and 24 hours after dosing on Treatment Day 84 (i.e., at Week 12). Baseline trough FEV1 is the mean of the two assessments made at -30 and -5 minutes (min) pre-dose on Treatment Day 1. Change from Baseline was calculated as the Day 85 value minus the Baseline value. Analysis was performed using a repeated measures model with covariates of treatment, Baseline (mean of the two assessments made at -30 and -5 min pre-dose on Treatment Day 1), smoking status, day, day by Baseline and day by treatment interactions. (NCT01772134)
Timeframe: Baseline and Day 85

InterventionLiters (Least Squares Mean)
Placebo QD + FSC 250/50 µg BID-0.022
UMEC 62.5 µg QD + FSC 250/50 µg BID0.125
UMEC 125 µg QD + FSC 250/50 µg BID0.116

[back to top]

Change From Baseline in the Mean Percentage of Rescue-free Days Over Weeks 1-12

A rescue-free day is defined as a day on which no rescue medication was taken. Baseline calculations include a period of the later of 27 days before Visit 2 and the day after Visit 1, up to and including Day 1. The Weeks 1-12 calculations include a period from Study Day 2 up to the earlier of Study Day 85 and the day before Visit 7. Change from Baseline was calculated as the Weeks 1-12 value minus the Baseline value. (NCT01772134)
Timeframe: Baseline and Weeks 1-12

InterventionPercentage of days (Mean)
Placebo QD + FSC 250/50 µg BID4.9
UMEC 62.5 µg QD + FSC 250/50 µg BID13.3
UMEC 125 µg QD + FSC 250/50 µg BID11.1

[back to top]

Change From Baseline in the Mean Number of Puffs Per Day of Rescue Albuterol/Salbutamol Over Weeks 1-12

The mean number of puffs per day of rescue albuterol/salbutamol at Baseline and on-treatment was recorded. The total puffs of rescue albuterol/salbutamol for each day was calculated as: (number of puffs + [2 * number of nebules]). Baseline calculations include a period of the later of 27 days before Visit 2 and the day after Visit 1, up to and including Day 1. The Weeks 1-12 calculations include a period from Study Day 2 up to the earlier of Study Day 85 and the day before Visit 7. Change from Baseline was calculated as the Weeks 1-12 value value minus the Baseline value. Analysis was performed using an analysis of covariance (ANCOVA) model with covariates of treatment, Baseline (mean during the 4 weeks prior to Day 1), and smoking status. (NCT01772134)
Timeframe: Baseline and Weeks 1-12

Interventionpuffs (Least Squares Mean)
Placebo QD + FSC 250/50 µg BID-0.2
UMEC 62.5 µg QD + FSC 250/50 µg BID-0.5
UMEC 125 µg QD + FSC 250/50 µg BID-0.5

[back to top]

Change From Baseline in the Mean Percentage of Rescue-free Days Over Weeks 1-12

A rescue-free day is defined as a day on which no rescue medication was taken. Baseline calculations include a period of the later of 27 days before Visit 2 and the day after Visit 1, up to and including Day 1. The Weeks 1-12 calculations include a period from Study Day 2 up to the earlier of Study Day 85 and the day before Visit 7. Change from Baseline was calculated as the Weeks 1-12 value minus the Baseline value. (NCT01772147)
Timeframe: Baseline and Weeks 1- 12

InterventionPercentage of days (Mean)
Placebo QD + FSC 250/50 µg BID1.9
UMEC 62.5 µg QD + FSC 250/50 µg BID8.4
UMEC 125 µg QD + FSC 250/50 µg BID15.2

[back to top]

Change From Baseline in the Mean Number of Puffs Per Day of Rescue Albuterol/Salbutamol Over Weeks 1-12

The mean number of puffs per day of rescue albuterol/salbutamol at Baseline and on-treatment was recorded. The total puffs of rescue albuterol/salbutamol for each day was calculated as: (number of puffs + [2 * number of nebules]). Baseline calculations include a period of the later of 27 days before Visit 2 and the day after Visit 1, up to and including Day 1. The Weeks 1-12 calculations include a period from Study Day 2 up to the earlier of Study Day 85 and the day before Visit 7. Change from Baseline was calculated as the Weeks 1-12 value minus the Baseline value. Analysis was performed using an analysis of covariance (ANCOVA) model with covariates of treatment, Baseline (mean during the 4 weeks prior to Day 1), and smoking status. (NCT01772147)
Timeframe: Baseline and Weeks1- 12

Interventionpuffs (Least Squares Mean)
Placebo QD + FSC 250/50 µg BID-0.2
UMEC 62.5 µg QD + FSC 250/50 µg BID-0.4
UMEC 125 µg QD + FSC 250/50 µg BID-0.7

[back to top]

Change From Baseline in Weighted Mean 0-6 Hour FEV1 Obtained Post-dose at Day 84

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. The weighted mean FEV1 was derived by calculating the area under the curve, and then dividing the value by the relevant time interval. The weighted mean was calculated using the 6-hour serial FEV1 measurements at Day 84, which included pre-dose, and post-dose at 15 min, 30 min, 1 hour, 3 hours, and 6 hours. Baseline trough FEV1 is the mean of the two assessments made at -30 and -5 min pre-dose on Treatment Day 1. Change from Baseline was calculated as the Day 84 value minus the Baseline value. Analysis was performed using a repeated measures model with covariates of treatment, Baseline (mean of the two assessments made at -30and -5 min pre-dose on Treatment Day 1), smoking status, day, day by Baseline, and day by treatment interactions. (NCT01772147)
Timeframe: Baseline and Day 84

InterventionLiters (Least Squares Mean)
Placebo QD + FSC 250/50 µg BID0.052
UMEC 62.5 µg QD + FSC 250/50 µg BID0.196
UMEC 125 µg QD + FSC 250/50 µg BID0.217

[back to top]

Change From Baseline in the Trough Forced Expiratory Volume in One Second (FEV1) on Day 85

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. Trough FEV1 on Treatment Day 85 is defined as the mean of the FEV1 values obtained 23 and 24 hours after dosing on Treatment Day 84 (i.e., at Week 12). Baseline trough FEV1 is the mean of the two assessments made at -30 and -5 minutes (min) pre-dose on Treatment Day 1. Change from Baseline was calculated as the Day 85 value minus the Baseline value. Analysis was performed using a repeated measures model with covariates of treatment, Baseline (mean of the two assessments made at -30 and -5 min pre-dose on Treatment Day 1), smoking status, day, day by Baseline, and day by treatment interactions. (NCT01772147)
Timeframe: Baseline and Day 85

InterventionLiters (Least Squares Mean)
Placebo QD + FSC 250/50 µg BID-0.001
UMEC 62.5 µg QD + FSC 250/50 µg BID0.126
UMEC 125 µg QD + FSC 250/50 µg BID0.147

[back to top]

Time of Maximum Observed Plasma Concentration (Tmax) of Salmeterol

Blood samples for measurement of plasma SAL concentrations were obtained during each treatment visit (subjects 18 years of age and older only) and pharmacokinetic parameters were derived. (NCT01772368)
Timeframe: Predose (0), and at 5, 10, 15 and 30 minutes, 1, 1.5, 2, 3, 4, 8, and 12 hours postdose

Interventionhours (Median)
FS MDPI 100/6.25 mcg0.1
FS MDPI 100/12.5mcg0.1
FS MDPI 100/25 mcg0.1
FS MDPI 100/50 mcg0.1
Advair Diskus 100/50 mcg0.5

[back to top]

Standardized Baseline-Adjusted Area Under the Curve For Forced Expiratory Volume In 1 Second Over 12 Hours Post-dose (FEV1 AUC0-12)

Standardized baseline-adjusted FEV1 AUC0-12 was defined as the area under the curve for baseline-adjusted FEV1 measurements from the predose to 12 hours postdose time points using the trapezoidal rule based on actual (not scheduled) time of measurement and was standardized by dividing the actual time of last non-missing FEV1 measurement. Baseline-adjusted FEV1 was calculated as postdose FEV1 after subtracting period-specific baseline FEV1. The period-specific baseline FEV1 was measured at predose within 5 minutes of AM dose administration at each treatment visit. If that value was missing, then FEV1 measured at 30 minutes predose was used as the period-specific baseline. (NCT01772368)
Timeframe: Pre-dose: 30 minutes prior, within 5 minutes of dose. Post-dose: 0.5, 1, 2, 3, 4, 5, 6, 9, 12 hours

InterventionmL (Least Squares Mean)
Fp MDPI 100 mcg52.13
FS MDPI 100/6.25 mcg203.84
FS MDPI 100/12.5mcg248.98
FS MDPI 100/25 mcg279.69
FS MDPI 100/50 mcg303.43
Advair Diskus 100/50 mcg245.56

[back to top]

Maximum Observed Plasma Concentration (Cmax) of Salmeterol

Blood samples for measurement of plasma SAL concentrations were obtained during each treatment visit (subjects 18 years of age and older only) and pharmacokinetic parameters were derived. The primary pharmacokinetic parameters were AUC0-t and Cmax for Salmeterol. (NCT01772368)
Timeframe: Predose (0), and at 5, 10, 15 and 30 minutes, 1, 1.5, 2, 3, 4, 8, and 12 hours postdose

Interventionpg/mL (Mean)
FS MDPI 100/6.25 mcg16.0
FS MDPI 100/12.5mcg35.8
FS MDPI 100/25 mcg67.5
FS MDPI 100/50 mcg154.5
Advair Diskus 100/50 mcg42.3

[back to top]

Patients With Treatment-Emergent Adverse Experiences (TEAE) During the Treatment Period

"TEAEs were recorded during each double-blind treatment. In addition, at the end of each treatment, patients continued to use 2 inhalations of Fp MDPI 50 mcg (100 mcg total dose) twice daily, so adverse events during this treatment were assigned to Fp MDPI 50 mcg.~An adverse event was defined as any untoward medical occurrence that develops or worsens in severity during the conduct of a clinical study and does not necessarily have a causal relationship to the study drug. Severity was rated by the investigator on a scale of mild, moderate and severe, with severe= an AE which prevents normal daily activities. Relationship of AE to treatment was determined by the investigator. Serious AEs include death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, OR an important medical event that jeopardized the patient and required medical in" (NCT01772368)
Timeframe: Day 1 up to Day 35

,,,,,,
InterventionParticipants (Count of Participants)
Any adverse eventSevere adverse eventTreatment-related adverse eventDeathsOther serious adverse eventsWithdrawn from treatment due to AE
Advair Diskus 100/50 mcg301000
Fp MDPI 100 mcg200000
Fp MDPI 50 mcg X 2 BID1711001
FS MDPI 100/12.5mcg301000
FS MDPI 100/25 mcg100000
FS MDPI 100/50 mcg110000
FS MDPI 100/6.25 mcg200000

[back to top]

Change From Baseline at 12 Hours Post-Dose in Forced Expiratory Volume in One Second (FEV1) By Treatment

"The secondary efficacy variable was the change from period-specific baseline in FEV1 at 12 hours, calculated as FEV1 measured at 12 hours postdose after subtracting period-specific baseline FEV1 at each treatment period.~The period-specific baseline FEV1 was measured at predose within 5 minutes of AM dose administration at each treatment visit. If that value was missing, then FEV1 measured at 30 minutes predose was used as the period-specific baseline." (NCT01772368)
Timeframe: Pre-dose: 30 minutes prior, within 5 minutes of dose. Post-dose: 12 hours

InterventionmL (Least Squares Mean)
Fp MDPI 100 mcg11.53
FS MDPI 100/6.25 mcg128.49
FS MDPI 100/12.5mcg170.51
FS MDPI 100/25 mcg209.85
FS MDPI 100/50 mcg238.30
Advair Diskus 100/50 mcg170.54

[back to top]

Area Under the Plasma Concentration-time Curve From Time Zero to the Time of the Last Measurable Concentration (AUC0-t) of Salmeterol

Blood samples for measurement of plasma SAL concentrations were obtained during each treatment visit (subjects 18 years of age and older only) and pharmacokinetic parameters were derived. The primary pharmacokinetic parameters were AUC0-t and Cmax for Salmeterol. (NCT01772368)
Timeframe: Predose (0), and at 5, 10, 15 and 30 minutes, 1, 1.5, 2, 3, 4, 8, and 12 hours postdose

Interventionpg*hr/mL (Mean)
FS MDPI 100/6.25 mcg32.8
FS MDPI 100/12.5mcg69.9
FS MDPI 100/25 mcg133.5
FS MDPI 100/50 mcg309.3
Advair Diskus 100/50 mcg173.5

[back to top]

COPD Exacerbation

Number of COPD exacerbations evaluated over 12 months. COPD exacerbation is defined as a new onset or worsening of at least 1 respiratory major symptoms (e.g. dyspnea, cough, sputum volume or sputum purulence) for at least 3 consecutive days, which results in recorded treatment change (antibiotics/steroids/oxygen therapy) OR recorded COPD related hospitalization/Emergency visit. COPD exacerbation is not considered as adverse event, and should only be recorded in COPD e-CRF. (NCT01794780)
Timeframe: Baseline,12 months

InterventionCOPD Exacerbations/year (Mean)
Indacaterol1.1
Tiotropium Bromide0.5
Salmeterol/Fluticasone1.1
Budesonide/ Formoterol0.4
LABA/ICS0.9
Indacaterol +Tiotropium4.1
LABA/ICS + Tiotropium0.8
Oral Theophylline1.0

[back to top]

Change From Baseline in Forced Expiratory Volume in 1 Second (FEV1)

Forced expiratory volume in 1 second (FEV1) is the amount of air that can be exhaled in one second. A positive change from baseline in FEV1 indicates improvement in lung function. Pulmonary function tests were performed at study visits including FEV1, and Force Vital Capacity (FVC). These were performed 30 minutes before treatment and not more than 2 hours in advance after stopping the long-acting bronchodilators eight hours before visits. In order to reduce the variation between each test, the same instrument was used in the whole research process if condition allowed. (NCT01794780)
Timeframe: Baseline,12 months

InterventionLiters (Mean)
Indacaterol0.056
Tiotropium Bromide-0.036
LABA/ICS0.056
Indacaterol +Tiotropium0.030
LABA/ICS + Tiotropium-0.028
Oral Theophylline0.046

[back to top]

Change From Baseline in Forced Expiratory Volume in 1 Second (FEV1)

Forced expiratory volume in 1 second (FEV1) is the amount of air that can be exhaled in one second. A positive change from baseline in FEV1 indicates improvement in lung function. Pulmonary function tests were performed at study visits including FEV1, and Force Vital Capacity (FVC). These were performed 30 minutes before treatment and not more than 2 hours in advance after stopping the Long-acting bronchodilators eight hours before visits. In order to reduce the variation between each test, the same instrument was used in the whole research process if condition allowed. (NCT01794780)
Timeframe: Baseline,3 months

InterventionLiters (Mean)
Indacaterol-0.042
Tiotropium0.006
LABA/ICS0.033
Indacaterol + Tiotropium0.022
LABA/ICS + Tiotropium0.011
Oral Theophylline0.012

[back to top]

Change From Baseline in Questionnaire COPD Assessment Test (CAT) Score

The COPD assessment test (CAT) is a short instrument scale used to quantify the symptom burden of COPD and will be used to assess the health status of patients in this study. It consists of eight items, each presented as a semantic 6-point differential scale, providing a total score out of 40. A higher score indicates a worse health status. Scores of 0 - 10, 11 - 20, 21 - 30 and 31 - 40 represent a mild, moderate, severe or very severe clinical impact of COPD upon the patient. (NCT01794780)
Timeframe: Baseline,3,6,9,12 months

,,,,,
InterventionScore on a scale (Mean)
3 Month6 Month9 Month12 Month
Indacaterol-1.9-1.9-4.4-5.1
Indacaterol +Tiotropium-1.9-2.7-9.0-7.7
LABA/ICS-2.3-2.7-3.5-4.1
LABA/ICS + Tiotropium-1.8-2.2-3.1-3.7
Oral Theophylline-1.8-2.5-3.1-2.4
Tiotropium Bromide-2.1-2.7-3.1-2.6

[back to top]

Change From Baseline Questionnaire Transition Dyspnea Index (TDI) Score

Transition Dyspnea Index (TDI) captures changes from baseline. The TDI score is based on three domains with each domain scored from -3 (major deterioration) to +3 (major improvement), to give an overall score of -9 to +9, a negative score indicating a deterioration from baseline. A TDI focal score of 1 is considered to be a clinically significant improvement from baseline. BDI/TDI was used to assess dyspnea from several aspects, caused by daily activities. These were evaluated by the investigators in the study at the scheduled study visits. The indices were to be evaluated by the same investigator.as far as possible. (NCT01794780)
Timeframe: Baseline,3,6,9,12 months

,,,,,
InterventionUnits on a scale (Mean)
Baseline3 Month6 Month9 Month12 Month
Indacaterol6.71.40.00.70.3
Indacaterol +Tiotropium5.40.4-0.51.01.0
LABA/ICS6.71.31.41.61.7
LABA/ICS + Tiotropium6.21.10.90.91.0
Oral Theophylline7.10.91.21.41.6
Tiotropium Bromide6.61.21.00.91.0

[back to top]

Change in Health Status Questionnaire MMRC

The mMRC scale is scored from 0 (less severe) to 4 (severe). 0 Not troubled with breathlessness except with strenuous exercise; 1 Troubled by shortness of breath when hurrying on the level or walking up a slight hill; 2 Walks slower than people of the same age on the level because of breathlessness or has to stop for breath when walking at own pace on the level; 3 Stops for breath after walking about 100 yards or after a few minutes on the level; 4 Too breathless to leave the house or breathless when dressing or undressing. The modified Medical Research Council (mMRC) Dyspnea Scale , is a five-item instrument (part of the Borg scale) to assess a patient's degree of breathlessness in relation to physical activity. Participants will be required to read a brief description of an activity and then select a statement that best describes their experience with dyspnea at Visit 101. The mMRC was assessed by the investigators at the scheduled visits. (NCT01794780)
Timeframe: Baseline,3,6,9,12 months

,,,,,
InterventionNumber of participants (Number)
Baseline scale item 0Baseline scale item 1Baseline scale item 2Baseline scale item 3Baseline scale item 43 month Scale item 03 month Scale item 13 month Scale item 23 month Scale item 33 month Scale item 46 month Scale item 06 month Scale item 16 month Scale item 26 month Scale item 36 month Scale item 49 month Scale item 09 month Scale item 19 month Scale item 29 month Scale item 39 month Scale item 412 month Scale item 012 month Scale item 112 month Scale item 212 month Scale item 312 month Scale item 4
Indacaterol411143039710258103541015220
Indacaterol +Tiotropium1413004300014100120002100
LABA/ICS1614353271541910136420367696290138545116256131424150275127419
LABA/ICS + Tiotropium632262111102254157133589371491054411451279941947138102329
Oral Theophylline316634194205226111154320402040195120521241
Tiotropium Bromide4011483363246954182235745133245230141246133103

[back to top]

Change From Baseline in Trough FEV1 on Day 85

Trough FEV1 on Day 85 is defined as the mean of the FEV1 values obtained 23 and 24 hours after morning dosing/11 and 12 hours after evening dosing on Day 84. Change from Baseline is calculated as the Day 85 value minus the Baseline value. Analysis was performed using a repeated measures model with covariates of treatment, Baseline (mean of the two assessments made 30 minutes and 5 minutes pre-dose on Day 1), smoking status, day, and day by Baseline and day by treatment interactions. (NCT01817764)
Timeframe: Baseline and Day 85

InterventionLiters (Least Squares Mean)
UMEC/VI 62.5/25 µg QD0.154
FSC 250/50 µg BID0.072

[back to top]

Change From Baseline in 24-hour Weighted-mean Serial FEV1 on Treatment Day 84

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. Weighted mean is calculated from the pre-dose FEV1 and post-dose FEV1 measurements at 5 and 15 minutes and 1, 3, 6, 9, 12 (pre-evening dose), 13, 15, 18, 23, and 24 hours after the morning dose. Change from Baseline was calculated as the value at Day 84 minus the value at Baseline. Analysis was performed using an analysis of covariance of treatment, Baseline (mean of the two assessments made 30 minutes and 5 minutes pre-dose on Day 1), and smoking status. par.=participants. (NCT01817764)
Timeframe: Baseline and Day 84

InterventionLiters (Least Squares Mean)
UMEC/VI 62.5/25 µg QD0.165
FSC 250/50 µg BID0.091

[back to top]

Change From Baseline (BL) in 0 to 24 Hour Weighted Mean Serial Forced Expiratory Volume in One Second (FEV1) at Day 84

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. The weighted mean was calculated from the pre-dose FEV1 and post-dose FEV1 measurements at 5 and 15 minutes and 1, 3, 6, 9, 12 (pre-evening dose), 13, 15, 18, 23, and 24 hours after the morning dose. Analysis was performed using an analysis of covariance (ANCOVA) model with covariates of treatment, Baseline FEV1 (mean of the two assessments made 30 minutes and 5 minutes pre-dose on Day 1), and smoking status. (NCT01822899)
Timeframe: Baseline and Day 84

InterventionLiters (Least Squares Mean)
UMEC/VI 62.5/25 µg0.166
FSC 500/50 µg0.087

[back to top]

Change From Baseline (BL) in Trough Forced Expiratory Volume in One Second (FEV1) at Day 85

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. BL is defined as the mean of the assessments made 30 and 5 minutes (min) pre-dose on Treatment Day 1. Trough FEV1 on Day 85 is defined as the mean of the FEV1values obtained 23 and 24 hours after the previous morning's dosing (i.e., trough FEV1 on Day 85 is the mean of the FEV1 values obtained 23 and 24 hours after morning dosing on Day 84). Analysis was performed using a repeated measures model with covariates of treatment, BL (mean of the two assessments made 30 min and 5 min pre-dose on Day 1), smoking status, day, and day by BL and day by treatment interactions. The model used all available trough FEV1 values recorded on Days 28, 56, 84, and 85. Missing data were not directly imputed in this analysis; however, all non-missing data for a participant were used within the analysis to estimate the treatment effect for trough FEV1 at Day 85. (NCT01822899)
Timeframe: Baseline and Day 85

InterventionLiters (Least Squares Mean)
UMEC/VI 62.5/25 µg0.151
FSC 500/50 µg0.062

[back to top]

Total Airway Resistance Increase

concentration of methacholine required to increase total airway resistance by 40% (PC40R5) (NCT01907334)
Timeframe: 1 to 7 days

Interventionln(mg/mL) (Geometric Mean)
Advair and Advair DiskusesAdvair and Flovent Diskuses
Increase in Airway Resistance After Methacholine4722.9

[back to top]

Peak Forced Expiratory Volume in One Second (FEV1) at Week 24

Peak FEV1 define at the highest value observed in the 3h after the morning IMP administration (NCT01908140)
Timeframe: At Week 24

InterventionLiters (Least Squares Mean)
Aclidinium Bromide / Formoterol Fumarate1.655
Salmeterol / Fluticasone1.562

[back to top]

Transition Dyspnoea Index (TDI) Focal Score at Week 24

"The TDI includes the same 3 categories as BDI and 7 ratings indicating the magnitude of the change from baseline in each category: from -3 (major deterioration) to zero (no change) to +3 (major improvement). Category scores are added to compute the Focal Score (from -9 to 9)" (NCT01908140)
Timeframe: At Week 24

InterventionTDI Focal Score (Least Squares Mean)
Aclidinium Bromide / Formoterol Fumarate1.9
Salmeterol / Fluticasone1.9

[back to top]

Rapidity of ∆Raw Change

The deviation of ∆Raw from the personal target, which was calculated as (measured Raw-target Raw)/target Raw multiplied by 100. (NCT01933984)
Timeframe: Airway resistance will be recorded everyday. If a patient's ventilator was liberated less than 28 days, the day of liberation was the reported time frame. If the day of ventilator liberation was over 28 days, the 28th day was the reported time frame.

Interventionpercentage of relative Raw deviation (Mean)
Individualized Dosing-3
Fixed Dosing0.4

[back to top]

The Participants of Breathing Without Assistance by Day 28

The number of participants who breath without ventilator by day 28 (NCT01933984)
Timeframe: the 28th day after enrollment

Interventionthe number of participants (Number)
Individualized Dosing19
Fixed Dosing22

[back to top] [back to top]

Number of Episode of Nosocomial Pneumonia

The number of episodes of nosocomial pneumonia happened by day 28. And nosocomial pneumonia is a lower respiratory infection that was not incubating at the time of hospital admission and that presents clinically 2 or more days after hospitalization. (NCT01933984)
Timeframe: the 28th day after enrollment

Interventionepisodes of nosocomial pneumonia (Median)
Individualized Dosing0
Fixed Dosing0

[back to top]

Number of Total Puff of Rescue Short-acting Bronchodilator

The number of total puff of rescue short-acting bronchodilator. (NCT01933984)
Timeframe: the 28th day after enrollment

Interventionpuffs (Number)
Individualized Dosing0
Fixed Dosing0

[back to top]

Ventilator-free Days From Day 1 to 28

Ventilator-free days from day 1 to 28 after enrollment (NCT01933984)
Timeframe: From day 1 to day 28 after enrollment

Interventionday (Number)
Individualized Dosing19
Fixed Dosing22

[back to top]

∆Raw (the Difference Between Measured and Target Airway Resistance)

The value can be expressed as relative deviation from target =(measured Raw - target Raw)/target Raw X100 (NCT01933984)
Timeframe: Airway resistance will be recorded everyday. If a patient's ventilator was liberated less than 28 days, the day of liberation was the reported time frame. If the day of ventilator liberation was over 28 days, the 28th day was the reported time frame.

Interventionpercentage of relative Raw deviation (Mean)
Individualized Dosing9
Fixed Dosing44

[back to top]

Mortality Rate

The percentage of participants died at day 180. (NCT01933984)
Timeframe: the 180th day after enrollment

Interventionpercentage of participants (Number)
Individualized Dosing35
Fixed Dosing40

[back to top]

FEV1 AUC (0-12h) Change From Patient Baseline After 6 Weeks of Treatment

"Change from patient baseline in Forced Expiratory Volume in one second (FEV1) Area Under the FEV1-time Curve from 0 to 12hours post-dose (AUC 0-12h) [L] after 6 weeks of treatment. Measured values presented are actually adjusted means.~The period baseline is defined as the pre-dose measurement taken at on the day 1 of each period. The patient baseline is defined as the mean of non-missing period baselines for each patient." (NCT01969721)
Timeframe: Baseline and 6 weeks.

InterventionLitres (Mean)
T+O 2.5/5 / F+S Placebo0.295
T+O 5/5 / F+S Placebo0.317
F+S 250/50 / T+O Placebo0.192
F+S 500/50 / T+O Placebo0.188

[back to top]

FEV1 AUC (12-24h) Change From Patient Baseline After 6 Weeks of Treatment

"Change from patient baseline in Forced Expiratory Volume in one second (FEV1) Area Under the FEV1-time Curve from 12 to 24 hours post-dose (AUC 12-24h) [L] after 6 weeks of treatment. Measured values presented are actually adjusted means.~The period baseline is defined as the pre-dose measurement taken at on the day 1 of each period. The patient baseline is defined as the mean of non-missing period baselines for each patient." (NCT01969721)
Timeframe: Baseline and 6 weeks.

InterventionLitres (Mean)
T+O 2.5/5 / F+S Placebo0.160
T+O 5/5 / F+S Placebo0.172
F+S 250/50 / T+O Placebo0.132
F+S 500/50 / T+O Placebo0.129

[back to top]

FEV1 Peak (0-3h) Change From Patient Baseline After 6 Weeks of Treatment

Change from patient baseline in Forced Expiratory Volume in one second (FEV1) peak (0-3 hours) after 6 weeks of treatment. FEV1 peak (0-3 hours) was defined as the maximum FEV1 value measured within the first three hours post dosing. Measured values presented are actually adjusted means. (NCT01969721)
Timeframe: Baseline and 6 weeks.

InterventionLitres (Mean)
T+O 2.5/5 / F+S Placebo0.401
T+O 5/5 / F+S Placebo0.432
F+S 250/50 / T+O Placebo0.291
F+S 500/50 / T+O Placebo0.285

[back to top]

Trough FEV1 Change From Patient Baseline After 6 Weeks of Treatment

"Change from patient baseline in Trough Forced Expiratory Volume in one second (FEV1) after 6 weeks of treatment. Trough FEV1 was defined as the mean of the 23h and 23h 50min (minutes) post-dose FEV1 measurements. Measured values presented are actually adjusted means.~The period baseline is defined as the pre-dose measurement taken at on the day 1 of each period. The patient baseline is defined as the mean of non-missing period baselines for each patient." (NCT01969721)
Timeframe: Baseline and 6 weeks.

InterventionLitres (Mean)
T+O 2.5/5 / F+S Placebo0.192
T+O 5/5 / F+S Placebo0.197
F+S 250/50 / T+O Placebo0.150
F+S 500/50 / T+O Placebo0.139

[back to top]

FEV1 AUC (0-24h) Change From Patient Baseline After 6 Weeks of Treatment

"Change from patient baseline in Forced Expiratory Volume in one second (FEV1) Area Under the FEV1-time Curve from 0 to 24 hours post-dose (AUC 0-24h) [L] after 6 weeks of treatment.~Measured values presented are actually adjusted means. The period baseline is defined as the pre-dose measurement taken at on the day 1 of each period. The patient baseline is defined as the mean of non-missing period baselines for each patient." (NCT01969721)
Timeframe: Baseline and 6 weeks.

InterventionLitres (Mean)
T+O 2.5/5 / F+S Placebo0.228
T+O 5/5 / F+S Placebo0.244
F+S 250/50 / T+O Placebo0.162
F+S 500/50 / T+O Placebo0.159

[back to top]

Spirometry Measures

"Measured pre/post BD (bronchodilator). Reported as ratio: %FEV1(Liters)/FVC(Liters).~FEV1 = forced expiratory volume at 1 second FVC = forced vital capacity" (NCT02024204)
Timeframe: Week 12

,
Intervention% FEV1(Liters)/FVC(Liters) (Median)
Pre-BD FEV1/FVCPost-BD FEV1/FVC
Visit 1 Controlled LRS81.277.7
Visit 1 Uncontrolled LRS78.578.3

[back to top]

Score on Voice Handicap Index 10 (VHI-10)

"Voice Handicap Index 10 is a measure of laryngeal dysfunction or hypersensitivity to capture the overall state of voice handicap. The normative value for this instrument is 2.83, with a score > 11 considered abnormal. There are 10 statements that are scored between 0 and 4 (0= never, 4= always). The total range is 0-40, where 40 is highest level of dysfunction." (NCT02024204)
Timeframe: Week 12

Interventionscore on VHI-10 scale (Median)
Visit 1 Uncontrolled LRS7
Visit 1 Controlled LRS1

[back to top]

Total EoS (Eosinophil) Counts

EoS counts were obtained by blood test - the total amount of blood drawn is 30 mL. (NCT02024204)
Timeframe: Week 1

Interventioneosiniphils *10^9/Liter (Median)
Visit 1 Uncontrolled LRS.10
Visit 1 Controlled LRS.10

[back to top]

Total IgE (Immunoglobulin E) Levels

IgE levels were obtained by blood test - the total amount of blood drawn is 30 mL. (NCT02024204)
Timeframe: Week 1

Interventionng/mL (Median)
Visit 1 Uncontrolled LRS41
Visit 1 Controlled LRS31

[back to top]

Forced Oscillation Technique (FOT) Measures

Small airway function measured pre/post BD (bronchodilator) impulse oscillometry at resistance 5 Hz (R5) and 5-20 Hz (R5-20). (NCT02024204)
Timeframe: Week 12

,
Interventionresonant frequency (Median)
Pre BD R5Pre BD R5-20Post BD R5Post BD R5-20
Visit 1 Controlled LRS3.70.64.00.6
Visit 1 Uncontrolled LRS4.41.04.10.8

[back to top]

Score on Leicester Cough Questionnaire (LCQ)

For rhinosinusitis symptoms, the Leicester Cough Questionnaire (LCQ) was used - a cough-specific health status questionnaire that assesses the physical, psychological, and social domains of cough. The LCQ is made up of 19 items; the total score range is 3-21; a higher score is associated with better health. (NCT02024204)
Timeframe: Week 12

Interventionscore on LCQ scale (Median)
Visit 1 Uncontrolled LRS12
Visit 1 Controlled LRS15.6

[back to top]

Levels of Fractional Exhaled Nitric Oxide (FeNO)

Measured using a portable device that measures the level of nitric oxide in parts per billion (PPB) in the air slowly exhaled out of the patient's lungs. (NCT02024204)
Timeframe: Week 12

Interventionparts per billion (ppb) (Median)
Visit 1 Uncontrolled LRS17.8
Visit 1 Controlled LRS13

[back to top]

Number of Participants With Positive Level of Paradoxical Vocal Fold Movement (PVFM)

measured by laryngoscopic visualization at rest or after provocation with various odors or exercise. (NCT02024204)
Timeframe: Week 12

InterventionParticipants (Count of Participants)
Visit 1 Uncontrolled LRS21
Visit 1 Controlled LRS6

[back to top]

Number of Participants With Positive Level of Bronchial Hyperreactivity (BHR)

To test whether bronchial Hyperreactivity (BHR), assessed by methacholine challenge, is associated with uncontrolled lower respiratory symptoms. (NCT02024204)
Timeframe: Week 12

InterventionParticipants (Count of Participants)
Visit 1 Uncontrolled LRS18
Visit 1 Controlled LRS6

[back to top]

Rhinosinusitis Score on International Classification of Sleep Disorders (ICSD)

For rhinosinusitis symptoms, the ICSD scoring system was used, with a likert scale of 1-10 for each symptom (total range of scale = 1-60, with higher scores reflecting more symptoms). (NCT02024204)
Timeframe: Week 12

Interventionscore on ICSD scale (Median)
Visit 1 Uncontrolled LRS35
Visit 1 Controlled LRS26

[back to top]

Change From Baseline in Mean Daily Number of Puffs of Rescue Medication Used Over the 24 Week Treatment

A day with no rescue medication use is defined from the diary data as any day where the patient recorded no rescue medicine use during the previous 12 hours. (NCT02055352)
Timeframe: 24 weeks

InterventionPuffs (Mean)
Budesonide/Indacaterol10.5
Fluticasone / Salmeterol12.9

[back to top]

Change From Baseline in Trough Forced Expiratory Volume in 1 Second (Non-inferiority Analysis).

Forced Expiratory Volume in 1 second (FEV1) is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation. (NCT02055352)
Timeframe: Baseline and week 12

InterventionLiters (Least Squares Mean)
Budesonide/Indacaterol0.080
Fluticasone / Salmeterol0.019

[back to top]

Change From Baseline in Trough Forced Expiratory Volume in 1 Second at Week 24 (Analysis of Superiority)

Forced Expiratory Volume in 1 second (FEV1) is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. (NCT02055352)
Timeframe: Baseline and week 24

InterventionLiters (Least Squares Mean)
Budesonide/Indacaterol0.063
Fluticasone / Salmeterol0.020

[back to top]

Change in Health Status - mMRC

Modified Medical Research Council scale (mMRC) questionnaire will be completed by participants. 0 Not troubled with breathlessness except with strenuous exercise; 1 Troubled by shortness of breath when hurrying on the level or walking up a slight hill; 2 Walks slower than people of the same age on the level because of breathlessness or has to stop for breath when walking at own pace on the level; 3 Stops for breath after walking about 100 yards or after a few minutes on the level; 4 Too breathless to leave the house or breathless when dressing or undressing (NCT02055352)
Timeframe: Baseline, week 12 and week 24

,
InterventionScore on a scale (Least Squares Mean)
Week 12Week 24
Budesonide/Indacaterol1.4521.315
Fluticasone / Salmeterol1.6231.414

[back to top]

Change in Health Status - SGRQ-C

St George's Respiratory Questionnaire short version questionnaire will be completed by participants. The SGRQ ranges from 0 (no impairment of quality of life) to 100 (highest impairment of quality of life) (NCT02055352)
Timeframe: Baseline, week 12 and week 24

,
InterventionScore on a scale (Least Squares Mean)
Week 12Week 24
Budesonide/Indacaterol-8.703-7.787
Fluticasone / Salmeterol-2.334-2.523

[back to top]

Asthma Control Test Scores at Screening (Visit 1, Week -8)

"The Asthma Control Test is a 5-item Likert scale questionnaire; Scaling of items 5-point scale (for symptoms and activities: 1=all the time to 5= not at all; for asthma control rating: 1=not controlled at all to 5=completely controlled); The score for each item is summed to generate a total score. The scores range from 5 (poor control of asthma) to 25 (complete control of asthma), with higher scores reflecting greater asthma control. An ACT score >19 indicates well-controlled asthma.~The study was powered to have greater than 90% power to detect a clinically meaningful difference of 3 in the ACT score between the MICT Trial Design and the LASST trial Design , assuming a mean score of 19 with a standard deviation of 4 (data from a previous ALA-ACRC trial)." (NCT02061280)
Timeframe: Screening (Visit 1, week -8)

Interventionscores on a scale (Median)
MICT Trial Design22
LASST Trial Design22

[back to top]

Caregiver Research Participant Assessment Score at Screening (Visit 1, Week -8)

The Research Participant Assessment Score (RPA Comprehension) was a 17-item questionnaire designed to assess comprehension of study information at screening (Visit 1, week -8) between MICT and LASST trial designs. The same 17-item questionnaire was administered to the adolescent participant and to the caregiver participant. The items were scored as 1=incorrect, 2=partially correct, 3=correct (minimum possible score=17 and maximum possible score=51). Scores were assigned by two trained coders who independently listed to audio recordings of the RPA Comprehension questionnaire administration. Scores from the two coders were averaged for a final score. Higher scores indicate better comprehension. Mean (95% Confidence Interval) are the outcome measure reported. (NCT02061280)
Timeframe: Screening (Visit 1, week -8)

InterventionScores on a scale (Mean)
MICT Trial Design43.2
LASST Trial Design42.9

[back to top]

Spirometry Quality Control Grade

"Spirometry grade scores in MICT participants (who performed spirometry at home) were compared with spirometry grade scores in LASST participants (who performed spirometry at the study sites). Spirometry grade scores were only available for LASST participants at Visit 3 (week 0), therefore only spirometry grade scores from Visit 3 were compared between MICT and LASST participants. Per the LASST trial no scoring was performed on the LASST participants for any other visit; the scoring for the LASST trial was for quality control only and was not a pre-specified trial outcome.~Spirometry grade score scale was: 4.00 (highest=best possible score), 3.00, 2.00, 1.00, 0.00 (lowest=worst possible score). The maximum score was 4.00, the minimum score was 0.00. Higher scores indicate better spirometry score and therefore better quality." (NCT02061280)
Timeframe: Visit 3 (week 0)

Interventionscores on a scale (Median)
MICT Trial Design3.75
LASST Trial Design4.00

[back to top]

Caregiver Research Participant Assessment Score at Study End (Visit 6, Week 12)

The Research Participant Assessment Score (RPA Comprehension) was a 17-item questionnaire designed to assess comprehension of study information at screening (Visit 6, week 12) between MICT and LASST trial designs. The same 17-item questionnaire was administered to the adolescent participant and to the caregiver participant. The items were scored as 1=incorrect, 2=partially correct, 3=correct (minimum possible score=17 and maximum possible score=51). Scores were assigned by two trained coders who independently listed to audio recordings of the RPA Comprehension questionnaire administration. Scores from the two coders were averaged for a final score. Higher scores indicate better comprehension. Mean (95% Confidence Interval) are the outcome measure reported. (NCT02061280)
Timeframe: Final Visit (Visit 6, Week12)

InterventionScores on a scale (Mean)
MICT Trial Design43.28
LASST Trial Design41.08

[back to top]

Adolescent Research Participant Assessment Score at Screening (Visit 1, Week -8)

The Research Participant Assessment Score (RPA Comprehension) was a 17-item questionnaire designed to assess comprehension of study information at screening (Visit 1, week -8) between MICT and LASST trial designs. The same 17-item questionnaire was administered to the adolescent participant and to the caregiver participant. The items were scored as 1=incorrect, 2=partially correct, 3=correct (minimum possible score=17 and maximum possible score=51). Scores were assigned by two trained coders who independently listed to audio recordings of the RPA Comprehension questionnaire administration. Scores from the two coders were averaged for a final score. Higher scores indicate better comprehension. Mean (95% Confidence Interval) are the outcome measure reported. (NCT02061280)
Timeframe: Screening (Visit 1, week -8)

InterventionScores on a scale (Mean)
MICT Trial Design41.08
LASST Trial Design42.26

[back to top]

Adolescent Research Participant Assessment Score at Study End (Visit 6, Week 12)

The Research Participant Assessment Score (RPA Comprehension) was a 17-item questionnaire designed to assess comprehension of study information at screening (Visit 6, week 12) between MICT and LASST trial designs. The same 17-item questionnaire was administered to the adolescent participant and to the caregiver participant. The items were scored as 1=incorrect, 2=partially correct, 3=correct (minimum possible score=17 and maximum possible score=51). Scores were assigned by two trained coders who independently listed to audio recordings of the RPA Comprehension questionnaire administration. Scores from the two coders were averaged for a final score. Higher scores indicate better comprehension. Mean (95% Confidence Interval) are the outcome measure reported. (NCT02061280)
Timeframe: Final Visit (Visit 6, Week12)

InterventionScores on a scale (Mean)
MICT Trial Design41.22
LASST Trial Design41.27

[back to top]

Asthma Control Test Score at Final Visit (Visit 6, Week12)

"The Asthma Control Test is a 5-item Likert scale questionnaire; Scaling of items 5-point scale (for symptoms and activities: 1=all the time to 5= not at all; for asthma control rating: 1=not controlled at all to 5=completely controlled); The score for each item is summed to generate a total score. The scores range from 5 (poor control of asthma) to 25 (complete control of asthma), with higher scores reflecting greater asthma control. An ACT score >19 indicates well-controlled asthma.~The study was powered to have greater than 90% power to detect a clinically meaningful difference of 3 in the ACT score between the MICT Trial Design and the LASST trial Design , assuming a mean score of 19 with a standard deviation of 4 (data from a previous ALA-ACRC trial)." (NCT02061280)
Timeframe: Final Visit (Visit 6, Week 12)

Interventionscores on a scale (Median)
MICT Trial Design24
LASST Trial Design23

[back to top]

Change From Baseline in the Weekly Average of the Total Daily (24-hour) Use of Albuterol/Salbutamol Inhalation Aerosol Over the 12-Week Treatment Period

Patients recorded the number of inhalations of rescue medication (albuterol/salbutamol HFA MDI) each AM and PM in the diary. The average number of daily inhalations over the 7 days before the randomization visit was the baseline value. The weekly average was based on the available data for the 7 days before each analysis week. The change from baseline in the weekly average of total daily (24-hour) use of albuterol/ salbutamol inhalation aerosol (number of inhalations) over weeks 1 to 12 was analyzed using a mixed model for repeated measures. (NCT02139644)
Timeframe: Days -6 to Day 1 (predose, baseline), up to week 12

Interventionpuffs (Least Squares Mean)
FS MDPI 100 / 12.5 mcg-0.677
FS MDPI 50 / 12.5 mcg-0.706
Fp MDPI 100 mcg-0.466
Fp MDPI 50 mcg-0.467
Placebo MDPI-0.003

[back to top]

Patients With Treatment-Emergent Adverse Experiences (TEAE) During the Treatment Period

An adverse event was defined as any untoward medical occurrence that develops or worsens in severity during the conduct of a clinical study and does not necessarily have a causal relationship to the study drug. Severity was rated by the investigator on a scale of mild, moderate and severe, with severe= an AE which prevents normal daily activities. Relationship of AE to treatment was determined by the investigator. Serious AEs include death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, OR an important medical event that jeopardized the patient and required medical intervention to prevent the previously listed serious outcomes. (NCT02139644)
Timeframe: Day 1 to Week 12 of the Treatment Period

,,,,
InterventionParticipants (Count of Participants)
>=1 TEAE>=1 severe TEAE>=1 treatment-related TEAE>=1 severe treatment-related TEAE>=1 serious TEAE>=1 TEAE leading to withdrawal>=1 nonserious TEAE>=1 TEAE resulting in death
Fp MDPI 100 mcg4015012390
Fp MDPI 50 mcg4417001440
FS MDPI 100 / 12.5 mcg3724010360
FS MDPI 50 / 12.5 mcg4604003460
Placebo MDPI4705026450

[back to top]

Kaplan-Meier Estimates for Time to 15% and 12% Improvement From Baseline in FEV1 Postdose on Day 1

"A subset of approximately 300 patients who performed postdose serial spirometry is based on sample size calculation. Baseline FEV1 was the average of 2 FEV1 measurements (30 and 10 minutes predose) on Day 1. If one of these was missing, the other measurement was used as baseline value. If both were missing, baseline was treated as missing. Time to target improvement (15% or 12%) was defined as the time elapsed from the time of first dose to the first time the target improvement in FEV1 was achieved. If an exact target increase was not achieved at a measured timepoint, then the time was estimated by linear interpolation between the timepoint when target was reached and the timepoint immediately before. Patients who did not achieve the target improvement were censored at the time of last serial spirometry assessment.~Values of 9999 indicate the values could not be estimated which happened when the estimated probability of not achieving target is more than 50%." (NCT02139644)
Timeframe: Day 1 of the Treatment Period (predose and postdose)

,,,,
Interventionhours (Median)
15% improvement12% improvement
Fp MDPI 100 mcgNANA
Fp MDPI 50 mcgNANA
FS MDPI 100 / 12.5 mcg4.31.0
FS MDPI 50 / 12.5 mcg1.30.5
Placebo MDPINANA

[back to top]

Standardized Baseline-Adjusted Forced Expiratory Volume in 1 Second (FEV1) Area Under the Effect Curve From Time Zero to 12 Hours Postdose (FEV1 AUEC0-12h) at Week 12

"A subset of approximately 300 patients who performed postdose serial spirometry is based on sample size calculation. Data from these assessments were used to analyze the primary endpoint of baseline adjusted FEV1 AUEC0-12h at week 12 using the trapezoidal rule based on actual time of measurement. It was standardized by dividing it by the number of hours between the start time of dose administration and the end time of the last nonmissing FEV1 measurement.~The baseline FEV1 was the average of the 2 predose FEV1 measurements (30 and 10 minutes predose). If 1 of these was missing, the nonmissing value was used; if both were missing, baseline was treated as missing. Baseline-adjusted FEV1 was calculated as postdose FEV1 after subtracting the baseline FEV1 value." (NCT02139644)
Timeframe: Day 1 (predose, baseline), Week 12 and was performed at the following times relative to the administration of study drug (±5 minutes): 15 and 30 minutes and 1, 2, 3, 4, 6, 8, 10, and 12 hours

Interventionliters (Least Squares Mean)
FS MDPI 100 / 12.5 mcg0.408
FS MDPI 50 / 12.5 mcg0.399
Fp MDPI 100 mcg0.254
Fp MDPI 50 mcg0.268
Placebo MDPI0.074

[back to top]

Kaplan-Meier Estimate of Probability of Remaining in Study At Week 12

The analysis of probability of remaining in the study at Week 12 used the time to patient withdrawal for worsening asthma, defined as the number of days elapsed from the date of randomization to the date of withdrawal due to worsening asthma. Patients who were lost to follow-up, who had not withdrawn due to worsening asthma by week 12, or who had withdrawn due to reasons other than worsening asthma were right-censored at the date of last assessment. (NCT02139644)
Timeframe: up to Week 12 of the Treatment Period

Interventionprobability (Number)
FS MDPI 100 / 12.5 mcg1.0000
FS MDPI 50 / 12.5 mcg0.9917
Fp MDPI 100 mcg0.9919
Fp MDPI 50 mcg0.9919
Placebo MDPI0.9681

[back to top]

Change From Baseline in the Weekly Average of the Total Daily Asthma Symptom Score Over the 12-Week Treatment Period

"The total daily asthma symptom score is the average of the daytime and nighttime scores as recorded in the patient diary (range 0-9).~Daytime Symptom Score:~0=No symptoms~Symptoms for 1 short period~Symptoms for 2+ short periods~Symptoms for most of the day - did not affect normal daily activities~Symptoms for most of the day - did affect normal daily activities~Symptoms so severe that I could not go to work or perform normal daily activities~Nighttime Symptom Score (determined in the AM):~0=No symptoms~Symptoms causing me to wake once (or wake early)~Symptoms causing me to wake twice or more (including waking early)~Symptoms causing me to be awake for most of the night~Symptoms so severe that I did not sleep Baseline was the average of recorded scores over the 7 days before randomization. The change from baseline in the weekly average over weeks 1 to 12 was analyzed using an mixed model for repeated measures (MMRM)." (NCT02139644)
Timeframe: Days -6 to Day 1 (predose, baseline) to Week 12

Interventionunits on a scale (Least Squares Mean)
FS MDPI 100 / 12.5 mcg-0.364
FS MDPI 50 / 12.5 mcg-0.329
Fp MDPI 100 mcg-0.300
Fp MDPI 50 mcg-0.278
Placebo MDPI-0.135

[back to top]

Change From Baseline in the Weekly Average of the Daily Morning Trough Peak Expiratory Flow (PEF) Over the 12 Week Treatment

Morning PEF tests were performed before administration of study drug or rescue medications (data were excluded if the time of PEF measurement was more than 5 minutes after the dose time). The patient recorded the highest value of 3 measurements obtained in the patient diary. The baseline PEF was the average value of recorded (nonmissing) morning assessments over the 7 days prior to randomization on Day 1. For efficacy analyses of weekly average morning PEF measurements, values were the averages based on available data for that week. (NCT02139644)
Timeframe: Days -6 to Day 1 (predose), Day 1 (postdose) daily until Week 12

Interventionliters/minute (Least Squares Mean)
FS MDPI 100 / 12.5 mcg24.415
FS MDPI 50 / 12.5 mcg24.864
Fp MDPI 100 mcg14.517
Fp MDPI 50 mcg10.609
Placebo MDPI3.591

[back to top]

Change From Baseline in the Asthma Quality of Life Questionnaire With Standardized Activities (AQLQ(S)) Score at Endpoint for Patients >=18 Years Old

"The AQLQ(S) (September 2010 version; patients aged ≥18 years) was self-administered by the patients at the investigational center at the randomization visit and at Week 12 or end of trial. The questionnaire is a tool to measure the impact of asthma on a patient's quality of life (physical, emotional, social, and occupational) with a recall period of 2 weeks. The AQLQ(S) was administered only to patients 18 years and older. The 32 individual questions in the AQLQ were equally weighted. The overall AQLQ score was the mean of the responses to each of the 32 questions, and ranged from 1 to 7. A score of 7.0 indicated that the patient had no impairments due to asthma and a score of 1.0 indicated severe impairment.~Positive change from baseline scores indicate improved quality of life." (NCT02139644)
Timeframe: Day 1 (predose, baseline), end of trial (up to week 12)

Interventionunits on a scale (Least Squares Mean)
FS MDPI 100 / 12.5 mcg0.808
FS MDPI 50 / 12.5 mcg0.565
Fp MDPI 100 mcg0.636
Fp MDPI 50 mcg0.588
Placebo MDPI0.335

[back to top]

Change From Baseline in Morning Trough Forced Expiratory Volume in 1 Second (FEV1) at Week 12

"Trough FEV1 was a morning spirometry taken predose and pre-rescue bronchodilator. If the patient inadvertently administered asthma medication/study drug at home on the AM of the visit, or if the patient took rescue medication within 6 hours of testing, the visit was rescheduled.~The baseline for predose FEV1 was defined as the average of the 30-minute and 10-minute predose measurements obtained at the randomization visit (Day 1)." (NCT02139644)
Timeframe: Day 1 (predose, baseline), Week 12

Interventionliters (Least Squares Mean)
FS MDPI 100 / 12.5 mcg0.315
FS MDPI 50 / 12.5 mcg0.319
Fp MDPI 100 mcg0.204
Fp MDPI 50 mcg0.172
Placebo MDPI0.053

[back to top]

Change From Baseline in Morning Trough Forced Expiratory Volume in 1 Second (FEV1) at Week 12

Trough FEV1 is a morning spirometry taken predose and pre-rescue bronchodilator. The baseline for predose FEV1 was defined as the average of the 30-minute and 10-minute predose measurements obtained at the randomization visit (Day 1). (NCT02141854)
Timeframe: Day 1 (predose, baseline), Week 12

Interventionliters (Least Squares Mean)
FS MDPI 200 / 12.5 mcg0.272
FS MDPI 100 / 12.5 mcg0.271
Fp MDPI 200 mcg0.179
Fp MDPI 100 mcg0.119
Placebo MDPI-0.004

[back to top]

Change From Baseline in the Asthma Quality of Life Questionnaire With Standardized Activities (AQLQ(S)) Score at Endpoint for Patients >=18 Years Old

"The AQLQ(S) (September 2010 version; patients aged ≥18 years) was self administered by the patients at the investigational center at the randomization visit and at Week 12 or end of trial. The questionnaire is a tool to measure the impact of asthma on a patient's quality of life (physical, emotional, social, and occupational) with a recall period of 2 weeks. The AQLQ(S) was administered only to patients 18 years and older. The 32 individual questions in the AQLQ were equally weighted. The overall AQLQ score was the mean of the responses to each of the 32 questions, and ranged from 1 to 7. A score 7.0 indicated that the patient had no impairments due to asthma and a score of 1.0 indicated severe impairment.~Positive change from baseline scores indicate improved quality of life." (NCT02141854)
Timeframe: Day 1 (predose, baseline), end of trial (up to week 12)

Interventionunits on a scale (Least Squares Mean)
FS MDPI 200 / 12.5 mcg0.534
FS MDPI 100 / 12.5 mcg0.592
Fp MDPI 200 mcg0.384
Fp MDPI 100 mcg0.340
Placebo MDPI-0.089

[back to top]

Change From Baseline in the Weekly Average of the Daily Morning Trough Peak Expiratory Flow (PEF) Over the 12 Week Treatment

"Morning PEF tests were performed before administration of study drug or rescue medications (data were excluded if the time of PEF measurement was more than 5 minutes after the dose time). The patient recorded the highest value of 3 measurements obtained in the patient diary.~The baseline PEF was the average value of recorded (nonmissing) morning assessments over the 7 days prior to randomization on Day 1. For efficacy analyses of weekly average morning PEF measurements, values were the averages based on available data for that week." (NCT02141854)
Timeframe: Days -6 to Day 1 (predose, baseline), Day 1 (postdose) daily until Week 12

Interventionliters/minute (Least Squares Mean)
FS MDPI 200 / 12.5 mcg20.235
FS MDPI 100 / 12.5 mcg18.610
Fp MDPI 200 mcg7.464
Fp MDPI 100 mcg5.731
Placebo MDPI-10.987

[back to top]

Change From Baseline in the Weekly Average of the Total Daily (24-hour) Use of Albuterol/Salbutamol Inhalation Aerosol Over the 12-Week Treatment Period

"Patients recorded the number of inhalations of rescue medication (albuterol/salbutamol HFA MDI) each AM and PM in the diary. The average number of daily inhalations over the 7 days before the randomization visit was the baseline value. The weekly average was based on the available data for the 7 days before each analysis week.~The change from baseline in the weekly average of total daily (24-hour) use of albuterol/ salbutamol inhalation aerosol (number of inhalations) over weeks 1 to 12 was analyzed using a mixed model for repeated measures." (NCT02141854)
Timeframe: Days -6 to Day 1 (predose, baseline), up to week 12

Interventionpuffs (Least Squares Mean)
FS MDPI 200 / 12.5 mcg-0.898
FS MDPI 100 / 12.5 mcg-0.821
Fp MDPI 200 mcg-0.534
Fp MDPI 100 mcg-0.439
Placebo MDPI0.168

[back to top]

Change From Baseline in the Weekly Average of the Total Daily Asthma Symptom Score Over the 12-Week Treatment Period

"The total daily asthma symptom score is the average of the daytime and nighttime scores as recorded in the patient diary.~Daytime Symptom Score:~0=No symptoms~1=Symptoms for 1 short period~2=Symptoms for 2+ short periods~3=Symptoms for most of the day - did not affect normal daily activities~4=Symptoms for most of the day - did affect normal daily activities~5=Symptoms so severe that I could not go to work or perform normal daily activities~Nighttime Symptom Score (determined in the AM):~0=No symptoms~1=Symptoms causing me to wake once (or wake early)~2=Symptoms causing me to wake twice or more (including waking early)~3=Symptoms causing me to be awake for most of the night~4=Symptoms so severe that I did not sleep Baseline was the average of recorded scores over the 7 days before randomization. The change from baseline in the weekly average over weeks 1 to 12 was analyzed using an mixed model for repeated measures (MMRM)." (NCT02141854)
Timeframe: Days -6 to Day 1 (predose, baseline), to Week 12

Interventionunits on a scale (Least Squares Mean)
FS MDPI 200 / 12.5 mcg-0.391
FS MDPI 100 / 12.5 mcg-0.364
Fp MDPI 200 mcg-0.242
Fp MDPI 100 mcg-0.282
Placebo MDPI-0.087

[back to top]

Kaplan-Meier Estimate of Probability of Remaining in Study At Week 12

The analysis of probability of remaining in the study at Week 12 used the time to patient withdrawal for worsening asthma, defined as the number of days elapsed from the date of randomization to the date of withdrawal due to worsening asthma. Patients who were lost to follow-up, who had not withdrawn due to worsening asthma by week 12, or who had withdrawn due to reasons other than worsening asthma were right-censored at the date of last assessment. (NCT02141854)
Timeframe: up to Week 12 of the Treatment Period

Interventionprobability (Number)
FS MDPI 200 / 12.5 mcg0.9719
FS MDPI 100 / 12.5 mcg0.9929
Fp MDPI 200 mcg0.9786
Fp MDPI 100 mcg0.9930
Placebo MDPI0.8528

[back to top]

Standardized Baseline-Adjusted Forced Expiratory Volume in 1 Second (FEV1) Area Under the Effect Curve From Time Zero to 12 Hours PostDose (FEV1 AUEC0-12) at Week 12

A subset of patients performed postdose serial spirometry. Data from these assessments were used to analyze the primary endpoint of baseline-adjusted FEV1 AUEC0-12h at week 12 using the trapezoidal rule based on actual time of measurement. It was standardized by dividing it by the number of hours between the start time of dose administration and the end time of the last nonmissing FEV1 measurement. The baseline FEV1 was the average of the 2 predose FEV1 measurements (30 and 10 minutes predose). If 1 of these was missing, the nonmissing value was used; if both were missing, baseline was treated as missing. Baseline-adjusted FEV1 was calculated as postdose FEV1 after subtracting the baseline FEV1 value. (NCT02141854)
Timeframe: Day 1 (predose, baseline), Week 12 and was performed at the following times relative to the administration of study drug (±5 minutes): 15 and 30 minutes and 1, 2, 3, 4, 6, 8, 10, and 12 hours

Interventionliters (Least Squares Mean)
FS MDPI 200 / 12.5 mcg0.446
FS MDPI 100 / 12.5 mcg0.442
Fp MDPI 200 mcg0.267
Fp MDPI 100 mcg0.260
Placebo MDPI0.121

[back to top]

Kaplan-Meier Estimates for Time to 15% and 12% Improvement From Baseline in FEV1 Postdose on Day 1

"The baseline forced expiratory volume in 1 second (FEV1) was the average of the 2 predose FEV1 measurements (30 and 10 minutes predose) on Day 1. If one of these was missing, the other measurement was used as baseline value. If both were missing, the baseline trough FEV1 was treated as missing.~Time to target improvement (15% or 12%) was defined as the time elapsed from the time of first dose to the first time the target improvement in FEV1 was achieved. If an exact target increase was not achieved at a measured timepoint, then the time was estimated by linear interpolation between the timepoint when target was reached and the timepoint immediately before. Patients who did not achieve the target improvement were censored at the time of last serial spirometry assessment.~Values of NA indicate the values could not be estimated which happened when the estimated probability of not achieving target is more than 50%." (NCT02141854)
Timeframe: Day 1 of the Treatment Period (predose and postdose)

,,,,
Interventionhours (Median)
15% improvement12% improvement
Fp MDPI 100 mcgNANA
Fp MDPI 200 mcgNA6.9
FS MDPI 100 / 12.5 mcg0.90.4
FS MDPI 200 / 12.5 mcg0.80.4
Placebo MDPINANA

[back to top]

Patients With Treatment-Emergent Adverse Experiences (TEAE) During the Treatment Period

An adverse event was defined as any untoward medical occurrence that develops or worsens in severity during the conduct of a clinical study and does not necessarily have a causal relationship to the study drug. Severity was rated by the investigator on a scale of mild, moderate and severe, with severe= an AE which prevents normal daily activities. Relation of AE to treatment was determined by the investigator. Serious AEs include death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, OR an important medical event that jeopardized the patient and required medical intervention to prevent the previously listed serious outcomes. (NCT02141854)
Timeframe: Day 1 to Week 12 of the Treatment Period

,,,,
InterventionParticipants (Count of Participants)
>=1 TEAE>=1 severe TEAE>=1 treatment-related TEAE>=1 severe treatment-related TEAE>=1 serious TEAE>=1 TEAE leading to withdrawal>=1 nonserious TEAE>=1 TEAE resulting in death
Fp MDPI 100 mcg5316012520
Fp MDPI 200 mcg6009010600
FS MDPI 100 / 12.5 mcg5924022581
FS MDPI 200 / 12.5 mcg6138122610
Placebo MDPI5215012520

[back to top]

Analysis of 24-Hour Urine Cortisol Free Over the 26-Week Treatment Period

"Samples for 24-hour urine cortisol were collected at baseline (Day 1, pretreatment), and Weeks 14 and 26. For participants requiring early termination (ET), this evaluation was performed at the ET visit. For participants requiring ET for safety reasons, the visit was not delayed in order to collect the 24-hour urine cortisol.~The analysis is based on a mixed model for repeated measures (MMRM) model with adjustment for visit, treatment, and a treatment*visit interaction. The urine cortisol result is log transformed prior to analysis and the results are back transformed after modeling. An unstructured covariance matrix is used in the MMRM model." (NCT02175771)
Timeframe: Baseline (Day 1, pre-treatment), Weeks 14 and 26 and early termination visit if applicable

Interventionmcg/24 hours (Geometric Mean)
Fp MDPI 100 mcg18.45
FLOVENT HFA 110 mcg13.94
Fp MDPI 200 mcg14.14
FLOVENT HFA 220 mcg17.50
FS MDPI 100/12.5 mcg17.56
ADVAIR DISKUS 250/50 mcg18.29
FS MDPI 200/12.5 mcg13.02
ADVAIR DISKUS 500/50 mcg15.42

[back to top]

Shifts From Baseline to Endpoint in Electrocardiogram (ECG) Findings

A 12 lead ECG was conducted at the screening visit and week 26 or the early termination visit. A qualified physician at a central diagnostic center was responsible for interpreting the ECG. The worst post-baseline finding for the participant is summarized. Endpoint refers to the last observation carried forward. (NCT02175771)
Timeframe: Screening (Day -14), Endpoint (week 26 if study was completed)

,,,,,,,
InterventionParticipants (Count of Participants)
Baseline normal - Endpoint normalBaseline normal - Endpoint abnormalBaseline abnormal - Endpoint normalBaseline abnormal - Endpoint abnormal
ADVAIR DISKUS 250/50 mcg30224
ADVAIR DISKUS 500/50 mcg28344
FLOVENT HFA 110 mcg31512
FLOVENT HFA 220 mcg33123
Fp MDPI 100 mcg898411
Fp MDPI 200 mcg936413
FS MDPI 100/12.5 mcg909125
FS MDPI 200/12.5 mcg101897

[back to top]

Participants With Treatment-Emergent Adverse Experiences (TEAE) During the Treatment Period

An adverse event was defined as any untoward medical occurrence that develops or worsens in severity during the conduct of a clinical study and does not necessarily have a causal relationship to the study drug. Severity was rated by the investigator on a scale of mild, moderate and severe, with severe= an AE which prevents normal daily activities. Relationship of AE to treatment was determined by the investigator. Serious AEs include death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, OR an important medical event that jeopardized the patient and required medical intervention to prevent the previously listed serious outcomes. (NCT02175771)
Timeframe: Day 1 to Week 26 of the Treatment Period

,,,,,,,
InterventionParticipants (Count of Participants)
>=1 TEAE>=1 severe TEAE>=1 treatment-related TEAE>=1 severe treatment-related TEAE>=1 serious TEAE>=1 TEAE leading to withdrawal>=1 nonserious TEAE>=1 TEAE resulting in death
ADVAIR DISKUS 250/50 mcg2914022280
ADVAIR DISKUS 500/50 mcg3038031290
FLOVENT HFA 110 mcg2932021270
FLOVENT HFA 220 mcg2935031290
Fp MDPI 100 mcg85810072850
Fp MDPI 200 mcg83116080820
FS MDPI 100/12.5 mcg9289063910
FS MDPI 200/12.5 mcg8612110130850

[back to top]

Participants With Potentially Clinically Significant Abnormal Vital Signs During the Treatment Period

"Data represents participants with potentially clinically significant (PCS) vital sign values during the Treatment period.~Significance criteria:~Systolic blood pressure - high: >=180 and increase >=20 mmHg~Systolic blood pressure - low: <=90 and decrease >=20 mmHg~Diastolic blood pressure - high: >=105 and increase of >=15 mmHg~Diastolic blood pressure - low: <=50 and decrease of >=15 mmHg~Pulse - high: >=120 and increase of >= 15 beats/minute from baseline~Pulse - low: <=50 and decrease of >=15 beats/minute" (NCT02175771)
Timeframe: Baseline (Day 1 pre-treatment), Weeks 2, 6, 10, 14, 18, 22 26, Endpoint

,,,,,,,
InterventionParticipants (Count of Participants)
>=1 abnormalitySystolic blood pressure - highSystolic blood pressure - lowDiastolic blood pressure - highDiastolic blood pressure - lowPulse - highPulse - low
ADVAIR DISKUS 250/50 mcg0000000
ADVAIR DISKUS 500/50 mcg0000000
FLOVENT HFA 110 mcg0000000
FLOVENT HFA 220 mcg1000100
Fp MDPI 100 mcg5011111
Fp MDPI 200 mcg0000000
FS MDPI 100/12.5 mcg2010100
FS MDPI 200/12.5 mcg2001100

[back to top]

Participants With Positive Swab Test Results for Oral Candidiasis

"Oropharyngeal examinations for visual evidence of oral candidiasis were conducted at each visit by a qualified healthcare professional. Any visual evidence of oral candidiasis during the oropharyngeal exam was evaluated by obtaining and analyzing a swab of the suspect area.~This outcomes indicates how many participants had positive swab test results. The total number of participants who had oropharyngeal exams at each timepoint are specified in the timepoint field. Appropriate therapy was to be initiated immediately at the discretion of the investigator and was not to be delayed for culture confirmation. Participants with a culture-positive infection could continue participation in the study on appropriate anti-infective therapy, provided this therapy was not prohibited by the protocol." (NCT02175771)
Timeframe: Baseline (Day 1 pre-treatment), Weeks 2, 6, 10, 14, 18, 22 26, Endpoint

,,,,,,,
InterventionParticipants (Count of Participants)
Baseline (n=127, 42, 124, 41, 120, 41, 133, 44)Week 2 (n=123, 42, 123, 40, 117, 39, 131, 43)Week 6 (n=119, 41, 119, 40, 115, 39, 125, 43)Week 10 (n=119, 37, 118, 39, 115, 39, 120, 40)Week 14 (n=116, 36, 115, 38, 113, 38, 120, 41)Week 18 (n=111, 37, 115, 38, 109, 38, 117, 40)Week 22 (n=110, 36, 113, 36, 110, 37, 116, 38)Week 26 (n=111, 35, 113, 36, 110, 36, 116, 38)Endpoint (n=125, 42, 123, 41, 119, 40, 132, 44)
ADVAIR DISKUS 250/50 mcg002101011
ADVAIR DISKUS 500/50 mcg020110200
FLOVENT HFA 110 mcg000000000
FLOVENT HFA 220 mcg000111111
Fp MDPI 100 mcg221011111
Fp MDPI 200 mcg010111111
FS MDPI 100/12.5 mcg011120100
FS MDPI 200/12.5 mcg011010200

[back to top]

Change From Baseline in Trough Forced Expiratory Volume in 1 Minute (FEV1) Over the 26-Week Treatment Period

"Spirometry measurements were obtained before the AM dose of study drug for the randomization visit (Day 1), at each of the treatment visits and at the early termination visit if applicable. At each visit where FEV1 was assessed, the highest acceptable results from each session were recorded.~The analysis is based on a mixed model for repeated measures (MMRM) with adjustment for baseline FEV1, sex, age, (pooled) investigational center, visit, treatment, and treatment-by-visit. An unstructured covariance matrix is used in the MMRM model." (NCT02175771)
Timeframe: Baseline (Day 1 pre-treatment), Weeks 2, 6, 10, 14, 18, 22 26, early termination visit if applicable

Interventionliters (Least Squares Mean)
Fp MDPI 100 mcg0.062
FLOVENT HFA 110 mcg0.053
Fp MDPI 200 mcg0.077
FLOVENT HFA 220 mcg0.090
FS MDPI 100/12.5 mcg0.116
ADVAIR DISKUS 250/50 mcg0.117
FS MDPI 200/12.5 mcg0.100
ADVAIR DISKUS 500/50 mcg0.041

[back to top]

Max Heart Rate

max heart rate at the 2, 6, or 12 inhalations dose, assessed at multiple times over 6 hours (NCT02232087)
Timeframe: Baseline through 6 hours

Interventionbpm (Mean)
Test Product A65.1
Reference Product D65.5
Test Product B68.9
Reference Product E69.9
Test Product C75.3
Reference Product F76.8

[back to top]

Max Plasma Glucose Level

maximum levels of glucose at the 2, 6 or 12 inhalations dose, assessed at multiple times over 6 hours. (NCT02232087)
Timeframe: baseline through 6 hours

Interventionmmol/L (Mean)
Test Product A5.31
Reference Product D5.31
Test Product B5.53
Reference Product E5.62
Test Product C5.88
Reference Product F5.98

[back to top]

Max QTcB

For each dose, the 95% CIs for the mean difference for the test product versus the reference product were calculated. (NCT02232087)
Timeframe: Baseline through 6 hours

Interventionms (Mean)
Test Product A422.3
Reference Product D422.1
Test Product B430.0
Reference Product E430.2
Test Product D441.0
Reference Product F444.0

[back to top]

Plasma Potassium Level

maximum plasma levels of potassium at 2, 6 or 12 inhalations dose inhalations dose, assessed a multiple times over 6 hours. (NCT02232087)
Timeframe: baseline through 6 hours

Interventionmmol/L (Mean)
Test Product A3.82
Reference Product D3.78
Test Product B3.76
Reference Product E3.75
Test Product C3.63
Reference Product F3.61

[back to top]

Relative Potency Max Heart Rate

Selection of steepest part of dose response curve for Relative Potency: 6 and 12 inhalation dose pairs. Slope of B and C line compared with slope of E and F to obtain relative potency value. Two inhalation dose not utilized as not on steepest part of curve. (NCT02232087)
Timeframe: Baseline, up to 6 hrs

Interventionunitless (Number)
Test B and C vs Reference E and F0.8619

[back to top]

Relative Potency QTcB Interval

Selection of steepest part of dose response curve for Relative Potency: 2 and 6 inhalation dose pairs. Slope of A and B line compared with slope of D and E to obtain relative potency value. Twelve inhalation dose not utilized as not on steepest part of curve. (NCT02232087)
Timeframe: Baseline up to 6 hrs

Interventionunitless (Number)
Test A and B vs Reference D and E1.0760

[back to top]

FEV1 Trough Value (Assay Sensitivity)

Change from baseline in trough (pre-dose) FEV1 at Day 29 was based on 2 pre-dose FEV1 assessments performed 30 minutes apart on Day 29. Baseline was calculated by taking the mean of [prebronchodilator FEV1 measured at a run-in visit and the mean of 2 predose FEV1 measures taken at Day 1]. To confirm assay sensitivity, both active treatments (MGR001 and Advair Diskus) had to be significantly superior to placebo. (NCT02245672)
Timeframe: Day 1 and Day 29

InterventionL (Least Squares Mean)
MGR0010.2927
Advair Diskus0.2720
Placebo0.0575

[back to top]

Forced Exhaled Volume in 1 Sec (FEV1) Area Under the Effect Curve on Day 1 (Bioequivalence)

The FEV1 AUEC(0-12) on Day 1 was calculated from FEV1 measurements collected 30 minutes prior to morning dose, 0 minutes prior to morning dose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours following completion of dosing on Day 1 (Visit 3). The baseline for the FEV1 AUEC(0-12) endpoint was the mean of the 2 predose FEV1 measures (NCT02245672)
Timeframe: 0-12 hours after dosing on Day 1

InterventionL*hr (Least Squares Mean)
MGR0013.9734
Advair Diskus3.5411
Placebo0.8400

[back to top]

Forced Exhaled Volume in 1 Sec (FEV1) Area Under the Effect Curve on Day 1 (Assay Sensitivity)

The FEV1 AUEC(0-12) on Day 1 was calculated from FEV1 measurements collected 30 minutes prior to morning dose, 0 minutes prior to morning dose, and at 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours following completion of dosing on Day 1 (Visit 3). The baseline for the FEV1 AUEC(0-12) endpoint was the mean of the 2 predose FEV1 measures. To confirm assay sensitivity, both active treatments (MGR001 and Advair Diskus) had to be significantly superior to placebo (NCT02245672)
Timeframe: 0-12 hours after dosing on Day 1

InterventionL*hr (Least Squares Mean)
MGR0013.9534
Advair Diskus3.4964
Placebo0.8191

[back to top]

FEV1 Trough Value (Bioequivalence)

Change from baseline in trough (pre-dose) FEV1 at Day 29 was based on 2 pre-dose FEV1 assessments performed 30 minutes apart on Day 29. Baseline was calculated by taking the mean of [prebronchodilator FEV1 measured at a run-in visit and the mean of 2 predose FEV1 measures taken at Day 1] (NCT02245672)
Timeframe: Day 1 and Day 29

InterventionL (Least Squares Mean)
MGR0010.2911
Advair Diskus0.2728
Placebo0.0574

[back to top]

Area Under the Serial FEV1-time Curve (AUC 0-12h)

Bioequivalence comparison of lung function (FEV1) for 12 hours after the first dose on Day 1 following OT329 Solis and Advair Diskus treatment. Serial lung function measurements were made pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose. (NCT02260492)
Timeframe: 0-12 hours after dosing on Day 1

InterventionLiters (Mean)
OT329 Solis29.610
Advair Diskus30.151
Placebo27.270

[back to top]

Number of Participants With Adverse Events

(NCT02260492)
Timeframe: From Screen (Day -28) until 1 week post last treatment

InterventionParticipants (Count of Participants)
OT329 Solis67
Advair Diskus66
Placebo7

[back to top]

FEV1 Trough

Bioequivalence comparison of trough lung function (FEV1) after 4 weeks of treatment with OT329 SOLIS or ADVAIR DISKUS. (NCT02260492)
Timeframe: Post-4 weeks of treatment

InterventionLiters (Mean)
OT329 Solis2.516
Advair Diskus2.579
Placebo2.323

[back to top]

Change From Baseline in PM FEV1 Using Per Protocol (PP) Population

FEV1 was defined as the volume of air that can be forced out in one second after taking a deep breath. FEV1 (pre-bronchodilator and pre-dose) was measured at Baseline up to Week 24 at evening using spirometry. Repeated Measures analysis was adjusted for Baseline, region, sex, age, treatment, visit, visit by Baseline interaction and visit by treatment interaction. Visit 3 values were taken as Baseline value and change from Baseline was defined as the difference between the value of the endpoint at the time point of interest and the Baseline value. Statistical analysis was performed using the MMRM models and least square mean and standard error were calculated. The analysis was performed on PP Population which comprised of all participants in the ITT Population who did not had any full protocol deviations. (NCT02301975)
Timeframe: Baseline and Week 24

InterventionL (Least Squares Mean)
FF/VI 100/25 mcg Once Daily0.020
FP/S 250/50 mcg Twice Daily0.014
FP 250 mcg Twice Daily-0.099

[back to top]

Change From Baseline in Evening (Post Meridiem [PM]) Forced Expiratory Volume in One Second (FEV1) Using Intent-to-Treat (ITT) Population

FEV1 was defined as the volume of air that can be forced out in one second after taking a deep breath. FEV1 (pre-bronchodilator and pre-dose) was measured at Baseline up to Week 24 at evening using spirometry. Repeated Measures analysis was adjusted for Baseline, region, sex, age, treatment, visit, visit by Baseline interaction and visit by treatment interaction. Visit 3 values were taken as Baseline value and change from Baseline was defined as the difference between the value of the endpoint at the time point of interest and the Baseline value. Statistical analysis was performed using the mixed model repeated measures (MMRM) model and least square mean and standard error were calculated. The analysis was performed on ITT Population which comprised of all participants randomized to treatment and who received at least one dose of study medication. (NCT02301975)
Timeframe: Baseline and Week 24

InterventionLiter (L) (Least Squares Mean)
FF/VI 100/25 mcg Once Daily0.019
FP/S 250/50 mcg Twice Daily0.000
FP 250 mcg Twice Daily-0.104

[back to top]

Change From Baseline in Morning (Ante Meridiem [AM]) Peak Expiratory Flow (PEF)

PEF was measured using an electric flow meter each morning. Change from Baseline (defined as the last 7 days prior to randomization of the participants) was calculated as the value of the averaged daily AM PEF over the 24-week treatment period minus the Baseline value. Statistical analysis was performed using an ANCOVA model with covariates of Baseline, region, sex, age and treatment and least square mean and standard error were calculated. (NCT02301975)
Timeframe: Baseline and Weeks 1-24

InterventionLiter per minute (L/min) (Least Squares Mean)
FF/VI 100/25 mcg Once Daily8.9
FP/S 250/50 mcg Twice Daily3.7
FP 250 mcg Twice Daily-12.6

[back to top]

Change From Baseline in PM PEF

PEF was measured using an electric flow meter each evening. Change from Baseline (defined as the last 7 days prior to randomization of the participants) was calculated as the value of the averaged daily PM PEF over the 24-week treatment period minus the Baseline value. Statistical analysis was performed using an ANCOVA model with covariates of Baseline, region, sex, age and treatment and least square mean and standard error were calculated. (NCT02301975)
Timeframe: Baseline and Weeks 1-24

InterventionL/min (Least Squares Mean)
FF/VI 100/25 mcg Once Daily5.5
FP/S 250/50 mcg Twice Daily0.5
FP 250 mcg Twice Daily-13.7

[back to top]

Change From Baseline in the Percentage of Rescue-free 24-hour Periods

The number of inhalations of rescue medication used during the day and night were recorded by participants using an electronic diary (e-diary). A 24-hour (hr) period in which a participant's responses to both the morning and evening assessments indicated no use of rescue medication was considered to be rescue free. The Baseline value was derived from the last 7 days of the daily eDiary prior to the randomization of the participant. Change from Baseline was calculated as the averaged value during the 24-week treatment period minus the Baseline value. Statistical analysis was performed using an Analysis of Covariance (ANCOVA) model with covariates of Baseline, region, sex, age and treatment and least square mean and standard error were calculated. (NCT02301975)
Timeframe: Baseline and Weeks 1-24

InterventionPercentage of rescue-free 24-hr periods (Least Squares Mean)
FF/VI 100/25 mcg Once Daily-3.0
FP/S 250/50 mcg Twice Daily-4.2
FP 250 mcg Twice Daily-5.7

[back to top]

Change From Baseline in the Percentage of Symptom-free 24-hour Periods

Change from Baseline in the percentage of symptom-free 24 hour period was evaluated. A 24-hour (hr) period in which a participant's responses to both the morning and evening assessments indicated no symptoms was considered to be symptom free. The Baseline value was derived from the last 7 days of the daily eDiary prior to the randomization of the participant. Change from Baseline was calculated as the averaged value during the 24-week treatment period minus the Baseline value.Statistical analysis was performed using an ANCOVA model with covariates of Baseline, region, sex, age and treatment and least square mean and standard error were calculated. (NCT02301975)
Timeframe: Baseline and Weeks 1-24

InterventionPercentage of symptom-free 24 hour perio (Least Squares Mean)
FF/VI 100/25 mcg Once Daily-3.5
FP/S 250/50 mcg Twice Daily-4.7
FP 250 mcg Twice Daily-6.2

[back to top]

Percentage of Participants With Asthma Control Test (ACT) Score Greater Than or Equal to 20

The ACT was a five-item questionnaire developed as a measure of participant's asthma control. The percentage of participants controlled, defined as having ACT score greater than or equal to 20 at the end of Week 24 were analyzed using logistic regression model with covariates of Baseline ACT score, region, sex, age and treatment group. (NCT02301975)
Timeframe: Week 24

InterventionPercentage of participants (Number)
FF/VI 100/25 mcg Once Daily92
FP/S 250/50 mcg Twice Daily93
FP 250 mcg Twice Daily91

[back to top]

Percent Change in Waist Circumference

(NCT02398188)
Timeframe: 8 weeks post the start of treatment

Interventionpercent change (Mean)
LIPO-20224.1
Placebo24.2

[back to top]

Percent Change in the Patient Reported Global Abdominal Perception Score

1 equals much improved, 7 equals much worse. The higher the scores the worse the outcome. (NCT02398188)
Timeframe: 8 weeks post the start of treatment

Interventionpercent change (Mean)
LIPO-202202
Placebo175

[back to top]

Percentage of Subjects Who Achieved a Composite P-GAPS1/CPnS2 Response

"The composite P-GAPS1/CPnS2 response was defined as at least a 1 point (grade) improvement in P-GAPS and at least a 2 point (grade) improvement in CPnS from baseline after 8 weeks of treatment.~Patient - Global Abdominal Perception Scale (P-GAPS) - a patient views and assesses the contour of their abdomen on a 5-point verbal scale ranging from Flat to Big Bulge.~Clinician Photonumeric Scale (CPnS) - a trained clinician rater examines the subject's abdomen and matches the subject's abdominal bulge/profile to the nearest gender-specific abdominal photo on the 6-point scale." (NCT02398188)
Timeframe: Baseline and End of Study (1 week post last treatment, 9 weeks after first treatment)

InterventionParticipants (Count of Participants)
LIPO-20237
Placebo48

[back to top]

Change From Baseline in Asthma Control Questionnaire (ACQ-5) on Day 15

The ACQ-5 measures 5 symptoms (woken at night by symptoms, wake in the morning with symptoms, limitation of daily activities, shortness of breath, and wheeze). The scale is 0-6, where 0=minimum and 6=maximum (NCT02433834)
Timeframe: Day 1-Day 15 in each of 5 treatment periods

InterventionScores on a scale (Least Squares Mean)
GP MDI 28.8 µg-0.167
GP MDI 14.4 µg-0.173
GP MDI 7.2 µg-0.113
GP MDI 3.6 µg-0.100
GP MDI 1.9 µg-0.205
Placebo MDI-0.056
SAL 50 µg-0.304

[back to top]

Change From Baseline in Average Daily Post-dose PEFR Over 14 Days

Daily pre-dose PEFR and daily post-dose PEFR will each be calculated as the average of the AM and PM measurements recorded for a given day. If either the AM or PM assessment is missing, only the single measurement will be used. Analyses of average daily pre-dose PEFR, average daily post-dose PEFR, and rescue Ventolin HFA usage will use the average of the non-missing daily values recorded in the subject diaries over each week and over the last week of treatment within each period. (NCT02433834)
Timeframe: Day 1-Day 15 in each of 5 treatment periods

InterventionL/min (Least Squares Mean)
GP MDI 28.8 µg5.53
GP MDI 14.4 µg-2.86
GP MDI 7.2 µg-5.38
GP MDI 3.6 µg3.09
GP MDI 1.9 µg-5.68
Placebo MDI-21.65
SAL 50 µg3.55

[back to top]

Change From Baseline in Average Daily Pre-dose PEFR Over 14 Days

Change from baseline in average daily pre-dose peak expiratory flow rate (PEFR) over 14 days Daily pre-dose PEFR and daily post-dose PEFR will each be calculated as the average of the AM and PM measurements recorded for a given day. If either the AM or PM assessment is missing, only the single measurement will be used. Analyses of average daily pre-dose PEFR, average daily post-dose PEFR, and rescue Ventolin HFA usage will use the average of the non-missing daily values recorded in the subject diaries over each week and over the last week of treatment within each period. (NCT02433834)
Timeframe: Day 1-Day 15 in each of 5 treatment periods

InterventionL/min (Least Squares Mean)
GP MDI 28.8 µg5.01
GP MDI 14.4 µg-6.54
GP MDI 7.2 µg-10.65
GP MDI 3.6 µg-2.98
GP MDI 1.9 µg-10.52
Placebo MDI-22.57
SAL 50 µg-3.00

[back to top]

Change From Baseline in Average Daily Rescue Medication Use Over 14 Days

Daily pre-dose PEFR and daily post-dose PEFR will each be calculated as the average of the AM and PM measurements recorded for a given day. If either the AM or PM assessment is missing, only the single measurement will be used. Analyses of average daily pre-dose PEFR, average daily post-dose PEFR, and rescue Ventolin HFA usage will use the average of the non-missing daily values recorded in the subject diaries over each week and over the last week of treatment within each period. (NCT02433834)
Timeframe: Day 1-Day 15 in each of 5 treatment periods

InterventionPuffs (Least Squares Mean)
GP MDI 28.8 µg-0.42
GP MDI 14.4 µg-0.25
GP MDI 7.2 µg-0.24
GP MDI 3.6 µg-0.24
GP MDI 1.9 µg-0.23
Placebo MDI-0.11
SAL 50 µg-0.63

[back to top]

Change From Baseline in Morning Pre-dose Trough FEV1 on Day 15

Change from baseline in morning pre-dose trough FEV1 on Day 15 (NCT02433834)
Timeframe: Day 1-Day 15 in each of 5 treatment periods

InterventionLiter (Least Squares Mean)
GP MDI 28.8 µg0.073
GP MDI 14.4 µg0.047
GP MDI 7.2 µg0.042
GP MDI 3.6 µg0.012
GP MDI 1.9 µg0.018
Placebo MDI-0.012
SAL 50 µg0.059

[back to top]

FEV1 AUC0-3 on Day 15

FEV1 AUC0-3 is the area under the curve for the change from baseline in FEV1 calculated using the trapezoidal rule. All observed data will be used with the trapezoidal rule to calculate AUC. To aid in interpretation, all AUC values will be normalized by dividing the AUC by the time from the first to the last non-missing value (typically 3 hours). (NCT02433834)
Timeframe: Day 1-Day 15 in each of 5 treatment periods

InterventionLiter (Least Squares Mean)
GP MDI 28.8 µg0.191
GP MDI 14.4 µg0.167
GP MDI 7.2 µg0.146
GP MDI 3.6 µg0.147
GP MDI 1.9 µg0.113
Placebo MDI0.038
SAL 50 µg0.190

[back to top]

Peak Change From Baseline in FEV1 Within 3 Hours Post-dosing on Day 15

Forced Expiratory Volume in 1 second (FEV1) within 3 hours post-dosing on Day 15 (NCT02433834)
Timeframe: From Day 1 to Within 3 hours post dosing on Day 15 in each of 5 treatment periods

InterventionLiter (Least Squares Mean)
GP MDI 28.8 µg0.284
GP MDI 14.4 µg0.261
GP MDI 7.2 µg0.252
GP MDI 3.6 µg0.237
GP MDI 1.9 µg0.215
Placebo MDI0.130
SAL 50 µg0.285

[back to top]

Area Under the Concentration Versus Time Curve (AUClast)

Area under the concentration of fluticasone versus time curve from the time of dosing to the last measurable concentration (NCT02441114)
Timeframe: Period 1 (day 1), 2 (day 15), and 3 (day 29) at 0 to 24 h post-dose

Interventionh*pg/mL (Mean)
Period 1Period 2Period 3
Inhalation of HCP0910 and HGP1011686.981247.631769.58

[back to top]

Maximum Observed Concentration (Cmax)

Maximum observed concentration of fluticasone (NCT02441114)
Timeframe: Period 1 (day 1), 2 (day 15), and 3 (day 29) at 0 to 24 h post-dose

Interventionpg/mL (Mean)
Period 1Period 2Period 3
Inhalation of HCP0910 and HGP101195.70173.56246.77

[back to top]

Time to Maximum Concentration (Tmax)

Time to maximum concentration of fluticasone (NCT02441114)
Timeframe: Period 1 (day 1), 2 (day 15), and 3 (day 29) at 0 to 24 h post-dose

Interventionh (Median)
Period 1Period 2Period 3
Inhalation of HCP0910 and HGP10110.760.500.88

[back to top]

Change From Baseline in ACT Total Score at Week 24

The ACT is a validated self-completed questionnaire consisting of 5 questions that evaluate asthma control on a 5-point categorical scale. Total scores are calculated from the sum of the scores from the 5 questions and can range from 5 to 25, with higher scores indicating better control. An ACT total score of 5 to 19 suggests that the participant's asthma is unlikely to be well controlled, whilst a score of 20 to 25 suggests that the participant's asthma is likely to be well controlled. Baseline value was the last assessment prior to randomization (Day 0). Change from Baseline was post-dose visit value minus the Baseline value. Least square mean change is presented. (NCT02446418)
Timeframe: Baseline and Week 24

InterventionScores on a Scale (Least Squares Mean)
Usual ICS/LABA3.6
FF/VI4.0

[back to top]

Change From Baseline in Asthma Control Test (ACT) Total Score at Week 12

The ACT is a validated self-completed questionnaire consisting of 5 questions that evaluate asthma control during the past 4 weeks on a 5-point categorical scale. Total scores are calculated from the sum of the scores from the 5 questions and can range from 5 to 25, with higher scores indicating better control. An ACT total score of 5 to 19 suggests that the participant's asthma is unlikely to be well controlled, whilst a score of 20 to 25 suggests that the participant's asthma is likely to be well controlled. Baseline value was the last assessment prior to randomization (Day 0). Change from Baseline was post-dose visit value minus the Baseline value. Least square mean change is presented. (NCT02446418)
Timeframe: Baseline and Week 12

InterventionScores on a Scale (Least Squares Mean)
Usual ICS/LABA2.8
FF/VI3.6

[back to top]

Percentage of Participants With Correct Use of Device, Defined as Not Making Any Critical or Non-critical Errors, at Week 12, and at Week 24 Independently of the Use at Week 12

Participants were asked to read the appropriate package insert for their prescribed inhaler and then the investigator (or suitably qualified designee) demonstrated the proper use of the inhaler. The participant was then asked to self-administer their first dose of study treatment under the supervision of the investigator and any critical and non-critical errors were recorded. Individual instruments for assessing correct inhaler use were provided for each of the three devices used in this study. (NCT02446418)
Timeframe: Week 12 and Week 24

,
InterventionPercentage of participants (Number)
Week 12; n= 195, 197Week 24; n= 191, 192
FF/VI9497
Usual ICS/LABA9396

[back to top]

Change From Baseline in FVC (Forced Vital Capacity)

Pulmonary function assessments were performed using centralized spirometry according to international standards. FVC wil follow the same analysis as for FEV1 (NCT02516592)
Timeframe: week 12

InterventionLiters (Least Squares Mean)
QVA149 110/50 Micrograms0.073
Salmeterol/Fluticasone 50/500 Micrograms-0.028

[back to top]

Change From Baseline in Mean Daily Use of Rescue Medication

Use of rescue medication (number of puffs taken in the previous 12 hours) is recorded morning and evening, by the patient, in a paper diary. A negative change from baseline indicates an improvement. (NCT02516592)
Timeframe: over 12 weeks

InterventionNumber of puffs (Least Squares Mean)
QVA149 110/50 Micrograms1.05
Salmeterol/Fluticasone 50/500 Micrograms1.09

[back to top]

Change From Baseline in Total Symptom Score- CAT (COPD Assessment Test)

The participants will record their COPD symptoms in this test before every clinic visit, this will include : cough, phlegm, chest tightness, breathlessness, limitation in activities, energy, soundly sleep, etc. A higher score indicates a worse health status. The result is immediately available without the need for any calculation, apart from summing the scores on individual items. Scores of 0 - 10 represent mild, 11 - 20 represent moderate, 21 - 30 represent severe and 31 - 40 represent very severe clinical impact of COPD upon the patient. (NCT02516592)
Timeframe: week 12

InterventionScore on a scale (Least Squares Mean)
QVA149 110/50 Micrograms13.4
Salmeterol/Fluticasone 50/500 Micrograms13.8

[back to top]

Change From Baseline in Trough Pre-dose FEV1 in Both Arms

Pulmonary function assessments were performed using centralized spirometry according to international standards. Mean trough pre-dose FEV1 at Week 12 is defined as the average of the measurements taken -45min and -15min pre study medication dose in the clinic after 12 weeks of treatment (Day 84). The baseline measurement is defined as the average of the scheduled FEV1 values prior to first intake of randomized study drug at Day 1 (Visit 2). (NCT02516592)
Timeframe: Baseline, week 12

InterventionLiters (Least Squares Mean)
QVA149 110/50 Micrograms0.036
Salmeterol/Fluticasone 50/500 Micrograms-0.009

[back to top]

Transitional Dyspnea Index (TDI) Focal Score

Transition Dyspnea Index (TDI) is an instrument used to assess a participant's level of dyspnea. The TDI focal score have three domains: functional impairment, magnitude of task and magnitude of effort. TDI domains were rated from -3 (major deterioration) to 3 (major improvement) and rates summed for transition focal score ranged from -9 to 9; negative scores indicate deterioration. A TDI focal score of ≥1 was defined as a clinically important improvement from baseline. (NCT02516592)
Timeframe: Baseline, week 12

InterventionScore on a scale (Least Squares Mean)
QVA149 110/50 Micrograms3.24
Salmeterol/Fluticasone 50/500 Micrograms2.79

[back to top]

Time in Days to Permanent Discontinuation of Study Medication Due to Asthma Exacerbations

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02554786)
Timeframe: Up to Week 52

Interventiondays (Median)
QMF149 150/320 μg367.0
QMF149 150/160 μg367.0
MF 800 μg367.0
MF 400 μg366.0
Salmeterol /Fluticasone 50/500 μg367.0

[back to top]

Pre-dose FEV1 at Weeks 4 and 12

Pre-dose trough FEV1 is defined as average of the two FEV1 measurements taken 45 min and 15 min pre evening dose. It was assessed by performing spirometric assessment. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. (NCT02554786)
Timeframe: Weeks 4 (Day 30) and 12 (Day 86)

,,,,
InterventionL (Least Squares Mean)
Day 30Day 86
MF 400 μg2.1712.177
MF 800 μg2.2372.245
QMF149 150/160 μg2.3672.361
QMF149 150/320 μg2.3692.368
Salmeterol /Fluticasone 50/500 μg0.23332.330

[back to top]

Percentage of Participants Achieving the Minimal Important Difference (MID) ACQ ≥ 0.5 at Weeks 26 and 52

Change from baseline in ACQ-7 scores of ≤ 0.5 was defined as minimal clinically important difference and were considered clinically meaningful. The ACQ-7 measured asthma symptom control and consists of 7 items: 5 on symptom assessment, 1 on rescue bronchodilator use and 1 on airway calibre (FEV1 % predicted). All 7 questions of the ACQ-7 were equally weighted. Items 1-5 were scored along a 7-point response scale, where 0 = totally controlled and 6 = severely uncontrolled. Item 6 is scored between 0 = no rescue medication and 6 = More than 16 puffs/inhalations most days. The 7th item was scored by the investigator based on the FEV1 % predicted from the masterscope at the site (i.e., Score = 0 means > 95% of predicted FEV1, 1 = 90 - 95%, 2 = 80 - 89%, 3 = 70 - 79%, 4 = 60 - 69%, 5 = 50 - 59%, and Score = 6 means < 50% of predicted FEV1). The total score was calculated as the mean of all questions (NCT02554786)
Timeframe: Weeks 26 (Day 183) and 52 (Day 364)

,,,,
Interventionpercentage of participants (Number)
Day 183Day 364
MF 400 μg66.969.2
MF 800 μg72.373.6
QMF149 150/160 μg76.282.1
QMF149 150/320 μg76.477.7
Salmeterol/Fluticasone 50/500 μg75.977.3

[back to top]

Percentage of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)

An AE is any untoward medical occurrence (i.e., any unfavorable and unintended sign including abnormal laboratory findings, symptom or disease) in a participant or clinical investigation participant after providing written informed consent for participation in the study. An SAE is defined as any adverse event (appearance of (or worsening of any pre-existing) undesirable sign(s), symptom(s) or medical conditions(s) which meets any one of the following criteria: is fatal or life-threatening, results in persistent or significant disability/incapacity, constitutes a congenital anomaly/birth defect, requires inpatient hospitalization or prolongation of existing hospitalization or is medically significant, i.e. defined as an event that jeopardizes the participants or may require medical or surgical intervention. (NCT02554786)
Timeframe: Approximately up to 56 weeks

,,,,
Interventionpercentage of participants (Number)
Adverse Events(AEs)Serious Adverse Events(SAEs)
MF 400 μg72.27.0
MF 800 μg70.04.8
QMF149 150/160 μg66.84.6
QMF149 150/320 μg64.64.7
Salmeterol/Fluticasone 50/500 μg65.34.7

[back to top]

Trough FEV1 Measured After 26 Weeks of Treatment

Trough FEV1 was assessed by performing spirometric assessment. It is defined as average of the two FEV1 measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. (NCT02554786)
Timeframe: Week 26

InterventionL (Least Squares Mean)
QMF149 150/320 μg2.383
QMF149 150/160 μg2.387
MF 800 μg2.250
MF 400 μg2.176
Salmeterol/Fluticasone 50/500 μg2.346

[back to top]

Percentage of Participants With at Least One Asthma Exacerbation by Exacerbation Category

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02554786)
Timeframe: Up to Week 52

,,,,
Interventionpercentage of participants (Number)
Moderate or severe asthma exacerbationSevere asthma exacerbationModerate asthma exacerbationMild asthma exacerbationAll (mild, moderate, severe) asthma exacerbation
MF 400 μg32.520.116.519.644.5
MF 800 μg26.114.514.317.536.1
QMF149 150/160 μg16.99.88.212.125.6
QMF149 150/320 μg14.98.17.713.325.5
Salmeterol/Fluticasone 50/500 μg19.111.99.215.130.6

[back to top]

Trough FEV1 at Week 52

Trough FEV1 was assessed by performing spirometric assessment. It is defined as average of the two FEV1 measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. (NCT02554786)
Timeframe: Week 52

InterventionL (Least Squares Mean)
QMF149 150/320 μg2.386
QMF149 150/160 μg2.357
MF 800 μg2.249
MF 400 μg2.148
Salmeterol/Fluticasone 50/500 μg2.338

[back to top]

Total Amounts of Systemic Corticosteroids (in Doses) Used to Treat Asthma Exacerbations

The treatment of asthma exacerbations including the initiation of systemic corticosteroids were done according to investigator's or treating physician's medical judgement and in line with national and international recommendations. If systemic corticosteroids were required, a participant could return to the study after successfully completing a taper of approximately 7-10 days. (NCT02554786)
Timeframe: Up to Week 52

Interventionmilligrams (Mean)
QMF149 150/320 μg26.0
QMF149 150/160 μg29.9
MF 800 μg28.0
MF 400 μg47.8
Salmeterol/Fluticasone 50/500 μg26.9

[back to top]

Time to First Hospitalization for Asthma Exacerbation

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02554786)
Timeframe: Up to Week 52

Interventiondays (Median)
QMF149 150/320 μg367.0
QMF149 150/160 μg367.0
MF 800 μg367.0
MF 400 μg366.0
Salmeterol/Fluticasone 50/500 μg367.0

[back to top]

Change Form Baseline in Percentage of Mornings With no Symptoms on Awakening

"All participants were provided with an electronic diary (e-Diary) to record clinical symptoms. They were instructed to routinely complete the e-Diary twice daily at the same time each morning and again approximately 12 hours later in the evening. The e-Diary was reviewed at each visit until study completion. The question asked for mornings with no symptoms on awakening was Did you have asthma symptoms upon awakening in the morning? to be answered with None with scores from 0 (no problem)-4 (very severe problems)." (NCT02554786)
Timeframe: Up to Week 52

Interventionpercentage of mornings (Least Squares Mean)
QMF149 150/320 μg25.5
QMF149 150/160 μg22.9
MF 800 μg19.1
MF 400 μg14.1
Salmeterol/Fluticasone 50/500 μg20.7

[back to top]

Percentage of Participants With Composite Endpoint of Serious Asthma Outcomes

A composite endpoint of serious asthma outcomes is defined as asthma-related hospitalization, asthma-related intubation, or asthma-related death and was reviewed by the Adjudication Committee. (NCT02554786)
Timeframe: Up to Week 52

Interventionpercentage of participants (Number)
QMF149 150/320 μg0.7
QMF149 150/160 μg0.5
MF 800 μg1.6
MF 400 μg1.8
Salmeterol/Fluticasone 50/500 μg0.5

[back to top]

Post Dose FEV1 (5 Minutes-1 Hour)

Post-dose FEV1 measurements were analyzed at 5 minutes, 15 minutes, 30 minutes and 1 hour. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. (NCT02554786)
Timeframe: Up to Week 52 (Day 364)

,,,,
InterventionL (Least Squares Mean)
Day 1: 5 minutesDay 1: 15 minutesDay 1: 30 minutesDay 1: 1 hourDay 30: 5 minutesDay 30: 30 minutesDay 30: 1 hourDay 86:5 minutesDay 86: 30 minutesDay 86:1 hourDay 183: 5 minutesDay 183: 30 minutesDay 183: 1 hourDay 364: 5 minutesDay 364: 30 minutesDay 364:1 hour
MF 400 μg2.1182.1372.1412.1422.1742.1742.1832.1782.1792.1882.1632.1682.1652.1302.1352.128
MF 800 μg2.1382.1592.1622.1662.2242.2382.2572.2482.2572.2692.2402.2502.2532.2452.2532.251
QMF149 150/160 μg2.2702.3122.3262.3472.4062.4262.4402.4092.4312.4362.4062.4272.4232.3792.3992.390
QMF149 150/320 μg2.2792.3212.3382.3432.4132.4322.4482.4112.4362.4562.4032.4262.4322.3842.4082.414
Salmeterol/Fluticasone 50/500 μg2.2242.2782.3102.3372.3602.3892.4112.3562.3982.4132.3592.3862.3932.3582.3772.383

[back to top]

Trough Forced Vital Capacity (FVC)

FVC is the total amount of air exhaled during the FEV test. Trough FVC is defined as average of the two FVC measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. It was assessed by performing spirometric assessment. (NCT02554786)
Timeframe: Up to Week 52 (Day 365)

,,,,
InterventionL (Least Squares Mean)
Day 2Day 184Day 365
MF 400 μg3.2033.2463.218
MF 800 μg3.2563.3223.319
QMF149 150/160 μg3.3423.3873.364
QMF149 150/320 μg3.3423.3723.394
Salmeterol/Fluticasone 50/500 μg3.3443.3553.358

[back to top]

Percentage of Participants Who Permanently Discontinued Study Medication Due to Asthma Exacerbations

(NCT02554786)
Timeframe: Up to Week 52

Interventionpercentage of participants (Number)
QMF149 150/320 μg0.2
QMF149 150/160 μg0
MF 800 μg0.9
MF 400 μg1.6
Salmeterol/Fluticasone 50/500 μg0.5

[back to top]

Change From Baseline in Percentage of Nights With no Night-time Awakenings

"All participants were provided with an electronic diary (e-Diary) to record clinical symptoms. They were instructed to routinely complete the e-Diary twice daily at the same time each morning and again approximately 12 hours later in the evening. The e-Diary was reviewed at each visit until study completion. The question asked for nights with no night-time awakenings was How did you sleep last night? had to be answered with I did not wake up because of any breathing problems with scores from 0 (no problem)-4 (very severe problems)." (NCT02554786)
Timeframe: Up to Week 52

Interventionpercentage of nights (Least Squares Mean)
QMF149 150/320 μg17.0
QMF149 150/160 μg16.4
MF 800 μg14.2
MF 400 μg12.5
Salmeterol/Fluticasone 50/500 μg16.1

[back to top]

Change From Baseline in Percentage of Asthma Symptoms Free Days

All participants were provided with an electronic diary (e-Diary) to record clinical symptoms. They were instructed to routinely complete the e-Diary twice daily at the same time each morning and again approximately 12 hours later in the evening. The e-Diary was reviewed at each visit until study completion. Asthma symptoms free days are days with no daytime symptoms, no night-time awakenings and no symptoms on awakening. The daytime asthma symptom score was based on the daily e-diary recordings by participants with respect to shortness of breath, wheeze, cough, chest tightness, and impact on usual daily activities due to symptoms. (NCT02554786)
Timeframe: Up to Week 52

Interventionpercentage of days (Least Squares Mean)
QMF149 150/320 μg28.3
QMF149 150/160 μg28.4
MF 800 μg22.5
MF 400 μg19.3
Salmeterol/Fluticasone 50/500 μg24.9

[back to top]

Trough Forced Expiratory Volume in One Second (Trough FEV1) at Week 26

Trough FEV1 was assessed by performing spirometric assessment. It is defined as average of the two FEV1 measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. (NCT02554786)
Timeframe: 26 weeks

Interventionlitre (L) (Least Squares Mean)
QMF149 150/320 μg2.383
QMF149 150/160 μg2.387
MF 800 μg2.250
MF 400 μg2.176
Salmeterol/Fluticasone 50/500 μg2.346

[back to top]

Change Form Baseline in Percentage of Days With no Daytime Symptoms

All participants were provided with an electronic diary (e-Diary) to record clinical symptoms. They were instructed to routinely complete the e-Diary twice daily at the same time each morning and again approximately 12 hours later in the evening. The e-Diary was reviewed at each visit until study completion. For days with no daytime symptoms, all 5 evening questions must have a score = 0 with respect to shortness of breath, wheeze, cough, chest tightness and impact on usual daily activities due to symptoms, each with scores from 0 (no problems) to 4 (very severe problems). (NCT02554786)
Timeframe: Up to Week 52

Interventionpercentage of days (Least Squares Mean)
QMF149 150/320 μg28.0
QMF149 150/160 μg28.0
MF 800 μg23.0
MF 400 μg20.0
Salmeterol/Fluticasone 50/500 μg24.8

[back to top]

Trough Forced Expiratory Flow (FEF)Between 25% and 75% of FVC (FEF25-75)

FEF is the flow (or speed) of air coming out of the lung during the middle portion of a forced expiration. Trough FEF25-75% is defined as average of the two FEF25-75% measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. It was assessed by performing spirometric assessment. (NCT02554786)
Timeframe: Up to Week 52 (Day 365)

,,,,
InterventionLitres/second (L/s) (Least Squares Mean)
Day 2Day 184Day 365
MF 400 μg1.4061.4731.440
MF 800 μg1.4551.5461.530
QMF149 150/160 μg1.6171.7381.686
QMF149 150/320 μg1.6441.7751.745
Salmeterol/Fluticasone 50/500 μg1.6621.6921.692

[back to top]

Time to First Asthma Exacerbation by Exacerbation Category

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02554786)
Timeframe: Up to Week 52

,,,,
Interventiondays (Median)
Moderate or severe asthma exacerbationSevere asthma exacerbationAll (mild, moderate or severe) asthma exacerbation
MF 400 μg364.0366306.0
MF 800 μg366.0366364.5
QMF149 150/160 μg366.0366366.0
QMF149 150/320 μg366.0367366.0
Salmeterol/Fluticasone 50/500 μg366.0366365.0

[back to top]

Annual Rate of Asthma Exacerbations by Exacerbation Category

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02554786)
Timeframe: Up to Week 52

,,,,
Interventionexacerbations per year (Mean)
Moderate or severe asthma exacerbationSevere asthma exacerbationAll (mild, moderate, severe) asthma exacerbation
MF 400 μg0.560.291.05
MF 800 μg0.390.180.74
QMF149 150/160 μg0.270.130.48
QMF149 150/320 μg0.250.130.49
Salmeterol/Fluticasone 50/500 μg0.270.140.52

[back to top]

Asthma Control Questionnaire (ACQ-7) at Weeks 4, 12, 26 and 52

The ACQ-7 measured asthma symptom control and consists of 7 items: 5 on symptom assessment, 1 on rescue bronchodilator use and 1 on airway calibre (FEV1 % predicted). All 7 questions of the ACQ-7 were equally weighted. Items 1-5 were scored along a 7-point response scale, where 0 = totally controlled and 6 = severely uncontrolled. Item 6 is scored between 0 = no rescue medication and 6 = More than 16 puffs/inhalations most days. The 7th item was scored by the investigator based on the FEV1 % predicted from the masterscope at the site (i.e., Score = 0 means > 95% of predicted FEV1, 1 = 90 - 95%, 2 = 80 - 89%, 3 = 70 - 79%, 4 = 60 - 69%, 5 = 50 - 59%, and Score = 6 means < 50% of predicted FEV1). The total score was calculated as the mean of all questions. (NCT02554786)
Timeframe: Weeks 4, 12, 26 and 52

,,,,
Interventionscore on a scale (Least Squares Mean)
Week 4Week 12Week 26Week 52
MF 400 μg1.7301.6251.5091.449
MF 800 μg1.6591.5231.4391.373
QMF149 150/160 μg1.5331.3771.2611.183
QMF149 150/320 μg1.4861.3941.2671.231
Salmeterol/Fluticasone 50/500 μg1.5411.4451.3221.221

[back to top]

Asthma Quality of Life Questionnaire (AQLQ)

"AQLQ is a 32-item disease specific questionnaire designed to measure functional impairments that are most important to patients with asthma, with a recall time of two weeks and each question to be answered on a 7-point scale (1-totally limited/problems all the time, 7-not at all limited/no problems). It consists of 4 domains:~Symptoms = Mean of Items 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 29, 30 (12 items)~Activity limitation = Mean of Items 1, 2, 3, 4, 5, 11, 19, 25, 28, 31, 32 (11 items)~Emotional function = Mean of Items 7, 13, 15, 21, 27 (5 items)~Environmental stimuli = Mean of Items 9, 17, 23, 26 (4 items)~Overall Score = Mean of Items 1 to 32 (32 items)" (NCT02554786)
Timeframe: Up to Week 52 (Day 364)

,,,,
Interventionscore on a scale (Least Squares Mean)
Day 30Day 86Day 183Day 254Day 364
MF 400 μg5.3745.5105.5815.6145.641
MF 800 μg5.4135.5645.5985.6895.705
QMF149 150/160 μg5.4985.6295.7385.7815.832
QMF149 150/320 μg5.5605.6185.7245.7615.783
Salmeterol/Fluticasone 50/500 μg5.5155.5925.6395.7005.742

[back to top]

Change From Baseline in Morning and Evening Peak Expiratory Flow Rate (PEF) Over 26 and 52 Weeks of Treatment

PEF is a person's maximum speed of expiration. All the participants were instructed to record PEF twice daily using a mini Peak Flow Meter device, once in the morning (before taking the morning dose) and once approximately 12 h later in the evening (before taking the evening dose). At each timepoint, the participant was instructed to perform 3 consecutive manoeuvres within 10 minutes. These PEF values were captured in the e-PEF/diary. The best of 3 values were used. (NCT02554786)
Timeframe: Up to Weeks 26 and 52

,,,,
InterventionL/min (Least Squares Mean)
Week 26: Mean morning PEFWeek 26:Mean evening PEFWeek 52:Mean morning PEFWeek 52:Mean evening PEF
MF 400 μg5.90.06.7-0.3
MF 800 μg12.87.713.47.4
QMF149 150/160 μg38.130.436.928.7
QMF149 150/320 μg42.432.542.131.2
Salmeterol/Fluticasone 50/500 μg29.123.928.322.1

[back to top]

Change From Baseline in Percentage of Rescue Medication Free Days

All participants were given salbutamol/albuterol to use as rescue medication throughout the study along with e-Diary to record rescue medication use. Rescue medication free days is defined as any day where the participant did not use any puffs of rescue medication during daytime and night-time. (NCT02554786)
Timeframe: Up to Weeks 26 and 52

,,,,
Interventionpercentage of days (Least Squares Mean)
Weeks 1-26Weeks 1-52
MF 400 μg19.120.8
MF 800 μg21.423.5
QMF149 150/160 μg27.429.4
QMF149 150/320 μg31.533.1
Salmeterol /Fluticasone 50/500 μg27.428.8

[back to top]

Rescue Medication Usage

All participants were given salbutamol/albuterol to use as rescue medication throughout the study along with e-Diary to record rescue medication use. The number of puffs of rescue medication during the past 12 hours is recorded twice (morning/evening) by the participant prior to taking study medication. The mean daily number of puffs of rescue medication use will be calculated for each participant, done separately for morning (night-time), evening (daytime), and daily (night-time plus daytime) rescue medication use (NCT02554786)
Timeframe: Up to Weeks 26 and 52

,,,,
Interventionnumber of puffs (Least Squares Mean)
Week1-26 Mean night-time number of puffsWeek1-26 Mean daytime number of puffsWeek1-26 Mean daily number of puffsWeek1-52 Mean night-time number of puffsWeek 1-52 Mean daytime number of puffsWeek 1-52 Mean daily number of puffs
MF 400 μg-0.19-0.34-0.53-0.20-0.36-0.56
MF 800 μg-0.26-0.38-0.65-0.29-0.43-0.72
QMF149 150/160 μg-0.27-0.46-0.73-0.30-0.51-0.80
QMF149 150/320 μg-0.38-0.57-0.96-0.40-0.60-1.00
Salmeterol/Fluticasone 50/500 μg-0.34-0.53-0.87-0.35-0.55-0.91

[back to top]

Duration in Days of Asthma Exacerbations by Exacerbation Category

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02554786)
Timeframe: Up to Week 52

,,,,
Interventiondays (Mean)
Moderate or severe asthma exacerbationSevere asthma exacerbationAll(mild, moderate,severe) asthma exacerbation
MF 400 μg5.83.210.1
MF 800 μg3.71.76.9
QMF149 150/160 μg3.01.75.0
QMF149 150/320 μg2.61.35.4
Salmeterol/Fluticasone 50/500 μg3.11.95.1

[back to top]

Change From Baseline in Percentage of Mornings With no Symptoms on Rising Over 52 Weeks

"All participants were provided with an electronic diary (e-Diary) to record clinical symptoms. They were instructed to routinely complete the e-Diary twice daily at the same time each morning and again approximately 12 hours later in the evening. The e-Diary was reviewed at each visit until study completion. The question asked for nights with no night-time awakenings was How did you sleep last night? had to be answered with I did not wake up because of any breathing problems with scores from 0 (no problem)-4 (very severe problems)." (NCT02571777)
Timeframe: Baseline, 52 weeks

InterventionPercentage of days (Least Squares Mean)
QVM149 150/50/160 µg o.d.19.5
QVM149 150/50/80 µg o.d.18.5
QMF149 150/320 µg o.d.19.9
QMF149 150/160 µg o.d.15.5
Salmeterol/Fluticasone 50/500 μg b.i.d.15.6

[back to top]

Pre-dose Forced Vital Capacity (FVC) at Week 4 and Week 12

Pre-dose FVC is defined as average of the two FVC measurements taken 45 min and 15 min pre evening dose. It was assessed by performing spirometric assessment. FVC is the total amount of air exhaled during the FEV test. (NCT02571777)
Timeframe: 4 weeks, 12 weeks

,,,,
Interventionlitre (L) (Least Squares Mean)
Week 4Week 12
QMF149 150/160 µg o.d.3.0203.014
QMF149 150/320 µg o.d.3.0183.011
QVM149 150/50/160 µg o.d.3.0913.067
QVM149 150/50/80 µg o.d.3.0593.065
Salmeterol/Fluticasone 50/500 μg b.i.d.2.9522.965

[back to top]

Time to First Asthma Exacerbation by Exacerbation Category

"Time from start of treatment until the first event (asthma exacerbation) or censoring. Patients without the event were considered as censored at the date of last treatment + 1 day. For patients having the event, the start date of the exacerbation was considered to calculate the time to event (i.e., the number of days from start of treatment up to the event start date).~The exacerbation categories were: All (mild, moderate and severe), combination of moderate or severe and severe." (NCT02571777)
Timeframe: 52 weeks on average, up to 416 days

,,,,
Interventiondays (Median)
Moderate or severe asthma exacerbationSevere asthma exacerbationAll (mild, moderate or severe) asthma exacerbation
QMF149 150/160 µg o.d.365.0366.0360.0
QMF149 150/320 µg o.d.366.0366.0361.0
QVM149 150/50/160 µg o.d.366.0366.0363.0
QVM149 150/50/80 µg o.d.366.0366.0364.0
Salmeterol/Fluticasone 50/500 μg b.i.d.365.0366.0278.0

[back to top]

Percentage of Patients Achieving the Minimal Clinically Important Difference (MCID) ACQ ≥ 0.5 at Week 26 and Week 52

Change from baseline in ACQ-7 scores of ≤ 0.5 was defined as minimal clinically important difference and were considered clinically meaningful. The ACQ-7 measured asthma symptom control and consists of 7 items: 5 on symptom assessment, 1 on rescue bronchodilator use and 1 on airway calibre (FEV1 % predicted). All 7 questions of the ACQ-7 were equally weighted. Items 1-5 were scored along a 7-point response scale, where 0 = totally controlled and 6 = severely uncontrolled. Item 6 is scored between 0 = no rescue medication and 6 = More than 16 puffs/inhalations most days. The 7th item was scored by the investigator based on the FEV1 % predicted from the masterscope at the site (i.e., Score = 0 means > 95% of predicted FEV1, 1 = 90 - 95%, 2 = 80 - 89%, 3 = 70 - 79%, 4 = 60 - 69%, 5 = 50 - 59%, and Score = 6 means < 50% of predicted FEV1). The total score was calculated as the mean of all questions. (NCT02571777)
Timeframe: 26 weeks, 52 weeks

,,,,
InterventionPercentage of participants (Number)
Week 26Week 52
QMF149 150/160 µg o.d.70.773.1
QMF149 150/320 µg o.d.74.277.9
QVM149 150/50/160 µg o.d.71.278.8
QVM149 150/50/80 µg o.d.71.772.8
Salmeterol/Fluticasone 50/500 μg b.i.d.67.472.8

[back to top]

Pre-dose FEV1 at Weeks 4 and 12

Pre-dose FEV1 is defined as average of the two FEV1 measurements taken 45 min and 15 min pre evening dose. It was assessed by performing spirometric assessment. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. (NCT02571777)
Timeframe: 4 weeks, 12 weeks

,,,,
Interventionlitres (Least Squares Mean)
Week 4Week 12
QMF149 150/160 µg o.d.1.9501.944
QMF149 150/320 µg o.d.1.9631.966
QVM149 150/50/160 µg o.d.2.0322.024
QVM149 150/50/80 µg o.d.1.9831.994
Salmeterol/Fluticasone 50/500 μg b.i.d.1.8871.907

[back to top]

Asthma Quality of Life Questionnaire (AQLQ) at Week 52

"AQLQ is a 32-item disease specific questionnaire designed to measure functional impairments that are most important to patients with asthma, with a recall time of two weeks and each question to be answered on a 7-point scale (1-totally limited/problems all the time, 7-not at all limited/no problems). It consists of 4 domains:~Symptoms = Mean of Items 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 29, 30 (12 items)~Activity limitation = Mean of Items 1, 2, 3, 4, 5, 11, 19, 25, 28, 31, 32 (11 items)~Emotional function = Mean of Items 7, 13, 15, 21, 27 (5 items)~Environmental stimuli = Mean of Items 9, 17, 23, 26 (4 items)~Overall Score = Mean of Items 1 to 32 (32 items) The overall AQLQ score reported below is the mean of all 32 responses and ranges from 1 to 7, where higher scores indicate better quality of life." (NCT02571777)
Timeframe: 52 weeks

InterventionScore on a scale (Least Squares Mean)
QVM149 150/50/160 µg o.d.5.555
QVM149 150/50/80 µg o.d.5.445
QMF149 150/320 µg o.d.5.535
QMF149 150/160 µg o.d.5.499
Salmeterol/Fluticasone 50/500 μg b.i.d.5.495

[back to top]

Change From Baseline in Percentage of Days With no Daytime Symptoms Over 52 Weeks

All participants were provided with an electronic diary (e-Diary) to record clinical symptoms. They were instructed to routinely complete the e-Diary twice daily at the same time each morning and again approximately 12 hours later in the evening. The e-Diary was reviewed at each visit until study completion. For days with no daytime symptoms, all 5 evening questions must have a score = 0 with respect to shortness of breath, wheeze, cough, chest tightness and impact on usual daily activities due to symptoms, each with scores from 0 (no problems) to 4 (very severe problems). (NCT02571777)
Timeframe: Baseline, 52 weeks

InterventionPercentage of days (Least Squares Mean)
QVM149 150/50/160 µg o.d.22.5
QVM149 150/50/80 µg o.d.17.9
QMF149 150/320 µg o.d.21.8
QMF149 150/160 µg o.d.18.0
Salmeterol/Fluticasone 50/500 μg b.i.d.18.8

[back to top]

Total Amount of Oral Corticosteroid Used (in Prednisone-equivalent mg Doses) to Treat Asthma Exacerbations

The treatment of asthma exacerbations including the initiation of systemic corticosteroids were done according to investigator's or treating physician's medical judgement and in line with national and international recommendations. If systemic corticosteroids were required, a participant could return to the study after successfully completing a taper of approximately 7-10 days. (NCT02571777)
Timeframe: Up to Week 52

Interventionprednisone-equivalent milligram (Mean)
QVM149 150/50/160 µg o.d.53.4
QVM149 150/50/80 µg o.d.72.0
QMF149 150/320 µg o.d.73.2
QMF149 150/160 µg o.d.82.5
Salmeterol/Fluticasone 50/500 μg b.i.d.86.0

[back to top]

Percentage of Participants With at Least One Asthma Exacerbation by Exacerbation Category

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02571777)
Timeframe: Up to Week 52

,,,,
Interventionpercentage of participants (Number)
Moderate or severe asthma exacerbationSevere asthma exacerbationAll (mild, moderate, severe) asthma exacerbation
QMF149 150/160 µg o.d.35.927.344.0
QMF149 150/320 µg o.d.31.823.241.9
QVM149 150/50/160 µg o.d.30.221.840.2
QVM149 150/50/80 µg o.d.32.524.640.2
Salmeterol/Fluticasone 50/500 μg b.i.d.39.729.750.5

[back to top]

Trough FEV1 at Week 52

Trough FEV1 was assessed by performing spirometric assessment. It is defined as average of the two FEV1 measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. (NCT02571777)
Timeframe: 52 weeks

Interventionlitre (L) (Least Squares Mean)
QVM149 150/50/160 µg o.d.2.050
QVM149 150/50/80 µg o.d.1.992
QMF149 150/320 µg o.d.1.965
QMF149 150/160 µg o.d.1.930
Salmeterol/Fluticasone 50/500 μg b.i.d.1.905

[back to top]

Change From Baseline in Percentage of Nights With no Night-time Awakenings Over 52 Weeks

"All participants were provided with an electronic diary (e-Diary) to record clinical symptoms. They were instructed to routinely complete the e-Diary twice daily at the same time each morning and again approximately 12 hours later in the evening. The e-Diary was reviewed at each visit until study completion. The question asked for nights with no night-time awakenings was How did you sleep last night? had to be answered with I did not wake up because of any breathing problems with scores from 0 (no problem)-4 (very severe problems)." (NCT02571777)
Timeframe: Baseline, 52 weeks

InterventionPercentage of days (Least Squares Mean)
QVM149 150/50/160 µg o.d.18.0
QVM149 150/50/80 µg o.d.17.6
QMF149 150/320 µg o.d.18.4
QMF149 150/160 µg o.d.16.1
Salmeterol/Fluticasone 50/500 μg b.i.d.16.9

[back to top]

Percentage of Participants With Composite Endpoint of Serious Asthma Outcomes

A composite endpoint of serious asthma outcomes is defined as asthma-related hospitalization, asthma-related intubation, or asthma-related death and was reviewed by the Adjudication Committee. (NCT02571777)
Timeframe: Up to Week 52

InterventionPercentage of participants (Number)
QVM149 150/50/160 µg o.d.1.4
QVM149 150/50/80 µg o.d.2.5
QMF149 150/320 µg o.d.1.9
QMF149 150/160 µg o.d.1.6
Salmeterol/Fluticasone 50/500 μg b.i.d.1.2

[back to top]

Time in Days to Permanent Discontinuation of Study Medication Due to Asthma Exacerbation

Time from start of treatment until the first event (permanent discontinuation of study medication due to asthma exacerbation) or censoring. Patients without the event were considered as censored at the date of last treatment + 1 day. For patients having the event, the date of the discontinuation of study medication was considered to calculate the time to event. (NCT02571777)
Timeframe: 52 weeks on average, up to 416 days

Interventiondays (Median)
QVM149 150/50/160 µg o.d.367.0
QVM149 150/50/80 µg o.d.367.0
QMF149 150/320 µg o.d.367.0
QMF149 150/160 µg o.d.367.0
Salmeterol/Fluticasone 50/500 μg b.i.d.367.0

[back to top]

Trough Forced Expiratory Flow (FEF) Between 25% and 75% of FVC (FEF25-75) at 52 Weeks

FEF is the flow (or speed) of air coming out of the lung during the middle portion of a forced expiration. Trough FEF25-75% is defined as average of the two FEF25-75% measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. It was assessed by performing spirometric assessment. (NCT02571777)
Timeframe: Up to Week 52

InterventionL/s (Least Squares Mean)
QVM149 150/50/160 µg o.d.1.354
QVM149 150/50/80 µg o.d.1.263
QMF149 150/320 µg o.d.1.260
QMF149 150/160 µg o.d.1.214
Salmeterol/Fluticasone 50/500 μg b.i.d.1.207

[back to top]

Trough Forced Expiratory Volume in 1 Second (Trough FEV1) of QVM149 Versus QMF149 at Week 26

"Trough FEV1 was assessed by performing spirometric assessment. It is defined as average of the two FEV1 measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing.~The primary endpoint considered the following 2 comparison groups:~QVM149 150/50/80 μg o.d. compared with QMF149 150/160 μg o.d. both delivered via Concept1~QVM149 150/50/160 μg o.d. compared with QMF149 150/320 μg o.d. both delivered via Concept1." (NCT02571777)
Timeframe: 26 weeks

Interventionlitre (L) (Least Squares Mean)
QVM149 150/50/160 µg o.d.2.050
QVM149 150/50/80 µg o.d.2.029
QMF149 150/320 µg o.d.1.984
QMF149 150/160 µg o.d.1.953
Salmeterol/Fluticasone 50/500 μg b.i.d.1.930

[back to top]

Trough Forced Expiratory Volume in 1 Second (Trough FEV1) of QVM149 Versus Salmeterol/Fluticasone at Week 26

"Trough FEV1 was assessed by performing spirometric assessment. It is defined as average of the two FEV1 measurements taken 23 hr 15 min and 23 hr 45 min post-evening dose. FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing.~This secondary endpoint considered the following 2 comparison groups:~QVM149 150/50/80 μg o.d. via Concept1 compared with salmeterol/fluticasone 50/500 μg b.i.d. via Accuhaler®~QVM149 150/50/160 μg o.d. via Concept 1 compared with salmeterol/fluticasone 50/500 μg b.i.d. via Accuhaler®" (NCT02571777)
Timeframe: 26 weeks

Interventionlitre (L) (Least Squares Mean)
QVM149 150/50/160 µg o.d.2.050
QVM149 150/50/80 µg o.d.2.029
QMF149 150/320 µg o.d.1.984
QMF149 150/160 µg o.d.1.953
Salmeterol/Fluticasone 50/500 μg b.i.d.1.930

[back to top]

Annual Rate of Asthma Exacerbations by Exacerbation Category

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02571777)
Timeframe: 52 weeks

,,,,
InterventionExacerbations per year (Mean)
Moderate or severe asthma exacerbationSevere asthma exacerbationAll (mild, moderate, severe) asthma exacerbation
QMF149 150/160 µg o.d.0.670.410.98
QMF149 150/320 µg o.d.0.540.330.93
QVM149 150/50/160 µg o.d.0.460.260.74
QVM149 150/50/80 µg o.d.0.580.380.86
Salmeterol/Fluticasone 50/500 μg b.i.d.0.720.451.23

[back to top]

Time to First Hospitalization for Asthma Exacerbation

Time from start of treatment until the first event (hospitalization for asthma exacerbation) or censoring. Patients without the event were considered as censored at the date of last treatment + 1 day. For patients having the event, the start date of the hospitalization was considered to calculate the time to event (i.e., the number of days from start of treatment up to the event start date). (NCT02571777)
Timeframe: 52 weeks on average, up to 416 days

Interventiondays (Median)
QVM149 150/50/160 µg o.d.367.0
QVM149 150/50/80 µg o.d.367.0
QMF149 150/320 µg o.d.367.0
QMF149 150/160 µg o.d.367.0
Salmeterol/Fluticasone 50/500 μg b.i.d.367.0

[back to top]

Change From Baseline in Percentage of Asthma Symptom-free Days Over 52 Weeks

All participants were provided with an electronic diary (e-Diary) to record clinical symptoms. They were instructed to routinely complete the e-Diary twice daily at the same time each morning and again approximately 12 hours later in the evening. The e-Diary was reviewed at each visit until study completion. Asthma symptoms free days are days with no daytime symptoms, no night-time awakenings and no symptoms on awakening. The daytime asthma symptom score was based on the daily e-diary recordings by participants with respect to shortness of breath, wheeze, cough, chest tightness, and impact on usual daily activities due to symptoms. (NCT02571777)
Timeframe: Baseline, 52 weeks

InterventionPercentage of days (Least Squares Mean)
QVM149 150/50/160 µg o.d.22.4
QVM149 150/50/80 µg o.d.18.0
QMF149 150/320 µg o.d.22.2
QMF149 150/160 µg o.d.18.0
Salmeterol/Fluticasone 50/500 μg b.i.d.18.9

[back to top]

Asthma Control Questionnaire (ACQ-7) at Week 26 and Week 52

The ACQ-7 measured asthma symptom control and consists of 7 items: 5 on symptom assessment, 1 on rescue bronchodilator use and 1 on airway calibre (FEV1 % predicted). All 7 questions of the ACQ-7 were equally weighted. Items 1-5 were scored along a 7-point response scale, where 0 = totally controlled and 6 = severely uncontrolled. Item 6 is scored between 0 = no rescue medication and 6 = More than 16 puffs/inhalations most days. The 7th item was scored by the investigator based on the FEV1 % predicted from the masterscope at the site (i.e., Score = 0 means > 95% of predicted FEV1, 1 = 90 - 95%, 2 = 80 - 89%, 3 = 70 - 79%, 4 = 60 - 69%, 5 = 50 - 59%, and Score = 6 means < 50% of predicted FEV1). The ACQ-7 total score reported below was calculated as the mean of scores of all 7 items and ranged between 0 and 6, with higher scores indicating worse asthma symptom control. (NCT02571777)
Timeframe: 26 weeks, 52 weeks

,,,,
InterventionScore on a scale (Least Squares Mean)
Week 26Week 52
QMF149 150/160 µg o.d.1.6141.545
QMF149 150/320 µg o.d.1.5281.465
QVM149 150/50/160 µg o.d.1.5421.406
QVM149 150/50/80 µg o.d.1.5431.535
Salmeterol/Fluticasone 50/500 μg b.i.d.1.6281.527

[back to top]

Change From Baseline in Morning and Evening Peak Expiratory Flow Rate (PEF) Over 26 and 52 Weeks of Treatment

PEF is a person's maximum speed of expiration. All the participants were instructed to record PEF twice daily using a mini Peak Flow Meter device, once in the morning (before taking the morning dose) and once approximately 12 h later in the evening (before taking the evening dose) at home. At each timepoint, the participant was instructed to perform 3 consecutive manoeuvres within 10 minutes. These PEF values were captured in the e-PEF/diary. The best of 3 values were used. (NCT02571777)
Timeframe: Baseline, 26 weeks, 52 weeks

,,,,
InterventionL/min (Least Squares Mean)
Week 26 - Mean morning PEFWeek 26 - Mean evening PEFWeek 52 - Mean morning PEFWeek 52 - Mean evening PEF
QMF149 150/160 µg o.d.25.620.625.620.1
QMF149 150/320 µg o.d.29.522.828.821.2
QVM149 150/50/160 µg o.d.47.739.647.538.7
QVM149 150/50/80 µg o.d.40.534.741.235.0
Salmeterol/Fluticasone 50/500 μg b.i.d.12.510.412.79.2

[back to top]

Change From Baseline in Percentage of Days Without Rescue Medication Use Over 26 and 52 Weeks

Percentage of days without rescue medication usage (100 μg salbutamol/90 μg albuterol via metered-dose inhaler) as recorded by e-diary over 26 and 52 weeks of treatment. (NCT02571777)
Timeframe: Baseline, 26 weeks, 52 weeks

,,,,
InterventionPercentage of days (Least Squares Mean)
Week 26Week 52
QMF149 150/160 µg o.d.18.220.8
QMF149 150/320 µg o.d.23.324.9
QVM149 150/50/160 µg o.d.22.525.0
QVM149 150/50/80 µg o.d.19.521.9
Salmeterol/Fluticasone 50/500 μg b.i.d.19.621.8

[back to top]

Change From Baseline in Percentage of Rescue Medication Free Days Over 26 and 52 Weeks

All participants were given salbutamol/albuterol to use as rescue medication throughout the study along with e-Diary to record rescue medication use. Rescue medication free days is defined as any day where the participant did not use any puffs of rescue medication during daytime and night-time. (NCT02571777)
Timeframe: Baseline, 26 weeks, 52 weeks

,,,,
InterventionPercentage of days (Least Squares Mean)
Week 26Week 52
QMF149 150/160 µg o.d.18.220.8
QMF149 150/320 µg o.d.23.324.9
QVM149 150/50/160 µg o.d.22.525.0
QVM149 150/50/80 µg o.d.19.521.9
Salmeterol/Fluticasone 50/500 μg b.i.d.19.621.8

[back to top]

Duration in Days of Asthma Exacerbations by Exacerbation Category

The exacerbation categories were: All (mild, moderate and severe) and combination of moderate or severe and severe. (NCT02571777)
Timeframe: Up to Week 52

,,,,
Interventiondays (Mean)
Moderate or severe asthma exacerbationSevere asthma exacerbationAll (mild, moderate, severe) asthma exacerbation
QMF149 150/160 µg o.d.7.14.59.6
QMF149 150/320 µg o.d.6.74.910.7
QVM149 150/50/160 µg o.d.4.52.87.0
QVM149 150/50/80 µg o.d.5.64.18.1
Salmeterol/Fluticasone 50/500 μg b.i.d.8.15.812.8

[back to top]

Change From Baseline in T-Helper Lymphocytes Count in the Bronchial Submucosa at Week 12

T-helper i.e. CD4 positive lymphocytes were counted in the bronchial submucosa of biopsy thin sections using quantitative immunohistochemistry and reported as the number of cells per square millimeter. (NCT02573233)
Timeframe: Baseline, Week 12

Interventioncells/mm^2 (Median)
Placebo7.26
Dupilumab62.34

[back to top]

Change From Baseline in T-Lymphocytes Count in the Bronchial Submucosa at Week 12

T-Lymphocytes i.e. CD3 positive cells were counted in the bronchial submucosa of biopsy thin sections using quantitative immunohistochemistry and reported as the number of cells per square millimeter. (NCT02573233)
Timeframe: Baseline, Week 12

Interventioncells/mm^2 (Median)
Placebo-36.70
Dupilumab34.21

[back to top]

Pharmacokinetics (PK) Assessment: Serum Functional Dupilumab Concentration

Serum functional dupilumab concentrations were determined using an enzyme-linked immunosorbent assay (ELISA) method. (NCT02573233)
Timeframe: Week 0, Week 2, 6, 8, 12, 18, End of study (Week 24)

Interventionng/mL (Mean)
Week 0Week 2Week 6Week 8Week 12Week 18Week 24
Dupilumab0.0052675.0059969.0061097.9567387.0020728.171851.20

[back to top]

Number of Participants With Treatment Emergent Adverse Events (TEAEs)

Adverse event (AE) was defined as any untoward medical occurrence in a participant who received investigational medicinal product (IMP) without regard to possibility of causal relationship with this treatment. TEAEs: AEs that developed or worsened or became serious during between the first administration of study medication to the end of the 12 week Post-treatment Period. Serious adverse event (SAE) was defined as any untoward medical occurrence that resulted in any of the following outcomes: death, life-threatening, required initial or prolonged in-patient hospitalization, persistent or significant disability/incapacity, congenital anomaly/birth defect, or considered as medically important event. Any TEAE included both serious and non-serious AEs. (NCT02573233)
Timeframe: Baseline up to Week 24

,
InterventionParticipants (Count of Participants)
Any TEAEAny treatment emergent SAEAny TEAE leading to deathAny TEAE leading to permanent discontinuation
Dupilumab15100
Placebo17000

[back to top]

Number of Participants With Antidrug Antibodies (ADA)

Anti-drug antibodies were detected using a validated immunoassay. Incidence of ADA were classified as following: 1) Pre-existing immunoreactivity - an ADA positive response in the assay at baseline with all post treatment ADA results negative or an ADA positive response at baseline with all post treatment ADA responses less than 4-fold over baseline titer levels. 2) Treatment-emergent ADA: an ADA positive response in the assay post first dose, when baseline results were negative or missing. 3) Treatment-boosted ADA: an ADA positive response in the assay post first dose that was greater-than or equal to 4-fold over baseline titer levels, when baseline results were positive. (NCT02573233)
Timeframe: From Baseline up to 24 weeks

,
InterventionParticipants (Count of Participants)
With pre-existing immunoreactivityWith treatment-emergent ADAWith treatment-boosted ADA
Dupilumab010
Placebo100

[back to top]

Average Change in Fractional Exhaled Nitric Oxide (FeNO) From Baseline to Week 6 Through Week 12

"FeNO is a surrogate marker for airway inflammation. FeNO was analyzed using a NIOX instrument or similar analyzer using a flow rate of 50 mL/s, and reported in ppb.~The average change in FeNO from baseline to Week 6 through Week 12 was calculated as follows: For each participant the change in FeNO from Baseline to Week 6, Week 8, Week 10 and Week 12 was calculated (value at Week X - value at baseline). Subsequently the weekly mean of these 4 change from baseline values was determined (Weeks 6, 8, 10 and 12). Using these weekly mean values the overall arithmetic mean and standard deviation of the average change in FeNO from baseline to Week 6 through Week 12 was calculated." (NCT02573233)
Timeframe: From Baseline to Week 6 through Week 12

Interventionppb (Mean)
Placebo3.5
Dupilumab-16.0

[back to top]

Change From Baseline in Eosinophils Cells Count in the Bronchial Submucosa at Week 12

Inflammatory cells i.e. eosinophils were counted in the bronchial submucosa of biopsy thin sections using quantitative immunohistochemistry and reported as the number of cells per square millimeter. (NCT02573233)
Timeframe: Baseline, Week 12

Interventioncells/mm^2 (Median)
Placebo5.80
Dupilumab-6.04

[back to top]

Change From Baseline in Fractional Exhaled Nitric Oxide (FeNO) at Week 12

FeNO is a surrogate marker for airway inflammation. FeNO was analyzed using a NIOX instrument or similar analyzer using a flow rate of 50 mL/second, and reported in ppb. (NCT02573233)
Timeframe: Baseline, Week 12

Interventionppb (Mean)
Placebo3.9
Dupilumab-15.1

[back to top]

Change From Baseline in Mast Cells Count (Chymase Positive) in the Bronchial Submucosa at Week 12

Inflammatory cells i.e. mast cells were counted in the bronchial submucosa of biopsy thin sections using quantitative immunohistochemistry and reported as the number of cells per square millimeter. (NCT02573233)
Timeframe: Baseline, Week 12

Interventioncells/mm^2 (Mean)
Placebo-14.80
Dupilumab1.76

[back to top]

Change From Baseline in Mast Cells Count (Tryptase Positive) in the Bronchial Submucosa at Week 12

Inflammatory cells i.e. mast cells were counted in the bronchial submucosa of biopsy thin sections using quantitative immunohistochemistry and reported as the number of cells per square millimeter. (NCT02573233)
Timeframe: Baseline, Week 12

Interventioncells/mm^2 (Mean)
Placebo2.37
Dupilumab-20.89

[back to top]

Change From Baseline in Mucin-Stained Area in the Bronchial Submucosa at Week 12

Mucin was identified by staining with Alcian-blue periodic acid-Schiff and/or immunostaining for MUC5AC and then the mucin-positive area was measured and expressed per square millimeter. (NCT02573233)
Timeframe: Baseline, Week 12

Interventioncells/mm^2 (Mean)
Placebo64.09
Dupilumab-142.74

[back to top]

Transition Dyspnea Index (TDI) Score

Transitional Dyspnea Index (TDI) score presents the degree of impairment due to dyspnea. The lower the score the worse the severity of dyspnea. The Baseline Dyspnea Index (BDI) / TDI is an instrument used to assess a participant's level of dyspnea. The BDI and TDI each have three domains: functional impairment, magnitude of task and magnitude of effort. BDI domains were rated from 0 (severe) to 4 (unimpaired) and rates summed for baseline focal score ranged from 0 to 12; lower scores mean worse severity. TDI domains were rated from -3 (major deterioration) to 3 (major improvement) and rates summed for transition focal score ranged from -9 to 9; negative scores indicate deterioration. A TDI focal score of ≥1 was defined as a clinically important improvement from baseline. (NCT02603393)
Timeframe: 12 weeks

InterventionScore on a scale (Least Squares Mean)
QVA1491.177
Tiotropium + Salmeterol/Fluticasone1.418

[back to top]

Mean Change From Baseline in St. George's Respiratory Questionnaire

"The St. George Respiratory Questionnaire C (SGRQ-C) is used to provide the health status measurements in this study. Baseline SGRQ-C is defined as the assessment taken right before the first dose of the double-blind drug on Day 1. Higher values correspond to greater impairment of health status. The SGRQ contains 50 items divided into 2 parts covering 3 aspects of health related to COPD: Part I covers Symptoms and is concerned with respiratory symptoms, their frequency and severity; Part II covers Activity and is concerned with activities that cause or are limited by breathlessness; Part II is also concerned with Impacts, which covers a range of aspects concerned with social functioning and psychological disturbances resulting from airways disease. A score was calculated for each of these 3 subscales and a Total score was calculated. In each case the lowest possible value is zero and the highest 100. Higher values correspond to greater impairment of health status." (NCT02603393)
Timeframe: Baseline, 26 weeks

InterventionScore on a scale (Least Squares Mean)
QVA149-1.0
Tiotropium + Salmeterol/Fluticasone-2.5

[back to top]

Mean Change From Baseline in St. George's Respiratory Questionnaire

"The St. George Respiratory Questionnaire C (SGRQ-C) is used to provide the health status measurements in this study. Baseline SGRQ-C is defined as the assessment taken right before the first dose of the double-blind drug on Day 1. Higher values correspond to greater impairment of health status. The SGRQ contains 50 items divided into 2 parts covering 3 aspects of health related to COPD: Part I covers Symptoms and is concerned with respiratory symptoms, their frequency and severity; Part II covers Activity and is concerned with activities that cause or are limited by breathlessness; Part II is also concerned with Impacts, which covers a range of aspects concerned with social functioning and psychological disturbances resulting from airways disease. A score was calculated for each of these 3 subscales and a Total score was calculated. In each case the lowest possible value is zero and the highest 100. Higher values correspond to greater impairment of health status." (NCT02603393)
Timeframe: Baseline, 12 weeks

InterventionScore on a scale (Least Squares Mean)
QVA149-0.7
Tiotropium + Salmeterol/Fluticasone-2.5

[back to top]

Mean Change From Baseline in Post-dose Trough FEV1

Mean change from baseline in post-dose trough forced expiratory volume in 1 second (FEV1) following 26 weeks of treatment. Trough FEV1 is defined as the mean of the two FEV1 values measured at 23 hr 15 min and 23 hr 45 min after the morning dose taken at site on Day 181. Baseline FEV1 is defined as the average of the pre-dose FEV1 measured at -45 min and -15 min at Day 1. (NCT02603393)
Timeframe: Baseline, 26 weeks

InterventionLiters (Least Squares Mean)
QVA149-0.029
Tiotropium + Salmeterol/Fluticasone-0.003

[back to top]

Mean Change From Baseline in Pre-dose Trough FEV1

Trough FEV1 is defined as the average of the pre-dose FEV1 measurements at -45 min and -15 min prior to dosing at each visit except Day 182 which is the average of the post-dose FEV1 measurements at 23h15min and 23h45min after dosing at Day 181. Baseline FEV1 is considered the Day 1 average of pre-dose measurements. (NCT02603393)
Timeframe: 26 weeks

InterventionLiters (Least Squares Mean)
QVA149-0.029
Tiotropium + Salmeterol/Fluticasone-0.003

[back to top]

Mean Change From Baseline in Forced Vital Capacity (FVC)

Change from baseline in forced vital capacity following 26 weeks of treatment. Trough FVC is defined as the average of the pre-dose FVC measurements at -45 min and -15 min prior to dosing at each visit except Day 182 which is the average of the post-dose FVC measurements at 23h15min and 23h45min after dosing at Day 181. Baseline is considered the Day 1 average of pre-dose measurements. (NCT02603393)
Timeframe: Baseline, 26 weeks

InterventionLiters (Least Squares Mean)
QVA149-0.030
Tiotropium + Salmeterol/Fluticasone-0.048

[back to top]

Change From Baseline in the Mean Daily Number of Puffs of Rescue Medication

Change from baseline in mean daily number of puffs of rescue medication (number of puffs taken in the previous 12 hours) over 26 weeks of treatment. (NCT02603393)
Timeframe: Baseline, 26 weeks

InterventionNumber of puffs per day (Least Squares Mean)
QVA149-0.307
Tiotropium + Salmeterol/Fluticasone-0.484

[back to top]

Annualized Rate of Moderate or Severe COPD Exacerbations

Moderate or severe COPD exacerbations starting between first dose and one day after last treatment are included. COPD exacerbations that occurred within 7 days of each other are collapsed as one event. (NCT02603393)
Timeframe: 26 weeks

InterventionCOPD exacerbations/year (Number)
QVA1490.52
Tiotropium + Salmeterol/Fluticasone0.48

[back to top]

Annualized Rate of COPD Exacerbations Requiring Treatment With Systemic Glucocorticosteroids and/or Antibiotics, Moderate Exacerbations Only

COPD exacerbations starting between first dose and one day after last treatment are included. COPD exacerbations that occurred within 7 days of each other are collapsed as one event (NCT02603393)
Timeframe: 26 weeks

InterventionCOPD Exacerbations/year (Number)
QVA1490.47
Tiotropium + Salmeterol/Fluticasone0.44

[back to top]

Annualized Rate of COPD Exacerbations Requiring Hospitalisation

COPD exacerbations starting between first dose and one day after last treatment are included. COPD exacerbations that occurred within 7 days of each other are collapsed as one event. (NCT02603393)
Timeframe: 26 weeks

InterventionCOPD Exacerbations/year (Number)
QVA1490.001
Tiotropium + Salmeterol/Fluticasone0.001

[back to top]

Transition Dyspnea Index (TDI) Score

Transitional Dyspnea Index (TDI) score presents the degree of impairment due to dyspnea. The lower the score the worse the severity of dyspnea. The Baseline Dyspnea Index (BDI) / TDI is an instrument used to assess a participant's level of dyspnea. The BDI and TDI each have three domains: functional impairment, magnitude of task and magnitude of effort. BDI domains were rated from 0 (severe) to 4 (unimpaired) and rates summed for baseline focal score ranged from 0 to 12; lower scores mean worse severity. TDI domains were rated from -3 (major deterioration) to 3 (major improvement) and rates summed for transition focal score ranged from -9 to 9; negative scores indicate deterioration. A TDI focal score of ≥1 was defined as a clinically important improvement from baseline. (NCT02603393)
Timeframe: 26 weeks

InterventionScore on a scale (Least Squares Mean)
QVA1491.382
Tiotropium + Salmeterol/Fluticasone1.671

[back to top]

Mean Change From Baseline in Trough Forced Expiratory Volume in 1 Second (FEV1) at Week 24

FEV1 is a measure of lung function and is defined as the maximal volume of air that can be forcefully exhaled in one second. Trough FEV1 on treatment is defined as the highest FEV1 value obtained prior to the morning dose of investigational product. Baseline value is the last acceptable/borderline acceptable pre-dose FEV1 prior to randomized treatment start date (pre-dose at Day 1). Change from Baseline value is the value at Week 24 minus the Baseline value. Intent-to-Treat (ITT) Population comprised of all randomized participants, excluding those who were randomized in error, who did not receive the study drug. Treatment policy estimand was assessed, including all on- and post-treatment data. Different participants may have been analyzed at different time points; thus, overall number of participants analyzed reflects everyone in ITT Population without missing covariate information, with Baseline and at least one post-baseline measurement. Mixed Model Repeated Measures(MMRM) was used. (NCT02924688)
Timeframe: Baseline (pre-dose at Day 1) and Week 24

InterventionLiters (Least Squares Mean)
FF/VI 100/25 mcg0.024
FF/UMEC/VI 100/ 31.25/25 mcg0.120
FF/UMEC/VI 100/62.5/25 mcg0.134
FF/VI 200/25 mcg0.076
FF/UMEC/VI 200/ 31.25/25 mcg0.157
FF/UMEC/VI 200/62.5/25 mcg0.168

[back to top]

Mean Change From Baseline in Saint George's Respiratory Questionnaire (SGRQ) Total Score at Week 24

The SGRQ had 50 questions (scored from 0 to 100 where 0 indicates best and 100 indicates worst health) designed to measure quality of life (QoL) of participants with airway obstruction, measuring symptoms, impact, and activity. The questions are designed to be self-completed by the participant with a recall over the past 3 months. SGRQ total score was calculated by summing the pre-assigned weights of answers, dividing by the sum of the maximum weights for items in SGRQ and multiplying by 100. SGRQ total score ranges from 0 to 100 where 0 indicates best and 100 indicates worst health. A change of 4 points is considered a clinically relevant change. Treatment policy estimand was assessed, including all on- and post-treatment data. Baseline value was at randomization visit (pre-dose at Day 1). Change from Baseline value is the value at Week 24 minus the Baseline value. (NCT02924688)
Timeframe: Baseline (pre-dose at Day 1) and Week 24

InterventionScores on a scale (Least Squares Mean)
FF/VI-11.39
FF/UMEC/VI (UMEC 31.25 mcg)-10.29
FF/UMEC/VI (UMEC 62.5 mcg)-11.69

[back to top]

Mean Change From Baseline in Pulse Rate at Week 24

Pulse Rate was measured in the sitting position after approximately 5 minutes rest. Baseline value is the last acceptable/borderline acceptable value prior to randomized treatment start date (pre-dose at Day 1). Change from Baseline value is the value at the clinic visit minus the Baseline value. Different participants may have been analyzed at different time points; thus, overall number of participants analyzed reflects everyone in ITT Population without missing covariate information, with Baseline and at least one post-baseline measurement. (NCT02924688)
Timeframe: Baseline (pre-dose at Day 1) and Week 24

InterventionBeats per minute (Least Squares Mean)
FF/VI 100/25 mcg-1.1
FF/UMEC/VI 100/ 31.25/25 mcg0.2
FF/UMEC/VI 100/62.5/25 mcg-1.0
FF/VI 200/25 mcg-0.7
FF/UMEC/VI 200/ 31.25/25 mcg-1.3
FF/UMEC/VI 200/62.5/25 mcg-0.5

[back to top]

Mean Change From Baseline in Clinic FEV1 at 3 Hours Post Study Treatment at Week 24

FEV1 is a measure of lung function and is defined as the maximal volume of air that can be forcefully exhaled in one second. Baseline value is the last acceptable/borderline acceptable pre-dose FEV1 prior to randomized treatment start date (pre-dose at Day 1). Change from Baseline value is the value at Week 24 (recorded at 3 hours post dose) minus the Baseline value. (NCT02924688)
Timeframe: Baseline (pre-dose at Day 1) and 3 hours post dose at Week 24

InterventionLiters (Least Squares Mean)
FF/VI 100/25 mcg0.132
FF/UMEC/VI 100/ 31.25/25 mcg0.220
FF/UMEC/VI 100/62.5/25 mcg0.243
FF/VI 200/25 mcg0.168
FF/UMEC/VI 200/ 31.25/25 mcg0.256
FF/UMEC/VI 200/62.5/25 mcg0.286

[back to top]

Mean Change From Baseline in Asthma Control Questionnaire-7 (ACQ-7) Total Score at Week 24

The ACQ-7 consists of 7 attributes of asthma control, of which 6 to be self-completed by participant in a 6-item questionnaire, enquire about frequency and/or severity of symptoms over the previous week on: nocturnal awakening, symptoms on waking in the morning, activity limitation, shortness of breath, wheeze, and rescue medication use. The seventh attribute measures the lung function, which was included via pre-bronchodilator FEV1 % predicted value. All 7 items of ACQ have response on 0-6 ordinal scale (0=no impairment/limitation, 6=total impairment/limitation). The total score is calculated as the average of all non-missing item responses, ranges from 0 to 6. Higher score indicates worst symptoms. Treatment policy estimand was assessed, including all on- and post-treatment data. Baseline value was at randomization visit (pre-dose,Day 1). Change from Baseline was defined as value at Week 24 minus Baseline value. (NCT02924688)
Timeframe: Baseline (pre-dose at Day 1) and Week 24

InterventionScores on a scale (Least Squares Mean)
FF/VI-0.678
FF/UMEC/VI (UMEC 31.25 mcg)-0.734
FF/UMEC/VI (UMEC 62.5 mcg)-0.767

[back to top]

Annualized Rate of Moderate and Severe Asthma Exacerbations

A moderate asthma exacerbation is considered to be a deterioration in asthma symptoms or in lung function, or increased rescue bronchodilator use lasting for at least 2 days or more, but not be severe enough to warrant systemic corticosteroid use (or a doubling or more of the maintenance systemic corticosteroid dose, if applicable) for 3 days or more and/or hospitalization. It is an event that, when recognized, should result in a temporary change in treatment, to prevent it from becoming severe. A severe asthma exacerbation is defined as the deterioration of asthma requiring the use of systemic corticosteroids (tablets,suspension or injection), or an increase from a stable maintenance dose (For participants receiving maintenance systemic corticosteroids, at least double the maintenance systemic corticosteroid dose for at least 3 days is required), for at least 3 days or an inpatient hospitalization or emergency department visit because of asthma, requiring systemic corticosteroids. (NCT02924688)
Timeframe: Up to Week 52

InterventionExacerbations per year (Mean)
FF/VI0.70
FF/UMEC/VI (UMEC 31.25 mcg)0.68
FF/UMEC/VI (UMEC 62.5 mcg)0.61

[back to top]

Mean Change From Baseline in Evaluating Respiratory Symptoms (E-RS) Total Score Over Weeks 21 to 24 (Inclusive) of the Treatment Period

The E-RS in Chronic Obstructive Pulmonary Disease (COPD) consists of 11 items. E-RS captures information related to respiratory symptoms, i.e. breathlessness, cough, sputum production, chest congestion and chest tightness. The E-RS was completed daily and data was derived by 4-weekly intervals, requiring at least 50% of data to be present during a period. 7 items are scored from 0 (not at all) to 4 (extreme) and 4 items are scored from 0 (not at all) to 3 (extreme). The E-RS total score was calculated by taking sum of all the items. The E-RS total score has a scoring range of 0 to 40, with higher scores indicating more severe respiratory symptoms. Treatment policy estimand was assessed, including all on- and post-treatment data. Baseline value was the mean value of 14 days prior to randomization. Change from Baseline was calculated as post-baseline value (mean of daily E-RS total scores during Week 21 to 24 ) minus Baseline value. (NCT02924688)
Timeframe: Baseline (14 days prior to randomization) and Weeks 21 to 24

InterventionScores on a scale (Least Squares Mean)
FF/VI-2.47
FF/UMEC/VI (UMEC 31.25 mcg)-2.60
FF/UMEC/VI (UMEC 62.5 mcg)-2.89

[back to top]

Number of Participants With Any Serious Adverse Event (SAE) and Common (>=3%) Non-SAE

Adverse event (AE) is any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, events associated with liver injury and impaired liver function, or any other situation according to medical or scientific judgment were categorized as SAE. Number of participants with any SAE and common (>=3%) non-SAEs are presented. (NCT02924688)
Timeframe: Up to Week 52

,,,,,
InterventionParticipants (Count of Participants)
Common non-SAESAE
FF/UMEC/VI 100/ 31.25/25 mcg15018
FF/UMEC/VI 100/62.5/25 mcg13523
FF/UMEC/VI 200/ 31.25/25 mcg12723
FF/UMEC/VI 200/62.5/25 mcg12221
FF/VI 100/25 mcg13625
FF/VI 200/25 mcg12221

[back to top]

Number of Participants With Abnormal Hematology Values

Blood samples were collected for assessment of hematology parameters, which included Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Platelets, Mean Corpuscular Hemoglobin (MCH) and Mean Corpuscular Volume (MCV). Abnormal laboratory results are categorized as high or low with respect to their normal ranges. Participants having High and Low values from normal ranges for any parameter at any time post-baseline visits are presented. (NCT02924688)
Timeframe: Up to Week 52

,,,,,
InterventionParticipants (Count of Participants)
Basophils, low, n=390,390,391,389,389,396Basophils, high, n=390,390,391,389,389,396Eosinophils, low, n=390,390,391,389,389,396Eosinophils, high, n=390,390,391,389,389,396Lymphocytes, low, n=390,390,391,389,389,396Lymphocytes, high, n=390,390,391,389,389,396Monocytes, low, n=390,390,391,389,389,396Monocytes, high, n=390,390,391,389,389,396Neutrophils, low, n=390,390,391,389,389,396Neutrophils, high, n=390,390,391,389,389,396Erythrocytes, low, n=391,390,392,391,391,397Erythrocytes, high, n=391,390,392,391,391,397Hematocrit, low, n=391,390,392,391,391,397Hematocrit, high, n=391,390,392,391,391,397Hemoglobin, low, n=391,390,392,391,391,397Hemoglobin, high, n=391,390,392,391,391,397Leukocytes, low, n=391,390,391,389,391,396Leukocytes, high, n=391,390,391,389,391,396Platelets, low, n=391,388,389,391,388,396Platelets, high, n=391,388,389,391,388,396MCH, low, n=391,390,392,391,391,397MCH, high, n=391,390,392,391,391,397MCV, low, n=391,390,392,391,391,397MCV, high, n=391,390,392,391,391,397
FF/UMEC/VI 100/ 31.25/25 mcg0027841156811020162128524713122921647322241
FF/UMEC/VI 100/62.5/25 mcg0025102131574161511131650408142031924221025
FF/UMEC/VI 200/ 31.25/25 mcg0032851365171215211720493710122651941251926
FF/UMEC/VI 200/62.5/25 mcg00287810663493422172649341384042125321437
FF/VI 100/25 mcg0126111132607142114242160321493841740182029
FF/VI 200/25 mcg00318487642101915122047401793142134171529

[back to top]

Number of Participants With Abnormal Clinical Chemistry Values

Blood samples were collected for assessment of clinical chemistry parameters, which included albumin, alkaline phosphatase (ALP), alanine aminotransferase (ALT), aspartate aminotransferase (AST), direct bilirubin, total bilirubin, calcium, creatinine, glucose, potassium, protein, sodium and urea. Abnormal laboratory results are categorized as high or low with respect to their normal ranges. Participants having High and Low values from normal ranges for any parameter at any time post-baseline visits are presented. (NCT02924688)
Timeframe: Up to Week 52

,,,,,
InterventionParticipants (Count of Participants)
Albumin, lowAlbumin, highALT, lowALT, highAST, lowAST, highALP, lowALP, highDirect bilirubin, lowDirect bilirubin, highBilirubin, lowBilirubin, highCalcium, lowCalcium, highCreatinine, lowCreatinine, highGlucose, lowGlucose, highPotassium, lowPotassium, highProtein, lowProtein, highSodium, lowSodium, highUrea, lowUrea, high
FF/UMEC/VI 100/ 31.25/25 mcg060290270150101291262711713130177417
FF/UMEC/VI 100/62.5/25 mcg0502401401000057104981170111533753
FF/UMEC/VI 200/ 31.25/25 mcg03027023116020174860912667121375311
FF/UMEC/VI 200/62.5/25 mcg0103001601201013376487736192137113
FF/VI 100/25 mcg2104102912101094454715742153056313
FF/VI 200/25 mcg1202802101202015711636776793254311

[back to top]

Mean Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Week 24

Blood pressure (systolic and diastolic) was measured in the sitting position after approximately 5 minutes rest. Baseline value is the last acceptable/borderline acceptable value prior to randomized treatment start date (pre-dose at Day 1). Change from Baseline value is the value at the clinic visit minus the Baseline value. Different participants may have been analyzed at different time points; thus, overall number of participants analyzed reflects everyone in ITT Population without missing covariate information, with Baseline and at least one post-baseline measurement. (NCT02924688)
Timeframe: Baseline (pre-dose at Day 1) and Week 24

,,,,,
InterventionMillimeter of mercury (Least Squares Mean)
SBPDBP
FF/UMEC/VI 100/ 31.25/25 mcg0.60.1
FF/UMEC/VI 100/62.5/25 mcg1.11.3
FF/UMEC/VI 200/ 31.25/25 mcg0.80.2
FF/UMEC/VI 200/62.5/25 mcg0.90.8
FF/VI 100/25 mcg1.60.4
FF/VI 200/25 mcg0.20.4

[back to top]

Number of Participants With Abnormal Electrocardiogram (ECG) Findings

Twelve-lead ECGs were performed during the study using an automated ECG machine. All ECG measurements were made with the participant in a supine position having rested in this position for approximately 5 minutes before each reading. The number of participants with worst case post-Baseline abnormal ECG findings were reported. (NCT02924688)
Timeframe: Up to Week 52

InterventionParticipants (Count of Participants)
FF/VI 100/25 mcg115
FF/UMEC/VI 100/ 31.25/25 mcg118
FF/UMEC/VI 100/62.5/25 mcg109
FF/VI 200/25 mcg109
FF/UMEC/VI 200/ 31.25/25 mcg106
FF/UMEC/VI 200/62.5/25 mcg108

[back to top]

For Fp MDPI Versus Placebo: Change From Baseline in Weekly Average of the Percent Predicted Trough Morning FEV1 at Week 12

FEV1 was the volume of air exhaled in the first second of a forced expiration as measured by spirometer. Baseline trough morning percent predicted FEV1 was defined as the average value of recorded (nonmissing) morning assessments 5 out of the last 7 days prior to randomization. The first day before randomization consisted of the electronic patient diary entry at home on the morning of the randomization visit (Baseline [Day 1]) and the first day postrandomization consisted of the electronic patient diary entry at home on the morning of the day after the randomization visit (Baseline [Day 1]). For postdose weekly average of trough morning percent predicted FEV1 measurements, the values were the averages based on the available data for that week. The averages were calculated as the sum of morning FEV1 values divided by the number of nonmissing assessments. (NCT02980133)
Timeframe: Baseline, Week 12

Interventionpercent predicted of FEV1 (Least Squares Mean)
Placebo MDPI7.3
Fp MDPI 25 mcg BID13.3
Fp MDPI 50 mcg BID14.2

[back to top]

Change From Baseline in the Weekly Average of Total Daily (24 Hour) Use of Albuterol/Salbutamol Inhalation Aerosol (Number of Inhalations) Over Weeks 1 Through 12

Participants recorded the number of inhalations of rescue medication (albuterol/salbutamol HFA MDI) each morning and evening in the electronic patient diary. An entry of 0 inhalations indicated no rescue medication was needed. To calculate the total daily use of albuterol/salbutamol inhalation aerosol (number of inhalations), the electronic patient diary entry on randomization visit (Baseline [Day 1]) was defined as the first day of analysis. The weekly average of the total daily inhalations was the average based on the available data for that week. The average was calculated as the sum of total daily inhalations over the 7 days for each analysis week divided by the number of nonmissing assessments. LS mean and standard error (SE) were obtained using mixed model for repeated measures (MMRM). (NCT02980133)
Timeframe: Baseline, Week 1 to 12

Interventioninhalations (Least Squares Mean)
Placebo MDPI-0.2
Fp MDPI 25 mcg BID-0.4
Fp MDPI 50 mcg BID-0.5
FS MDPI 50/12.5 mcg BID-0.4

[back to top]

Change From Baseline in the Weekly Average of the Total Daily Asthma Symptom Score Over Weeks 1 Through 12

Asthma symptom scores were recorded in the patient diary. Each participant assessed the symptoms of cough, wheeze, shortness of breath, and chest tightness and entered a single score that was inclusive of all symptoms. Daytime Symptom Score (determined in the evening) ranged from 0=No symptoms during the day to 5=Symptoms so severe that I could not go to work or perform normal daily activities. Nighttime Symptom Score (determined in the morning) ranged from 0=No symptoms during the night to 4=Symptoms so severe that I did not sleep at all. The total daily asthma symptom score was the average of the daytime and nighttime scores. The total daily asthma symptom score ranged from 0 - 9 with 0=no symptoms during the day or night and 9=severe symptoms both day and night. The weekly average was calculated as the sum of total daily asthma symptom scores over the 7 days for each analysis week divided by the number of nonmissing assessments. LS mean and SE were obtained using MMRM. (NCT02980133)
Timeframe: Baseline, Week 1 to 12

Interventionunits on a scale (Least Squares Mean)
Placebo MDPI-0.1
Fp MDPI 25 mcg BID-0.2
Fp MDPI 50 mcg BID-0.2
FS MDPI 50/12.5 mcg BID-0.2

[back to top]

Change From Baseline in Asthma Control (Measured by Childhood Asthma Control Test [C-ACT] Score) Over the 12 Week Treatment Period

C-ACT was a simple, participant-completed tool used for the assessment of overall asthma control. The first 4 items of the test were completed by the participant, while the last 3 items were completed by the participant's parents/legal guardians/caregivers. A total sum score based upon responses to all items was calculated to provide an overall measure of asthma control. The derived C-ACT score ranging from 0 to 27. These scores spanned the continuum of poor control of asthma (score ≤5) to complete control of asthma (score ≥25), with a cut off score of 19 indicating participants with poorly controlled asthma. LS mean and SE were obtained using MMRM. (NCT02980133)
Timeframe: Baseline, Week 1 to 12

Interventionunits on a scale (Least Squares Mean)
Placebo MDPI4.5
Fp MDPI 25 mcg BID5.1
Fp MDPI 50 mcg BID5.5
FS MDPI 50/12.5 mcg BID5.4

[back to top]

Change From Baseline in the Weekly Average of Daily Trough Morning (Predose and Pre-Rescue Bronchodilator) Peak Expiratory Flow (PEF) Over the 12 Week Treatment Period

PEF is defined as the maximum airflow during a forced expiration beginning with the lungs fully inflated. Morning PEF was determined in the morning, before administration of IMP or rescue medications. Baseline trough morning PEF was defined as the average value of recorded (nonmissing) morning assessments 5 out of the last 7 days prior to randomization. The first day before randomization consisted of the electronic patient diary entry at home on the morning of the randomization visit (Baseline [Day 1]) and the first day postrandomization consisted of the electronic patient diary entry at home on the morning of the day after the randomization visit (Baseline [Day 1]). For postdose weekly average of trough morning PEF measurements, the values were the averages based on the available data for that week. The averages were calculated as the sum of morning PEF values divided by the number of nonmissing assessments. (NCT02980133)
Timeframe: Baseline, Week 1 to 12

Interventionliters/minute (Least Squares Mean)
Placebo MDPI12.3
Fp MDPI 25 mcg BID28.9
Fp MDPI 50 mcg BID26.3
FS MDPI 50/12.5 mcg BID32.0

[back to top]

Time to First Onset of Effect

The time to first onset of effect, defined as the first decrease from baseline in daily rescue medication use, was calculated based on the number of inhalations of rescue medication (albuterol/salbutamol hydrofluoroalkane metered-dose inhaler [HFA MDI] [90 mcg ex actuator] or equivalent) recorded by the participant each morning and evening in the patient diary built into the handheld device. (NCT02980133)
Timeframe: Baseline up to Week 12

Interventiondays (Median)
Placebo MDPI20.0
Fp MDPI 25 mcg BIDNA
Fp MDPI 50 mcg BID2.0
FS MDPI 50/12.5 mcg BID6.0

[back to top]

Percentage of Participants Who Discontinued From Investigational Medicinal Product (IMP) for Asthma Exacerbation During the 12 Week Treatment Period

(NCT02980133)
Timeframe: Baseline up to Week 12

Interventionpercentage of participants (Number)
Placebo MDPI6
Fp MDPI 25 mcg BID2
Fp MDPI 50 mcg BID1
FS MDPI 50/12.5 mcg BID2

[back to top]

For FS MDPI Versus Fp MDPI: Change From Baseline in 1-Hour Postdose Percent Predicted Morning Forced Expiratory Volume in 1 Second (FEV1) at Week 12

FEV1 was the volume of air exhaled in the first second of a forced expiration as measured by spirometer. The baseline 1-hour trough morning percent predicted FEV1 was defined as the predose trough morning percent predicted FEV1 measurement at the randomization visit (Baseline [Day 1]) at the investigational center. The IMP dose was administered right after the predose FEV1 measurement (within a 10 minute window). Participant then performed 1-hour (±10 minutes) postdose lung function assessments on Week 12 at the investigational center. (NCT02980133)
Timeframe: Baseline, Week 12

Interventionpercent predicted of FEV1 (Least Squares Mean)
Fp MDPI 25 mcg BID16.8
Fp MDPI 50 mcg BID16.4
FS MDPI 50/12.5 mcg BID18.2

[back to top]

Mean Change From Baseline in Evaluating Respiratory Symptoms (E-RS) Total Score

The E-RS is intended to capture information related to respiratory symptoms. A daily symptom score for E-RS is derived by summing 11 item-scores. The domains include: respiratory symptoms (RS)-breathlessness (RS-BRL comprised of 5 items, score range [0-17]), RS-cough and sputum (RS-CSP comprised of 3 items, score range [0-11]), and RS-chest symptoms (RS-CSY comprised of 3 items, score range [0-12]). Total score ranged between 0-40 and higher values indicates severe respiratory symptoms. The instrument was completed each night prior to going to bed. Baseline E-RS score is the mean within-participant daily score over 7 days prior to randomization. Change from Baseline is the difference at Week 21-Week 24 value and Baseline value. Analysis was performed using MMRM with covariates of Baseline score, geographical region, stratum (no. of bronchodilators per day during run-in), 4-weekly period, treatment, 4-weekly period by Baseline and 4-weekly period by treatment interactions. (NCT03034915)
Timeframe: Baseline (Pre-dose on Day 1) and Week 21 to Week 24

InterventionScores on a scale (Least Squares Mean)
UMEC/VI 62.5/25 mcg+ Placebo-1.52
UMEC 62.5 mcg + Placebo-0.99
Salmeterol 50 mcg+Placebo-0.69

[back to top]

Percentage of E-RS Responders According to E-RS Total Score

The E-RS is intended to capture information related to respiratory symptoms. A daily symptom score for E-RS is derived by summing 11 item-scores. The domains include: RS-BRL comprised of 5 items, score range (0-17); RS-CSP comprised of 3 items, score range (0-11); and RS-CSY comprised of 4 items, score range (0-12). Total score ranged between 0-40 and higher values indicates severe respiratory symptoms. The instrument was completed each night prior to going to bed. Response is defined as an E-RS total score of at least 2 or 3.35 below Baseline. Participants with a Baseline but all missing post-Baseline data are also considered a non-responder. Analysis was performed using a generalized linear mixed model with treatment as an explanatory variable and four-weekly period, Baseline score, stratum (no. of bronchodilators per day during run-in), geographical region, four-weekly period by baseline and four-weekly period by treatment interactions included as covariates. (NCT03034915)
Timeframe: Week 21 to Week 24

InterventionPercentage of responders (Number)
UMEC/VI 62.5/25 mcg+ Placebo36
UMEC 62.5 mcg + Placebo27
Salmeterol 50 mcg+Placebo27

[back to top]

Change From Baseline in Trough Forced Expiratory Volume in One Second (FEV1) at Week 24

FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. Trough FEV1 at Week 24 is defined as the mean of the FEV1 values obtained 23 and 24 hours after dosing on the previous day. Baseline trough FEV1 is the mean of the values measured at 30 minutes and 5 minutes pre-dose on Day 1. Change from Baseline was calculated as the trough FEV1 value on Week 24 minus the Baseline value. Analysis was performed using a repeated measures model (MMRM) with covariates of Baseline FEV1, geographical region, stratum (number of bronchodilators per day during run-in), visit, treatment, visit by Baseline and visit by treatment interaction. ITT population comprised of all randomized participants (excluding those who were randomized in error) who received at least one dose of study medication. (NCT03034915)
Timeframe: Baseline (Pre-dose on Day 1) and Week 24

InterventionLiters (Least Squares Mean)
UMEC/VI 62.5/25 mcg+ Placebo0.122
UMEC 62.5 mcg + Placebo0.056
Salmeterol 50 mcg+Placebo-0.019

[back to top]

Change From Baseline in St George's Respiratory Questionnaire (SGRQ) Total Score

SGRQ is a disease-specific questionnaire designed to measure impact of respiratory disease and its treatment on HRQoL of participants with COPD. It contains 14 questions with a total of 40 items grouped into domains (Symptoms, Activity and Impacts). SGRQ total score was calculated as 100 multiplied by summed weights from all positive items divided by sum of weights for all items in questionnaire. It ranges from 0 to 100, higher score indicates poor HRQoL. Baseline is last non-missing score recorded prior to dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the value at Week 24. Analysis was performed using mixed model repeated measures (MMRM) with covariates of Baseline SGRQ total score, geographical region, stratum (no. of bronchodilators per day during run-in), visit, treatment, visit by Baseline and visit by treatment interactions. (NCT03034915)
Timeframe: Baseline (Pre-dose on Day 1) and Week 24

InterventionScores on a scale (Least Squares Mean)
UMEC/VI 62.5/25 mcg+ Placebo-4.98
UMEC 62.5 mcg + Placebo-5.23
Salmeterol 50 mcg+Placebo-3.29

[back to top]

Change From Baseline in COPD Assessment Test (CAT)

The CAT is a participant-completed instrument designed to provide a simple and reliable measure of health status in COPD for the assessment and long-term follow-up of the individual participant. The CAT consists of eight items, each formatted on a differential scale. Participants rated their experience on a 6-point scale for each question, ranging from 0 (no impact) to 5 (high impact). A total CAT score was calculated by summing the non-missing scores on the eight items ranging from 0 to 40 with higher scores indicating greater disease impact. Baseline is defined as the last non-missing score recorded prior to dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the value at Week 24. Analysis was performed using mixed model repeated measures (MMRM) with covariates of Baseline CAT score, geographical region, stratum (no. of bronchodilators per day during run-in), visit, treatment, visit by Baseline and visit by treatment interactions. (NCT03034915)
Timeframe: Baseline (Pre-dose on Day 1) and Week 24

InterventionScores on a scale (Least Squares Mean)
UMEC/VI 62.5/25 mcg+ Placebo-3.5
UMEC 62.5 mcg + Placebo-3.4
Salmeterol 50 mcg+Placebo-2.9

[back to top]

Number of Participants With on Treatment Adverse Events (AE) and Serious Adverse Events (SAE)

An AE is any untoward medical occurrence in a participant or clinical investigation participant , temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment or all events associated with liver injury and impaired liver function based on pre-defined criteria were categorized as SAE. (NCT03034915)
Timeframe: Up to Week 24

,,
InterventionParticipants (Number)
Any AEAny SAE
Salmeterol 50 mcg+Placebo31438
UMEC 62.5 mcg + Placebo31635
UMEC/VI 62.5/25 mcg+ Placebo31549

[back to top]

Percentage of Responders According to CAT

The CAT is a participant-completed instrument designed to provide a simple and reliable measure of health status in COPD for the assessment and long-term follow-up of the individual participant. The CAT consists of eight items. Participants rated their experience on a 6-point scale for each question, ranging from 0 (no impact) to 5 (high impact). A total CAT score was calculated by summing the non-missing scores on the eight items ranging from 0 to 40 with higher scores indicate greater disease impact. Response was defined as an CAT score of >=2 below Baseline. Non response was defined as CAT score <2 units below Baseline or a missing CAT score with no subsequent on treatment scores. Analysis performed using a generalized linear mixed model with treatment as an explanatory variable and visit, baseline CAT score, stratum (no. of bronchodilators per day during run-in), geographical region, visit by baseline and visit by treatment interactions included as covariates. (NCT03034915)
Timeframe: Week 24

InterventionPercentage of responders (Number)
UMEC/VI 62.5/25 mcg+ Placebo55
UMEC 62.5 mcg + Placebo48
Salmeterol 50 mcg+Placebo50

[back to top]

Percentage of Responders Based on the Saint (St) George Respiratory Questionnaire COPD Specific (SGRQ) Total Score

SGRQ is a disease-specific questionnaire designed to measure impact of respiratory disease and its treatment on HRQoL of participants with COPD. It contains 14 questions with a total of 40 items grouped into domains (Symptoms, Activity and Impacts). SGRQ total score was calculated as 100 multiplied by summed weights from all positive items divided by sum of weights for all items in questionnaire. It ranges from 0 to 100, higher score indicates poor HRQoL. Analysis was performed using a generalized linear mixed model with treatment as an explanatory variable and visit, Baseline SGRQ score, stratum (no. of bronchodilators per day during run-in), geographical region, visit by Baseline and visit by treatment interactions included as covariates. Response was defined as an SGRQ total score of 4 or more units below Baseline. (NCT03034915)
Timeframe: Week 24

InterventionPercentage of responders (Number)
UMEC/VI 62.5/25 mcg+ Placebo45
UMEC 62.5 mcg + Placebo41
Salmeterol 50 mcg+Placebo36

[back to top]

Percentage of TDI Responders According to SAC TDI Focal Score

TDI focal score comprises of 3 individual scales (Functional Impairment, Magnitude of Task, Magnitude of Effort). Each of these scales had a possible score ranging from -6 to +6, lower scores indicates impairment. TDI focal score was calculated as the sum of 3 individual scores (range is -18 to +18). Lower score indicates deterioration of dyspnea. If a score is missing for any of the three scales, then TDI focal score was set to missing. A participant was considered as a responder if the on-treatment TDI focal score was at least 1 unit at that visit. Non-response was SAC TDI focal score of less than 1 unit or a missing SAC TDI focal score with no subsequent non-missing on-treatment scores. Analysis was performed using a generalized linear mixed model with treatment as an explanatory variable and visit, SAC BDI focal score, stratum (no. of bronchodilators per day during run-in), geographical region, visit by SAC BDI and visit by treatment interactions included as covariates. (NCT03034915)
Timeframe: Week 24

InterventionPercentage of responders (Number)
UMEC/VI 62.5/25 mcg+ Placebo50
UMEC 62.5 mcg + Placebo42
Salmeterol 50 mcg+Placebo41

[back to top]

Self Administered Computerized (SAC) Transient Dyspnea Index (TDI) Focal Score at Week 24

TDI focal score comprises of 3 individual scales (Functional Impairment, Magnitude of Task, Magnitude of Effort). Each of these scales had a possible score ranging from -6 to +6, lower scores indicates impairment. TDI focal score was calculated as the sum of 3 individual scores (range is -18 to +18). Lower score indicates deterioration of dyspnea. If a score is missing for any of the three scales, then the TDI focal score was set to missing. Analysis was performed using mixed model repeated measures (MMRM) with covariates of SAC BDI focal score, geographical region, stratum (no. of bronchodilators per day during run-in), visit, treatment, visit by SAC BDI and visit by treatment interactions. (NCT03034915)
Timeframe: Week 24

InterventionScores on a scale (Least Squares Mean)
UMEC/VI 62.5/25 mcg+ Placebo1.68
UMEC 62.5 mcg + Placebo1.30
Salmeterol 50 mcg+Placebo1.22

[back to top]

Mean Change From Baseline in E-RS Subscale Score

The E-RS is intended to capture information related to respiratory symptoms. A daily symptom score for E-RS is derived by summing 11 item-scores. The domains include: respiratory symptoms (RS)-breathlessness (RS-BRL comprised of 5 items, score range [0-17]), RS-cough and sputum (RS-CSP comprised of 3 items, score range [0-11]), and RS-chest symptoms (RS-CSY comprised of 3 items, score range [0-12]). Total score ranged between 0-40 and higher values indicates severe respiratory symptoms. The instrument was completed each night prior to going to bed. Baseline E-RS score is the mean within-participant daily score over 7 days prior to randomization. Change from Baseline is the difference at Week 21-Week 24 value and Baseline value. Analysis was performed using MMRM with covariates of Baseline score, geographical region, stratum (no. of bronchodilators per day during run-in), 4-weekly period, treatment, 4-weekly period by Baseline and 4-weekly period by treatment interactions. (NCT03034915)
Timeframe: Baseline (Pre-dose on Day 1) and Week 21 to Week 24

,,
InterventionScores on a scale (Least Squares Mean)
RS-BRLRS-CSPRS-CSY
Salmeterol 50 mcg+Placebo-0.22-0.32-0.15
UMEC 62.5 mcg + Placebo-0.40-0.38-0.22
UMEC/VI 62.5/25 mcg+ Placebo-0.67-0.45-0.39

[back to top]

Change From Baseline in Aortic Distensibility After 6 Weeks of Treatment

Change from baseline in aortic distensibility is presented. Aortic distensibility measurements as measure of arterial stiffness were derived from cine images acquired at end-expiration in planes perpendicular to the thoracic aorta at the level of the pulmonary artery (ascending and descending section of thoracic aorta), abdominal aorta, and perpendicularly to the main, right, and left pulmonary arteries. (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionPercentage/millimeter of mercury(%/mmHg) (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)-0.006
Tiotropium + Olodaterol FDC (T+O 5/5)-0.005

[back to top]

Change From Baseline in 1.5 Hour Post Dose Forced Expiratory Volume in 1st Second (FEV1) After 6 Weeks of Treatment

Change from baseline in 1.5 hour post dose Forced Expiratory Volume in 1st second (FEV1) is presented. (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionLitre (L) (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)0.158
Tiotropium + Olodaterol FDC (T+O 5/5)0.339

[back to top]

Change From Baseline in Left Ventricular End Diastolic Volume Index (LVEDVI) in the 6th Week of Treatment

"LVEDVI is normalised left ventricular end diastolic volume, divided by body surface area.~Baseline was defined as the value obtained during the assessment performed in a week prior to Visit 2 (Day 1). The change from baseline was calculated as the value obtained in a week prior to Visits 3 and 4 (end of each treatment periods) minus the baseline value." (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionMillilitre/ meter^2 (mL/m^2) (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)2.855
Tiotropium + Olodaterol FDC (T+O 5/5)2.317

[back to top]

Change From Baseline in Functional Residual Capacity Body Plethysmography (FRCpleth) % Predicted After 6 Weeks of Treatment

Change from Baseline in Functional Residual Capacity Body Plethysmography (FRCpleth) % predicted is presented. Functional residual capacity, percent predicted is a lung volume at the end of normal expiration assessed/measured by body plethysmography and compared to predicted capacity for such subject, if nonsmoker and without a disease which could compromise their ventilator function, to give a percentage predicted. (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionPercentage of FRCpleth (%) (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)-10.211
Tiotropium + Olodaterol FDC (T+O 5/5)-18.168

[back to top]

Change From Baseline in Central Systolic Pressure After 6 Weeks of Treatment

Change from baseline in central systolic pressure is presented. (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionmmHg (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)0.202
Tiotropium + Olodaterol FDC (T+O 5/5)2.271

[back to top]

Change From Baseline in Aortic Augmentation Index After 6 Weeks of Treatment

Change from baseline in aortic augmentation index is presented. Augmentation index was derived from brachial pulse wave separation analysis as augmentation pressure (pressure difference between the reflection wave to the ejection wave) divided by central pulse pressure (at the central aortic site) multiplied by 100. (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionPercentage of index (%) (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)1.723
Tiotropium + Olodaterol FDC (T+O 5/5)1.404

[back to top]

Change From Baseline in 1.5 Hour Post Dose Forced Vital Capacity (FVC) After 6 Weeks of Treatment

Change from baseline in 1.5 hour post dose Forced Vital Capacity (FVC) is presented. (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionLitre (L) (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)0.159
Tiotropium + Olodaterol FDC (T+O 5/5)0.445

[back to top]

Change From Baseline in Pulmonary Artery Pulsatility After 6 Weeks of Treatment

Change from baseline in pulmonary artery pulsatility (PAP) is presented. Pulmonary artery pulsatility measurements as measure of arterial stiffness were derived from cine images acquired at end-expiration in planes perpendicular to the thoracic aorta at the level of the pulmonary artery (ascending and descending section of thoracic aorta), abdominal aorta, and perpendicularly to the main, right, and left pulmonary arteries. (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionPercentage of PAP (%) (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)-0.175
Tiotropium + Olodaterol FDC (T+O 5/5)1.105

[back to top]

Change From Baseline in Pulse Pressure After 6 Weeks of Treatment

Change from baseline in pulse pressure is presented. (NCT03055988)
Timeframe: Baseline and 6 weeks

InterventionmmHg (Least Squares Mean)
Fluticasone Propionate + Salmeterol FDC (F+S 1000/100)0.170
Tiotropium + Olodaterol FDC (T+O 5/5)0.579

[back to top]

Peak FEV1 (L) Defined as the Highest Bronchodilatory Effect on FEV1 During a Period of 5 Min to 4 h After the Last Evening Dose of Each Treatment Period

The highest bronchodilator effect on FEV1 during a period of 5 min to 4 h after the last evening dose of each treatment period . To demonstrate superiority in peak bronchodilator effect of QVM149 at a dose of 150/50/160 μg o.d. and 150/50/80 μg o.d. compared to a FDC of salmeterol/fluticasone at a dose of 50/500 μg b.i.d. after 3 weeks of treatment in patients with asthma (NCT03063086)
Timeframe: 3 weeks

InterventionLiters (Least Squares Mean)
QVM149 150/50/160 μg o.d.2.792
QVM149 150/50/80 μg o.d.2.779
Salmeterol/Fluticasone 50/500 µg b.i.d2.620

[back to top]

FEV1 AUC 5 Min - 1 h (Day 21) FEV1 AUC 5 Min - 4 h (Day 21) and FEV1 AUC 5 Min - 23 h 45 Min (Day 21)

To evaluate the bronchodilator effect of each dose of QVM149 compared to salmeterol/ fluticasone FDC by measuring standardized FEV1 AUCs after 3 weeks of treatment respective period. (NCT03063086)
Timeframe: 3 weeks

,,
InterventionLiters (Least Squares Mean)
FEV1 AUC 5 min - 1 hFEV1 AUC 5 min - 4 hFEV1 AUC 5 min - 23 h 45 min
QVM149 150/50/160 μg o.d.2.6732.6872.677
QVM149 150/50/80 μg o.d.2.6442.6692.652
Salmeterol/Fluticasone 50/500 µg b.i.d2.5132.5102.515

[back to top]

FEV1 Over 24 h After 21 Days of Treatment in Relation to Evening Dose

To evaluate the bronchodilator effect of each dose of QVM149 compared to salmeterol/fluticasone FDC after 3 weeks of treatment at -45 min, -15 min, 5 min, 15 min, 30 min, 1 h, 2 h, 3h, 4 h, 8 h, 10 h, 11 h 55 min, 14 h, 18 h, 21 h, 23 h 15 min, 23 h 45 min. (NCT03063086)
Timeframe: -45 min, -15 min, 5 min, 15 min, 30 min, 1 h, 2 h, 3h, 4 h, 8 h, 10 h, 11 h 55 min, 14 h, 18 h, 21 h, 23 h 15 min, 23 h 45 min at 3 weeks

,,
InterventionLiters (Least Squares Mean)
-45 min-15 min5 min15 min30 min1 h2 h3 h4 h8 h10 h11h 55 min14 h18 h21 h23 h 15 min23 h 45 min
QVM149 150/50/160 μg o.d.2.62372.60232.64122.66962.68732.69222.70332.69952.68152.68012.69992.70422.68292.63452.61132.61432.5966
QVM149 150/50/80 μg o.d.2.56392.56302.61792.61372.65042.68252.69962.67192.65652.65502.67962.66412.65412.60732.59892.59502.5722
Salmeterol/Fluticasone 50/500 µg b.i.d2.49312.48352.50352.51722.52862.53982.52442.52962.51642.49182.49082.48412.53542.53292.51332.48542.4913

[back to top]

FEV1/FVC Ratio Over 24 h After 21 Days of Treatment in Relation to Evening Dose

To evaluate the bronchodilator effect of each dose of QVM149 compared to salmeterol/fluticasone FDC after 3 weeks of treatment at -45 min, -15 min, 5 min, 15 min, 30 min, 1 h, 2 h, 3h, 4 h, 8 h, 10 h, 11 h 55 min, 14 h, 18 h, 21 h, 23 h 15 min, 23 h 45 min. (NCT03063086)
Timeframe: -45 min, -15 min, 5 min, 15 min, 30 min, 1 h, 2 h, 3h, 4 h, 8 h, 10 h, 11 h 55 min, 14 h, 18 h, 21 h, 23 h 15 min, 23 h 45 min at 3 weeks

,,
InterventionRatio (Mean)
-45min-15min5min15min30min1h2h3h4h8h10h11h 55min14h18h21h23h 15min23h 45min
QVM149 150/50/160 μg o.d.0.67010.67070.67880.68730.68780.69000.69390.69680.68970.68420.69160.68530.68460.68010.6790068210.6782
QVM149 150/50/80 μg o.d.0.66120.66690.67540.67780.68440.68950.69320.68900.68790.68020.68580.67910.68480.67410.67850.67910.6776
Salmeterol/Fluticasone 50/500 μg b.i.d0.65270.65390.65630.65600.65730.66320.66470.66340.66050.64920.64890.64820.65670.65460.65620.65480.6537

[back to top]

FVC Over 24 h After 21 Days of Treatment in Relation to Evening Dose

To evaluate the bronchodilator effect of each dose of QVM149 compared to salmeterol/fluticasone FDC after 3 weeks of treatment at -45 min, -15 min, 5 min, 15 min, 30 min, 1 h, 2 h, 3h, 4 h, 8 h, 10 h, 11 h 55 min, 14 h, 18 h, 21 h, 23 h 15 min, 23 h 45 min. (NCT03063086)
Timeframe: -45 min, -15 min, 5 min, 15 min, 30 min, 1 h, 2 h, 3h, 4 h, 8 h, 10 h, 11 h 55 min, 14 h, 18 h, 21 h, 23 h 15 min, 23 h 45 min at 3 weeks

,,
InterventionLiters (Mean)
-45min-15min5min15min30min1h2h3h4h8h10h11h 55min14h18h21h23h 15min23h 45min
QVM149 150/50/160 μg o.d.3.90463.87433.86563.86693.87003.87563.86983.85763.87443.90203.89763.92713.90913.86753.84383.79973.8034
QVM149 150/50/80 μg o.d.3.85383.85713.89763.89713.90023.89933.89853.87663.86273.92173.95043.94053.92103.91513.86943.86733.8603
Salmeterol/Fluticasone 50/500 μg b.i.d3.76263.72303.75363.72903.76953.75303.76293.75753.76293.76833.78093.79113.80893.78243.76803.73953.7431

[back to top]

Trough FEV1 After 21 Days of Treatment

To evaluate post-dose trough bronchodilator effect of each dose of QVM149 compared to salmeterol/fluticasone FDC after 3 weeks of treatment in the respective treatment period. The trough FEV1 is the mean value of FEV1 at 23 h 15 min and 23 h 45 min post-dose (NCT03063086)
Timeframe: 3 weeks

InterventionLiters (Least Squares Mean)
QVM149 150/50/160 μg o.d.2.623
QVM149 150/50/80 μg o.d.2.6046
Salmeterol/Fluticasone 50/500 µg b.i.d2.4998

[back to top]

Percentage of Patients Achieving the Minimally Clinically Important Difference (MCID) Change From Baseline AQLQ ≥ 0.5

The AQLQ is a 32-item asthma specific questionnaire designed to measure functional impairments that are most important to patients with asthma, with a recall time of two weeks and each question to be answered on a 7-point scale, where 1=totally limited/problems all the time and 7= not at all limited/no problems. It consists of 4 domains: symptoms, activity limitation, emotional function and environmental stimuli. The overall score is calculated as the mean of 32 items. Higher AQLQ scores indicate better health-related quality of life. An improvement of 0.5 points in AQLQ score is considered to be the minimally clinically important difference in asthma. (NCT03158311)
Timeframe: Baseline and Week 24

InterventionParticipants (Count of Participants)
QVM149 150/50/80 μg318
QVM149 150/50/160 μg333
Salmeterol/Fluticasone 50/500 μg Plus Tiotropium 5 μg299

[back to top]

Change From Baseline in Forced Expiratory Flow Between 25% and 75% of Forced Vital Capacity (FEF25-75)

Forced expiratory flow during the mid (25 - 75%) portion of the FVC. It was assessed by performing spirometric assessment. (NCT03158311)
Timeframe: Baseline, Week 8, Week 16 and Week 24

,,
InterventionLitres/second (L/s) (Least Squares Mean)
Week 8Week 16Week 24
QVM149 150/50/160 μg0.3320.3550.375
QVM149 150/50/80 μg0.2900.2910.290
Salmeterol/Fluticasone 50/500 μg Plus Tiotropium 5 μg0.2700.2970.286

[back to top]

Change From Baseline in Asthma Control Questionnaire (ACQ-7) Total Score

The ACQ-7 measured asthma symptom control and consists of 7 items: 5 on symptom assessment, 1 on rescue medication use and 1 on airway calibre (FEV1 % predicted). All seven items are scored on a 7-point Likert scale, with 0 indicating total control and 6 indicating poor control. The questions are equally weighted and the total score is the mean of the seven items. Higher score indicates worst symptoms. The first 6 questions of the ACQ-7 were completed by the participant while the last question was completed by the study investigator using data from the Master Scope spirometer. A negative change from baseline indicates improvement in lung function. (NCT03158311)
Timeframe: Baseline, Week 16 and Week 24

,,
InterventionScore on a scale (Least Squares Mean)
Week 16Week 24
QVM149 150/50/160 μg-1.098-1.172
QVM149 150/50/80 μg-1.043-1.080
Salmeterol/Fluticasone 50/500 μg Plus Tiotropium 5 μg-1.020-1.048

[back to top]

Percentage of Patients Achieving the Minimally Clinically Important Difference (MCID) Decrease From Baseline ACQ-7 ≥ 0.5

The ACQ-7 measured asthma symptom control and consists of 7 items: 5 on symptom assessment, 1 on rescue medication use and 1 on airway calibre (FEV1 % predicted). All seven items are scored on a 7-point Likert scale, with 0 indicating total control and 6 indicating poor control. The questions are equally weighted and the total score is the mean of the seven items. Higher score indicates worst symptoms. The first 6 questions of the ACQ-7 were completed by the participant while the last question was completed by the study investigator using data from the Master Scope spirometer. A negative change from baseline indicates improvement in lung function. Decrease of ACQ-7 score of at least 0.5 from baseline was considered clinically meaningful. (NCT03158311)
Timeframe: Baseline and Week 24

InterventionParticipants (Count of Participants)
QVM149 150/50/80 μg393
QVM149 150/50/160 μg387
Salmeterol/Fluticasone 50/500 μg Plus Tiotropium 5 μg375

[back to top]

Change From Baseline in Forced Vital Capacity (FVC)

FVC is the total volume of air exhaled during a expiratory maneuvre. It was assessed by performing a spirometry assessment. (NCT03158311)
Timeframe: Baseline, Week 8, Week 16 and Week 24

,,
InterventionLitre (L) (Least Squares Mean)
Week 8Week 16Week 24
QVM149 150/50/160 μg0.2720.2750.280
QVM149 150/50/80 μg0.2160.2210.214
Salmeterol/Fluticasone 50/500 μg Plus Tiotropium 5 μg0.2190.2170.186

[back to top]

Change From Baseline in Trough Forced Expiratory Volume in 1 Second (FEV1)

FEV1 is the amount of air which can be forcibly exhaled from the lungs in the first second of a forced exhalation, measured through spirometry testing. Trough FEV1 is the mean of two FEV1 values measures taken 15 minutes (min) and 45 min prior to evening dose. (NCT03158311)
Timeframe: Baseline, Week 8, Week 16 and Week 24

,,
InterventionLitre (L) (Least Squares Mean)
Week 8Week 16Week 24
QVM149 150/50/160 μg0.3090.3190.334
QVM149 150/50/80 μg0.2460.2510.248
Salmeterol/Fluticasone 50/500 μg Plus Tiotropium 5 μg0.2430.2530.238

[back to top]

Change From Baseline in AQLQ Total Score

The AQLQ is a 32-item asthma specific questionnaire designed to measure functional impairments that are most important to patients with asthma, with a recall time of two weeks and each question to be answered on a 7-point scale, where 1=totally limited/problems all the time and 7= not at all limited/no problems. It consists of 4 domains: symptoms, activity limitation, emotional function and environmental stimuli. The overall score is calculated as the mean of 32 items. Higher AQLQ scores indicate better health-related quality of life. (NCT03158311)
Timeframe: Baseline and Week 16

InterventionScore on a scale (Least Squares Mean)
QVM149 150/50/80 μg0.690
QVM149 150/50/160 μg0.755
Salmeterol/Fluticasone 50/500 μg Plus Tiotropium 5 μg0.673

[back to top]

Change From Baseline in Asthma Quality of Life Questionnaire (AQLQ) Total Score

The AQLQ is a 32-item asthma specific questionnaire designed to measure functional impairments that are most important to patients with asthma, with a recall time of two weeks and each question to be answered on a 7-point scale, where 1=totally limited/problems all the time and 7= not at all limited/no problems. It consists of 4 domains: symptoms, activity limitation, emotional funtion, and emotional stimuli. The overall score is calculated as the mean of 32 items. Higher AQLQ scores indicate better health-related quality of life. (NCT03158311)
Timeframe: Baseline and Week 24

InterventionScore on a scale (Least Squares Mean)
QVM149 150/50/80 μg0.715
QVM149 150/50/160 μg0.827
Salmeterol/Fluticasone 50/500 μg Plus Tiotropium 5 μg0.753

[back to top]

Change From Baseline in Pulse Rate (PR)

Pulse rate was measured in semi-supine position after 5 minutes rest. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. Data for change from Baseline for post dose values have been presented. (NCT03207243)
Timeframe: Baseline and Week 0 (Post-dose), Week1, Week 2, Week 4 (Pre and Post dose), Week 6, Week 8 (Pre and Post dose), Week 10, Week 12 (Pre and Post dose), Week 14, Week 16, Week 20, Week 24 and Week 28

,
InterventionBeats per minute (Mean)
Post-dose: Week0; n=82, 83Week1; n=79, 75Week2; n=73, 75Pre-dose:Week4; n=49, 59Post-dose:Week4; n=48, 59Week6; n=45, 57Pre-dose: Week8; n=34, 47Post-dose: Week8; n=34, 47Week10; n=34, 46Pre-dose: Week12; n=24, 39Post-dose: Week12; n=24, 39Week14; n=24, 39Week16; n=24, 39Week20; n=76, 78Week24; n=75, 76Week28; n=74, 77
GSK3772847-0.13.11.70.1-1.02.81.0-0.62.41.7-1.23.62.63.62.52.3
Placebo-2.20.82.9-0.3-2.03.3-0.3-0.92.62.80.93.13.52.12.32.5

[back to top]

Change From Baseline Between Post-dose and Pre-dose in Pulse Rate

Pulse rate was measured pre-dose and post-dose in semi-supine position after 5 minutes rest. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 0, 4, 8 and 12

,
InterventionBeats per minute (Mean)
Week0; n=82, 83Week4; n=48, 59Week8; n=34, 47Week12; n=24, 39
GSK3772847-0.1-1.1-1.6-2.9
Placebo-2.2-1.6-0.5-2.0

[back to top]

Change From Baseline in St George's Respiratory Questionnaire (SGRQ) Total Score

SGRQ is a disease-specific questionnaire designed to measure impact of respiratory disease and its treatment on Health-related quality of life (HRQoL) of participants with Chronic Obstructive Pulmonary Disease (COPD). It contains 14 questions with a total of 40 items grouped into domains (Symptoms, Activity and Impacts). SGRQ total score was calculated as 100 multiplied by summed weights from all positive items divided by sum of weights for all items in questionnaire. It ranges from 0 to 100, higher score indicates poor HRQoL. Baseline is defined as the latest available assessment prior to first dose (Day 1). Change from Baseline was calculated by subtracting Baseline value from the specified time point value. Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 4, 8, 12 and 16

,
InterventionScores on a scale (Mean)
Week4; n=43, 52Week8; n=31, 42Week12; n=23, 35Week16; n=16, 26
GSK3772847-7.0-7.2-12.9-16.5
Placebo-10.0-10.7-15.8-12.4

[back to top]

Change From Baseline Between Post-dose and Pre-dose in DBP and SBP

DBP and SBP was measured pre-dose and post-dose in semi-supine position after 5 minutes rest. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 0, 4, 8 and 12

,
InterventionmmHg (Mean)
SBP: Week0; n=82, 83SBP: Week4; n=48, 59SBP: Week8; n=34, 47SBP: Week12; n=24, 39DBP: Week0; n=82, 83DBP: Week4; n=48, 59DBP: Week8; n=34, 47DBP: Week12; n=24, 39
GSK37728471.32.41.91.8-0.3-0.10.8-1.1
Placebo-2.0-0.4-0.8-0.9-0.70.40.2-0.3

[back to top]

Change Between Pre-dose and Post-dose of QRS Axis

Triplicate 12-lead ECGs were recorded pre-dose and post-dose with participant in semi-supine position after 5 minutes rest. At each time point ECG was taken using an ECG machine that automatically measures QRS axis. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 0, 4, 8 and 12

,
InterventionDegrees (Mean)
Week0; n=80, 80Week4; n=48, 59Week8; n=33, 47Week12; n=24, 39
GSK37728471.9-0.9-0.22.8
Placebo-0.8-0.31.2-1.6

[back to top]

Change Between Pre-dose and Post-dose of PR Interval, QRS Duration, Uncorrected QT Interval, QTcF Interval and RR Interval

Triplicate 12-lead ECGs were recorded pre-dose and post-dose with participant in semi-supine position after 5 minutes rest. At each time point ECG was taken using an ECG machine that automatically measures PR interval, QRS duration, uncorrected QT interval, QTcF interval and RR interval. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 0, 4, 8 and 12

,
Interventionmilliseconds (Mean)
PR:Week0; n=80, 80PR: Week4; n=48, 59PR: Week8; n=33, 47PR: Week12; n=24, 39QRS:Week0; n=80, 80QRS: Week4; n=48, 59QRS:Week8; n=33, 47QRS:Week12; n=24, 39QT:Week0; n=80, 80QT:Week4; n=48, 59QT:Week8; n=33, 47QT:Week12; n=24, 39QTcFWeek0; n=80, 80QTcF:Week4; n=48, 59QTcF:Week8; n=33, 47QTcF:Week12; n=24, 39RR:Week0; n=80, 80RR:Week4; n=48, 59RR:Week8; n=33, 47RR:Week12; n=24, 39
GSK37728473.10.5-0.13.00.2-0.80.4-0.93.56.911.54.63.82.96.62.0-0.229.534.420.7
Placebo1.81.70.32.20.00.10.30.77.410.83.41.94.25.4-0.71.124.037.629.38.8

[back to top]

Change Between Pre-dose and Post-dose of Heart Rate

Triplicate 12-lead ECGs were recorded pre-dose and post-dose with participant in semi-supine position after 5 minutes rest. At each time point ECG was taken using an ECG machine that automatically measures heart rate. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 0, 4, 8 and 12

,
InterventionBeats per minute (Mean)
Week0; n=80, 80Week4; n=48, 59Week8; n=33, 47Week12; n=24, 39
GSK37728470.2-1.7-2.3-0.9
Placebo-1.6-2.9-1.8-0.2

[back to top]

Time to Loss of Asthma Control

Time to loss of asthma control was analyzed using Kaplan-Meier analysis. In this analysis, participants were either be counted as an event or they were censored. An event is defined as participants who experience loss of asthma control during the study. Censoring is defined as participants who discontinued investigational product for reasons other than loss of asthma control. The analysis shown is for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. Participants who didn't experience loss of asthma control were also censored at day 113. (NCT03207243)
Timeframe: Up to Week 16

InterventionDays (Median)
Placebo50
GSK377284796

[back to top]

Rate Per 1000 Person-years of Participants With Hospitalization

An event is defined as an on-treatment asthma-related hospitalization or emergency room visit and participants can contribute to more than one event. Rate is calculated as number of events * 1000 divided by (number of participants in treatment group * mean treatment exposure in years). Data has been presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Up to Week 16

InterventionEvents per person-year (Number)
Placebo70.5
GSK37728470

[back to top]

Percentage of Participants With Loss of Asthma Control Over Weeks 0-6

Loss of asthma control is defined as: ACQ-5 score increase from Baseline >=0.5 point or pre-bronchodilator FEV1 decrease from Baseline >7.5 % or inability to titrate inhaled corticosteroid or a clinically significant asthma exacerbation (requiring oral OCS and/or hospitalization). The analysis shown is for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. Baseline is defined as Day1. Percentage of participants experiencing loss of asthma control up to Week 6 has been presented. (NCT03207243)
Timeframe: Up to Week 6

InterventionPercentage of participants (Number)
Placebo50
GSK377284736

[back to top]

Change From Baseline in Hematology Parameter: Erythrocytes Distribution Width (%)

Blood samples were collected for the analysis of Erythrocytes Distribution Width (%) at indicated time points. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
InterventionPercentage (%) of Erythrocytes (Mean)
Week 1: n=78,74Week 2: n=71, 74Week 4: n=49, 57Week 6: n=44, 56Week 8: n=34, 47Week 10: n=34, 45Week 12: n=24, 39Week 14: n=24, 39Week 16: n=24, 39Week 28: n=65, 63
GSK3772847-0.08-0.20-0.33-0.37-0.29-0.38-0.34-0.38-0.41-0.01
Placebo-0.06-0.02-0.22-0.33-0.40-0.35-0.27-0.28-0.25-0.09

[back to top]

Percentage of Participants With Loss of Asthma Control Over Weeks 0-16

Loss of asthma control is defined as: Asthma Control Questionnaire (ACQ-5) score increase from Baseline >=0.5 point or pre-bronchodilator forced expiratory volume in 1 second (FEV1) decrease from baseline >7.5 % or inability to titrate inhaled corticosteroid or a clinically significant asthma exacerbation (requiring oral corticosteroid [OCS] and/or hospitalization). The analysis shown is for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. Baseline is defined as Day1. Percentage of participants experiencing loss of asthma control up to Week 16 has been presented. Modified Intent-to-Treat (Loss of Control) (mITT_LoC) population consisted of all randomized participants who took at least 1 dose of study treatment and if participants experienced loss of asthma control, they were analyzed according to actual treatment at time of loss of control. (NCT03207243)
Timeframe: Up to Week 16

InterventionPercentage of participants (Number)
Placebo81
GSK377284767

[back to top]

Percentage of Participants With Inability to Titrate Inhaled Corticosteroids (ICS)

Corticosteroid titration allows overall clinical evaluation of the participant's asthma status taking into account both lung function and symptom control. Inability to titrate inhaled corticosteroids indicates loss of asthma control. (NCT03207243)
Timeframe: Up to Week 16

InterventionPercentage of participants (Number)
Placebo23
GSK377284730

[back to top]

Percentage of Participants With Clinically Significant Asthma Exacerbation or Inability to Titrate

A clinically significant asthma exacerbation is defined as one requiring oral corticosteroid and/or hospitalization. Participants with clinically significant asthma exacerbation or inability to titrate FP indicated loss of asthma control. (NCT03207243)
Timeframe: Up to Week 16

InterventionPercentage of participants (Number)
Placebo25
GSK377284740

[back to top]

Percentage of Participants With Clinically Significant Asthma Exacerbation

A clinically significant asthma exacerbation is defined as one requiring oral corticosteroid and/or hospitalization. (NCT03207243)
Timeframe: Up to Week 16

InterventionPercentage of participants (Number)
Placebo7
GSK377284713

[back to top]

Percentage of Participants With >=0.5 Point Asthma Control Questionnaire (ACQ-5) Score Increase From Baseline

The ACQ-5 is a five-item, self-completed questionnaire, which measures asthma control of a participant. The five questions (concerning nocturnal awakening, waking in the morning, activity limitation, shortness of breath and wheeze) enquire about the frequency and/or severity of symptoms over the previous week. The response options for all these questions range from zero (no impairment/limitation) to six (total impairment/ limitation) scale. ACQ-5 score ranges from 0 (totally controlled) to 6 (severely uncontrolled). Higher score indicate lower asthma control. Baseline is the latest available assessment prior to first dose (Day 1). Change from Baseline was calculated by subtracting Baseline value from the specified time point value. A change of >=0.5 in score suggests a clinically important change in score. Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment (NCT03207243)
Timeframe: Baseline and up to Week 16

InterventionPercentage of participants (Number)
Placebo39
GSK377284730

[back to top]

Percentage of Participants Who Have Pre-bronchodilator FEV1 Decrease From Baseline >7.5 %

Pulmonary function is measured by FEV1. FEV1 is the amount of air expired in 1 second. Pre-bronchodilator FEV1 measurements were taken by spirometry. Baseline is defined as the latest available pre-dose assessment (Day 1). Decrease from Baseline >7.5 % in score suggests worsening of condition. (NCT03207243)
Timeframe: Baseline and up to Week 16

InterventionPercentage of participants (Number)
Placebo63
GSK377284768

[back to top]

Change From Baseline in Supraventricular Couplets, Supraventricular Ectopics, Supraventricular Runs, Supraventricular Singles, Ventricular Couplets, Ventricular Ectopics, Ventricular Runs, Ventricular Singles

Using a Holter monitor, supraventricular couplets, supraventricular ectopics, supraventricular runs, supraventricular singles, ventricular couplets, ventricular ectopics, ventricular runs, ventricular singles were recorded at Baseline, Weeks 0, 4 and 12 through 24 hours. Participants with analyzable time of at least 16 hours were evaluated. Baseline is the value from the screening visit assessment. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 0, 4 and 12

,
InterventionEvents per hour (Mean)
supraventricular couplets: Week0; n=81, 80supraventricular couplets: Week4; n=49, 58supraventricular couplets: Week12; n=24, 37supraventricular ectopics: Week0; n=81, 80supraventricular ectopics: Week4; n=49, 58supraventricular ectopics: Week12; n=24, 37supraventricular runs: Week0; n=81, 80supraventricular runs: Week4; n=49, 58supraventricular runs: Week12; n=24, 37supraventricular singles: Week0; n=81, 80supraventricular singles: Week4; n=49, 58supraventricular singles: Week12; n=24, 37ventricular couplets: Week0; n=81, 80ventricular couplets: Week4; n=49, 58ventricular couplets: Week12; n=24, 37ventricular ectopics: Week0; n=81, 80ventricular ectopics: Week4; n=49, 58ventricular ectopics: Week12; n=24, 37ventricular runs: Week0; n=81, 80ventricular runs: Week4; n=49, 58ventricular runs: Week12; n=24, 37ventricular singles: Week0; n=81, 80ventricular singles: Week4; n=49, 58ventricular singles: Week12; n=24, 37
GSK377284716.5-2.2-0.56.8-7.39.40.2-0.6-0.4-13.1-3.18.4-0.10.10.3-12.26.4176.00.00.00.0-12.26.3174.5
Placebo-2.0-1.9-3.92.6-30.934.9-0.5-0.1-1.19.0-25.345.50.70.20.044.6-10.7-5.30.00.00.044.0-10.4-5.4

[back to top]

Serum Concentrations of GSK3772847

Blood samples were collected at given time points to evaluate pharmacokinetics (PK) of GSK3772847 in participants with moderately severe asthma. (NCT03207243)
Timeframe: Weeks 2, 4 (Pre-dose), 8 (Pre-dose), 12 (Pre-dose and Post-dose), 16, 20, 24 and 28

InterventionMicrograms per milliliter (Mean)
Week2; n=75Week4; Pre-dose;n=59Week8; Pre-dose; n= 47Week12; Pre-dose; n=39Week12; Post-dose; n=39Week16; n=38Week20; n=75Week24; n=75Week28; n=75
GSK377284778.4044.4261.4463.42224.2163.0325.7512.916.14

[back to top]

Percentage of Participants With <=-0.5 Point ACQ-5 Score Decrease From Baseline (Responder)

ACQ-5 is a five-item, self-completed questionnaire, which measures asthma control of a participant. The five questions (concerning nocturnal awakening, waking in the morning, activity limitation, shortness of breath & wheeze) enquire about the frequency &/or severity of symptoms over the previous week. The response options range from zero (no impairment/limitation) to six (total impairment/limitation) scale. ACQ-5 score ranges from 0 (totally controlled) to 6 (severely uncontrolled). Higher score indicate lower asthma control. Baseline is the latest available assessment prior to first dose (Day 1). Change from Baseline was calculated by subtracting Baseline value from the specified time point value. A responder is defined as participants with change from Baseline of <= -0.5 point at given time point. Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 and Week 16

,
InterventionPercentage of participants (Number)
Week1; n=72, 73Week2; n=67, 68Week3; n=61, 61Week4; n=54, 59Week5; n= 42, 52Week6; n=40, 48Week7; n=34, 46Week8; n=33, 44Week9; n=30, 42Week10; n=29, 41Week11; n=22, 38Week12; n=23, 38Week13; n=17,32Week14; n=17, 31Week15; n=17, 27Week16; n=12, 21
GSK377284741565661656965737176797975747481
Placebo38464959626374707069645782717667

[back to top]

Number of Hospitalizations or Emergency Room Visits Per Participants

The number of hospitalization or emergency room visit made by per participant due to loss of asthma control have been presented in category titles. Data has been presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Up to Week 16

,
InterventionParticipants (Count of Participants)
012>=3
GSK377284778000
Placebo77100

[back to top]

Change From Baseline in Pre-bronchodilator Forced Expiratory Volume in One Second (FEV1)

Pre-bronchodilator FEV1 is a measure of lung function and is defined as the maximal amount of air that can be forcefully exhaled in one second. Baseline is defined as the latest available assessment prior to first dose (Day 1) and change from Baseline was calculated by subtracting Baseline value from the specified time point value. Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 2, 4, 6, 8, 10, 12, 14 and 16

,
InterventionLiters (Mean)
Week2; n=64, 66Week4; n=48, 56Week6; n=38, 50Week8; n=33, 45Week10; n=33, 43Week12; n=23, 36Week14; n=21, 36Week16; n=15, 26
GSK37728470.0890.0860.1350.0890.0660.0370.0470.025
Placebo0.0940.0740.0780.0490.0470.0610.0790.063

[back to top]

Change From Baseline in QRS Axis

Triplicate 12-lead ECGs were recorded with participant in semi-supine position after 5 minutes rest. At each time point ECG was taken using an ECG machine that automatically measures QRS axis. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Week 4 (Pre and Post dose), Week 8 (Pre and Post dose), Week 12 (Pre and Post dose) and Week 16

,
InterventionDegrees (Mean)
Post-dose: Week0; n=80, 80Pre-dose: Week4; n=49, 59Post-dose: Week4; n=48, 59Pre-dose: Week8; n=34, 47Post-dose: Week8; n=33, 47Pre-dose:Week12; n=24, 39Post-dose Week12; n=24, 39Week16; n=24, 39
GSK37728471.92.31.4-1.0-1.22.0-1.2-1.4
Placebo-0.80.7-0.1-0.21.00.2-1.32.3

[back to top]

Change From Baseline in PR Interval, QRS Duration, Uncorrected QT Interval, QT Corrected Interval-Fredericia [QTcF] Interval and RR Interval

Triplicate 12-lead ECGs were recorded pre-dose and post-dose with participant in semi-supine position after 5 minutes rest. At each time point ECG was taken using an ECG machine that automatically measures PR interval, QRS duration, uncorrected QT interval, QTcF interval and RR interval. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Week 0 (Post-dose), Week 4 (Pre and Post dose), Week 8 (Pre and Post dose), Week 12 (Pre and Post dose) and Week 16

,
Interventionmilliseconds (Mean)
PR: Post-dose: Week0; n=80, 80PR: Pre-dose: Week4; n=49, 59PR: Post-dose: Week4; n=48, 59PR: Pre-dose: Week8; n=34, 47PR:Post-dose: Week8; n=33, 47PR: Pre-dose:Week12; n=24, 39PR: Post-dose Week12; n=24, 39PR: Week16; n=24, 39QRS:Post-dose Week0; n=80, 80QRS:Pre-dose Week4; n=49, 59QRS: Post-dose:Week4; n=48, 59QRS:Pre-dose:Week8; n=34, 47QRS:Post-dose:Week8; n=33, 47QRS:Pre-dose: Week12; n=24, 39QRS:Post-dose: Week12; n=24, 39QRS:Week16; n=24, 39QT:Post-dose: Week0; n=80, 80QT:Pre-dose: Week4; n=49, 59QT:Post-dose: Week4; n=48, 59QT:Pre-dose: Week8; n=34, 47QT:Pre-dose: Week8; n=33, 47QT Pre-dose:Week12; n=24, 39QT:Post-dose:Week12; n=24, 39QT:Week16; n=24,39QTcF:Post-dose:Week0; n=80, 80QTcF:Pre-dose:Week4; n=49, 59QTcF:Post-dose:Week4; n=48, 59QTcF:Pre-dose:Week8; n=34, 47QTcF:Post-dose:Week8; n=33, 47QTcF:Pre-dose:Week12; n=24, 39QTcF:Post-dose: Week12; n=24, 39QTcF: Week16; n=24, 39RR:Post-dose: Week0; n=80, 80RR:Pre-dose: Week4; n=49, 59RR:Post-dose: Week4; n=48, 59RR:Pre-dose:Week8; n=34, 47RR:Post-dose:Week8; n=33, 47RR:Pre-dose:Week12; n=24, 39RR:Post-dose:Week12; n=24, 39RR:Week16; n=24, 39
GSK37728473.11.31.91.41.5-0.52.2-0.70.20.70.1-0.10.1-1.1-1.8-2.03.5-1.85.1-4.77.0-3.12.4-7.33.8-1.02.0-0.95.80.42.9-2.2-0.2-2.026.7-24.210.7-21.61.3-33.9
Placebo1.8-0.41.20.00.5-1.31.3-0.60.0-0.5-0.20.20.5-1.3-0.7-1.67.4-1.78.93.56.71.53.3-2.24.2-1.44.06.45.53.34.4-0.524.0-1.336.2-17.410.8-12.6-4.8-14.4

[back to top]

Change From Baseline in Percent Night-time Awakenings Due to Asthma Symptoms Requiring Rescue Medication Use

Participant captured night-time awakenings (yes/no) and use of rescue medication during these awakenings (yes/no) was recorded in e-Diary each morning. Percentage of night-time awakenings is calculated by number of nights with awakenings due to asthma and requiring rescue medication divided by number of nights with data available*100. Baseline was calculated over the last 7 days of run-in period prior to Visit 2 (Week 0). Participants having at least 4 full days of data in the last 7 days of run-in were included. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. Night-time awakenings due to asthma symptoms requiring rescue medication was calculated for each participant during the four weekly periods (Weeks 1-4; Weeks 5-8, Weeks 9-12 and Weeks 13-16). Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 1-4; Weeks 5-8, Weeks 9-12 and Weeks 13-16

,
InterventionPercentage of nights with awakenings (Mean)
Weeks 1-4, n=77, 76Weeks 5-8,n=50, 56Weeks 9-12,n=31, 43Weeks 13-16,n=20, 38
GSK3772847-7.42-10.49-13.43-14.91
Placebo-3.80-7.85-5.67-2.31

[back to top]

Change From Baseline in Mean Morning Peak Expiratory Flow (PEF) and Mean Evening PEF

PEF is maximum speed of expiration measured, using spirometer. The device was distributed to participants at Visit 1, to measure PEF twice-daily (morning upon waking & in the evening just before going to bed). Participants were encouraged to perform morning & evening PEF measurements before the use of any long-acting beta-agonists (LABAs) or rescue medication. Highest of 3 values were recorded in eDairy.Baseline was calculated over the last 7 days of run-in period prior to Visit 2 (Week 0). Participants with at least 4 full days of data in the last 7 days of run-in were included. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. Mean PEF was calculated for each participant during the four weekly periods (Weeks 1-4; Weeks 5-8, Weeks 9-12 and Weeks 13-16).Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment (NCT03207243)
Timeframe: Baseline and Weeks 1-4; Weeks 5-8, Weeks 9-12 and Weeks 13-16.

,
InterventionLiters/minute (Mean)
Morning PEF: Weeks 1-4,n=76, 76Morning PEF: Weeks 5-8,n=50, 56Morning PEF: Weeks 9-12,n=31, 43Morning PEF: Weeks 13-16,n=20, 38Evening PEF: Weeks 1-4,n=76, 77Evening PEF: Weeks 5-8,n=52, 58Evening PEF: Weeks 9-12,n=33, 44Evening PEF: Weeks 13-16,n=21, 38
GSK37728474.32-3.82-1.69-1.832.45-4.38-0.58-1.16
Placebo4.13-1.84-4.15-7.880.43-6.96-0.77-10.81

[back to top]

Change From Baseline in Mean Daytime Asthma Symptom Score Over Each Four Weeks of the 16 Week Treatment Period

Asthma symptoms experienced by participants during the day was recorded in e-Diary every evening before going to bed in form of scores on a 5-point rating scale. Scores ranged from 0=no daytime asthma symptoms to 4=very severe daytime asthma symptoms. Baseline was calculated over the last 7 days of run-in period prior to Visit 2 (Week 0). Participants with at least 4 full days of data in the last 7 days of run-in were included. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. The mean asthma symptom score was calculated for each participant during the four weekly periods (Weeks 1-4; Weeks 5-8, Weeks 9-12 and Weeks 13-16). Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 1-4; Weeks 5-8, Weeks 9-12 and Weeks 13-16

,
InterventionScores on a scale (Mean)
Weeks 1-4, n=77, 78Weeks 5-8, n=52, 59Weeks 9-12 ,n=33,34Weeks 13-16, n=21, 38
GSK3772847-0.02-0.09-0.08-0.17
Placebo-0.09-0.18-0.29-0.29

[back to top]

Change From Baseline in Mean Daily Rescue Medication Use (Albuterol/Salbutamol)

The mean number of inhalation of rescue medication (albuterol/salbutamol) used to relieve symptoms immediately during the day and night was recorded in eDiary from Baseline until Week 16. Baseline was calculated over the last 7 days of run-in period prior to Visit 2 (Week 0). Participants with at least 4 full days of data in the last 7 days of run-in were included. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. The mean rescue medication use was calculated for each participant during the four weekly periods (Weeks 1-4; Weeks 5-8, Weeks 9-12 and Weeks 13-16). Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 1-4; Weeks 5-8, Weeks 9-12 and Weeks 13-16

,
InterventionInhalations per day (Mean)
Weeks 1-4, n=78, 75Weeks 5-8, n=56, 57Weeks 9-12, n=32, 42Weeks 13-16, n=24, 37
GSK3772847-1.09-1.24-1.59-1.90
Placebo-0.52-0.52-0.170.01

[back to top]

Change From Baseline in Maximum, Minimum and Average Changes in Heart Rate

Using a Holter monitor, maximum, minimum and average changes in heart rate was recorded at Baseline, Weeks 0, 4 and 12 through 24 hours. Participants with analyzable time of at least 16 hours were evaluated. Baseline is the value from the screening visit assessment. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 0, 4 and 12

,
InterventionBeats per minute (Mean)
Mean Heart Rate: Week0; n=81, 80Mean Heart Rate: Week4; n=49, 58Mean Heart Rate: Week12; n=24, 37Maximum Heart Rate: Week0; n=81, 80Maximum Heart Rate: Week4; n=49, 58Maximum Heart Rate: Week12; n=24, 37Minimum Heart Rate: Week0; n=81, 80Minimum Heart Rate: Week4; n=49, 58Minimum Heart Rate: Week12; n=24, 37
GSK3772847-2.080.079.9-5.0130.3132.1-0.853.853.4
Placebo-1.176.878.8-0.3128.3128.5-0.850.653.6

[back to top]

Change From Baseline in Hematology Parameters: Basophil, Eosinophils, Leukocytes, Lymphocytes, Neutrophils, Monocytes, and Platelets

Blood samples were collected at given time points to assess hematology parameters including basophil, eosinophils, leukocytes, lymphocytes, leutrophils, monocytes, and platelets . Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
Intervention10^9 cells per liter (Mean)
Basophil: Week 1; n=77, 74Basophil:Week 2; n= 68, 72Basophil:Week 4; n=48, 57Basophil:Week 6; n=43, 54Basophil:Week 8; n=33, 46Basophil:Week 10; n= 32, 44Basophil:Week 12; n=24, 39Basophil:Week 14; n=23, 39Basophil:Week 16; n=23, 39Basophil:Week 28; n= 65, 60Eosinophil: Week 1; n=77, 74Eosinophil:Week 2; n=68, 72Eosinophil:Week 4; n=48, 57Eosinophil:Week 6; n =43, 54Eosinophil:Week 8; n= 33, 46Eosinophil:Week 10 n=32, 44Eosinophil:Week 12; n=24, 39Eosinophil:Week 14; n=23, 39Eosinophil:Week 16; n=23, 39Eosinophil:Week 28; n= 65, 60Leukocytes: Week 1; n=78, 74Leukocytes:Week 2; n= 68, 73Leukocytes:Week 4; n =48, 57Leukocytes:Week 6; n=43, 54Leukocytes:Week 8; n=33, 47Leukocytes:Week 10; n=33, 45Leukocytes:Week 12; n=24, 39Leukocytes:Week 14; n= 23, 39Leukocytes:Week 16; n=23, 39Leukocytes:Week 28; n=65, 63Lymphocytes: Week 1; n=77, 74Lymphocytes:Week 2; n=68, 72Lymphocytes:Week 4; n=48, 57Lymphocytes:Week 6; n=43, 54Lymphocytes:Week 8; n=33, 46Lymphocytes:Week 10; n=32, 44Lymphocytes:Week 12; n=24, 39Lymphocytes:Week 14; n=23, 39Lymphocytes:Week 16; n=23, 39Lymphocytes:Week 28; n=65, 60Neutrophils: Week 1; n=77, 74Neutrophils:Week 2; n=68, 72Neutrophils:Week 4; n=48, 57Neutrophils:Week 6; n=43, 54Neutrophils:Week 8; n=33, 46Neutrophils:Week 10; n=32, 44Neutrophils:Week 12; n=24, 39Neutrophils:Week 14; n=23, 39Neutrophils:Week 16; n=23, 39Neutrophils:Week 28; n=65, 60Monocytes: Week 1; n=77, 74Monocytes:Week 2; n=68, 72Monocytes:Week 4; n=48, 57Monocytes:Week 6; n=43, 54Monocytes:Week 8; n=33, 46Monocytes:Week 10; n=32, 44Monocytes:Week 12; n=24, 39Monocytes:Week 14; n=23, 39Monocytes:Week 16; n=23, 39Monocytes:Week 28; n=65, 60Platelets: Week 1; n=78, 74Platelets:Week 2; n=71, 74Platelets:Week 4; n=49, 57Platelets:Week 6; n=44, 56Platelets:Week 8; n=34, 47Platelets:Week 10; n=34, 45Platelets:Week 12; n=24, 39Platelets:Week 14; n=24, 39Platelets:Week 16; n=24, 38Platelets:Week 28; n=64, 62
GSK3772847-0.0010.0050.0040.007-0.0010.0100.0100.0120.0060.007-0.038-0.051-0.119-0.119-0.096-0.041-0.066-0.034-0.093-0.0870.070.090.19-0.120.140.030.180.260.180.09-0.0080.0390.0610.0860.0330.1050.0440.1190.0750.1620.0920.0350.217-0.1260.3310.0410.1580.0730.142-0.0450.0150.0220.0270.0380.0230.0380.0250.0820.0530.0668.79.85.33.9-1.14.76.65.56.33.0
Placebo0.0010.0030.0050.0060.0020.0040.010-0.003-0.0050.006-0.031-0.050-0.048-0.023-0.0140.000-0.0390.018-0.0180.0100.140.010.240.370.080.010.13-0.17-0.41-0.080.0360.0060.0430.1400.1320.1030.0980.0090.020.0650.0790.0230.1870.203-0.080-0.192-0.013-0.263-0.448-0.2010.0260.0200.0510.0500.0450.0900.0730.0590.0400.0411.57.64.018.28.610.93.6-6.4-0.5-3.5

[back to top]

Change From Baseline in Hematology Parameter: Mean Corpuscular Hemoglobin Concentration

Blood samples were collected for the analysis of mean corpuscular hemoglobin concentration at indicated time points.Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
InterventionGrams per liter (Mean)
Week 1: n=78,74Week 2: n=71, 74Week 4: n=49, 57Week 6: n=44, 56Week 8: n=34, 47Week 10: n=34, 45Week 12: n=24, 39Week 14: n=24, 39Week 16: n=24, 39Week 28: n=65, 63
GSK37728470.50.21.51.31.13.43.22.45.71.5
Placebo0.8-0.61.21.93.03.32.30.42.11.2

[back to top]

Change From Baseline in Hematology Parameter: Mean Corpuscular Hemoglobin

Blood samples were collected for the analysis of mean corpuscular hemoglobin at indicated time points. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
InterventionPicogram (Mean)
Week 1: n=78,74Week 2: n=71, 74Week 4: n=49, 57Week 6: n=44, 56Week 8: n=34, 47Week 10: n=34, 45Week 12: n=24, 39Week 14: n=24, 39Week 16: n=24, 39Week 28: n=65, 63
GSK37728470.01-0.07-0.040.00-0.11-0.01-0.12-0.29-0.26-0.78
Placebo0.170.010.010.060.02-0.06-0.07-0.23-0.05-0.40

[back to top]

Change From Baseline in Hematology Parameter: Hemoglobin

Blood samples were collected for the analysis of hemoglobin level at indicated time points. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
InterventionGrams per liter (Mean)
Week 1: n=78,74Week 2: n=71, 74Week 4: n=49, 57Week 6: n=44, 56Week 8: n=34, 47Week 10: n=34, 45Week 12: n=24, 39Week 14: n=24, 39Week 16: n=24, 39Week 28: n=65, 63
GSK3772847-0.70.0-0.4-1.2-0.1-0.8-1.8-0.30.0-0.7
Placebo0.50.51.61.50.5-0.41.0-0.6-0.51.0

[back to top]

Change From Baseline in Hematology Parameter: Hematocrit Level

Blood samples were collected for the analysis of hematocrit at indicated time points. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
InterventionProportion of red blood cells in blood (Mean)
Week 1: n=78,74Week 2: n=71, 74Week 4: n=49, 57Week 6: n=44, 56Week 8: n=34, 47Week 10: n=34, 45Week 12: n=24, 39Week 14: n=24, 39Week 16: n=24, 39Week 28: n=65, 63
GSK3772847-0.0025-0.0046-0.0033-0.0050-0.0015-0.0061-0.0088-0.0038-0.0071-0.0041
Placebo0.00070.00240.00380.0024-0.0019-0.00500.0009-0.0018-0.00420.0016

[back to top]

Number of Participants Reporting Serious Adverse Events (SAEs) and Non-Serious Adverse Events (Non-SAEs)

A non-SAE is any untoward medical occurrence in a participant or clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment were categorized as SAE. (NCT03207243)
Timeframe: Up to Week 16

,
InterventionParticipants (Count of Participants)
non-SAESAE
GSK3772847192
Placebo201

[back to top]

Number of Participants With Incidence and Titres of Anti- GSK3772847 Antibodies

Blood samples were collected at given time points and the presence of anti-GSK3772847 antibodies were assessed using a a tiered approach including a screening assay, a confirmation assay and calculation of titer. Data for participants who showed positive results for confirmation assay has been presented (NCT03207243)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16, 20, 24 and 28

,
InterventionParticipants (Count of Participants)
Week2; n=73, 74Week4; n=49, 59Week8; n=34, 47Week12; n=24, 39Week16; n=23, 39Week20; n=73, 75Week24; n=74, 75Week28; n=74, 74
GSK377284700000000
Placebo00000100

[back to top]

Percent Change From Baseline in Fractional Exhaled Nitric Oxide (FeNO)

FeNO was assessed as a measure of airway inflammation using a handheld electronic device. The measurements recorded were according to standardized procedures by the American Thoracic Society and the European Respiratory Society Recommendations for Standardized Procedures for the Online and Offline Measurement of Exhaled Lower Respiratory Nitric Oxide and Nasal Nitric Oxide. FeNO measurements were obtained prior to FEV1 assessments. Participants did not use their rescue medication for at least 6 hours before each FeNO assessment, unless essential for clinical need. Baseline is defined as the latest available assessment prior to first dose (Day 1). Percent change from Baseline is calculated as ratio to Baseline minus one and multiplied by 100. Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 4, 6, 8, 10, 12, 14 and 16

,
InterventionPercent Change (Median)
Week1; n=60, 63Week2; n=58, 59Week4; n=41, 50Week6; n=34, 46Week8; n=29, 38Week10; n=29, 37Week12; n=19, 31Week14; n=19, 30Week16; n=13, 22
GSK3772847-4.90.03.30.0-2.90.08.81.712.7
Placebo-3.615.415.25.015.913.831.428.185.9

[back to top]

Percent Change From Baseline in Total Soluble ST2 Concentration

Blood samples were collected at given time points to measure total soluble ST2 concentration. Baseline is defined as the latest available assessment prior to first dose (Day 1). Analysis was performed using mixed model repeated measures. Percent change from Baseline is calculated as ratio to Baseline minus 1 and multiplied by 100. (NCT03207243)
Timeframe: Baseline and Week 4 (Pre-dose), Week 8 (Pre-dose), Week 12 (Pre-dose) and Week 16

,
InterventionPercent change (Number)
Week4; Pre-dose; n=48, 56Week8; Pre-dose; n=33, 45Week12; Pre-dose; n=23, 37Week16; n=16, 26
GSK37728472691.12326.91858.02330.8
Placebo16.3-6.9-13.4-12.0

[back to top]

Percent Change From Baseline in Free Soluble Suppressor of Tumorigenicity 2 (ST2) Concentration

Blood samples were collected at given time points to measure free soluble ST2 concentration. Baseline is defined as the latest available assessment prior to first dose (Day 1). Analysis was performed using mixed model repeated measures. Percent change from Baseline is calculated as ratio to Baseline minus 1 and multiplied by 100. (NCT03207243)
Timeframe: Baseline and Week 4 (Pre-dose), Week 8 (Pre-dose), Week 12 (Pre-dose) and Week 16

,
InterventionPercent change (Number)
Week4; Pre-dose; n=48, 56Week8; Pre-dose; n=33, 45Week12; Pre-dose; n=23, 37Week16; n=16, 26
GSK3772847-93.8-93.5-92.5-92.0
Placebo-5.6-8.510.519.8

[back to top] [back to top]

Percentage of Participants With at Least a 4 Units Improvement From Baseline of St. George's Respiratory Questionnaire (SGRQ)

SGRQ is a disease-specific questionnaire designed to measure impact of respiratory disease and its treatment on HRQoL of participants with COPD. It contains 14 questions with a total of 40 items grouped into domains (Symptoms, Activity and Impacts). SGRQ total score was calculated as 100 multiplied by summed weights from all positive items divided by sum of weights for all items in questionnaire. It ranges from 0 to 100, higher score indicates poor HRQoL. Baseline is defined as the latest available assessment prior to first dose (Day 1). A responder is defined as a change from Baseline of <= -4 at the given time point. Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 4, 8, 12 and 16

,
InterventionPercentage of participants (Number)
Week4; n=43, 52Week8; n=31, 42Week12; n=23, 35Week16; n=16, 26
GSK377284758677488
Placebo60617069

[back to top]

Change From Baseline in Hematology Parameter: Erythrocytes

Blood samples were collected for the analysis of erythrocytes at indicated time points. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
Intervention10^12 cells per liter (Mean)
Week 1: n=78,74Week 2: n=71, 74Week 4: n=49, 57Week 6: n=44, 56Week 8: n=34, 47Week 10: n=34, 45Week 12: n=24, 39Week 14: n=24, 39Week 16: n=24, 39Week 28: n=65, 63
GSK3772847-0.030.01-0.01-0.040.02-0.02-0.030.040.030.09
Placebo-0.010.010.050.050.020.000.060.030.000.09

[back to top]

Change From Baseline in Hematology Parameter: Erythrocyte Mean Corpuscular Volume

Blood samples were collected for the analysis of erythrocyte mean corpuscular volume at indicated time points.Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
InterventionFemtoliters (Mean)
Week 1: n=78,74Week 2: n=71, 74Week 4: n=49, 57Week 6: n=44, 56Week 8: n=34, 47Week 10: n=34, 45Week 12: n=24, 39Week 14: n=24, 39Week 16: n=24, 39Week 28: n=65, 63
GSK3772847-0.1-0.2-0.6-0.4-0.6-0.9-1.3-1.5-2.3-2.9
Placebo0.30.2-0.4-0.3-0.9-1.1-0.7-0.7-0.6-1.6

[back to top]

Change From Baseline in Diastolic Blood Pressure (DBP) and Systolic Blood Pressure (SBP)

DBP and SBP were measured in semi-supine position after 5 minutes rest. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. Data for change from Baseline for post dose values have been presented. (NCT03207243)
Timeframe: Baseline and Week 0 (Post-dose), Week1, Week 2, Week 4 (Pre and Post dose), Week 6, Week 8 (Pre and Post dose), Week 10, Week 12 (Pre and Post dose), Week 14, Week 16, Week 20, Week 24 and Week 28

,
InterventionMillimeters of Mercury (mmHg) (Mean)
SBP: Post-dose: Week0; n=82, 83SBP: Week1; n=79, 75SBP: Week2; n=73, 75SBP: Pre-dose: Week4; n=49, 59SBP: Post-dose: Week4; n=48, 59SBP:Week6; n=45, 57SBP: Pre-Dose:Week8; n=34, 47SBP: Post-DoseWeek8; n=34, 47SBP: Week10; n=34, 46SBP: Pre-dose: Week12; n=24, 39SBP: Post-dose: Week12; n=24, 39SBP: Week14; n=24, 39SBP: Week16; n=24, 39SBP: Week20; n=76, 78SBP: Week24; n=75, 76SBP: Week28; n=74, 77DBP: Post-dose: Week0; n=82,83DBP: Week1; n=79, 75DBP: Week2; n=73, 75DBP: Pre-dose: Week4; n=49, 59DBP: Post-dose: Week4; n=48, 59DBP:Week6; n=45, 57DBP: Pre-Dose:Week8; n=34, 47DBP: Post-DoseWeek8; n=34, 47DBP: Week10; n=34, 46DBP: Pre-dose: Week12; n=24, 39DBP: Post-dose: Week12; n=24, 39DBP: Week14; n=24, 39DBP: Week16; n=24, 39DBP: Week20; n=76, 78DBP: Week24; n=75, 76DBP: Week28; n=74, 77
GSK37728471.30.4-1.3-0.12.20.90.42.30.71.53.32.11.51.71.71.0-0.30.7-0.80.40.3-1.0-2.0-1.2-0.20.6-0.50.5-0.50.70.3-0.4
Placebo-2.0-0.9-1.3-2.0-2.0-1.7-1.9-2.7-2.50.3-0.7-1.6-2.8-1.0-2.4-1.3-0.70.3-0.7-1.1-0.40.6-0.4-0.1-0.10.30.00.0-0.3-0.40.1-0.3

[back to top]

Change From Baseline in ECG Heart Rate

Triplicate 12-lead ECGs were recorded pre-dose and post-dose with participant in semi-supine position after 5 minutes rest. At each time point ECG was taken using an ECG machine that automatically measures heart rate. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Week 0 (Post-dose), Week 4 (Pre and Post dose), Week 8 (Pre and Post dose), Week 12 (Pre and Post dose) and Week 16

,
InterventionBeats per minute (Mean)
Post-dose: Week0; n=82, 83Pre-dose: Week4; n=49, 59Post-dose: Week4; n=48, 59Pre-dose: Week8; n=34, 47Post-dose: Week8; n=33, 47Pre-dose:Week12; n=24, 39Post-dose Week12; n=24, 39Week16; n=24, 39
GSK37728470.20.7-1.01.9-0.41.60.53.1
Placebo-1.60.4-2.41.5-0.30.60.40.5

[back to top]

Change From Baseline in Clinical Chemistry Parameters: Total Protein and Albumin

Blood samples were collected at given time points to assess clinical chemistry parameters including total protein and albumin levels. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16 and 28

,
InterventionGrams per liter (Mean)
Total Protein: Week 2, n=72, 74Total Protein:Week 4, n=47,59Total Protein:Week 8, n=34,47Total Protein:Week 12, n=24, 36Total Protein:Week 16, n=24, 39Total Protein:Week 28, n=74, 73Albumin: Week 2, n=72, 74Albumin:Week 4, n=47,59Albumin:Week 8, n=34,47Albumin:Week 12, n=24, 36Albumin:Week 16, n=24, 39Albumin:Week 28, n=74, 73
GSK37728470.4-0.40.8-0.60.4-0.2-0.4-0.80.0-0.9-0.4-0.6
Placebo-0.5-0.40.10.20.5-0.8-0.5-0.5-0.4-0.3-0.1-0.6

[back to top]

Change From Baseline in Clinical Chemistry Parameters: Glucose, Potassium, Sodium, Calcium, Phosphate, Chloride, Urea and Carbon Dioxide (CO2)

Blood samples were collected at given time points to assess clinical chemistry parameters including glucose, potassium, sodium, calcium, Phosphate, chloride, urea and CO2 levels. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16 and 28

,
InterventionMillimoles per liter (Mean)
Glucose: Week 2; n=72, 74Glucose:Week 4; n=47,59Glucose:Week 8; n=34,47Glucose:Week 12; n=24, 36Glucose:Week 16; n=24, 39Glucose:Week 28; n=74, 73Potassium: Week 2; n=72, 74Potassium:Week 4; n=47,59Potassium:Week 8; n=34,47Potassium:Week 12; n=24, 36Potassium:Week 16; n=24, 39Potassium:Week 28; n=74, 73Sodium: Week 2; n=72, 74Sodium:Week 4; n=47,59Sodium:Week 8; n=34,47Sodium:Week 12; n=24, 36Sodium:Week 16; n=24, 39Sodium:Week 28; n=74, 73Calcium: Week 2; n=72, 74Calcium:Week 4; n=47,59Calcium:Week 8; n=34,47Calcium:Week 12; n=24, 36Calcium:Week 16; n=24, 39Calcium:Week 28; n=74, 73Phosphate: Week 2; n=72, 74Phosphate:Week 4; n=47,59Phosphate:Week 8; n=34,47Phosphate:Week 12; n=24, 36Phosphate:Week 16; n=24, 39Phosphate:Week 28; n=74, 73Chloride: Week 2; n=72, 74Chloride:Week 4; n=47,59Chloride:Week 8; n=34,47Chloride:Week 12; n=24, 36Chloride:Week 16; n=24, 39Chloride:Week 28; n=74, 73CO2: Week 2; n=72, 74CO2:Week 4; n=47,59CO2:Week 8; n=34,46CO2:Week 12; n=24, 36CO2:Week 16; n=24, 39CO2:Week 28; n=74, 73Urea: Week 2; n=72, 74Urea:Week 4; n=47,59Urea:Week 8; n=34,47Urea:Week 12; n=24, 36Urea:Week 16; n=24, 39Urea:Week 28; n=74, 73
GSK37728470.050.190.000.200.120.040.130.05-0.040.000.000.01-0.1-0.9-0.6-1.1-0.3-0.20.001-0.005-0.003-0.0040.0170.001-0.023-0.011-0.049-0.013-0.019-0.0180.1-0.30.0-0.3-0.20.70.40.3-0.3-0.10.10.3-0.14-0.140.27-0.060.030.16
Placebo0.130.180.26-0.04-0.100.300.140.04-0.010.02-0.090.010.30.0-0.1-0.3-0.20.5-0.006-0.013-0.0050.0180.0140.0010.0310.0030.0060.025-0.006-0.0130.30.0-0.2-0.1-0.40.6-0.4-0.4-0.3-0.5-0.5-0.10.080.16-0.040.580.480.08

[back to top]

Change From Baseline in Clinical Chemistry Parameters: Creatinine, Total Bilirubin and Direct Bilirubin

Blood samples were collected for the analysis of clinical chemistry parameters including total bilirubin, creatinine and direct bilirubin at indicated time points. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16 and 28

,
InterventionMicromoles per liter (Mean)
Creatinine: Week 2; n=72, 74Creatinine:Week 4; n=47, 59Creatinine:Week 8; n=34, 47Creatinine:Week 12; n=24, 36Creatinine:Week 16; n=24, 39Creatinine:Week 28; n=74, 73Total Bilirubin : Week 2; n=72, 74Total Bilirubin :Week 4; n=47, 59Total Bilirubin :Week 8; n=34, 47Total Bilirubin :Week 12; n=24, 36Total Bilirubin :Week 16; n=24, 39Total Bilirubin :Week 28; n=74, 74Direct bilirubin : Week 2; n=72, 74Direct bilirubin :Week 4; n=47,59Direct bilirubin :Week 8; n=34, 47Direct bilirubin :Week 12; n=24, 36Direct bilirubin :Week 16; n=24, 39Direct bilirubin :Week 28; n=74, 74
GSK37728471.710.721.760.020.912.90.1-0.4-0.20.1-0.3-0.50.00.10.20.20.10.1
Placebo2.352.351.182.422.504.32-0.1-0.3-0.1-0.60.00.1-0.1-0.1-0.1-0.40.10.1

[back to top]

Change From Baseline in Clinical Chemistry Parameter: Aspartate Aminotransferase (AST), Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Gamma- Glutamyl Transferase (GGT) and Creatine Kinase (CK)

Blood samples were collected for the analysis of clinical chemistry parameters including AST, ALT, ALP, GGT and CK at indicated time points. Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 2, 4, 8, 12, 16 and 28

,
InterventionInternational units per liter (Mean)
ALT: Week 2; n=72, 74ALT:Week 4; n=47,59ALT: Week 8; n=34,47ALT: Week 12; n=24, 36ALT: Week 16; n=24, 39ALT: Week 28; n=74, 74ALP: Week 2; n=72, 74ALP:Week 4; n=47, 59ALP:Week 8; n=34, 47ALP:Week 12; n =24, 36ALP:Week 16; n=24, 39ALP:Week 28; n=74, 74AST: Week 2; n=72, 74AST:Week 4; n=47,59AST:Week 8, n=34,47AST:Week 12, n=24, 36AST:Week 16, n=24, 39AST:Week 28, n=74, 74CK: Week 2, n=72, 74CK:Week 4, n=47,59CK:Week 8, n=34,47CK:Week 12, n=24, 36CK:Week 16, n=24, 39CK:Week 28, n=74, 74GGT: Week 2, n=72, 74GGT:Week 4, n=47,59GGT:Week 8, n=34,47GGT:Week 12, 24, 36GGT:Week 16, n=24, 39GGT:Week 28, n=74, 73
GSK3772847-0.2-2.6-2.4-2.4-2.6-0.9-0.8-1.0-2.3-3.0-2.3-1.2-1.5-2.5-2.7-4.1-3.3-1.7-18.8-45.1-32.9-54.5-46.8-30.7-1.2-2.5-2.8-5.4-3.9-0.7
Placebo-0.9-0.5-0.1-1.6-1.2-1.1-1.9-0.80.92.41.0-0.4-0.8-1.0-1.6-1.8-1.4-2.3-12.5-30.3-26.6-5.0-20.8-8.5-3.2-3.9-3.5-0.3-1.1-3.2

[back to top]

Change From Baseline in Cardiac Marker: N-Terminal ProB-type Natriuretic Peptide

Blood samples were collected for the analysis of N-Terminal ProB-type Natriuretic Peptide at indicated time points.Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
InterventionNanograms per liter (Mean)
Week 1: n=79,75Week 2: n=73,75Week 4: n=49, 59Week 6: n=45, 57Week 8: n=34, 47Week 10: n=34, 46Week 12: n=24, 38Week 14: n=24, 39Week 16: n=24, 39Week 28: n=65, 65
GSK37728478.4023-2.5196-4.55603.61949.650914.91198.853120.01494.77600.9810
Placebo-14.8442-10.8134-17.9849-5.0620-8.6398-12.7377-13.6951-4.8082-19.4899-6.1970

[back to top]

Change From Baseline in Cardiac Marker: Cardiac Troponin I

Blood samples were collected for the analysis of Troponin I at indicated time points.Baseline is defined as the most recent recorded value before dosing on Day 1. Change from Baseline was calculated by subtracting Baseline value from the specified time point value. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 4, 6, 8, 10, 12, 14, 16 and 28

,
InterventionMicrograms per liter (Mean)
Week 1: n=78,74Week 2: n=73, 73Week 4: n=49, 58Week 6: n=45, 57Week 8: n=34, 46Week 10: n=34, 38Week 12: n=24, 39Week 14: n=24, 39Week 16: n=24, 39Week 28: n=63, 63
GSK37728470.0000.0000.0000.0000.0000.0000.0000.0000.000-0.001
Placebo0.0000.0000.0010.0000.0000.0060.0000.0000.0000.000

[back to top]

Change From Baseline in Asthma Control Questionnaire (ACQ-5) Total Score

ACQ-5 is a five-item, self-completed questionnaire, which measures asthma control of a participant. The five questions (concerning nocturnal awakening, waking in the morning, activity limitation, shortness of breath & wheeze) enquire about the frequency &/or severity of symptoms over the previous week. The response options range from zero (no impairment/limitation) to six (total impairment/limitation) scale. ACQ-5 score ranges from 0 (totally controlled) to 6 (severely uncontrolled). Higher score indicate lower asthma control. Baseline is the latest available assessment prior to first dose (Day 1). Change from Baseline was calculated by subtracting Baseline value from the specified time point value. Data is presented for primary estimand which includes all data collected, except for data collected after the date of loss of asthma control or early withdrawal from study treatment. (NCT03207243)
Timeframe: Baseline and Weeks 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 and Week 16

,
InterventionScores on a scale (Mean)
Week1; n=72, 73Week2; n=67, 68Week3; n=61, 61Week4; n=54, 59Week5; n= 42, 52Week6; n=40, 48Week7; n=34, 46Week8; n=33, 44Week9; n=30, 42Week10; n=29, 41Week11; n=22, 38Week12; n=23, 38Week13; n=17,32Week14; n=17, 31Week15; n=17, 27Week16; n=12, 21
GSK3772847-0.48-0.74-0.78-0.79-0.78-0.93-0.93-1.00-0.97-0.99-1.07-1.16-1.06-1.14-1.21-1.17
Placebo-0.36-0.53-0.59-0.69-0.80-0.80-0.92-0.95-0.93-0.97-1.05-0.88-1.40-1.33-1.22-1.15

[back to top]

Peak 0-3 Hours Forced Expiratory Volume in One Second (FEV1) Response (Change From Baseline) [L] After 12 Weeks Treatment

Peak 0-3 hours Forced Expiratory Volume in one second (FEV1) response (change from baseline) [L] after 12 weeks treatment. Peak 0-3h was defined as the maximum value measured within the first three hours post doing. (NCT03240575)
Timeframe: 30 minutes, 1 h, 2h and 3h post dose at baseline and week 12.

InterventionLitre (L) (Mean)
Tiotropium+Olodaterol (5μg/5μg) - Main Study0.341
Fluticasone Propionate+Salmeterol (500μg/100μg) - Main Study0.243
Tiotropium+Olodaterol (5μg/5μg) - DH-studyNA
Fluticasone Propionate+Salmeterol (500μg/100μg) - DH-studyNA

[back to top]

Forced Expiratory Volume in One Second (FEV1) Area Under the Curve From 0 to 24 Hours (AUC0-24) Response (Change From Baseline) [L] After 12 Weeks of Treatment

Forced Expiratory Volume in one second (FEV1) Area under the Curve from 0 to 24 hours (AUC0-24) response (change from baseline) [L] after 12 weeks of treatment. FEV1 AUC0-24 was calculated as the area under the FEV1-time curve from 0-24 hours post-dose using the trapezoidal rule, divided by the duration (24 hours) and reported in liters. FEV1 AUC0-24 response (change from baseline) was defined as FEV1 AUC0-24 mius baseline FEV1. (NCT03240575)
Timeframe: 1 hours (h) and 10 minutes (min) before first dose at day1 of weeks 1 for baseline.10 min before and 30 min, 1 h, 2h, 3h, 4h, 6h, 8h, 10h, 11h 50min, 12h 30 min, 13h, 14h, 22h, 23h, and 24h post morning dose at week 12.

InterventionLitre*hours (L*h) (Mean)
Tiotropium+Olodaterol (5μg/5μg) - Main Study0.174
Fluticasone Propionate+Salmeterol (500μg/100μg) - Main Study0.122
Tiotropium+Olodaterol (5μg/5μg) - DH-studyNA
Fluticasone Propionate+Salmeterol (500μg/100μg) - DH-studyNA

[back to top]

Forced Expiratory Volume in One Second (FEV1) Area Under the Curve From 0 to 12 Hours (AUC0-12) Response (Change From Baseline) [L] After 12 Weeks of Treatment

"Forced Expiratory Volume in one second (FEV1) Area under the Curve from 0 to 12 hours (AUC0-12) response (change from baseline) [L] after 12 weeks of treatment.~FEV1 AUC0-12 was calculated as the area under the FEV1-time curve from 0-12 hours post-dose using the trapezoidal rule, divided by the duration (12 hours) and reported in liters. FEV1 AUC0-12 response (change from baseline) was defined as FEV1 AUC0-12 minus baseline FEV1." (NCT03240575)
Timeframe: 1 hours (h) and 10 minutes (min) before first dose at day1 of weeks 1 for baseline. 10 min before and 30 min, 1 h, 2h, 3h, 4h, 6h, 8h, 10h, 11h 50min post morning dose at week 12.

InterventionLitre*hours (L*h) (Mean)
Tiotropium+Olodaterol (5μg/5μg) - Main Study0.237
Fluticasone Propionate+Salmeterol (500μg/100μg) - Main Study0.147
Tiotropium+Olodaterol (5μg/5μg) - DH-studyNA
Fluticasone Propionate+Salmeterol (500μg/100μg) - DH-studyNA

[back to top]

Trough Forced Expiratory Volume in One Second (FEV1) Response (Change From Baseline) [L] After 12 Weeks Treatment

Trough Forced Expiratory Volume in one second (FEV1) response (change from baseline) [L] after 12 weeks treatment. Trough FEV1 was defined as the mean of the FEV1 value measured at 23 hours and at 24 hours after the trial medication administration. Through FEV1 response (change from baseline) was defined as trough FEV1 minus baseline FEV1. (NCT03240575)
Timeframe: At 23 h and 24 h post dose at baseline and at 23h and 24 h post dose at week 12.

InterventionLitre (L) (Mean)
Tiotropium+Olodaterol (5μg/5μg) - Main Study0.118
Fluticasone Propionate+Salmeterol (500μg/100μg) - Main Study0.114
Tiotropium+Olodaterol (5μg/5μg) - DH-studyNA
Fluticasone Propionate+Salmeterol (500μg/100μg) - DH-studyNA

[back to top]

Percentage of Participants With Loss of Asthma Control

An LOAC event during the 12-week treatment period was a deterioration of asthma defined as any of the following: a) 30 percent (%) or greater reduction from baseline in morning peak expiratory flow (PEF) on 2 consecutive days; b) greater than or equal to (>=) 6 additional reliever puffs of salbutamol/albuterol or levosalbutamol/levalbuterol in a 24-hour period (compared to baseline) on 2 consecutive days; c) increase in inhaled corticosteroid (ICS) >=4 times the last prescribed ICS dose (or >=50% of the prescribed ICS dose at Baseline if background therapy withdrawal completed); d) required use of systemic (oral and/or parenteral) steroid treatment; e) required hospitalization or emergency room visit. (NCT03387852)
Timeframe: From Baseline up to Week 12

Interventionpercentage of participants (Number)
Placebo40.5
SAR440340 300 mg21.9
SAR440340 + Dupilumab27.0
Dupilumab 300 mg18.9

[back to top]

Change From Baseline at Week 12 in Pre-bronchodilator Forced Expiratory Volume in 1 Second (FEV1)

FEV1 was the volume of air exhaled in the first second of a forced expiration as measured by spirometer. Pre-bronchodilator FEV1 refers to the spirometry performed after a wash period of bronchodilators (i.e., not earlier than 6 hours) after the last dose of albuterol/salbutamol or levalbuterol/levosalbutamol from a primed meter dose inhaler and withholding the last dose of long-acting β2 adrenergic agonist (LABA) for at least 12 hours, and prior to administration of study drug. (NCT03387852)
Timeframe: Baseline, Week 12

Interventionliters (Mean)
Placebo0.06
SAR440340 300 mg0.11
SAR440340 + Dupilumab0.06
Dupilumab 300 mg0.14

[back to top]

Change From Baseline at Week 12 in Post-bronchodilator Forced Expiratory Volume in 1 Second

FEV1 was the volume of air exhaled in the first second of a forced expiration as measured by spirometer. Post-bronchodilator FEV1 refers to the spirometry performed within 30 minutes after administration of bronchodilator. (NCT03387852)
Timeframe: Baseline, Week 12

Interventionliters (Mean)
Placebo-0.02
SAR440340 300 mg-0.00
SAR440340 + Dupilumab0.06
Dupilumab 300 mg0.09

[back to top]

Baseline-adjusted Pre-dose FEV1 Measured in the Morning Following 28 Days of Treatment.

Baseline-adjusted pre-dose FEV1 measured in the morning following 28 days of treatment. Only the active treatments (test and reference) are compared in this analysis. The placebo arm was used in superiority analysis only. (NCT03756883)
Timeframe: 28 days

InterventionLiters (Least Squares Mean)
Test0.33
Reference0.34

[back to top]

Statistical Superiority of Test and Reference Over Placebo Treatment in Baseline-adjusted Area Under the Serial FEV1-time Curve

Statistical Superiority of Test and Reference over Placebo Treatment in Baseline-adjusted area under the serial FEV1-time curve (NCT03756883)
Timeframe: 12 hours

Interventionliters x hours (Least Squares Mean)
Test4.02
Reference3.94
Placebo1.21

[back to top]

Statistical Superiority of Test and Reference Over Placebo Treatment in Baseline-adjusted Pre-dose FEV1 Measured in the Morning Following 28 Days of Treatment

Statistical Superiority of Test and Reference over Placebo Treatment in Baseline-adjusted pre-dose FEV1 measured in the morning following 28 days of treatment (NCT03756883)
Timeframe: 28 days

InterventionLiters (Least Squares Mean)
Test0.33
Reference0.33
Placebo0.11

[back to top]

Baseline-adjusted Area Under the Serial FEV1-time Curve Calculated From Time Zero to 12 Hours (AUC0-12h) on Day 1 of Treatment

Baseline-adjusted area under the serial FEV1-time curve calculated from time zero to 12 hours (AUC0-12h) on Day 1 of treatment. LSMeans will be used for the statistical analysis. Only the active treatments (test and reference) are compared in this analysis. The placebo arm was used in superiority analysis only. (NCT03756883)
Timeframe: 12 hours

Interventionliters x hours (Least Squares Mean)
Test4.03
Reference3.96

[back to top]

Adherence of Asthma Controller Medication

Adherence was measured using the Propeller Health Inhaler monitor and web-based software management platform that tracks adherence of asthma medications. The change in adherence was calculated between V1 (baseline) to V3 (12 Months). (NCT04179461)
Timeframe: Baseline to 12 months

Interventionpercentage of medication taken (Median)
V1V3
Personalized Treatment4236

[back to top]

Pulmonary Function Measured by Spirometry: Forced Expiratory Volume in 1 Second (FEV1) / Forced Vital Capacity (FVC)

"FEV1 is air volume exhaled in 1 second during spirometry. Forced vital capacity is the amount of air that can be forcibly exhaled from the lungs after taking the deepest breath possible. The change in FEV1/FVC was calculated between V1 (Baseline), V2 (Guideline Care - before intervention), and V3 (12 Months). This will be used as a measurement in asthma severity.~[A lower FEV1/FVC ratio indicates more severe asthma]" (NCT04179461)
Timeframe: Baseline to 12 months

InterventionRatio (Median)
V1V2V3
Personalized Treatment0.810.80.8

[back to top]

Change in Composite Asthma Severity Index (CASI)

"CASI was measured by questionnaire and is a severity score of symptom burden, exacerbations, healthcare utilization, lung function and dose of inhaled corticosteroids. The change in CASI score was calculated between V1 (Baseline), V2 (Guideline Care - before intervention), and V3 (12 Months).~[The CASI score has a minimum value = 0, maximum value = 20, a higher score indicates greater asthma severity]" (NCT04179461)
Timeframe: Baseline to 12 months

Interventionscore on a scale (Median)
V1V2V3
Personalized Treatment555

[back to top]

Asthma Control Test (ACT)

"ACT was measured by questionnaire, assessing frequency of reported asthma symptoms, rescue medication use, the effect of asthma on daily functioning, and overall asthma control. The change in ACT score was calculated between V1 (Baseline), V2 (Guideline Care - before intervention), and V3 (12 Months).~[The ACT score has a minimum value = 5, maximum value = 25, a score 19 indicates well-controlled asthma]" (NCT04179461)
Timeframe: Baseline to 12 months

Interventionscore on a scale (Median)
V1V2V3
Personalized Treatment23.021.722.5

[back to top]

Number of Participants With Adverse Events (AEs)

An AE was defined as any untoward medical occurrence that develops or worsens in severity during the conduct of a clinical study and does not necessarily have a causal relationship to the study drug. SAEs included death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, or an important medical event that jeopardized the participant and required medical intervention to prevent 1 of the outcomes listed in this definition. A summary of serious and non-serious AEs regardless of causality is located in 'Reported Adverse Events module'. Number of participants with any AEs, and device-related AEs has been reported. (NCT04677959)
Timeframe: Baseline up to Week 26

,
InterventionParticipants (Count of Participants)
Any AEsDevice-related AEs
Digital System (DS)773
Standard of Care (SoC)560

[back to top]

Change From Baseline in Work Productivity and Activity Impairment (WPAI) Asthma Questionnaire Score at Week 24

WPAI-asthma is a self-administered instrument to measure asthma-specific performance impairment of work and regular daily activity within the last 7 days and yields 4 types of scores: work time missed (absenteeism), impairment while working (presenteeism or reduced on-the-job effectiveness), overall work impairment (WI) (work productivity loss or absenteeism plus presenteeism) and activity impairment (daily activity impairment). Total score and each score ranged from 0 (not affected/no impairment) to 100 (completely affected/impaired). Higher scores indicated greater impairment and less productivity. (NCT04677959)
Timeframe: Baseline, Week 24

,
Interventionunits on a scale (Mean)
AbsenteeismPresenteeismWork productivity lossActivity impairment
Digital System (DS)-0.05-10.43-9.87-15.33
Standard of Care (SoC)-3.56-10.98-12.18-11.22

[back to top]

Number of Participants Achieving Well-Controlled Asthma or Reaching Clinically Important Improvement in Asthma Control

A well-controlled asthma was defined as an Asthma Control Test (ACT) score of greater than or equal to 20. Clinically important improvement in asthma control was defined by an increase of at least 3 ACT units from baseline. The ACT was a simple, participant-completed tool used for the assessment of overall asthma control. The ACT included 5 items that assessed daytime and nighttime asthma symptoms, use of reliever medication, and impact of asthma on daily functioning. Each item in the ACT was scored on a 5-point scale ranging from 1 (poor control of asthma) to 5 (well control of asthma), with summation of all items providing scores ranging from 5 to 25. The scores span the continuum of poor control of asthma (score of 5) to complete control of asthma (score of 25), with a cutoff score of 19 and below indicating participants with poorly controlled asthma. (NCT04677959)
Timeframe: Week 24

InterventionParticipants (Count of Participants)
Standard of Care (SoC)112
Digital System (DS)134

[back to top]

Number of Decreased Doses of Inhaled Medication

Number of participants who received decreased dose of inhaled medication during the 24-week treatment period are reported. (NCT04677959)
Timeframe: Baseline up to Week 24

InterventionParticipants (Count of Participants)
Standard of Care (SoC)0
Digital System (DS)0

[back to top]

Change From Baseline in the Number of SABA-free Days at Week 24 for the DS Group

Number of days a participant did not use the rescue medication in a week are reported. (NCT04677959)
Timeframe: Baseline, Week 24

Interventiondays (Mean)
Digital System (DS)0.4

[back to top]

Change From Baseline in Mean Weekly SABA Usage at Week 24 for the DS Group

(NCT04677959)
Timeframe: Baseline, Week 24

Interventionmicrograms (μg) (Mean)
Digital System (DS)-12.26

[back to top]

Change From Baseline in Brief Illness Perception Questionnaire (BIPQ) Illness Comprehensibility Subscale Score at Week 24

The BIPQ was a 9-item questionnaire designed to rapidly assess cognitive and emotional representations of illness. Only one item assesses illness comprehensibility or coherence of illness (Item 7: How well do you feel you understand your illness?). This item was rated using a 0 (do not understand at all) to 10 (understand very clearly) response scale. A higher score indicates a stronger illness comprehensibility. (NCT04677959)
Timeframe: Baseline, Week 24

Interventionunits on a scale (Mean)
Standard of Care (SoC)-0.0
Digital System (DS)0.1

[back to top]

Change From Baseline in BIPQ Emotional Representations Subscale Score at Week 24

BIPQ was a 9-item questionnaire designed to rapidly assess cognitive and emotional representations of illness. It comprised 2 items on emotional representation: concern (Item 6: How concerned are you about your illness? Response range 0 [not at all concerned] - 10 [extremely concerned]) and emotions (Item 8: How much does your illness affect you emotionally; for example, does it make you angry, scared, upset or depressed? Response range 0 [not at all affected emotionally] - 10 [extremely affected emotionally]). Total BIPQ Emotional Subscale Score was the sum of above 2 items score and ranged from 0 to 20. A higher score indicates extreme emotional representation. (NCT04677959)
Timeframe: Baseline, Week 24

Interventionunits on a scale (Mean)
Standard of Care (SoC)-1.1
Digital System (DS)-1.3

[back to top]

Change From Baseline in BIPQ Cognitive Subscale Score at Week 24

BIPQ was a 9-item questionnaire designed to rapidly assess cognitive and emotional representations of illness. It comprised 5 items on cognitive representation of illness perception: consequences (Item 1: How much does your illness affect your life? Response range 0 [no affect] - 10 [severe affect]), timeline (Item 2: How long do you think your illness will continue? Response range 0 [a very short time] - 10 [forever]), personal control (Item 3: How much control do you feel you have over your illness? Response range 0 [no control] - 10 [extreme amount of control]), treatment control (Item 4: How much do you think your treatment can help your illness? Response range 0 [not at all] - 10 [extremely helpful]), and identity (Item 5: How much do you experience symptoms from your illness? Response range 0 [no symptoms] - 10 [severe symptoms]). Total BIPQ Cognitive Subscale Score was the sum of all item score and ranged from 0 to 50. A higher score indicates stronger illness perception. (NCT04677959)
Timeframe: Baseline, Week 24

Interventionunits on a scale (Mean)
Standard of Care (SoC)-2.5
Digital System (DS)-3.3

[back to top]

Change From Baseline in Adherence to Maintenance Treatment (FS eMDPI) at Week 24 for the DS Group

Adherence to maintenance treatment was defined as the percentage of actual inhalation doses taken out of the total number of inhalation doses prescribed over the 24- week treatment period. (NCT04677959)
Timeframe: Baseline, Week 24

Interventionpercentage of inhalation (Mean)
Digital System (DS)-10.87

[back to top]

Change From Baseline in BMQ Necessity Subscale Score at Week 24

The BMQ was used to assess cognitive representations of medicine. The Beliefs About Medicines Questionnaire-Specific 11 (BMQ-S11) was an 11-item questionnaire that assessed the representation of medication prescribed for personal use and the BMQ-General assesses beliefs about medicines in general. BMQ necessity is a 5-item scale assessing participant's beliefs about necessity of medications for controlling disease. Participants indicated degree of agreement on a 5-point scale, ranging from 1=strongly disagree to 5=strongly agree. Scores obtained for individual items were summed, divided by the total number of items and multiplied by 5 to give a total score ranging from 5 to 25 (higher scores=stronger beliefs). (NCT04677959)
Timeframe: Baseline, Week 24

Interventionunits on a scale (Mean)
Standard of Care (SoC)-0.4
Digital System (DS)-1.3

[back to top]

Change From Baseline in Beliefs About Medicines Questionnaire (BMQ) Concern Subscale Score at Week 24

The BMQ was used to assess cognitive representations of medicine. The Beliefs About Medicines Questionnaire-Specific 11 (BMQ-S11) was an 11-item questionnaire that assessed the representation of medication prescribed for personal use and the BMQ-General assesses beliefs about medicines in general. BMQ concern is a 6-item scale assessing participant's concerns about potential adverse consequences (range: 1=strongly disagree to 5=strongly agree). Participants indicated their degree of agreement on a 5-point scale, ranging from 1=strongly disagree to 5=strongly agree. Scores obtained for individual items were summed, divided by the total number of items and multiplied by 5 to give a total score ranging from 5 to 25 (higher scores=stronger beliefs). (NCT04677959)
Timeframe: Baseline, Week 24

Interventionunits on a scale (Mean)
Standard of Care (SoC)-0.8
Digital System (DS)-0.9

[back to top]

System Usability Scale (SUS) Overall Score for DS Group

The SUS was used to explore device acceptability and usability for participants in the DS group. It covered a variety of aspects of system usability, such as the need for support, training, and complexity, and thus giving a global view of subjective assessments of usability. It was a 10-question tool (with five response options; from 1=strongly disagree to 5=strongly agree) that provided a composite measure, ranging from 0 to 100, of the overall usability of the system being studied. Higher scores represent better usability level for the tool. (NCT04677959)
Timeframe: Week 24

Interventionunits on a scale (Mean)
SUS Overall Score (completed by participants)Site SUS Overall Score (completed by site)
Digital System (DS)70.073.2

[back to top]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		2.07106-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
quinacrine
Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.. quinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9.		2.0510acridines;
aromatic ether;
organochlorine compound;
tertiary amino compound		antimalarial;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
beta-alanine
[no description available]		2.0710amino acid zwitterion;
beta-amino acid		agonist;
fundamental metabolite;
human metabolite;
inhibitor;
neurotransmitter
benzene
[no description available]		4.811aromatic annulene;
benzenes;
volatile organic compound		carcinogenic agent;
environmental contaminant;
non-polar solvent
1-butanol
1-Butanol: A four carbon linear hydrocarbon that has a hydroxy group at position 1.. butan-1-ol : A primary alcohol that is butane in which a hydrogen of one of the methyl groups is substituted by a hydroxy group. It it produced in small amounts in humans by the gut microbes.		1.9910alkyl alcohol;
primary alcohol;
short-chain primary fatty alcohol		human metabolite;
mouse metabolite;
protic solvent
carbamates
[no description available]		6.3442amino-acid anion
carbon monoxide
Carbon Monoxide: Carbon monoxide (CO). A poisonous colorless, odorless, tasteless gas. It combines with hemoglobin to form carboxyhemoglobin, which has no oxygen carrying capacity. The resultant oxygen deprivation causes headache, dizziness, decreased pulse and respiratory rates, unconsciousness, and death. (From Merck Index, 11th ed). carbon monoxide : A one-carbon compound in which the carbon is joined only to a single oxygen. It is a colourless, odourless, tasteless, toxic gas.		3.4611carbon oxide;
gas molecular entity;
one-carbon compound		biomarker;
EC 1.9.3.1 (cytochrome c oxidase) inhibitor;
human metabolite;
ligand;
metabolite;
mitochondrial respiratory-chain inhibitor;
mouse metabolite;
neurotoxin;
neurotransmitter;
P450 inhibitor;
probe;
signalling molecule;
vasodilator agent
aminooxyacetic acid
Aminooxyacetic Acid: A compound that inhibits aminobutyrate aminotransferase activity in vivo, thereby raising the level of gamma-aminobutyric acid in tissues.. (aminooxy)acetic acid : A member of the class of hydroxylamines that is acetic acid substituted at postion 2 by an aminooxy group. It is a compound which inhibits aminobutyrate aminotransferase activity in vivo, resulting in increased levels of gamma-aminobutyric acid in tissues.		2.0510amino acid;
hydroxylamines;
monocarboxylic acid		anticonvulsant;
EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor;
EC 4.2.1.22 (cystathionine beta-synthase) inhibitor;
nootropic agent
catechol
[no description available]		2.4520catecholsallelochemical;
genotoxin;
plant metabolite
chlorine
chloride : A halide anion formed when chlorine picks up an electron to form an an anion.		2.0510halide anion;
monoatomic chlorine		cofactor;
Escherichia coli metabolite;
human metabolite
coumarin
2H-chromen-2-one: coumarin derivative		7.1710coumarinsfluorescent dye;
human metabolite;
plant metabolite
salicylic acid
Scalp: The outer covering of the calvaria. It is composed of several layers: SKIN; subcutaneous connective tissue; the occipitofrontal muscle which includes the tendinous galea aponeurotica; loose connective tissue; and the pericranium (the PERIOSTEUM of the SKULL).		2.0510monohydroxybenzoic acidalgal metabolite;
antifungal agent;
antiinfective agent;
EC 1.11.1.11 (L-ascorbate peroxidase) inhibitor;
keratolytic drug;
plant hormone;
plant metabolite
taxifolin
[no description available]		2.05103'-hydroxyflavanones;
4'-hydroxyflavanones;
dihydroflavonols;
pentahydroxyflavanone;
secondary alpha-hydroxy ketone
phosphonoacetic acid
Phosphonoacetic Acid: A simple organophosphorus compound that inhibits DNA polymerase, especially in viruses and is used as an antiviral agent.. phosphonoacetic acid : A member of the class of phosphonic acids that is phosphonic acid in which the hydrogen attached to the phosphorous is replaced by a carboxymethyl group.		2.0510monocarboxylic acid;
phosphonic acids		antiviral agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor
3,4-dihydroxyphenylacetic acid
3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.. (3,4-dihydroxyphenyl)acetic acid : A dihydroxyphenylacetic acid having the two hydroxy substituents located at the 3- and 4-positions. It is a metabolite of dopamine.. dihydroxyphenylacetic acid : A dihydroxy monocarboxylic acid consisting of phenylacetic acid having two phenolic hydroxy substituents.		2.0510catechols;
dihydroxyphenylacetic acid		human metabolite
aminocaproic acid
Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator.		2.0510amino acid zwitterion;
epsilon-amino acid;
omega-amino fatty acid		antifibrinolytic drug;
hematologic agent;
metabolite
lactic acid
Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.		4.11312-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
glycine
[no description available]		6.6154alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
dalteparin
Dalteparin: A low-molecular-weight fragment of heparin, prepared by nitrous acid depolymerization of porcine mucosal heparin. The mean molecular weight is 4000-6000 daltons. It is used therapeutically as an antithrombotic agent. (From Merck Index, 11th ed)		3.4111
histamine
[no description available]		8.681811aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter
hydroquinone
[no description available]		2.0510benzenediol;
hydroquinones		antioxidant;
carcinogenic agent;
cofactor;
Escherichia coli metabolite;
human xenobiotic metabolite;
mouse metabolite;
skin lightening agent
methanol
Methanol: A colorless, flammable liquid used in the manufacture of FORMALDEHYDE and ACETIC ACID, in chemical synthesis, antifreeze, and as a solvent. Ingestion of methanol is toxic and may cause blindness.. primary alcohol : A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.. methanol : The primary alcohol that is the simplest aliphatic alcohol, comprising a methyl and an alcohol group.		210alkyl alcohol;
one-carbon compound;
primary alcohol;
volatile organic compound		amphiprotic solvent;
Escherichia coli metabolite;
fuel;
human metabolite;
mouse metabolite;
Mycoplasma genitalium metabolite
melatonin
[no description available]		2.0810acetamides;
tryptamines		anticonvulsant;
central nervous system depressant;
geroprotector;
hormone;
human metabolite;
immunological adjuvant;
mouse metabolite;
radical scavenger
nickel
Nickel: A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.. nickel ion : A nickel atom having a net electric charge.. nickel atom : Chemical element (nickel group element atom) with atomic number 28.		4.811metal allergen;
nickel group element atom		epitope;
micronutrient
nitrates
Nitrates: Inorganic or organic salts and esters of nitric acid. These compounds contain the NO3- radical.		3.411monovalent inorganic anion;
nitrogen oxoanion;
reactive nitrogen species
nitroxyl
nitroxyl: hydroxamic acid oxidized to nitroxyl free radical. nitroxyl : A nitrogen oxoacid consisting of an oxygen atom double-bonded to an NH group.		4.811nitrogen oxoacid
pyrazinamide
pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.		2.0810monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug
sulfites
Sulfites: Inorganic salts of sulfurous acid.. sulfites : Any sulfurous acid derivative that is a salt or an ester of sulfurous acid.. organosulfonate oxoanion : An organic anion obtained by deprotonation of the sufonate group(s) of any organosulfonic acid.. sulfite : A sulfur oxoanion that is the conjugate base of hydrogen sulfite (H2SO3).		2.0510divalent inorganic anion;
sulfur oxide;
sulfur oxoanion
succinic acid
Succinic Acid: A water-soluble, colorless crystal with an acid taste that is used as a chemical intermediate, in medicine, the manufacture of lacquers, and to make perfume esters. It is also used in foods as a sequestrant, buffer, and a neutralizing agent. (Hawley's Condensed Chemical Dictionary, 12th ed, p1099; McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed, p1851). succinic acid : An alpha,omega-dicarboxylic acid resulting from the formal oxidation of each of the terminal methyl groups of butane to the corresponding carboxy group. It is an intermediate metabolite in the citric acid cycle.		4.811alpha,omega-dicarboxylic acid;
C4-dicarboxylic acid		anti-ulcer drug;
fundamental metabolite;
micronutrient;
nutraceutical;
radiation protective agent
sulfuric acid
sulfuric acid : A sulfur oxoacid that consists of two oxo and two hydroxy groups joined covalently to a central sulfur atom.		2.1710sulfur oxoacidcatalyst
sulfur dioxide
Sulfur Dioxide: A highly toxic, colorless, nonflammable gas. It is used as a pharmaceutical aid and antioxidant. It is also an environmental air pollutant.		4.6632sulfur oxideEscherichia coli metabolite;
food bleaching agent;
refrigerant
toluene
methylbenzene : Any alkylbenzene that is benzene substituted with one or more methyl groups.		4.811methylbenzene;
toluenes;
volatile organic compound		cholinergic antagonist;
fuel additive;
neurotoxin;
non-polar solvent
uracil
2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder		2.1310pyrimidine nucleobase;
pyrimidone		allergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
prodrug;
Saccharomyces cerevisiae metabolite
uric acid
Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.. uric acid : An oxopurine that is the final oxidation product of purine metabolism.. 6-hydroxy-1H-purine-2,8(7H,9H)-dione : A tautomer of uric acid having oxo groups at C-2 and C-8 and a hydroxy group at C-6.. 7,9-dihydro-1H-purine-2,6,8(3H)-trione : An oxopurine in which the purine ring is substituted by oxo groups at positions 2, 6, and 8.		4.811uric acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		5.8132isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
sk&f-38393
2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.. 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol : A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine bearing a phenyl substituent at position 1 and two hydroxy substituents at positions 7 and 8.. SKF 38393 : A racemate comprising equimolar amounts of (R)- and (S)-SKF 38393		2.0510benzazepine;
catechols;
secondary amino compound
1,10-diaminodecane
[no description available]		2.0510
1,3-dipropyl-8-cyclopentylxanthine
DPCPX : An oxopurine that is 7H-xanthine substituted at positions 1 and 3 by propyl groups and at position 8 by a cyclohexyl group.		2.0510oxopurineadenosine A1 receptor antagonist;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
pk 11195
PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine		2.0510aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes		antineoplastic agent
1-(3-chlorophenyl)piperazine
1-(3-chlorophenyl)piperazine: supposed metabolite of TRAZODONE; RN given refers to parent cpd; structure. 1-(3-chlorophenyl)piperazine : A N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone.		2.0810monochlorobenzenes;
N-arylpiperazine		drug metabolite;
environmental contaminant;
serotonergic agonist;
xenobiotic
1-aminobenzotriazole
[no description available]		2.0510
1h-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one
1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one: structure given in first source; inhibits guanylyl cyclase. 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one : A member of the class of oxadiazoloquinoxalines that is 1H-[1,2,4]oxadiazolo[4,3-a]quinoxaline substituted at position 1 by an oxo group.		2.0510oxadiazoloquinoxalineEC 4.6.1.2 (guanylate cyclase) inhibitor
2,2'-dipyridyl
2,2'-Dipyridyl: A reagent used for the determination of iron.. 2,2'-bipyridine : A bipyridine in which the two pyridine moieties are linked by a bond between positions C-2 and C-2'.		2.0510bipyridinechelator;
ferroptosis inhibitor
2,4,5-trichlorophenoxyacetic acid
2,4,5-Trichlorophenoxyacetic Acid: An herbicide with strong irritant properties. Use of this compound on rice fields, orchards, sugarcane, rangeland, and other noncrop sites was terminated by the EPA in 1985. (From Merck Index, 11th ed). (2,4,5-trichlorophenoxy)acetic acid : A chlorophenoxyacetic acid that is phenoxyacetic acid in which the ring hydrogens at postions 2, 4 and 5 are substituted by chlorines.		2.0210chlorophenoxyacetic acid;
trichlorobenzene		defoliant;
phenoxy herbicide;
synthetic auxin
3,4-dichloroisocoumarin
3,4-dichloroisocoumarin : A member of the class of isocoumarins that is isocoumarin substituted by chloro groups at positions 3 and 4. It is a serine protease inhibitor.		2.0510isocoumarins;
organochlorine compound		geroprotector;
serine protease inhibitor
cgp 52411
4,5-dianilinophthalimide: structure given in first source. 4,5-dianilinophthalimide : Phthalimide substituted at the 4- and 5-positions by anilino groups.		2.0510phthalimidesgeroprotector;
tyrosine kinase inhibitor
4-amino-1,8-naphthalimide
4-amino-1,8-naphthalimide: inhibits ADP-ribosylation; sometimes abreviated as 4-AN;		2.0510benzoisoquinoline;
dicarboximide
homovanillic acid
Homovanillic Acid: A 3-O-methyl ETHER of (3,4-dihydroxyphenyl)acetic acid.. homovanillate : A hydroxy monocarboxylic acid anion which is obtained by deprotonation of the carboxy group of homovanillic acid.. homovanillic acid : A monocarboxylic acid that is the 3-O-methyl ether of (3,4-dihydroxyphenyl)acetic acid. It is a catecholamine metabolite.		2.0510guaiacols;
monocarboxylic acid		human metabolite;
mouse metabolite
4-phenyl-3-furoxancarbonitrile
4-phenyl-3-furoxancarbonitrile: structure given in first source. 4-phenyl-3-furoxancarbonitrile : A 1,2,5-oxadiazole substituted by an oxido, cyano and phenyl groups at positions 2, 3 and 4, respectively. It is a vasodilator and inhibitor of platelet aggregation.		2.05101,2,5-oxadiazole;
benzenes;
N-oxide;
nitrile		geroprotector;
nitric oxide donor;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent
phenytoin
[no description available]		2.0510imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
5-(n,n-hexamethylene)amiloride
5-(N,N-hexamethylene)amiloride: inhibitor of Na+-H+ exchange; has anti-HIV-1 activity. 5-(N,N-hexamethylene)amiloride : A member of the class of pyrazines that is amiloride in which the two amino hydrogens at position N-5 are replaced by a hexamethylene moiety, resulting in the formation of an azepane ring.		2.0510aromatic amine;
azepanes;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines		antineoplastic agent;
apoptosis inducer;
odorant receptor antagonist;
sodium channel blocker
ethylisopropylamiloride
ethylisopropylamiloride: structure in first source. ethylisopropylamiloride : A member of the class of pyrazines that is amiloride in which the amino substitutent of the pyrazine ring that is adjacent to the chloro substituent has been substituted by an ethyl group and by an isopropyl group.		2.0510aromatic amine;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines;
tertiary amino compound		anti-arrhythmia drug;
neuroprotective agent;
sodium channel blocker
5-fluoroindole-2-carboxylic acid
5-fluoroindole-2-carboxylic acid: N-methyl-D-aspartate receptor antagonist		2.0510indolyl carboxylic acid
phenanthridone
phenanthridone: coal tar derivative; structure given in first source. phenanthridone : A member of the class of phenanthridines that is phenanthridine with an oxo substituent at position 6. A poly(ADP-ribose) polymerase (PARP) inhibitor, it has been shown to exhibit immunosuppressive activity.		2.0510lactam;
phenanthridines		EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
immunosuppressive agent;
mutagen
6-nitroso-1,2-benzopyrone
[no description available]		2.0510
8-(4-sulfophenyl)theophylline
8-(4-sulfophenyl)theophylline: adenosine antagonist		2.0510
tacrine
Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.		2.0810acridines;
aromatic amine		EC 3.1.1.7 (acetylcholinesterase) inhibitor
aa 861
2,3,5-trimethyl-6-(12-hydroxy-5,10-dodecadiynyl)-1,4-benzoquinone: structure given in first source. docebenone : A member of the class of benzoquinones that is p-benzoquinone in which the hydrogens are substituted by three methyl groups and a 12-hydroxydodeca-5,10-diyn-1-yl group.		2.05101,4-benzoquinones;
acetylenic compound;
primary alcohol		EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor
acebutolol
Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.		2.0510aromatic amide;
ethanolamines;
ether;
monocarboxylic acid amide;
propanolamine;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympathomimetic agent
acetaminophen
Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group.		2.4720acetamides;
phenols		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
cyclooxygenase 3 inhibitor;
environmental contaminant;
ferroptosis inducer;
geroprotector;
hepatotoxic agent;
human blood serum metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
acetazolamide
Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)		4.2360monocarboxylic acid amide;
sulfonamide;
thiadiazoles		anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
acetohydroxamic acid
acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group.		2.0510acetohydroxamic acids;
carbohydroximic acid		algal metabolite;
EC 3.5.1.5 (urease) inhibitor
ag 127
tyrphostin AG 126: inhibits development of postoperative ileus induced by surgical manipulation of murine colon		2.0510nitrophenol
rtki cpd
[no description available]		2.0510aromatic ether;
monochlorobenzenes;
quinazolines		antineoplastic agent;
antiviral agent;
epidermal growth factor receptor antagonist;
geroprotector
tyrphostin a23
tyrphostin A23: inhibits EGF-stimulated thymidine incorporation as well as EGF-stimulated receptor autophosphorylation & tyrosine phosphorylation & cell proliferation; structure given in first source		2.0510catechols
tyrphostin 25
[no description available]		2.0510benzenetriol
albendazole
[no description available]		5.0421aryl sulfide;
benzimidazoles;
benzimidazolylcarbamate fungicide;
carbamate ester		anthelminthic drug;
microtubule-destabilising agent;
tubulin modulator
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).		28.081,675671phenols;
phenylethanolamines;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
environmental contaminant;
xenobiotic
alendronate
alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups.		4.81211,1-bis(phosphonic acid);
primary amino compound		bone density conservation agent;
EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		2.0510organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
alprenolol
Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.. alprenolol : A secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent.		2.7530secondary alcohol;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
amantadine
amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source		2.0310adamantanes;
primary aliphatic amine		analgesic;
antiparkinson drug;
antiviral drug;
dopaminergic agent;
NMDA receptor antagonist;
non-narcotic analgesic
diatrizoic acid
Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography.		2.0810acetamides;
benzoic acids;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
aminoglutethimide
Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.. aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position.		2.4720dicarboximide;
piperidones;
substituted aniline		adrenergic agent;
anticonvulsant;
antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
theophylline
[no description available]		13.655625dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
amiodarone
Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.		2.47201-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
dan 2163
[no description available]		2.0810aromatic amide;
aromatic amine;
benzamides;
pyrrolidines;
sulfone		environmental contaminant;
second generation antipsychotic;
xenobiotic
amitriptyline
Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.		2.4720carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
amlexanox
amlexanox: SRA-A antagonist;structure given in first source. amlexanox : A pyridochromene-derived monocarboxylic acid having an amino substituent at the 2-position, an oxo substituent at the 5-position and an isopropyl substituent at the 7-position.		2.0810monocarboxylic acid;
pyridochromene		anti-allergic agent;
anti-ulcer drug;
non-steroidal anti-inflammatory drug
amlodipine
Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.		2.4720dihydropyridine;
ethyl ester;
methyl ester;
monochlorobenzenes;
primary amino compound		antihypertensive agent;
calcium channel blocker;
vasodilator agent
amoxapine
Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.		2.4720dibenzooxazepineadrenergic uptake inhibitor;
antidepressant;
dopaminergic antagonist;
geroprotector;
serotonin uptake inhibitor
amsacrine
Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.. amsacrine : A sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity.		2.0810acridines;
aromatic ether;
sulfonamide		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
anastrozole
[no description available]		2.0810nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
anthralin
Anthralin: An anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.. anthralin : An anthracene compound derived by the substitution of -OH groups for hydrogen at C-1 and C-8, and with an oxo group at C-9.		2.0810anthracenesantipsoriatic
antipyrine
Antipyrine: An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29). antipyrine : A pyrazolone derivative that is 1,2-dihydropyrazol-3-one substituted with methyl groups at N-1 and C-5 and with a phenyl group at N-2.		2.0810pyrazoloneantipyretic;
cyclooxygenase 3 inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
aprindine
Aprindine: A class Ib anti-arrhythmia agent used to manage ventricular and supraventricular arrhythmias.		2.0510indanes
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		4.3541benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
astemizole
Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.		2.0810benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
atenolol
Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.		2.4720ethanolamines;
monocarboxylic acid amide;
propanolamine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
aurintricarboxylic acid
Aurintricarboxylic Acid: A dye which inhibits protein biosynthesis at the initial stages. The ammonium salt (aluminon) is a reagent for the colorimetric estimation of aluminum in water, foods, and tissues.. aurintricarboxylic acid : A member of the class of quinomethanes that is 3-methylidene-6-oxocyclohexa-1,4-diene-1-carboxylic acid in which the methylidene hydrogens are replaced by 4-carboxy-3-hydroxyphenyl groups. The trisodium salt is the biological stain 'chrome violet CG' while the triammonium salt is 'aluminon'.		2.0510monohydroxybenzoic acid;
quinomethanes;
tricarboxylic acid		fluorochrome;
histological dye;
insulin-like growth factor receptor 1 antagonist
azathioprine
Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS.		2.7530aryl sulfide;
C-nitro compound;
imidazoles;
thiopurine		antimetabolite;
antineoplastic agent;
carcinogenic agent;
DNA synthesis inhibitor;
hepatotoxic agent;
immunosuppressive agent;
prodrug
baclofen
[no description available]		2.0810amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound		central nervous system depressant;
GABA agonist;
muscle relaxant
bay-k-8644
3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester: A dihydropyridine derivative, which, in contrast to NIFEDIPINE, functions as a calcium channel agonist. The compound facilitates Ca2+ influx through partially activated voltage-dependent Ca2+ channels, thereby causing vasoconstrictor and positive inotropic effects. It is used primarily as a research tool.. Bay-K-8644 : A racemate comprising equimolar amounts of (R)- and (S)-Bay-K-8644. methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylate : A pentasubstituted dihydropyridine carrying methoxycarbonyl, 2-(trifluoromethyl)phenyl and nitro substituents at positions 3, 4 and 5 respectively as well as two methyl substituents at positions 2 and 6.		2.0510(trifluoromethyl)benzenes;
C-nitro compound;
dihydropyridine;
methyl ester
benzbromarone
Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication.		2.08101-benzofurans;
aromatic ketone		uricosuric drug
benzocaine
Benzocaine: A surface anesthetic that acts by preventing transmission of impulses along NERVE FIBERS and at NERVE ENDINGS.. dextran sulfate sodium : An organic sodium salt of dextran sulfate. It induces colitis in mice.. benzocaine : A benzoate ester having 4-aminobenzoic acid as the acid component and ethanol as the alcohol component. A surface anaesthetic, it is used to suppress the gag reflex, and as a lubricant and topical anaesthetic on the larynx, mouth, nasal cavity, respiratory tract, oesophagus, rectum, urinary tract, and vagina.		2.0810benzoate ester;
substituted aniline		allergen;
antipruritic drug;
sensitiser;
topical anaesthetic
bepridil
Bepridil: A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist.. bepridil : A tertiary amine in which the substituents on nitrogen are benzyl, phenyl and 3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl.		2.0510pyrrolidines;
tertiary amine		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
bicalutamide
bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism.		2.0810(trifluoromethyl)benzenes;
monocarboxylic acid amide;
monofluorobenzenes;
nitrile;
sulfone;
tertiary alcohol
bay h 4502
bifonazole : A racemate comprising equimolar amounts of R- and S-bifonazole. It is a broad spectrum antifungal drug used for the treatment of fungal skin and nail infections.. 1-[biphenyl-4-yl(phenyl)methyl]imidazole : A member of the class of imidazoles carrying an alpha-(biphenyl-4-yl)benzyl substituent at position 1.		2.0810biphenyls;
imidazoles
bisacodyl
Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871)		2.0810diarylmethane
bisoprolol
Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.		2.7330secondary alcohol;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bml 190
indomethacin morpholinylamide: an inverse agonist of the cannabinoid CB2 receptor		2.0510N-acylindole
bretylium
bretylium: RN given refers to parent cpd. bretylium : A quaternary ammonium cation having 2-bromobenzyl, ethyl and two methyl groups attached to the nitrogen. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation.		2.0510quaternary ammonium ionadrenergic antagonist;
anti-arrhythmia drug;
antihypertensive agent
brimonidine
[no description available]		2.0510imidazoles;
quinoxaline derivative;
secondary amine		adrenergic agonist;
alpha-adrenergic agonist;
antihypertensive agent
bromhexine
Bromhexine: A mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p744). bromhexine : A substituted aniline that is 2,4-dibromoaniline which is substituted at position 6 by a [cyclohexyl(methyl)amino]methyl group. It is used (as the monohydrochloride salt) as a mucolytic for the treatment of respiratory disorders associated with productive cough (i.e. a cough characterised by the production of sputum).		2.0510organobromine compound;
substituted aniline;
tertiary amino compound		mucolytic
bromopride
bromopride: RN given refers to parent cpd; structure		2.0810benzamides
bronopol
[no description available]		2.0810nitro compound
bu 224
BU 224: a selective imidazoline 2-receptor blocker		2.0510quinolines
bumetanide
[no description available]		2.4720amino acid;
benzoic acids;
sulfonamide		diuretic;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor
busulfan
[no description available]		2.0810methanesulfonate esteralkylating agent;
antineoplastic agent;
carcinogenic agent;
insect sterilant;
teratogenic agent
caffeine
[no description available]		2.0810purine alkaloid;
trimethylxanthine		adenosine A2A receptor antagonist;
adenosine receptor antagonist;
adjuvant;
central nervous system stimulant;
diuretic;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
environmental contaminant;
food additive;
fungal metabolite;
geroprotector;
human blood serum metabolite;
mouse metabolite;
mutagen;
plant metabolite;
psychotropic drug;
ryanodine receptor agonist;
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.		2.4720aromatic ether;
nitrile;
polyether;
tertiary amino compound
candesartan
candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.		3.2310benzimidazolecarboxylic acid;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		2.4720dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
carmustine
Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.		2.4720N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
carprofen
carprofen: RN given refers to cpd without isomeric designation. carprofen : Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs.		2.0810carbazoles;
organochlorine compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug;
photosensitizing agent
carteolol
Carteolol: A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent.		2.0510quinolone;
secondary alcohol		anti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
carvedilol
[no description available]		3.0540carbazoles;
secondary alcohol;
secondary amino compound		alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
celecoxib
[no description available]		2.0810organofluorine compound;
pyrazoles;
sulfonamide;
toluenes		cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
cefixime
Cefixime: A third-generation cephalosporin antibiotic that is stable to hydrolysis by beta-lactamases.. cefixime : A third-generation cephalosporin antibiotic bearing vinyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(carboxymethoxy)imino]acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. It is used in the treatment of gonorrhoea, tonsilitis, pharyngitis, bronchitis, and urinary tract infections.		1.9710
cetirizine
Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.		1.9910ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines		anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
cgp 12177
CGP 12177 : A benzimidazole that is benzimidazol-2-one substituted at position 4 by a 3-(tert-butylamino)-2-hydroxypropoxy group.		2.4520aromatic ether;
benzimidazoles;
secondary alcohol;
secondary amino compound		beta-adrenergic antagonist
cgs 15943
9-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine: non-xanthine triazoloquinazoline adenosine antagonist. CGS 15943 : A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors.		2.0510aromatic amine;
biaryl;
furans;
organochlorine compound;
primary amino compound;
quinazolines;
triazoloquinazoline		adenosine A1 receptor antagonist;
adenosine A2A receptor antagonist;
antineoplastic agent;
central nervous system stimulant
chlorambucil
Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.		2.4720aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
chlordiazepoxide
Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2.		2.4720benzodiazepine
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		5.4941aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
chlorpheniramine
Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma.		2.4420monochlorobenzenes;
pyridines;
tertiary amino compound		anti-allergic agent;
antidepressant;
antipruritic drug;
H1-receptor antagonist;
histamine antagonist;
serotonin uptake inhibitor
chlorpromazine
Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.		2.4720organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
chlorpropamide
Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification.		2.4720monochlorobenzenes;
N-sulfonylurea		hypoglycemic agent;
insulin secretagogue
chlorthalidone
Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic.		2.4720isoindoles;
monochlorobenzenes;
sulfonamide
chlorzoxazone
Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm.		2.08101,3-benzoxazoles;
heteroaryl hydroxy compound;
organochlorine compound		muscle relaxant;
sedative
cifenline
[no description available]		2.0810diarylmethane
ciclopirox
[no description available]		2.0810cyclic hydroxamic acid;
hydroxypyridone antifungal drug;
pyridone		antibacterial agent;
antiseborrheic
ciglitazone
ciglitazone: structure given in second source; PPAR agonist used for type II diabetes. ciglitazone : An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist.		2.0810aromatic ether;
thiazolidinone		antineoplastic agent;
insulin-sensitizing drug
cilostamide
cilostamide: selective inhibitor of cyclic AMP phosphodiesterase & platelet aggregation; structure		2.0510quinolines
cilostazol
[no description available]		2.4720lactam;
tetrazoles		anticoagulant;
bronchodilator agent;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
fibrin modulating drug;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent
cimetidine
Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.		2.7530aliphatic sulfide;
guanidines;
imidazoles;
nitrile		adjuvant;
analgesic;
anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
cinoxacin
Cinoxacin: Synthetic antimicrobial related to OXOLINIC ACID and NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.. cinoxacin : A member of the class of cinnolines that is 6,7-methylenedioxycinnolin-4(1H)-one bearing an ethyl group at position 1 and a carboxylic acid group at position 3. An analogue of oxolinic acid, it has similar antibacterial actions. It was formerly used for the treatment of urinary tract infections.		2.0510cinnolines;
oxacycle;
oxo carboxylic acid		antibacterial drug;
antiinfective agent
ciprofibrate
[no description available]		2.0810cyclopropanes;
monocarboxylic acid;
organochlorine compound		antilipemic drug
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.		2.0810aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
citalopram
Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.		2.47202-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
clenbuterol
Clenbuterol: A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.. clenbuterol : A substituted aniline that is 2,6-dichloroaniline in which the hydrogen at position 4 has been replaced by a 2-(tert-butylamino)-1-hydroxyethyl group.		4.6280amino alcohol;
dichlorobenzene;
ethanolamines;
primary arylamine;
secondary amino compound;
substituted aniline		beta-adrenergic agonist;
bronchodilator agent;
sympathomimetic agent
clioquinol
Clioquinol: A potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide.. 5-chloro-7-iodoquinolin-8-ol : A monohydroxyquinoline that is quinolin-8-ol in which the hydrogens at positions 5 and 7 are replaced by chlorine and iodine, respectively. It has antibacterial and atifungal properties, and is used in creams for the treatment of skin infections. It has also been investigated as a chelator of copper and zinc ions for the possible treatment of Alzheimer's disease.		2.4720monohydroxyquinoline;
organochlorine compound;
organoiodine compound		antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
antiprotozoal drug;
chelator;
copper chelator
clobazam
Clobazam: A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.. clobazam : 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics.		2.08101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
GABA modulator
clofazimine
Clofazimine: A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619). clofazimine : 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients.		2.0810monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug
clofibrate
angiokapsul: contains clofibrate & insoitolnicotinate		2.7330aromatic ether;
ethyl ester;
monochlorobenzenes		anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist
clomiphene
[no description available]		2.0810tertiary amineestrogen antagonist;
estrogen receptor modulator
clomipramine
Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias.		2.4720dibenzoazepineanticoronaviral agent;
antidepressant;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
serotonergic antagonist;
serotonergic drug;
serotonin uptake inhibitor
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		2.0510clonidine;
imidazoline
4-chloro-N-(2,6-dimethyl-1-piperidinyl)-3-sulfamoylbenzamide
[no description available]		2.0810sulfonamide
chlorazepate
clorazepic acid : A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively.		2.05101,4-benzodiazepinoneanticonvulsant;
anxiolytic drug;
GABA modulator;
prodrug
clotrimazole
[no description available]		2.0510conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes		antiinfective agent;
environmental contaminant;
xenobiotic
dapsone
[no description available]		2.4720substituted aniline;
sulfone		anti-inflammatory drug;
antiinfective agent;
antimalarial;
leprostatic drug
debrisoquin
Debrisoquin: An adrenergic neuron-blocking drug similar in effects to GUANETHIDINE. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism.		2.0510carboxamidine;
isoquinolines		adrenergic agent;
antihypertensive agent;
human metabolite;
sympatholytic agent
desipramine
Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.		2.4720dibenzoazepine;
secondary amino compound		adrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
cholinergic antagonist;
drug allergen;
EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
serotonin uptake inhibitor
nordazepam
Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.. nordazepam : A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety.		2.17101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
GABA modulator;
human metabolite;
sedative
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		2.47201,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
diazoxide
Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.		2.4720benzothiadiazine;
organochlorine compound;
sulfone		antihypertensive agent;
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
diuretic;
K-ATP channel agonist;
sodium channel blocker;
sympathomimetic agent;
vasodilator agent
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		2.0510amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
3,4-dihydroxybenzohydroxamic acid
[no description available]		2.0510benzoic acids
diflunisal
Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position.		2.0510monohydroxybenzoic acid;
organofluorine compound		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
dimercaprol
Dimercaprol: An anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning.. dimercaprol : A dithiol that is propane-1,2-dithiol in which one of the methyl hydrogens is replaced by a hydroxy group. a chelating agent originally developed during World War II as an experimental antidote against the arsenic-based poison gas Lewisite, it has been used clinically since 1949 for the treatment of poisoning by arsenic, mercury and gold. It can also be used for treatment of poisoning by antimony, bismuth and possibly thallium, and (with sodium calcium edetate) in cases of acute leaad poisoning. Administration is by (painful) intramuscular injection of a suspension of dimercaprol in peanut oil, typically every 4 hours for 2-10 days depending on the toxicity. In the past, dimercaprol was also used for the treatment of Wilson's disease, a severely debilitating genetic disorder in which the body tends to retain copper, with resultant liver and brain injury.		2.0510dithiol;
primary alcohol		chelator
dipyridamole
Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots.		2.4720piperidines;
pyrimidopyrimidine;
tertiary amino compound;
tetrol		adenosine phosphodiesterase inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
disopyramide
Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug.		2.0810monocarboxylic acid amide;
pyridines;
tertiary amino compound		anti-arrhythmia drug
disulfiram
[no description available]		2.7230organic disulfide;
organosulfur acaricide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor
2,3-dimethoxy-1,4-naphthoquinone
2,3-dimethoxynaphthalene-1,4-dione : A naphthoquinone that is 1,4-naphthoquinone bearing two methoxy substituents at positions 2 and 3. Redox-cycling agent that induces intracellular superoxide anion formation and, depending on the concentration, induces cell proliferation, apoptosis or necrosis. Used to study the role of ROS in cell toxicity, apoptosis, and necrosis.		2.05101,4-naphthoquinones
domperidone
Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.		2.7530benzimidazoles;
heteroarylpiperidine		antiemetic;
dopaminergic antagonist
donepezil
Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group.		2.4620aromatic ether;
indanones;
piperidines;
racemate		EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
nootropic agent
doxepin
Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug.		2.0810dibenzooxepine;
tertiary amino compound		antidepressant
droperidol
Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon.		2.0510aromatic ketone;
benzimidazoles;
organofluorine compound		anaesthesia adjuvant;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic
ebastine
[no description available]		2.0810organic molecular entity
ebselen
ebselen : A benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase.		2.0510benzoselenazoleanti-inflammatory drug;
antibacterial agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
EC 3.5.4.1 (cytosine deaminase) inhibitor;
EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor;
enzyme mimic;
ferroptosis inhibitor;
genotoxin;
hepatoprotective agent;
neuroprotective agent;
radical scavenger
ellipticine
ellipticine : A organic heterotetracyclic compound that is pyrido[4,3-b]carbazole carrying two methyl substituents at positions 5 and 11.		2.0510indole alkaloid;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound;
polycyclic heteroarene		antineoplastic agent;
plant metabolite
emodin
Emodin: Purgative anthraquinone found in several plants, especially RHAMNUS PURSHIANA. It was formerly used as a laxative, but is now used mainly as a tool in toxicity studies.. emodin : A trihydroxyanthraquinone that is 9,10-anthraquinone which is substituted by hydroxy groups at positions 1, 3, and 8 and by a methyl group at position 6. It is present in the roots and barks of numerous plants (particularly rhubarb and buckthorn), moulds, and lichens. It is an active ingredient of various Chinese herbs.		2.0510trihydroxyanthraquinoneantineoplastic agent;
laxative;
plant metabolite;
tyrosine kinase inhibitor
enoxacin
Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.. enoxacin : A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea.		2.08101,8-naphthyridine derivative;
amino acid;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-arylpiperazine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor
ethacrynic acid
Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor.		2.4720aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid		EC 2.5.1.18 (glutathione transferase) inhibitor;
ion transport inhibitor;
loop diuretic
ethosuximide
Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures.		2.4720dicarboximide;
pyrrolidinone		anticonvulsant;
geroprotector;
T-type calcium channel blocker
ethyl loflazepate
ethyl loflazepate: structure given in first source		2.0510organic molecular entity
brl 42810
[no description available]		2.08102-aminopurines;
acetate ester		antiviral drug;
prodrug
4-biphenylylacetic acid
biphenyl-4-ylacetic acid : A monocarboxylic acid in which one of the alpha-hydrogens is substituted by a biphenyl-4-yl group. An active metabolite of fenbufen, it is used as a topical medicine to treat muscle inflammation and arthritis.		2.0810biphenyls;
monocarboxylic acid		non-steroidal anti-inflammatory drug
felodipine
Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris.		2.7530dichlorobenzene;
dihydropyridine;
ethyl ester;
methyl ester		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		2.4720aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
berotek
Fenoterol: A synthetic adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.. fenoterol : A member of the class resorcinols that is 5-(1-hydroxyethyl)benzene-1,3-diol in which one of the methyl hydrogens is replaced by a 1-(4-hydroxyphenyl)propan-2-amino group. A beta2-adrenergic agonist, it is used (as the hydrobromide salt) as a bronchodilator in the management of reversible airway obstruction.		8.11224resorcinols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
sympathomimetic agent;
tocolytic agent
fentanyl
Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.		2.0510anilide;
monocarboxylic acid amide;
piperidines		adjuvant;
anaesthesia adjuvant;
anaesthetic;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
fexofenadine
fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.		3.4111piperidines;
tertiary amine		anti-allergic agent;
H1-receptor antagonist
flecainide
Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		2.0510aromatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines		anti-arrhythmia drug
fleroxacin
Fleroxacin: A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.. fleroxacin : A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria.		2.0810difluorobenzene;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
quinolines		antibacterial drug;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
fluconazole
Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.		2.0810conazole antifungal drug;
difluorobenzene;
tertiary alcohol;
triazole antifungal drug		environmental contaminant;
P450 inhibitor;
xenobiotic
flucytosine
Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.		2.0810aminopyrimidine;
nucleoside analogue;
organofluorine compound;
pyrimidine antifungal drug;
pyrimidone		prodrug
fluphenazine
[no description available]		2.0510N-alkylpiperazine;
organofluorine compound;
phenothiazines		anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug
flumazenil
Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.		2.0810ethyl ester;
imidazobenzodiazepine;
organofluorine compound		antidote to benzodiazepine poisoning;
GABA antagonist
fluorescite
fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer.		2.0810benzoic acids;
cyclic ketone;
hydroxy monocarboxylic acid;
organic heterotricyclic compound;
phenols;
xanthene dye		fluorescent dye;
radioopaque medium
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		2.4720nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
fluoxetine
Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.		2.7830(trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound
flurbiprofen
Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.		2.0510fluorobiphenyl;
monocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
fluspirilene
Fluspirilene: A long-acting injectable antipsychotic agent used for chronic schizophrenia.		2.0510diarylmethane
flutamide
Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.		2.7530(trifluoromethyl)benzenes;
monocarboxylic acid amide		androgen antagonist;
antineoplastic agent
formoterol fumarate
N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamide : A phenylethanoloamine having 4-hydroxy and 3-formamido substituents on the phenyl ring and an N-(4-methoxyphenyl)propan-2-yl substituent.		2.0510formamides;
phenols;
phenylethanolamines;
secondary alcohol;
secondary amino compound
fpl 64176
FPL 64176: an activator of L-type calcium channels; structure given in first source. FPL 64176 : 1H-Pyrrole substituted at C-2 and -5 by methyl groups, at C-3 by methoxycarbonyl and at C-4 by a 2-benzylbenzoyl group.		2.0510carboxylic ester;
pyrroles		calcium channel agonist
furafylline
[no description available]		1.9910oxopurine
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		2.9940chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
gemfibrozil
[no description available]		2.0810aromatic etherantilipemic drug
gliclazide
Gliclazide: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.		2.0810N-sulfonylureahypoglycemic agent;
insulin secretagogue;
radical scavenger
glimepiride
glimepiride: structure given in first source		2.0810sulfonamide
glipizide
Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus.		2.0810aromatic amide;
monocarboxylic acid amide;
N-sulfonylurea;
pyrazines		EC 2.7.1.33 (pantothenate kinase) inhibitor;
hypoglycemic agent;
insulin secretagogue
glutethimide
Glutethimide: A hypnotic and sedative. Its use has been largely superseded by other drugs.		2.0510piperidines
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		2.9540monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
guaifenesin
Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations.		4.5640methoxybenzenes
guanethidine
Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid.		2.0510azocanes;
guanidines		adrenergic antagonist;
antihypertensive agent;
sympatholytic agent
guanfacine
Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.		2.0810acetamides
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		2.4720aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
hydrochlorothiazide
Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure.		2.7230benzothiadiazine;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
hydroflumethiazide
Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide.		2.0810benzothiadiazine;
thiazide		antihypertensive agent;
diuretic
hydroxyurea
[no description available]		6.8171one-carbon compound;
ureas		antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent
hydroxyzine
Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.		2.0510hydroxyether;
monochlorobenzenes;
N-alkylpiperazine		anticoronaviral agent;
antipruritic drug;
anxiolytic drug;
dermatologic drug;
H1-receptor antagonist
ibuprofen
Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine		3.8421monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
ic 261
[no description available]		2.0510indoles
phenelzine
Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC.		2.0510primary amine
lidocaine
Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.		3.8330benzenes;
monocarboxylic acid amide;
tertiary amino compound		anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
ifosfamide
[no description available]		2.0810ifosfamidesalkylating agent;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
xenobiotic
imipramine
Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.		2.4720dibenzoazepineadrenergic uptake inhibitor;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
amrinone
Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure.		2.4720bipyridinesEC 3.1.4.* (phosphoric diester hydrolase) inhibitor
incadronate
[no description available]		2.05101,1-bis(phosphonic acid)
indapamide
Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine.		2.4720indoles;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic
indirubin-3'-monoxime
indirubin-3'-monoxime: has antiangiogenic activity. indirubin-3'-monoxime : A member of the class of biindoles that is indirubin in which the keto group at position 3' has undergone condensation with hydroxylamine to form the corresponding oxime.		2.0510
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		2.9640aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
iohexol
Iohexol: An effective non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Its low systemic toxicity is the combined result of low chemotoxicity and low osmolality.. iohexol : A benzenedicarboxamide compound having N-(2,3-dihydroxypropyl)carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and an N-(2,3-dihydroxypropyl)acetamido group at the 5-position.		2.0810benzenedicarboxamide;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
iproniazid
[no description available]		2.0810carbohydrazide;
pyridines
avapro
Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.		2.0810azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
1-methyl-3-isobutylxanthine
1-Methyl-3-isobutylxanthine: A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES. 3-isobutyl-1-methylxanthine : An oxopurine that is xanthine which is substituted at positions 1 and 3 by methyl and isobutyl groups, respectively.		2.4203-isobutyl-1-methylxanthine
isoniazid
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		2.0810carbohydrazideantitubercular agent;
drug allergen
4-piperidinecarboxylic acid
4-piperidinecarboxylic acid: structure in first source		2.0510
2-propanol
2-Propanol: An isomer of 1-PROPANOL. It is a colorless liquid having disinfectant properties. It is used in the manufacture of acetone and its derivatives and as a solvent. Topically, it is used as an antiseptic.. propan-2-ol : A secondary alcohol that is propane in which one of the hydrogens attached to the central carbon is substituted by a hydroxy group.		2.0410secondary alcohol;
secondary fatty alcohol		protic solvent
isoproterenol
Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.		6.61390catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
isradipine
Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.		2.0810benzoxadiazole;
dihydropyridine;
isopropyl ester;
methyl ester
itraconazole
[no description available]		2.0810piperazines
jl 18
JL 18: a pyridobenzodiazepine derivative bioisoster of clozapine		2.0510
nsc 664704
kenpaullone: inhibits CDK1/cyclin B; structure in first source. kenpaullone : An indolobenzazepine that is paullone in which the hydrogen at position 9 is replaced by a bromo substituent. It is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3beta (GSK3beta).		2.4620indolobenzazepine;
lactam;
organobromine compound		cardioprotective agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
geroprotector
ketamine
Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group.		2.4720cyclohexanones;
monochlorobenzenes;
secondary amino compound		analgesic;
environmental contaminant;
intravenous anaesthetic;
neurotoxin;
NMDA receptor antagonist;
xenobiotic
ketanserin
Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.. ketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group.		2.4720aromatic ketone;
organofluorine compound;
piperidines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		2.9540dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
ketoprofen
Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.		2.0510benzophenones;
oxo monocarboxylic acid		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
ketotifen
Ketotifen: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.. ketotifen : An organic heterotricyclic compound that is 4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one which is substituted at position 4 by a 1-methylpiperidin-4-ylidene group. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is used (usually as its hydrogen fumarate salt) for the treatment of asthma, where it may take several weeks to exert its full effect.		4.8542cyclic ketone;
olefinic compound;
organic heterotricyclic compound;
organosulfur heterocyclic compound;
piperidines;
tertiary amino compound		anti-asthmatic drug;
H1-receptor antagonist
labetalol
Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5.		2.0510benzamides;
benzenes;
phenols;
primary carboxamide;
salicylamides;
secondary alcohol;
secondary amino compound
lamotrigine
[no description available]		2.08101,2,4-triazines;
dichlorobenzene;
primary arylamine		anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
lansoprazole
Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.		2.7530benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
beta-lapachone
beta-lapachone: antineoplastic inhibitor of reverse transcriptase, DNA topoisomerase, and DNA polymerase. beta-lapachone : A benzochromenone that is 3,4-dihydro-2H-benzo[h]chromene-5,6-dione substituted by geminal methyl groups at position 2. Isolated from Tabebuia avellanedae, it exhibits antineoplastic and anti-inflammatory activities.		2.0510benzochromenone;
orthoquinones		anti-inflammatory agent;
antineoplastic agent;
plant metabolite
leflunomide
Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide.		2.0810(trifluoromethyl)benzenes;
isoxazoles;
monocarboxylic acid amide		antineoplastic agent;
antiparasitic agent;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
hepatotoxic agent;
immunosuppressive agent;
non-steroidal anti-inflammatory drug;
prodrug;
pyrimidine synthesis inhibitor;
tyrosine kinase inhibitor
letrozole
[no description available]		2.4620nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
linopirdine
linopirdine: acetylcholine releasing drug		2.0510indoles
lofepramine
Lofepramine: A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE.		2.4720aromatic ketone;
dibenzoazepine;
monochlorobenzenes;
tertiary amino compound		antidepressant
lomustine
[no description available]		2.4720N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
loratadine
Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.		2.7830benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
lorazepam
Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.		2.0510benzodiazepine
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		2.4420chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
maprotiline
Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.		2.4720anthracenes
mazindol
Mazindol: Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.		2.0510organic molecular entity
mebendazole
Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5.		2.0810aromatic ketone;
benzimidazoles;
carbamate ester		antinematodal drug;
microtubule-destabilising agent;
tubulin modulator
mechlorethamine
nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR.		2.0510nitrogen mustard;
organochlorine compound		alkylating agent
mefenamic acid
Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.		2.0810aminobenzoic acid;
secondary amino compound		analgesic;
antipyretic;
antirheumatic drug;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
mefloquine hydrochloride
[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4.		2.0510organofluorine compound;
piperidines;
quinolines;
secondary alcohol
mephenytoin
Mephenytoin: An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.. mephenytoin : An imidazolidine-2,4-dione (hydantoin) in which the imidazolidine nucleus carries a methyl group at N-3 and has ethyl and phenyl substituents at C-5. An anticonvulsant, it is no longer available in the USA or the UK but is still studied largely because of its interesting hydroxylation polymorphism.		2.0510imidazolidine-2,4-dioneanticonvulsant
metaproterenol
Metaproterenol: A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.. orciprenaline : A racemate composed of equimolar amounts of (R)- and (S)-orciprenaline. Used (as its sulfate salt) to relax the airway muscles and improve breathing for patients suffering from asthma or bronchitis.. 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol : A member of the class of resorcinols bearing an additional 1-hydroxy-2-(isopropanylamino)ethyl substituent at position 5 of resorcinol itself.		2.4120aralkylamino compound;
phenylethanolamines;
resorcinols;
secondary alcohol;
secondary amino compound
metformin
Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.		5.0421guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
methadone
Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4.		3.1210benzenes;
diarylmethane;
ketone;
tertiary amino compound
methoxyamine
methoxyamine: analytical reagent for aldehydes and ketones; strong irritant, can probably produce methemoglobinemia; RN given refers to parent cpd; structure		2.0510organooxygen compound
methoxyflurane
Methoxyflurane: An inhalation anesthetic. Currently, methoxyflurane is rarely used for surgical, obstetric, or dental anesthesia. If so employed, it should be administered with NITROUS OXIDE to achieve a relatively light level of anesthesia, and a neuromuscular blocking agent given concurrently to obtain the desired degree of muscular relaxation. (From AMA Drug Evaluations Annual, 1994, p180). methoxyflurane : An ether in which the two groups attached to the central oxygen atom are methyl and 2,2-dichloro-1,1-difluoroethyl.		2.0510ether;
organochlorine compound;
organofluorine compound		hepatotoxic agent;
inhalation anaesthetic;
nephrotoxic agent;
non-narcotic analgesic
nocodazole
[no description available]		2.0510aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes		antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
methylphenidate
Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group.		2.0510beta-amino acid ester;
methyl ester;
piperidines
metoclopramide
Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.		2.4720benzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound		antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic
metolazone
Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics.		2.0510organochlorine compound;
quinazolines;
sulfonamide		antihypertensive agent;
diuretic;
ion transport inhibitor
metoprolol
Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.		2.0810aromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound		antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic
metronidazole
Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.		2.7630C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic
mexiletine
Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol.		2.4720aromatic ether;
primary amino compound		anti-arrhythmia drug
mianserin
Mianserin: A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.. mianserin : A dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere.		2.0510dibenzoazepineadrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
H1-receptor antagonist;
histamine agonist;
sedative;
serotonergic antagonist
midazolam
Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.		2.4220imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
minoxidil
Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6.		2.4720dialkylarylamine;
tertiary amino compound
mirtazapine
Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders.		2.0810benzazepine;
tetracyclic antidepressant		alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
oneirogen;
serotonergic antagonist
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		2.0510dihydroxyanthraquinoneanalgesic;
antineoplastic agent
ml 7
ML-7 : An N-sulfonyldiazepane resullting from the formal condensation of 5-iodo-1-naphthylsulfonic acid with one of the nitrogens of 1,4-diazepane. It is a selective inhibitor of myosin light chain kinase (EC 2.7.11.18).		2.0510N-sulfonyldiazepane;
organoiodine compound		EC 2.7.11.18 (myosin-light-chain kinase) inhibitor
ml 9
[no description available]		2.0510naphthalenes;
sulfonic acid derivative
moclobemide
Moclobemide: A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.. moclobemide : A member of the class of benzamides that is benzamide substituted by a chloro group at position 4 and a 2-(morpholin-4-yl)ethyl group at the nitrogen atom. It acts as a reversible monoamine oxidase inhibitor and is used in the treatment of depression.		2.0810benzamides;
monochlorobenzenes;
morpholines		antidepressant;
environmental contaminant;
xenobiotic
acecainide
Acecainide: A major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure.. N-acetylprocainamide : A benzamide obtained via formal condensation of 4-acetamidobenzoic acid and 2-(diethylamino)ethylamine.		2.0810acetamides;
benzamides		anti-arrhythmia drug
fg 7142
FG 7142: benzodiazepine receptor agonist		2.0510beta-carbolines
n 0840
N(6)-cyclopentyl-9-methyladenine: selective, orally active A(1) adenosine receptor antagonist		2.0510
nabumetone
Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs.		2.0510methoxynaphthalene;
methyl ketone		cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
nadolol
[no description available]		2.0810tetralins
nalidixic acid
[no description available]		2.08101,8-naphthyridine derivative;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
DNA synthesis inhibitor
nefazodone
nefazodone: may be useful as an opiate adjunct		2.0810aromatic ether;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazoles		alpha-adrenergic antagonist;
analgesic;
antidepressant;
serotonergic antagonist;
serotonin uptake inhibitor
nefopam
Nefopam: Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26). nefopam : A racemate comprising equal amounts of (R)- and (S)-nefopam. The hydrochloride is a centrally acting non-opiate analgesic commonly used for the treatment of moderate to severe pain.. 5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine : A member of the class of benzoxazocines that is 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine substituted by phenyl and methyl groups at positions 1 and 5 respectively.		2.0810benzoxazocine;
tertiary amino compound
neostigmine
Neostigmine: A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.. neostigmine : A quaternary ammonium ion comprising an anilinium ion core having three methyl substituents on the aniline nitrogen, and a 3-[(dimethylcarbamoyl)oxy] substituent at position 3. It is a parasympathomimetic which acts as a reversible acetylcholinesterase inhibitor.		2.0810quaternary ammonium ionantidote to curare poisoning;
EC 3.1.1.7 (acetylcholinesterase) inhibitor
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		2.0810cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nialamide
Nialamide: An MAO inhibitor that is used as an antidepressive agent.		2.0510organonitrogen compound;
organooxygen compound
nicardipine
Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively.		2.0810benzenes;
C-nitro compound;
diester;
dihydropyridine;
methyl ester;
tertiary amino compound
niclosamide
Niclosamide: An antihelmintic that is active against most tapeworms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p48). niclosamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-chlorosalicylic acid with the amino group of 2-chloro-4-nitroaniline. It is an oral anthelmintic drug approved for use against tapeworm infections.		2.0510benzamides;
C-nitro compound;
monochlorobenzenes;
salicylanilides;
secondary carboxamide		anthelminthic drug;
anticoronaviral agent;
antiparasitic agent;
apoptosis inducer;
molluscicide;
piscicide;
STAT3 inhibitor
nifedipine
Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.		4.3570C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
nimesulide
nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.		2.4220aromatic ether;
C-nitro compound;
sulfonamide		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
nimodipine
Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm.		2.47202-methoxyethyl ester;
C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
isopropyl ester		antihypertensive agent;
calcium channel blocker;
cardiovascular drug;
vasodilator agent
nisoldipine
Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris.		2.0810C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
methyl ester
nitrazepam
Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic.. nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome).		2.08101,4-benzodiazepinone;
C-nitro compound		anticonvulsant;
antispasmodic drug;
drug metabolite;
GABA modulator;
sedative
nitrendipine
Nitrendipine: A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.. nitrendipine : A dihydropyridine that is 1,4-dihydropyridine substituted by methyl groups at positions 2 and 6, a 3-nitrophenyl group at position 4, a ethoxycarbonyl group at position 3 and a methoxycarbonyl group at position 5. It is a calcium-channel blocker used in the treatment of hypertension.		2.7530C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
ethyl ester;
methyl ester		antihypertensive agent;
calcium channel blocker;
geroprotector;
vasodilator agent
nitroglycerin
Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain.		2.0510nitroglycerolexplosive;
muscle relaxant;
nitric oxide donor;
prodrug;
tocolytic agent;
vasodilator agent;
xenobiotic
nomifensine
Nomifensine: An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266). nomifensine : An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively.		2.0510isoquinolinesdopamine uptake inhibitor
masoprocol
nordihydroguaretic acid: antioxidant compound found in the creosote bush (Larrea tridentata)		2.0510catechols;
lignan;
tetrol		antioxidant;
ferroptosis inhibitor;
geroprotector;
plant metabolite
norfloxacin
Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase.		2.4720fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug;
DNA synthesis inhibitor;
environmental contaminant;
xenobiotic
nortriptyline
Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline.		2.7830organic tricyclic compound;
secondary amine		adrenergic uptake inhibitor;
analgesic;
antidepressant;
antineoplastic agent;
apoptosis inducer;
drug metabolite
5-nitro-2-(3-phenylpropylamino)benzoic acid
5-nitro-2-(3-phenylpropylamino)benzoic acid: structure given in first source; chloride channel antagonist		2.0510nitrobenzoic acid
ns 1619
NS 1619: structure given in first source. NS 1619 : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which the hydrogens at positions 1 and 5 are replaced are replaced by 2-hydroxy-5-(trifluoromethyl)phenyl and trifluoromethyl groups, respectively. It is an opener/activator of the large-conductance calcium-activated potassium channel (Bkca).		2.0510(trifluoromethyl)benzenes;
benzimidazoles;
phenols		potassium channel opener
ofloxacin
Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.		5.28313-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
olomoucine
olomoucine: inhibits protein P34CDC2. olomoucine : A 9H-purine that is substituted by a (2-hydroxyethyl)nitrilo, benzylnitrilo and a methyl group at positions 2,6 and 9, respectively. It is a cyclin-dependent kinase inhibitor.		2.46202,6-diaminopurines;
ethanolamines		EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
omeprazole
Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.		2.4720aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
ondansetron
Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.		2.0810carbazoles
oxaprozin
Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis.		2.47201,3-oxazoles;
monocarboxylic acid		analgesic;
non-steroidal anti-inflammatory drug
oxatomide
oxatomide: structure; an anti-allergic & an anti-asthmatic. oxatomide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one substituted by a 3-[4-(diphenylmethyl)piperazin-1-yl]propyl group at position 1. It is an anti-allergic drug.		2.4620benzimidazoles;
diarylmethane;
N-alkylpiperazine		anti-allergic agent;
anti-inflammatory agent;
geroprotector;
H1-receptor antagonist;
serotonergic antagonist
oxazepam
Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.		2.05101,4-benzodiazepinone;
organochlorine compound		anxiolytic drug;
environmental contaminant;
xenobiotic
oxprenolol
Oxprenolol: A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.		2.0510aromatic ether
oxybutynin
oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder.		4.9442acetylenic compound;
carboxylic ester;
racemate;
tertiary alcohol;
tertiary amino compound		antispasmodic drug;
calcium channel blocker;
local anaesthetic;
muscarinic antagonist;
muscle relaxant;
parasympatholytic
oxyphenbutazone
Oxyphenbutazone: A non-steroidal anti-inflammatory drug. Oxyphenbutazone eyedrops have been used abroad in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. (From AMA, Drug Evaluations Annual, 1994, p2000) It had been used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p27). oxyphenbutazone : A metabolite of phenylbutazone obtained by hydroxylation at position 4 of one of the phenyl rings. Commonly used (as its hydrate) to treat pain, swelling and stiffness associated with arthritis and gout, it was withdrawn from the market 1984 following association with blood dyscrasis and Stevens-Johnson syndrome.		2.0510phenols;
pyrazolidines		antimicrobial agent;
antineoplastic agent;
antipyretic;
drug metabolite;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite
aminosalicylic acid
Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4.		2.0510aminobenzoic acid;
phenols		antitubercular agent
palmidrol
palmidrol: a cannabinoid receptor-inactive eCB-related molecule used as prophylactic in helping to prevent respiratory viral infection. palmitoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of palmitic (hexadecanoic) acid.		2.0510endocannabinoid;
N-(long-chain-acyl)ethanolamine;
N-(saturated fatty acyl)ethanolamine		anti-inflammatory drug;
anticonvulsant;
antihypertensive agent;
neuroprotective agent
pamidronate
[no description available]		2.0510phosphonoacetic acid
pantoprazole
Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2.		2.520aromatic ether;
benzimidazoles;
organofluorine compound;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
environmental contaminant;
xenobiotic
papaverine
Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum.		2.4720benzylisoquinoline alkaloid;
dimethoxybenzene;
isoquinolines		antispasmodic drug;
vasodilator agent
pd 169316
2-(4-nitrophenyl)-4-(4-fluorophenyl)-5-(4-pyridinyl)-1H-imidazole: p38 MAP kinase inhibitor		2.0510imidazoles
pd 98059
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.		2.4320aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
pemoline
Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity.		2.08101,3-oxazolescentral nervous system stimulant
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		2.4720aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
pentoxifylline
[no description available]		2.0810oxopurine
perphenazine
Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.		2.7530N-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
organochlorine compound;
phenothiazines		antiemetic;
dopaminergic antagonist;
phenothiazine antipsychotic drug
phenacetin
Saridon: contains phenacetin, caffeine, propyphenazone & pyrithyldione		2.4720acetamides;
aromatic ether		cyclooxygenase 3 inhibitor;
non-narcotic analgesic;
peripheral nervous system drug
phenindione
Phenindione: An indandione that has been used as an anticoagulant. Phenindione has actions similar to WARFARIN, but it is now rarely employed because of its higher incidence of severe adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p234)		2.0510aromatic ketone;
beta-diketone		anticoagulant
phentermine
Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity.		2.0510primary amineadrenergic agent;
appetite depressant;
central nervous system drug;
central nervous system stimulant;
dopaminergic agent;
sympathomimetic agent
phenyl biguanide
phenyl biguanide: RN given refers to parent cpd. phenyl biguanide : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a phenyl group.		2.0510guanidinescentral nervous system drug
phenylbutazone
Phenylbutazone: A butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ANKYLOSING SPONDYLITIS; RHEUMATOID ARTHRITIS; and REACTIVE ARTHRITIS.. phenylbutazone : A member of the class of pyrazolidines that is 1,2-diphenylpyrazolidine-3,5-dione carrying a butyl group at the 4-position.		2.4620pyrazolidinesantirheumatic drug;
EC 1.1.1.184 [carbonyl reductase (NADPH)] inhibitor;
metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug
phloretin
[no description available]		2.0510dihydrochalconesantineoplastic agent;
plant metabolite
picotamide
picotamide: has anticoagulant & fibrinolytic properties; structure		2.0510benzamides
pinacidil
Pinacidil: A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)		2.4820pyridines
pindolol
Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.		3.150indoles;
secondary amine		antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
serotonergic antagonist;
vasodilator agent
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		2.0810aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
piracetam
Piracetam: A compound suggested to be both a nootropic and a neuroprotective agent.		2.0810organonitrogen compound;
organooxygen compound
pirbuterol
pirbuterol: structure		3.5420pyridines
pirenperone
[no description available]		2.0510aromatic ketone
piribedil
Piribedil: A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist.		2.0810N-arylpiperazine
potassium chloride
Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.		1.9910inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer
ono 1078
pranlukast: SRS-A antagonist; leukotriene D4 receptor antagonist		5.4341chromones
pyranoprofen
pyranoprofen: RN given refers to unlabled parent cpd; structure given in first source		2.0810pyridochromene
praziquantel
azinox: Russian drug		2.4720isoquinolines
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		2.0810aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
primaquine
Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia.		2.4720aminoquinoline;
aromatic ether;
N-substituted diamine		antimalarial
primidone
Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures.		2.0810pyrimidoneanticonvulsant;
environmental contaminant;
xenobiotic
probenecid
Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.		2.0810benzoic acids;
sulfonamide		uricosuric drug
procainamide
Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias.		2.4720benzamidesanti-arrhythmia drug;
platelet aggregation inhibitor;
sodium channel blocker
procaine
Procaine: A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016).. procaine : A benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-diethylaminoethanol but formed experimentally by reaction of ethyl 4-aminobenzoate with 2-diethylaminoethanol.		2.0510benzoate ester;
substituted aniline;
tertiary amino compound		central nervous system depressant;
drug allergen;
local anaesthetic;
peripheral nervous system drug
procarbazine
Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		2.0510benzamides;
hydrazines		antineoplastic agent
procaterol
Procaterol: A long-acting beta-2-adrenergic receptor agonist.		4.8560quinolines
prochlorperazine
Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.		2.0810N-alkylpiperazine;
N-methylpiperazine;
organochlorine compound;
phenothiazines		alpha-adrenergic antagonist;
antiemetic;
cholinergic antagonist;
dopamine receptor D2 antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic
procyclidine
Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3.		2.0810pyrrolidines;
tertiary alcohol		antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist
promethazine
Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety.		2.4720phenothiazines;
tertiary amine		anti-allergic agent;
anticoronaviral agent;
antiemetic;
antipruritic drug;
H1-receptor antagonist;
local anaesthetic;
sedative
propafenone
Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.		2.0810aromatic ketone;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug
propentofylline
[no description available]		2.0510oxopurine
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		6.25192naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
pyrilamine
Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.. mepyramine : An ethylenediamine derivative that is ethylenediamine in which one of the amino nitrogens is substituted by two methyl groups and the remaining amino nitrogen is substituted by a 4-methoxybenzyl and a pyridin-2-yl group.		1.9910aromatic ether;
ethylenediamine derivative		H1-receptor antagonist
pyrimethamine
Maloprim: contains above 2 cpds		5.0121aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
rabeprazole
Rabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.		2.0510benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
ranitidine
[no description available]		2.4720aralkylamine
pf 5901
alpha-pentyl-3-(2-quinolinylmethoxy)benzenemethanol: structure given in first source; platelet activating factor antagonist		2.0510quinolines
riluzole
Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.		2.4720benzothiazoles
risperidone
Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.		2.47201,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
ritanserin
Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.. ritanserin : A thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.		2.0510organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
rofecoxib
[no description available]		2.0810butenolide;
sulfone		analgesic;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
rolipram
[no description available]		5.5380pyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
saccharin
Saccharin: Flavoring agent and non-nutritive sweetener.. saccharin : A 1,2-benzisothiazole having a keto-group at the 3-position and two oxo substituents at the 1-position. It is used as an artificial sweetening agent.		3.38111,2-benzisothiazole;
N-sulfonylcarboxamide		environmental contaminant;
sweetening agent;
xenobiotic
sb 202190
4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole: structure given in first source; inhibits p38 MAP kinase		2.0510imidazoles;
organofluorine compound;
phenols;
pyridines		apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
sulfadiazine
Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines.		2.0810pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
antimicrobial agent;
antiprotozoal drug;
coccidiostat;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
sodium fluoride
[no description available]		4.9321fluoride saltmutagen
risedronic acid
Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION.		2.0510pyridines
sotalol
Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.		2.6930ethanolamines;
secondary alcohol;
secondary amino compound;
sulfonamide		anti-arrhythmia drug;
beta-adrenergic antagonist;
environmental contaminant;
xenobiotic
spiroxatrine
spiroxatrine: structure		2.0510imidazolidines
stearic acid
octadecanoic acid : A C18 straight-chain saturated fatty acid component of many animal and vegetable lipids. As well as in the diet, it is used in hardening soaps, softening plastics and in making cosmetics, candles and plastics.		2.0510long-chain fatty acid;
saturated fatty acid;
straight-chain saturated fatty acid		algal metabolite;
Daphnia magna metabolite;
human metabolite;
plant metabolite
imatinib
[no description available]		2.0810aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		2.0810dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
sulfamethoxazole
Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position.		2.0810isoxazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial agent;
antiinfective agent;
antimicrobial agent;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
epitope;
P450 inhibitor;
xenobiotic
sulfanitran
[no description available]		2.0810sulfonamide
sulfaphenazole
Sulfaphenazole: A sulfonilamide anti-infective agent.. sulfaphenazole : A sulfonamide that is sulfanilamide in which the sulfonamide nitrogen is substituted by a 1-phenyl-1H-pyrazol-5-yl group. It is a selective inhibitor of cytochrome P450 (CYP) 2C9 isozyme, and antibacterial agent.		1.9910primary amino compound;
pyrazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor;
P450 inhibitor
sulfasalazine
Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.		2.0810
sulfisoxazole
Sulfisoxazole: A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms.. sulfisoxazole : A sulfonamide antibacterial with an oxazole substituent. It has antibiotic activity against a wide range of gram-negative and gram-positive organisms.		2.0810isoxazoles;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
drug allergen
sulforaphane
sulforaphane: from Cardaria draba L.. sulforaphane : An isothiocyanate having a 4-(methylsulfinyl)butyl group attached to the nitrogen.		2.0510isothiocyanate;
sulfoxide		antineoplastic agent;
antioxidant;
EC 3.5.1.98 (histone deacetylase) inhibitor;
plant metabolite
sumatriptan
Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.		2.0810sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
t0156
[no description available]		2.0510naphthyridine derivative
gatifloxacin
Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.		2.0810N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
tazarotene
tazarotene: a topical acetylenic retinoid; a topical kerytolytic. tazarotene : The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.		2.0810acetylenic compound;
ethyl ester;
pyridines;
retinoid;
thiochromane		keratolytic drug;
prodrug;
teratogenic agent
temozolomide
[no description available]		5.0421imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
terazosin
Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia		2.0810furans;
piperazines;
primary amino compound;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
terbutaline
Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.		12.64222phenylethanolamines;
resorcinols		anti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
hypoglycemic agent;
sympathomimetic agent;
tocolytic agent
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		4.3541diarylmethane
tetraisopropylpyrophosphamide
Tetraisopropylpyrophosphamide: N,N',N'',N'''-Tetraisopropylpyrophosphamide. A specific inhibitor of pseudocholinesterases. It is commonly used experimentally to determine whether pseudo- or acetylcholinesterases are involved in an enzymatic process.		2.0510phosphoramide
thioridazine
Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.		2.0510phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
thiotepa
Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed).		2.0810aziridines
tiapride
[no description available]		2.0810benzamides
ticlopidine
Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.		2.0510monochlorobenzenes;
thienopyridine		anticoagulant;
fibrin modulating drug;
hematologic agent;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
tilorone
Tilorone: An antiviral agent used as its hydrochloride. It is the first recognized synthetic, low-molecular-weight compound that is an orally active interferon inducer, and is also reported to have antineoplastic and anti-inflammatory actions.. tilorone : A member of the class of fluoren-9-ones that is 9H-fluoren-9-one which is substituted by a 2-(diethylamino)ethoxy group at positions 2 and 7. It is an interferon inducer and a selective alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) agonist. Its hydrochloride salt is used as an antiviral drug.		2.0810aromatic ether;
diether;
fluoren-9-ones;
tertiary amino compound		anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
interferon inducer;
nicotinic acetylcholine receptor agonist
tinidazole
Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent.		2.0810imidazolesantiamoebic agent;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug
tizanidine
tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites.		2.0810benzothiadiazole;
imidazoles		alpha-adrenergic agonist;
muscle relaxant
nikethamide
Nikethamide: A central nervous system stimulant. It was formerly used in the treatment of barbiturate overdose but is now considered to be of no value for such purposes and may be dangerous. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1229)		2.0810pyridinecarboxamide
tolbutamide
Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.		2.4720N-sulfonylureahuman metabolite;
hypoglycemic agent;
insulin secretagogue;
potassium channel blocker
tolnaftate
[no description available]		2.0810monothiocarbamic esterantifungal drug
ici 136,753
[no description available]		2.0510pyrazolopyridine
trazodone
Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.		2.0810monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazolopyridine		adrenergic antagonist;
antidepressant;
anxiolytic drug;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
triamterene
Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema.		2.7530pteridinesdiuretic;
sodium channel blocker
triazolam
Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries.		2.0510triazolobenzodiazepinesedative
trifluoperazine
[no description available]		2.0510N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines		antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug
trimethadione
Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent.		2.0510oxazolidinoneanticonvulsant;
geroprotector
trimethoprim
Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.		2.7530aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
trimetrexate
Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.		1.9810
tripelennamine
Tripelennamine: A histamine H1 antagonist with low sedative action but frequent gastrointestinal irritation. It is used to treat ASTHMA; HAY FEVER; URTICARIA; and RHINITIS; and also in veterinary applications. Tripelennamine is administered by various routes, including topically.		210aromatic amine
troglitazone
Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.		2.4520chromanes;
thiazolidinone		anticoagulant;
anticonvulsant;
antineoplastic agent;
antioxidant;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
hypoglycemic agent;
platelet aggregation inhibitor;
vasodilator agent
thenoyltrifluoroacetone
Thenoyltrifluoroacetone: Chelating agent and inhibitor of cellular respiration.		2.0810
tulobuterol
[no description available]		8.18109organochlorine compound
tyrphostin a9
[no description available]		2.0510alkylbenzenegeroprotector
undecylenic acid
undecylenic acid: a fatty acid with a terminal double bond. 10-undecenoic acid : An undecenoic acid having its double bond in the 10-position. It is derived from castor oil and is used for the treatment of skin problems.. undecenoic acid : A C11, straight-chain fatty acid carrying a C=C double bond at any position.		2.0810undecenoic acidantifungal drug;
plant metabolite
urapidil
[no description available]		2.0810piperazines
venlafaxine
venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.		2.0810cyclohexanols;
monomethoxybenzene;
tertiary alcohol;
tertiary amino compound		adrenergic uptake inhibitor;
analgesic;
antidepressant;
dopamine uptake inhibitor;
environmental contaminant;
serotonin uptake inhibitor;
xenobiotic
vigabatrin
[no description available]		2.0810gamma-amino acidanticonvulsant;
EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor
pirinixic acid
pirinixic acid: structure		2.4520aryl sulfide;
organochlorine compound;
pyrimidines
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine: adenosine receptor antagonist		2.0510
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole: antineoplastic; activates platelet guanylate cyclase; a radiosensitizing agent and guanylate cyclase activator; structure in first source. lificiguat : A member of the class of indazoles that is 1H-indazole which is substituted by a benzyl group at position 1 and a 5-(hydroxymethyl)-2-furyl group at position 3. It is an activator of soluble guanylate cyclase and inhibits platelet aggregation.		2.0510aromatic primary alcohol;
furans;
indazoles		antineoplastic agent;
apoptosis inducer;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent
ici 204,219
zafirlukast: a leukotriene D4 receptor antagonist		8.38123carbamate ester;
indoles;
N-sulfonylcarboxamide		anti-asthmatic agent;
leukotriene antagonist
zaleplon
zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam. zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position.		2.0810nitrile;
pyrazolopyrimidine		anticonvulsant;
anxiolytic drug;
central nervous system depressant;
sedative
zonisamide
Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position.		2.08101,2-benzoxazoles;
sulfonamide		anticonvulsant;
antioxidant;
central nervous system drug;
protective agent;
T-type calcium channel blocker
zopiclone
zopiclone: S(+)-enantiomer of racemic zopiclone; azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; was term of zopiclone 2004-2007. zopiclone : A pyrrolo[3,4-b]pyrazine compound having a 4-methylpiperazine-1-carboxyl group at the 5-position, a 5-chloropyridin-2-yl group at the 6-position and an oxo-substituent at the 7-position.		2.4720monochloropyridine;
pyrrolopyrazine		central nervous system depressant;
sedative
corticosterone
[no description available]		2.051011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone		human metabolite;
mouse metabolite
prednisolone
Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.		5.586311beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic
reserpine
Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.		2.7530alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
phentolamine
Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension.		1.9810imidazoles;
phenols;
substituted aniline;
tertiary amino compound		alpha-adrenergic antagonist;
vasodilator agent
sorbitol
D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol).		2.0310glucitolcathartic;
Escherichia coli metabolite;
food humectant;
human metabolite;
laxative;
metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite;
sweetening agent
isoproterenol hydrochloride
[no description available]		2.0510catechols
hydroxyproline
Hydroxyproline: A hydroxylated form of the imino acid proline. A deficiency in ASCORBIC ACID can result in impaired hydroxyproline formation.. hydroxyproline : A proline derivative that is proline substituted by at least one hydroxy group.		3.38114-hydroxyproline;
L-alpha-amino acid zwitterion		human metabolite;
mouse metabolite;
plant metabolite
thyroxine
Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.		2.48202-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine zwitterion;
thyroxine		antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		4.7871ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
spironolactone
Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.		2.05103-oxo-Delta(4) steroid;
oxaspiro compound;
steroid lactone;
thioester		aldosterone antagonist;
antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
penicillamine
Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group.		2.4620non-proteinogenic alpha-amino acid;
penicillamine		antirheumatic drug;
chelator;
copper chelator;
drug allergen
prednisone
Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.		10.1814711-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
estrone
Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.		2.051017-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols		antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
paramethasone
Paramethasone: A glucocorticoid with the general properties of corticosteroids. It has been used by mouth in the treatment of all conditions in which corticosteroid therapy is indicated except adrenal-deficiency states for which its lack of sodium-retaining properties makes it less suitable than HYDROCORTISONE with supplementary FLUDROCORTISONE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p737)		2.0510fluorinated steroid
androsterone
[no description available]		2.051017-oxo steroid;
3alpha-hydroxy steroid;
androstanoid;
C19-steroid		androgen;
anticonvulsant;
human blood serum metabolite;
human metabolite;
human urinary metabolite;
mouse metabolite;
pheromone
dehydroepiandrosterone
Dehydroepiandrosterone: A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.. dehydroepiandrosterone : An androstanoid that is androst-5-ene substituted by a beta-hydroxy group at position 3 and an oxo group at position 17. It is a naturally occurring steroid hormone produced by the adrenal glands.		2.131017-oxo steroid;
3beta-hydroxy-Delta(5)-steroid;
androstanoid		androgen;
human metabolite;
mouse metabolite
promazine hydrochloride
[no description available]		2.0510hydrochloride
pilocarpine
Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.		1.9810pilocarpineantiglaucoma drug
dimethylphenylpiperazinium iodide
Dimethylphenylpiperazinium Iodide: A selective nicotinic cholinergic agonist used as a research tool. DMPP activates nicotinic receptors in autonomic ganglia but has little effect at the neuromuscular junction.		2.0510N-arylpiperazine;
organic iodide salt;
piperazinium salt;
quaternary ammonium salt		nicotinic acetylcholine receptor agonist
racepinephrine hydrochloride
[no description available]		2.0510
(4-(m-chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride
(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride: A drug that selectively activates certain subclasses of muscarinic receptors and also activates postganglionic nicotinic receptors. It is commonly used experimentally to distinguish muscarinic receptor subtypes.		2.0510
carbon tetrachloride
Carbon Tetrachloride: A solvent for oils, fats, lacquers, varnishes, rubber waxes, and resins, and a starting material in the manufacturing of organic compounds. Poisoning by inhalation, ingestion or skin absorption is possible and may be fatal. (Merck Index, 11th ed). tetrachloromethane : A chlorocarbon that is methane in which all the hydrogens have been replaced by chloro groups.		2.0810chlorocarbon;
chloromethanes		hepatotoxic agent;
refrigerant
cantharidin
Cantharidin: A toxic compound, isolated from the Spanish fly or blistering beetle (Lytta (Cantharis) vesicatoria) and other insects. It is a potent and specific inhibitor of protein phosphatases 1 (PP1) and 2A (PP2A). This compound can produce severe skin inflammation, and is extremely toxic if ingested orally.. cantharidin : A monoterpenoid with an epoxy-bridged cyclic dicarboxylic anhydride structure secreted by many species of blister beetle, and most notably by the Spanish fly, Lytta vesicatoria. Natural toxin inhibitor of protein phosphatases 1 and 2A.		2.0510cyclic dicarboxylic anhydride;
monoterpenoid		EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
herbicide
tetraethylammonium chloride
tetraethylammonium chloride : A quarternary ammonium chloride salt in which the cation has four ethyl substituents around the central nitrogen.		2.0510organic chloride salt;
quaternary ammonium salt		potassium channel blocker
alanine
Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.		1.9910alanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid		EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
chloramphenicol
Amphenicol: Chloramphenicol and its derivatives.		2.0810C-nitro compound;
carboxamide;
diol;
organochlorine compound		antibacterial drug;
antimicrobial agent;
Escherichia coli metabolite;
geroprotector;
Mycoplasma genitalium metabolite;
protein synthesis inhibitor
glutamine
Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.		5.522amino acid zwitterion;
glutamine family amino acid;
glutamine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
Escherichia coli metabolite;
human metabolite;
metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
lysine
Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine.		3.3811aspartate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
lysine;
organic molecular entity;
proteinogenic amino acid		algal metabolite;
anticonvulsant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
cetrimonium bromide
cetyltrimethylammonium bromide : The organic bromide salt that is the bromide salt of cetyltrimethylammonium; one of the components of the topical antiseptic cetrimide.		2.0510organic bromide salt;
quaternary ammonium salt		detergent;
surfactant
physostigmine
Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.		2.0510carbamate ester;
indole alkaloid		antidote to curare poisoning;
EC 3.1.1.8 (cholinesterase) inhibitor;
miotic
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		2.081017-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
tubocurarine
Tubocurarine: A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.. tubocurarine : A benzylisoquinoline alkaloid muscle relaxant which constitutes the active component of curare.. isoquinoline alkaloid : Any alkaloid that has a structure based on an isoquinoline nucleus. They are derived from the amino acids like tyrosine and phenylalanine.		2.0810bisbenzylisoquinoline alkaloiddrug allergen;
muscle relaxant;
nicotinic antagonist
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		2.0810aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
promethazine hydrochloride
[no description available]		2.0510hydrochlorideanti-allergic agent;
anticoronaviral agent;
antiemetic;
antipruritic drug;
geroprotector;
H1-receptor antagonist;
local anaesthetic;
sedative
kanamycin a
Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components.		2.0810kanamycinsbacterial metabolite
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.		15.244917monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		2.4720amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		4.811amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
methoxamine hydrochloride
[no description available]		2.0510dimethoxybenzene
adenosine monophosphate
Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.		10.031411adenosine 5'-phosphate;
purine ribonucleoside 5'-monophosphate		adenosine A1 receptor agonist;
cofactor;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
EC 3.1.3.11 (fructose-bisphosphatase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
papaverine hydrochloride
[no description available]		2.0510
bretylium tosylate
Bretylium Tosylate: An agent that blocks the release of adrenergic transmitters and may have other actions. It was formerly used as an antihypertensive agent, but is now proposed as an anti-arrhythmic.. bretylium tosylate : The tosylate salt of bretylium. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation.		2.0510organosulfonate salt;
quaternary ammonium salt		adrenergic antagonist;
anti-arrhythmia drug;
antihypertensive agent
methacholine chloride
Methacholine Chloride: A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)		14.135643quaternary ammonium salt
androstenedione
Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.. androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads.		2.051017-oxo steroid;
3-oxo-Delta(4) steroid;
androstanoid		androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
lactose
Lactose: A disaccharide of GLUCOSE and GALACTOSE in human and cow milk. It is used in pharmacy for tablets, in medicine as a nutrient, and in industry.. lactose : A glycosylglucose disaccharide, found most notably in milk, that consists of D-galactose and D-glucose fragments bonded through a beta-1->4 glycosidic linkage. The glucose fragment can be in either the alpha- or beta-pyranose form, whereas the galactose fragment can only have the beta-pyranose form.. beta-lactose : The beta-anomer of lactose.		4.41200lactose
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		4.3340alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
yohimbine hydrochloride
[no description available]		2.0510
fluocinolone acetonide
Fluocinolone Acetonide: A glucocorticoid derivative used topically in the treatment of various skin disorders. It is usually employed as a cream, gel, lotion, or ointment. It has also been used topically in the treatment of inflammatory eye, ear, and nose disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p732). fluocinolone acetonide : A fluorinated steroid that is flunisolide in which the hydrogen at position 9 is replaced by fluorine. A corticosteroid with glucocorticoid activity, it is used (both as the anhydrous form and as the dihydrate) in creams, gels and ointments for the treatment of various skin disorders.		5.213111beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic ketal;
fluorinated steroid;
glucocorticoid;
organic heteropentacyclic compound;
primary alpha-hydroxy ketone		anti-inflammatory drug;
antipruritic drug
triamcinolone diacetate
triamcinolone diacetate: lysyl oxidase antagonist; Polcortolon may also refers to triamcinolone		2.0810corticosteroid hormone
17-alpha-hydroxyprogesterone
17alpha-hydroxyprogesterone : A 17alpha-hydroxy steroid that is the 17alpha-hydroxy derivative of progesterone.		2.051017alpha-hydroxy-C21-steroid;
17alpha-hydroxy steroid;
tertiary alpha-hydroxy ketone		human metabolite;
metabolite;
mouse metabolite;
progestin
quinacrine monohydrochloride
[no description available]		2.0510
chlorpromazine hydrochloride
[no description available]		2.0510hydrochloride;
phenothiazines		anticoronaviral agent;
phenothiazine antipsychotic drug
mannitol
[no description available]		2.4520mannitolallergen;
antiglaucoma drug;
compatible osmolytes;
Escherichia coli metabolite;
food anticaking agent;
food bulking agent;
food humectant;
food stabiliser;
food thickening agent;
hapten;
metabolite;
osmotic diuretic;
sweetening agent
cytarabine
[no description available]		2.4720beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
medroxyprogesterone acetate
[no description available]		2.081020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
corticosteroid;
steroid ester		adjuvant;
androgen;
antineoplastic agent;
antioxidant;
female contraceptive drug;
inhibitor;
progestin;
synthetic oral contraceptive
sulfobromophthalein sodium
bromosulfophthalein sodium : An organic sodium salt that is the disodium salt of bromosulfophthalein.. bromosulfophthalein : An organosulfonic acid that consists of phthalide bearing four bromo substituents at positions 4, 5, 6 and 7 as well as two 4-hydroxy-3-sulfophenyl groups both located at position 1.		2.0510organic sodium saltdye
valine
Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine.		2.1310L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid;
valine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.0510erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
lidocaine hydrochloride
lidocaine hydrochloride : The anhydrous form of the hydrochloride salt of lidocaine.		2.0510hydrochlorideanti-arrhythmia drug;
local anaesthetic
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		10.32116arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
1,1,2-trichloro-1,2,2-trifluoroethane
[no description available]		2.4120chlorofluorocarbon;
haloalkane		NMR solvent;
refrigerant
triamcinolone acetonide
Triamcinolone Acetonide: An esterified form of TRIAMCINOLONE. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.. triamcinolone acetonide : A synthetic glucocorticoid that is the 16,17-acetonide of triamcinolone. Used to treat various skin infections.		7.596311beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
cyclic ketal;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone		anti-allergic agent;
anti-inflammatory drug
phencyclidine
Phencyclidine: A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.. phencyclidine : A member of the class of piperidines that is piperidine in which the nitrogen is substituted with a 1-phenylcyclohexyl group. Formerly used as an anaesthetic agent, it exhibits both hallucinogenic and neurotoxic effects.		6.763benzenes;
piperidines		anaesthetic;
neurotoxin;
NMDA receptor antagonist;
psychotropic drug
acrylic acid
acrylic acid: RN given refers to parent cpd. acrylic acid : A alpha,beta-unsaturated monocarboxylic acid that is ethene substituted by a carboxy group.		4.811alpha,beta-unsaturated monocarboxylic acidmetabolite
rhodamine b
rhodamine B: RN & N1 from 9th CI Form Index; RN given refers to parent cpd; structure in Merck Index, 9th ed, #7973; TETRAETHYLRHODAMINE was see RHODAMINES 1975-93; use RHODAMINES to search TETRAETHYLRHODAMINE 1975-93. rhodamine B : An organic chloride salt having N-[9-(2-carboxyphenyl)-6-(diethylamino)-3H-xanthen-3-ylidene]-N-ethylethanaminium as the counterion. An amphoteric dye commonly used as a fluorochrome.		4.811organic chloride salt;
xanthene dye		fluorescent probe;
fluorochrome;
histological dye
methylprednisolone
Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.		3.15506-methylprednisolone;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antiemetic;
environmental contaminant;
neuroprotective agent;
xenobiotic
rotenone
Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.		2.4720organic heteropentacyclic compound;
rotenones		antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin
pyocyanine
Pyocyanine: Antibiotic pigment produced by Pseudomonas aeruginosa.. pyocyanine : An iminium betaine that is 5-methylphenazin-5-ium which is substituted at position 1 by an oxidanidyl group. An antibiotic pigment produced by Pseudomonas aeruginosa.		2.3920iminium betaine;
phenazines		antibacterial agent;
bacterial metabolite;
biological pigment;
virulence factor
1-hydroxy-2-naphthoic acid
1-hydroxy-2-naphthoic acid: RN given refers to parent cpd. 1-hydroxy-2-naphthoic acid : A naphthoic acid with the carboxy group at position 2 and carrying a hydroxy substituent at the 1-position. It is a xenobiotic metabolite produced by the biodegradation of phenanthrene by microorganisms.		10.1731hydroxy monocarboxylic acid;
naphthoic acid;
naphthols		bacterial xenobiotic metabolite;
fungal xenobiotic metabolite
n-vinyl-2-pyrrolidinone
N-vinyl-2-pyrrolidinone: monomer of POVIDONE; structure given in first source		4.811pyrrolidin-2-ones
pseudoephedrine
Pseudoephedrine: A phenethylamine that is an isomer of EPHEDRINE which has less central nervous system effects and usage is mainly for respiratory tract decongestion.. pseudoephedrine : A member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group.		2.0510phenylethanolamines;
secondary alcohol;
secondary amino compound		anti-asthmatic drug;
bronchodilator agent;
central nervous system drug;
nasal decongestant;
plant metabolite;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
2-naphthylamine
2-Naphthylamine: A naphthalene derivative with carcinogenic action.. 2-naphthylamine : A naphthylamine carrying the amino group at position 2.		2.1310naphthylaminecarcinogenic agent
ethylbenzene
[no description available]		4.811alkylbenzene
quinuclidines
Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group.		7.0441quinuclidines;
saturated organic heterobicyclic parent
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		2.3820pyrrole;
secondary amine
imipramine hydrochloride
[no description available]		2.0510hydrochlorideantidepressant
phenformin
Phenformin: A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). phenformin : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis.		2.4720biguanidesantineoplastic agent;
geroprotector;
hypoglycemic agent
framycetin
Framycetin: A component of NEOMYCIN that is produced by Streptomyces fradiae. On hydrolysis it yields neamine and neobiosamine B. (From Merck Index, 11th ed). framycetin : A tetracyclic antibacterial agent derived from neomycin, being a glycoside ester of neamine and neobiosamine B.		4.811aminoglycosideallergen;
antibacterial drug;
Escherichia coli metabolite
suramin sodium
suramin sodium : An organic sodium salt that is the hexasodium salt of suramin. It is an FDA approved drug for African sleeping sickness and river blindness.		2.0510organic sodium saltangiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
pyrazolanthrone
pyrazolanthrone: JNK (c-Jun N-terminal kinase) inhibitor; structure in first source. anthra[1,9-cd]pyrazol-6(2H)-one : A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase.		2.0510anthrapyrazole;
aromatic ketone;
cyclic ketone		antineoplastic agent;
c-Jun N-terminal kinase inhibitor;
geroprotector
2-naphthol
2-naphthol: RN given refers to parent cpd. 2-naphthol : A naphthol carrying a hydroxy group at position 2.. naphthols : Any hydroxynaphthalene derivative that has a single hydroxy substituent.		5.1731naphtholantinematodal drug;
genotoxin;
human urinary metabolite;
human xenobiotic metabolite;
mouse metabolite;
radical scavenger
methapyrilene hydrochloride
methapyrilene hydrochloride : A hydrochloride that is the monohydrochloride salt of methapyrilene.		2.0510hydrochlorideanti-allergic agent;
carcinogenic agent;
H1-receptor antagonist;
sedative
sterogenol
hexadecylpyridinium bromide: structure in first source. cetylpyridinium bromide : A pyridinium salt that has N-hexadecylpyridinium as the cation and bromide as the anion.		2.0510bromide salt;
pyridinium salt		antiseptic drug;
EC 2.7.11.18 (myosin-light-chain kinase) inhibitor;
surfactant
ethyl acetoacetate
ethyl acetoacetate: RN given refers to unlabeled parent cpd. ethyl acetoacetate : An ethyl ester resulting from the formal condensation of the carboxy group of acetoacetic acid with ethanol.		2.1710ethyl esterantibacterial agent;
flavouring agent;
plant metabolite
2-chloroadenosine
5-chloroformycin A: structure given in first source		2.0510purine nucleoside
copper phthalocyanine
copper phthalocyanine: structure. copper(II) phthalocyanine : A metallophthalocyanine that is copper(2+) forming a coordination complex with phthalocyanine. It is a synthetic blue pigment which is used as a colorant in paints and dyes.		210
diphenhydramine hydrochloride
Antitussive Agents: Agents that suppress cough. They act centrally on the medullary cough center. EXPECTORANTS, also used in the treatment of cough, act locally.. diphenhydramine hydrochloride : The hydrochloride salt of diphenhydramine.		2.5220hydrochloride;
organoammonium salt		anti-allergic agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
sedative
cycloguanil
cycloguanil: the active metabolite of proguanil; antifolate drug; structure in first source. cycloguanil : A triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil.		2.0510triazinesantifolate;
antiinfective agent;
antimalarial;
antiparasitic agent;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.0710azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		4.811indazole
thiazoles
[no description available]		4.8111,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		2.3110diazine;
pyrazines		Daphnia magna metabolite
propantheline bromide
[no description available]		2.0510xanthenes
ephedrine
Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.. (-)-ephedrine : A phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively.		210phenethylamine alkaloid;
phenylethanolamines		bacterial metabolite;
environmental contaminant;
nasal decongestant;
plant metabolite;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
hydrazine
diamine : Any polyamine that contains two amino groups.		4.811azane;
hydrazines		EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor
pargyline hydrochloride
[no description available]		2.0510
hemicholinium 3
Hemicholinium 3: A potent inhibitor of the high affinity uptake system for CHOLINE. It has less effect on the low affinity uptake system. Since choline is one of the components of ACETYLCHOLINE, treatment with hemicholinium can deplete acetylcholine from cholinergic terminals. Hemicholinium 3 is commonly used as a research tool in animal and in vitro experiments.		2.110
evans blue
Evans Blue: An azo dye used in blood volume and cardiac output measurement by the dye dilution method. It is very soluble, strongly bound to plasma albumin, and disappears very slowly.. Evans blue : An organic sodium salt that is the tetrasodium salt of 6,6'-{(3,3'-dimethyl[1,1'-biphenyl]-4,4'-diyl)bis[diazene-2,1-diyl]}bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate). It is sometimes used as a counterstain, especially in fluorescent methods to suppress background autofluorescence.		2.420organic sodium saltfluorochrome;
histological dye;
sodium channel blocker;
teratogenic agent
aminophylline
Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio.		2.7130mixturebronchodilator agent;
cardiotonic drug
orphenadrine hydrochloride
orphenadrine hydrochloride : A hydrochloride comprising equimolar amounts of ophenadrine and hydrogen chloride.		2.0510hydrochlorideantiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist;
muscle relaxant;
NMDA receptor antagonist;
parasympatholytic
galantamine
Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils.		2.0810benzazepine alkaloid fundamental parent;
benzazepine alkaloid;
organic heterotetracyclic compound;
tertiary amino compound		antidote to curare poisoning;
cholinergic drug;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
plant metabolite
procarbazine hydrochloride
procarbazine hydrochloride : A hydrochloride obtained by combining procarbazine with one equivalent of hydrochloric acid. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		2.0810hydrochlorideantineoplastic agent
betamethasone
Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)		2.753011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-asthmatic agent;
anti-inflammatory drug;
immunosuppressive agent
benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(n,n-dimethyl-n-2-propenyl-), dibromide
Benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(N,N-dimethyl-N-2-propenyl-), Dibromide: Proposed cholinesterase inhibitor.		2.0510
cyproterone acetate
[no description available]		2.051020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
chlorinated steroid;
steroid ester		androgen antagonist;
geroprotector;
progestin
hydantoins
Hydantoins: Compounds based on imidazolidine dione. Some derivatives are ANTICONVULSANTS.. imidazolidine-2,4-dione : An imidazolidinone with oxo groups at position 2 and 4.		4.811imidazolidine-2,4-dione
dextropropoxyphene
Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene.		2.05101-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoatemu-opioid receptor agonist;
opioid analgesic
emetine
Emetine: The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS.. emetine : A pyridoisoquinoline comprising emetam having methoxy substituents at the 6'-, 7'-, 10- and 11-positions. It is an antiprotozoal agent and emetic. It inhibits SARS-CoV2, Zika and Ebola virus replication and displays antimalarial, antineoplastic and antiamoebic properties.		2.4720isoquinoline alkaloid;
pyridoisoquinoline		antiamoebic agent;
anticoronaviral agent;
antiinfective agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
expectorant;
plant metabolite;
protein synthesis inhibitor
benzohydroxamic acid
[no description available]		2.0510
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		9.48113
podophyllotoxin
Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA.		2.0510furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
medroxyprogesterone
[no description available]		2.051017alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
tertiary alpha-hydroxy ketone		contraceptive drug;
progestin;
synthetic oral contraceptive
luminol
Luminol: 5-Amino-2,3-dihydro-1,4-phthalazinedione. Substance that emits light on oxidation. It is used in chemical determinations.		210
tetrahydrozoline hydrochloride
tetrahydrozoline hydrochloride : The hydrochloride salt of tetryzoline. It is used as a nasal decongestant.		2.0510hydrochloridenasal decongestant;
sympathomimetic agent;
vasoconstrictor agent
dequalinium chloride
dequalinium chloride : An organic chloride salt that is the dichloride salt of dequalinium.		2.0510organic chloride saltantifungal agent;
antineoplastic agent;
antiseptic drug;
mitochondrial NADH:ubiquinone reductase inhibitor
dimenhydrinate
gravinol: has antioxidant and ant-inflammatory activities; structure in first source		2.0810diarylmethane
decamethonium dibromide
[no description available]		2.0510
malondialdehyde
Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form.		3.821dialdehydebiomarker
amitriptyline hydrochloride
[no description available]		2.0510organic tricyclic compound
naphazoline hydrochloride
[no description available]		2.0510organic molecular entity
1-naphthylisothiocyanate
1-Naphthylisothiocyanate: A tool for the study of liver damage which causes bile stasis and hyperbilirubinemia acutely and bile duct hyperplasia and biliary cirrhosis chronically, with changes in hepatocyte function. It may cause skin and kidney damage.		2.0810isothiocyanateinsecticide
doxylamine succinate
[no description available]		2.0510organic molecular entity
formestane
[no description available]		2.051017-oxo steroid;
3-oxo-Delta(4) steroid;
enol;
hydroxy steroid		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
megestrol acetate
[no description available]		2.472020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
steroid ester		antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive
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.		11.981510organic bromide salt;
quaternary ammonium salt
erythromycin
Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.		2.4720cyclic ketone;
erythromycin
hydroxychloroquine sulfate
[no description available]		2.0810
levonorgestrel
Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.		5.042117beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin;
synthetic oral contraceptive
norflurane
norflurane: may replace R 12 as air-conditioning refrigerant; structure given in first source		4.9833
Mecamylamine hydrochloride
[no description available]		2.0510monoterpenoid
cyproheptadine hydrochloride (anhydrous)
cyproheptadine hydrochloride (anhydrous) : The hydrochloride salt of cyproheptadine. Note that the drug named cyproheptadine hydrochloride generally refers to cyproheptadine hydrochloride sesquihydrate.		2.0510hydrochloride
ethambutol hydrochloride
ethambutol dihydrochloride : The dihydrchloride salt of ethambutol. A bacteriostatic antimycobacterial drug, it is effective against Mycobacterium tuberculosis and some other mycobacteria. It is used in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol dihydrochloride is used alone.		2.0810hydrochlorideantitubercular agent
calcium peroxide
[no description available]		4.811calcium oxides
manganese dioxide
[no description available]		4.811manganese molecular entity;
metal oxide
zinc oxide
Zinc Oxide: A mild astringent and topical protectant with some antiseptic action. It is also used in bandages, pastes, ointments, dental cements, and as a sunblock.		4.811zinc molecular entity
antimycin a
[no description available]		2.0810benzamides;
formamides;
macrodiolide;
phenols		antifungal agent;
mitochondrial respiratory-chain inhibitor;
piscicide
d-alpha tocopherol
Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.		3.3911alpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
pregnenolone carbonitrile
Pregnenolone Carbonitrile: A catatoxic steroid and microsomal enzyme inducer having significant effects on the induction of cytochrome P450. It has also demonstrated the potential for protective capability against acetaminophen-induced liver damage.		2.0810aliphatic nitrile
metylperon
metylperon: RN given refers to parent cpd		2.0810aromatic ketone
amiloride
Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid.		1.9910aromatic amine;
guanidines;
organochlorine compound;
pyrazines		diuretic;
sodium channel blocker
pimozide
Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.		2.0510benzimidazoles;
heteroarylpiperidine;
organofluorine compound		antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
sulfadoxine
Sulfadoxine: A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections.. sulfadoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial.		2.0510pyrimidines;
sulfonamide		antibacterial drug;
antimalarial
antazoline hydrochloride
[no description available]		2.0510
acetophenazine
acetophenazine: major descriptor (73-85); minor descriptor (64-72); on-line search PHENOTHIAZINES (64-85); Index Medicus search PHENOTHIAZINES (64-72); ACETOPHENAZINE (73-85); RN given refers to parent cpd. acetophenazine : A member of the class of phenothiazines that is 10H-phenothiazine substituted by a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at the nitogen atom and an acetyl group at position 2.		2.0510N-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
phenothiazines		phenothiazine antipsychotic drug
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		2.0810dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
dicloxacillin
Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group.		2.0810dichlorobenzene;
penicillin		antibacterial drug
fluorescein-5-isothiocyanate
Fluorescein-5-isothiocyanate: Fluorescent probe capable of being conjugated to tissue and proteins. It is used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.. fluorescein 5-isothiocyanate : The 5-isomer of fluorescein isothiocyanate. Acts as a fluorescent probe capable of being conjugated to tissue and proteins; used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.		2.1710fluorescein isothiocyanate
cladribine
[no description available]		2.0810organochlorine compound;
purine 2'-deoxyribonucleoside		antineoplastic agent;
immunosuppressive agent
beclomethasone
[no description available]		2.462011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
chlorinated steroid;
corticosteroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-asthmatic drug;
anti-inflammatory drug
pyrodifenium bromide
pyrodifenium bromide: was heading 1976-94 (see under PYRROLIDINES 1976-90); PRIFINIUM BROMIDE was see PYRODIFENIUM BROMIDE 1976-94: use PYRROLIDINES to search PYRODIFENIUM BROMIDE 1976-94; quaternary ammonium anticholinergic agent more specific for the gastrointestinal tract than atropine		2.0510organic molecular entity
buthionine sulfoximine
Buthionine Sulfoximine: A synthetic amino acid that depletes glutathione by irreversibly inhibiting gamma-glutamylcysteine synthetase. Inhibition of this enzyme is a critical step in glutathione biosynthesis. It has been shown to inhibit the proliferative response in human T-lymphocytes and inhibit macrophage activation. (J Biol Chem 1995;270(33):1945-7). 2-amino-4-(S-butylsulfonimidoyl)butanoic acid : A non-proteinogenic alpha-amino acid that is homocysteine in which the thiol group carries an oxo, imino and butyl groups.. S-butyl-DL-homocysteine (S,R)-sulfoximine : A sulfoximide that is the sulfoximine derivative of an analogue of DL-methionine in which the S-methyl group is replaced by S-butyl.		2.0510diastereoisomeric mixture;
homocysteines;
non-proteinogenic alpha-amino acid;
sulfoximide		EC 6.3.2.2 (glutamate--cysteine ligase) inhibitor;
ferroptosis inducer
metocurine
metocurine: from Chinese herb Cyclea hainanensis Mrr		2.0810isoquinolines
mexiletine hydrochloride
mexiletine hydrochloride : A hydrochloride composed of equimolar amounts of mexiletine and hydrogen chloride.		2.0510hydrochlorideanti-arrhythmia drug
cyclobenzaprine hydrochloride
cyclobenzaprine hydrochloride : The hydrochloride salt of cyclobenzaprine. A centrally acting skeletal muscle relaxant, it is used in the symptomatic treatment of painful muscle spasm.		2.0510hydrochlorideantidepressant;
muscle relaxant
3-deazaadenosine
3-deazaadenosine: RN given refers to parent cpd.		2.0510
metoclopramide hydrochloride
metoclopramide hydrochloride : A hydrate that is the monohydrate form of metoclopramide monohydrochloride.		2.0510
isoetharine mesylate
[no description available]		2.0510
etidronate disodium
etidronate disodium : An organic sodium salt resulting from the replacement of two protons from etidronic acid (one from from each of the phosphonic acid groups) by sodium ions.		2.0810organic sodium saltantineoplastic agent;
bone density conservation agent;
chelator
manganese
Manganese: A trace element with atomic symbol Mn, atomic number 25, and atomic weight 54.94. It is concentrated in cell mitochondria, mostly in the pituitary gland, liver, pancreas, kidney, and bone, influences the synthesis of mucopolysaccharides, stimulates hepatic synthesis of cholesterol and fatty acids, and is a cofactor in many enzymes, including arginase and alkaline phosphatase in the liver. (From AMA Drug Evaluations Annual 1992, p2035). manganese(4+) : A manganese cation that is monoatomic and has a formal charge of +4.		4.811elemental manganese;
manganese group element atom		Escherichia coli metabolite;
micronutrient
mercury
Mercury: A silver metallic element that exists as a liquid at room temperature. It has the atomic symbol Hg (from hydrargyrum, liquid silver), atomic number 80, and atomic weight 200.59. Mercury is used in many industrial applications and its salts have been employed therapeutically as purgatives, antisyphilitics, disinfectants, and astringents. It can be absorbed through the skin and mucous membranes which leads to MERCURY POISONING. Because of its toxicity, the clinical use of mercury and mercurials is diminishing.. mercury(0) : Elemental mercury of oxidation state zero.		4.811elemental mercury;
zinc group element atom		neurotoxin
molybdenum
Molybdenum: A metallic element with the atomic symbol Mo, atomic number 42, and atomic weight 95.95. It is an essential trace element, being a component of the enzymes xanthine oxidase, aldehyde oxidase, and nitrate reductase.		4.811chromium group element atommicronutrient
silver
Silver: An element with the atomic symbol Ag, atomic number 47, and atomic weight 107.87. It is a soft metal that is used medically in surgical instruments, dental prostheses, and alloys. Long-continued use of silver salts can lead to a form of poisoning known as ARGYRIA.		4.811copper group element atom;
elemental silver		Escherichia coli metabolite
titanium
Titanium: A dark-gray, metallic element of widespread distribution but occurring in small amounts with atomic number, 22, atomic weight, 47.867 and symbol, Ti; specific gravity, 4.5; used for fixation of fractures.		5.1421titanium group element atom
europium
Europium: An element of the rare earth family of metals. It has the atomic symbol Eu, atomic number 63, and atomic weight 152. Europium is used in the form of its salts as coatings for cathode ray tubes and in the form of its organic derivatives as shift reagents in NMR spectroscopy.		7.2110f-block element atom;
lanthanoid atom
gold
Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.		10.0621copper group element atom;
elemental gold
zalcitabine
Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.		2.0810pyrimidine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
acetylglucosamine
Acetylglucosamine: The N-acetyl derivative of glucosamine.. N-acetyl-beta-D-glucosamine : An N-acetyl-D-glucosamine having beta-configuration at the anomeric centre.		2.0810N-acetyl-D-glucosamineepitope
galactosamine
2-amino-2-deoxy-D-galactopyranose : The pyranose form of D-galactosamine.. D-galactosamine : The D-stereoisomer of galactosamine.		4.9321D-galactosamine;
primary amino compound		toxin
phosphoric acid, trisodium salt
[no description available]		3.1510sodium phosphate
propionylpromazine hydrochloride
[no description available]		2.0510
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.4720delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
zinc sulfate
Zinc Sulfate: A compound given in the treatment of conditions associated with zinc deficiency such as acrodermatitis enteropathica. Externally, zinc sulfate is used as an astringent in lotions and eye drops. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995). zinc sulfate : A metal sulfate compound having zinc(2+) as the counterion.		4.811metal sulfate;
zinc molecular entity		fertilizer
sodium sulfite
[no description available]		2.0510inorganic sodium salt;
sulfite salt		food preservative;
reducing agent
tricalcium phosphate
tricalcium phosphate: a form of tricalcium phosphate used as bioceramic bone replacement material; see also records for alpha-tricalcium phosphate, beta-tricalcium phosphate, calcium phosphate; apatitic tricalcium phosphate Ca9(HPO4)(PO4)5(OH) is the calcium orthophosphate leading to beta tricalcium phosphate Ca3(PO4)2 (b-TCP). calcium phosphate : A calcium salt composed of calcium and phosphate/diphosphate ions; present in milk and used for the mineralisation of calcified tissues.		4.811calcium phosphate
deuterium
Deuterium: The stable isotope of hydrogen. It has one neutron and one proton in the nucleus.		2.1710dihydrogen
ozone
Ozone: The unstable triatomic form of oxygen, O3. It is a powerful oxidant that is produced for various chemical and industrial uses. Its production is also catalyzed in the ATMOSPHERE by ULTRAVIOLET RAY irradiation of oxygen or other ozone precursors such as VOLATILE ORGANIC COMPOUNDS and NITROGEN OXIDES. About 90% of the ozone in the atmosphere exists in the stratosphere (STRATOSPHERIC OZONE).. ozone : An elemental molecule with formula O3. An explosive, pale blue gas (b.p. -112degreeC) that has a characteristic, pungent odour, it is continuously produced in the upper atmosphere by the action of solar ultraviolet radiation on atmospheric oxygen. It is an antimicrobial agent used in the production of bottled water, as well as in the treatment of meat, poultry and other foodstuffs.		3.4311elemental molecule;
gas molecular entity;
reactive oxygen species;
triatomic oxygen		antiseptic drug;
disinfectant;
electrophilic reagent;
greenhouse gas;
mutagen;
oxidising agent;
tracer
amopyroquine
amopyroquine: RN given refers to parent cpd; structure		2.0510
trolamine salicylate
Arthritis: Acute or chronic inflammation of JOINTS.		2.0310
mafenide acetate
[no description available]		2.0810carboxylic acid
titanium dioxide
titanium dioxide: used medically as protectant against externally caused irritation & sunlight; high concentrations of dust may cause irritation to respiratory tract; RN given refers to titanium oxide (TiO2); structure. titanium dioxide : A titanium oxide with the formula TiO2. A naturally occurring oxide sourced from ilmenite, rutile and anatase, it has a wide range of applications.		4.811titanium oxidesfood colouring
soterenol
soterenol: adrenergic beta-2 agonist used as bronchodilator; it has a number of gastrointestinal side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search ETHANOLAMINES (75-86); RN given refers to parent cpd without isomeric designation		1.9910
diacerein
diacerein: chelates with bivalent metals; a quinone which possesses redox properties; metabolized to active rhein; proposed mechanisms include inhibiting IL1 and metalloproteinases; called a slow acting symptomatic drug in osteoarthritis; no effect of cyclooxygenase;		2.0810anthraquinone
xipamide
Xipamide: A sulfamoylbenzamide analog of CLOPAMIDE. It is diuretic and saluretic with antihypertensive activity. It is bound to PLASMA PROTEINS, thus has a delayed onset and prolonged action.		2.0510benzamides
selegiline hydrochloride, (r)-isomer
[no description available]		2.0810hydrochloride;
terminal acetylenic compound		antiparkinson drug;
dopaminergic agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor
levamisole
Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine.		2.05106-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazoleantinematodal drug;
antirheumatic drug;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
immunological adjuvant;
immunomodulator
benserazide hydrochloride
benserazide hydrochloride : A hydrochloride that is the monohydrochloride salt of benserazide. An aromatic-L-amino-acid decarboxylase inhibitor (DOPA decarboxylase inhibitor) that does not enter the central nervous system, it is used as an adjunct to levodopa in the treatment of parkinsonism. By preventing the conversion of levodopa to dopamine in the periphery, it causes an increase in the amount of levodopa reaching the central nervous system and so reduces the required dose. Benserazide hydrochloride has no antiparkinson actions when given alone.		2.0510hydrochlorideantiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
thiamphenicol
[no description available]		2.0810monocarboxylic acid amide;
sulfone		antimicrobial agent;
immunosuppressive agent
pancuronium bromide
pancuronium bromide : A bromide salt consisting of two bromide ions and one pancuronium dication.		2.4720bromide saltcholinergic antagonist;
muscle relaxant;
nicotinic antagonist
cromolyn sodium
Cromolyn Sodium: A chromone complex that acts by inhibiting the release of chemical mediators from sensitized MAST CELLS. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack.. disodium cromoglycate : An organic sodium salt that is the disodium salt of cromoglycic acid.		8.51115organic sodium saltanti-asthmatic drug;
drug allergen
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		2.4220acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
ornidazole
Ornidazole: A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.. ornidazole : A C-nitro compound that is 5-nitroimidazole in which the hydrogens at positions 1 and 2 are replaced by 3-chloro-2-hydroxypropyl and methyl groups, respectively. It is used in the treatment of susceptible protozoal infections and for the treatment of anaerobic bacterial infections.		2.0810C-nitro compound;
imidazoles;
organochlorine compound;
secondary alcohol		antiamoebic agent;
antibacterial drug;
antiinfective agent;
antiprotozoal drug;
antitrichomonal drug;
epitope
danazol
Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders.		2.753017beta-hydroxy steroid;
terminal acetylenic compound		anti-estrogen;
estrogen antagonist;
geroprotector
metergoline
Metergoline: A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.. metergoline : An ergoline alkaloid that is the N-benzyloxycarbonyl derivative of lysergamine. A 5-HT2 antagonist. Also 5-HT1 antagonist and 5-HT1D ligand. Has moderate affinity for 5-HT6 and high affinity for 5-HT7.		2.0510carbamate ester;
ergoline alkaloid		dopamine agonist;
geroprotector;
serotonergic antagonist
fludarabine phosphate
fludarabine phosphate: structure given in first source. fludarabine phosphate : A purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas.		2.0810nucleoside analogue;
organofluorine compound;
purine arabinonucleoside monophosphate		antimetabolite;
antineoplastic agent;
antiviral agent;
DNA synthesis inhibitor;
immunosuppressive agent;
prodrug
disopyramide phosphate
[no description available]		2.0510organoammonium phosphate
2-bromoergocryptine mesylate
[no description available]		2.0510methanesulfonate saltantiparkinson drug
bromocriptine
Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.		2.0510indole alkaloidantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
hormone antagonist
phenyl acetate
phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.		15.818240benzenes;
phenyl acetates
1,4-dioxane
1,4-dioxane: dehydrating agent; polar solvent miscible both with water & most organic solvents. dioxane : Any member of the class of dioxanes that is a cyclohexane in which two carbon atoms are replaced by oxygen atoms.. 1,4-dioxane : A dioxane with oxygen atoms at positions 1 and 4.		3.110dioxane;
volatile organic compound		carcinogenic agent;
metabolite;
NMR chemical shift reference compound;
non-polar solvent
triamcinolone
Triamcinolone: A glucocorticoid given, as the free alcohol or in esterified form, orally, intramuscularly, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. (From Martindale, The Extra Pharmacopoeia, 30th ed, p739). triamcinolone : A C21-steroid hormone that is 1,4-pregnadiene-3,20-dione carrying four hydroxy substituents at positions 11beta, 16alpha, 17alpha and 21 as well as a fluoro substituent at position 9. Used in the form of its 16,17-acetonide to treat various skin infections.		6.364111beta-hydroxy steroid;
16alpha-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-allergic agent;
anti-inflammatory drug
benzonidazole
benzonidazole: used in treatment of Chagas' disease. benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease.		2.4720C-nitro compound;
imidazoles;
monocarboxylic acid amide		antiprotozoal drug
halazepam
halazepam: structure		2.0510organic molecular entity
4-methoxyamphetamine
4-methoxyamphetamine: para-methoxy derivative to amphetamine with hallucinogenic properties; minor descriptor (75-86); on line & INDEX MEDICUS search AMPHETAMINES (75-86); RN given refers to parent compound without isomeric designation		2.0510
du-21220
Ritodrine: An adrenergic beta-2 agonist used to control PREMATURE LABOR.. 4-[2-[[1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]phenol : A secondary amino compound that is 4-(2-amino-1-hydroxypropyl)phenol in which one of the hydrogens attached to the nitrogen is replaced by a 2-(4-hydroxyphenyl)ethyl group.		2.1110benzyl alcohols;
polyphenol;
secondary alcohol;
secondary amino compound
8-bromo cyclic adenosine monophosphate
8-Bromo Cyclic Adenosine Monophosphate: A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.. 8-Br-cAMP : A 3',5'-cyclic purine nucleotide that is 3',5'-cyclic AMP bearing an additional bromo substituent at position 8 on the adenine ring. An activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.		2.92403',5'-cyclic purine nucleotide;
adenyl ribonucleotide;
organobromine compound		antidepressant;
protein kinase agonist
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		3.3811glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
dexchlorpheniramine
dexchlorpheniramine: RN given refers to parent cpd(S)-isomer		2.0510chlorphenamine
azides
Azides: Organic or inorganic compounds that contain the -N3 group.. azide : Any nitrogen molecular entity containing the group -N3.		210pseudohalide anionmitochondrial respiratory-chain inhibitor
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		2.0810penicillin allergen;
penicillin		antibacterial drug
timolol
(S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine.		2.4720timololanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
indoramin
Indoramin: An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent.		2.0810tryptamines
oxcarbazepine
Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy.		2.0810cyclic ketone;
dibenzoazepine		anticonvulsant;
drug allergen
carbidopa
carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa.		2.0810catechols;
hydrazines;
monocarboxylic acid		antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
amineptin
amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne.		2.0510amino acid;
carbocyclic fatty acid;
carbotricyclic compound;
secondary amino compound		antidepressant;
dopamine uptake inhibitor
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		2.0810azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
feprazone
Feprazone: A pyrazole that has analgesic, anti-inflammatory, and antipyretic properties. It has been used in mild to moderate pain, fever, and inflammation associated with musculoskeletal and joint disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p15)		2.0810organic molecular entity
7-ethoxycoumarin
7-ethoxycoumarin : A member of the class of coumarins that is umbelliferone in which the hydroxy group at position 7 is replaced by an ethoxy group.		210aromatic ether;
coumarins
tobramycin
Tobramycin: An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the PSEUDOMONAS species. It is a 10% component of the antibiotic complex, NEBRAMYCIN, produced by the same species.. tobramycin : A amino cyclitol glycoside that is kanamycin B lacking the 3-hydroxy substituent from the 2,6-diaminoglucose ring.		2.0810amino cyclitol glycosideantibacterial agent;
antimicrobial agent;
toxin
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.4720taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
buspirone hydrochloride
buspirone hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of buspirone and hydrogen chloride.		2.0510hydrochlorideanxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
etoposide
[no description available]		2.7530beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
substance p
[no description available]		210peptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent
propafenone hydrochloride
propafenone hydrochloride : A hydrochloride that is the monohydrochloride salt of propafenone. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used in the management of supraventricular and ventricular arrhythmias.		2.0510hydrochlorideanti-arrhythmia drug
etazolate hydrochloride
[no description available]		2.0510
halofantrine
halofantrine: used in treatment of mild to moderate acute malaria		2.0510phenanthrenes
ribavirin
Rebetron: Rebetron is tradename		2.47201-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
amikacin
Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group.		2.0810alpha-D-glucoside;
amino cyclitol glycoside;
aminoglycoside;
carboxamide		antibacterial drug;
antimicrobial agent;
nephrotoxin
carbidopa
[no description available]		2.0510catechols;
hydrate;
hydrazines;
monocarboxylic acid		antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
hydroxymaprotilin
hydroxymaprotilin: RN given refers to cpd without isomeric designation		2.0510
methyldopa
Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring.		2.0510L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		alpha-adrenergic agonist;
antihypertensive agent;
hapten;
peripheral nervous system drug;
sympatholytic agent
tocainide
Tocainide: An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS.. tocainide : A monocarboxylic acid amide in which 2,6-dimethylphenylaniline and isobutyric acid have combined to form the amide bond; used as a local anaesthetic.		2.0510monocarboxylic acid amideanti-arrhythmia drug;
local anaesthetic;
sodium channel blocker
sq-11725
Nadolol: A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.. nadolol : Nadolol is a diastereoisomeric mixture consisting of equimolar amounts of the four possible 2,3-cis-isomers of 5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol.		2.0510
diltiazem
Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension.		2.47205-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
1-methyl-4-phenylpyridinium
1-Methyl-4-phenylpyridinium: An active neurotoxic metabolite of 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE. The compound reduces dopamine levels, inhibits the biosynthesis of catecholamines, depletes cardiac norepinephrine and inactivates tyrosine hydroxylase. These and other toxic effects lead to cessation of oxidative phosphorylation, ATP depletion, and cell death. The compound, which is related to PARAQUAT, has also been used as an herbicide.. N-methyl-4-phenylpyridinium : A pyridinium ion that is N-methylpyridinium having a phenyl substituent at the 4-position.		2.0310pyridinium ionapoptosis inducer;
herbicide;
human xenobiotic metabolite;
neurotoxin
vecuronium bromide
Vecuronium Bromide: Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents.. vecuronium bromide : The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium substituents.		2.0810organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent;
nicotinic antagonist
pinazepam
pinazepam: structure		2.0510benzodiazepine
flecainide acetate
flecainide acetate : An acetate salt obtained by combining flecainide with one molar equivalent of acetic acid. An antiarrhythmic agent used to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		2.0510acetate saltanti-arrhythmia drug
nicardipine hydrochloride
[no description available]		2.0510dihydropyridinegeroprotector
butibufen
butibufen: RN given refers to parent cpd		2.0510monoterpenoid
nitazoxanide
nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug		2.0810benzamides;
carboxylic ester
acarbose
[no description available]		2.0810tetrasaccharide derivativeEC 3.2.1.1 (alpha-amylase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
geroprotector;
hypoglycemic agent
torsemide
Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure.		1.9810aminopyridine;
N-sulfonylurea;
secondary amino compound		antihypertensive agent;
loop diuretic
lorcainide
[no description available]		2.0810acetamides
idarubicin
Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA.		2.0510anthracycline antibiotic;
deoxy hexoside;
monosaccharide derivative
cefonicid
Cefonicid: A second-generation cephalosporin administered intravenously or intramuscularly. Its bactericidal action results from inhibition of cell wall synthesis. It is used for urinary tract infections, lower respiratory tract infections, and soft tissue and bone infections.. cefonicid : A cephalosporin bearing {[1-(sulfomethyl)-1H-tetrazol-5-yl]sulfanyl}methyl and (R)-2-hydroxy-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		3.1310cephalosporinantibacterial drug
piperacillin
Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group.		6.9810penicillin allergen;
penicillin		antibacterial drug
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		2.0510aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
captopril
Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.		2.4720alkanethiol;
L-proline derivative;
N-acylpyrrolidine;
pyrrolidinemonocarboxylic acid		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
staurosporine
[no description available]		2.4720indolocarbazole alkaloid;
organic heterooctacyclic compound		apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
terazosin hydrochloride anhydrous
[no description available]		2.0510
foscarnet sodium
trisodium phosphonoformate : The trisodium salt of phosphonoformic acid. It is used as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		2.0810one-carbon compound;
organic sodium salt		antiviral drug
atracurium besylate
atracurium besylate : The bisbenzenesulfonate salt of atracurium.		2.0810organosulfonate salt;
quaternary ammonium salt		muscle relaxant;
nicotinic antagonist
nicorandil
Nicorandil: A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.. nicorandil : A pyrimidinecarboxamide that is nicotinamide in which one of the hydrogens attached to the carboxamide nitrogen is replaced by a 2-(nitrooxy)ethyl group. It has both nitrate-like and ATP-sensitive potassium channel activator properties, and is used for the prevention and treatment of angina pectoris.		2.0810nitrate ester;
pyridinecarboxamide		potassium channel opener;
vasodilator agent
pergolide mesylate
pergolide mesylate : A methanesulfonate salt obtained from pergolide by mixing eqimolar amount of pergolide and methanesulfonic acid. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		2.4720methanesulfonate saltantiparkinson drug;
dopamine agonist;
geroprotector
colforsin
Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.		3.73100acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
cefadroxil anhydrous
Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		2.0810cephalosporinantibacterial drug
talniflumate
talniflumate: an anti-inflammatory molecule for the treatment of cystic fibrosis, chronic obstructive pulmonary disease and asthma		2.0810benzofurans
fenoldopam mesylate
[no description available]		2.0810benzazepine
nedocromil
Nedocromil: A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with ASTHMA, including EOSINOPHILS; NEUTROPHILS; MACROPHAGES; MAST CELLS; MONOCYTES; AND PLATELETS.		5.1962dicarboxylic acid;
organic heterotricyclic compound		anti-allergic agent;
anti-asthmatic drug;
non-steroidal anti-inflammatory drug
cefaclor anhydrous
Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		2.0810cephalosporinantibacterial drug;
drug allergen
pefloxacin
Pefloxacin: A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.. pefloxacin : A quinolone that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6 and 7 by ethyl, carboxy, fluorine, and 4-methylpiperazin-1-yl groups, respectively.		2.0810fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
antiinfective agent;
DNA synthesis inhibitor
alfentanil
Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position.		2.0510monocarboxylic acid amide;
piperidines		central nervous system depressant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
peripheral nervous system drug
cefotetan
Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms.		2.0810
lovastatin
Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).		2.0810delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		anticholesteremic drug;
antineoplastic agent;
Aspergillus metabolite;
prodrug
flupirtine
flupirtine: RN given refers to parent cpd without isomeric designation		2.0810aminopyridine
enoximone
Enoximone: A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE.		2.0810aromatic ketone
stepronin
[no description available]		2.0810N-acyl-amino acid
piritrexim
piritrexim: RN given refers to parent cpd; structure given in first source		2.0510
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		2.0810delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
idazoxan
Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.. idazoxan : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group.		2.0810benzodioxine;
imidazolines		alpha-adrenergic antagonist
remoxipride
Remoxipride: An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.		2.0810dimethoxybenzene
cabergoline
Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia.		2.0810N-acylureaantineoplastic agent;
antiparkinson drug;
dopamine agonist
bambuterol
bambuterol: selective inhibitor of butyrylcholinesterase & acetylcholinesterase. bambuterol : A carbamate ester that is terbutaline in which both of the phenolic hydroxy groups have been protected as the corresponding N,N-dimethylcarbamates. A long acting beta-adrenoceptor agonist used in the treatment of asthma, it is a prodrug for terbutaline.		6.8493carbamate ester;
phenylethanolamines		anti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
prodrug;
sympathomimetic agent;
tocolytic agent
atomoxetine hydrochloride
Atomoxetine Hydrochloride: A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.. atomoxetine hydrochloride : The hydrochloride salt of atomoxetine.		2.0810hydrochlorideadrenergic uptake inhibitor;
antidepressant
atomoxetine
atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents.		2.0510aromatic ether;
secondary amino compound;
toluenes		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
xenobiotic
quinapril
Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure.		2.0810dicarboxylic acid monoester;
ethyl ester;
isoquinolines;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
raloxifene hydrochloride
Raloxifene Hydrochloride: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.. raloxifene hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride.		2.0510hydrochloridebone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
mifepristone
Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.		2.97403-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound		abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
itraconazole
Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.. itraconazole : An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis.		2.2110aromatic ether;
conazole antifungal drug;
cyclic ketal;
dichlorobenzene;
dioxolane;
N-arylpiperazine;
triazole antifungal drug;
triazoles		EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
Hedgehog signaling pathway inhibitor;
P450 inhibitor
finasteride
Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.		2.47203-oxo steroid;
aza-steroid;
delta-lactam		androgen antagonist;
antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
imiquimod
Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis.		2.0810imidazoquinolineantineoplastic agent;
interferon inducer
sertindole
sertindole : A phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-oxoimidazolidin-1-yl)ethyl group.		2.0810heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole		alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist
adapalene
Adapalene: A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.. adapalene : A naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether.		2.0810adamantanes;
monocarboxylic acid;
naphthoic acid		dermatologic drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
non-steroidal anti-inflammatory drug
aromasil
[no description available]		2.081017-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor;
environmental contaminant;
xenobiotic
sparfloxacin
[no description available]		2.0810fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
zileuton
[no description available]		6.68611-benzothiophenes;
ureas		anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
cidofovir anhydrous
Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients.		2.0810phosphonic acids;
pyrimidone		anti-HIV agent;
antineoplastic agent;
antiviral drug;
photosensitizing agent
mibefradil dihydrochloride
[no description available]		2.0510
eliprodil
1-(4-chlorophenyl)-2-[4-(4-fluorobenzyl)piperidin-1-yl]ethanol : A member of the class of piperidines that is piperidine substituted by a 2-(4-chlorophenyl)-2-hydroxyethyl group at position 1 and by a 4-fluorobenzyl group at position 4.		2.0510monochlorobenzenes;
monofluorobenzenes;
piperidines;
secondary alcohol;
tertiary amino compound
bromfenac
bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure.		2.0810aromatic amino acid;
benzophenones;
organobromine compound;
substituted aniline		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
gemcitabine hydrochloride
[no description available]		2.0810hydrochloride;
organofluorine compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral drug;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
immunosuppressive agent;
radiosensitizing agent
aripiprazole
Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.		2.0810aromatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone		drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist
atorvastatin calcium anhydrous
[no description available]		2.0810organic calcium salt
lamivudine
[no description available]		2.0810monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
duloxetine hydrochloride
Duloxetine Hydrochloride: A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.. (S)-duloxetine hydrochloride : A duloxetine hydrochloride in which the duloxetine moiety has S configuration.		2.0810duloxetine hydrochlorideantidepressant
aptiganel hydrochloride
[no description available]		2.0510
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		2.0810biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
ibandronic acid
Ibandronic Acid: Aminobisphosphonate that is a potent inhibitor of BONE RESORPTION. It is used in the treatment of HYPERCALCEMIA associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of POSTMENOPAUSAL OSTEOPOROSIS.		2.0510
zolmitriptan
zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine.		2.0810oxazolidinone;
tryptamines		anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
adefovir dipivoxil
bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine: structure given in first source. adefovir pivoxil : An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection.		2.08106-aminopurines;
carbonate ester;
ether;
organic phosphonate		antiviral drug;
DNA synthesis inhibitor;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent;
prodrug
emtricitabine
Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection.		2.0810monothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone		antiviral drug;
HIV-1 reverse transcriptase inhibitor
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		5.8332adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
phenelzine sulfate
[no description available]		2.0510organic molecular entity
fluoxetine hydrochloride
fluoxetine hydrochloride : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine hydrochloride. A selective serotonin reuptake inhibitor (SSRI), it is used for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.		2.0510hydrochloride;
N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine
paroxetine hydrochloride
paroxetine hydrochloride : The hydrochloride salt of paroxetine. It is an antidepressant drug.		2.0810hydrochlorideantidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
propranolol hydrochloride
Inderex: combination of above cpds; used in treatment of hypertension		2.0510hydrochloride
bupropion hydrochloride
[no description available]		2.4720aromatic ketone
trazodone hydrochloride
Triticum: A plant genus of the family POACEAE that is the source of EDIBLE GRAIN. A hybrid with rye (SECALE CEREALE) is called TRITICALE. The seed is ground into FLOUR and used to make BREAD, and is the source of WHEAT GERM AGGLUTININS.. trazodone hydrochloride : A hydrochloride salt prepared from equimolar amounts of trazodone and hydrogen chloride.		2.4720hydrochlorideadrenergic antagonist;
antidepressant;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
trovafloxacin
trovafloxacin: a trifluoronaphthyridone derivative of 7-(3-azabicyclo(3.1.0)hexyl)naphthyridone; has antineoplastic activity. trovafloxacin : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 6-amino-3-azabicyclo[3.1.0]hex-3-yl substituents at positions 1, 6 and 7 respectively. A broad-spectrum antibiotic that was withdrawn from the market due to risk of liver failure.		2.0510
verapamil hydrochloride
verapamil hydrochloride : A racemate comprising equimolar amounts of dexverapamil hydrochloride and (S)-verapamil hydrochloride.		2.0510
doxazosin mesylate
Cardura: Trade name in United States.		2.4720methanesulfonate saltgeroprotector
terfenadine
[no description available]		2.0510diarylmethane
sertraline hydrochloride
sertraline hydrochloride : A hydrochloride resulting from the reaction of equimolar amounts of sertraline and hydrogen chloride. A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder.		2.0510hydrochlorideantidepressant;
serotonin uptake inhibitor
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		2.0810acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nelfinavir
Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.		2.0810aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound		antineoplastic agent;
HIV protease inhibitor
amantadine hydrochloride
[no description available]		2.0510hydrochlorideantiviral agent;
dopamine agonist;
NMDA receptor antagonist
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.		6.1552D-glucopyranoseepitope;
mouse metabolite
mevastatin
mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure. mevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.		2.08102-pyranones;
carboxylic ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		antifungal agent;
apoptosis inducer;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
fungal metabolite;
Penicillium metabolite
bupivacaine hydrochloride
bupivacaine hydrochloride (anhydrous) : A racemate composed of equimolar amounts of dextrobupivacaine hydrochloride and levobupivacaine hydrochloride. The monohydrate form is commonly used as a local anaesthetic.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride : A hydrochloride obtained by combining 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide with one molar equivalent of hydrochloric acid.		2.0810hydrochloride;
racemate		adrenergic antagonist;
amphiphile;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor;
local anaesthetic
chloroquine diphosphate
[no description available]		2.0510
ursolic acid
[no description available]		2.0510hydroxy monocarboxylic acid;
pentacyclic triterpenoid		geroprotector;
plant metabolite
propamidine
propamidine: structure given in first source. propamidine : A polyether that is the bis(4-guanidinophenyl) ether of propane-1,3-diol. Used (as its isethionate salt) for the treatment of minor eye or eyelid infections, such as conjunctivitis and blepharitis.		2.0510aromatic ether;
guanidines;
polyether		antimicrobial agent;
antiseptic drug
plerixafor
plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma.		2.0810azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound		anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant
amprenavir
[no description available]		2.0810carbamate ester;
sulfonamide;
tetrahydrofuryl ester		antiviral drug;
HIV protease inhibitor
1,2-dipalmitoyl-3-phosphatidylethanolamine
1,2-dipalmitoyl-3-phosphatidylethanolamine: RN given refers to parent cpd without isomeric designation		2.1710
dobutamine hydrochloride
dobutamine hydrochloride : The hydrochloride salt of dobutamine. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used to increase the contractility of the heart in the management of acute heart failure.		2.0510hydrochloridebeta-adrenergic agonist;
cardiotonic drug;
sympathomimetic agent
desipramine hydrochloride
desipramine hydrochloride : The hydrochloride salt of desipramine.		2.0510hydrochloridedrug allergen
ticlopidine hydrochloride
[no description available]		2.0810hydrochloride
dopamine hydrochloride
P 498: structure in first source; do not confuse with dopamine chloride, also known as P 498		2.0510catecholamine
proadifen hydrochloride
[no description available]		2.0510
epirubicin hydrochloride
[no description available]		2.0810
4-nitrobenzylthioinosine
4-nitrobenzylthioinosine: inhibitor of nucleoside transport; acts on ENT1		2.0510purine nucleoside
sinefungin
[no description available]		2.0510adenosines;
non-proteinogenic alpha-amino acid		antifungal agent;
antimicrobial agent
proxicromil
proxicromil: RN given refers to parent cpd; structure		1.9910
droxicam
droxicam: structure given in first source. droxicam : An organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis.		2.0510organic heterotricyclic compound;
pyridines		cyclooxygenase 1 inhibitor;
hepatotoxic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor;
prodrug
rutecarpine
rutacarpine: from Evodia rutaecarpa; an ingredient in zhuyu hewei zhitong capsules		2.0510beta-carbolines
etofibrate
etofibrate: analog of clofibrate with nicotinic acid substituted on the 2-carbon of the ethyl ester group; structure; RN given refers to parent cpd		2.0510monocarboxylic acid
pazufloxacin
[no description available]		2.0810quinolines
repaglinide
[no description available]		2.0810piperidines
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		2.0810benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
trihexyphenidyl hydrochloride
[no description available]		2.0510aralkylamine
thioridazine hydrochloride
[no description available]		2.0510hydrochloridefirst generation antipsychotic;
geroprotector
siquil
[no description available]		2.0510hydrochlorideanticoronaviral agent
trimethylsilanol
[no description available]		2.0110
oxymetazoline hydrochloride
oxymetazoline hydrochloride : A hydrochloride salt resulting from the reaction of equimolar quantities of oxymetazoline and hydrogen chloride. A direct-acting sympathomimetic with marked alpha-adrenergic activity, it is a vasoconstrictor that is used to relieve nasal congestion.		2.0510hydrochloridealpha-adrenergic agonist;
nasal decongestant;
sympathomimetic agent;
vasoconstrictor agent
dexfenfluramine
Dexfenfluramine: The S-isomer of FENFLURAMINE. It is a serotonin agonist and is used as an anorectic. Unlike fenfluramine, it does not possess any catecholamine agonist activity.. (S)-fenfluramine : The S-enantiomer of fenfluramine. It stimulates the release of serotonin and selectively inhibits its reuptake, but unlike fenfluramine it does not possess catecholamine agonist activity. It was formerly given by mouth as the hydrochloride in the treatment of obesity, but, like fenfluramine, was withdrawn wolrdwide following reports of valvular heart defects.		2.0510fenfluramineappetite depressant;
serotonergic agonist;
serotonin uptake inhibitor
alprenolol hydrochloride
[no description available]		2.0510hydrochloride
2-methoxyestradiol
2-methoxy-17beta-estradiol : A 17beta-hydroxy steroid, being 17beta-estradiol methoxylated at C-2.		2.051017beta-hydroxy steroid;
3-hydroxy steroid		angiogenesis modulating agent;
antimitotic;
antineoplastic agent;
human metabolite;
metabolite;
mouse metabolite
synthalin a
synthalin A: RN given refers to parent cpd; structure. synthalin : A hydrochloride resulting from the reaction of decamethylenediguanidine with 2 mol eq. of hydrogen chloride.. synthalin A : A member of the class of guanidines that is decane having guanidino groups at the 1- and 10-positions.		2.0510guanidineshepatotoxic agent;
hypoglycemic agent;
nephrotoxin
fluphenazine hydrochloride
[no description available]		2.0510phenothiazinesanticoronaviral agent
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		2.47201,2,3-triazole
tryptamine monohydrochloride
[no description available]		2.0510
apaflurane
[no description available]		6.82107
clomipramine hydrochloride
clomipramine hydrochloride : A hydrochloride resulting from the reaction of equimolar amounts of clomipramine and hydrogen chloride. One of the more sedating tricyclic antidepressants, it is used for the treatment of depression as well as obsessive-compulsive disorder and phobias.		2.0510hydrochlorideanticoronaviral agent;
antidepressant;
serotonergic antagonist;
serotonergic drug
amiloride hydrochloride
amiloride hydrochloride dihydrate : A hydrate that is the dihydrate of amiloride hydrochloride.		2.0510hydratediuretic;
sodium channel blocker
prazosin hydrochloride
[no description available]		2.0510hydrochloride
mianserin hydrochloride
mianserin hydrochloride : The hydrochloride salt of mianserin, a tetracyclic compound with antidepressant effects.		2.0510hydrochloridegeroprotector
miconazole nitrate
miconazole nitrate : A racemate composed of equimolar amounts of (R)- and (S)-miconazole nitrate. An antifungal used for the treatment of athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.		2.0810
ibopamine
ibopamine: structure given in UD 31;67a & in 2nd source		2.0510benzoate ester;
phenols
fluorodeoxyglucose f18
Fluorodeoxyglucose F18: The compound is given by intravenous injection to do POSITRON-EMISSION TOMOGRAPHY for the assessment of cerebral and myocardial glucose metabolism in various physiological or pathological states including stroke and myocardial ischemia. It is also employed for the detection of malignant tumors including those of the brain, liver, and thyroid gland. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1162)		4.8112-deoxy-2-((18)F)fluoro-D-glucose;
2-deoxy-2-fluoro-aldehydo-D-glucose
lomefloxacin hydrochloride
lomefloxacin hydrochloride : The hydrochloride salt of lomefloxacin. It is administered by mouth to treat bacterial infections including bronchitis and urinary tract infections. It is also used topically as eye drops for the treatment of bacterial conjunctivitis, and as ear drops for the treatment of otitis externa and otitis media.		2.0510hydrochlorideantimicrobial agent;
antitubercular agent;
photosensitizing agent
fenspiride hydrochloride
[no description available]		2.0510
nilverm
[no description available]		2.0510organic molecular entity
sanguinarine chloride
[no description available]		2.0510
ropinirole hydrochloride
[no description available]		2.0510indoles
zoledronic acid
Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position.		2.47201,1-bis(phosphonic acid);
imidazoles		bone density conservation agent
pirlindole
pirlindole: RN given refers to parent cpd; synonym pyrazidol refers to mono-HCl; structure in Negwer, 5th ed, #2812		2.0510carbazoles
artemisinin
(+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.0810organic peroxide;
sesquiterpene lactone		antimalarial;
plant metabolite
brinzolamide
brinzolamide: an antiglaucoma agent		2.0810sulfonamide;
thienothiazine		antiglaucoma drug;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
drospirenone
drospirenone: a progestational compound with antimineralocorticoid and antiandrogenic activity; structure given in first source		2.08103-oxo-Delta(4) steroid;
steroid lactone		aldosterone antagonist;
contraceptive drug;
progestin
artemether
Artemether: An artemisinin derivative that is used in the treatment of MALARIA.. artemether : An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.4720artemisinin derivative;
cyclic acetal;
organic peroxide;
semisynthetic derivative;
sesquiterpenoid		antimalarial
dihydroergotamine mesylate
dihydroergotamine mesylate : The methanesulfonic acid salt of dihydroergotamine, a semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine. Both the mesylate and the tartrate salts are used for the treatment of migraine and orthostatic hypotension.		2.0510methanesulfonate saltnon-narcotic analgesic;
serotonergic agonist;
vasoconstrictor agent
cromakalim
Cromakalim: A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also been tried in patients with asthma. (Martindale, The Extra Pharmacopoeia, 30th ed, p352)		2.3820
6-amino-1-hydroxyhexane-1,1-diphosphonate
6-amino-1-hydroxyhexane-1,1-diphosphonate: used for therapy of Paget's disease of bone & malignant hypercalcaemia		2.05101,1-bis(phosphonic acid)
ranolazine hydrochloride
[no description available]		2.0510
uk 68798
[no description available]		2.0810aromatic ether;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
potassium channel blocker
hp 873
iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia.		2.08101,2-benzoxazoles;
aromatic ether;
aromatic ketone;
methyl ketone;
monoamine;
organofluorine compound;
piperidines;
tertiary amino compound		dopaminergic antagonist;
second generation antipsychotic;
serotonergic antagonist
loxapine succinate
[no description available]		2.4720succinate saltgeroprotector
guanfacine hydrochloride
[no description available]		2.0510acetamidesgeroprotector
labetalol hydrochloride
[no description available]		2.0510salicylamides
loperamide hydrochloride
loperamide hydrochloride : A hydrochloride obtained by combining loperamide with one equivalent of hydrochloric acid. Used for treatment of diarrhoea resulting from gastroenteritis or inflammatory bowel disease.		2.0510hydrochlorideanticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
maprotiline hydrochloride
[no description available]		2.0510anthracenes
opipramol hydrochloride
[no description available]		2.0510
voriconazole
Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4.		2.0810conazole antifungal drug;
difluorobenzene;
pyrimidines;
tertiary alcohol;
triazole antifungal drug		P450 inhibitor
betamipron
[no description available]		2.0810organonitrogen compound;
organooxygen compound
rexigen
clobenzorex: RN given refers to (+)-isomer; structure		2.0510
uroxatral
[no description available]		2.0810hydrochloride
aceclofenac
[no description available]		2.4720amino acid;
carboxylic ester;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
clociguanil
clociguanil: RN given refers to parent cpd; structure		2.0510
tebuquine
[no description available]		2.0510
thiocolchicoside
[no description available]		2.0810glycoside
chelerythrine chloride
[no description available]		2.0510
tosyllysine chloromethyl ketone
[no description available]		2.0510
doripenem
Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS.		2.0810carbapenems
5-(n-methyl-n-isobutyl)amiloride
5-(N-methyl-N-isobutyl)amiloride: inhibitor of the Na+-H+ antiporter		2.0510
1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride
1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride : A hydrochloride salt prepared from anileridine and two molar equivalents of hydrogen chloride.		2.0510hydrochlorideEC 2.7.11.13 (protein kinase C) inhibitor
amperozide hydrochloride
amperozide hydrochloride : The hydrochloride salt of amperozide.		2.0510hydrochlorideanxiolytic drug;
dopamine uptake inhibitor;
geroprotector;
second generation antipsychotic;
serotonergic antagonist
pyrrolidine dithiocarbamic acid
[no description available]		2.0510
oxazolidin-2-one
Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.		2.0110carbamate ester;
oxazolidinone		metabolite
atovaquone
Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.		2.0510hydroxy-1,2-naphthoquinone
p-Aminobenzamidine dihydrochloride
[no description available]		2.0510organic molecular entity
rosiglitazone
[no description available]		2.4620aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
tamiflu
[no description available]		2.0810phosphate salt
cryptolepine
cryptolepine: fused indole-quinoline; structure in first source; from CRYPTOLEPIS sanguinolenta. cryptolepine : An organic heterotetracyclic compound that is 5H-indolo[3,2-b]quinoline in which the hydrogen at position N-5 is replaced by a methyl group.		2.0510indole alkaloid;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound		anti-inflammatory agent;
antimalarial;
antineoplastic agent;
cysteine protease inhibitor;
plant metabolite
bexarotene
[no description available]		2.0810benzoic acids;
naphthalenes;
retinoid		antineoplastic agent
s20098
[no description available]		2.0810acetamides
flunisolide
flunisolide: flunisolide HFA is a formulation of flunisolide using hydrofluoroalkane (HFA) as propellant in place of chlorofluorocarbon (CFC) ones		5.213111beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic ketal;
fluorinated steroid;
primary alpha-hydroxy ketone		anti-asthmatic drug;
anti-inflammatory drug;
immunosuppressive agent
ketorolac tromethamine
Ketorolac Tromethamine: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.. ketorolac tromethamine : An organoammonium salt resulting from the mixture of equimolar amounts of ketorolac and tromethamine (tris). It has potent non-sedating analgesic and moderate anti-inflammatory effects. It is used in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis.		2.0810organoammonium saltanalgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor
clarithromycin
Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis.		2.0810macrolide antibioticantibacterial drug;
environmental contaminant;
protein synthesis inhibitor;
xenobiotic
nicotine
(S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.		2.08103-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
carbetapentane citrate
[no description available]		2.0510carbonyl compound
cinchonine
[no description available]		2.0510(8xi)-cinchonan-9-ol;
cinchona alkaloid		metabolite
fibrinogen
Fibrinogen: Plasma glycoprotein clotted by thrombin, composed of a dimer of three non-identical pairs of polypeptide chains (alpha, beta, gamma) held together by disulfide bonds. Fibrinogen clotting is a sol-gel change involving complex molecular arrangements: whereas fibrinogen is cleaved by thrombin to form polypeptides A and B, the proteolytic action of other enzymes yields different fibrinogen degradation products.. D-iditol : The D-enantiomer of iditol.		4.811iditolfungal metabolite
phentolamine mesylate
[no description available]		2.0510
mephentermine
sphinganine : A 2-aminooctadecane-1,3-diol having (2S,3R)-configuration.		2.05102-aminooctadecane-1,3-diolEC 2.7.11.13 (protein kinase C) inhibitor;
human metabolite;
mouse metabolite
oxybutynin hydrochloride
[no description available]		2.0510hydrochloride
gliquidone
gliquidone: structure; RN given refers to parent cpd		2.0810isoquinolines
8-((4-chlorophenyl)thio)cyclic-3',5'-amp
8-((4-chlorophenyl)thio)cyclic-3',5'-AMP: lowers cAMP in heart & fat cells; cAMP-dependent kinase inhibitor. 8-(4-chlorophenylthio)-cAMP : A 3',5'-cyclic purine nucleotide that is 3',5'-cyclic AMP in which the hydrogen at position 2 on the purine fragment is replaced by a 4-chlorophenylthio group.		2.03103',5'-cyclic purine nucleotide;
adenyl ribonucleotide;
aryl sulfide;
organochlorine compound		protein kinase agonist
prilocaine hydrochloride
prilocaine hydrochloride : The monohydrochloride salt of prilocaine.		2.0510hydrochloridelocal anaesthetic
n-hexadecyl-n,n-dimethyl-3-ammonio-1-propanesulfonate
[no description available]		2.0510
lopinavir
[no description available]		2.0810amphetamines;
dicarboxylic acid diamide		anticoronaviral agent;
antiviral drug;
HIV protease inhibitor
brexanolone
brexanolone: a mixture of allopregnanolone and sulfobutylether‐beta‐cyclodextrin for treatment of postpartum depression. brexanolone : A 3-hydroxy-5alpha-pregnan-20-one in which the hydroxy group at position 3 has alpha-configuration. It is a metabolite of the sex hormone progesterone and used for the treatment of postpartum depression in women.		2.05103-hydroxy-5alpha-pregnan-20-oneantidepressant;
GABA modulator;
human metabolite;
intravenous anaesthetic;
sedative
desethylchloroquine
desethylchloroquine: metabolite of chloroquine		2.0510aminoquinoline
6-(4-nitrobenzylthio)guanosine
6-(4-nitrobenzylthio)guanosine: inhibitor of nucleoside transport		2.0510
zpck
ZPCK: alkylates histidine residue at active center of bovine chymotrypsin		2.0510
wr 159412
[no description available]		2.0510
moxifloxacin hydrochloride
moxifloxacin hydrochloride : A hydrochloride comprising equimolar amounts of moxifloxacin and hydrogen chloride.		2.0810hydrochlorideantibacterial drug
cinchonidine
cinchonidine: has antimalarial activity; diastereoisomer of cinchonine with distinct physiochemical properties; RN given refers to parent cpd(8alpha,9R)-isomer. cinchonidine : 8-epi-Cinchonan in which a hydrogen at position 9 is substituted by hydroxy (R configuration). A diasteroisomer of cinchonine, it occurs in the bark of most varieties of Cinchona shrubs, and is frequently used for directing chirality in asymmetric synthesis.		2.0510(8xi)-cinchonan-9-ol;
cinchona alkaloid		metabolite
tetrahydrodeoxycorticosterone
tetrahydrodeoxycorticosterone: RN given refers to (3alpha,5beta)-isomer		2.051021-hydroxy steroid
benzyloxyamine
benzyloxyamine: RN given refers to parent cpd		2.0510
fulvestrant
Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.		2.081017beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide		antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist
mizoribine
[no description available]		2.0810imidazolesanticoronaviral agent
sr141716
[no description available]		2.0810amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist
bosentan anhydrous
Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS.		2.0810primary alcohol;
pyrimidines;
sulfonamide		antihypertensive agent;
endothelin receptor antagonist
cp-55,940
[no description available]		2.0510
vanoxerine
vanoxerine dihydrochloride : A hydrochloride salt that is obtained by reaction of vanoxerine with two equivalents of hydrogen chloride. Potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration.		2.0510hydrochloridedopamine uptake inhibitor
1-(2-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenylethyl)-1h-imidazole
1-(2-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenylethyl)-1H-imidazole: inhibits platelet aggregation & Ca2+ entry into platelets. SKF-96365 free base : An ether that is 2-(1H-imidazol-1-yl)-1-(4-methoxyphenyl)ethanol in which the hydrogen of the hydroxy group has been substituted by a 3-(4-methoxyphenyl)propyl group.		2.0510ether;
imidazoles;
monomethoxybenzene		TRP channel blocker
methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate
methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate: structure given in first source		2.0510beta-carbolines
u 69593
U 69593: selective ligand for opioid K-receptor. U69593 : A monocarboxylic acid amide obtained by formal condensation between the carboxy group of phenylacetic acid and the secodary amino group of (5R,7S,8S)-N-methyl-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-amine.		2.0510monocarboxylic acid amide;
N-alkylpyrrolidine;
organic heterobicyclic compound;
oxaspiro compound		anti-inflammatory agent;
diuretic;
kappa-opioid receptor agonist
u 78517f
U 78517F: iron-catalyzed lipid peroxidation inhibitor; structure given in first source; RN given is for diHCl		2.0510
cv 3988
CV 3988: platelet activating factor antagonist; structure given in first source		2.0510
beta-carboline-3-carboxylic acid methyl ester
beta-carboline-3-carboxylic acid methyl ester: structure given in first source		2.0510beta-carbolines
racecadotril
racecadotril: parenterally active enkephalinase inhibitor		2.0810N-acyl-amino acid
methoctramine
methoctramine: structure given in first source. methoctramine : A tetramine that is N,N'-bis(6-aminohexyl)octane-1,8-diamine where the primary amino groups both carry 2-methoxybenzyl substituents.. methoctramine tetrahydrochloride : A hydrochloride obtained by combining methoctramine with four molar equivalents of hydrochloric acid.		2.0510hydrochloridemuscarinic antagonist
pyronaridine
[no description available]		2.0510aminoquinoline
1-hydroxymethylmidazolam
1-hydroxymethylmidazolam: metabolite of midazolam. 1-hydroxymidazolam : An imidazobenzodiazepine that is midazolam in which one of the hydrogens of the methyl group is substituted by a hydroxy group. It is the major metabolite of the anesthetic, midazolam.		1.9910aromatic primary alcohol;
imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		drug metabolite;
human blood serum metabolite;
human urinary metabolite
betaxolol hydrochloride
betaxolol hydrochloride : The hydrochloride salt of betaxolol.		2.0510hydrochlorideantihypertensive agent;
beta-adrenergic antagonist
1-(2-methoxyphenyl)-4-(4-(2-phthalimido)butyl)piperazine
NAN 190 hydrobromide : A hydrobromide obtained by reaction of NAN 190 with one equivalent of hydrobromic acid.		2.0510hydrobromideserotonergic antagonist
parthenolide
[no description available]		2.0510germacranolide
1-hexadecyl-2-acetyl-glycero-3-phosphocholine
Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.. 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine : A 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.		5.44822-acetyl-1-alkyl-sn-glycero-3-phosphocholineantihypertensive agent;
beta-adrenergic antagonist;
bronchoconstrictor agent;
hematologic agent;
vasodilator agent
deoxyglucose
Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.		2.0710
tadalafil
[no description available]		3.3920benzodioxoles;
pyrazinopyridoindole		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
3',4'-dichlorobenzamil
3',4'-dichlorobenzamil: inhibits Na-Ca exchange in membrane vesicle & papillary muscle preparations from guinea pig heart		2.0510guanidines;
pyrazines
homoorientin
homoorientin: isolated from Swertia japonica; structure given in first source		4.811flavone C-glycoside;
tetrahydroxyflavone		antineoplastic agent;
radical scavenger
tafenoquine
tafenoquine : A racemate comprising equimolar amounts of (R)- and (S)-tafenoquine.. N(4)-{2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl}pentane-1,4-diamine : An aminoquinoline that is 8-aminoquinoline which is substituted by methoxy groups at positions 2 and 6, a methyl group at position 4, and a m-(trifluoromethyl)phenoxy group at position 5, and in which the amino substituent at position 8 is itself substituted by a 5-aminopentan-2-yl group.		2.0510(trifluoromethyl)benzenes;
aminoquinoline;
aromatic ether;
primary amino compound;
secondary amino compound
plavix
[no description available]		2.0810azaheterocycle sulfate salt;
organoammonium sulfate salt		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
clofarabine
[no description available]		2.0810adenosines;
organofluorine compound		antimetabolite;
antineoplastic agent
gr 113808
GR 113808: structure given in first source; a 5-HT(4) receptor antagonist: GR 125487 is the HCl salt. GR 113808 : An indolyl carboxylate ester obtained by formal condensation between the carboxy group of 1-methylindole-3-carboxylic acid with the hydroxy group of N-{2-[4-(hydroxymethyl)piperidin-1-yl]ethyl}methanesulfonamide.		2.0510indolyl carboxylate ester;
piperidines;
sulfonamide		serotonergic antagonist
gallopamil hydrochloride
[no description available]		2.0510
buthionine sulfoximine
L-buthionine-(S,R)-sulfoximine : A 2-amino-4-(S-butylsulfonimidoyl)butanoic acid which has S-configuration. It is a inhibitor of gamma-glutamylcysteine synthetase and glutathione (GSH) biosynthesis and is capable of enhancing the apoptotic effects of several chemotherapeutic agents.		2.05102-amino-4-(S-butylsulfonimidoyl)butanoic acidEC 6.3.2.2 (glutamate--cysteine ligase) inhibitor;
ferroptosis inducer
pramipexole
Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively.		2.0810benzothiazoles;
diamine		antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
radical scavenger
valdecoxib
[no description available]		2.0810isoxazoles;
sulfonamide		antipyretic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
sb 204070a
SB 204070A: structure given in first source; a selective 5-HT(4) receptor antagonist		2.0510
1-(2-(4-aminophenyl)ethyl)-4-(3-trifluoromethylphenyl)piperazine
LY 165163: structure given in first source; a serotonin agonist. LY-165163 : A N-arylpiperazine that is piperazine substituted by 2-(4-aminophenyl)ethyl and 3-(trifluoromethyl)phenyl groups at positions 1 and 4, respectively. It is a selective 5-HT1A serotonin receptor agonist and 5-HT1D serotonin receptor antagonist.		2.0510(trifluoromethyl)benzenes;
N-alkylpiperazine;
N-arylpiperazine;
primary arylamine;
substituted aniline		geroprotector;
serotonergic agonist
desethylamodiaquine
desethylamodiaquine: metabolite of amodiaquine		2.0510
san 58035
[no description available]		2.0510
n,n-dideethylchloroquine
[no description available]		2.0510
mk 0663
[no description available]		2.0810bipyridines;
organochlorine compound;
sulfone		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
gefitinib
[no description available]		2.0810aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
mk 912
[no description available]		2.0510
3-iodopindolol
3-iodopindolol: RN given refers to 125I-labeled cpd(-)-isomer; structure given in first source		210
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide: a highly-selective, nonpeptide delta opioid receptor agonist; structure given in first source		2.0510diarylmethane
sk&f 86466
benalfocin: RN & RR given from first source; RN not in Chemline 9/28/83; structure given in first source		2.0510benzazepine
e 64
E 64: cysteine protease inhibitor of microbial origin, which inhibits cathepsin B (EC 3.4.22.1) and cathepsin L (EC 3.4.22.-)		2.0510dicarboxylic acid monoamide;
epoxy monocarboxylic acid;
guanidines;
L-leucine derivative;
zwitterion		antimalarial;
antiparasitic agent;
protease inhibitor
desloratadine
desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.		2.5220benzocycloheptapyridineanti-allergic agent;
cholinergic antagonist;
drug metabolite;
H1-receptor antagonist
w 7
[no description available]		2.0510
pre 084
2-(4-morpholino)ethyl-1-phenylcyclohexane-1-carboxylate: structure given in first source		2.0510morpholines
methotrexate
[no description available]		3.8230dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
3,6-diamino-9-(4-(methylsulfonyl)aminophenyl)aminoacridine
[no description available]		2.0510
1-(2-allylphenoxy)-3-((8-bromoacetylamino-4-menthane-1-yl)amino)-1-propanol
1-(2-allylphenoxy)-3-((8-bromoacetylamino-4-menthane-1-yl)amino)-1-propanol: irreversibly inactivates the dihydroalprenolol binding site; alprenolol analog; isopropylamino group of alprenolol replaced by 8-bromoacetylamino-1-amino-p-menthane moiety in the 1 position; structure given in first source		2.0510
sr 2640
SR 2640: leukotriene D4 and E4 antagonist		2.0510quinolines
ne 58051
NE 58051: inhibits tumor cell adhesion to extracellular matrices; structure in first source		2.0510
sulbactam
[no description available]		2.0810penicillanic acids
olmesartan medoxomil
Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION.		2.0810biphenyls
n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide
N,N-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide: binds with high affinity to glial mitochondrial diazepam binding inhibitor receptors & increases mitochondrial steroidogenesis		2.0510phenylindole
4-(benzodioxan-5-yl)-1-(indan-2-yl)piperazine
[no description available]		2.0510
abiraterone
[no description available]		2.08103beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
pyridines		antineoplastic agent;
EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor
8-cyclopentyl-3-(3-((4-(fluorosulfonyl)benzoyl)oxy)propyl)-1-propylxanthine
8-cyclopentyl-3-(3-((4-(fluorosulfonyl)benzoyl)oxy)propyl)-1-propylxanthine: structure given in first source		2.0510
l 741626
3-(4-(4-chlorophenyl-4-hydroxypiperidino)methyl)indole: structure in first source		2.0510piperidines
wr 242511
WR 242511: RN given refers to parent cpd		2.0510
febuxostat
Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout.		2.08101,3-thiazolemonocarboxylic acid;
aromatic ether;
nitrile		EC 1.17.3.2 (xanthine oxidase) inhibitor
nisoxetine hydrochloride
[no description available]		2.0510
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(+-)-isomer
[no description available]		2.0510
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		2.1310amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
lexapro
Lexapro: Trade name of escitalopram, the active S-enantiomer of the racemic citalopram.		2.0810
docetaxel anhydrous
Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.		2.0810secondary alpha-hydroxy ketone;
tetracyclic diterpenoid		antimalarial;
antineoplastic agent;
photosensitizing agent
nsc-141549
[no description available]		2.0510
levofloxacin
Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.		2.08109-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
ezetimibe
Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).		2.0810azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
cox 189
lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity.		2.0810amino acid;
monocarboxylic acid;
organochlorine compound;
organofluorine compound;
secondary amino compound		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
cilomilast
[no description available]		4.0540methoxybenzenes
idazoxan hydrochloride
[no description available]		2.0510
cyanopindolol
[no description available]		210indoles
xamoterol
Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist.		2.5720morpholines
ro 363
[no description available]		1.9810
naproxen
Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.		2.4720methoxynaphthalene;
monocarboxylic acid		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
atazanavir sulfate
Atazanavir Sulfate: An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS.		2.0310organic sulfate salt
telbivudine
[no description available]		2.0810pyrimidine 2'-deoxyribonucleosideantiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
cyc 202
seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.		2.46202,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
urapidil monohydrochloride
[no description available]		2.0510
aminopterin
Aminopterin: A folic acid derivative used as a rodenticide that has been shown to be teratogenic.		2.0510dicarboxylic acidEC 1.5.1.3 (dihydrofolate reductase) inhibitor;
mutagen
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		4.811amino acid zwitterion;
angiotensin II		human metabolite
abt 980
[no description available]		2.0510
sk&f 75670
SK&F 75670: RN refers to HBr; N-methyl derivative of SK&F 38393		2.0510
atropine
tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.		2.4720
sb 203580
[no description available]		2.0110imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
nbi 27914
[no description available]		2.0510dialkylarylamine;
tertiary amino compound
sb 216763
[no description available]		2.0510indoles;
maleimides
organophosphonates
hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.		4.811divalent inorganic anion;
phosphite ion
dizocilpine
[no description available]		2.0510secondary amino compound;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
memantine hydrochloride
[no description available]		2.0510hydrochlorideantidepressant;
antiparkinson drug;
dopaminergic agent;
neuroprotective agent;
NMDA receptor antagonist
pongidae
[no description available]		2.0510
deflazacort
deflazacort: structure		2.0510corticosteroid hormone
sb 205384
SB 205384: structure in first source		2.0510thienopyridine
hydrastine
[no description available]		2.0510isoquinolinesmetabolite
olpadronic acid
[no description available]		2.0510
ramelteon
ramelteon: melatonin MT1/MT2 receptor agonist		2.0810indanes
deferasirox
Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions.		2.0810benzoic acids;
monocarboxylic acid;
phenols;
triazoles		iron chelator
bms204352
BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source		2.0810
tbc-11251
sitaxsentan: endothelin A receptor antagonist; structure in first source		2.0810benzodioxoles
tolvaptan
[no description available]		2.4620benzazepine;
benzenedicarboxamide		aquaretic;
vasopressin receptor antagonist
lenalidomide
[no description available]		5.0421aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
lacosamide
Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES.		2.0810N-acyl-amino acid
vincaleukoblastine
[no description available]		2.0810acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite
vincristine sulfate
[no description available]		2.4720organic sulfate saltantineoplastic agent;
geroprotector
estramustine
Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid.		2.051017beta-hydroxy steroid;
carbamate ester;
organochlorine compound		alkylating agent;
antineoplastic agent;
radiation protective agent
lupeol
[no description available]		2.0510pentacyclic triterpenoid;
secondary alcohol		anti-inflammatory drug;
plant metabolite
nsc 95397
[no description available]		2.05101,4-naphthoquinones
wortmannin
[no description available]		2.4720acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent
nsc 352122
trimetrexate glucuronate: an orphan drug and AIDS drug; used for treatment of Pneumocytis carinii pneumonia in patients with AIDS		1.9810
bortezomib
[no description available]		5.0421amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
neocryptolepine
neocryptolepine: isolated from the roots of the African plant Cryptolepis sanguinolenta; structure in first source		2.0510
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		2.97401,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
1-hydroxypentane-1,1-bisphosphonate
[no description available]		2.0510
cimadronate
cimadronate: increases serum 1,25-dihydroxyvitamin D in rats via stimulating renal 1-hydroxylase activity; structure given in first source		2.0510
1,1-hydroxyoctanodiphosphonate
[no description available]		2.0510
glycogen
glycogen : A polydisperse, highly branched glucan composed of chains of D-glucopyranose residues in alpha(1->4) glycosidic linkage, joined together by alpha(1->6) glycosidic linkages. A small number of alpha(1->3) glycosidic linkages and some cumulative alpha(1->6) links also may occur. The branches in glycogen typically contain 8 to 12 glucose residues.		2.1310
n-acetylneuraminic acid
N-Acetylneuraminic Acid: An N-acyl derivative of neuraminic acid. N-acetylneuraminic acid occurs in many polysaccharides, glycoproteins, and glycolipids in animals and bacteria. (From Dorland, 28th ed, p1518). N-acetylneuraminic acid : An N-acylneuraminic acid where the N-acyl group is specified as acetyl.		1.9810N-acetylneuraminic acidsantioxidant;
bacterial metabolite;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
human metabolite;
mouse metabolite
bradykinin
[no description available]		2.0110oligopeptidehuman blood serum metabolite;
vasodilator agent
glucosamine
D-glucosamine : An amino sugar whose structure comprises D-glucose having an amino substituent at position 2.. 2-amino-2-deoxy-D-glucopyranose : A D-glucosamine whose structure comprises D-glucopyranose having an amino substituent at position 2.		2.0210D-glucosamineEscherichia coli metabolite;
geroprotector;
mouse metabolite
oxytocin
Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.		2.0510heterodetic cyclic peptide;
peptide hormone		oxytocic;
vasodilator agent
inositol 1,4,5-trisphosphate
Inositol 1,4,5-Trisphosphate: Intracellular messenger formed by the action of phospholipase C on phosphatidylinositol 4,5-bisphosphate, which is one of the phospholipids that make up the cell membrane. Inositol 1,4,5-trisphosphate is released into the cytoplasm where it releases calcium ions from internal stores within the cell's endoplasmic reticulum. These calcium ions stimulate the activity of B kinase or calmodulin.		1.9810myo-inositol trisphosphatemouse metabolite
ouabain
Ouabain: A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE.. cardiac glycoside : Steroid lactones containing sugar residues that act on the contractile force of the cardiac muscles.. ouabain : A steroid hormone that is a multi-hydroxylated alpha-L-rhamnosyl cardenoloide. It binds to and inhibits the plasma membrane Na(+)/K(+)-ATPase (sodium pump). It has been isolated naturally from Strophanthus gratus.		2.462011alpha-hydroxy steroid;
14beta-hydroxy steroid;
5beta-hydroxy steroid;
alpha-L-rhamnoside;
cardenolide glycoside;
steroid hormone		anti-arrhythmia drug;
cardiotonic drug;
EC 2.3.3.1 [citrate (Si)-synthase] inhibitor;
EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
ion transport inhibitor;
plant metabolite
pentostatin
Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia.		2.0810coformycinsantimetabolite;
antineoplastic agent;
Aspergillus metabolite;
bacterial metabolite;
EC 3.5.4.4 (adenosine deaminase) inhibitor
cortodoxone
Cortodoxone: 17,21-Dihydroxypregn-4-ene-3,20-dione. A 17-hydroxycorticosteroid with glucocorticoid and anti-inflammatory activities.. 11-deoxycortisol : A deoxycortisol that is cortisol in which the hydroxy group at position 11 has been replaced by a hydrogen.		2.0510deoxycortisol;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		human metabolite;
mouse metabolite
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		2.7230cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
meropenem
Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.		2.0810alpha,beta-unsaturated monocarboxylic acid;
carbapenemcarboxylic acid;
organic sulfide;
pyrrolidinecarboxamide		antibacterial agent;
antibacterial drug;
drug allergen
digitoxin
Digitoxin: A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665). digitoxin : A cardenolide glycoside in which the 3beta-hydroxy group of digitoxigenin carries a 2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl trisaccharide chain.		2.4720cardenolide glycosideEC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor
saquinavir
Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.		2.0810L-asparagine derivative;
quinolines		antiviral drug;
HIV protease inhibitor
perindopril erbumine
[no description available]		2.0810addition compoundantihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
miglitol
[no description available]		2.0810piperidines
amiodarone hydrochloride
[no description available]		2.0510aromatic ketone
mometasone furoate
Mometasone Furoate: A pregnadienediol derivative ANTI-ALLERGIC AGENT and ANTI-INFLAMMATORY AGENT that is used in the management of ASTHMA and ALLERGIC RHINITIS. It is also used as a topical treatment for skin disorders.		10.695111beta-hydroxy steroid;
2-furoate ester;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
organochlorine compound;
steroid ester		anti-allergic agent;
anti-inflammatory drug
dicyclomine hydrochloride
dicyclomine hydrochloride : The hydrochloride salt of dicyclomine. An anticholinergic, it is used to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome.		2.0510hydrochlorideantispasmodic drug;
muscarinic antagonist
rocuronium bromide
rocuronium bromide : The organic bromide salt of a 5alpha androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents.		2.0810organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent
nortriptyline hydrochloride
[no description available]		2.0510organic tricyclic compoundgeroprotector
linezolid
[no description available]		2.0810acetamides;
morpholines;
organofluorine compound;
oxazolidinone		antibacterial drug;
protein synthesis inhibitor
canaline
canaline: structure		2.0510amino acid zwitterion;
non-proteinogenic L-alpha-amino acid		antimetabolite;
antineoplastic agent;
phytogenic insecticide;
plant metabolite
n-formylmethionine leucyl-phenylalanine
N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.. N-formyl-L-methionyl-L-leucyl-L-phenylalanine : A tripeptide composed of L-Met, L-Leu and L-Phe in a linear sequence with a formyl group at the amino terminus. It acts as a potent inducer of leucocyte chemotaxis and macrophage activator as well as a ligand for the FPR receptor.		2.4120tripeptide
hydroxylamine hydrochloride
[no description available]		2.0510organic molecular entity
sb 228357
SB 228357: a neuroleptic with equivalent or higher antagonist affinity for 5-HT2 than for dopamine D2 receptor		2.0510indolyl carboxylic acid
actinonin
actinonin: natural hydroxamic acid, pseudopeptide antibiotic isolated from Streptomyces species; structure		2.0510
pemirolast potassium salt
[no description available]		2.0810
eplerenone
Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION.		2.08103-oxo-Delta(4) steroid;
epoxy steroid;
gamma-lactone;
methyl ester;
organic heteropentacyclic compound;
oxaspiro compound;
steroid acid ester		aldosterone antagonist;
antihypertensive agent
vinpocetine
vinpocetine: whole issue of Arzneim Forsch (23 articles) discuss this drug; Arzneim Forsch 26(10a);1976; RN given refers to parent cpd with unspecified isomeric designation		2.0510alkaloidgeroprotector
ao 128
AO 128: alpha-glucosidase inhibitor; structure given in first source		2.0810organic molecular entity
loteprednol etabonate
Loteprednol Etabonate: An androstadiene derivative corticosteroid that is used as an ANTI-ALLERGIC AGENT for the treatment of inflammatory and allergic eye conditions.		2.081011beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
etabonate ester;
organochlorine compound;
steroid acid ester;
steroid ester		anti-inflammatory drug
dihydroergocristine monomesylate
dihydroergocristine mesylate : The methanesulfonic acid salt of dihydroergocristine. It has been used as the for the symptomatic treatment of mental deterioration associated with cerebrovascular insufficiency and in peripheral vascular disease. It is also a component of ergoloid mesylate (codergocrine mesilate), a mixture of ergot alkaloid derivatives that is used as a vasodilator and has shown mild benefits in the treatment of vascular dementia.		2.0510methanesulfonate saltalpha-adrenergic antagonist;
geroprotector;
vasodilator agent
fluticasone propionate
fluticasone propionate : 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 propionyl substituent at position 17; has anti-inflammatory, anti-asthmatic and anti-allergic activity.		2.081011beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
corticosteroid;
fluorinated steroid;
propanoate ester;
steroid ester;
thioester		adrenergic agent;
anti-allergic agent;
anti-asthmatic drug;
anti-inflammatory drug;
bronchodilator agent;
dermatologic drug
tretinoin
Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.		2.4720retinoic acid;
vitamin A		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
arachidonic acid
icosa-5,8,11,14-tetraenoic acid : Any icosatetraenoic acid with the double bonds at positions 5, 8, 11 and 14.. arachidonate : A long-chain fatty acid anion resulting from the removal of a proton from the carboxy group of arachidonic acid.		2.9310icosa-5,8,11,14-tetraenoic acid;
long-chain fatty acid;
omega-6 fatty acid		Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
human metabolite;
mouse metabolite
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		2.0510resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
oleic acid
Oleic Acid: An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed). oleic acid : An octadec-9-enoic acid in which the double bond at C-9 has Z (cis) stereochemistry.		3.3711octadec-9-enoic acidantioxidant;
Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
Escherichia coli metabolite;
mouse metabolite;
plant metabolite;
solvent
tacrolimus
Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.		2.4920macrolide lactambacterial metabolite;
immunosuppressive agent
thapsigargin
Thapsigargin: A sesquiterpene lactone found in roots of THAPSIA. It inhibits SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES.. thapsigargin : An organic heterotricyclic compound that is a hexa-oxygenated 6,7-guaianolide isolated fron the roots of Thapsia garganica L., Apiaceae. A potent skin irritant, it is used in traditional medicine as a counter-irritant. Thapsigargin inhibits Ca(2+)-transporting ATPase mediated uptake of calcium ions into sarcoplasmic reticulum and is used in experimentation examining the impacts of increasing cytosolic calcium concentrations.		2.0510butyrate ester;
organic heterotricyclic compound;
sesquiterpene lactone		calcium channel blocker;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
mupirocin
Mupirocin: A topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing.. mupirocin : An alpha,beta-unsaturated ester resulting from the formal condensation of the alcoholic hydroxy group of 9-hydroxynonanoic acid with the carboxy group of (2E)-4-[(2S)-tetrahydro-2H-pyran-2-yl]-3-methylbut-2-enoic acid in which the tetrahydropyranyl ring is substituted at positions 3 and 4 by hydroxy groups and at position 5 by a {(2S,3S)-3-[(2S,3S)-3-hydroxybutan-2-yl]oxiran-2-yl}methyl group. Originally isolated from the Gram-negative bacterium Pseudomonas fluorescens, it is used as a topical antibiotic for the treatment of Gram-positive bacterial infections.		2.0810alpha,beta-unsaturated carboxylic ester;
epoxide;
monocarboxylic acid;
oxanes;
secondary alcohol;
triol		antibacterial drug;
bacterial metabolite;
protein synthesis inhibitor
clindamycin
Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.		2.0510
5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol
5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol: estrogen receptor ligand; structure in first source. (R,R)-5,11-diethyl-5,6,11,12-tetrahydro-2,8-chrysenediol : A carbotetracyclic compound that is 5,6,11,12-tetrahydrochrysene substituted by hydroxy groups at positions 2 and 8 and by ethyl groups at positions 5 and 11 (the 5R,11R-stereoisomer). It is an agonist of ER-alpha and antagonist of ER-beta receptors.		2.0510carbotetracyclic compound;
polyphenol		estrogen receptor agonist;
estrogen receptor antagonist;
geroprotector;
neuroprotective agent
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		5.0731macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
prostaglandin d2
Prostaglandin D2: The principal cyclooxygenase metabolite of arachidonic acid. It is released upon activation of mast cells and is also synthesized by alveolar macrophages. Among its many biological actions, the most important are its bronchoconstrictor, platelet-activating-factor-inhibitory, and cytotoxic effects.. prostaglandin D2 : A member of the class of prostaglandins D that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9 and 15 and an oxo group at position 11 (the 5Z,9alpha,13E,15S- stereoisomer).		4.4851prostaglandins Dhuman metabolite;
mouse metabolite
6-bromoindirubin-3'-oxime
6-bromoindirubin-3'-oxime: structure in first source. 6-bromoindirubin-3'-oxime : A member of the class of biindoles that is indirubin substituted at position 6 by a bromo group and in which the keto group at position 3' has undergone condensation with hydroxylamine to form the corresponding oxime.		2.0510
roflumilast
[no description available]		9.48113aromatic ether;
benzamides;
chloropyridine;
cyclopropanes;
organofluorine compound		anti-asthmatic drug;
phosphodiesterase IV inhibitor
h 89
N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source. N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor.. (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration.		2.0510N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
decitabine
[no description available]		2.08102'-deoxyribonucleoside
teniposide
[no description available]		2.0810aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
valrubicin
[no description available]		2.0810anthracycline;
trifluoroacetamide
purvalanol a
6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer;		2.0510purvalanol
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		2.7530L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
posaconazole
[no description available]		2.0810aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles		trypanocidal drug
rubitecan
rubitecan: RN refers to (+-)-isomer; anti-HIV agent; DNA Topoisomerases, Type I inhibitor. rubitecan : A pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin.		2.0810C-nitro compound;
delta-lactone;
pyranoindolizinoquinoline;
semisynthetic derivative;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
Tetrahydropiperine
[no description available]		2.0510benzodioxoles
carbenoxolone
[no description available]		2.0510
piperine
piperine : A N-acylpiperidine that is piperidine substituted by a (1E,3E)-1-(1,3-benzodioxol-5-yl)-5-oxopenta-1,3-dien-5-yl group at the nitrogen atom. It is an alkaloid isolated from the plant Piper nigrum.		2.0510benzodioxoles;
N-acylpiperidine;
piperidine alkaloid;
tertiary carboxamide		food component;
human blood serum metabolite;
NF-kappaB inhibitor;
plant metabolite
isoliquiritigenin
[no description available]		2.0510chalconesantineoplastic agent;
biological pigment;
EC 1.14.18.1 (tyrosinase) inhibitor;
GABA modulator;
geroprotector;
metabolite;
NMDA receptor antagonist
ilepcimide
ilepcimide: structure given in first source; RN given refers to compound with no isomeric designation		2.0510benzodioxoles
buprenorphine
Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.. buprenorphine : A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain.		3.1210morphinane alkaloiddelta-opioid receptor antagonist;
kappa-opioid receptor antagonist;
mu-opioid receptor agonist;
opioid analgesic
arginine vasopressin
Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6.		2.0810vasopressincardiovascular drug;
hematologic agent;
mitogen
gw9662
2-chloro-5-nitrobenzanilide: pretreatment of peroxisome proliferator activated receptors with GW9662 results in the irreversible loss of ligand binding		2.0510benzamides
calmidazolium
calmidazolium chloride : The organic choride salt of calmidazolium.		2.0510organic chloride saltapoptosis inducer;
calmodulin antagonist
trilostane
trilostane: inhibits conversion of pregnenolone to progesterone; adrenal blocking agent used in treatment of Cushing's syndrome. trilostane : An epoxy steroid that is 3,17beta-dihydroxy-5alpha-androst-2-ene-2-carbonitrile in which the oxygen of the epoxy group is joined to the 4alpha and 5 alpha positions.		2.081017beta-hydroxy steroid;
3-hydroxy steroid;
androstanoid;
epoxy steroid;
nitrile		abortifacient;
antineoplastic agent;
EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor
tropisetron hydrochloride
[no description available]		2.0510
quinidine sulfate
[no description available]		2.0510
leuprolide acetate
leuprolide acetate : An acetate salt obtained by combining the nonapeptide leuprolide with acetic acid. A long lasting GnRH analog, LH-Rh agonist. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.		2.0810acetate saltantineoplastic agent;
gonadotropin releasing hormone agonist
leuprolide
Leuprolide: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.. leuprolide : An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.		2.0510oligopeptideanti-estrogen;
antineoplastic agent;
gonadotropin releasing hormone agonist
octotropine methylbromide
octotropine methylbromide: minor descriptor (65-86); on line & INDEX MEDICUS search TROPANES (69-86); RN given refers to endo-isomer. anisotropine methylbromide : A quaternary ammonium salt resulting from the reaction of the amino group of anisotropine with methyl bromide.		2.0510
propylthiouracil
Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group.		2.0810pyrimidinethioneantidote to paracetamol poisoning;
antimetabolite;
antioxidant;
antithyroid drug;
carcinogenic agent;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
hormone antagonist
ipratropium bromide anhydrous
[no description available]		2.0510
r 59949
R 59949: diacylglycerol kinase inhibitor		2.0510diarylmethane
n(6)-cyclopentyladenosine
[no description available]		2.0510
mercaptopurine
Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis.		2.0810aryl thiol;
purines;
thiocarbonyl compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent
sb 366791
N-(3-methoxyphenyl)-4-chlorocinnamanilide: a TRPV1 antagonist; structure in first source		2.0510
ag-213
tyrphostin 47: inhibits protein-tyrosine kinase activity of EGF-R both in vitro and in living cells;		2.0510
3,3',4,5'-tetrahydroxystilbene
3,3',4,5'-tetrahydroxystilbene: demethyl derivative of isorhapontigenin; structure in first source; a Syk kinase inhibitor; found in heartwood of FABACEAE; inhibitor of photosynthesis in spinach chloroplasts; may be inhibitor of plant growth; RN given refers to (E)-isomer. piceatannol : A stilbenol that is trans-stilbene in which one of the phenyl groups is substituted by hydroxy groups at positions 3 and 4, while the other phenyl group is substituted by hydroxy groups at positions 3 and 5.		2.0510catechols;
polyphenol;
resorcinols;
stilbenol		antineoplastic agent;
apoptosis inducer;
geroprotector;
hypoglycemic agent;
plant metabolite;
protein kinase inhibitor;
tyrosine kinase inhibitor
bemesetron
[no description available]		2.0510
levosulpiride
(S)-(-)-sulpiride : An optically active form of sulpiride having (S)-configuration. The active enantiomer of the racemic drug sulpiride. Selective D2-like dopamine antagonist (Ki values are ~ 0.015. ~ 0.013, 1, ~ 45 and ~ 77 muM at D2, D3, D4, D1 and D5 receptors respectively).		2.0810sulpirideantidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
4-fluorophenyl-L-alanine
4-fluorophenyl-L-alanine : A L-phenylalanine derivative that is L-phenylalanine in which the hydrogen at position 4 on the benzene ring is replaced by a fluoro group.		2.05104-fluorophenylalanine;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid
phenylthiazolylthiourea
Phenylthiazolylthiourea: A dopamine-beta-hydroxylase inhibitor.		2.0510
(2'-(4-aminophenyl)-(2,5'-bi-1h-benzimidazol)-5-amine)
[no description available]		2.0510benzimidazoles
cotinine
Cotinine: The N-glucuronide conjugate of cotinine is a major urinary metabolite of NICOTINE. It thus serves as a biomarker of exposure to tobacco SMOKING. It has CNS stimulating properties.. (-)-cotinine : An N-alkylpyrrolidine that consists of N-methylpyrrolidinone bearing a pyridin-3-yl substituent at position C-5 (the 5S-enantiomer). It is an alkaloid commonly found in Nicotiana tabacum.		4.7621N-alkylpyrrolidine;
pyridines;
pyrrolidin-2-ones;
pyrrolidine alkaloid		antidepressant;
biomarker;
human xenobiotic metabolite;
plant metabolite
flunarizine
Flunarizine: Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.		2.0510diarylmethane
eszopiclone
Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use.		2.0810zopiclonecentral nervous system depressant;
sedative
thiohydantoins
Thiohydantoins: Sulfur analogs of hydantoins with one or both carbonyl groups replaced by thiocarbonyl groups.		4.811
methimazole
Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen.		2.08101,3-dihydroimidazole-2-thionesantithyroid drug
cinnarizine
Cinnarizine: A piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.		2.4720diarylmethane;
N-alkylpiperazine;
olefinic compound		anti-allergic agent;
antiemetic;
calcium channel blocker;
geroprotector;
H1-receptor antagonist;
histamine antagonist;
muscarinic antagonist
sulindac
Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.		2.4720monocarboxylic acid;
organofluorine compound;
sulfoxide		analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent
epalrestat
epalrestat : A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy.		2.0810monocarboxylic acid;
thiazolidines		EC 1.1.1.21 (aldehyde reductase) inhibitor
drotaverin
drotaverin: Hungarian drug; RN given refers to parent cpd; structure		2.0810isoquinolines
chlorogenic acid
caffeoylquinic acid: Antiviral Agent; structure in first source. chlorogenate : A monocarboxylic acid anion that is the conjugate base of chlorogenic acid; major species at pH 7.3.		4.811cinnamate ester;
tannin		food component;
plant metabolite
tg 003
TG 003: a Clk inhibitor; structure in first source		2.0510
(1R,2S)-tranylcypromine hydrochloride
(1R,2S)-tranylcypromine hydrochloride : A hydrochloride obtained by combining (1R,2S)-tranylcypromine with one equivalent of hydrochloric acid.		2.0510hydrochloride
tacrine hydrochloride
[no description available]		2.0510
thiourea
Thiourea: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.. thiourea : The simplest member of the thiourea class, consisting of urea with the oxygen atom substituted by sulfur.		4.811one-carbon compound;
thioureas;
ureas		antioxidant;
chromophore
4-bromotetramisole, oxalate (1:1), salt(s)-isomer
[no description available]		2.0510
digoxin
Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.		2.0510cardenolide glycoside;
steroid saponin		anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope
3-hydroxybenzylhydrazine hydrochloride
[no description available]		2.0510
1-(3-chlorophenyl)biguanide hydrochloride
[no description available]		2.0510
capsazepine
capsazepine: modified capsaicin molecule; a capsaicin receptor antagonist. capsazepine : A benzazepine that is 2,3,4,5-tetrahydro-1H-2-benzazepine which is substituted by hydroxy groups at positions 7 and 8 and on the nitrogen atom by a 2-(p-chlorophenyl)ethylaminothiocarbonyl group. A synthetic analogue of capsaicin, it was the first reported capsaicin receptor antagonist.		2.0510benzazepine;
catechols;
monochlorobenzenes;
thioureas		capsaicin receptor antagonist
diphenyleneiodium chloride
dibenziodolium chloride : An organic chloride salt having dibenziodolium as the counterion.		2.0510organic chloride saltEC 1.6.3.1. [NAD(P)H oxidase (H2O2-forming)] inhibitor;
G-protein-coupled receptor agonist
tamoxifen citrate
[no description available]		2.0510citrate saltangiogenesis inhibitor;
anticoronaviral agent
tamoxifen
[no description available]		2.0810stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
ethionamide
Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide.		2.0510pyridines;
thiocarboxamide		antilipemic drug;
antitubercular agent;
fatty acid synthesis inhibitor;
leprostatic drug;
prodrug
eskazine
[no description available]		2.0510
3-(n,n-dimethylsulfonamido)-4-methyl-nitrobenzene
BRL-50481 : A C-nitro compound that is benzene substituted by N,N-dimethylaminosulfonyl, methyl and nitro groups at positions 1, 2 and 5, respectively. It is a phosphodiesterase inhibitor selective for the PDE7 subtype (Ki = 180 nM).		2.0510C-nitro compound;
sulfonamide;
toluenes		bone density conservation agent;
EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor;
geroprotector
fusidic acid
Fusidic Acid: An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.. fusidic acid : A steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum.		2.081011alpha-hydroxy steroid;
3alpha-hydroxy steroid;
alpha,beta-unsaturated monocarboxylic acid;
steroid acid;
steroid antibiotic;
sterol ester		EC 2.7.1.33 (pantothenate kinase) inhibitor;
Escherichia coli metabolite;
protein synthesis inhibitor
artemotil
artemotil: structure given in first source; RN given refers to cpd without isomeric designation		2.0510artemisinin derivative
valinomycin
Valinomycin: A cyclododecadepsipeptide ionophore antibiotic produced by Streptomyces fulvissimus and related to the enniatins. It is composed of 3 moles each of L-valine, D-alpha-hydroxyisovaleric acid, D-valine, and L-lactic acid linked alternately to form a 36-membered ring. (From Merck Index, 11th ed) Valinomycin is a potassium selective ionophore and is commonly used as a tool in biochemical studies.. valinomycin : A twelve-membered cyclodepsipeptide composed of three repeating D-alpha-hydroxyisovaleryl-D-valyl-L-lactoyl-L-valyl units joined in sequence. An antibiotic found in several Streptomyces strains.		2.0810cyclodepsipeptide;
macrocycle		antimicrobial agent;
antiviral agent;
bacterial metabolite;
potassium ionophore
hmr 3647
[no description available]		2.0810
latoconazole
latoconazole: RN refers to cpd without isomeric designation; latoconazole is (E)-isomer; structure given in first source		2.0810conazole antifungal drug;
imidazole antifungal drug
maraviroc
[no description available]		2.0810tropane alkaloid
toremifene citrate
[no description available]		2.0810stilbenoidanticoronaviral agent
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.0510aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
nelarabine
nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G).		2.0810beta-D-arabinoside;
monosaccharide derivative;
purine nucleoside		antineoplastic agent;
DNA synthesis inhibitor;
prodrug
4-diphenylacetoxy-n-methylpiperidine methiodide
4-DAMP methiodide : A quaternary ammonium salt obtained by combining equimolar amounts of 4-diphenylacetoxy-N-methylpiperidine and iodomethane.		2.0510iodide salt;
quaternary ammonium salt		cholinergic antagonist;
muscarinic antagonist
nitrogen dioxide
Nitrogen Dioxide: Nitrogen oxide (NO2). A highly poisonous gas. Exposure produces inflammation of lungs that may only cause slight pain or pass unnoticed, but resulting edema several days later may cause death. (From Merck, 11th ed) It is a major atmospheric pollutant that is able to absorb UV light that does not reach the earth's surface.		3.4311nitrogen oxide
gestodene
Gestodene: synthetic steroid with progestational activity; RN given refers to (17alpha)-isomer		2.4720steroidestrogen
glucametacin
glucametacin: indomethacin analog; structure		2.0510
orlistat
Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug.		2.0810beta-lactone;
carboxylic ester;
formamides;
L-leucine derivative		anti-obesity agent;
bacterial metabolite;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor
quinine
[no description available]		2.7530cinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide
2-chloro-N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide: structure given in first source		2.0510
bp 897
BP 897: a dopamine D3 receptor agonist; structure in first source		2.0510naphthalenecarboxamide
azilect
[no description available]		2.0810
trequinsin hydrochloride
[no description available]		2.0510
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		2.08101,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
benzatropine methanesulfonate
benzatropine mesylate : The methanesulfonate salt of benzatropine. An acetylcholine receptor antagonist, it is used in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments.		2.0510
n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea
N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a 5-HT(2B) receptor antagonist; structure given in first source. 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea : A member of ther class of ureas that is urea in which a hydrogen attached to one of the nitrogens has been replaced by an N-methylindol-5-yl group, while a hydrogen attached to the other nitrogen has been replaced by a 3-methyl-1,2-thiazol-5-yl group. It is a potent and selective antagonist for the 5-hydroxytryptamine 2B (5-HT2B) receptor.		2.05101,2-thiazoles;
indoles;
ureas		receptor modulator;
serotonergic antagonist
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		3.76100
gw 7647
GW 7647: a PPAR-alpha agonist; structure in first source. GW 7647 : A monocarboxylic acid that is 2-(phenylsulfanyl)isobutyric acid in which the phenyl group is substituted at the para- position by a 3-aza-7-cyclohexylhept-1-yl group in which the nitrogen is acylated by a (cyclohexylamino)carbonyl group.		2.0510aryl sulfide;
monocarboxylic acid;
ureas		PPARalpha agonist
ro 41-0960
[no description available]		2.0510
n-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide
N-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide: dopamine D4 ligand; structure in first source		2.0510
l 663536
MK-886: orally active leukotriene biosynthesis inhibitor. 3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid : A member of the class of indoles that is 1H-indole substituted by a isopropyl group at position 5, a tert-butylsulfanediyl group at position 3, a 4-chlorobenzyl group at position 1 and a 2-carboxy-2-methylpropyl group at position 2. It acts as an inhibitor of arachidonate 5-lipoxygenase.		2.0510aryl sulfide;
indoles;
monocarboxylic acid;
monochlorobenzenes		antineoplastic agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
leukotriene antagonist
brl 15572
3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol : An N-alkylpiperazine that is 1-(3-chlorophenyl)piperazine carrying a 3,3-diphenyl-2-hydroxyprop-1-yl group at position 4. A selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.		2.0510monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
secondary alcohol		geroprotector;
serotonergic antagonist
mrs 1523
2,3-diethyl-4,5-dipropyl-6-phenylpyridine-3-thiocarboxylate-5-carboxylate: adenosine A3 receptor antagonist		2.0510
fg 9041
FG 9041: structure given in first source		2.0510quinoxaline derivative
sb 415286
3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione: a glycogen synthase kinase-3 inhibitor; structure in first source		2.0510C-nitro compound;
maleimides;
monochlorobenzenes;
phenols;
secondary amino compound;
substituted aniline		antioxidant;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent
dm 235
DM 235: structure in first source		2.0510
jhw 015
[no description available]		2.0510indolecarboxamide
bw 723c86
[no description available]		2.0510tryptamines
sc 560
SC560 : A member of the class of pyrazoles that is 1H-pyrazole which is substituted at positions 1, 3 and 5 by 4-methoxyphenyl, trifluoromethyl and 4-chlorophenyl groups, respectively. Unlike many members of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors, SC-560 is selective for COX-1.		2.0510aromatic ether;
monochlorobenzenes;
organofluorine compound;
pyrazoles		angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 1 inhibitor;
non-steroidal anti-inflammatory drug
le 300
[no description available]		2.0510indoles
sitagliptin
sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.		2.0810triazolopyrazine;
trifluorobenzene		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
environmental contaminant;
hypoglycemic agent;
serine proteinase inhibitor;
xenobiotic
ly 367265
LY 367265: a 5-hydroxytryptamine transporter inhibitor; a 5-HT(2A) receptor antagonist; structure in first source. LY-367,265 : A fluoroindole that is 1H-indole in which the hydrogens at positions 3 and 6 are replaced by 1-[2-(2,2-dioxo-5,6-dihydro-4H-2lambda(6)-[1,2,5]thiadiazolo[4,3,2-ij]quinolin-1(2H)-yl)ethyl]-1,2,3,6-tetrahydropyridin-4-yl and fluoro groups, respectively. It is an inhibitor of the 5-hydroxytryptamine transporter (Ki = 2.3 nM) and an antagonist of 5-hydroxytryptamine(2A) receptor (Ki = 0.81 nM).		2.0510dihydropyridine;
fluoroindole;
tertiary amino compound;
thiadiazoloquinoline		antidepressant;
geroprotector;
serotonergic antagonist;
serotonin uptake inhibitor
tolcapone
Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase.		2.08102-nitrophenols;
benzophenones;
catechols		antiparkinson drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
alsterpaullone
alsterpaullone: structure in first source. alsterpaullone : An organic heterotetracyclic compound that is 1,3-dihydro-2H-1-benzazepin-2-one which shares its 4-5 bond with the 3-2 bond of 5-nitro-1H-indole.		2.0510C-nitro compound;
caprolactams;
organic heterotetracyclic compound		anti-HIV-1 agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor
cgp 7930
2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)phenol: structure in first source		2.0510alkylbenzene
1,3,5-tris(4-hydroxyphenyl)-4-propyl-1h-pyrazole
4,4',4''-(4-propylpyrazole-1,3,5-triyl)trisphenol : A pyrazole that is 1H-pyrazole bearing three 4-hydroxyphenyl substituents at positions 1, 3 and 5 as well as a propyl substituent at position 4. Potent, subtype-selective estrogen receptor agonist (EC50 ~ 200 pM); displays 410-fold selectivity for ERalpha over ERbeta. Prevents ovariectomy-induced weight gain and loss of bone mineral density, and induces gene expression in the hypothalamus following systemic administration in vivo.		2.0510phenols;
pyrazoles		estrogen receptor agonist
sib 1757
SIB 1757: a selective mGluR5 antagonist; structure in first source		2.0510
quercetin
[no description available]		2.08107-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		3.8110prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
dinoprost
Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.		2.3820monocarboxylic acid;
prostaglandins Falpha		human metabolite;
mouse metabolite
apigenin
Chamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.		2.0510trihydroxyflavoneantineoplastic agent;
metabolite
luteolin
[no description available]		4.8113'-hydroxyflavonoid;
tetrahydroxyflavone		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
c-Jun N-terminal kinase inhibitor;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
immunomodulator;
nephroprotective agent;
plant metabolite;
radical scavenger;
vascular endothelial growth factor receptor antagonist
calcitriol
dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes		2.0810D3 vitamins;
hydroxycalciol;
triol		antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical
leukotriene b4
Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene B4 : A leukotriene composed of (6Z,8E,10E,14Z)-icosatetraenoic acid having (5S)- and (12R)-hydroxy substituents. It is a lipid mediator of inflammation that is generated from arachidonic acid via the 5-lipoxygenase pathway.		4.7671dihydroxy monocarboxylic acid;
hydroxy polyunsaturated fatty acid;
leukotriene;
long-chain fatty acid		human metabolite;
mouse metabolite;
plant metabolite;
vasoconstrictor agent
leukotriene c4
Leukotriene C4: The conjugation product of LEUKOTRIENE A4 and glutathione. It is the major arachidonic acid metabolite in macrophages and human mast cells as well as in antigen-sensitized lung tissue. It stimulates mucus secretion in the lung, and produces contractions of nonvascular and some VASCULAR SMOOTH MUSCLE. (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene C4 : A leukotriene that is (5S,7E,9E,11Z,14Z)-5-hydroxyicosa-7,9,11,14-tetraenoic acid in which a glutathionyl group is attached at position 6 via a sulfide linkage.		3.6130leukotrienebronchoconstrictor agent;
human metabolite;
mouse metabolite
thromboxane a2
Thromboxane A2: An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).. thromboxane A2 : A thromboxane which is produced by activated platelets and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation.		1.9810epoxy monocarboxylic acid;
thromboxanes A		mouse metabolite
daphnetin
[no description available]		2.0510hydroxycoumarin
alprostadil
[no description available]		2.4720prostaglandins Eanticoagulant;
human metabolite;
platelet aggregation inhibitor;
vasodilator agent
vitamin d 2
Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa.		2.0810hydroxy seco-steroid;
seco-ergostane;
vitamin D		bone density conservation agent;
nutraceutical;
plant metabolite;
rodenticide
leukotriene e4
Leukotriene E4: A biologically active principle of SRS-A that is formed from LEUKOTRIENE D4 via a peptidase reaction that removes the glycine residue. The biological actions of LTE4 are similar to LTC4 and LTD4. (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene E4 : A leukotriene that is (7E,9E,11Z,14Z)-icosa-7,9,11,14-tetraenoic acid substituted by a hydroxy group at position 5 (5S) and an L-cystein-S-yl group at position 6 (6R).		6.3243amino dicarboxylic acid;
L-cysteine thioether;
leukotriene;
non-proteinogenic L-alpha-amino acid;
secondary alcohol
gamma-linolenic acid
gamma-Linolenic Acid: An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed). gamma-linolenic acid : A C18, omega-6 acid fatty acid comprising a linolenic acid having cis- double bonds at positions 6, 9 and 12.		1.9710linolenic acid;
omega-6 fatty acid		human metabolite;
mouse metabolite;
plant metabolite
genistein
[no description available]		1.99107-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
amphotericin b
Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.		2.0510antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic		antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
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.		16.61053111beta-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
oxymetholone
Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects.		2.0810
eprosartan
eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.		2.0810dicarboxylic acid;
imidazoles;
thiophenes		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
montelukast
montelukast: a leukotriene D4 receptor antagonist		15.818240aliphatic sulfide;
monocarboxylic acid;
quinolines		anti-arrhythmia drug;
anti-asthmatic drug;
leukotriene antagonist
timolol maleate
(S)-timolol maleate : The maleic acid salt of the active (S)-enantiomer of timolol, comprising equimolar amounts of (S)-timolol and maleic acid.		2.0510maleate saltanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
brompheniramine maleate
brompheniramine maleate : The maleic acid salt of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.4720maleate saltanti-allergic agent
chlorpheniramine maleate
[no description available]		2.0510organic molecular entity
clemastine fumarate
clemastine fumarate : The fumaric acid salt of clemastine. An antihistamine with antimuscarinic and moderate sedative properties, it is used for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.		2.0510fumarate saltanti-allergic agent;
antipruritic drug;
H1-receptor antagonist;
muscarinic antagonist
dexchlorpheniramine maleate
[no description available]		2.0810organic molecular entity
methylergonovine maleate
[no description available]		2.0510ergoline alkaloidgeroprotector
carboprost
Carboprost: A nonsteroidal abortifacient agent that is effective in both the first and second trimesters of PREGNANCY.. carboprost : Prostaglandin F2alpha in which the hydrogen at position 15 is substituted by methyl (S configuration). It is used as an abortifacient agent that is effective in both the first and second trimesters of pregnancy.		1.9710hydroxy monocarboxylic acidabortifacient;
oxytocic
mycophenolate mofetil
mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases.		2.0810carboxylic ester;
ether;
gamma-lactone;
phenols;
tertiary amino compound		anticoronaviral agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
immunosuppressive agent;
prodrug
entacapone
entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group.		2.08102-nitrophenols;
catechols;
monocarboxylic acid amide;
nitrile		antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
astaxanthine
astaxanthine: a keto form of carotene; pigment in flesh of Scottish salmon (Salmo salar) crustacoa-lobster (Homarus gammarus, flamingo feathers; structure; a carotenoid without vitamin A activity, has shown anti-oxidant and anti-inflammatory activities. astaxanthin : A carotenone that consists of beta,beta-carotene-4,4'-dione bearing two hydroxy substituents at positions 3 and 3' (the 3S,3'S diastereomer). A carotenoid pigment found mainly in animals (crustaceans, echinoderms) but also occurring in plants. It can occur free (as a red pigment), as an ester, or as a blue, brown or green chromoprotein.		2.0510carotenol;
carotenone		animal metabolite;
anticoagulant;
antioxidant;
food colouring;
plant metabolite
harman
harman: a beta-carboline; RN given refers to parent cpd; structure. harman : An indole alkaloid fundamental parent with a structure of 9H-beta-carboline carrying a methyl substituent at C-1. It has been isolated from the bark of Sickingia rubra, Symplocus racemosa, Passiflora incarnata, Peganum harmala, Banisteriopsis caapi and Tribulus terrestris, as well as from tobacco smoke. It is a specific, reversible inhibitor of monoamine oxidase A.		2.0510harmala alkaloid;
indole alkaloid fundamental parent;
indole alkaloid		anti-HIV agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
plant metabolite
usambarensine
usambarensine: structure given in first source		2.0510harmala alkaloid
humulene
humulene: structure given in first source. (1E,4E,8E)-alpha-humulene : The (1E,4E,8E)-isomer of alpha-humulene.		4.811alpha-humulene
chrysin
chrysin : A dihydroxyflavone in which the two hydroxy groups are located at positions 5 and 7.		2.31107-hydroxyflavonol;
dihydroxyflavone		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
EC 2.7.11.18 (myosin-light-chain kinase) inhibitor;
hepatoprotective agent;
plant metabolite
myricetin
[no description available]		2.05107-hydroxyflavonol;
hexahydroxyflavone		antineoplastic agent;
antioxidant;
cyclooxygenase 1 inhibitor;
food component;
geroprotector;
hypoglycemic agent;
plant metabolite
cynarine
cynarine: active principle of the artichoke; functions primarily as a cholagogue and choleretic and also as antilipemic agent		2.0510alkyl caffeate ester;
quinic acid		plant metabolite
caffeic acid phenethyl ester
phenethyl caffeate : An alkyl caffeate ester in which 2-phenylethyl is the alkyl component.		2.0510alkyl caffeate esteranti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
antioxidant;
antiviral agent;
immunomodulator;
metabolite;
neuroprotective agent
rottlerin
rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1);. rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis.		2.0510aromatic ketone;
benzenetriol;
chromenol;
enone;
methyl ketone		anti-allergic agent;
antihypertensive agent;
antineoplastic agent;
apoptosis inducer;
K-ATP channel agonist;
metabolite
l 660,711
[no description available]		2.0810quinolines
l 683590
immunomycin: from Streptomyces hygroscopicus; structure given in first source		2.110ether;
lactol;
macrolide;
secondary alcohol		antifungal agent;
bacterial metabolite;
immunosuppressive agent
n-oleoyldopamine
N-oleoyldopamine: putative capsaicin receptor ligand; produces hyperalgesia; isolated from the brain. N-oleoyldopamine : A fatty amide resulting from the formal condensation of the carboxy group of oleic acid with the amino group of dopamine. Synthesised in catecholaminergic neurons, it crosses the blood-brain barrier and might be considered as a carrier of dopamine into the brain. It is a transient receptor potential vanilloid type 1 (TRPV1) receptor agonist.		2.0510catechols;
fatty amide;
N-(fatty acyl)-dopamine;
secondary carboxamide		TRPV1 agonist
pheniramine maleate
Naphcon A: tradename; contains above compounds; ophthalmic solution		2.0510organic molecular entity
travoprost
Travoprost: A cloprostenol derivative that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.. travoprost : The isopropyl ester of prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophthalmic solutions of travoprost are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. It is a pro-drug; the isopropyl ester group is hydrolysed by esterases in the cornea to the biologically active free acid, fluprostenol.		2.0810(trifluoromethyl)benzenes;
isopropyl ester;
prostaglandins Falpha		antiglaucoma drug;
antihypertensive agent;
ophthalmology drug;
prodrug;
prostaglandin receptor agonist
tranilast
tranilast: antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis. tranilast : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.		2.4720amidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide		anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent
trimipramine maleate
[no description available]		2.0510maleate saltantidepressant
imipenem
[no description available]		2.0810carbapenems
etretinate
retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof.		2.0810enoate ester;
ethyl ester;
retinoid		keratolytic drug
isotretinoin
Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases.		2.4720retinoic acidantineoplastic agent;
keratolytic drug;
teratogenic agent
xylometazoline hydrochloride
[no description available]		2.0510
flunarizine hydrochloride
[no description available]		2.0510diarylmethane
ketotifen fumarate
ketotifen fumarate : An organoammonium salt consisting of equimolar amounts of ketotifen(1+) and fumarate(1-) ions. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is a non-bronchodilator anti-asthmatic drug.		2.4720organoammonium saltanti-asthmatic drug;
H1-receptor antagonist
dinoprost tromethamine
[no description available]		2.0810organic molecular entity
triprolidine
Triprolidine: Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.. triprolidine : An N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders.		2.0510N-alkylpyrrolidine;
olefinic compound;
pyridines		H1-receptor antagonist
rosuvastatin calcium
S 4522: structure in first source		2.0810N-acyl-15-methylhexadecasphinganine-1-phosphoethanolamine;
organic calcium salt		anti-inflammatory agent;
cardioprotective agent;
CETP inhibitor
terbinafine hydrochloride
terbinafine hydrochloride : A hydrochloride obtained by reaction of terbinafine with one molar equivalent of hydrogen chloride.		2.0810allylamine antifungal drug;
hydrochloride		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
P450 inhibitor
cis-flupenthixol dihydrochloride
cis-flupenthixol dihydrochloride : The dihydrochloride salt of cis-flupenthixol.		2.0510hydrochloridegeroprotector
thromboxane b2
Thromboxane B2: A stable, physiologically active compound formed in vivo from the prostaglandin endoperoxides. It is important in the platelet-release reaction (release of ADP and serotonin).. thromboxane B2 : A member of the class of thromboxanes B that is (5Z,13E)-thromboxa-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15.		3.7821thromboxanes Bhuman metabolite;
mouse metabolite
n-arachidonylglycine
N-arachidonylglycine: structure in first source. N-arachidonoylglycine : Biologically active derivative of anandamide		2.0510fatty amide;
N-acylglycine
n-oleoylethanolamine
N-oleoylethanolamine: ceramidase inhibitor. oleoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of oleic acid. The monounsaturated analogue of the endocannabinoid anandamide.		2.0510endocannabinoid;
N-(long-chain-acyl)ethanolamine;
N-acylethanolamine 18:1		EC 3.5.1.23 (ceramidase) inhibitor;
geroprotector;
PPARalpha agonist
codeine
[no description available]		2.0510morphinane alkaloid;
organic heteropentacyclic compound		antitussive;
drug allergen;
environmental contaminant;
opioid analgesic;
opioid receptor agonist;
prodrug;
xenobiotic
cyclosporine
ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF		2.4720homodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
phenoxybenzamine hydrochloride
[no description available]		2.0510organic molecular entity
natamycin
[no description available]		2.0810antibiotic antifungal drug;
dicarboxylic acid monoester;
epoxide;
macrolide antibiotic;
monosaccharide derivative;
polyene antibiotic		antifungal agrochemical;
antimicrobial food preservative;
apoptosis inducer;
bacterial metabolite;
ophthalmology drug
mepyramine maleate
histosol: proprietary mixture of synthetic aromatic hydrocarbons forming an extremely nonpolar organic solvent		2.0510
acitretin
Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9.		2.0810acitretin;
alpha,beta-unsaturated monocarboxylic acid;
retinoid		keratolytic drug
dihydrocodeine
dihydrocodeine: RN refers to parent cpd(5alpha,6alpha)-isomer		2.0510morphinane alkaloid
granisetron
Granisetron: A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.. granisetron : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 1-methyl-1H-indazole-3-carboxylic acid with the primary amino group of (3-endo)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine. A selective 5-HT3 receptor antagonist, it is used (generally as the monohydrochloride salt) to manage nausea and vomiting caused by cancer chemotherapy and radiotherapy, and to prevent and treat postoperative nausea and vomiting.		1.9810aromatic amide;
indazoles
levetiracetam
Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine.		2.0810pyrrolidin-2-onesanticonvulsant;
environmental contaminant;
xenobiotic
ly 163892
loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria.		2.0510carbacephem;
zwitterion		antibacterial drug;
antimicrobial agent
nalmefene
nalmefene: RN given refers to 5-alpha isomer		2.0810morphinane alkaloid
naloxone
Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		2.4720morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
topiramate
Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine.		2.0810cyclic ketal;
ketohexose derivative;
sulfamate ester		anticonvulsant;
sodium channel blocker
brefeldin a
[no description available]		2.0510macrolide antibioticPenicillium metabolite
fenretinide
Fenretinide: A synthetic retinoid that is used orally as a chemopreventive against prostate cancer and in women at risk of developing contralateral breast cancer. It is also effective as an antineoplastic agent.. 4-hydroxyphenyl retinamide : A retinoid obtained by formal condensation of the carboxy group of all-trans retinoic acid and the anilino group of 4-hydroxyaniline. Synthetic retinoid agonist. Antiproliferative, antioxidant and anticancer agent with a long half-life in vivo. Apoptotic effects appear to be mediated by a mechanism distinct from that of 'classical' retinoids.		2.0510monocarboxylic acid amide;
retinoid		antineoplastic agent;
antioxidant
morphine
Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.		3.5420morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
demycarosylturimycin h
[no description available]		2.0810
su 9516
[no description available]		2.0510
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid: RN refers to (E)-isomer; structure given in first source. arotinoid acid : A retinoid that consists of benzoic acid substituted at position 4 by a 2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl group. It is a synthetic retinoid that acts as a selective agonist for the retinoic acid receptors (RAR).		2.0510benzoic acids;
naphthalenes;
retinoid		antineoplastic agent;
retinoic acid receptor agonist;
teratogenic agent
acipimox
acipimox: lipolysis inhibitor		2.0810pyrazinecarboxylic acid
atosiban
[no description available]		2.0810oligopeptide
bimatoprost
Bimatoprost: A cloprostenol-derived amide that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.		2.0810monocarboxylic acid amideantiglaucoma drug;
antihypertensive agent
denopamine
denopamine: structure given in first source		1.9910dimethoxybenzene
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.		24.5860727411beta-hydroxy steroid;
17alpha-hydroxy steroid;
3-oxo-Delta(4) steroid;
corticosteroid;
fluorinated steroid;
thioester		anti-allergic agent;
anti-asthmatic drug
l 655,708
[no description available]		2.0510
15-deoxy-delta(12,14)-prostaglandin j2
15-deoxy-delta(12,14)-prostaglandin J2: 15-deoxy-PGJ2 is also available; check for double bonds (indicated by delta) at 12 and 14 positions. 15-deoxy-Delta(12,14)-prostaglandin J2 : A prostaglandin J derivative comprising prostaglandin J2 lacking the 15-hydroxy group and having C=C double bonds at the 12- and 14-positions.		2.0210prostaglandins Jelectrophilic reagent;
insulin-sensitizing drug;
metabolite
lacidipine
[no description available]		2.0510cinnamate ester;
tert-butyl ester
latanoprost
Latanoprost: A prostaglandin F analog used to treat OCULAR HYPERTENSION in patients with GLAUCOMA.. latanoprost : A prostaglandin Falpha that is the isopropyl ester prodrug of latanoprost free acid. Used in the treatment of open-angle glaucoma and ocular hypertension.		2.0810isopropyl ester;
prostaglandins Falpha;
triol		antiglaucoma drug;
antihypertensive agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
prodrug
ml 10302
2-piperidinoethyl 4-amino-5-chloro-2-methoxybenzoate: structure in first source		2.0510
nateglinide
Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus.		2.0810phenylalanine derivative
sb 200646a
[no description available]		2.0510
vinorelbine
[no description available]		2.0510acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
ring assembly;
vinca alkaloid		antineoplastic agent;
photosensitizing agent
cl 316243
disodium (R,R)-5-(2-((2-(3-chlorophenyl)-2-hydroxyethyl)-amino)propyl)-1,3-benzodioxole-2,3-dicarboxylate: structure given in first source		2.3920
su 6656
SU 6656: a c-Src kinase inhibitor; used to probe growth signaling; structure in first source. SU6656 : A member of the class of oxindoles that is 3-methyleneoxindole in which the hydrogeh at position 5 has been replaced by a dimethylaminosulfonyl group and in which one of the hydrogens of the methylene group has been replaced by a 4,5,6,7-tetrahydro-indol-2-yl group. It is a specific inhibitor of Src family kinase.		2.0510
1,2-oleoylphosphatidylcholine
1,2-oleoylphosphatidylcholine: RN given refers to (Z,Z)-isomer. dioleoyl phosphatidylcholine : A phosphatidylcholine in which the phosphatidyl acyl groups are both oleoyl.		2.3920phosphatidylcholine(1+)
licochalcone a
licochalcone A: has both anti-inflammatory and antineoplastic activities; structure given in first source; isolated from root of Glycyrrhiza inflata; RN given refers to (E)-isomer		2.0510chalcones
ag 538
AG 538: an IGF-1 receptor kinase inhibitor; structure in first source		2.0510
tyrphostin ag 555
[no description available]		2.0510
tyrphostin b44
tyrphostin B44: inhibits protein kinases; an analog of tyrphostin B46; B44(+) is B50, and is the stereoisomer of B44(-)		2.0510
ag-490
[no description available]		2.0510catechols;
enamide;
monocarboxylic acid amide;
nitrile;
secondary carboxamide		anti-inflammatory agent;
antioxidant;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector;
STAT3 inhibitor
ag 112
[no description available]		2.0510
ag 183
AG 183: structure given in first source		2.0510
semaxinib
semaxanib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is replaced by a 3,5-dimethylpyrrol-2-yl group.		2.0510olefinic compound;
oxindoles;
pyrroles		angiogenesis modulating agent;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist
stilbamidine
stilbamidine: RN given refers to parent cpd		2.0510
8-(3-chlorostyryl)caffeine
8-(3-chlorostyryl)caffeine: adenosine antagonist. 8-(3-chlorostyryl)caffeine : Caffeine substituted at its 8-position by an (E)-3-chlorostyryl group.		2.0510monochlorobenzenes;
trimethylxanthine		adenosine A2A receptor antagonist;
EC 1.4.3.4 (monoamine oxidase) inhibitor
bay 11-7085
BAY11-7085 : A sulfone that is benzene substituted by [(E)-2-cyanoethenyl]sulfonyl and tert-butyl groups at position 1 and 4, respectively. It is an irreversible inhibitor of IkappaB-alpha phosphorylation in cells (IC50 = 10 muM) and prevents the activation of NF-kappaB.		2.0510benzenes;
nitrile;
sulfone		anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
ferroptosis inducer;
NF-kappaB inhibitor
bw b70c
BW B70C: arachidonic acid antagonist. BW B70C : A hydroxamic acid that is urea in which both the hydrogens attached to one of the nitrogens are replaced by a hydroxy and a (1E)-1-[3-(4-fluorophenoxy)phenyl]but-1-en-3-yl group. A selective inhibitor of arachidonate 5-lipoxygenase, it can be used for the treatment of asthma.		2.0510aromatic ether;
hydroxamic acid;
organofluorine compound;
ureas		EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers.		2.0810dihydroxy monocarboxylic acid;
indoles;
organofluorine compound
molsidomine
[no description available]		2.0810ethyl ester;
morpholines;
oxadiazole;
zwitterion		antioxidant;
apoptosis inhibitor;
cardioprotective agent;
nitric oxide donor;
vasodilator agent
15-hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic acid
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid: A stable prostaglandin endoperoxide analog which serves as a thromboxane mimetic. Its actions include mimicking the hydro-osmotic effect of VASOPRESSIN and activation of TYPE C PHOSPHOLIPASES. (From J Pharmacol Exp Ther 1983;224(1): 108-117; Biochem J 1984;222(1):103-110)		1.9810
nomifensine maleate
[no description available]		2.0510
strontium
Strontium: An element of the alkaline earth family of metals. It has the atomic symbol Sr, atomic number 38, and atomic weight 87.62.		4.811alkaline earth metal atom
bismuth
Bismuth: A metallic element that has the atomic symbol Bi, and atomic number 83. Its principal isotope is Bismuth 209.		4.811metal atom;
pnictogen
nalbuphine hydrochloride
[no description available]		2.0510hydrochloride
butorphanol
Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain.		2.0810morphinane alkaloidantitussive;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
cefixime
[no description available]		2.0810cephalosporinantibacterial drug;
drug allergen
lisinopril
Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.		2.0810dipeptideEC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
ramipril
Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles.		2.0810azabicycloalkane;
cyclopentapyrrole;
dicarboxylic acid monoester;
dipeptide;
ethyl ester		bradykinin receptor B2 agonist;
cardioprotective agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
matrix metalloproteinase inhibitor;
prodrug
indinavir sulfate
Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.		2.0810dicarboxylic acid diamide;
N-(2-hydroxyethyl)piperazine;
piperazinecarboxamide		HIV protease inhibitor
sulfur
Sulfur: An element that is a member of the chalcogen family. It has an atomic symbol S, atomic number 16, and atomic weight [32.059; 32.076]. It is found in the amino acids cysteine and methionine.		4.811chalcogen;
nonmetal atom		macronutrient
piperic acid
piperinic acid: from Piper longum; structure in first source. (E,E)-piperic acid : A monocarboxylic acid that is (E)-penta-2,4-dienoic acid substituted by a 1,3-benzodioxol-5-yl group at position 5. It has been isolated from black pepper (Piper nigrum).		2.0510alpha,beta-unsaturated monocarboxylic acid;
benzodioxoles		plant metabolite
enalapril maleate
enalapril maleate : The maleic acid salt of enalapril. It contains one molecule of maleic acid for each molecule of enalapril. Following oral administration, the ethyl ester group of enalapril is hydrolysed to afford the corresponding carboxylic acid, enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor. Enalapril is thus a prodrug for enalaprilat (which, unlike enalapril, is not absorbed by mouth), and its maleate is used in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients.		2.0810maleate saltantihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		2.1710dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
vinblastine sulfate
[no description available]		2.0510
dextromethorphan hydrobromide
dextromethorphan hydrobromide : The hydrobromide and monohydrate of the antitussive drug dextromethorphan.		2.0510hydrate;
hydrobromide
enalaprilat anhydrous
Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate.		2.0810dicarboxylic acid;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
s-trans,trans-farnesylthiosalicylic acid
farnesylthiosalicylic acid: structure in first source		2.0510sesquiterpenoid
ici 118551
ICI 118551: RN given refers to (R*,R*)-(+-)-isomer; structure in first source; ICI 111581 is hydrochloride of ICI 118551. ICI 118551 : An indane substituted at position 7 by a methyl group and at position 4 by a 3-(isopropylamino)-2-hydroxybutoxy group (the 2R,3S-diastereomer).		3.7100aromatic ether;
indanes;
secondary alcohol;
secondary amino compound		beta-adrenergic antagonist
trandolapril
trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension.		2.0810dicarboxylic acid monoester;
dipeptide;
ethyl ester;
organic heterobicyclic compound;
secondary amino compound;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
naltrexone hydrochloride
naltrexone hydrochloride : A hydrochloride obtained by reaction of oxycodone with one molar equivalent of hydrochloric acid. it is a mu-opioid receptor antagonist that is used to treat alcohol dependence.		2.0510hydrochlorideantidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
pregabalin
Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.		2.0810gamma-amino acidanticonvulsant;
calcium channel blocker
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.		20.6716973
alvimopan anhydrous
alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain		2.0810peptide
guanabenz acetate
[no description available]		2.0510dichlorobenzenegeroprotector
nylidrin hydrochloride
[no description available]		2.0510alkylbenzene
triprolidine hydrochloride anhydrous
triprolidine hydrochloride (anh.) : A hydrochloride resulting from the formal reaction of equimolar amounts of triprolidine and hydrogen chloride. Its monohydrate is used for the symptomatic relief of uticaria, rhinitis, and various pruritic skin disorders.		2.0510hydrochlorideH1-receptor antagonist
famotidine
[no description available]		2.08101,3-thiazoles;
guanidines;
sulfonamide		anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
quipazine maleate
[no description available]		2.0510
tulobuterol hydrochloride
[no description available]		2.0510organic molecular entity
hp 029
[no description available]		2.0510
cefotaxime
Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups.		1.97101,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen
6-(bromomethylene)tetrahydro-3-(1-naphthaleneyl)-2h-pyran-2-one
6-(bromomethylene)tetrahydro-3-(1-naphthaleneyl)-2H-pyran-2-one: structure given in first source; potent irreversible, mechanism-based inhibitor of myocardial calcium-independent phospholipase A2		2.0510naphthalenes
nf 449
[no description available]		2.0510
7-chloro-4-hydroxy-2-phenyl-1,8-naphthyridine
[no description available]		2.0510
proguanil
Proguanil: A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.. proguanil : A biguanide compound which has isopropyl and p-chlorophenyl substituents on the terminal N atoms. A prophylactic antimalarial drug, it works by inhibiting the enzyme dihydrofolate reductase, which is involved in the reproduction of the malaria parasites Plasmodium falciparum and P. vivax within the red blood cells.		2.0510biguanides;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
cci 15641
[no description available]		2.0810cephalosporin
mastoparan
[no description available]		210mastoparans;
peptidyl amide		antimicrobial agent
tenofovir disoproxil fumarate
tenofovir disoproxil fumarate : A fumarate salt prepared from equimolar amounts of tenofovir disoproxil and fumaric acid. It is used in combination therapy for the treatment of HIV infection.		2.0810fumarate saltantiviral drug;
HIV-1 reverse transcriptase inhibitor;
prodrug
homatropine hydrobromide, (endo-(+-)-isomer)
[no description available]		2.0510
dizocilpine maleate
Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.		2.0510maleate salt;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
dexbrompheniramine maleate
dexbrompheniramine maleate : The maleic acid salt of the (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.0810brompheniramine maleateanti-allergic agent;
H1-receptor antagonist
mg 624
triethyl-(beta-4-stilbenoxyethyl)ammonium: inhibits alpha7 nicotinic receptors; structure in first source		2.0510
flupirtine
[no description available]		2.0510
zimelidine hydrochloride
[no description available]		2.0510
1-palmitoyl-2-oleoylphosphatidylcholine
1-palmitoyl-2-oleoylphosphatidylcholine: RN given refers to (Z)-isomer		2.1510
rifaximin
[no description available]		2.0810acetate ester;
cyclic ketal;
lactam;
macrocycle;
organic heterohexacyclic compound;
rifamycins;
semisynthetic derivative		antimicrobial agent;
gastrointestinal drug;
orphan drug
bwa 4c
[no description available]		1.9810
9-hydroxy-11,15-dioxo-2,3,18,19-tetranorprost-5-ene-1,20-dioic acid
9-hydroxy-11,15-dioxo-2,3,18,19-tetranorprost-5-ene-1,20-dioic acid: urinary metabolite of PGD2		3.3811
everolimus
[no description available]		2.0810cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol		anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
pregna-4,17-diene-3,16-dione, (17z)-isomer
[no description available]		2.0510
su 4312
SU4312 : A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group. SU 4312 is a vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 and platelet derived growth factor (PDGF) receptor inhibitor. It also inhibits the neuronal nitric oxide synthase (NOS) and exhibits neuroprotection against NO-mediated neurotoxicity.		2.0510
nifuroxime
5-nitro-2-furaldehyde oxime: structure in first source		2.0510
gw 1929
GW 1929: activates peroxisome proliferator-activated receptor-gamma; structure in first source		2.0510benzophenones
cefpodoxime proxetil
cefpodoxime proxetil: structure given in first source; prodrug for cefpodoxime. cefpodoxime proxetil : The 1-[(isopropoxycarbonyl)oxy]ethyl (proxetil) ester prodrug of cefpodoxime. After swallowing, hydrolysis of the ester group occurs in the intestinal epithelium, to release active cefpodoxime in the bloodstream. It is used to treat acute otitis media, pharyngitis, and sinusitis.		2.0810carboxylic acid;
carboxylic ester;
cephalosporin		antibacterial drug;
prodrug
1-methyl-d-lysergic acid butanolamide
[no description available]		2.0510ergot alkaloid;
monocarboxylic acid amide		serotonergic antagonist;
sympatholytic agent;
vasoconstrictor agent
beta-escin
[no description available]		2.4110
fluphenazine
[no description available]		2.0810
protriptyline hydrochloride
[no description available]		2.0510hydrochlorideantidepressant
n-(3-(cyclohexylidene-(1h-imidazol-4-ylmethyl))phenyl)ethanesulfonamide
[no description available]		2.0510
b 43
RK-24466 : A member of the class of pyrrolopyrimidines that is 7H-pyrrolo[2,3-d]pyrimidine substituted by amino, 4-phenoxyphenyl, and cyclopentyl groups at positions 4, 5 and 7, respectively. It is a potent inhibitor of Lck that inhibits Lck (64-509) and LckCD isoforms (IC50 of less than 1 and 2 nM, respectively).		2.0510aromatic amine;
aromatic ether;
cyclopentanes;
primary amino compound;
pyrrolopyrimidine		EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
2-(3,3-diphenylpropylamino)acetamide
[no description available]		2.0510diarylmethane
l 162313
L 162313: a biphenylimidazole derivative; a non-peptide angiotensin agonist; no further information available 2/95		2.0510
5-(4-phenylbutoxy)psoralen
5-(4-phenylbutoxy)psoralen: structure in first source. psora 4 : A member of the class of psoralens that is psoralen substituted by a 4-phenylbutoxy group at position 5. It is a potent inhibitor of the voltage-gated potassium channel Kv1.3 (EC50 = 3 nM).		2.0510aromatic ether;
benzenes;
psoralens		geroprotector;
immunosuppressive agent;
potassium channel blocker
sb 222200
[no description available]		2.0510quinolines
dantrolene sodium
dantrolene sodium (anhydrous) : The anhydrous sodium salt of dantrolene.		2.0510
cr 2945
CR 2945: a member of non-peptide CCKB receptor antagonist		2.0510
nitrofurantoin
Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA.		2.0810imidazolidine-2,4-dione;
nitrofuran antibiotic;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic		antibacterial drug;
antiinfective agent;
hepatotoxic agent
sb 218795
SB 218795: structure in first source		2.0510quinolines
nifurtimox
Nifurtimox: A nitrofuran thiazine that has been used against TRYPANOSOMIASIS.		2.0510nitrofuran antibiotic
epinephrine bitartrate
[no description available]		2.0510
bicuculline methobromide
[no description available]		2.0510
butylscopolammonium bromide
Butylscopolammonium Bromide: Antimuscarinic quaternary ammonium derivative of scopolamine used to treat cramps in gastrointestinal, urinary, uterine, and biliary tracts, and to facilitate radiologic visualization of the gastrointestinal tract.		2.0510
butaclamol hydrochloride
[no description available]		2.0510
roxithromycin
(E)-roxithromycin : A major geometrical isomer of roxithromycin.		2.4720roxithromycinenvironmental contaminant;
xenobiotic
cefdinir
[no description available]		2.0810cephalosporin;
ketoxime		antibacterial drug
a 38503
[no description available]		2.0510
bisoprolol, fumarate (1:1) salt
[no description available]		2.4720
cv 1808
2-phenylaminoadenosine: has coronary & cardiohemodynamic effects		2.0510purine nucleoside
8-(n,n-diethylamino)octyl-3,4,5-trimethoxybenzoate hydrochloride
[no description available]		2.0510
artesunate
artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether		2.4720artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid		antimalarial;
antineoplastic agent;
ferroptosis inducer
oxitropium
oxitropium: RN given refers to bromide; structure		6.5854
etoposide phosphate
[no description available]		2.0810furonaphthodioxole
ciclesonide
ciclesonide: nasal spray approved for seasonal and perennial allergic rhinitis		6.6973organic molecular entity
desisobutyrylciclesonide
desisobutyrylciclesonide: an active metabolite of ciclesonide		3.4411
temsirolimus
[no description available]		2.0810macrolide lactam
dutasteride
Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland.		2.0810(trifluoromethyl)benzenes;
aza-steroid;
delta-lactam		antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
tekturna
[no description available]		2.0810fumarate saltantihypertensive agent
vildagliptin
[no description available]		2.0810amino acid amide
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.		14.724314indanes;
monohydroxyquinoline;
quinolone;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent
sgd 301-76
[no description available]		2.0810conazole antifungal drug;
imidazole antifungal drug;
organic nitrate salt		antiinfective agent
fluvoxamine maleate
[no description available]		2.4720(trifluoromethyl)benzenes
thioacetazone
Thioacetazone: A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the International Union Against Tuberculosis and are used in some developing countries to reduce drug costs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p217). thiosemicarbazone : A hydrazone resulting from the formal condensation of an aldehyde or ketone with the non-thioacylated nitrogen of thiosemicarbazide or its substituted derivatives.		2.0810
chlorproguanil
chlorproguanil: dichloro-derivative of chloroguanide; RN given refers to parent cpd; structure		2.0510dichlorobenzene
dexlansoprazole
Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE.		2.0810benzimidazoles;
sulfoxide
gemifloxacin mesylate
gemifloxacin mesylate : The mesylate salt of gemifloxacin.		2.0810methanesulfonate saltantimicrobial agent;
topoisomerase IV inhibitor
naloxone benzoylhydrazone
[no description available]		2.0510
2-methyl-6-(phenylethynyl)pyridine hydrochloride
2-methyl-6-(phenylethynyl)pyridine hydrochloride : A hydrochloride salt obtained by reaction of 2-methyl-6-(phenylethynyl)pyridine with one equivalent of hydrochloric acid. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.		2.0510hydrochlorideanxiolytic drug;
metabotropic glutamate receptor antagonist
(R)-fluoxetine hydrochloride
(R)-fluoxetine hydrochloride : A hydrochloride obtained by reaction of (R)-fluoxetine with one equivalent of hydrochloric acid.		2.0510hydrochlorideantidepressant;
serotonin uptake inhibitor
ro 8-4304
[no description available]		2.0510
uk-432097
UK-432097: a highly potent and selective agonist and drug candidate for chronic obstructive pulmonary disease (COPD) treatment; structure in first source		2.0710
brl 37344
BRL 37344: SB 206606 is the (R,R)-isomer		1.9910monocarboxylic acid
3-morpholino-sydnonimine monohydrochloride
[no description available]		2.0510
mocetinostat
mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).		4.7321aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
t 1032
T 1032: a cyclic GMP phosphodiesterase-5 inhibitor; structure in first source		2.0510
rivaroxaban
Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.		2.0810aromatic amide;
lactam;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
oxazolidinone;
thiophenes		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
(S)-fluoxetine hydrochloride
(S)-fluoxetine hydrochloride : A hydrochloride obtained by reaction of (S)-fluoxetine with one equivalent of hydrochloric acid.		2.0510hydrochlorideantidepressant;
serotonin uptake inhibitor
sr 59230a
3-(2-ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate: structure given in first source		2.0510
u 74389g
[no description available]		2.0510
1-(2-methoxyphenyl)piperazine hydrochloride
[no description available]		2.0510
ic 87114
IC 87114: structure in first source		2.07106-aminopurines;
biaryl;
quinazolines		EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
n1-phenyl-3,5-dinitro-n4,n4-di-n-propylsulfanilamide
N1-phenyl-3,5-dinitro-N4,N4-di-n-propylsulfanilamide: a potent, selective antimitotic agent against kinetoplastid parasites; structure in first source		2.0510
hki 272
[no description available]		2.0810nitrile;
quinolines		antineoplastic agent;
tyrosine kinase inhibitor
sb 203186
[no description available]		2.0510
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		2.0810N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
noscapine hydrochloride
[no description available]		2.0510
a 77636
(1R,3S)-3-(adamantan-1-yl)-1-(aminomethyl)-3,4-dihydroisochromene-5,6-diol hydrochloride : A hydrochloride salt obtained by mixing equimolar amounts of (1R,3S)-3-(adamantan-1-yl)-1-(aminomethyl)-3,4-dihydroisochromene-5,6-diol with hydrochloric acid. Potent and selective dopamine D1-like receptor agonist (pEC50 values are 8.97 and < 5 for D1-like and D2-like receptors respectively). Displays anti-Parkinsonian activity following oral administration in vivo.		2.0510hydrochlorideantiparkinson drug;
dopamine agonist
aluminum oxide
Aluminum Oxide: An oxide of aluminum, occurring in nature as various minerals such as bauxite, corundum, etc. It is used as an adsorbent, desiccating agent, and catalyst, and in the manufacture of dental cements and refractories.		4.811
cgp 20712a
CGP 20712A: structure given in first source; CGP 26505, a beta1-selective beta-adrenoceptor antagonist, is the (S)-isomer of CGP 20712A		2.4120
pazopanib
pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.		2.0810aminopyrimidine;
indazoles;
sulfonamide		angiogenesis modulating agent;
antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
levodopa methyl ester hydrochloride
[no description available]		2.0510
vilanterol
[no description available]		8.5882benzyl alcohols;
dichlorobenzene;
ether;
phenols;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent
artenimol
artenimol: derivative of antimalarial drug artemisinin (quinghaosu)		2.0510
4-phenoxyphenoxyethyl thiocyanate
4-phenoxyphenoxyethyl thiocyanate: has antiparasitic activity; structure in first source		2.0510
lu 19005
[no description available]		2.0510
batefenterol
batefenterol: a bronchodilator		6.1132
benoxathian hydrochloride
[no description available]		2.0510
((2-n-butyl-6,7-dichloro-2-cyclopentyl-2,3-dihydro-1-oxo-1h-inden-5-yl)oxy)acetic acid, (+)-isomer
[no description available]		2.0510
amg 009
AMG 009: an anti-inflammatory agent; structure in first source		2.0810
cefotaxime sodium
[no description available]		2.0810organic sodium salt
calpain inhibitor iii
calpain inhibitor III: potential anticataract drug		2.0510
GR 127935 hydrochloride
GR 127935 hydrochloride : A hydrochloride obtained by reaction of GR 127935 with one equivalent of hydrochloric acid. Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.		2.0510hydrochlorideserotonergic antagonist
olodaterol
[no description available]		3.8821aromatic ether;
benzoxazine;
phenols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent
gsk573719
GSK573719: Muscarinic Antagonist. umeclidinium : A quaternary ammonium ion that is quinuclidine substituted at positions 1 and 4 by 2-(benzyloxy)ethyl and hydroxy(diphenyl)methyl groups respectively.		7.0441
mrs 1845
[no description available]		2.0510
carfilzomib
[no description available]		4.811epoxide;
morpholines;
tetrapeptide		antineoplastic agent;
proteasome inhibitor
ru 66647
telithromycin: a ketolide; semisynthetic derivative of erythromycin with cycling of the C11-12 positions to form a carbamate ring to avoid acquired resistance to macrolides; binds 70S bacterial rRNA, specifically to the 23S part (23S RIBOSOMAL RNA), preventing protein synthesis;		2.0310
losartan potassium
Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.		2.4620
empagliflozin
[no description available]		4.811aromatic ether;
C-glycosyl compound;
monochlorobenzenes;
tetrahydrofuryl ether		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
diflucortolone
Diflucortolone: A topical glucocorticoid used in various DERMATOSES. It is absorbed through the skin, bound to plasma albumin, and may cause adrenal suppression. It is also administered as the valerate.		2.051021-hydroxy steroid
1-aminocyclopropane-1-carboxylic acid hydrochloride
[no description available]		2.0510
alaproclate hydrochloride
[no description available]		2.0510
ubenimex
[no description available]		2.0510peptide
dsp 4 hydrochloride
[no description available]		2.0510
calcimycin
Calcimycin: An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.		2.9240benzoxazole
(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzodioxan hydrochloride
N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine hydrochloride : A hydrochloride salt that is obtained by reaction of N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine with one equivalent of hydrogen chloride. An alpha1A-adrenergic selective antagonist.		2.0510hydrochloridealpha-adrenergic antagonist
2-cyclooctyl-2-hydroxyethylamine hydrochloride
[no description available]		2.0510
cirazoline monohydrochloride
[no description available]		2.0510
adtn
[no description available]		2.0510
apocodeine hydrochloride, (r)-isomer
[no description available]		2.0510
2-hydroxyapomorphine, (r)-isomer
[no description available]		2.0510
lilly 78335
[no description available]		2.0510
efaroxan hydrochloride
[no description available]		2.0510
fenoldopam hydrobromide
[no description available]		2.0510
1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride : A hydrochloride salt that is obtained by reaction of 1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine with two equivalents of hydrogen chloride. Potent and selective inhibitor of dopamine uptake (KD = 5.5 nM in rat striatal membranes).		2.0510hydrochloridedopamine uptake inhibitor
7-hydroxy-2-n,n-dipropylaminotetralin hydrobromide
[no description available]		2.0510
8-hydroxy-2-(di-n-propylamino)tetralin hydrobromide, (r)-isomer,
[no description available]		2.0510organic molecular entity
1-(2-(4-(4-fluoro-benzoyl)-piperidin-1-yl)-ethyl)-3,3-dimethyl-1,2-dihydro-indol-2-one
LY-310762 hydrochloride : A hydrochloride resulting from the formal reation of equimolar amount of LY-310762 with hydrogen chloride. A potent and selective antagonist for the 5-hydroxytryptamine 1D (5-HT1D) receptor.		2.0510hydrochloridereceptor modulator;
serotonergic antagonist
4-iodoclonidine
[no description available]		2.0510
alpha-methyltyrosine methyl ester, monohydrochloride
[no description available]		2.0510
octoclothepine maleate
[no description available]		2.0510
2-(n-phenethyl-n-propyl)amino-5-hydroxytetralin hydrochloride
[no description available]		2.0510
du 24565
[no description available]		2.0510
2-methoxyidazoxan hydrochloride
[no description available]		2.0510
N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol hydrobromide
N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol hydrobromide : A hydrobromide salt prepared from N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol and one equivalent of hydrogen bromide. Dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors respectively). May act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonising the behavioral effects of cocaine.		2.0510hydrobromidedopamine agonist;
prodrug
ro 25-6981
[no description available]		2.0510
sk&f 77434
N-allyl-1-phenyl-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol hydrobromide : A hydrobromide salt prepared from N-allyl-1-phenyl-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol and one equivalent of hydrogen bromide. Selective dopamine D1-like receptor partial agonist (IC50 values are 19.7 and 2425 nM for binding to D1-like and D2-like receptors respectively). Centrally active following systemic administration in vivo.		2.0510hydrobromidedopamine agonist;
prodrug
3-[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline-9-yl]-1,1-diethylurea
[no description available]		2.0510organic heterotetracyclic compound;
organonitrogen heterocyclic compound
dactolisib
dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR. dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.		2.0810imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
demethylcantharidin
demethylcantharidin: has antineoplastic activity; structure in first source		2.0510
atropine sulfate
[no description available]		2.0510
deoxoartemisinin
deoxoartemisinin: structure given in first source		2.0510
rabeprazole sodium
[no description available]		2.0810organic sodium salt
win 62577
[no description available]		2.0510
amodiaquine hydrochloride
[no description available]		2.0510
cytochrome c-t
Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV.		2.5520
bivalirudin
bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant.		2.0810polypeptideanticoagulant;
EC 3.4.21.5 (thrombin) inhibitor
somatostatin
[no description available]		2.0810heterodetic cyclic peptide;
peptide hormone
ro 25-1553
Ro 25-1553: a cyclic peptide analog and agonist of vasoactive intestinal peptide; a VPAC(2) receptor agonist; amino acid sequence given in first source		210
oligonucleotides
[no description available]		2.1710
ly-146032
[no description available]		2.0810heterodetic cyclic peptide;
lipopeptide antibiotic;
lipopeptide;
macrocycle;
macrolide		antibacterial drug;
bacterial metabolite;
calcium-dependent antibiotics
warfarin sodium
warfarin sodium : A racemate comprising equal amounts of (R)- and (S)-warfarin sodium. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.		2.0810
cellulose
DEAE-Cellulose: Cellulose derivative used in chromatography, as ion-exchange material, and for various industrial applications.		4.811glycoside
quinine sulfate
[no description available]		2.0510hydrate
quercetin
[no description available]		2.0510
endothelin-1
Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)		2.0310
phosphatidylcholines
Phosphatidylcholines: Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a CHOLINE moiety.		4.49511,2-diacyl-sn-glycero-3-phosphocholine
(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.		16.4744321-hydroxy steroid
rv 538, (r-(r*,r*))-isomer
[no description available]		2.0510
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (1s-cis)-isomer
[no description available]		2.0510
pravastatin sodium
pravastatin sodium : An organic sodium salt that is the sodium salt of pravastatin. A reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA), it is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		2.0810organic sodium salt;
statin (semi-synthetic)		anticholesteremic drug
alendronate sodium
[no description available]		2.0810
valproate sodium
Epilim: oral sodium valproate used as antidepressive agent. sodium valproate : The sodium salt of valproic acid.. valproate : A branched-chain saturated fatty acid anion that is the conjugate base of valproic acid.		2.0510organic sodium saltgeroprotector
sl 80.0750
[no description available]		2.0810
chitosan
[no description available]		2.0810
s-nitro-n-acetylpenicillamine
S-nitro-N-acetylpenicillamine: a NO donor		2.0310
mesna
Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE.		2.0810organosulfonic acid
bucladesine
Bucladesine: A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed). bucladesine : A 3',5'-cyclic purine nucleotide that is the 2'-butanoate ester and 6-N-butanoyl derivative of 3',5'-cyclic AMP.		2.7303',5'-cyclic purine nucleotide
clavulanate potassium
potassium clavulanate : A potassium salt having clavulanate as the counterion. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes and has only weak anitbiotic activity when administered alone. However it can be used in combination with amoxicillin trihydrate (under the trade name Augmentin) for treatment of a variety of bacterial infections, where it prevents antibiotic inactivation by microbial lactamases.		2.0810potassium saltantibacterial drug;
antimicrobial agent;
EC 3.5.2.6 (beta-lactamase) inhibitor
taurocholic acid, monosodium salt
[no description available]		2.0510bile salt
piperacillin sodium
[no description available]		2.0810organic sodium salt
oxacillin sodium
[no description available]		2.0810organic sodium salt
fusidate sodium
[no description available]		2.0510
cefazolin sodium
cefazolin sodium : A cephalosporin organic sodium salt having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups.		2.4720organic sodium salt
azlocillin sodium
[no description available]		2.0810organic sodium salt
cortisol succinate, sodium salt
hydrocortisone hemisuccinate: RN given refers to (11beta)-isomer; Synonyms Solu-Cortef & sopolcort H refer to Na salt		2.0510organic molecular entity
combivent respimat
Albuterol, Ipratropium Drug Combination: A combined pharmaceutical preparation of Ipratropium Bromide and Albuterol Sulfate that is used to treat the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE.		2.1110
niraparib
niraparib: structure in first source. niraparib : A 2-[4-(piperidin-3-yl)phenyl]-2H-indazole-7-carboxamide that has S-configuration. It is a potent inhibitor of PARP1 and PARP2 (IC50 of 3.8 and 2.1 nM, respectively) and approved as a first-line maintenance treatment for women with advanced ovarian cancer after responding to platinum-based chemotherapy.		4.8112-[4-(piperidin-3-yl)phenyl]-2H-indazole-7-carboxamideantineoplastic agent;
apoptosis inducer;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
radiosensitizing agent
plx4032
[no description available]		4.811aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide		antineoplastic agent;
B-Raf inhibitor
piperidines
Piperidines: A family of hexahydropyridines.		4.9921
interleukin-8
Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.		9.08216
abt-450
paritaprevir: inhibits HCV NS3 protease. paritaprevir : An azamacrocycle which is used which is in combination with dasabuvir sodium hydrate, ombitasvir and ritonavir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		2.1310
butyrolactone i
butyrolactone I: selective inhibitor of cdk2 & cdc2 kinase; structure given in first source		2.0510butenolide
vasoactive intestinal peptide
Vasoactive Intestinal Peptide: A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).		210
ascorbic acid
Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.		2.0510ascorbic acid;
vitamin C		coenzyme;
cofactor;
flour treatment agent;
food antioxidant;
food colour retention agent;
geroprotector;
plant metabolite;
skin lightening agent
tetracycline
Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.		2.4720
oxytetracycline, anhydrous
Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae.		2.0510
minocycline
Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.		2.0510
piroxicam
[no description available]		2.7530benzothiazine;
monocarboxylic acid amide;
pyridines		analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
roquinimex
roquinimex: structure in first source		2.0810aromatic amide
mobic
Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis.		2.08101,3-thiazoles;
benzothiazine;
monocarboxylic acid amide		analgesic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
mobiflex
tenoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It is also indicated for short term treatment of acute musculoskeletal disorders including strains, sprains and other soft-tissue injuries.		2.4720heteroaryl hydroxy compound;
monocarboxylic acid amide;
pyridines;
thienothiazine		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
isoxicam
isoxicam : A monocarboxylic acid amide that is piroxicam in which the pyrid-2-yl group is replaced by a 5-methyl-1,2-oxazol-3-yl group. A non-steroidal anti-inflammatory drug, it was withdrawn from the market in the 1980s following its association with cases of Stevens-Johnson syndrome.		2.0810benzothiazine;
isoxazoles;
monocarboxylic acid amide		antirheumatic drug;
non-steroidal anti-inflammatory drug
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		2.4520benzenes;
hydroxycoumarin;
methyl ketone
rolitetracycline
Rolitetracycline: A pyrrolidinylmethyl TETRACYCLINE.. rolitetracycline : A derivative of tetracycline in which the amide function is substituted with a pyrrolidinomethyl group.		2.0510
hispidin
hispidin: metabolite of Basidiomycete Polyporus hispidus. hispidin : Fungal metabolite first found in basidiomycete Inonotus hispidus (formerly Polyporus hispidus).		2.05102-pyranones;
catechols		antioxidant;
EC 2.7.11.13 (protein kinase C) inhibitor;
fungal metabolite
minocycline hydrochloride
[no description available]		2.4720
demeclocycline hydrochloride
demeclocycline hydrochloride : The hydrochloride salt of demeclocycline. A tetracycline antibiotic, it is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective.		2.0510
tigecycline
[no description available]		2.0810
lornoxicam
lornoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 6-chloro-4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain, primarily resulting from inflammatory diseases of the joints, osteoarthritis, surgery, sciatica and other inflammations.		2.0810heteroaryl hydroxy compound;
monocarboxylic acid amide;
organochlorine compound;
pyridines;
thienothiazine		antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
abt-267
ombitasvir: inhibits HCV NS5A protein, component of Viekirax. ombitasvir : A dipeptide derivative which is used which is in combination with dasabuvir sodium hydrate, paritaprevir and ritonavir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		2.1310aromatic amide;
carbamate ester;
dipeptide;
pyrrolidines		antiviral drug;
hepatitis C virus nonstructural protein 5A inhibitor
abt-333
dasabuvir: an antiviral agent. dasabuvir : A member of the class of pyrimidone, which is (as the monohydrate of its sodium salt) in combination with ombitasvir, paritaprevir and ritonavir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		2.1310aromatic ether;
naphthalenes;
pyrimidone;
sulfonamide		antiviral drug;
nonnucleoside hepatitis C virus polymerase inhibitor
byl719
[no description available]		4.811proline derivative
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.		5.2660
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.		14.674620
epidermal growth factor
Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.		2.4620
transforming growth factor beta
Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.		2.0310
cyclin d1
Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.		2.0410
transforming growth factor alpha
Transforming Growth Factor alpha: An EPIDERMAL GROWTH FACTOR related protein that is found in a variety of tissues including EPITHELIUM, and maternal DECIDUA. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form which binds to the EGF RECEPTOR.		2.420
cyclosporine
Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).		3.110
lactoferrin
Lactoferrin: An iron-binding protein that was originally characterized as a milk protein. It is widely distributed in secretory fluids and is found in the neutrophilic granules of LEUKOCYTES. The N-terminal part of lactoferrin possesses a serine protease which functions to inactivate the TYPE III SECRETION SYSTEM used by bacteria to export virulence proteins for host cell invasion.		2.2110
thromboplastin
Thromboplastin: Constituent composed of protein and phospholipid that is widely distributed in many tissues. It serves as a cofactor with factor VIIa to activate factor X in the extrinsic pathway of blood coagulation.		3.4211
muramidase
Muramidase: A basic enzyme that is present in saliva, tears, egg white, and many animal fluids. It functions as an antibacterial agent. The enzyme catalyzes the hydrolysis of 1,4-beta-linkages between N-acetylmuramic acid and N-acetyl-D-glucosamine residues in peptidoglycan and between N-acetyl-D-glucosamine residues in chitodextrin. EC 3.2.1.17.		3.8121
entecavir
entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B.		2.08102-aminopurines;
oxopurine;
primary alcohol;
secondary alcohol		antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
acyclovir
Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections.		2.08102-aminopurines;
oxopurine		antimetabolite;
antiviral drug
cyclic gmp
Cyclic GMP: Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed). 3',5'-cyclic GMP : A 3',5'-cyclic purine nucleotide in which the purine nucleobase is specified as guanidine.		1.99103',5'-cyclic purine nucleotide;
guanyl ribonucleotide		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
guanosine 5'-o-(3-thiotriphosphate)
Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.		210nucleoside triphosphate analogue
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.4720cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
clozapine
Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.		4.2850benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
dacarbazine
(E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration.		2.0810dacarbazine
didanosine
Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS.		2.0810purine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor;
geroprotector;
HIV-1 reverse transcriptase inhibitor
ganciclovir
[no description available]		2.08102-aminopurines;
oxopurine		antiinfective agent;
antiviral drug
valtrex
[no description available]		2.0810organic molecular entity
olanzapine
Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.		2.0810benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
zaprinast
zaprinast: anaphylaxis inhibitor; structure		2.0510triazolopyrimidines
raltitrexed
[no description available]		2.0810N-acyl-amino acid
allopurinol
Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.		2.4720nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger
citrovorum factor
[no description available]		2.0810tetrahydrofolic acid
rifapentine
rifapentine: cyclopentyl derivative of rifampicin		2.0810N-alkylpiperazine;
N-iminopiperazine;
rifamycins		antitubercular agent;
leprostatic drug
thiolactomycin
thiolactomycin: from actinomycetes; structure given in first source		2.0510
3,4,5-trihydroxybenzamidoxime
3,4,5-trihydroxybenzamidoxime: structure given in first source		2.0510benzenetriol
norclozapine
norclozapine: structure given in first source. N-desmethylclozapine : A dibenzodoazepine substituted with chloro and piperazino groups which is a major metabolite of clozapine; a potent and selective 5-HT2C serotonin receptor antagonist.		2.1310dibenzodiazepine;
organochlorine compound;
piperazines		delta-opioid receptor agonist;
metabolite;
serotonergic antagonist
sildenafil citrate
Sildenafil Citrate: A PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.. sildenafil citrate : The citrate salt of sildenafil.		3.8840citrate saltEC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
aprepitant
Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.		2.0810(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
triazoles		antidepressant;
antiemetic;
neurokinin-1 receptor antagonist;
peripheral nervous system drug;
substance P receptor antagonist
tegaserod maleate
[no description available]		2.0810maleate saltserotonergic agonist
rifabutin
[no description available]		2.0810
8-bromocyclic gmp, sodium salt
sodium 8-bromo-3',5'-cyclic GMP : An organic sodium salt having 8-bromoguanosine 3',5'-cyclic phosphate as the counterion. A membrane permeable cGMP analogue that activates protein kinase G (PKG). It is 4.3-fold more potent than cGMP in activating PKG1alpha and promotes relaxation of tracheal and vascular smooth muscle tissue in vitro.		2.0510organic sodium saltmuscle relaxant;
protein kinase G agonist
ag-879
AG-879: structure given in first source		2.0510
leptin
Leptin: A 16-kDa peptide hormone secreted from WHITE ADIPOCYTES. Leptin serves as a feedback signal from fat cells to the CENTRAL NERVOUS SYSTEM in regulation of food intake, energy balance, and fat storage.		4.811
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.0310amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
acetamide
acetimidic acid : A carboximidic acid that is acetic acid in which the carbonyl oxygen is replaced by an imino group.		2.0310acetamides;
carboximidic acid;
monocarboxylic acid amide;
N-acylammonia
quinacrine
Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.. quinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9.		3.5920acridines;
aromatic ether;
organochlorine compound;
tertiary amino compound		antimalarial;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
catechol
[no description available]		2.0310catecholsallelochemical;
genotoxin;
plant metabolite
bupropion
Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring.		2.0210aromatic ketone;
monochlorobenzenes;
secondary amino compound		antidepressant;
environmental contaminant;
xenobiotic
taxifolin
[no description available]		2.03103'-hydroxyflavanones;
4'-hydroxyflavanones;
dihydroflavonols;
pentahydroxyflavanone;
secondary alpha-hydroxy ketone
phosphonoacetic acid
Phosphonoacetic Acid: A simple organophosphorus compound that inhibits DNA polymerase, especially in viruses and is used as an antiviral agent.. phosphonoacetic acid : A member of the class of phosphonic acids that is phosphonic acid in which the hydrogen attached to the phosphorous is replaced by a carboxymethyl group.		2.0310monocarboxylic acid;
phosphonic acids		antiviral agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor
3,4-dihydroxyphenylacetic acid
3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.. (3,4-dihydroxyphenyl)acetic acid : A dihydroxyphenylacetic acid having the two hydroxy substituents located at the 3- and 4-positions. It is a metabolite of dopamine.. dihydroxyphenylacetic acid : A dihydroxy monocarboxylic acid consisting of phenylacetic acid having two phenolic hydroxy substituents.		2.0310catechols;
dihydroxyphenylacetic acid		human metabolite
aminocaproic acid
Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator.		2.4320amino acid zwitterion;
epsilon-amino acid;
omega-amino fatty acid		antifibrinolytic drug;
hematologic agent;
metabolite
diacetyl
butane-2,3-dione : An alpha-diketone that is butane substituted by oxo groups at positions 2 and 3. It is a metabolite produced during the malolactic fermentation.		2.0310alpha-diketoneEscherichia coli metabolite;
Saccharomyces cerevisiae metabolite
hydroquinone
[no description available]		2.0310benzenediol;
hydroquinones		antioxidant;
carcinogenic agent;
cofactor;
Escherichia coli metabolite;
human xenobiotic metabolite;
mouse metabolite;
skin lightening agent
melatonin
[no description available]		2.0310acetamides;
tryptamines		anticonvulsant;
central nervous system depressant;
geroprotector;
hormone;
human metabolite;
immunological adjuvant;
mouse metabolite;
radical scavenger
n-acetylserotonin
N-acetylserotonin : An N-acylserotonin resulting from the formal condensation of the primary amino group of serotonin with the carboxy group of acetic acid.		2.0310acetamides;
N-acylserotonin;
phenols		antioxidant;
human metabolite;
mouse metabolite;
tropomyosin-related kinase B receptor agonist
pyrazinamide
pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.		2.0310monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug
quinolinic acid
Quinolinic Acid: A metabolite of tryptophan with a possible role in neurodegenerative disorders. Elevated CSF levels of quinolinic acid are correlated with the severity of neuropsychological deficits in patients who have AIDS.. pyridinedicarboxylic acid : Any member of the class of pyridines carrying two carboxy groups.. quinolinic acid : A pyridinedicarboxylic acid that is pyridine substituted by carboxy groups at positions 2 and 3. It is a metabolite of tryptophan.		2.0310pyridinedicarboxylic acidEscherichia coli metabolite;
human metabolite;
mouse metabolite;
NMDA receptor agonist
taurine
[no description available]		2.0310amino sulfonic acid;
zwitterion		antioxidant;
Escherichia coli metabolite;
glycine receptor agonist;
human metabolite;
mouse metabolite;
nutrient;
radical scavenger;
Saccharomyces cerevisiae metabolite
2-amino-5-phosphonovalerate
2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.		2.0310non-proteinogenic alpha-amino acidNMDA receptor antagonist
alpha-methyl-4-carboxyphenylglycine
[no description available]		2.0310
3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid
3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid: structure given in first source; NMDA receptor antagonist		2.0310
1-hydroxy-3-amino-2-pyrrolidone
1-hydroxy-3-amino-2-pyrrolidone: a CNS depressant; structure in first source		2.0310
ibotenic acid
Ibotenic Acid: A neurotoxic isoxazole (similar to KAINIC ACID and MUSCIMOL) found in AMANITA mushrooms. It causes motor depression, ataxia, and changes in mood, perceptions and feelings, and is a potent excitatory amino acid agonist.		2.0310non-proteinogenic alpha-amino acidneurotoxin
n(8)-bromoacetyl-n(1)-3'-(4-indolyloxy)-2'-hydroxypropyl-1,8-diamino-4-menthane
N(8)-bromoacetyl-N(1)-3'-(4-indolyloxy)-2'-hydroxypropyl-1,8-diamino-4-menthane: structure given in first source		2.0310
sk&f-38393
2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.. 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol : A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine bearing a phenyl substituent at position 1 and two hydroxy substituents at positions 7 and 8.. SKF 38393 : A racemate comprising equimolar amounts of (R)- and (S)-SKF 38393		2.0310benzazepine;
catechols;
secondary amino compound
vanilmandelic acid
Vanilmandelic Acid: A 3-O-methyl ether of 3,4-dihydroxymandelic acid. It is an end-stage metabolite of CATECHOLAMINES; EPINEPHRINE; and NOREPINEPHRINE.. vanillylmandelic acid : An aromatic ether that is the 3-O-methyl ether of 3,4-dihydroxymandelic acid.		2.03102-hydroxy monocarboxylic acid;
aromatic ether;
phenols		human metabolite
1,10-diaminodecane
[no description available]		2.0310
1,3-diethyl-8-phenylxanthine
1,3-diethyl-8-phenylxanthine: structure given in first source		2.0310
1,3-dipropyl-8-cyclopentylxanthine
DPCPX : An oxopurine that is 7H-xanthine substituted at positions 1 and 3 by propyl groups and at position 8 by a cyclohexyl group.		2.0310oxopurineadenosine A1 receptor antagonist;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
1,3-dipropyl-8-(4-sulfophenyl)xanthine
1,3-dipropyl-8-(4-sulfophenyl)xanthine: adenosine receptor antagonist		2.0310
1,5-dihydroxyisoquinoline
1,5-dihydroxyisoquinoline: structure in first source. isoquinoline-1,5-diol : An isoquinolinol that is isoquinoline in which the hydrogens at positions 1 and 5 are replaced by hydroxy groups.		2.0310isoquinolinolEC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
pk 11195
PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine		2.0310aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes		antineoplastic agent
1-(2-trifluoromethylphenyl)imidazole
1-(2-trifluoromethylphenyl)imidazole: an inhibitor of neuronal nitric oxide synthase in mouse		2.0310imidazoles
1-aminobenzotriazole
[no description available]		2.0310
1-methylimidazole
1-methyl-1H-imidazole : A 1H-imidazole having a methyl substituent at the N-1 position.		2.0310imidazoles
edelfosine
edelfosine: RN given refers to parent cpd. edelfosine : A racemate comprising equimolar amounts of (R)- and (S)-edelfosine.. 1-octadecyl-2-methylglycero-3-phosphocholine : A glycerophosphocholine that is glycero-3-phosphocholine substituted at positions 1 and 2 by octadecyl and methyl groups respectively.		2.0310glycerophosphocholine
1h-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one
1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one: structure given in first source; inhibits guanylyl cyclase. 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one : A member of the class of oxadiazoloquinoxalines that is 1H-[1,2,4]oxadiazolo[4,3-a]quinoxaline substituted at position 1 by an oxo group.		2.0310oxadiazoloquinoxalineEC 4.6.1.2 (guanylate cyclase) inhibitor
2,2'-dipyridyl
2,2'-Dipyridyl: A reagent used for the determination of iron.. 2,2'-bipyridine : A bipyridine in which the two pyridine moieties are linked by a bond between positions C-2 and C-2'.		2.0310bipyridinechelator;
ferroptosis inhibitor
2-hydroxysaclofen
2-hydroxysaclofen: structure given in first source		2.0310organochlorine compound
3,4-dichloroisocoumarin
3,4-dichloroisocoumarin : A member of the class of isocoumarins that is isocoumarin substituted by chloro groups at positions 3 and 4. It is a serine protease inhibitor.		2.0310isocoumarins;
organochlorine compound		geroprotector;
serine protease inhibitor
phaclofen
phaclofen: peripheral & central baclofen & GABA antagonist; structure given in first source		2.0310organophosphate oxoanion;
zwitterion
3-aminobenzamide
[no description available]		2.0310benzamides;
substituted aniline		EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
3-bromo-7-nitroindazole
[no description available]		2.0310
enprofylline
enprofylline : Xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.		2.0310oxopurineanti-arrhythmia drug;
anti-asthmatic drug;
bronchodilator agent;
non-steroidal anti-inflammatory drug
3-nitropropionic acid
3-nitropropionic acid: succinate dehydrogenase inactivator; biosynthesized by FABACEAE plants from ASPARAGINE. 3-nitropropanoic acid : A C-nitro compound that is propanoic acid in which one of the methyl hydrogens has been replaced by a nitro group.		2.0310C-nitro compoundantimycobacterial drug;
EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor;
mycotoxin;
neurotoxin
4-amino-1,8-naphthalimide
4-amino-1,8-naphthalimide: inhibits ADP-ribosylation; sometimes abreviated as 4-AN;		2.0310benzoisoquinoline;
dicarboximide
4-aminopyridine
[no description available]		2.0310aminopyridine;
aromatic amine		avicide;
orphan drug;
potassium channel blocker
homovanillic acid
Homovanillic Acid: A 3-O-methyl ETHER of (3,4-dihydroxyphenyl)acetic acid.. homovanillate : A hydroxy monocarboxylic acid anion which is obtained by deprotonation of the carboxy group of homovanillic acid.. homovanillic acid : A monocarboxylic acid that is the 3-O-methyl ether of (3,4-dihydroxyphenyl)acetic acid. It is a catecholamine metabolite.		2.0310guaiacols;
monocarboxylic acid		human metabolite;
mouse metabolite
4-hydroxybenzoic acid hydrazide
4-hydroxybenzoic acid hydrazide: metabolite of nifuroxazide. 4-hydroxybenzohydrazide : A carbohydrazide obtained by formal condensation of the carboxy group of 4-hydroxybenzoic acid with hydrazine.		2.0310carbohydrazide;
phenols
4-phenyl-3-furoxancarbonitrile
4-phenyl-3-furoxancarbonitrile: structure given in first source. 4-phenyl-3-furoxancarbonitrile : A 1,2,5-oxadiazole substituted by an oxido, cyano and phenyl groups at positions 2, 3 and 4, respectively. It is a vasodilator and inhibitor of platelet aggregation.		2.03101,2,5-oxadiazole;
benzenes;
N-oxide;
nitrile		geroprotector;
nitric oxide donor;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent
5,5-dimethyl-1-pyrroline-1-oxide
5,5-dimethyl-1-pyrroline-1-oxide: do not confuse with DMPO (4',5'-dihydroxy-7-methoxy-4-phenyl-5,2'-oxidocoumarin). 5,5-dimethyl-1-pyrroline N-oxide : A member of the class of 1-pyrroline nitrones (1-pyrroline N-oxides) resulting from the formal N-oxidation of 5,5-dimethyl-1-pyrroline. Used as a spin trap for the study of radicals formed by enzymatic acetaldehyde oxidation.		2.03101-pyrroline nitronesneuroprotective agent;
spin trapping reagent
phenytoin
[no description available]		2.4320imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
5,7-dichlorokynurenic acid
5,7-dichlorokynurenic acid: potent antagonist at the N-methyl-D-aspartate receptor-associated glycine binding site		2.0310quinolines
5-(n,n-hexamethylene)amiloride
5-(N,N-hexamethylene)amiloride: inhibitor of Na+-H+ exchange; has anti-HIV-1 activity. 5-(N,N-hexamethylene)amiloride : A member of the class of pyrazines that is amiloride in which the two amino hydrogens at position N-5 are replaced by a hexamethylene moiety, resulting in the formation of an azepane ring.		2.0310aromatic amine;
azepanes;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines		antineoplastic agent;
apoptosis inducer;
odorant receptor antagonist;
sodium channel blocker
ethylisopropylamiloride
ethylisopropylamiloride: structure in first source. ethylisopropylamiloride : A member of the class of pyrazines that is amiloride in which the amino substitutent of the pyrazine ring that is adjacent to the chloro substituent has been substituted by an ethyl group and by an isopropyl group.		2.0310aromatic amine;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines;
tertiary amino compound		anti-arrhythmia drug;
neuroprotective agent;
sodium channel blocker
5-fluoroindole-2-carboxylic acid
5-fluoroindole-2-carboxylic acid: N-methyl-D-aspartate receptor antagonist		2.0310indolyl carboxylic acid
hydroxyindoleacetic acid
(5-hydroxyindol-3-yl)acetic acid : A member of the class of indole-3-acetic acids that is indole-3-acetic acid substituted by a hydroxy group at C-5.		2.0310indole-3-acetic acidsdrug metabolite;
human metabolite;
mouse metabolite
phenanthridone
phenanthridone: coal tar derivative; structure given in first source. phenanthridone : A member of the class of phenanthridines that is phenanthridine with an oxo substituent at position 6. A poly(ADP-ribose) polymerase (PARP) inhibitor, it has been shown to exhibit immunosuppressive activity.		2.0310lactam;
phenanthridines		EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
immunosuppressive agent;
mutagen
6-chloromelatonin
[no description available]		2.0310acetamides
6-hydroxymelatonin
6-hydroxymelatonin : A member of the class of tryptamines that is melatonin with a hydroxy group substituent at position 6.		2.0310acetamides;
tryptamines		metabolite;
mouse metabolite
6-methoxytryptoline
6-methoxytryptoline: RN given refers to parent cpd; structure		2.0310
6-nitroso-1,2-benzopyrone
[no description available]		2.0310
7-chlorokynurenic acid
7-chlorokynurenic acid: selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex; structure given in first source. 7-chlorokynurenic acid : A quinolinemonocarboxylic acid that is quinaldic acid which is substituted by a hydroxy group at position 4 and by a chlorine at position 7. It is a potent NMDA glutamate receptor antagonist which antagonizes the strychnine-insensitive glycine site of the NMDA receptor. It also prevents neurodegeneration produced by quinolinic acid.		2.0310organochlorine compound;
quinolinemonocarboxylic acid		neuroprotective agent;
NMDA receptor antagonist
7-nitroindazole
7-nitroindazole: an inhibitor of nitric oxide synthase; exhibits anti-nociceptive activity without increasing blood pressure		2.0310
8-(4-sulfophenyl)theophylline
8-(4-sulfophenyl)theophylline: adenosine antagonist		2.0310
8-cyclopentyl-1,3-dimethylxanthine
8-cyclopentyl-1,3-dimethylxanthine: prolongs epileptic seizures in rats		2.0310oxopurine
8-phenyltheophylline
8-phenyltheophylline: purinergic P1 receptor antagonist		2.0310
tacrine
Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.		2.0210acridines;
aromatic amine		EC 3.1.1.7 (acetylcholinesterase) inhibitor
acebutolol
Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.		2.4220aromatic amide;
ethanolamines;
ether;
monocarboxylic acid amide;
propanolamine;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympathomimetic agent
acetaminophen
Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group.		2.0210acetamides;
phenols		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
cyclooxygenase 3 inhibitor;
environmental contaminant;
ferroptosis inducer;
geroprotector;
hepatotoxic agent;
human blood serum metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
acetazolamide
Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)		2.0310monocarboxylic acid amide;
sulfonamide;
thiadiazoles		anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
acetohexamide
Acetohexamide: A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.. acetohexamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is replaced by a p-acetylphenylsulfonyl group, while a hydrogen attached to the other nitrogen is replaced by a cyclohexyl group.		2.0310acetophenones;
N-sulfonylurea		hypoglycemic agent;
insulin secretagogue
acetohydroxamic acid
acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group.		2.0210acetohydroxamic acids;
carbohydroximic acid		algal metabolite;
EC 3.5.1.5 (urease) inhibitor
ag 127
tyrphostin AG 126: inhibits development of postoperative ileus induced by surgical manipulation of murine colon		2.0310nitrophenol
rtki cpd
[no description available]		2.0310aromatic ether;
monochlorobenzenes;
quinazolines		antineoplastic agent;
antiviral agent;
epidermal growth factor receptor antagonist;
geroprotector
tyrphostin a23
tyrphostin A23: inhibits EGF-stimulated thymidine incorporation as well as EGF-stimulated receptor autophosphorylation & tyrosine phosphorylation & cell proliferation; structure given in first source		2.0310catechols
tyrphostin 25
[no description available]		2.0310benzenetriol
tyrphostin a1
[no description available]		2.0310methoxybenzenesgeroprotector
1-aminoindan-1,5-dicarboxylic acid
1-aminoindan-1,5-dicarboxylic acid: structure given in first source		2.0310
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).		4.7790phenols;
phenylethanolamines;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
environmental contaminant;
xenobiotic
alendronate
alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups.		2.02101,1-bis(phosphonic acid);
primary amino compound		bone density conservation agent;
EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor
alpha-methyltyrosine methyl ester
alpha-methyltyrosine methyl ester: RN given refers to parent cpd		2.0310
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		2.0210organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
alprenolol
Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.. alprenolol : A secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent.		2.0210secondary alcohol;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
altretamine
Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine.		2.4320triamino-1,3,5-triazine
amantadine
amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source		2.0210adamantanes;
primary aliphatic amine		analgesic;
antiparkinson drug;
antiviral drug;
dopaminergic agent;
NMDA receptor antagonist;
non-narcotic analgesic
amfonelic acid
amfonelic acid: CNS-stimulant		2.0310
amifostine anhydrous
Amifostine: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.. amifostine : An organic thiophosphate that is the S-phospho derivative of 2-[(3-aminopropyl)amino]ethanethiol. A prodrug for the free thiol, WR-1065, which is used as a cytoprotectant in cancer chemotherapy and radiotherapy.		2.4320diamine;
organic thiophosphate		antioxidant;
prodrug;
radiation protective agent
aminoglutethimide
Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.. aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position.		2.0210dicarboximide;
piperidones;
substituted aniline		adrenergic agent;
anticonvulsant;
antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
theophylline
[no description available]		2.4320dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
amiodarone
Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.		2.42201-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
amitriptyline
Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.		2.0210carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
amlexanox
amlexanox: SRA-A antagonist;structure given in first source. amlexanox : A pyridochromene-derived monocarboxylic acid having an amino substituent at the 2-position, an oxo substituent at the 5-position and an isopropyl substituent at the 7-position.		2.0210monocarboxylic acid;
pyridochromene		anti-allergic agent;
anti-ulcer drug;
non-steroidal anti-inflammatory drug
amlodipine
Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.		2.0210dihydropyridine;
ethyl ester;
methyl ester;
monochlorobenzenes;
primary amino compound		antihypertensive agent;
calcium channel blocker;
vasodilator agent
amodiaquine
Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.. amodiaquine : A quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position.		3.3110aminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
amoxapine
Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.		2.4320dibenzooxazepineadrenergic uptake inhibitor;
antidepressant;
dopaminergic antagonist;
geroprotector;
serotonin uptake inhibitor
anastrozole
[no description available]		2.0210nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
aniracetam
[no description available]		2.0310N-acylpyrrolidine;
pyrrolidin-2-ones
2-amino-4-phosphonobutyric acid
2-amino-4-phosphonobutyric acid: glutamate antagonist in locust muscle; structure; do not confuse with L-AP4, which is the propionic acid version		2.0310
apraclonidine
apraclonidine: relieves postoperative intraocular pressure following trabeculoplasty; RN given refers to parent cpd. apraclonidine : An imidazoline that is 2-amino 4,5-dihydro-1H-imidazoline in which one of the exocyclic amino hydrogens has been replaced by a 4-amino-2,6-dichlorophenyl group.		2.0210dichlorobenzene;
guanidines;
imidazolines		alpha-adrenergic agonist;
antiglaucoma drug;
beta-adrenergic agonist;
diagnostic agent;
ophthalmology drug
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		2.4320benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
astemizole
Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.		2.4420benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
atenolol
Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.		2.9640ethanolamines;
monocarboxylic acid amide;
propanolamine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
alpha-amino-3-hydroxy-5-tert-butyl-4-isoxazolepropionate
alpha-amino-3-hydroxy-5-tert-butyl-4-isoxazolepropionate: a glutamate agonist		2.0310alpha-amino acid
aurintricarboxylic acid
Aurintricarboxylic Acid: A dye which inhibits protein biosynthesis at the initial stages. The ammonium salt (aluminon) is a reagent for the colorimetric estimation of aluminum in water, foods, and tissues.. aurintricarboxylic acid : A member of the class of quinomethanes that is 3-methylidene-6-oxocyclohexa-1,4-diene-1-carboxylic acid in which the methylidene hydrogens are replaced by 4-carboxy-3-hydroxyphenyl groups. The trisodium salt is the biological stain 'chrome violet CG' while the triammonium salt is 'aluminon'.		2.0310monohydroxybenzoic acid;
quinomethanes;
tricarboxylic acid		fluorochrome;
histological dye;
insulin-like growth factor receptor 1 antagonist
azathioprine
Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS.		2.4320aryl sulfide;
C-nitro compound;
imidazoles;
thiopurine		antimetabolite;
antineoplastic agent;
carcinogenic agent;
DNA synthesis inhibitor;
hepatotoxic agent;
immunosuppressive agent;
prodrug
azelaic acid
nonanedioic acid : An alpha,omega-dicarboxylic acid that is heptane substituted at positions 1 and 7 by carboxy groups.		2.4320alpha,omega-dicarboxylic acid;
dicarboxylic fatty acid		antibacterial agent;
antineoplastic agent;
dermatologic drug;
plant metabolite
azelastine
azelastine: azeptin is azelastine hydrochloride; structure; eye drop formulation effective in relieving symptoms of allergic conjunctivitis; do not confuse with 5-loxin which is an extract of Boswellia. azelastine : A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.		2.4220monochlorobenzenes;
phthalazines;
tertiary amino compound		anti-allergic agent;
anti-asthmatic drug;
bronchodilator agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
H1-receptor antagonist;
platelet aggregation inhibitor
baclofen
[no description available]		2.4320amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound		central nervous system depressant;
GABA agonist;
muscle relaxant
bay-k-8644
3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester: A dihydropyridine derivative, which, in contrast to NIFEDIPINE, functions as a calcium channel agonist. The compound facilitates Ca2+ influx through partially activated voltage-dependent Ca2+ channels, thereby causing vasoconstrictor and positive inotropic effects. It is used primarily as a research tool.. Bay-K-8644 : A racemate comprising equimolar amounts of (R)- and (S)-Bay-K-8644. methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylate : A pentasubstituted dihydropyridine carrying methoxycarbonyl, 2-(trifluoromethyl)phenyl and nitro substituents at positions 3, 4 and 5 respectively as well as two methyl substituents at positions 2 and 6.		2.0310(trifluoromethyl)benzenes;
C-nitro compound;
dihydropyridine;
methyl ester
benzamide
benzamide : An aromatic amide that consists of benzene bearing a single carboxamido substituent. The parent of the class of benzamides.		2.0310benzamides
bepridil
Bepridil: A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist.. bepridil : A tertiary amine in which the substituents on nitrogen are benzyl, phenyl and 3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl.		2.7230pyrrolidines;
tertiary amine		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
betaxolol
[no description available]		2.0210propanolamineantihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bicalutamide
bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism.		2.0210(trifluoromethyl)benzenes;
monocarboxylic acid amide;
monofluorobenzenes;
nitrile;
sulfone;
tertiary alcohol
bisoprolol
Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.		2.7330secondary alcohol;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bml 190
indomethacin morpholinylamide: an inverse agonist of the cannabinoid CB2 receptor		2.0310N-acylindole
brimonidine
[no description available]		2.4320imidazoles;
quinoxaline derivative;
secondary amine		adrenergic agonist;
alpha-adrenergic agonist;
antihypertensive agent
bumetanide
[no description available]		2.4320amino acid;
benzoic acids;
sulfonamide		diuretic;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor
bupranolol
Bupranolol: An adrenergic-beta-2 antagonist that has been used for cardiac arrhythmia, angina pectoris, hypertension, glaucoma, and as an antithrombotic.		2.0210aromatic ether
buspirone
Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.		2.0210azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
busulfan
[no description available]		2.0210methanesulfonate esteralkylating agent;
antineoplastic agent;
carcinogenic agent;
insect sterilant;
teratogenic agent
butenafine
butenafine: studied on experimental dermatophytosis. butenafine : Trimethylamine in which hydrogen atoms attached to different methyl groups are substituted by 1-naphthyl and 4-tert-butylphenyl groups. It is an inhibitor of squalene epoxidase, an enzyme responsible for the creation of sterols needed in fungal cell membranes, and is used as its hydrochloride salt for treatment of dermatological fungal infections.		2.0210naphthalenes;
tertiary amine		antifungal drug;
EC 1.14.13.132 (squalene monooxygenase) inhibitor
caffeine
[no description available]		2.0310purine alkaloid;
trimethylxanthine		adenosine A2A receptor antagonist;
adenosine receptor antagonist;
adjuvant;
central nervous system stimulant;
diuretic;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
environmental contaminant;
food additive;
fungal metabolite;
geroprotector;
human blood serum metabolite;
mouse metabolite;
mutagen;
plant metabolite;
psychotropic drug;
ryanodine receptor agonist;
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.		2.4220aromatic ether;
nitrile;
polyether;
tertiary amino compound
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		2.4320dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
carbetapentane
carbetapentane: RN given refers to parent cpd		2.0310benzenes
carisoprodol
Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202). carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.		2.0310carbamate estermuscle relaxant
carmustine
Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.		2.4320N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
carteolol
Carteolol: A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent.		2.0210quinolone;
secondary alcohol		anti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
carvedilol
[no description available]		2.4220carbazoles;
secondary alcohol;
secondary amino compound		alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
cetirizine
Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.		2.0210ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines		anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
cgp 20712a
[no description available]		2.0210imidazoles
cgp 12177
CGP 12177 : A benzimidazole that is benzimidazol-2-one substituted at position 4 by a 3-(tert-butylamino)-2-hydroxypropoxy group.		2.4620aromatic ether;
benzimidazoles;
secondary alcohol;
secondary amino compound		beta-adrenergic antagonist
cgs 12066
4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline : A pyrroloquinoxaline that is pyrrolo[1,2-a]quinoxaline bearing additional 4-methylpiperazin-1-yl and trifluoromethyl substituents at positions 4 and 7 respectively. A 5-hydroxytryptamine receptor 1B (5-HT1B) full agonist, 10-fold selective over 5-HT1A and 1000-fold selective over 5-HT2C receptors. Centrally active following systemic administration.		2.0310N-arylpiperazine;
organofluorine compound;
pyrroloquinoxaline		serotonergic agonist
cgs 15943
9-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine: non-xanthine triazoloquinazoline adenosine antagonist. CGS 15943 : A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors.		2.0310aromatic amine;
biaryl;
furans;
organochlorine compound;
primary amino compound;
quinazolines;
triazoloquinazoline		adenosine A1 receptor antagonist;
adenosine A2A receptor antagonist;
antineoplastic agent;
central nervous system stimulant
chlorambucil
Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.		2.0310aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
chlormezanone
Chlormezanone: A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.. chlormezanone : A 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions.		2.43201,3-thiazine;
lactam;
monochlorobenzenes;
sulfone		antipsychotic agent;
anxiolytic drug;
muscle relaxant
chlorothiazide
Chlorothiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812). thiazide : Heterocyclic compound with sulfur and nitrogen in the ring.. chlorothiazide : 4H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position is substituted by chlorine and that at position 7 is substituted by a sulfonamide group. A diuretic, it is used for treatment of oedema and hypertension.		2.0310benzothiadiazineantihypertensive agent;
diuretic
chlorpropamide
Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification.		2.0310monochlorobenzenes;
N-sulfonylurea		hypoglycemic agent;
insulin secretagogue
chlorzoxazone
Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm.		2.03101,3-benzoxazoles;
heteroaryl hydroxy compound;
organochlorine compound		muscle relaxant;
sedative
ciclopirox
[no description available]		2.0210cyclic hydroxamic acid;
hydroxypyridone antifungal drug;
pyridone		antibacterial agent;
antiseborrheic
cilostamide
cilostamide: selective inhibitor of cyclic AMP phosphodiesterase & platelet aggregation; structure		2.0310quinolines
cilostazol
[no description available]		2.0310lactam;
tetrazoles		anticoagulant;
bronchodilator agent;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
fibrin modulating drug;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent
cimetidine
Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.		2.0310aliphatic sulfide;
guanidines;
imidazoles;
nitrile		adjuvant;
analgesic;
anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
cinoxacin
Cinoxacin: Synthetic antimicrobial related to OXOLINIC ACID and NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.. cinoxacin : A member of the class of cinnolines that is 6,7-methylenedioxycinnolin-4(1H)-one bearing an ethyl group at position 1 and a carboxylic acid group at position 3. An analogue of oxolinic acid, it has similar antibacterial actions. It was formerly used for the treatment of urinary tract infections.		2.4320cinnolines;
oxacycle;
oxo carboxylic acid		antibacterial drug;
antiinfective agent
ciprofibrate
[no description available]		2.0310cyclopropanes;
monocarboxylic acid;
organochlorine compound		antilipemic drug
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.		2.0210aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
cisapride
Cisapride: A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed). cisapride : The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oesophageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere.		2.4420benzamides
clofazimine
Clofazimine: A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619). clofazimine : 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients.		2.4220monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug
clofibrate
angiokapsul: contains clofibrate & insoitolnicotinate		2.0310aromatic ether;
ethyl ester;
monochlorobenzenes		anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist
clomipramine
Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias.		2.0210dibenzoazepineanticoronaviral agent;
antidepressant;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
serotonergic antagonist;
serotonergic drug;
serotonin uptake inhibitor
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		2.0210clonidine;
imidazoline
chlorazepate
clorazepic acid : A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively.		2.02101,4-benzodiazepinoneanticonvulsant;
anxiolytic drug;
GABA modulator;
prodrug
clotrimazole
[no description available]		2.0310conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes		antiinfective agent;
environmental contaminant;
xenobiotic
cx546
1-(1,4-benzodioxan-6-ylcarbonyl)piperidine: structure in first source		2.0310
cyclobenzaprine
cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure. cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm.		2.0210carbotricyclic compoundantidepressant;
muscle relaxant;
tranquilizing drug
cyclothiazide
cyclothiazide: inhibits the desensitization of AMPA-type receptors; structure. cyclothiazide : 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted at positions 3, 5 and 6 by a 2-norbornen-5-yl group, chlorine, and a sulfonamide group, respectively. A thiazide diuretic, it has been used in the management of hypertension and oedema.		2.0310benzothiadiazineantihypertensive agent;
diuretic
dephostatin
dephostatin: from Streptomyces sp. MJ742-NF5; structure given in first source		2.0310
nonivamide
nonivamide: has effect on sensory neurons. nonivamide : A capsaicinoid that is the carboxamide resulting from the formal condensation of the amino group of 4-hydroxy-3-methoxybenzylamine with the carboxy group of nonanoic acid. It is the active ingredient in many pepper sprays.		2.0310capsaicinoid;
phenols		lachrymator
r 59022
R 59022: diacylglycerol kinase inhibitor; structure given in first source; platelet activator factor antagonist		2.0310diarylmethane
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		2.02101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
diazoxide
Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.		2.0310benzothiadiazine;
organochlorine compound;
sulfone		antihypertensive agent;
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
diuretic;
K-ATP channel agonist;
sodium channel blocker;
sympathomimetic agent;
vasodilator agent
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		2.0210amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
pentetic acid
Pentetic Acid: An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium.		2.0310pentacarboxylic acidcopper chelator
diflunisal
Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position.		2.0210monohydroxybenzoic acid;
organofluorine compound		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
diphenyleneiodonium
diphenyleneiodonium: structure in first source; NADPH oxidase inhibitor. dibenziodolium : An organic cation that is fluorene in which the methylene group is replaced by a positively charged iodine.		2.0310organic cation
dipivefrin
dipivefrin: used in treatment of both primary & open angle glaucoma; RN given refers to (+-)-isomer. dipivefrin : The dipivalate ester of (+-)-epinephrine (racepinephrine). A pro-drug of epinephrine, the hydrochloride is used topically as eye drops to reduce intra-ocular pressure in the treatment of open-angle glaucoma or ocular hypertension.		2.0210ethanolamines;
pivalate ester		adrenergic agonist;
antiglaucoma drug;
ophthalmology drug;
prodrug;
sympathomimetic agent
dipyridamole
Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots.		2.4320piperidines;
pyrimidopyrimidine;
tertiary amino compound;
tetrol		adenosine phosphodiesterase inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
disopyramide
Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug.		2.4320monocarboxylic acid amide;
pyridines;
tertiary amino compound		anti-arrhythmia drug
disulfiram
[no description available]		2.4320organic disulfide;
organosulfur acaricide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor
valproic acid
Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.		2.0210branched-chain fatty acid;
branched-chain saturated fatty acid		anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
2-amino-7-phosphonoheptanoic acid
2-amino-7-phosphonoheptanoic acid: (D)-isomer active as an antagonist of N-methyl-D-aspartate excitation of central neurons; (L)-isomer inactive; RN given refers to cpd without isomeric designation		2.0310
thiorphan
Thiorphan: A potent inhibitor of membrane metalloendopeptidase (ENKEPHALINASE). Thiorphan potentiates morphine-induced ANALGESIA and attenuates naloxone-precipitated withdrawal symptoms.		2.0310N-acyl-amino acid
2,3-dimethoxy-1,4-naphthoquinone
2,3-dimethoxynaphthalene-1,4-dione : A naphthoquinone that is 1,4-naphthoquinone bearing two methoxy substituents at positions 2 and 3. Redox-cycling agent that induces intracellular superoxide anion formation and, depending on the concentration, induces cell proliferation, apoptosis or necrosis. Used to study the role of ROS in cell toxicity, apoptosis, and necrosis.		2.03101,4-naphthoquinones
domperidone
Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.		2.0310benzimidazoles;
heteroarylpiperidine		antiemetic;
dopaminergic antagonist
doxazosin
Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure.		2.0210aromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines		alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent
doxepin
Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug.		2.0210dibenzooxepine;
tertiary amino compound		antidepressant
droperidol
Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon.		2.4320aromatic ketone;
benzimidazoles;
organofluorine compound		anaesthesia adjuvant;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic
ebastine
[no description available]		2.0210organic molecular entity
ebselen
ebselen : A benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase.		2.0310benzoselenazoleanti-inflammatory drug;
antibacterial agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
EC 3.5.4.1 (cytosine deaminase) inhibitor;
EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor;
enzyme mimic;
ferroptosis inhibitor;
genotoxin;
hepatoprotective agent;
neuroprotective agent;
radical scavenger
econazole
Econazole: An imidazole derivative that is commonly used as a topical antifungal agent.. econazole : A racemate composed of equimolar amounts of (R)- and (S)-econazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections.. 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 4-chlorobenzyl group.		2.0210dichlorobenzene;
ether;
imidazoles;
monochlorobenzenes
ellipticine
ellipticine : A organic heterotetracyclic compound that is pyrido[4,3-b]carbazole carrying two methyl substituents at positions 5 and 11.		2.0310indole alkaloid;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound;
polycyclic heteroarene		antineoplastic agent;
plant metabolite
emodin
Emodin: Purgative anthraquinone found in several plants, especially RHAMNUS PURSHIANA. It was formerly used as a laxative, but is now used mainly as a tool in toxicity studies.. emodin : A trihydroxyanthraquinone that is 9,10-anthraquinone which is substituted by hydroxy groups at positions 1, 3, and 8 and by a methyl group at position 6. It is present in the roots and barks of numerous plants (particularly rhubarb and buckthorn), moulds, and lichens. It is an active ingredient of various Chinese herbs.		2.0310trihydroxyanthraquinoneantineoplastic agent;
laxative;
plant metabolite;
tyrosine kinase inhibitor
enflurane
Enflurane: An extremely stable inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate.. enflurane : An ether in which the oxygen atom is connected to 2-chloro-1,1,2-trifluoroethyl and difluoromethyl groups.		2.0210ether;
organochlorine compound;
organofluorine compound		anaesthetic
enoxacin
Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.. enoxacin : A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea.		2.02101,8-naphthyridine derivative;
amino acid;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-arylpiperazine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor
estazolam
Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia.		2.0210triazoles;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA modulator
ethosuximide
Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures.		2.0310dicarboximide;
pyrrolidinone		anticonvulsant;
geroprotector;
T-type calcium channel blocker
etidronate
Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces.		2.02101,1-bis(phosphonic acid)antineoplastic agent;
bone density conservation agent;
chelator
etodolac
Etodolac: A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).. etodolac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl moiety. A preferential inhibitor of cyclo-oxygenase 2 and non-steroidal anti-inflammatory, it is used for the treatment of rheumatoid arthritis and osteoarthritis, and for the alleviation of postoperative pain. Administered as the racemate, only the (S)-enantiomer is active.		2.4320monocarboxylic acid;
organic heterotricyclic compound		antipyretic;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
brl 42810
[no description available]		2.02102-aminopurines;
acetate ester		antiviral drug;
prodrug
felbamate
Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.. felbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy.		2.4320carbamate esteranticonvulsant;
neuroprotective agent
felodipine
Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris.		2.4320dichlorobenzene;
dihydropyridine;
ethyl ester;
methyl ester		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
fenfluramine
Fenfluramine: A centrally active drug that apparently both blocks serotonin uptake and provokes transport-mediated serotonin release.. fenfluramine : A secondary amino compound that is 1-phenyl-propan-2-amine in which one of the meta-hydrogens is substituted by trifluoromethyl, and one of the hydrogens attached to the nitrogen is substituted by an ethyl group. It binds to the serotonin reuptake pump, causing inhbition of serotonin uptake and release of serotonin. The resulting increased levels of serotonin lead to greater serotonin receptor activation which in turn lead to enhancement of serotoninergic transmission in the centres of feeding behavior located in the hypothalamus. This suppresses the appetite for carbohydrates. Fenfluramine was used as the hydrochloride for treatment of diabetes and obesity. It was withdrawn worldwide after reports of heart valve disease and pulmonary hypertension.		2.0210(trifluoromethyl)benzenes;
secondary amino compound		appetite depressant;
serotonergic agonist;
serotonin uptake inhibitor
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		2.0310aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
fentanyl
Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.		2.0210anilide;
monocarboxylic acid amide;
piperidines		adjuvant;
anaesthesia adjuvant;
anaesthetic;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
fexofenadine
fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.		2.4420piperidines;
tertiary amine		anti-allergic agent;
H1-receptor antagonist
flecainide
Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		2.0210aromatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines		anti-arrhythmia drug
fluconazole
Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.		2.0210conazole antifungal drug;
difluorobenzene;
tertiary alcohol;
triazole antifungal drug		environmental contaminant;
P450 inhibitor;
xenobiotic
flucytosine
Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.		2.0210aminopyrimidine;
nucleoside analogue;
organofluorine compound;
pyrimidine antifungal drug;
pyrimidone		prodrug
fluphenazine
[no description available]		2.4220N-alkylpiperazine;
organofluorine compound;
phenothiazines		anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug
flumazenil
Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.		2.4320ethyl ester;
imidazobenzodiazepine;
organofluorine compound		antidote to benzodiazepine poisoning;
GABA antagonist
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		2.4320nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
fluoxetine
Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.		3.5720(trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound
fluphenazine depot
fluphenazine decanoate : The prodrug of fluphenazine, an antipsychotic drug used for the symptomatic management of psychosis in patients with schizophrenia.		2.0210decanoate ester;
N-alkylpiperazine;
organofluorine compound;
phenothiazines		dopaminergic antagonist;
phenothiazine antipsychotic drug;
prodrug
fluphenazine enanthate
[no description available]		2.0210phenothiazines
flurbiprofen
Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.		2.0210fluorobiphenyl;
monocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
fluspirilene
Fluspirilene: A long-acting injectable antipsychotic agent used for chronic schizophrenia.		2.0310diarylmethane
flutamide
Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.		2.4320(trifluoromethyl)benzenes;
monocarboxylic acid amide		androgen antagonist;
antineoplastic agent
formoterol fumarate
N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamide : A phenylethanoloamine having 4-hydroxy and 3-formamido substituents on the phenyl ring and an N-(4-methoxyphenyl)propan-2-yl substituent.		5.23180formamides;
phenols;
phenylethanolamines;
secondary alcohol;
secondary amino compound
foscarnet
Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		2.0210carboxylic acid;
one-carbon compound;
phosphonic acids		antiviral drug;
geroprotector;
HIV-1 reverse transcriptase inhibitor;
sodium-dependent Pi-transporter inhibitor
fpl 64176
FPL 64176: an activator of L-type calcium channels; structure given in first source. FPL 64176 : 1H-Pyrrole substituted at C-2 and -5 by methyl groups, at C-3 by methoxycarbonyl and at C-4 by a 2-benzylbenzoyl group.		2.0310carboxylic ester;
pyrroles		calcium channel agonist
furafylline
[no description available]		2.0310oxopurine
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		2.4320chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
fusaric acid
Fusaric Acid: A picolinic acid derivative isolated from various Fusarium species. It has been proposed for a variety of therapeutic applications but is primarily used as a research tool. Its mechanisms of action are poorly understood. It probably inhibits DOPAMINE BETA-HYDROXYLASE, the enzyme that converts dopamine to norepinephrine. It may also have other actions, including the inhibition of cell proliferation and DNA synthesis.		2.0310aromatic carboxylic acid;
pyridines
gabapentin
Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome.		2.4320gamma-amino acidanticonvulsant;
calcium channel blocker;
environmental contaminant;
xenobiotic
4-amino-5-hexynoic acid
4-amino-5-hexynoic acid: structure		2.0310
gemfibrozil
[no description available]		2.0210aromatic etherantilipemic drug
glimepiride
glimepiride: structure given in first source		2.0210sulfonamide
glipizide
Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus.		2.4320aromatic amide;
monocarboxylic acid amide;
N-sulfonylurea;
pyrazines		EC 2.7.1.33 (pantothenate kinase) inhibitor;
hypoglycemic agent;
insulin secretagogue
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		2.7330monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
granisetron
[no description available]		2.0210aromatic amide;
indazoles
guanfacine
Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.		2.0210acetamides
1-(5-isoquinolinesulfonyl)piperazine
[no description available]		2.0310isoquinolines
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		2.4320aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
halothane
[no description available]		2.0210haloalkane;
organobromine compound;
organochlorine compound;
organofluorine compound		inhalation anaesthetic
hemicholinium 3
[no description available]		2.0310morpholines
4-fluorohexahydrosiladifenidol
[no description available]		2.0310
hydrochlorothiazide
Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure.		2.4320benzothiadiazine;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
hydroxychloroquine
Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions.		3.3110aminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug
hydroxyurea
[no description available]		2.4320one-carbon compound;
ureas		antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent
hydroxyzine
Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.		2.0210hydroxyether;
monochlorobenzenes;
N-alkylpiperazine		anticoronaviral agent;
antipruritic drug;
anxiolytic drug;
dermatologic drug;
H1-receptor antagonist
ibudilast
[no description available]		2.0310pyrazolopyridine
ibuprofen
Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine		2.4320monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
ic 261
[no description available]		2.0310indoles
phenelzine
Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC.		2.0210primary amine
ici 118551
[no description available]		2.0210indanes
ifenprodil
ifenprodil: NMDA receptor antagonist		2.0310piperidines
ifosfamide
[no description available]		2.0210ifosfamidesalkylating agent;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
xenobiotic
amrinone
Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure.		2.0210bipyridinesEC 3.1.4.* (phosphoric diester hydrolase) inhibitor
indapamide
Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine.		2.0210indoles;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic
indirubin-3'-monoxime
indirubin-3'-monoxime: has antiangiogenic activity. indirubin-3'-monoxime : A member of the class of biindoles that is indirubin in which the keto group at position 3' has undergone condensation with hydroxylamine to form the corresponding oxime.		2.0310
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		2.4320aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
iodixanol
iodixanol: dimeric contrast media; structure given in first source. iodixanol : A dimeric, non-ionic, water-soluble, radiographic contrast agent, used particularly in coronary angiography.		2.0210organoiodine compoundradioopaque medium
iodoacetamide
[no description available]		2.0310
iohexol
Iohexol: An effective non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Its low systemic toxicity is the combined result of low chemotoxicity and low osmolality.. iohexol : A benzenedicarboxamide compound having N-(2,3-dihydroxypropyl)carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and an N-(2,3-dihydroxypropyl)acetamido group at the 5-position.		2.0210benzenedicarboxamide;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
iopromide
iopromide: structure given in first source. iopromide : A dicarboxylic acid diamide that consists of N-methylisophthalamide bearing three iodo substituents at positions 2, 4 and 6, a methoxyacetyl substituent at position 5 and two 2,3-dihydroxypropyl groups attached to the amide nitrogens. A water soluble x-ray contrast agent for intravascular administration.		2.0210dicarboxylic acid diamide;
organoiodine compound		environmental contaminant;
nephrotoxic agent;
radioopaque medium;
xenobiotic
iodipamide
Iodipamide: A water-soluble radiographic contrast media for cholecystography and intravenous cholangiography.. adipiodone : An organoiodine compound that is 3-amino-2,4,6-triiodobenzoic acid in which one of the amino hydrogens is substituted by a 6-(3-carboxy-2,4,6-triiodoanilino)-6-oxohexanoyl group. It is a water-soluble radiographic contrast media for cholecystography and intravenous cholangiography.		2.0510benzoic acids;
organoiodine compound;
secondary carboxamide		radioopaque medium
ioversol
[no description available]		2.0210amidobenzoic acid
1-methyl-3-isobutylxanthine
1-Methyl-3-isobutylxanthine: A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES. 3-isobutyl-1-methylxanthine : An oxopurine that is xanthine which is substituted at positions 1 and 3 by methyl and isobutyl groups, respectively.		2.03103-isobutyl-1-methylxanthine
isoflurane
Isoflurane: A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.		2.0210organofluorine compoundinhalation anaesthetic
isoniazid
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		2.0210carbohydrazideantitubercular agent;
drug allergen
4-piperidinecarboxylic acid
4-piperidinecarboxylic acid: structure in first source		2.0310
isoproterenol
Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.		3.5980catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
isradipine
Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.		2.0210benzoxadiazole;
dihydropyridine;
isopropyl ester;
methyl ester
itraconazole
[no description available]		2.0210piperazines
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline
WHI P131: a quinazoline derivative, inhibitor of glioblastoma cell adhesion and migration		2.0310
jl 18
JL 18: a pyridobenzodiazepine derivative bioisoster of clozapine		2.0310
nsc 664704
kenpaullone: inhibits CDK1/cyclin B; structure in first source. kenpaullone : An indolobenzazepine that is paullone in which the hydrogen at position 9 is replaced by a bromo substituent. It is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3beta (GSK3beta).		2.0310indolobenzazepine;
lactam;
organobromine compound		cardioprotective agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
geroprotector
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		2.4320dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
ketoprofen
Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.		2.4320benzophenones;
oxo monocarboxylic acid		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
ketorolac
Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed). ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.. 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively.		2.0210amino acid;
aromatic ketone;
monocarboxylic acid;
pyrrolizines;
racemate		analgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
kynurenic acid
Kynurenic Acid: A broad-spectrum excitatory amino acid antagonist used as a research tool.. kynurenic acid : A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4.		2.0310monohydroxyquinoline;
quinolinemonocarboxylic acid		G-protein-coupled receptor agonist;
human metabolite;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist;
Saccharomyces cerevisiae metabolite
2-amino-3-phosphonopropionic acid
2-amino-3-phosphonopropionic acid: metabotropic glutamate receptor antagonist; do not confuse AP-3 used as an abbreviation for this with enhancer-binding protein AP-3 (a trans-activator) or clathrin assembly protein AP-3. 2-amino-3-phosphonopropanoic acid : A non-proteinogenc alpha-amino acid that is alanine in which one of the hydrogens of the terminal methyl group has been replaced by a dihydroxy(oxido)-lambda(5)-phosphanyl group.		2.0310alanine derivative;
non-proteinogenic alpha-amino acid;
phosphonic acids		human metabolite;
metabotropic glutamate receptor antagonist
labetalol
Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5.		2.4220benzamides;
benzenes;
phenols;
primary carboxamide;
salicylamides;
secondary alcohol;
secondary amino compound
lamotrigine
[no description available]		2.43201,2,4-triazines;
dichlorobenzene;
primary arylamine		anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
lansoprazole
Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.		2.4320benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
beta-lapachone
beta-lapachone: antineoplastic inhibitor of reverse transcriptase, DNA topoisomerase, and DNA polymerase. beta-lapachone : A benzochromenone that is 3,4-dihydro-2H-benzo[h]chromene-5,6-dione substituted by geminal methyl groups at position 2. Isolated from Tabebuia avellanedae, it exhibits antineoplastic and anti-inflammatory activities.		2.0310benzochromenone;
orthoquinones		anti-inflammatory agent;
antineoplastic agent;
plant metabolite
leflunomide
Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide.		2.0310(trifluoromethyl)benzenes;
isoxazoles;
monocarboxylic acid amide		antineoplastic agent;
antiparasitic agent;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
hepatotoxic agent;
immunosuppressive agent;
non-steroidal anti-inflammatory drug;
prodrug;
pyrimidine synthesis inhibitor;
tyrosine kinase inhibitor
linopirdine
linopirdine: acetylcholine releasing drug		2.0310indoles
lomefloxacin
lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.		2.0210fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antimicrobial agent;
antitubercular agent;
photosensitizing agent
loperamide
Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.		2.0210monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol		anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
loratadine
Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.		2.4320benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		2.0210biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
loxapine
Loxapine: An antipsychotic agent used in SCHIZOPHRENIA.		2.0210dibenzooxazepineantipsychotic agent;
dopaminergic antagonist
loxoprofen
loxoprofen: RN given refers to parent cpd without isomeric designation; structure in first source. loxoprofen : A monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-[(2-oxocyclopentyl)methyl]phenyl group. A prodrug that is rapidly converted into its active trans-alcohol metabolite following oral administration.		2.0310cyclopentanones;
monocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		2.0310chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
maprotiline
Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.		2.0210anthracenes
mebendazole
Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5.		2.0210aromatic ketone;
benzimidazoles;
carbamate ester		antinematodal drug;
microtubule-destabilising agent;
tubulin modulator
meclofenamic acid
Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.		2.0210aminobenzoic acid;
organochlorine compound;
secondary amino compound		analgesic;
anticonvulsant;
antineoplastic agent;
antipyretic;
antirheumatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
meclofenamate sodium anhydrous
[no description available]		2.0310organic sodium salt
mefenamic acid
Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.		2.0210aminobenzoic acid;
secondary amino compound		analgesic;
antipyretic;
antirheumatic drug;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
mefloquine hydrochloride
[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4.		2.0210organofluorine compound;
piperidines;
quinolines;
secondary alcohol
mesalamine
Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position.		2.0210amino acid;
aromatic amine;
monocarboxylic acid;
monohydroxybenzoic acid;
phenols		non-steroidal anti-inflammatory drug
metformin
Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.		2.0210guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
methiothepin
Methiothepin: A serotonin receptor antagonist in the CENTRAL NERVOUS SYSTEM used as an antipsychotic.. methiothepin : A dibenzothiepine that is 10,11-dihydrodibenzo[b,f]thiepine bearing additional methylthio and 4-methylpiperazin-1-yl substituents at positions 8 and 10 respectively. Potent 5-HT2 antagonist, also active as 5-HT1 antagonist. Differentiates 5-HT1D sub-types. Also displays affinity for rodent 5-HT5B, 5-HT5A, 5-HT7 and 5-HT6 receptors (pK1 values are 6.6, 7.0, 8.4 and 8.7 respectively).		2.0310aryl sulfide;
dibenzothiepine;
N-alkylpiperazine;
tertiary amino compound		antipsychotic agent;
dopaminergic antagonist;
geroprotector;
serotonergic antagonist
methoctramine
[no description available]		2.0310aromatic ether;
tetramine		muscarinic antagonist
nocodazole
[no description available]		2.0310aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes		antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
3-Hydroxy-alpha-methyl-DL-tyrosine
[no description available]		2.0310benzenes;
monocarboxylic acid
metoclopramide
Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.		2.0210benzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound		antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic
metolazone
Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics.		2.0310organochlorine compound;
quinazolines;
sulfonamide		antihypertensive agent;
diuretic;
ion transport inhibitor
metoprolol
Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.		2.7330aromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound		antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic
metronidazole
Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.		2.0210C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic
mexiletine
Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol.		2.0210aromatic ether;
primary amino compound		anti-arrhythmia drug
midazolam
Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.		2.0210imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
midodrine
Midodrine: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.. midodrine : An aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine.		2.0210amino acid amide;
aromatic ether;
secondary alcohol		alpha-adrenergic agonist;
prodrug;
sympathomimetic agent;
vasoconstrictor agent
milrinone
[no description available]		2.0310bipyridines;
nitrile;
pyridone		cardiotonic drug;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
minoxidil
Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6.		2.4320dialkylarylamine;
tertiary amino compound
mirtazapine
Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders.		2.0210benzazepine;
tetracyclic antidepressant		alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
oneirogen;
serotonergic antagonist
mitotane
Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.		2.0310diarylmethane
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		2.4320dihydroxyanthraquinoneanalgesic;
antineoplastic agent
ml 7
ML-7 : An N-sulfonyldiazepane resullting from the formal condensation of 5-iodo-1-naphthylsulfonic acid with one of the nitrogens of 1,4-diazepane. It is a selective inhibitor of myosin light chain kinase (EC 2.7.11.18).		2.0310N-sulfonyldiazepane;
organoiodine compound		EC 2.7.11.18 (myosin-light-chain kinase) inhibitor
n-(4-aminobutyl)-5-chloro-2-naphthalenesulfonamide
N-(4-aminobutyl)-5-chloro-2-naphthalenesulfonamide: calmodulin antagonist; structure given in first source. N-(4-aminobutyl)-5-chloronaphthalene-2-sulfonamide : A sulfonamide that is 5-chloronaphthalene-2-sulfonamide in which one of the hydrogens of the nitrogen atom is substituted by a 4-aminobutyl group.		2.0310naphthalenes;
organochlorine compound;
primary amino compound;
sulfonamide
n-bromoacetamide
[no description available]		2.0310
ethylmaleimide
Ethylmaleimide: A sulfhydryl reagent that is widely used in experimental biochemical studies.		2.0310maleimidesanticoronaviral agent;
EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor;
EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor;
EC 2.7.1.1 (hexokinase) inhibitor
fg 7142
FG 7142: benzodiazepine receptor agonist		2.0310beta-carbolines
fenamic acid
fenamic acid: has chloride and potassium channel-blocking activity; RN given refers to parent cpd. fenamic acid : An aminobenzoic acid that is the N-phenyl derivative of anthranilic acid. It acts as a parent skeleton for the synthesis of several non-steroidal anti-inflammatory drugs.		2.0310aminobenzoic acid;
secondary amino compound		membrane transport modulator
n 0840
N(6)-cyclopentyl-9-methyladenine: selective, orally active A(1) adenosine receptor antagonist		2.0310
nabumetone
Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs.		2.0210methoxynaphthalene;
methyl ketone		cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
nadolol
[no description available]		2.1310tetralins
nefazodone
nefazodone: may be useful as an opiate adjunct		2.4220aromatic ether;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazoles		alpha-adrenergic antagonist;
analgesic;
antidepressant;
serotonergic antagonist;
serotonin uptake inhibitor
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		2.0210cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nialamide
Nialamide: An MAO inhibitor that is used as an antidepressive agent.		2.0310organonitrogen compound;
organooxygen compound
nicardipine
Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively.		2.0210benzenes;
C-nitro compound;
diester;
dihydropyridine;
methyl ester;
tertiary amino compound
niclosamide
Niclosamide: An antihelmintic that is active against most tapeworms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p48). niclosamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-chlorosalicylic acid with the amino group of 2-chloro-4-nitroaniline. It is an oral anthelmintic drug approved for use against tapeworm infections.		3.5920benzamides;
C-nitro compound;
monochlorobenzenes;
salicylanilides;
secondary carboxamide		anthelminthic drug;
anticoronaviral agent;
antiparasitic agent;
apoptosis inducer;
molluscicide;
piscicide;
STAT3 inhibitor
nifedipine
Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.		2.4320C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
niflumic acid
Niflumic Acid: An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.		2.0310aromatic carboxylic acid;
pyridines
nilutamide
[no description available]		2.4320(trifluoromethyl)benzenes;
C-nitro compound;
imidazolidinone		androgen antagonist;
antineoplastic agent
nimesulide
nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.		2.0310aromatic ether;
C-nitro compound;
sulfonamide		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
nimodipine
Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm.		2.43202-methoxyethyl ester;
C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
isopropyl ester		antihypertensive agent;
calcium channel blocker;
cardiovascular drug;
vasodilator agent
nipecotic acid
nipecotic acid: RN given refers to cpd without isomeric designation. nipecotic acid : A piperidinemonocarboxylic acid that is piperidine in which one of the hydrogens at position 3 is substituted by a carboxylic acid group.		2.0310beta-amino acid;
piperidinemonocarboxylic acid
nisoldipine
Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris.		2.0210C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
methyl ester
nitrendipine
Nitrendipine: A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.. nitrendipine : A dihydropyridine that is 1,4-dihydropyridine substituted by methyl groups at positions 2 and 6, a 3-nitrophenyl group at position 4, a ethoxycarbonyl group at position 3 and a methoxycarbonyl group at position 5. It is a calcium-channel blocker used in the treatment of hypertension.		2.0310C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
ethyl ester;
methyl ester		antihypertensive agent;
calcium channel blocker;
geroprotector;
vasodilator agent
nizatidine
[no description available]		2.02101,3-thiazoles;
C-nitro compound;
carboxamidine;
organic sulfide;
tertiary amino compound		anti-ulcer drug;
cholinergic drug;
H2-receptor antagonist
masoprocol
nordihydroguaretic acid: antioxidant compound found in the creosote bush (Larrea tridentata)		2.4320catechols;
lignan;
tetrol		antioxidant;
ferroptosis inhibitor;
geroprotector;
plant metabolite
norfloxacin
Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase.		2.0210fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug;
DNA synthesis inhibitor;
environmental contaminant;
xenobiotic
nortriptyline
Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline.		2.0210organic tricyclic compound;
secondary amine		adrenergic uptake inhibitor;
analgesic;
antidepressant;
antineoplastic agent;
apoptosis inducer;
drug metabolite
5-nitro-2-(3-phenylpropylamino)benzoic acid
5-nitro-2-(3-phenylpropylamino)benzoic acid: structure given in first source; chloride channel antagonist		2.0310nitrobenzoic acid
ns 2028
NS 2028: structure in first source		2.0310
ns 1619
NS 1619: structure given in first source. NS 1619 : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which the hydrogens at positions 1 and 5 are replaced are replaced by 2-hydroxy-5-(trifluoromethyl)phenyl and trifluoromethyl groups, respectively. It is an opener/activator of the large-conductance calcium-activated potassium channel (Bkca).		2.0310(trifluoromethyl)benzenes;
benzimidazoles;
phenols		potassium channel opener
o(6)-benzylguanine
O(6)-benzylguanine: a suicide inhibitor of O(6)-methylguanine-DNA methyltransferase activity		2.0310
ofloxacin
Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.		2.43203-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
olomoucine
olomoucine: inhibits protein P34CDC2. olomoucine : A 9H-purine that is substituted by a (2-hydroxyethyl)nitrilo, benzylnitrilo and a methyl group at positions 2,6 and 9, respectively. It is a cyclin-dependent kinase inhibitor.		2.03102,6-diaminopurines;
ethanolamines		EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
omeprazole
Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.		2.0210aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
ondansetron
Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.		2.0210carbazoles
oxaprozin
Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis.		2.43201,3-oxazoles;
monocarboxylic acid		analgesic;
non-steroidal anti-inflammatory drug
oxatomide
oxatomide: structure; an anti-allergic & an anti-asthmatic. oxatomide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one substituted by a 3-[4-(diphenylmethyl)piperazin-1-yl]propyl group at position 1. It is an anti-allergic drug.		2.0310benzimidazoles;
diarylmethane;
N-alkylpiperazine		anti-allergic agent;
anti-inflammatory agent;
geroprotector;
H1-receptor antagonist;
serotonergic antagonist
oxiracetam
oxiracetam: structure in first source		2.0310organonitrogen compound;
organooxygen compound
oxolinic acid
quinolone antibiotic : An organonitrogen heterocyclic antibiotic whose structure contains a quinolone or quinolone-related skeleton.		2.0310aromatic carboxylic acid;
organic heterotricyclic compound;
oxacycle;
quinolinemonocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antifungal agent;
antiinfective agent;
antimicrobial agent;
enzyme inhibitor
benoxinate
benoxinate: RN given refers to parent cpd; structure. oxybuprocaine : A benzoate ester in which 4-amino-3-butoxybenzoic acid and 2-(diethylamino)ethanol have combined to form the ester bond; an ester-based local anaesthetic (ester "caine") used especially in ophthalmology and otolaryngology.		2.0210amino acid ester;
benzoate ester;
substituted aniline;
tertiary amino compound		drug allergen;
local anaesthetic;
topical anaesthetic
oxybutynin
oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder.		2.0210acetylenic compound;
carboxylic ester;
racemate;
tertiary alcohol;
tertiary amino compound		antispasmodic drug;
calcium channel blocker;
local anaesthetic;
muscarinic antagonist;
muscle relaxant;
parasympatholytic
quinone
benzoquinone : The simplest members of the class of benzoquinones, consisting of cyclohexadiene which is substituted by two oxo groups.. 1,4-benzoquinone : The simplest member of the class of 1,4-benzoquinones, obtained by the formal oxidation of hydroquinone to the corresponding diketone. It is a metabolite of benzene.. quinone : Compounds having a fully conjugated cyclic dione structure, such as that of benzoquinones, derived from aromatic compounds by conversion of an even number of -CH= groups into -C(=O)- groups with any necessary rearrangement of double bonds (polycyclic and heterocyclic analogues are included).		2.03101,4-benzoquinonescofactor;
human xenobiotic metabolite;
mouse metabolite
fenclonine
Fenclonine: A selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine acts pharmacologically to deplete endogenous levels of serotonin.		2.0310phenylalanine derivative
palmidrol
palmidrol: a cannabinoid receptor-inactive eCB-related molecule used as prophylactic in helping to prevent respiratory viral infection. palmitoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of palmitic (hexadecanoic) acid.		2.0310endocannabinoid;
N-(long-chain-acyl)ethanolamine;
N-(saturated fatty acyl)ethanolamine		anti-inflammatory drug;
anticonvulsant;
antihypertensive agent;
neuroprotective agent
pamidronate
[no description available]		2.0210phosphonoacetic acid
1,7-dimethylxanthine
1,7-dimethylxanthine : A dimethylxanthine having the two methyl groups located at positions 1 and 7. It is a metabolite of caffeine and theobromine in animals.		2.0310dimethylxanthinecentral nervous system stimulant;
human blood serum metabolite;
human xenobiotic metabolite;
mouse metabolite
pd 98059
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.		2.0310aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
pemoline
Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity.		2.02101,3-oxazolescentral nervous system stimulant
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		2.4320aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
pentoxifylline
[no description available]		2.4320oxopurine
perphenazine
Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.		2.4320N-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
organochlorine compound;
phenothiazines		antiemetic;
dopaminergic antagonist;
phenothiazine antipsychotic drug
phenyl biguanide
phenyl biguanide: RN given refers to parent cpd. phenyl biguanide : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a phenyl group.		2.0310guanidinescentral nervous system drug
phenylbutazone
Phenylbutazone: A butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ANKYLOSING SPONDYLITIS; RHEUMATOID ARTHRITIS; and REACTIVE ARTHRITIS.. phenylbutazone : A member of the class of pyrazolidines that is 1,2-diphenylpyrazolidine-3,5-dione carrying a butyl group at the 4-position.		2.0310pyrazolidinesantirheumatic drug;
EC 1.1.1.184 [carbonyl reductase (NADPH)] inhibitor;
metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug
phloretin
[no description available]		2.0310dihydrochalconesantineoplastic agent;
plant metabolite
picotamide
picotamide: has anticoagulant & fibrinolytic properties; structure		2.0310benzamides
pinacidil
Pinacidil: A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)		2.0310pyridines
pindolol
Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.		2.4320indoles;
secondary amine		antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
serotonergic antagonist;
vasodilator agent
piperidine-4-sulfonic acid
piperidine-4-sulfonic acid: specific GABA agonist		2.0310
piracetam
Piracetam: A compound suggested to be both a nootropic and a neuroprotective agent.		2.0310organonitrogen compound;
organooxygen compound
pirbuterol
pirbuterol: structure		2.0210pyridines
pirenperone
[no description available]		2.0310aromatic ketone
practolol
Practolol: A beta-1 adrenergic antagonist that has been used in the emergency treatment of CARDIAC ARRYTHMIAS.. practolol : N-(4-Hydroxyphenyl)acetamide in which the hydrogen of the phenolic hydroxy group is substituted by a 3-(isopropylaminoamino)-2-hydroxypropyl group. A selective beta blocker, it has been used in the emergency treatment of cardiac arrhythmias.		2.0210acetamides;
ethanolamines;
propanolamine;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug;
beta-adrenergic antagonist
prazepam
Prazepam: A benzodiazepine that is used in the treatment of ANXIETY DISORDERS.		2.0210benzodiazepine
praziquantel
azinox: Russian drug		2.4320isoquinolines
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		2.0210aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
primidone
Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures.		2.4320pyrimidoneanticonvulsant;
environmental contaminant;
xenobiotic
probenecid
Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.		2.0210benzoic acids;
sulfonamide		uricosuric drug
procainamide
Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias.		2.0210benzamidesanti-arrhythmia drug;
platelet aggregation inhibitor;
sodium channel blocker
procarbazine
Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		2.0210benzamides;
hydrazines		antineoplastic agent
procaterol
Procaterol: A long-acting beta-2-adrenergic receptor agonist.		3.420quinolines
prochlorperazine
Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.		3.3110N-alkylpiperazine;
N-methylpiperazine;
organochlorine compound;
phenothiazines		alpha-adrenergic antagonist;
antiemetic;
cholinergic antagonist;
dopamine receptor D2 antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic
proglumide
Proglumide: A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.. proglumide : A racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for treatment of stomach ulcers, but has been replaced by newer drugs.. N(2)-benzoyl-N,N-dipropyl-alpha-glutamine : A dicarboxylic acid monoamide obtained by formal condensation of the alpha-carboxy group of N-benzoylglutamic acid with dippropylamine.		2.0310benzamides;
dicarboxylic acid monoamide;
glutamine derivative;
racemate		anti-ulcer drug;
cholecystokinin antagonist;
cholinergic antagonist;
delta-opioid receptor agonist;
drug metabolite;
gastrointestinal drug;
opioid analgesic;
xenobiotic metabolite
pronethalol
pronethalol: was heading 1964-94 (Prov 1964-66); NAPHTHYLISOPROTERENOL was see PRONETHALOL 1977-94; use ETHANOLAMINES to search PRONETHALOL 1966-94		2.0210naphthalenes
propafenone
Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.		2.4420aromatic ketone;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug
propentofylline
[no description available]		2.0310oxopurine
propofol
Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group.		2.4320phenolsanticonvulsant;
antiemetic;
intravenous anaesthetic;
radical scavenger;
sedative
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		2.4620naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
sch 16134
quazepam: structure given in first source		2.0210benzodiazepine
ranitidine
[no description available]		2.0210aralkylamine
pf 5901
alpha-pentyl-3-(2-quinolinylmethoxy)benzenemethanol: structure given in first source; platelet activating factor antagonist		2.0310quinolines
riluzole
Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.		2.4320benzothiazoles
rimantadine
Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza.		2.0210alkylamine
risperidone
Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.		2.43201,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
ritanserin
Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.. ritanserin : A thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.		2.4320organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone: Inhibitor of phosphodiesterases.		2.0310methoxybenzenes
rolipram
[no description available]		2.0310pyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
sb 202190
4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole: structure given in first source; inhibits p38 MAP kinase		2.0310imidazoles;
organofluorine compound;
phenols;
pyridines		apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
sevoflurane
Sevoflurane: A non-explosive inhalation anesthetic used in the induction and maintenance of general anesthesia. It does not cause respiratory irritation and may also prevent PLATELET AGGREGATION.. sevoflurane : An ether compound having fluoromethyl and 1,1,1,3,3,3-hexafluoroisopropyl as the two alkyl groups.		2.0210ether;
organofluorine compound		central nervous system depressant;
inhalation anaesthetic;
platelet aggregation inhibitor
sulfadiazine
Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines.		2.0210pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
antimicrobial agent;
antiprotozoal drug;
coccidiostat;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
sobuzoxane
sobuzoxane: used in treatment of leukemia L1210		2.0310organic molecular entity
sotalol
Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.		2.4220ethanolamines;
secondary alcohol;
secondary amino compound;
sulfonamide		anti-arrhythmia drug;
beta-adrenergic antagonist;
environmental contaminant;
xenobiotic
spiroxatrine
spiroxatrine: structure		2.0310imidazolidines
sq 22536
9-(tetrahydrofuryl)adenine : A nucleoside analogue that is adenine in which the nitrogen at position 9 has been substituted by a tetrahydrofuran-2-yl group. It is an adenylate cyclase inhibitor.		2.0310nucleoside analogue;
oxolanes		EC 4.6.1.1 (adenylate cyclase) inhibitor
sulconazole
sulconazole: RN given refers to cpd with unspecified isomeric designation; structure given in first source. sulconazole : A racemate comprising equimolar amounts of (R)- and (S)-sulconazole. An antifungal agent with activity against Candida species, it is used (generally as the nitrate salt) for the topical treatment of fungal skin infections.. 1-{2-[(4-chlorobenzyl)sulfanyl]-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole : A member of the class of imidazoles that is 1-ethyl-1H-imidazole in which one of the hydrogens of the methyl group is replaced by a (4-chlorobenzyl)sulfanediyl group while a second is replaced by a 2,4-dichlorophenyl group.		2.0210dichlorobenzene;
imidazoles;
monochlorobenzenes;
organic sulfide
sulfaphenazole
Sulfaphenazole: A sulfonilamide anti-infective agent.. sulfaphenazole : A sulfonamide that is sulfanilamide in which the sulfonamide nitrogen is substituted by a 1-phenyl-1H-pyrazol-5-yl group. It is a selective inhibitor of cytochrome P450 (CYP) 2C9 isozyme, and antibacterial agent.		2.0310primary amino compound;
pyrazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor;
P450 inhibitor
sulfasalazine
Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.		2.0210
sulpiride
Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed). sulpiride : A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine.		2.0310benzamides;
N-alkylpyrrolidine;
sulfonamide		antidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
sumatriptan
Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.		2.0210sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
suprofen
Suprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.. suprofen : An aromatic ketone that is thiophene substituted at C-2 by a 4-(1-carboxyethyl)benzoyl group.		2.0210aromatic ketone;
monocarboxylic acid;
thiophenes		antirheumatic drug;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug
t0156
[no description available]		2.0310naphthyridine derivative
tazarotene
tazarotene: a topical acetylenic retinoid; a topical kerytolytic. tazarotene : The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.		2.0210acetylenic compound;
ethyl ester;
pyridines;
retinoid;
thiochromane		keratolytic drug;
prodrug;
teratogenic agent
1,4-bis(2-(3,5-dichloropyridyloxy))benzene
1,4-bis(2-(3,5-dichloropyridyloxy))benzene: potent phenobarbital-like inducer of microsomal monooxygenase activity; structure given in first source		2.0310
temazepam
Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent.		2.0210benzodiazepine
terazosin
Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia		2.0210furans;
piperazines;
primary amino compound;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
terbutaline
Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.		2.4420phenylethanolamines;
resorcinols		anti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
hypoglycemic agent;
sympathomimetic agent;
tocolytic agent
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		2.9540diarylmethane
tetraisopropylpyrophosphamide
Tetraisopropylpyrophosphamide: N,N',N'',N'''-Tetraisopropylpyrophosphamide. A specific inhibitor of pseudocholinesterases. It is commonly used experimentally to determine whether pseudo- or acetylcholinesterases are involved in an enzymatic process.		2.0310phosphoramide
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.		2.0310phthalimides;
piperidones
theobromine
Theobromine: 3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9). theobromine : A dimethylxanthine having the two methyl groups located at positions 3 and 7. A purine alkaloid derived from the cacao plant, it is found in chocolate, as well as in a number of other foods, and is a vasodilator, diuretic and heart stimulator.		2.0310dimethylxanthineadenosine receptor antagonist;
bronchodilator agent;
food component;
human blood serum metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
thiethylperazine
Thiethylperazine: A dopamine antagonist that is particularly useful in treating the nausea and vomiting associated with anesthesia, mildly emetic cancer chemotherapy agents, radiation therapy, and toxins. This piperazine phenothiazine does not prevent vertigo or motion sickness. (From AMA Drug Evaluations Annual, 1994, p457). thiethylperazine : A member of the class of phenothiazines that is perazine substituted by a ethylsulfanyl group at position 2.		2.0210N-methylpiperazine;
phenothiazines		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
phenothiazine antipsychotic drug;
serotonergic antagonist
thioridazine
Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.		2.4220phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
thiotepa
Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed).		2.0210aziridines
ticlopidine
Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.		2.0210monochlorobenzenes;
thienopyridine		anticoagulant;
fibrin modulating drug;
hematologic agent;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
tioconazole
tioconazole : A racemate comprising equimolar amounts of (R)- and (S)-tioconazole.. 1-{2-[(2-chloro-3-thienyl)methoxy]-2-(2,4-dichlorophenyl)ethyl}imidazole : A member of the class of imidazoles that comprises 2-(2,4-dichlorophenyl)ethylimidazole carrying an additional (2-chloro-3-thienyl)methoxy substituent at position 2.		2.0210dichlorobenzene;
ether;
imidazoles;
thiophenes
tiopronin
Tiopronin: Sulfhydryl acylated derivative of GLYCINE.		2.0210N-acyl-amino acid
tizanidine
tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites.		2.0210benzothiadiazole;
imidazoles		alpha-adrenergic agonist;
muscle relaxant
8-(n,n-diethylamino)octyl-3,4,5-trimethoxybenzoate
8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate: intracellular calcium antagonist; RN given refers to parent cpd		2.0310trihydroxybenzoic acid
tolazamide
Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.. tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus.		2.0310N-sulfonylureahypoglycemic agent;
potassium channel blocker
tolbutamide
Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.		2.0310N-sulfonylureahuman metabolite;
hypoglycemic agent;
insulin secretagogue;
potassium channel blocker
(1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid
(1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid: a GABA-C receptor antagonist; structure in first source		2.0310
ici 136,753
[no description available]		2.0310pyrazolopyridine
ultram
2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively.		2.0210aromatic ether;
tertiary alcohol;
tertiary amino compound
trazodone
Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.		2.0210monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazolopyridine		adrenergic antagonist;
antidepressant;
anxiolytic drug;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
triamterene
Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema.		2.0310pteridinesdiuretic;
sodium channel blocker
triazolam
Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries.		2.0210triazolobenzodiazepinesedative
trientine
Trientine: An ethylenediamine derivative used as stabilizer for EPOXY RESINS, as ampholyte for ISOELECTRIC FOCUSING and as chelating agent for copper in HEPATOLENTICULAR DEGENERATION.. TETA : An azamacrocyle in which four nitrogen atoms at positions 1, 4, 8 and 11 of a fouteen-membered ring are each substituted with a carboxymethyl group.. 2,2,2-tetramine : A polyazaalkane that is decane in which the carbon atoms at positions 1, 4, 7 and 10 are replaced by nitrogens.		2.0210polyazaalkane;
tetramine		copper chelator
trifluoperazine
[no description available]		2.0210N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines		antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug
trimebutine
Trimebutine: Proposed spasmolytic with possible local anesthetic action used in gastrointestinal disorders.		2.0210trihydroxybenzoic acid
trimethadione
Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent.		2.0210oxazolidinoneanticonvulsant;
geroprotector
trimethoprim
Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.		2.0310aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
trimetrexate
Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.		2.0210
trimipramine
Trimipramine: Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties.. trimipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant.		2.0210dibenzoazepine;
tertiary amino compound		antidepressant;
environmental contaminant;
xenobiotic
tropicamide
Tropicamide: One of the MUSCARINIC ANTAGONISTS with pharmacologic action similar to ATROPINE and used mainly as an ophthalmic parasympatholytic or mydriatic.		2.0310acetamides
tyrphostin a9
[no description available]		2.0310alkylbenzenegeroprotector
venlafaxine
venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.		2.0210cyclohexanols;
monomethoxybenzene;
tertiary alcohol;
tertiary amino compound		adrenergic uptake inhibitor;
analgesic;
antidepressant;
dopamine uptake inhibitor;
environmental contaminant;
serotonin uptake inhibitor;
xenobiotic
vigabatrin
[no description available]		2.0310gamma-amino acidanticonvulsant;
EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine: adenosine receptor antagonist		2.0310
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole: antineoplastic; activates platelet guanylate cyclase; a radiosensitizing agent and guanylate cyclase activator; structure in first source. lificiguat : A member of the class of indazoles that is 1H-indazole which is substituted by a benzyl group at position 1 and a 5-(hydroxymethyl)-2-furyl group at position 3. It is an activator of soluble guanylate cyclase and inhibits platelet aggregation.		2.0310aromatic primary alcohol;
furans;
indazoles		antineoplastic agent;
apoptosis inducer;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent
ici 204,219
zafirlukast: a leukotriene D4 receptor antagonist		2.0210carbamate ester;
indoles;
N-sulfonylcarboxamide		anti-asthmatic agent;
leukotriene antagonist
zardaverine
zardaverine: structure given in first source. zardaverine : A pyridazinone derivative in which pyridazin-3(2H)-one is substituted at C-6 with a 4-(difluoromethoxy)-3-methoxyphenyl group. It is a phosphodiesterase inhibitor, selective for PDE3 and 4.		2.0310organofluorine compound;
pyridazinone		anti-asthmatic drug;
bronchodilator agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
peripheral nervous system drug
zolpidem
Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.		2.0210imidazopyridinecentral nervous system depressant;
GABA agonist;
sedative
zomepirac
zomepirac: RN given refers to parent cpd; structure		2.0210aromatic ketone;
monocarboxylic acid;
monochlorobenzenes;
pyrroles		cardiovascular drug;
non-steroidal anti-inflammatory drug
cortisone acetate
Cortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders.		2.0310corticosteroid hormone
corticosterone
[no description available]		2.031011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone		human metabolite;
mouse metabolite
reserpine
Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.		2.0310alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
floxuridine
Floxuridine: An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.. floxuridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.		2.0210nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
radiosensitizing agent
procaine hydrochloride
Gerovital H3: Contains mainly procaine & small amounts of benzoic acid, potassium metabisulfite & disodium phosphate		2.0310organic molecular entity
isoproterenol hydrochloride
[no description available]		2.4920catechols
histamine dihydrochloride
Ceplene: Tradename for histamine dihydrochloride.		2.0310
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		2.0310ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
spironolactone
Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.		2.43203-oxo-Delta(4) steroid;
oxaspiro compound;
steroid lactone;
thioester		aldosterone antagonist;
antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
penicillamine
Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group.		2.0210non-proteinogenic alpha-amino acid;
penicillamine		antirheumatic drug;
chelator;
copper chelator;
drug allergen
prednisone
Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.		2.021011-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
estrone
Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.		2.031017-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols		antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
androsterone
[no description available]		2.031017-oxo steroid;
3alpha-hydroxy steroid;
androstanoid;
C19-steroid		androgen;
anticonvulsant;
human blood serum metabolite;
human metabolite;
human urinary metabolite;
mouse metabolite;
pheromone
promazine hydrochloride
[no description available]		2.0310hydrochloride
pilocarpine hydrochloride
pilocarpine hydrochloride : The hydrochloride salt of (+)-pilocarpine, a medication used to treat increased pressure inside the eye and dry mouth.		2.0310hydrochloride
pilocarpine
Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.		2.0210pilocarpineantiglaucoma drug
dimethylphenylpiperazinium iodide
Dimethylphenylpiperazinium Iodide: A selective nicotinic cholinergic agonist used as a research tool. DMPP activates nicotinic receptors in autonomic ganglia but has little effect at the neuromuscular junction.		2.0310N-arylpiperazine;
organic iodide salt;
piperazinium salt;
quaternary ammonium salt		nicotinic acetylcholine receptor agonist
pentylenetetrazole
Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis.		2.0310organic heterobicyclic compound;
organonitrogen heterocyclic compound
racepinephrine hydrochloride
[no description available]		2.0310
(4-(m-chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride
(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride: A drug that selectively activates certain subclasses of muscarinic receptors and also activates postganglionic nicotinic receptors. It is commonly used experimentally to distinguish muscarinic receptor subtypes.		2.0310
hexamethonium bromide
[no description available]		2.0310
cystamine dihydrochloride
[no description available]		2.0310
cantharidin
Cantharidin: A toxic compound, isolated from the Spanish fly or blistering beetle (Lytta (Cantharis) vesicatoria) and other insects. It is a potent and specific inhibitor of protein phosphatases 1 (PP1) and 2A (PP2A). This compound can produce severe skin inflammation, and is extremely toxic if ingested orally.. cantharidin : A monoterpenoid with an epoxy-bridged cyclic dicarboxylic anhydride structure secreted by many species of blister beetle, and most notably by the Spanish fly, Lytta vesicatoria. Natural toxin inhibitor of protein phosphatases 1 and 2A.		2.0310cyclic dicarboxylic anhydride;
monoterpenoid		EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
herbicide
tetraethylammonium chloride
tetraethylammonium chloride : A quarternary ammonium chloride salt in which the cation has four ethyl substituents around the central nitrogen.		2.0310organic chloride salt;
quaternary ammonium salt		potassium channel blocker
aspartic acid
Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.. aspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent. L-aspartic acid : The L-enantiomer of aspartic acid.		2.0310aspartate family amino acid;
aspartic acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
mouse metabolite;
neurotransmitter
glutamine
Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.		2.0310amino acid zwitterion;
glutamine family amino acid;
glutamine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
Escherichia coli metabolite;
human metabolite;
metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
vincristine
[no description available]		2.4320acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
physostigmine
Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.		2.0310carbamate ester;
indole alkaloid		antidote to curare poisoning;
EC 3.1.1.8 (cholinesterase) inhibitor;
miotic
testosterone propionate
Testosterone Propionate: An ester of TESTOSTERONE with a propionate substitution at the 17-beta position.. androgen : A sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors.		2.0210steroid ester
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		2.0310aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
promethazine hydrochloride
[no description available]		2.0310hydrochlorideanti-allergic agent;
anticoronaviral agent;
antiemetic;
antipruritic drug;
geroprotector;
H1-receptor antagonist;
local anaesthetic;
sedative
bromodeoxyuridine
Bromodeoxyuridine: A nucleoside that substitutes for thymidine in DNA and thus acts as an antimetabolite. It causes breaks in chromosomes and has been proposed as an antiviral and antineoplastic agent. It has been given orphan drug status for use in the treatment of primary brain tumors.		2.0310pyrimidine 2'-deoxyribonucleosideantimetabolite;
antineoplastic agent
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		2.0310amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
acepromazine
Acepromazine: A phenothiazine that is used in the treatment of PSYCHOSES.. acepromazine : A member of the class of phenothiazines that is 10H-phenothiazine substituted by an acetyl group at position 2 and a 3-(dimethylamino)propyl group at position 10.		2.0210aromatic ketone;
methyl ketone;
phenothiazines;
tertiary amino compound		phenothiazine antipsychotic drug
methoxamine hydrochloride
[no description available]		2.0310dimethoxybenzene
papaverine hydrochloride
[no description available]		2.0310
bretylium tosylate
Bretylium Tosylate: An agent that blocks the release of adrenergic transmitters and may have other actions. It was formerly used as an antihypertensive agent, but is now proposed as an anti-arrhythmic.. bretylium tosylate : The tosylate salt of bretylium. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation.		2.4320organosulfonate salt;
quaternary ammonium salt		adrenergic antagonist;
anti-arrhythmia drug;
antihypertensive agent
berlition
berlition: antioxidant preparation containing alpha-lipoic acid, used in the neuroprotective therapy of chronic brain ischemia for correction of free-radical processes. (R)-lipoic acid : The (R)-enantiomer of lipoic acid. A vitamin-like, C8 thia fatty acid with anti-oxidant properties.. lipoic acid : A heterocyclic thia fatty acid comprising pentanoic acid with a 1,2-dithiolan-3-yl group at the 5-position.		2.0310dithiolanes;
heterocyclic fatty acid;
lipoic acid;
thia fatty acid		cofactor;
nutraceutical;
prosthetic group
methacholine chloride
Methacholine Chloride: A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)		2.0310quaternary ammonium salt
androstenedione
Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.. androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads.		2.031017-oxo steroid;
3-oxo-Delta(4) steroid;
androstanoid		androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		2.0310alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
yohimbine hydrochloride
[no description available]		2.0310
gallamine triethiodide
Gallamine Triethiodide: A synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of TUBOCURARINE, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)		2.0310
cycloheximide
Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.		2.0310antibiotic fungicide;
cyclic ketone;
dicarboximide;
piperidine antibiotic;
piperidones;
secondary alcohol		anticoronaviral agent;
bacterial metabolite;
ferroptosis inhibitor;
neuroprotective agent;
protein synthesis inhibitor
egtazic acid
Egtazic Acid: A chelating agent relatively more specific for calcium and less toxic than EDETIC ACID.. ethylene glycol bis(2-aminoethyl)tetraacetic acid : A diether that is ethylene glycol in which the hydrogens of the hydroxy groups have been replaced by 2-[bis(carboxymethyl)amino]ethyl group respectively.		2.0310diether;
tertiary amino compound;
tetracarboxylic acid		chelator
cycloserine
Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis).		2.03104-amino-1,2-oxazolidin-3-one;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic;
zwitterion		antiinfective agent;
antimetabolite;
antitubercular agent;
metabolite;
NMDA receptor agonist
17-alpha-hydroxyprogesterone
17alpha-hydroxyprogesterone : A 17alpha-hydroxy steroid that is the 17alpha-hydroxy derivative of progesterone.		2.031017alpha-hydroxy-C21-steroid;
17alpha-hydroxy steroid;
tertiary alpha-hydroxy ketone		human metabolite;
metabolite;
mouse metabolite;
progestin
quinacrine monohydrochloride
[no description available]		2.0310
chlorpromazine hydrochloride
[no description available]		2.0310hydrochloride;
phenothiazines		anticoronaviral agent;
phenothiazine antipsychotic drug
cytarabine hydrochloride
[no description available]		2.0310
cytarabine
[no description available]		2.0210beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
trifluridine
Trifluridine: An antiviral derivative of THYMIDINE used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to HERPES SIMPLEX virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557). trifluridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-trifluoromethyluracil as the nucleobase. An antiviral drug used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis.		2.0210nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
EC 2.1.1.45 (thymidylate synthase) inhibitor
medroxyprogesterone acetate
[no description available]		2.021020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
corticosteroid;
steroid ester		adjuvant;
androgen;
antineoplastic agent;
antioxidant;
female contraceptive drug;
inhibitor;
progestin;
synthetic oral contraceptive
mestranol
[no description available]		2.021017beta-hydroxy steroid;
aromatic ether;
terminal acetylenic compound		prodrug;
xenoestrogen
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.0310erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
lidocaine hydrochloride
lidocaine hydrochloride : The anhydrous form of the hydrochloride salt of lidocaine.		2.0310hydrochlorideanti-arrhythmia drug;
local anaesthetic
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		2.0310arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
chlorphenoxamine
chlorphenoxamine: minor descriptor (66-84); on-line & Index Medicus search ETHYLAMINES (66-84); RN given refers to parent cpd		2.0210diarylmethaneanticoronaviral agent
methylprednisolone
Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.		2.02106-methylprednisolone;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antiemetic;
environmental contaminant;
neuroprotective agent;
xenobiotic
rotenone
Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.		2.0310organic heteropentacyclic compound;
rotenones		antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin
synephrine
[no description available]		2.0310ethanolamines;
phenethylamine alkaloid;
phenols		alpha-adrenergic agonist;
plant metabolite
pyridostigmine bromide
Pyridostigmine Bromide: A cholinesterase inhibitor with a slightly longer duration of action than NEOSTIGMINE. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants.		2.0310pyridinium salt
estradiol dipropionate
estradiol dipropionate: RN given refers to (17beta)-isomer; RN for cpd without isomeric designation not in Chemline 7/83		2.0210steroid ester
imipramine hydrochloride
[no description available]		2.0310hydrochlorideantidepressant
neostigmine bromide
neostigmine bromide : The bromide salt of neostigmine.		2.0310bromide salt
edrophonium chloride
edrophonium chloride : The chloride salt of edrophonium. A reversible inhibitor of cholinesterase with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes), it is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals.		2.0310chloride salt;
quaternary ammonium salt		antidote;
diagnostic agent;
EC 3.1.1.8 (cholinesterase) inhibitor
suramin sodium
suramin sodium : An organic sodium salt that is the hexasodium salt of suramin. It is an FDA approved drug for African sleeping sickness and river blindness.		2.0310organic sodium saltangiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
pyrazolanthrone
pyrazolanthrone: JNK (c-Jun N-terminal kinase) inhibitor; structure in first source. anthra[1,9-cd]pyrazol-6(2H)-one : A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase.		2.0310anthrapyrazole;
aromatic ketone;
cyclic ketone		antineoplastic agent;
c-Jun N-terminal kinase inhibitor;
geroprotector
methapyrilene hydrochloride
methapyrilene hydrochloride : A hydrochloride that is the monohydrochloride salt of methapyrilene.		2.0310hydrochlorideanti-allergic agent;
carcinogenic agent;
H1-receptor antagonist;
sedative
tetrracaine hydrochloride
leocaine: a crystal beta-modification of the beta-dimethylaminoethyl ether of n-butylaminobenzoic acid hydrochloride		2.0310benzoate ester
chelidamic acid
[no description available]		2.0310
2-chloroadenosine
5-chloroformycin A: structure given in first source		2.0310purine nucleoside
diphenhydramine hydrochloride
Antitussive Agents: Agents that suppress cough. They act centrally on the medullary cough center. EXPECTORANTS, also used in the treatment of cough, act locally.. diphenhydramine hydrochloride : The hydrochloride salt of diphenhydramine.		2.0310hydrochloride;
organoammonium salt		anti-allergic agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
sedative
nafcillin
Nafcillin: A semi-synthetic antibiotic related to penicillin.. nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group.		2.0210penicillin allergen;
penicillin		antibacterial drug
methohexital
Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups.		2.0210acetylenic compound;
barbiturates		drug allergen;
intravenous anaesthetic
cysteamine hydrochloride
[no description available]		2.0310
propantheline bromide
[no description available]		2.0310xanthenes
hydralazine hydrochloride
hydralazine hydrochloride : The hydrochloride salt of hydralazine; a direct-acting vasodilator that is used as an antihypertensive agent.		2.0310hydrochlorideantihypertensive agent;
vasodilator agent
ethamivan
ethamivan: minor descriptor (65-72); major descriptor (73-86); on-line search BENZAMIDES (66-86); INDEX MEDICUS search BENZAMIDES (65-72); ETHAMIVAN (73-86). etamivan : Phenol substituted at C-2 and C-4 by a methoxy group and an N,N-diethylaminocarbonyl group respectively. A respiratory stimulant drug related to nikethamide, it has now fallen largely into disuse.		2.0310methoxybenzenes;
phenols
pargyline hydrochloride
[no description available]		2.0310
estradiol 17 beta-cypionate
[no description available]		2.0210steroid ester
testosterone enanthate
[no description available]		2.0210heptanoate ester;
sterol ester		androgen
aminophylline
Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio.		2.0310mixturebronchodilator agent;
cardiotonic drug
azacitidine
Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia.		2.0310N-glycosyl-1,3,5-triazine;
nucleoside analogue		antineoplastic agent
orphenadrine hydrochloride
orphenadrine hydrochloride : A hydrochloride comprising equimolar amounts of ophenadrine and hydrogen chloride.		2.0310hydrochlorideantiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist;
muscle relaxant;
NMDA receptor antagonist;
parasympatholytic
betamethasone
Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)		2.432011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-asthmatic agent;
anti-inflammatory drug;
immunosuppressive agent
benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(n,n-dimethyl-n-2-propenyl-), dibromide
Benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(N,N-dimethyl-N-2-propenyl-), Dibromide: Proposed cholinesterase inhibitor.		2.0310
cyproterone acetate
[no description available]		2.031020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
chlorinated steroid;
steroid ester		androgen antagonist;
geroprotector;
progestin
chenodeoxycholic acid
Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3.		2.0210bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
emetine
Emetine: The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS.. emetine : A pyridoisoquinoline comprising emetam having methoxy substituents at the 6'-, 7'-, 10- and 11-positions. It is an antiprotozoal agent and emetic. It inhibits SARS-CoV2, Zika and Ebola virus replication and displays antimalarial, antineoplastic and antiamoebic properties.		2.0210isoquinoline alkaloid;
pyridoisoquinoline		antiamoebic agent;
anticoronaviral agent;
antiinfective agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
expectorant;
plant metabolite;
protein synthesis inhibitor
bicuculline
Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.. bicuculline : A benzylisoquinoline alkaloid that is 6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline which is substituted at the 5-pro-S position by a (6R)-8-oxo-6,8-dihydrofuro[3,4-e][1,3]benzodioxol-6-yl group. A light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.		2.0310benzylisoquinoline alkaloid;
isoquinoline alkaloid;
isoquinolines		agrochemical;
central nervous system stimulant;
GABA-gated chloride channel antagonist;
GABAA receptor antagonist;
neurotoxin
kainic acid
Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.		2.0310dicarboxylic acid;
L-proline derivative;
non-proteinogenic L-alpha-amino acid;
pyrrolidinecarboxylic acid		antinematodal drug;
excitatory amino acid agonist
podophyllotoxin
Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA.		2.4320furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
tetrahydrozoline hydrochloride
tetrahydrozoline hydrochloride : The hydrochloride salt of tetryzoline. It is used as a nasal decongestant.		2.0310hydrochloridenasal decongestant;
sympathomimetic agent;
vasoconstrictor agent
dequalinium chloride
dequalinium chloride : An organic chloride salt that is the dichloride salt of dequalinium.		2.0310organic chloride saltantifungal agent;
antineoplastic agent;
antiseptic drug;
mitochondrial NADH:ubiquinone reductase inhibitor
levocarnitine
(R)-carnitine : The (R)-enantiomer of carnitine.		2.0210carnitineantilipemic drug;
nootropic agent;
nutraceutical;
Saccharomyces cerevisiae metabolite;
water-soluble vitamin (role)
decamethonium dibromide
[no description available]		2.0310
amitriptyline hydrochloride
[no description available]		2.0310organic tricyclic compound
naphazoline hydrochloride
[no description available]		2.0310organic molecular entity
doxylamine succinate
[no description available]		2.0310organic molecular entity
carbamylhydrazine monohydrochloride
[no description available]		2.0310organic molecular entity
formestane
[no description available]		2.031017-oxo steroid;
3-oxo-Delta(4) steroid;
enol;
hydroxy steroid		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
debrisoquin sulfate
[no description available]		2.0310organic sulfate salt
betaine hydrochloride
[no description available]		2.0310
bethanechol chloride
bethanechol chloride : The chloride salt of bethanechol. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention.		2.0310carbamate ester;
chloride salt;
quaternary ammonium salt		muscarinic agonist
megestrol acetate
[no description available]		2.021020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
steroid ester		antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive
acetylcysteine
N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine.		2.4320acetylcysteine;
L-cysteine derivative;
N-acetyl-L-amino acid		antidote to paracetamol poisoning;
antiinfective agent;
antioxidant;
antiviral drug;
ferroptosis inhibitor;
geroprotector;
human metabolite;
mucolytic;
radical scavenger;
vulnerary
erythromycin
Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.		2.0210cyclic ketone;
erythromycin
levonorgestrel
Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.		2.021017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin;
synthetic oral contraceptive
Mecamylamine hydrochloride
[no description available]		2.0310monoterpenoid
vinblastine
[no description available]		2.0310
cyproheptadine hydrochloride (anhydrous)
cyproheptadine hydrochloride (anhydrous) : The hydrochloride salt of cyproheptadine. Note that the drug named cyproheptadine hydrochloride generally refers to cyproheptadine hydrochloride sesquihydrate.		2.0310hydrochloride
estradiol valerate
[no description available]		2.0210steroid ester
ethambutol
Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone.		2.0210ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic
5 alpha-androstane-3 alpha,17 beta-diol
5alpha-androstane-3alpha,17beta-diol : The 5alpha-stereoisomer of androstane-3alpha,17beta-diol.		2.0310androstane-3alpha,17beta-diolDaphnia magna metabolite;
human metabolite
dronabinol
Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.		2.0210benzochromene;
diterpenoid;
phytocannabinoid;
polyketide		cannabinoid receptor agonist;
epitope;
hallucinogen;
metabolite;
non-narcotic analgesic
pimozide
Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.		2.4320benzimidazoles;
heteroarylpiperidine;
organofluorine compound		antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
azetidyl-2-carboxylic acid
azetidyl-2-carboxylic acid: a proline analog (with 4-membered ring in place of 5); a toxic non-protein amino acid that is misincorporated into protein in place of proline; induces nonfunctional heat-shock proteins; inhibits acquired thermotolerance; RN given refers to (L)-isomer; found in beets and Liliaceae. (S)-azetidine-2-carboxylic acid : The (S)-enantiomer of azetidine-2-carboxylic acid.. azetidinecarboxylic acid : A member of the class of azetidines that is azetidine substituted by at least one carboxy group at unspecified position.		2.0310azetidine-2-carboxylic acid
betamethasone valerate
Betamethasone Valerate: The 17-valerate derivative of BETAMETHASONE. It has substantial topical anti-inflammatory activity and relatively low systemic anti-inflammatory activity.. betamethasone valerate : A steroid ester that is betamethasone in which the hydroxy group at the 17alpha position has been converted to the corresponding pentanoate ester.		2.021011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
primary alpha-hydroxy ketone;
steroid ester		anti-inflammatory drug
muscarine
[no description available]		2.0310
methylprednisolone hemisuccinate
Methylprednisolone Hemisuccinate: A water-soluble ester of METHYLPREDNISOLONE used for cardiac, allergic, and hypoxic emergencies.		2.0210corticosteroid hormone;
hemisuccinate
antazoline hydrochloride
[no description available]		2.0310
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		2.0210dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
doxifluridine
doxifluridine : A pyrimidine 5'-deoxyribonucleoside that is 5-fluorouridine in which the hydroxy group at the 5' position is replaced by a hydrogen. It is an oral prodrug of the antineoplastic agent 5-fluorouracil. Designed to circumvent the rapid degradation of 5-fluorouracil by dihydropyrimidine dehydrogenase in the gut wall, it is converted into 5-fluorouracil in the presence of pyrimidine nucleoside phosphorylase.		2.0310organofluorine compound;
pyrimidine 5'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
prodrug
cyclacillin
Cyclacillin: A cyclohexylamido analog of PENICILLANIC ACID.		2.0210penicillinantibacterial drug
meclofenoxate hydrochloride
[no description available]		2.0310
tranylcypromine
Tranylcypromine: A propylamine formed from the cyclization of the side chain of amphetamine. This monoamine oxidase inhibitor is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in panic and phobic disorders. (From AMA Drug Evaluations Annual, 1994, p311). tranylcypromine : A racemate comprising equal amounts of (1R,2S)- and (1S,2R)-2-phenylcyclopropan-1-amine. An irreversible monoamine oxidase inhibitor that is used as an antidepressant (INN tranylcypromine).. (1R,2S)-tranylcypromine : A 2-phenylcyclopropan-1-amine that is the (1R,2S)-enantiomer of tranylcypromine.		2.02102-phenylcyclopropan-1-amine
clonidine hydrochloride
[no description available]		2.0310dichlorobenzene
cladribine
[no description available]		2.0210organochlorine compound;
purine 2'-deoxyribonucleoside		antineoplastic agent;
immunosuppressive agent
beclomethasone
[no description available]		2.432011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
chlorinated steroid;
corticosteroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-asthmatic drug;
anti-inflammatory drug
estradiol enanthate
[no description available]		2.0210steroid ester
buthionine sulfoximine
Buthionine Sulfoximine: A synthetic amino acid that depletes glutathione by irreversibly inhibiting gamma-glutamylcysteine synthetase. Inhibition of this enzyme is a critical step in glutathione biosynthesis. It has been shown to inhibit the proliferative response in human T-lymphocytes and inhibit macrophage activation. (J Biol Chem 1995;270(33):1945-7). 2-amino-4-(S-butylsulfonimidoyl)butanoic acid : A non-proteinogenic alpha-amino acid that is homocysteine in which the thiol group carries an oxo, imino and butyl groups.. S-butyl-DL-homocysteine (S,R)-sulfoximine : A sulfoximide that is the sulfoximine derivative of an analogue of DL-methionine in which the S-methyl group is replaced by S-butyl.		2.0310diastereoisomeric mixture;
homocysteines;
non-proteinogenic alpha-amino acid;
sulfoximide		EC 6.3.2.2 (glutamate--cysteine ligase) inhibitor;
ferroptosis inducer
mexiletine hydrochloride
mexiletine hydrochloride : A hydrochloride composed of equimolar amounts of mexiletine and hydrogen chloride.		2.0310hydrochlorideanti-arrhythmia drug
betamethasone-17,21-dipropionate
[no description available]		2.021011beta-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
propanoate ester;
steroid ester		antipsoriatic
olsalazine
olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease.		2.0210azobenzenes;
dicarboxylic acid		non-steroidal anti-inflammatory drug;
prodrug
cyclophosphamide
cyclophosphamide hydrate : The monohydrate of cyclophosphamide.		2.0310hydratealkylating agent;
antineoplastic agent;
carcinogenic agent;
immunosuppressive agent
suxamethonium chloride
succinylcholine chloride (anhydrous) : A chloride salt in which the negative charge of the chloride ions is balanced by succinylcholine dications.		2.0310chloride saltmuscle relaxant
cyclobenzaprine hydrochloride
cyclobenzaprine hydrochloride : The hydrochloride salt of cyclobenzaprine. A centrally acting skeletal muscle relaxant, it is used in the symptomatic treatment of painful muscle spasm.		2.0310hydrochlorideantidepressant;
muscle relaxant
n-methylaspartate
N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).. N-methyl-D-aspartic acid : An aspartic acid derivative having an N-methyl substituent and D-configuration.		2.0310amino dicarboxylic acid;
D-alpha-amino acid;
D-aspartic acid derivative;
secondary amino compound		neurotransmitter agent
3-deazaadenosine
3-deazaadenosine: RN given refers to parent cpd.		2.0310
metoclopramide hydrochloride
metoclopramide hydrochloride : A hydrate that is the monohydrate form of metoclopramide monohydrochloride.		2.0310
isoetharine mesylate
[no description available]		2.0310
zalcitabine
Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.		2.4320pyrimidine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
propionylpromazine hydrochloride
[no description available]		2.0310
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.0310delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
nsc-145,668
[no description available]		2.0310hydrochlorideantimetabolite;
antineoplastic agent
clodronic acid
Clodronic Acid: A diphosphonate which affects calcium metabolism. It inhibits bone resorption and soft tissue calcification.. clodronic acid : An organochlorine compound that is methylene chloride in which both hydrogens are replaced by phosphonic acid groups. It inhibits bone resorption and soft tissue calcification, and is used (often as the disodium salt tetrahydrate) as an adjunct in the treatment of severe hypercalcaemia associated with malignancy, and in the management of osteolytic lesions and bone pain associated with skeletal metastases.		2.03101,1-bis(phosphonic acid);
one-carbon compound;
organochlorine compound		antineoplastic agent;
bone density conservation agent
selegiline
Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.		2.0210selegiline;
terminal acetylenic compound		geroprotector
levamisole
Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine.		2.02106-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazoleantinematodal drug;
antirheumatic drug;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
immunological adjuvant;
immunomodulator
benserazide hydrochloride
benserazide hydrochloride : A hydrochloride that is the monohydrochloride salt of benserazide. An aromatic-L-amino-acid decarboxylase inhibitor (DOPA decarboxylase inhibitor) that does not enter the central nervous system, it is used as an adjunct to levodopa in the treatment of parkinsonism. By preventing the conversion of levodopa to dopamine in the periphery, it causes an increase in the amount of levodopa reaching the central nervous system and so reduces the required dose. Benserazide hydrochloride has no antiparkinson actions when given alone.		2.0310hydrochlorideantiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
pancuronium bromide
pancuronium bromide : A bromide salt consisting of two bromide ions and one pancuronium dication.		2.0310bromide saltcholinergic antagonist;
muscle relaxant;
nicotinic antagonist
cephalexin
Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.. cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract.		2.0210beta-lactam antibiotic allergen;
cephalosporin;
semisynthetic derivative		antibacterial drug
isosorbide-5-mononitrate
isosorbide-5-mononitrate: for prevention of angina pectoris; structure given in first source; a Russian drug		2.0210glucitol derivative;
nitrate ester		nitric oxide donor;
vasodilator agent
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		2.0310acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
danazol
Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders.		2.432017beta-hydroxy steroid;
terminal acetylenic compound		anti-estrogen;
estrogen antagonist;
geroprotector
metergoline
Metergoline: A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.. metergoline : An ergoline alkaloid that is the N-benzyloxycarbonyl derivative of lysergamine. A 5-HT2 antagonist. Also 5-HT1 antagonist and 5-HT1D ligand. Has moderate affinity for 5-HT6 and high affinity for 5-HT7.		2.0310carbamate ester;
ergoline alkaloid		dopamine agonist;
geroprotector;
serotonergic antagonist
lisuride
Lisuride: An ergot derivative that acts as an agonist at dopamine D2 receptors (DOPAMINE AGONISTS). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (SEROTONIN RECEPTOR AGONISTS).		2.0310monocarboxylic acid amideantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
serotonergic agonist
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		2.0210aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
cephapirin
Cephapirin: Cephalosporin antibiotic, partly plasma-bound, that is effective against gram-negative and gram-positive organisms.. cephapirin : A cephalosporin with acetoxymethyl and 2(pyridin-4-ylsulfanyl)acetamido substituents at positions 3 and 7, respectively, of the cephem skeleton. It is used (as its sodium salt) as an antibiotic, being effective against gram-negative and gram-positive organisms.		2.0210cephalosporinantibacterial drug
disopyramide phosphate
[no description available]		2.0310organoammonium phosphate
bromocriptine
Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.		4.0740indole alkaloidantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
hormone antagonist
ergocristine
ergocristine: an ergot alkaloid; one of the three components of ergotoxine; has alpha blocking action, stimulates smooth muscles & antagonizes serotonin; used as oxytocic & in peripheral disorders; minor descriptor (77-86); on-line & INDEX MEDICUS search EROLINES (77-86); RN given refers to ((5'alpha)-isomer). ergocristine : Ergotaman bearing benzyl, hydroxy, and isopropyl groups at the 5', 12' and 2' positions, respectively, and oxo groups at positions 3', 6', and 18. It is a natural ergot alkaloid.		2.0310ergot alkaloid
triamcinolone
Triamcinolone: A glucocorticoid given, as the free alcohol or in esterified form, orally, intramuscularly, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. (From Martindale, The Extra Pharmacopoeia, 30th ed, p739). triamcinolone : A C21-steroid hormone that is 1,4-pregnadiene-3,20-dione carrying four hydroxy substituents at positions 11beta, 16alpha, 17alpha and 21 as well as a fluoro substituent at position 9. Used in the form of its 16,17-acetonide to treat various skin infections.		2.031011beta-hydroxy steroid;
16alpha-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-allergic agent;
anti-inflammatory drug
ursodeoxycholic acid
Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		2.0210bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
metipranolol
Metipranolol: A beta-adrenergic antagonist effective for both beta-1 and beta-2 receptors. It is used as an antiarrhythmic, antihypertensive, and antiglaucoma agent.. metipranolol : 3-(Propan-2-ylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is substituted by a 4-acetoxy-2,3,5-trimethylphenoxy group. A non-cardioselective beta-blocker, it is used to lower intra-ocular pressure in the management of open-angle glaucoma.		2.0210acetate ester;
aromatic ether;
propanolamine;
secondary amino compound		anti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
halazepam
halazepam: structure		2.0210organic molecular entity
du-21220
Ritodrine: An adrenergic beta-2 agonist used to control PREMATURE LABOR.. 4-[2-[[1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]phenol : A secondary amino compound that is 4-(2-amino-1-hydroxypropyl)phenol in which one of the hydrogens attached to the nitrogen is replaced by a 2-(4-hydroxyphenyl)ethyl group.		2.0210benzyl alcohols;
polyphenol;
secondary alcohol;
secondary amino compound
cefazolin
Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively.		2.0210beta-lactam antibiotic allergen;
cephalosporin;
tetrazoles;
thiadiazoles		antibacterial drug
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		2.0210penicillin allergen;
penicillin		antibacterial drug
timolol
(S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine.		2.4220timololanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
moricizine
Moricizine: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.. moricizine : A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group.		2.0210carbamate ester;
morpholines;
phenothiazines		anti-arrhythmia drug
bitolterol
bitolterol: RN given refers to parent cpd; structure. bitolterol : The di-4-toluate ester of (+-)-N-tert-butylnoradrenaline (colterol). A pro-drug for colterol, a beta2-adrenergic receptor agonist, bitolterol is used as its methanesulfonate salt for relief of bronchospasm in conditions such as asthma, chronic bronchitis and emphysema.		2.0210carboxylic ester;
diester;
ethanolamines;
secondary alcohol;
secondary amino compound		anti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent;
prodrug
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		2.4320azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
tobramycin
Tobramycin: An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the PSEUDOMONAS species. It is a 10% component of the antibiotic complex, NEBRAMYCIN, produced by the same species.. tobramycin : A amino cyclitol glycoside that is kanamycin B lacking the 3-hydroxy substituent from the 2,6-diaminoglucose ring.		2.0210amino cyclitol glycosideantibacterial agent;
antimicrobial agent;
toxin
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.4320taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
buspirone hydrochloride
buspirone hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of buspirone and hydrogen chloride.		2.0310hydrochlorideanxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
etoposide
[no description available]		2.4320beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
propafenone hydrochloride
propafenone hydrochloride : A hydrochloride that is the monohydrochloride salt of propafenone. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used in the management of supraventricular and ventricular arrhythmias.		2.0310hydrochlorideanti-arrhythmia drug
dobutamine
Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure.		2.0210catecholamine;
secondary amine		beta-adrenergic agonist;
cardiotonic drug;
sympathomimetic agent
etazolate hydrochloride
[no description available]		2.0310
butaclamol
[no description available]		2.0310amino alcohol;
organic heteropentacyclic compound;
tertiary alcohol;
tertiary amino compound		dopaminergic antagonist
penbutolol
Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent.		2.0210ethanolamines
ribavirin
Rebetron: Rebetron is tradename		2.43201-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
zinterol
[no description available]		3.3820
carbidopa
[no description available]		2.0310catechols;
hydrate;
hydrazines;
monocarboxylic acid		antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
cephradine
Cephradine: A semi-synthetic cephalosporin antibiotic.. cephradine : A first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton.		2.0310beta-lactam antibiotic allergen;
cephalosporin		antibacterial drug
guanadrel
guanadrel: RN given refers to parent cpd; structure. guanadrel : A spiroketal resulting from the formal condensation of the keto group of cyclohexanone with the hydroxy groups of 1-(2,3-dihydroxypropyl)guanidine. A postganglionic adrenergic blocking agent formerly used (generally as the sulfate salt) for the management of hypertension, it has been largely superseded by other drugs less likely to cause orthostatic hypotension (dizzy spells on standing up or stretching).		2.0210guanidines;
spiroketal		adrenergic antagonist;
antihypertensive agent
methyldopa
Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring.		2.4320L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		alpha-adrenergic agonist;
antihypertensive agent;
hapten;
peripheral nervous system drug;
sympatholytic agent
tocainide
Tocainide: An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS.. tocainide : A monocarboxylic acid amide in which 2,6-dimethylphenylaniline and isobutyric acid have combined to form the amide bond; used as a local anaesthetic.		2.0210monocarboxylic acid amideanti-arrhythmia drug;
local anaesthetic;
sodium channel blocker
sq-11725
Nadolol: A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.. nadolol : Nadolol is a diastereoisomeric mixture consisting of equimolar amounts of the four possible 2,3-cis-isomers of 5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol.		2.4220
diltiazem
Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension.		2.42205-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
levobunolol
Levobunolol: The L-Isomer of bunolol.. levobunolol : A cyclic ketone that is 3,4-dihydronaphthalen-1-one substituted at position 5 by a 3-(tert-butylamino)-2-hydroxypropoxy group (the S-enantiomer). A non-selective beta-adrenergic antagonist used (as its hydrochloride salt) for treatment of glaucoma.		2.0210aromatic ether;
cyclic ketone;
propanolamine		antiglaucoma drug;
beta-adrenergic antagonist
lonidamine
lonidamine: structure. lonidamine : A member of the class of indazoles that is 1H-indazole that is substituted at positions 1 and 3 by 2,4-dichlorobenzyl and carboxy groups, respectively.		2.0310dichlorobenzene;
indazoles;
monocarboxylic acid		antineoplastic agent;
antispermatogenic agent;
EC 2.7.1.1 (hexokinase) inhibitor;
geroprotector
vecuronium bromide
Vecuronium Bromide: Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents.. vecuronium bromide : The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium substituents.		2.0210organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent;
nicotinic antagonist
dexibuprofen
dexibuprofen: structure in first source		2.0310ibuprofennon-narcotic analgesic;
non-steroidal anti-inflammatory drug
permethrin
hemoglobin Atlanta-Coventry: Leu replaced by Pro at beta75 and Leu deleted at beta141		2.0210cyclopropanecarboxylate ester;
cyclopropanes		agrochemical;
ectoparasiticide;
pyrethroid ester acaricide;
pyrethroid ester insecticide;
scabicide
quisqualic acid
Quisqualic Acid: An agonist at two subsets of excitatory amino acid receptors, ionotropic receptors that directly control membrane channels and metabotropic receptors that indirectly mediate calcium mobilization from intracellular stores. The compound is obtained from the seeds and fruit of Quisqualis chinensis.		2.0310non-proteinogenic alpha-amino acid
pirfenidone
pirfenidone : A pyridone that is 2-pyridone substituted at positions 1 and 5 by phenyl and methyl groups respectively. An anti-inflammatory drug used for the treatment of idiopathic pulmonary fibrosis.		2.0310pyridoneantipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
mefloquine
(-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.		3.3110[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
flecainide acetate
flecainide acetate : An acetate salt obtained by combining flecainide with one molar equivalent of acetic acid. An antiarrhythmic agent used to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		2.0310acetate saltanti-arrhythmia drug
nicardipine hydrochloride
[no description available]		2.0310dihydropyridinegeroprotector
sufentanil
Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.. sufentanil : An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid.		2.4220anilide;
ether;
piperidines;
thiophenes		anaesthesia adjuvant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
torsemide
Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure.		2.0210aminopyridine;
N-sulfonylurea;
secondary amino compound		antihypertensive agent;
loop diuretic
cefmetazole
Cefmetazole: A semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. It has a high rate of efficacy in many types of infection and to date no severe side effects have been noted.. cefmetazole : A second-generation cephalosporin antibiotic having N(1)-methyltetrazol-5-ylthiomethyl, {[(cyanomethyl)sulfanyl]acetyl}amino and methoxy side-groups at positions 3, 7beta and 7alpha respectively of the parent cephem bicyclic structure.		2.0210cephalosporinantibacterial drug
desflurane
Desflurane: A fluorinated ether that is used as a volatile anesthetic for maintenance of general anesthesia.		2.0210organofluorine compoundinhalation anaesthetic
idarubicin
Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA.		2.4320anthracycline antibiotic;
deoxy hexoside;
monosaccharide derivative
cefonicid
Cefonicid: A second-generation cephalosporin administered intravenously or intramuscularly. Its bactericidal action results from inhibition of cell wall synthesis. It is used for urinary tract infections, lower respiratory tract infections, and soft tissue and bone infections.. cefonicid : A cephalosporin bearing {[1-(sulfomethyl)-1H-tetrazol-5-yl]sulfanyl}methyl and (R)-2-hydroxy-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		2.0210cephalosporinantibacterial drug
piperacillin
Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group.		2.0210penicillin allergen;
penicillin		antibacterial drug
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		2.0210aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
captopril
Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.		2.4320alkanethiol;
L-proline derivative;
N-acylpyrrolidine;
pyrrolidinemonocarboxylic acid		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
cefoperazone
Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance.		2.0210cephalosporinantibacterial drug
terazosin hydrochloride anhydrous
[no description available]		2.0310
lodoxamide
[no description available]		2.0210organonitrogen compound;
organooxygen compound
atracurium
Atracurium: A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.. atracurium : A diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups.		2.0210diester;
quaternary ammonium ion		muscle relaxant;
nicotinic antagonist
butoconazole
butoconazole: RN given refers to parent cpd; structure. butoconazole : A member of the class of imidazoles that is 1H-imidazole in which the hydrogen attached to the nitrogen is substituted by a 4-(4-chlorophenyl)-2-[(2,6-dichlorophenyl)sulfanyl]butyl group. An antifungal agent, it is used as its nitrate salt in gynaecology for treatment of vulvovaginal infections caused by Candida species, particularly Candida albicans.		2.0210aryl sulfide;
conazole antifungal drug;
dichlorobenzene;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes
naftifine
naftifine: allylamine der; RN given refers to unlabeled parent cpd. naftifine : A tertiary amine in which the nitrogen is substituted by methyl, alpha-naphthylmethyl, and (1E)-cinnamyl groups. It is used (usually as its hydrochloride salt) for the treatment of fungal skin infections.		2.0210allylamine antifungal drug;
naphthalenes;
tertiary amine		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
sterol biosynthesis inhibitor
pergolide
Pergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.. pergolide : A diamine that is ergoline in which the beta-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		2.0210diamine;
methyl sulfide;
organic heterotetracyclic compound		antiparkinson drug;
dopamine agonist
pergolide mesylate
pergolide mesylate : A methanesulfonate salt obtained from pergolide by mixing eqimolar amount of pergolide and methanesulfonic acid. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		2.0310methanesulfonate saltantiparkinson drug;
dopamine agonist;
geroprotector
ranitidine hydrochloride
label : A role played by a part of a molecular entity distinguishable by the observer but not by the system and used to identify a tracer.		2.0310
colforsin
Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.		2.0310acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
cefadroxil anhydrous
Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		2.0210cephalosporinantibacterial drug
encainide
Encainide: One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM.. encainide : 4-Methoxy-N-phenylbenzamide in which the hydrogen at the 2 position of the phenyl group is substituted by a 2-(1-methylpiperidin-2-yl)ethyl group. A class Ic antiarrhythmic, the hydrochloride was used for the treatment of severe or life-threatening ventricular arrhythmias, but it was associated with increased death rates in patients who had asymptomatic heart rhythm abnormalities after a recent heart attack and was withdrawn from the market.		2.0210benzamides;
piperidines		anti-arrhythmia drug;
sodium channel blocker
nedocromil
Nedocromil: A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with ASTHMA, including EOSINOPHILS; NEUTROPHILS; MACROPHAGES; MAST CELLS; MONOCYTES; AND PLATELETS.		2.0210dicarboxylic acid;
organic heterotricyclic compound		anti-allergic agent;
anti-asthmatic drug;
non-steroidal anti-inflammatory drug
cefaclor anhydrous
Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		2.4320cephalosporinantibacterial drug;
drug allergen
alfentanil
Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position.		2.0210monocarboxylic acid amide;
piperidines		central nervous system depressant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
peripheral nervous system drug
alo 2145
apraclonidine hydrochloride : The hydrochloride salt of apraclonidine.		2.0310hydrochloridealpha-adrenergic agonist;
antiglaucoma drug
cefotetan
Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms.		2.0210
lovastatin
Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).		2.0210delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		anticholesteremic drug;
antineoplastic agent;
Aspergillus metabolite;
prodrug
enoximone
Enoximone: A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE.		2.0310aromatic ketone
levocabastine
levocabastine: for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis		2.0210piperidines
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		2.0210delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
quinpirole
Quinpirole: A dopamine D2/D3 receptor agonist.. quinpirole : A pyrazoloquinoline that is (4aR,8aR)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrazolo[3,4-g]quinoline substituted by a propyl group at position 5. It acts as a dopamine agonist.		2.1310pyrazoloquinolinedopamine agonist
pravastatin
Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		2.02103-hydroxy carboxylic acid;
carbobicyclic compound;
carboxylic ester;
hydroxy monocarboxylic acid;
secondary alcohol;
statin (semi-synthetic)		anticholesteremic drug;
environmental contaminant;
metabolite;
xenobiotic
cabergoline
Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia.		2.0210N-acylureaantineoplastic agent;
antiparkinson drug;
dopamine agonist
atomoxetine
atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents.		2.0310aromatic ether;
secondary amino compound;
toluenes		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
xenobiotic
quinapril
Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure.		2.0210dicarboxylic acid monoester;
ethyl ester;
isoquinolines;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
raloxifene hydrochloride
Raloxifene Hydrochloride: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.. raloxifene hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride.		2.0310hydrochloridebone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
mifepristone
Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.		2.03103-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound		abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
quinpirole hydrochloride
[no description available]		2.0310
imazodan
imazodan: RN & structure given in first source;		2.0310
fosphenytoin
fosphenytoin: structure given in first & second source		2.0210imidazolidine-2,4-dione
finasteride
Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.		2.02103-oxo steroid;
aza-steroid;
delta-lactam		androgen antagonist;
antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
esmolol
methyl 3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate : A methyl ester that is methyl 3-(4-hydroxyphenyl)propanoate in which the hydrogen attached to the phenolic hydroxy group is substituted by a 2-hydroxy-3-(isopropylamino)propyl group.. esmolol : A racemate comprising equimolar amounts of (R)- and (S)-esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used as the hydrochloride salt in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery. While the S enantiomer possesses all of the heart rate control, both enantiomers contribute to lowering blood pressure.		2.0210aromatic ether;
ethanolamines;
methyl ester;
secondary alcohol;
secondary amino compound
adapalene
Adapalene: A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.. adapalene : A naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether.		2.0210adamantanes;
monocarboxylic acid;
naphthoic acid		dermatologic drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
non-steroidal anti-inflammatory drug
sparfloxacin
[no description available]		2.0210fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
zileuton
[no description available]		2.02101-benzothiophenes;
ureas		anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
cidofovir anhydrous
Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients.		2.0210phosphonic acids;
pyrimidone		anti-HIV agent;
antineoplastic agent;
antiviral drug;
photosensitizing agent
(S)-betaxolol
(S)-betaxolol : The (S)-enantiomer of betaxolol.		2.0210betaxolol
mibefradil dihydrochloride
[no description available]		2.0310
topotecan
Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.		2.0210pyranoindolizinoquinolineantineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		2.0210organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
ibutilide
ibutilide: RN & structure in first source; RN refers to the fumarate salt		2.0210benzenes;
organic amino compound
remifentanil
Remifentanil: A piperidine-propionate derivative and opioid analgesic structurally related to FENTANYL. It functions as a short-acting MU OPIOID RECEPTOR agonist, and is used as an analgesic during induction or maintenance of general anesthesia, following surgery, during childbirth, and in mechanically ventilated patients under intensive care.. remifentanil : A piperidinecarboxylate ester that is methyl piperidine-4-carboxylate in which the hydrogen attached to the nitrogen is substituted by a 3-methoxy-3-oxopropyl group and the hydrogen at position 4 is substituted the nitrogen of N-propanoylaniline.		2.0210alpha-amino acid ester;
anilide;
monocarboxylic acid amide;
piperidinecarboxylate ester		intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
sedative
atorvastatin
[no description available]		2.0210aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
lamivudine
[no description available]		2.0210monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
irinotecan
[no description available]		2.0210carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
aptiganel hydrochloride
[no description available]		2.0310
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		2.0210biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		2.4320adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
phenelzine sulfate
[no description available]		2.0310organic molecular entity
fluoxetine hydrochloride
fluoxetine hydrochloride : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine hydrochloride. A selective serotonin reuptake inhibitor (SSRI), it is used for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.		2.0310hydrochloride;
N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine
propranolol hydrochloride
Inderex: combination of above cpds; used in treatment of hypertension		2.0310hydrochloride
bupropion hydrochloride
[no description available]		2.0310aromatic ketone
diltiazem hydrochloride
Carex: fluoride (1.8%) containing varnish; no further information available 8/91. diltiazem hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of diltiazem and hydrogen chloride. A calcium-channel blocker and vasodilator, it is used in the management of angina pectoris and hypertension.		2.0310hydrochlorideantihypertensive agent;
calcium channel blocker;
vasodilator agent
trazodone hydrochloride
Triticum: A plant genus of the family POACEAE that is the source of EDIBLE GRAIN. A hybrid with rye (SECALE CEREALE) is called TRITICALE. The seed is ground into FLOUR and used to make BREAD, and is the source of WHEAT GERM AGGLUTININS.. trazodone hydrochloride : A hydrochloride salt prepared from equimolar amounts of trazodone and hydrogen chloride.		2.0310hydrochlorideadrenergic antagonist;
antidepressant;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
verapamil hydrochloride
verapamil hydrochloride : A racemate comprising equimolar amounts of dexverapamil hydrochloride and (S)-verapamil hydrochloride.		2.0310
cefprozil
[no description available]		2.0210cephalosporin;
semisynthetic derivative		antibacterial drug
doxazosin mesylate
Cardura: Trade name in United States.		2.0310methanesulfonate saltgeroprotector
terfenadine
[no description available]		2.0310diarylmethane
methylprednisolone aceponate
methylprednisolone aceponate: RN given for (6alpha,11beta)-isomer		2.0210corticosteroid hormone
dexamethasone 17-valerate
dexamethasone 17-valerate: RN given refers to (11beta,16alpha)-isomer; structure		2.021021-hydroxy steroid
dexamethasone dipropionate
[no description available]		2.0210corticosteroid hormone
carmoterol
carmoterol: CHF4226.01 and CHF4232.01 are diastereoisomers; structure in first source		2.0510
nelfinavir
Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.		3.3110aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound		antineoplastic agent;
HIV protease inhibitor
amantadine hydrochloride
[no description available]		2.0310hydrochlorideantiviral agent;
dopamine agonist;
NMDA receptor antagonist
mevastatin
mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure. mevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.		2.03102-pyranones;
carboxylic ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		antifungal agent;
apoptosis inducer;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
fungal metabolite;
Penicillium metabolite
chloroquine diphosphate
[no description available]		2.0310
betulinic acid
[no description available]		3.3110hydroxy monocarboxylic acid;
pentacyclic triterpenoid		anti-HIV agent;
anti-inflammatory agent;
antimalarial;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
plant metabolite
baicalin
[no description available]		3.3110dihydroxyflavone;
glucosiduronic acid;
glycosyloxyflavone;
monosaccharide derivative		antiatherosclerotic agent;
antibacterial agent;
anticoronaviral agent;
antineoplastic agent;
antioxidant;
cardioprotective agent;
EC 2.7.7.48 (RNA-directed RNA polymerase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
ferroptosis inhibitor;
neuroprotective agent;
non-steroidal anti-inflammatory drug;
plant metabolite;
prodrug
dobutamine hydrochloride
dobutamine hydrochloride : The hydrochloride salt of dobutamine. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used to increase the contractility of the heart in the management of acute heart failure.		2.0310hydrochloridebeta-adrenergic agonist;
cardiotonic drug;
sympathomimetic agent
desipramine hydrochloride
desipramine hydrochloride : The hydrochloride salt of desipramine.		2.0310hydrochloridedrug allergen
dopamine hydrochloride
P 498: structure in first source; do not confuse with dopamine chloride, also known as P 498		2.0310catecholamine
proadifen hydrochloride
[no description available]		2.0310
4-nitrobenzylthioinosine
4-nitrobenzylthioinosine: inhibitor of nucleoside transport; acts on ENT1		2.0310purine nucleoside
iopamidol
Iopamidol: A non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiological procedures.. iopamidol : A benzenedicarboxamide compound having N-substituted carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and a (2S)-2-hydroxypropanamido group at the 5-position.		2.0210benzenedicarboxamide;
organoiodine compound;
pentol		environmental contaminant;
radioopaque medium;
xenobiotic
fluazuron
fluazuron: a benzoyl phenylurea compound; ACATAK (tradename) is a pour-on tick development inhibitor containing fluazuron as its active ingredient. fluazuron : An N-acylurea that is urea in which one of the hydrogens has been replaced by a 3,6-difluorobenzoyl group, while a hydrogen attached to the other nitrogen has been replaced by a 4-chloro-3-{[3-chloro-5-(trifluoromethyl)pyridin-2-yl]oxy}phenyl group. It is used to control ticks in cattle.		2.0510aromatic ether;
chloropyridine;
monochlorobenzenes;
N-acylurea;
organochlorine acaricide;
organofluorine acaricide;
phenylureas		acaricide;
mite growth regulator
metrifudil
[no description available]		2.0310
rutecarpine
rutacarpine: from Evodia rutaecarpa; an ingredient in zhuyu hewei zhitong capsules		2.0310beta-carbolines
trihexyphenidyl hydrochloride
[no description available]		2.0310aralkylamine
thioridazine hydrochloride
[no description available]		2.0310hydrochloridefirst generation antipsychotic;
geroprotector
procainamide hydrochloride
procainamide hydrochloride : A hydrochloride which has procainamide as the amino component.		2.0310hydrochlorideanti-arrhythmia drug
siquil
[no description available]		2.0310hydrochlorideanticoronaviral agent
sotalol hydrochloride
sotalol hydrochloride : A hydrochloride salt that is the monohydrochloride of sotalol. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.		2.0310hydrochlorideanti-arrhythmia drug;
beta-adrenergic antagonist
oxymetazoline hydrochloride
oxymetazoline hydrochloride : A hydrochloride salt resulting from the reaction of equimolar quantities of oxymetazoline and hydrogen chloride. A direct-acting sympathomimetic with marked alpha-adrenergic activity, it is a vasoconstrictor that is used to relieve nasal congestion.		2.0310hydrochloridealpha-adrenergic agonist;
nasal decongestant;
sympathomimetic agent;
vasoconstrictor agent
dexfenfluramine
Dexfenfluramine: The S-isomer of FENFLURAMINE. It is a serotonin agonist and is used as an anorectic. Unlike fenfluramine, it does not possess any catecholamine agonist activity.. (S)-fenfluramine : The S-enantiomer of fenfluramine. It stimulates the release of serotonin and selectively inhibits its reuptake, but unlike fenfluramine it does not possess catecholamine agonist activity. It was formerly given by mouth as the hydrochloride in the treatment of obesity, but, like fenfluramine, was withdrawn wolrdwide following reports of valvular heart defects.		2.0210fenfluramineappetite depressant;
serotonergic agonist;
serotonin uptake inhibitor
alprenolol hydrochloride
[no description available]		2.0310hydrochloride
2-methoxyestradiol
2-methoxy-17beta-estradiol : A 17beta-hydroxy steroid, being 17beta-estradiol methoxylated at C-2.		2.031017beta-hydroxy steroid;
3-hydroxy steroid		angiogenesis modulating agent;
antimitotic;
antineoplastic agent;
human metabolite;
metabolite;
mouse metabolite
fluphenazine hydrochloride
[no description available]		2.0310phenothiazinesanticoronaviral agent
tryptamine monohydrochloride
[no description available]		2.0310
clomipramine hydrochloride
clomipramine hydrochloride : A hydrochloride resulting from the reaction of equimolar amounts of clomipramine and hydrogen chloride. One of the more sedating tricyclic antidepressants, it is used for the treatment of depression as well as obsessive-compulsive disorder and phobias.		2.0310hydrochlorideanticoronaviral agent;
antidepressant;
serotonergic antagonist;
serotonergic drug
amiloride hydrochloride
amiloride hydrochloride dihydrate : A hydrate that is the dihydrate of amiloride hydrochloride.		2.0310hydratediuretic;
sodium channel blocker
prazosin hydrochloride
[no description available]		2.0310hydrochloride
mianserin hydrochloride
mianserin hydrochloride : The hydrochloride salt of mianserin, a tetracyclic compound with antidepressant effects.		2.0310hydrochloridegeroprotector
sertraline
Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression.. sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder.		2.4220dichlorobenzene;
secondary amino compound;
tetralins		antidepressant;
serotonin uptake inhibitor
lomefloxacin hydrochloride
lomefloxacin hydrochloride : The hydrochloride salt of lomefloxacin. It is administered by mouth to treat bacterial infections including bronchitis and urinary tract infections. It is also used topically as eye drops for the treatment of bacterial conjunctivitis, and as ear drops for the treatment of otitis externa and otitis media.		2.0310hydrochlorideantimicrobial agent;
antitubercular agent;
photosensitizing agent
fenspiride hydrochloride
[no description available]		2.0310
nilverm
[no description available]		2.0310organic molecular entity
sanguinarine chloride
[no description available]		2.0310
ropinirole hydrochloride
[no description available]		2.0310indoles
plasmenylserine
plasmenylserine: RN given refers to (L)-isomer. O-phospho-L-serine : The L-enantiomer of O-phosphoserine.. O-phosphoserine : A serine derivative that is serine substituted at the oxygen atom by a phosphono group.		2.0310O-phosphoserineEC 1.4.7.1 [glutamate synthase (ferredoxin)] inhibitor;
EC 2.5.1.49 (O-acetylhomoserine aminocarboxypropyltransferase) inhibitor;
EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
5-aminovaleric acid hydrochloride
[no description available]		2.0310
n-acetyltryptamine
N-acetyltryptamine: antagonizes the melatonin-induced inhibition of dopamine release from retina; RN given refers to parent cpd. N-acetyltryptamine : A tryptamine compound having an acetyl substituent attached to the side-chain amino function.		2.0310acetamides;
indoles
D-serine
[no description available]		2.0310D-alpha-amino acid;
serine zwitterion;
serine		Escherichia coli metabolite;
human metabolite;
NMDA receptor agonist
dihydroergotamine mesylate
dihydroergotamine mesylate : The methanesulfonic acid salt of dihydroergotamine, a semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine. Both the mesylate and the tartrate salts are used for the treatment of migraine and orthostatic hypotension.		2.0310methanesulfonate saltnon-narcotic analgesic;
serotonergic agonist;
vasoconstrictor agent
erythromycin propionate
erythromycin propionate: form in which erythromycin estolate is principally absorbed		2.0210erythromycin derivative
ranolazine hydrochloride
[no description available]		2.0310
dexrazoxane
Dexrazoxane: The (+)-enantiomorph of razoxane.		2.0210razoxaneantineoplastic agent;
cardiovascular drug;
chelator;
immunosuppressive agent
loxapine succinate
[no description available]		2.0310succinate saltgeroprotector
guanfacine hydrochloride
[no description available]		2.0310acetamidesgeroprotector
pirenzepine dihydrochloride
[no description available]		2.0310hydrochloride
labetalol hydrochloride
[no description available]		2.0310salicylamides
acecainide hydrochloride
[no description available]		2.0310
loperamide hydrochloride
loperamide hydrochloride : A hydrochloride obtained by combining loperamide with one equivalent of hydrochloric acid. Used for treatment of diarrhoea resulting from gastroenteritis or inflammatory bowel disease.		2.0310hydrochlorideanticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
antebate
betamethasone butyrate propionate: a topical corticosteroid		2.0210corticosteroid hormone
maprotiline hydrochloride
[no description available]		2.0310anthracenes
protoporphyrin ix, disodium salt
[no description available]		2.0310
carazolol
carazolol: RN given refers to parent cpd without isomeric designation; structure		2.2110carbazoles
siguazodan
[no description available]		2.0310pyridazinone
3-octadecanamido-2-ethoxypropylphosphocholine
3-octadecanamido-2-ethoxypropylphosphocholine: anti-HIV agent; RN & structure given in first source		2.0310
honokiol
[no description available]		3.3110biphenyls
chelerythrine chloride
[no description available]		2.0310
lycorine
lycorine: from bulbs of LYCORIS & other plants; RN given refers to (1 alpha,2 beta)-isomer; structure in Merck Index, 9th ed, #5444. lycorine : An indolizidine alkaloid that is 3,12-didehydrogalanthan substituted by hydroxy groups at positions and 2 and a methylenedioxy group across positions 9 and 10. Isolated from Crinum asiaticum, it has been shown to exhibit antimalarial activity.		3.3110indolizidine alkaloidanticoronaviral agent;
antimalarial;
plant metabolite;
protein synthesis inhibitor
pacein
PAcein: structure. pacein : A member of the class of benzofurans that is dibenzo[b,d]furan-3,7-dione bearing two methyl substituents at positions 1 and 9 as well as two 2,4-dihydroxy-6-methylanilino substituents at positions 2 and 8.. orcein : A variable mixture of several compounds isolated from lichens, the eight most abundant being alpha-aminoorcein, alpha-hydroxyorcein, beta-aminoorcein, gamma-aminoorcein, beta-hydroxyorcein, gamma-hydroxyorcein, beta-aminoorceimine and beta-aminoorceimine (all are phenoxazine-based). It is used for the demonstration of elastic fibres as well as to stain the rough endoplasmic reticulum of hepatitis B infected liver cells.		3.3110
tosyllysine chloromethyl ketone
[no description available]		2.0310
5-(n-methyl-n-isobutyl)amiloride
5-(N-methyl-N-isobutyl)amiloride: inhibitor of the Na+-H+ antiporter		2.0310
1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride
1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride : A hydrochloride salt prepared from anileridine and two molar equivalents of hydrogen chloride.		2.0310hydrochlorideEC 2.7.11.13 (protein kinase C) inhibitor
amperozide hydrochloride
amperozide hydrochloride : The hydrochloride salt of amperozide.		2.0310hydrochlorideanxiolytic drug;
dopamine uptake inhibitor;
geroprotector;
second generation antipsychotic;
serotonergic antagonist
pyrrolidine dithiocarbamic acid
[no description available]		2.0310
agroclavine
agroclavine: structure. agroclavine : An ergot alkaloid that is ergoline which contains a double bond between positions 8 and 9, and which is substituted by methyl groups at positions 6 and 8.		2.0310ergot alkaloid
atovaquone
Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.		2.0210hydroxy-1,2-naphthoquinone
s-methylisothiourea sulfate
[no description available]		2.0310
p-Aminobenzamidine dihydrochloride
[no description available]		2.0310organic molecular entity
enpiperate
enpiperate: RN given refers to parent cpd		2.1110
benzamidine hydrochloride
[no description available]		2.0310
flunisolide
flunisolide: flunisolide HFA is a formulation of flunisolide using hydrofluoroalkane (HFA) as propellant in place of chlorofluorocarbon (CFC) ones		2.021011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic ketal;
fluorinated steroid;
primary alpha-hydroxy ketone		anti-asthmatic drug;
anti-inflammatory drug;
immunosuppressive agent
ketorolac tromethamine
Ketorolac Tromethamine: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.. ketorolac tromethamine : An organoammonium salt resulting from the mixture of equimolar amounts of ketorolac and tromethamine (tris). It has potent non-sedating analgesic and moderate anti-inflammatory effects. It is used in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis.		2.0310organoammonium saltanalgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor
clarithromycin
Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis.		2.0210macrolide antibioticantibacterial drug;
environmental contaminant;
protein synthesis inhibitor;
xenobiotic
methionine sulfoximine
L-methionine sulfoximine : A methionine sulfoximine in which the amino group has S-stereochemistry.		2.0310L-alpha-amino acid zwitterion;
L-methionine derivative;
methionine sulfoximine;
non-proteinogenic L-alpha-amino acid		EC 6.3.1.2 (glutamate--ammonia ligase) inhibitor;
geroprotector
tretazicar
tretazicar: minor descriptor (75-84); on-line & Index Medicus search AZIRIDINES (75-84)		2.0310
nicotine
(S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.		2.02103-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
carbetapentane citrate
[no description available]		2.0310carbonyl compound
moexipril
[no description available]		2.0210peptide
phentolamine mesylate
[no description available]		2.0310
mephentermine
sphinganine : A 2-aminooctadecane-1,3-diol having (2S,3R)-configuration.		2.03102-aminooctadecane-1,3-diolEC 2.7.11.13 (protein kinase C) inhibitor;
human metabolite;
mouse metabolite
oxybutynin hydrochloride
[no description available]		2.0310hydrochloride
nimustine
nimustine hydrochloride : A hydrochloride obtained by combining nimustine with one equivalent of hydrochloric acid. An antineoplastic agent especially effective against malignant brain tumors.		2.0310hydrochlorideantineoplastic agent
cordium
bepridil hydrochloride monohydrate : The hydrochloride monohydrate of bepridril.		2.0310hydrate;
hydrochloride
L-2-aminoadipic acid
L-2-aminoadipic acid : The L-enantiomer of 2-aminoadipic acid.		2.03102-aminoadipic acidEscherichia coli metabolite;
human metabolite
prilocaine hydrochloride
prilocaine hydrochloride : The monohydrochloride salt of prilocaine.		2.0310hydrochloridelocal anaesthetic
mor-14
N-methyldeoxynojirimycin: glucosidase inhibitor		2.0310hydroxypiperidine;
piperidine alkaloid;
tertiary amino compound		anti-HIV agent;
cardioprotective agent;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
plant metabolite
brexanolone
brexanolone: a mixture of allopregnanolone and sulfobutylether‐beta‐cyclodextrin for treatment of postpartum depression. brexanolone : A 3-hydroxy-5alpha-pregnan-20-one in which the hydroxy group at position 3 has alpha-configuration. It is a metabolite of the sex hormone progesterone and used for the treatment of postpartum depression in women.		2.03103-hydroxy-5alpha-pregnan-20-oneantidepressant;
GABA modulator;
human metabolite;
intravenous anaesthetic;
sedative
phenylisopropyladenosine
[no description available]		2.0310aromatic amine;
benzenes;
hydrocarbyladenosine;
purine nucleoside;
secondary amino compound		adenosine A1 receptor agonist;
neuroprotective agent
hexamethonium chloride
[no description available]		2.0310
6-(4-nitrobenzylthio)guanosine
6-(4-nitrobenzylthio)guanosine: inhibitor of nucleoside transport		2.0310
3-aminopropylphosphonic acid
3-aminopropylphosphonic acid: RN given refers to parent cpd; structure. (3-aminopropyl)phosphonic acid : A phosphonic acid in which the hydrogen attached to the phosphorus of phosphonic acid is substituted by a 3-aminopropyl group. It is a partial agonist of GABAB receptors.		2.0310phosphonic acids;
primary amino compound;
zwitterion		GABAB receptor agonist
5'-n-methylcarboxamideadenosine
5'-N-methylcarboxamideadenosine: RN given refers to (beta-D)-isomer		2.0310
3,7-dimethyl-1-propargylxanthine
3,7-dimethyl-1-propargylxanthine: potent & selective in vivo antagonist of adenosine analogs		2.0310
zpck
ZPCK: alkylates histidine residue at active center of bovine chymotrypsin		2.0310
n(6)-phenyladenosine
[no description available]		2.0310purine nucleoside
tetrahydrodeoxycorticosterone
tetrahydrodeoxycorticosterone: RN given refers to (3alpha,5beta)-isomer		2.031021-hydroxy steroid
n-methyladenosine
N-methyladenosine: is a inhibitor of cell differentiation. N(6)-methyladenosine : A methyladenosine compound with one methyl group attached to N(6) of the adenine nucleobase.		2.0310methyladenosine
fulvestrant
Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.		2.051017beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide		antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist
mizoribine
[no description available]		2.0310imidazolesanticoronaviral agent
1-amino-1,3-dicarboxycyclopentane
1-amino-1,3-dicarboxycyclopentane: RN given refers to (cis)-isomer		2.0310
u 73122
1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione: structure given in first source. U-73122 : An aza-steroid that is 3-O-methyl-17beta-estradiol in which the 17beta-hydroxy group is replaced by a 6-(maleimid-1-yl)hexylamino group. An inibitor of phospholipase C.		2.0310aromatic ether;
aza-steroid;
maleimides		EC 3.1.4.11 (phosphoinositide phospholipase C) inhibitor
alphaxalone
alphaxalone: RN given refers to (3alpha,5alpha)-isomer; structure		2.0310corticosteroid hormone
s-nitrosoglutathione
[no description available]		2.0310glutathione derivative;
nitrosothio compound		bronchodilator agent;
nitric oxide donor;
platelet aggregation inhibitor;
signalling molecule
cp-55,940
[no description available]		2.0310
vanoxerine
vanoxerine dihydrochloride : A hydrochloride salt that is obtained by reaction of vanoxerine with two equivalents of hydrogen chloride. Potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration.		2.0310hydrochloridedopamine uptake inhibitor
methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate
methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate: structure given in first source		2.0310beta-carbolines
u 69593
U 69593: selective ligand for opioid K-receptor. U69593 : A monocarboxylic acid amide obtained by formal condensation between the carboxy group of phenylacetic acid and the secodary amino group of (5R,7S,8S)-N-methyl-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-amine.		2.0310monocarboxylic acid amide;
N-alkylpyrrolidine;
organic heterobicyclic compound;
oxaspiro compound		anti-inflammatory agent;
diuretic;
kappa-opioid receptor agonist
cv 3988
CV 3988: platelet activating factor antagonist; structure given in first source		2.0310
beta-carboline-3-carboxylic acid methyl ester
beta-carboline-3-carboxylic acid methyl ester: structure given in first source		2.0310beta-carbolines
methoctramine
methoctramine: structure given in first source. methoctramine : A tetramine that is N,N'-bis(6-aminohexyl)octane-1,8-diamine where the primary amino groups both carry 2-methoxybenzyl substituents.. methoctramine tetrahydrochloride : A hydrochloride obtained by combining methoctramine with four molar equivalents of hydrochloric acid.		2.0310hydrochloridemuscarinic antagonist
hypotaurine
[no description available]		2.0310aminosulfinic acid;
zwitterion		human metabolite;
metabolite;
mouse metabolite
dihydrokainate
[no description available]		2.0310dicarboxylic acid
gabazine
[no description available]		2.0310
cl 218872
CL 218872: shows specific action on benzodiazepine receptors; structure		2.0310pyridazines;
ring assembly
betaxolol hydrochloride
betaxolol hydrochloride : The hydrochloride salt of betaxolol.		2.0310hydrochlorideantihypertensive agent;
beta-adrenergic antagonist
catechin
(+)-catechin monohydrate : The monohydrate of (+)-catechin.		2.0310hydrategeroprotector
1-(2-methoxyphenyl)-4-(4-(2-phthalimido)butyl)piperazine
NAN 190 hydrobromide : A hydrobromide obtained by reaction of NAN 190 with one equivalent of hydrobromic acid.		2.0310hydrobromideserotonergic antagonist
s-methylthiocitrulline
S-methylthiocitrulline: a nitric oxide synthase inhibitor; structure in first source. S-methyl-L-thiocitrulline : An L-arginine derivative in which the guanidino NH2 group of L-arginine is replaced by a methylsufanyl group.		2.0310imidothiocarbamic ester;
L-arginine derivative;
L-ornithine derivative;
non-proteinogenic L-alpha-amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
neuroprotective agent
dihydrocapsaicin
[no description available]		2.0310capsaicinoid
ml 9
[no description available]		2.0310
parthenolide
[no description available]		2.0310germacranolide
3',4'-dichlorobenzamil
3',4'-dichlorobenzamil: inhibits Na-Ca exchange in membrane vesicle & papillary muscle preparations from guinea pig heart		2.0310guanidines;
pyrazines
1-(carboxymethylthio)tetradecane
1-(carboxymethylthio)tetradecane: structure given in first source; alkylthio acetic acid, non-beta-oxidizable		2.0310straight-chain fatty acid
2-iodomelatonin
[no description available]		2.0310acetamides
arcaine, sulfate
[no description available]		2.0310
gr 113808
GR 113808: structure given in first source; a 5-HT(4) receptor antagonist: GR 125487 is the HCl salt. GR 113808 : An indolyl carboxylate ester obtained by formal condensation between the carboxy group of 1-methylindole-3-carboxylic acid with the hydroxy group of N-{2-[4-(hydroxymethyl)piperidin-1-yl]ethyl}methanesulfonamide.		2.0310indolyl carboxylate ester;
piperidines;
sulfonamide		serotonergic antagonist
gallopamil hydrochloride
[no description available]		2.0310
gamma-glutamylaminomethylsulfonic acid
[no description available]		2.0310
buthionine sulfoximine
L-buthionine-(S,R)-sulfoximine : A 2-amino-4-(S-butylsulfonimidoyl)butanoic acid which has S-configuration. It is a inhibitor of gamma-glutamylcysteine synthetase and glutathione (GSH) biosynthesis and is capable of enhancing the apoptotic effects of several chemotherapeutic agents.		2.03102-amino-4-(S-butylsulfonimidoyl)butanoic acidEC 6.3.2.2 (glutamate--cysteine ligase) inhibitor;
ferroptosis inducer
pramipexole
Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively.		2.1310benzothiazoles;
diamine		antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
radical scavenger
sb 204070a
SB 204070A: structure given in first source; a selective 5-HT(4) receptor antagonist		2.0310
1-(2-(4-aminophenyl)ethyl)-4-(3-trifluoromethylphenyl)piperazine
LY 165163: structure given in first source; a serotonin agonist. LY-165163 : A N-arylpiperazine that is piperazine substituted by 2-(4-aminophenyl)ethyl and 3-(trifluoromethyl)phenyl groups at positions 1 and 4, respectively. It is a selective 5-HT1A serotonin receptor agonist and 5-HT1D serotonin receptor antagonist.		2.0310(trifluoromethyl)benzenes;
N-alkylpiperazine;
N-arylpiperazine;
primary arylamine;
substituted aniline		geroprotector;
serotonergic agonist
l 655240
L 655240: thromboxane and prostaglandin endoperoxide receptor antagonist; structure given in first source; RN given is for parent cpd		2.0310methylindole
san 58035
[no description available]		2.0310
ici 89406
ICI 89406: RN given refers to parent cpd		2.0210ureas
nnc 711
NNC 711: structure in first source		2.0310
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-n,n-diethylbenzamide
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide: a highly-selective, nonpeptide delta opioid receptor agonist; structure given in first source		2.0310diarylmethane
e 64
E 64: cysteine protease inhibitor of microbial origin, which inhibits cathepsin B (EC 3.4.22.1) and cathepsin L (EC 3.4.22.-)		2.0310dicarboxylic acid monoamide;
epoxy monocarboxylic acid;
guanidines;
L-leucine derivative;
zwitterion		antimalarial;
antiparasitic agent;
protease inhibitor
azetidine-2,4-dicarboxylic acid
azetidine-2,4-dicarboxylic acid: activates neuronal metabotropic receptors; RN given refers to (trans-isomer); RN for cpd without isomeric designation not avail 10/93		2.0310
pre 084
2-(4-morpholino)ethyl-1-phenylcyclohexane-1-carboxylate: structure given in first source		2.0310morpholines
methotrexate
[no description available]		2.4320dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
1-(2-allylphenoxy)-3-((8-bromoacetylamino-4-menthane-1-yl)amino)-1-propanol
1-(2-allylphenoxy)-3-((8-bromoacetylamino-4-menthane-1-yl)amino)-1-propanol: irreversibly inactivates the dihydroalprenolol binding site; alprenolol analog; isopropylamino group of alprenolol replaced by 8-bromoacetylamino-1-amino-p-menthane moiety in the 1 position; structure given in first source		2.0310
sr 2640
SR 2640: leukotriene D4 and E4 antagonist		2.0310quinolines
ici 204448
[no description available]		2.0310
4-amino-1-(6-chloro-2-pyridyl)piperidine hydrochloride
4-amino-1-(6-chloro-2-pyridyl)piperidine hydrochloride: has high affinity and selectivity for 5-HT3 receptors; structure given in first source		2.0310
n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide
N,N-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide: binds with high affinity to glial mitochondrial diazepam binding inhibitor receptors & increases mitochondrial steroidogenesis		2.0310phenylindole
3,5-bis(trifluoromethyl)benzyl n-acetyltryptophan
3,5-bis(trifluoromethyl)benzyl N-acetyltryptophan: structure given in first source; substance P and neurokinin receptor antagonist		2.0310
8-cyclopentyl-3-(3-((4-(fluorosulfonyl)benzoyl)oxy)propyl)-1-propylxanthine
8-cyclopentyl-3-(3-((4-(fluorosulfonyl)benzoyl)oxy)propyl)-1-propylxanthine: structure given in first source		2.0310
l 741626
3-(4-(4-chlorophenyl-4-hydroxypiperidino)methyl)indole: structure in first source		2.0310piperidines
nisoxetine hydrochloride
[no description available]		2.0310
ng-nitroarginine methyl ester
N(gamma)-nitro-L-arginine methyl ester hydrochloride : A hydrochloride obtained by combining N(gamma)-nitro-L-arginine methyl ester with one equivalent of hydrochloric acid.		2.0310hydrochlorideEC 1.14.13.39 (nitric oxide synthase) inhibitor
tilarginine acetate
[no description available]		2.0310
alpha-guanidinoglutaric acid
alpha-guanidinoglutaric acid: identified in the convulsive period of cobalt-induced seizures from cat cerebral cortex; RN given for cpd with unspecified guanidino-locant		2.0310L-glutamic acid derivative
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(+-)-isomer
[no description available]		2.0310
imidazole-4-acetic acid hydrochloride
[no description available]		2.0310
docetaxel
[no description available]		2.0210hydrate;
secondary alpha-hydroxy ketone		antineoplastic agent
nsc-141549
[no description available]		2.0310
levofloxacin
Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.		2.02109-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
ezetimibe
Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).		3.3110azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
2-chloro-2-deoxyglucose
[no description available]		2.0310
idazoxan hydrochloride
[no description available]		2.0310
isoguvacine hydrochloride
[no description available]		2.0310
schizandrin a
schizandrin A: the major lignan, 2-9%, of Schisandra plant; has hepatoprotective, antioxidant, and antineoplastic activities		3.3110
cyanopindolol
[no description available]		2.1310indoles
8-methoxymethyl-3-isobutyl-1-methylxanthine
8-methoxymethyl-3-isobutyl-1-methylxanthine: inhibitor of phosphodiesterase I		2.0310oxopurine
naproxen
Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.		2.0210methoxynaphthalene;
monocarboxylic acid		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
cyc 202
seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.		2.03102,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
Serotonin hydrochloride
[no description available]		2.0310tryptamines
n-phthaloylglutamic acid
N-phthaloyl-L-glutamic acid : A glutamic acid derivative that is L-glutamic acid in which the two hydrogens on the amino group are substituted by a phthaloyl group.		2.0310L-glutamic acid derivative;
phthalimides
1,3-dipropyl-7-methylxanthine
1,3-dipropyl-7-methylxanthine: structure given in first source		2.0310
ag 3-5
icilin: a cooling compound that activates TRPM8		2.0310C-nitro compound
n-n-propylnorapomorphine
[no description available]		2.0310aporphine alkaloid
urapidil monohydrochloride
[no description available]		2.0310
aminopterin
Aminopterin: A folic acid derivative used as a rodenticide that has been shown to be teratogenic.		2.0310dicarboxylic acidEC 1.5.1.3 (dihydrofolate reductase) inhibitor;
mutagen
azepexole, dihydrochloride
[no description available]		2.0310
2,5-dimethoxy-4-iodoamphetamine hydrochloride
[no description available]		2.0310
abt 980
[no description available]		2.0310
sk&f 75670
SK&F 75670: RN refers to HBr; N-methyl derivative of SK&F 38393		2.0310
esatenolol
esatenolol : The (S)-enantiomer of atenolol.		2.0310atenololbeta-adrenergic antagonist
ropivacaine
Ropivacaine: An anilide used as a long-acting local anesthetic. It has a differential blocking effect on sensory and motor neurons.. ropivacaine : The piperidinecarboxamide obtained by the formal condensation of N-propylpipecolic acid and 2,6-dimethylaniline.. (S)-ropivacaine : A piperidinecarboxamide-based amide-type local anaesthetic (amide caine) in which (S)-N-propylpipecolic acid and 2,6-dimethylaniline are combined to form the amide bond.		2.0210piperidinecarboxamide;
ropivacaine		local anaesthetic
nbi 27914
[no description available]		2.0310dialkylarylamine;
tertiary amino compound
sb 216763
[no description available]		2.0310indoles;
maleimides
erlotinib
[no description available]		3.3110aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
(R)-atenolol
(R)-atenolol : The (R)-enantiomer of atenolol.		2.0310atenolol
memantine hydrochloride
[no description available]		2.0310hydrochlorideantidepressant;
antiparkinson drug;
dopaminergic agent;
neuroprotective agent;
NMDA receptor antagonist
sibenadet
sibenadet: structure in first source		2.7730
pefabloc
[no description available]		2.0310
pongidae
[no description available]		2.0310
succinylproline
[no description available]		2.0310N-acyl-amino acid
sb 205384
SB 205384: structure in first source		2.0310thienopyridine
hydrastine
[no description available]		2.0310isoquinolinesmetabolite
gabaculine hydrochloride
[no description available]		2.0310
etiron monohydrobromide
[no description available]		2.0310
bmy 7378
[no description available]		2.0310
vesamicol
[no description available]		2.0310
estradiol 3-benzoate
17beta-estradiol 3-benzoate : A benzoate ester resulting from the formal condensation of benzoic acid with the phenolic hydroxy group of 17beta-estradiol.		2.021017beta-hydroxy steroid;
benzoate ester		estrogen receptor agonist;
xenoestrogen
cortisone
[no description available]		2.031011-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		human metabolite;
mouse metabolite
vincristine sulfate
[no description available]		2.0310organic sulfate saltantineoplastic agent;
geroprotector
estramustine
Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid.		2.021017beta-hydroxy steroid;
carbamate ester;
organochlorine compound		alkylating agent;
antineoplastic agent;
radiation protective agent
lupeol
[no description available]		3.3110pentacyclic triterpenoid;
secondary alcohol		anti-inflammatory drug;
plant metabolite
n-methylserotonin oxalate salt
[no description available]		2.0310
nsc 95397
[no description available]		2.03101,4-naphthoquinones
wortmannin
[no description available]		2.0310acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		2.02101,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
lithium chloride
Lithium Chloride: A salt of lithium that has been used experimentally as an immunomodulator.. lithium chloride : A metal chloride salt with a Li(+) counterion.		2.0310inorganic chloride;
lithium salt		antimanic drug;
geroprotector
canavanine
L-canavanine : A non-proteinogenic L-alpha-amino acid that is L-homoserine substituted at oxygen with a guanidino (carbamimidamido) group. Although structurally related to L-arginine, it is non-proteinogenic.		2.0310amino acid zwitterion;
non-proteinogenic L-alpha-amino acid		phytogenic insecticide;
plant metabolite
naringenin
(S)-naringenin : The (S)-enantiomer of naringenin.		3.3110(2S)-flavan-4-one;
naringenin		expectorant;
plant metabolite
5-hydroxytryptophan
hydroxytryptophan : A hydroxy-amino acid that is tryptophan substituted by at least one hydroxy group at unspecified position.. 5-hydroxy-L-tryptophan : The L-enantiomer of 5-hydroxytryptophan.		2.03105-hydroxytryptophan;
amino acid zwitterion;
hydroxy-L-tryptophan;
non-proteinogenic L-alpha-amino acid		human metabolite;
mouse metabolite;
plant metabolite
ouabain
Ouabain: A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE.. cardiac glycoside : Steroid lactones containing sugar residues that act on the contractile force of the cardiac muscles.. ouabain : A steroid hormone that is a multi-hydroxylated alpha-L-rhamnosyl cardenoloide. It binds to and inhibits the plasma membrane Na(+)/K(+)-ATPase (sodium pump). It has been isolated naturally from Strophanthus gratus.		2.031011alpha-hydroxy steroid;
14beta-hydroxy steroid;
5beta-hydroxy steroid;
alpha-L-rhamnoside;
cardenolide glycoside;
steroid hormone		anti-arrhythmia drug;
cardiotonic drug;
EC 2.3.3.1 [citrate (Si)-synthase] inhibitor;
EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
ion transport inhibitor;
plant metabolite
tosylphenylalanyl chloromethyl ketone
Tosylphenylalanyl Chloromethyl Ketone: An inhibitor of Serine Endopeptidases. Acts as alkylating agent and is known to interfere with the translation process.. N-tosyl-L-phenylalanyl chloromethyl ketone : The N-tosyl derivative of L-phenylalanyl chloromethyl ketone.		2.0310alpha-chloroketone;
sulfonamide		alkylating agent;
serine proteinase inhibitor
pentostatin
Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia.		2.0210coformycinsantimetabolite;
antineoplastic agent;
Aspergillus metabolite;
bacterial metabolite;
EC 3.5.4.4 (adenosine deaminase) inhibitor
monoiodotyrosine
Monoiodotyrosine: A product from the iodination of tyrosine. In the biosynthesis of thyroid hormones (THYROXINE and TRIIODOTHYRONINE), tyrosine is first iodized to monoiodotyrosine.. iodotyrosine : A tyrosine derivative which has at least one iodo-substituent on the benzyl moiety.. monoiodotyrosine : An iodotyrosine carrying a single iodo substituent.. 3-iodo-L-tyrosine : The monoiodotyrosine that is L-tyrosine carrying an iodo-substituent at position C-3 of the benzyl group.		2.0310amino acid zwitterion;
L-tyrosine derivative;
monoiodotyrosine;
non-proteinogenic L-alpha-amino acid		EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor;
human metabolite;
mouse metabolite
nitroarginine
Nitroarginine: An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6). N(gamma)-nitro-L-arginine : An L-arginine derivative that is L-arginine in which the terminal nitrogen of the guanidyl group is replaced by a nitro group.		2.0310guanidines;
L-arginine derivative;
N-nitro compound;
non-proteinogenic L-alpha-amino acid
willardiine
willardiine: isolated from seeds of Acacia willariana; structure. 3-(uracil-1-yl)-L-alanine : The 3-(uracil-1-yl) derivative of L-alanine.		2.0310amino acid zwitterion;
L-alanine derivative;
non-proteinogenic L-alpha-amino acid
cortodoxone
Cortodoxone: 17,21-Dihydroxypregn-4-ene-3,20-dione. A 17-hydroxycorticosteroid with glucocorticoid and anti-inflammatory activities.. 11-deoxycortisol : A deoxycortisol that is cortisol in which the hydroxy group at position 11 has been replaced by a hydrogen.		2.0310deoxycortisol;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		human metabolite;
mouse metabolite
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		2.0210cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
meropenem
Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.		2.0210alpha,beta-unsaturated monocarboxylic acid;
carbapenemcarboxylic acid;
organic sulfide;
pyrrolidinecarboxamide		antibacterial agent;
antibacterial drug;
drug allergen
griseofulvin
Griseofulvin: An antifungal agent used in the treatment of TINEA infections.. griseofulvin : An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment.		2.02101-benzofurans;
antibiotic antifungal drug;
benzofuran antifungal drug;
organochlorine compound;
oxaspiro compound		antibacterial agent;
Penicillium metabolite
cefoxitin
Cefoxitin: A semisynthetic cephamycin antibiotic resistant to beta-lactamase.. cefoxitin : A semisynthetic cephamycin antibiotic which, in addition to the methoxy group at the 7alpha position, has 2-thienylacetamido and carbamoyloxymethyl side-groups. It is resistant to beta-lactamase.		2.0210beta-lactam antibiotic allergen;
cephalosporin;
cephamycin;
semisynthetic derivative		antibacterial drug
saquinavir
Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.		2.0210L-asparagine derivative;
quinolines		antiviral drug;
HIV protease inhibitor
netilmicin
Netilmicin: Semisynthetic 1-N-ethyl derivative of SISOMYCIN, an aminoglycoside antibiotic with action similar to gentamicin, but less ear and kidney toxicity.		2.0210
amiodarone hydrochloride
[no description available]		2.0310aromatic ketone
dicyclomine hydrochloride
dicyclomine hydrochloride : The hydrochloride salt of dicyclomine. An anticholinergic, it is used to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome.		2.0310hydrochlorideantispasmodic drug;
muscarinic antagonist
metyrosine
alpha-methyl-L-tyrosine : An L-tyrosine derivative that consists of L-tyrosine bearing an additional methyl substituent at position 2. An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma.		2.4320L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		antihypertensive agent;
EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor
rocuronium bromide
rocuronium bromide : The organic bromide salt of a 5alpha androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents.		2.0210organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent
nortriptyline hydrochloride
[no description available]		2.0310organic tricyclic compoundgeroprotector
paromomycin sulfate
paromomycin sulfate : An aminoglycoside sulfate salt resulting from the treatment of paromomycin with sulfuric acid. A broad-spectrum antibiotic, it is used for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis.		2.0310
terconazole
terconazole: structure & RN for (cis)-isomer from first source. terconazole : A racemate consisting of equimolar amounts of (2R,4S)- and (2S,4R)-terconazole. It has broad-spectrum antifungal activitiy and is used for the treatment of vaginal yeast infections (Candida).. (2R,4S)-terconazole : A 1-(4-{[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)-4-isopropylpiperazine in which positions 2 and 4 of the 1,3-dioxolane moiety have R and S configuration, respectively.		2.02101-(4-{[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)-4-isopropylpiperazine
bacampicillin
bacampicillin: ester prodrug that is hydrolyzed to ampicillin after its absorption from the gastrointestinal tract; RN given refers to parent cpd; structure. bacampicillin : A penicillanic acid ester that is the 1-ethoxycarbonyloxyethyl ester of ampicillin. It is a semi-synthetic, microbiologically inactive prodrug of ampicillin.		2.0210penicillanic acid esterprodrug
Dubinidine
[no description available]		2.0310organic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
cyclopamine
[no description available]		2.0310piperidinesglioma-associated oncogene inhibitor
s-(4-azidophenacyl)glutathione
S-(4-azidophenacyl)glutathione: photoaffinity label deriv of glutathione; inhibits glyoxalase I (EC 4.4.1.5)		2.0310peptide
hydroxylamine hydrochloride
[no description available]		2.0310organic molecular entity
L-isoprenaline
L-isoprenaline : An optically active phenylethanolamine compound having an isopropyl substituent attached to the nitrogen atom.		2.5420catecholamine;
phenylethanolamines		beta-adrenergic agonist;
sympathomimetic agent
sb 228357
SB 228357: a neuroleptic with equivalent or higher antagonist affinity for 5-HT2 than for dopamine D2 receptor		2.0310indolyl carboxylic acid
3,5-dihydroxyphenylglycine
(S)-3,5-dihydroxyphenylglycine : A glycine derivative that is L-alpha-phenylglycine substituted at positions 3 and 5 on the phenyl ring by hydroxy groups.		2.0310amino acid zwitterion;
non-proteinogenic L-alpha-amino acid;
resorcinols
actinonin
actinonin: natural hydroxamic acid, pseudopeptide antibiotic isolated from Streptomyces species; structure		2.0310
1-O-Acetyllycorine
1-acetyllycorine: has antiviral activity; structure in first source		3.3110alkaloid
dironyl
dironyl: pronounced antifertility agent in rats; lactation suppressor in other species; serotonin antagonist; RN given refers to parent cpd; structure		2.0210organic molecular entity
erythromycin ethylsuccinate
Erythromycin Ethylsuccinate: A macrolide antibiotic, produced by Streptomyces erythreus. This compound is an ester of erythromycin base and succinic acid. It acts primarily as a bacteriostatic agent. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin ethylsuccinate : A erythromycin derivative that is erythromycin A in which the hydroxy group at position 3R is substituted by a (4-ethoxy-4-oxobutanoyl)oxy group. It is used for the treatment of a wide variety of bacterial infections.		2.0210cyclic ketone;
erythromycin derivative;
ethyl ester;
succinate ester
vinpocetine
vinpocetine: whole issue of Arzneim Forsch (23 articles) discuss this drug; Arzneim Forsch 26(10a);1976; RN given refers to parent cpd with unspecified isomeric designation		2.0310alkaloidgeroprotector
amcinonide
amcinonide: structure		2.021011beta-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
acetate ester;
corticosteroid;
fluorinated steroid;
spiroketal		anti-inflammatory drug
betamethasone acetate
[no description available]		2.021011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
acetate ester;
fluorinated steroid;
steroid ester;
tertiary alpha-hydroxy ketone
darifenacin
darifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence.		2.47201-benzofurans;
monocarboxylic acid amide;
pyrrolidines		antispasmodic drug;
muscarinic antagonist
dihydroergocristine monomesylate
dihydroergocristine mesylate : The methanesulfonic acid salt of dihydroergocristine. It has been used as the for the symptomatic treatment of mental deterioration associated with cerebrovascular insufficiency and in peripheral vascular disease. It is also a component of ergoloid mesylate (codergocrine mesilate), a mixture of ergot alkaloid derivatives that is used as a vasodilator and has shown mild benefits in the treatment of vascular dementia.		2.0310methanesulfonate saltalpha-adrenergic antagonist;
geroprotector;
vasodilator agent
acarbose
[no description available]		2.0210amino cyclitol;
glycoside
tretinoin
Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.		2.4320retinoic acid;
vitamin A		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		2.0310resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
oleic acid
Oleic Acid: An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed). oleic acid : An octadec-9-enoic acid in which the double bond at C-9 has Z (cis) stereochemistry.		2.0310octadec-9-enoic acidantioxidant;
Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
Escherichia coli metabolite;
mouse metabolite;
plant metabolite;
solvent
thapsigargin
Thapsigargin: A sesquiterpene lactone found in roots of THAPSIA. It inhibits SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES.. thapsigargin : An organic heterotricyclic compound that is a hexa-oxygenated 6,7-guaianolide isolated fron the roots of Thapsia garganica L., Apiaceae. A potent skin irritant, it is used in traditional medicine as a counter-irritant. Thapsigargin inhibits Ca(2+)-transporting ATPase mediated uptake of calcium ions into sarcoplasmic reticulum and is used in experimentation examining the impacts of increasing cytosolic calcium concentrations.		2.0310butyrate ester;
organic heterotricyclic compound;
sesquiterpene lactone		calcium channel blocker;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
mycophenolic acid
Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases.		2.02102-benzofurans;
gamma-lactone;
monocarboxylic acid;
phenols		anticoronaviral agent;
antimicrobial agent;
antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
environmental contaminant;
immunosuppressive agent;
mycotoxin;
Penicillium metabolite;
xenobiotic
mupirocin
Mupirocin: A topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing.. mupirocin : An alpha,beta-unsaturated ester resulting from the formal condensation of the alcoholic hydroxy group of 9-hydroxynonanoic acid with the carboxy group of (2E)-4-[(2S)-tetrahydro-2H-pyran-2-yl]-3-methylbut-2-enoic acid in which the tetrahydropyranyl ring is substituted at positions 3 and 4 by hydroxy groups and at position 5 by a {(2S,3S)-3-[(2S,3S)-3-hydroxybutan-2-yl]oxiran-2-yl}methyl group. Originally isolated from the Gram-negative bacterium Pseudomonas fluorescens, it is used as a topical antibiotic for the treatment of Gram-positive bacterial infections.		2.0210alpha,beta-unsaturated carboxylic ester;
epoxide;
monocarboxylic acid;
oxanes;
secondary alcohol;
triol		antibacterial drug;
bacterial metabolite;
protein synthesis inhibitor
brivudine
brivudine: anti-herpes agent		2.0310
5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol
5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol: estrogen receptor ligand; structure in first source. (R,R)-5,11-diethyl-5,6,11,12-tetrahydro-2,8-chrysenediol : A carbotetracyclic compound that is 5,6,11,12-tetrahydrochrysene substituted by hydroxy groups at positions 2 and 8 and by ethyl groups at positions 5 and 11 (the 5R,11R-stereoisomer). It is an agonist of ER-alpha and antagonist of ER-beta receptors.		2.0310carbotetracyclic compound;
polyphenol		estrogen receptor agonist;
estrogen receptor antagonist;
geroprotector;
neuroprotective agent
fosfomycin
Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus.		2.0210epoxide;
phosphonic acids		antimicrobial agent;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		2.0210macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
2-amino-3-(5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl)propionic acid
2-amino-3-(5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl)propionic acid: structure in first source		2.0310
adenosine-5'-(n-ethylcarboxamide)
Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.. N-ethyl-5'-carboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group.		2.0310adenosines;
monocarboxylic acid amide		adenosine A1 receptor agonist;
adenosine A2A receptor agonist;
antineoplastic agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
L-cycloserine
L-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has S configuration. An antibiotic isolated from Erwinia uredovora.		2.03104-amino-1,2-oxazolidin-3-oneanti-HIV agent;
anticonvulsant;
EC 2.3.1.50 (serine C-palmitoyltransferase) inhibitor
1,4-dideoxy-1,4-imino-d-arabinitol
[no description available]		2.0310
teniposide
[no description available]		2.0210aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
purvalanol a
6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer;		2.0310purvalanol
cefamandole
Cefamandole: Semisynthetic wide-spectrum cephalosporin with prolonged action, probably due to beta-lactamase resistance. It is used also as the nafate.. cefamandole : A cephalosporin compound having (R)-mandelamido and N-methylthiotetrazole side-groups.		2.0210cephalosporin;
semisynthetic derivative		antibacterial drug
dactinomycin
Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)		2.0210actinomycinmutagen
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		2.4320L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
posaconazole
[no description available]		3.3110aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles		trypanocidal drug
sch 22219
alclometasone dipropionate : A prednisolone compound having an alpha-chloro substituent at the 7-position, an alpha-methyl substituent at the 16-position and O-propanoyl groups at the 17- and 21-positions.		2.021011beta-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
chlorinated steroid;
glucocorticoid;
propanoate ester;
steroid ester		anti-inflammatory drug
carbenoxolone
[no description available]		3.3110
citral
citral: Xref geranial: geraniol is also available; Xref neral: nerol is also available; vitamin A antagonist; oxygenated monoterpene; inhibits cytosolic dehydrogenases; structure. citral : An enal that consists of octa-2,6-dienal bearing methyl substituents at positions 3 and 7. A mixture of the two geometric isomers geranial and neral, it is the major constituent (75-85%) of oil of lemon grass, the volatile oil of Cymbopogon citratus, or of C. flexuosus. It also occurs in oils of verbena, lemon, and orange.		3.3110enal;
monoterpenoid;
polyprenal		plant metabolite;
volatile oil component
isoliquiritigenin
[no description available]		2.0310chalconesantineoplastic agent;
biological pigment;
EC 1.14.18.1 (tyrosinase) inhibitor;
GABA modulator;
geroprotector;
metabolite;
NMDA receptor antagonist
rauwolscine
Rauwolscine: A stereoisomer of yohimbine.		2.0310methyl 17-hydroxy-20xi-yohimban-16-carboxylate
gw9662
2-chloro-5-nitrobenzanilide: pretreatment of peroxisome proliferator activated receptors with GW9662 results in the irreversible loss of ligand binding		2.0310benzamides
calmidazolium
calmidazolium chloride : The organic choride salt of calmidazolium.		2.0310organic chloride saltapoptosis inducer;
calmodulin antagonist
mezlocillin
Mezlocillin: Semisynthetic ampicillin-derived acylureido penicillin. It has been proposed for infections with certain anaerobes and may be useful in inner ear, bile, and CNS infections.. mezlocillin : A penicillin in which the substituent at position 6 of the penam ring is a (2R)-2-[3-(methanesulfonyl)-2-oxoimidazolidine-1-carboxamido]-2-phenylacetamido group.		2.0210penicillin allergen;
penicillin		antibacterial drug
lanatoside c
lanatoside C: RN given refers to (3beta,5beta,12beta)-isomer		3.3110
cholinophyllin
[no description available]		2.0210
tropisetron hydrochloride
[no description available]		2.0310
Reactive blue 2
[no description available]		2.0310anthraquinone
5,6-dichloro-1-ethyl-1,3-dihydro-2h-benzimidazol-2-one
5,6-dichloro-1-ethyl-1,3-dihydro-2H-benzimidazol-2-one: stimulates Cl- secretion in the mouse jejunum		2.0310dichlorobenzene
quinidine sulfate
[no description available]		2.0310
fludarabine
[no description available]		2.0210purine nucleoside
propylthiouracil
Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group.		2.0210pyrimidinethioneantidote to paracetamol poisoning;
antimetabolite;
antioxidant;
antithyroid drug;
carcinogenic agent;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
hormone antagonist
ipratropium bromide anhydrous
[no description available]		2.4320
ipratropium
[no description available]		2.1110
methamilane methiodide
[no description available]		2.0310
pilocarpine nitrate
[no description available]		2.0310
r 59949
R 59949: diacylglycerol kinase inhibitor		2.0310diarylmethane
n(6)-cyclopentyladenosine
[no description available]		2.0310
methylatropine nitrate
[no description available]		2.0310
chlorprothixene
Chlorprothixene: A thioxanthine with effects similar to the phenothiazine antipsychotics.. (Z)-chlorprothixene : A chlorprothixene in which the double bond adopts a (Z)-configuration.		2.0210chlorprothixene
etomidate
Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity.		2.0210ethyl ester;
imidazoles		intravenous anaesthetic;
sedative
mercaptopurine
Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis.		2.0210aryl thiol;
purines;
thiocarbonyl compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent
sb 366791
N-(3-methoxyphenyl)-4-chlorocinnamanilide: a TRPV1 antagonist; structure in first source		2.0310
ag-213
tyrphostin 47: inhibits protein-tyrosine kinase activity of EGF-R both in vitro and in living cells;		2.0310
3,3',4,5'-tetrahydroxystilbene
3,3',4,5'-tetrahydroxystilbene: demethyl derivative of isorhapontigenin; structure in first source; a Syk kinase inhibitor; found in heartwood of FABACEAE; inhibitor of photosynthesis in spinach chloroplasts; may be inhibitor of plant growth; RN given refers to (E)-isomer. piceatannol : A stilbenol that is trans-stilbene in which one of the phenyl groups is substituted by hydroxy groups at positions 3 and 4, while the other phenyl group is substituted by hydroxy groups at positions 3 and 5.		2.0310catechols;
polyphenol;
resorcinols;
stilbenol		antineoplastic agent;
apoptosis inducer;
geroprotector;
hypoglycemic agent;
plant metabolite;
protein kinase inhibitor;
tyrosine kinase inhibitor
bemesetron
[no description available]		2.0310
(S)-(-)-pindolol
[no description available]		2.0310pindolol
levosulpiride
(S)-(-)-sulpiride : An optically active form of sulpiride having (S)-configuration. The active enantiomer of the racemic drug sulpiride. Selective D2-like dopamine antagonist (Ki values are ~ 0.015. ~ 0.013, 1, ~ 45 and ~ 77 muM at D2, D3, D4, D1 and D5 receptors respectively).		2.0310sulpirideantidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
caffeic acid
trans-caffeic acid : The trans-isomer of caffeic acid.		2.0310caffeic acidgeroprotector;
mouse metabolite
4-fluorophenyl-L-alanine
4-fluorophenyl-L-alanine : A L-phenylalanine derivative that is L-phenylalanine in which the hydrogen at position 4 on the benzene ring is replaced by a fluoro group.		2.03104-fluorophenylalanine;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid
urocanic acid
Urocanic Acid: 4-Imidazoleacrylic acid.. urocanic acid : An alpha,beta-unsaturated monocarboxylic acid that is prop-2-enoic acid substituted by a 1H-imidazol-4-yl group at position 3. It is a metabolite of hidtidine.. trans-urocanic acid : A urocanic acid in which the double bond of the carboxyethene moiety has E configuration.		2.0310urocanic acidhuman metabolite
cotinine
Cotinine: The N-glucuronide conjugate of cotinine is a major urinary metabolite of NICOTINE. It thus serves as a biomarker of exposure to tobacco SMOKING. It has CNS stimulating properties.. (-)-cotinine : An N-alkylpyrrolidine that consists of N-methylpyrrolidinone bearing a pyridin-3-yl substituent at position C-5 (the 5S-enantiomer). It is an alkaloid commonly found in Nicotiana tabacum.		2.0310N-alkylpyrrolidine;
pyridines;
pyrrolidin-2-ones;
pyrrolidine alkaloid		antidepressant;
biomarker;
human xenobiotic metabolite;
plant metabolite
thiothixene
[no description available]		2.4220N-methylpiperazineanticoronaviral agent
curcumin
Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.		3.3110aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
benztropine
Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.. benzatropine : Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments.		2.0210diarylmethane
cinnarizine
Cinnarizine: A piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.		2.0310diarylmethane;
N-alkylpiperazine;
olefinic compound		anti-allergic agent;
antiemetic;
calcium channel blocker;
geroprotector;
H1-receptor antagonist;
histamine antagonist;
muscarinic antagonist
sulindac
Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.		2.4320monocarboxylic acid;
organofluorine compound;
sulfoxide		analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent
enclomiphene
Enclomiphene: The trans or (E)-isomer of clomiphene.		2.0210
terbinafine
[no description available]		2.0210acetylenic compound;
allylamine antifungal drug;
enyne;
naphthalenes;
tertiary amine		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
P450 inhibitor;
sterol biosynthesis inhibitor
cysteine sulfinic acid
3-sulfino-L-alanine : The organosulfinic acid arising from oxidation of the sulfhydryl group of L-cysteine.		2.0310organosulfinic acid;
S-substituted L-cysteine		Escherichia coli metabolite;
human metabolite;
metabotropic glutamate receptor agonist;
mouse metabolite
d-ap7
[no description available]		2.0310
thioguanine anhydrous
Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia.		2.02102-aminopurinesanticoronaviral agent;
antimetabolite;
antineoplastic agent
(1R,2S)-tranylcypromine hydrochloride
(1R,2S)-tranylcypromine hydrochloride : A hydrochloride obtained by combining (1R,2S)-tranylcypromine with one equivalent of hydrochloric acid.		2.0310hydrochloride
tacrine hydrochloride
[no description available]		2.0310
4-bromotetramisole, oxalate (1:1), salt(s)-isomer
[no description available]		2.0310
succimer
Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.. succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning.		2.0210dicarboxylic acid;
dithiol;
sulfur-containing carboxylic acid		chelator
3-hydroxybenzylhydrazine hydrochloride
[no description available]		2.0310
1-(3-chlorophenyl)biguanide hydrochloride
[no description available]		2.0310
4-chlorophenylalanine methyl ester, hydrochloride, (dl)-isomer
[no description available]		2.0310
streptozocin
[no description available]		2.0210
capsazepine
capsazepine: modified capsaicin molecule; a capsaicin receptor antagonist. capsazepine : A benzazepine that is 2,3,4,5-tetrahydro-1H-2-benzazepine which is substituted by hydroxy groups at positions 7 and 8 and on the nitrogen atom by a 2-(p-chlorophenyl)ethylaminothiocarbonyl group. A synthetic analogue of capsaicin, it was the first reported capsaicin receptor antagonist.		2.0310benzazepine;
catechols;
monochlorobenzenes;
thioureas		capsaicin receptor antagonist
diphenyleneiodium chloride
dibenziodolium chloride : An organic chloride salt having dibenziodolium as the counterion.		2.0310organic chloride saltEC 1.6.3.1. [NAD(P)H oxidase (H2O2-forming)] inhibitor;
G-protein-coupled receptor agonist
azetidine-2,4-dicarboxylic acid, (cis)-isomer
[no description available]		2.0310
tamoxifen citrate
[no description available]		2.0310citrate saltangiogenesis inhibitor;
anticoronaviral agent
tamoxifen
[no description available]		2.0210stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
pimagedine hydrochloride
[no description available]		2.0310
Betaine Aldehyde Chloride
[no description available]		2.0310quaternary ammonium salt
ethionamide
Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide.		2.0210pyridines;
thiocarboxamide		antilipemic drug;
antitubercular agent;
fatty acid synthesis inhibitor;
leprostatic drug;
prodrug
eskazine
[no description available]		2.0310
monastrol
monastrol: stops mitosis by fostering formation of monopolar spindles; structure in first source. (S)-monastrol : An ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate that has S configuration.. monastrol : A racemate comprising equimolar amounts of R- and S-monastrol.. ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate : A member of the class of thioureas that is 3,4-dihydropyrimidine-2(1)-thione substituted by a 3-hydroxyphenyl group at position 4, an ethoxycarbonyl group at position 5, and a methyl group at position 6.		2.0310enoate ester;
ethyl ester;
phenols;
racemate;
thioureas		antileishmanial agent;
antimitotic;
antineoplastic agent;
EC 3.5.1.5 (urease) inhibitor
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.0310aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
4-diphenylacetoxy-n-methylpiperidine methiodide
4-DAMP methiodide : A quaternary ammonium salt obtained by combining equimolar amounts of 4-diphenylacetoxy-N-methylpiperidine and iodomethane.		2.0310iodide salt;
quaternary ammonium salt		cholinergic antagonist;
muscarinic antagonist
dezocine
dezocine: potent analgesic; RN given refers to ((5R-(5alpha,11alpha,13S*)))-isomer (dezocin); structure. dezocine : (7S,8S)-7-Amino-8-methyl-5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogen at position 8 and one of the hydrogens at position 6 are substituted by each end of a tetramethylene bridge. A synthetic opioid analgesic, it has mixed opiod agonist and antagonist properties. Although it is used for pain management, it can produce opioid withdrawal syndrome in patients already dependent on other opioids, and its clinical application is limited by side effects such as dizziness.		2.0210phenols;
primary amino compound		opioid analgesic
dapiprazole
[no description available]		2.0210N-alkylpiperazine;
N-arylpiperazine;
pyridines		alpha-adrenergic antagonist;
antipsychotic agent;
miotic;
ophthalmology drug
quinine
[no description available]		3.3110cinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
1-(4-hydroxybenzyl)imidazole-2-thiol
1-(4-hydroxybenzyl)imidazole-2-thiol: RN & structure given in first source; RN not in Chemline 3/87		2.0310
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide
2-chloro-N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide: structure given in first source		2.0310
hirsutine
[no description available]		3.3110
bp 897
BP 897: a dopamine D3 receptor agonist; structure in first source		2.0310naphthalenecarboxamide
trequinsin hydrochloride
[no description available]		2.0310
neboglamine
neboglamine: potential memory enhancer		2.0310
arformoterol
arformoterol : An N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamide in which both of the stereocentres have R configuration. The active enantiomer of formoterol, it is administered by inhalation (generally as the tartrate salt) as a direct-acting sympathomimetic and bronchodilator for the treatment of chronic obstructive pulmonary disease (any progressive respiratory disease that makes it harder to breathe over time, such as chronic bronchitis and emphysema).		3.8630N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamideanti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent
benzatropine methanesulfonate
benzatropine mesylate : The methanesulfonate salt of benzatropine. An acetylcholine receptor antagonist, it is used in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments.		2.0310
sb 203186
[no description available]		2.0310indolyl carboxylic acid
n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea
N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a 5-HT(2B) receptor antagonist; structure given in first source. 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea : A member of ther class of ureas that is urea in which a hydrogen attached to one of the nitrogens has been replaced by an N-methylindol-5-yl group, while a hydrogen attached to the other nitrogen has been replaced by a 3-methyl-1,2-thiazol-5-yl group. It is a potent and selective antagonist for the 5-hydroxytryptamine 2B (5-HT2B) receptor.		2.03101,2-thiazoles;
indoles;
ureas		receptor modulator;
serotonergic antagonist
gw 7647
GW 7647: a PPAR-alpha agonist; structure in first source. GW 7647 : A monocarboxylic acid that is 2-(phenylsulfanyl)isobutyric acid in which the phenyl group is substituted at the para- position by a 3-aza-7-cyclohexylhept-1-yl group in which the nitrogen is acylated by a (cyclohexylamino)carbonyl group.		2.0310aryl sulfide;
monocarboxylic acid;
ureas		PPARalpha agonist
ro 41-0960
[no description available]		2.0310
cgp 13501
CGP 13501: structure in first source		2.0310alkylbenzene
n-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide
N-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide: dopamine D4 ligand; structure in first source		2.0310
brl 15572
3-[4-(3-chlorophenyl)piperazin-1-yl]-1,1-diphenylpropan-2-ol : An N-alkylpiperazine that is 1-(3-chlorophenyl)piperazine carrying a 3,3-diphenyl-2-hydroxyprop-1-yl group at position 4. A selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.		2.0310monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
secondary alcohol		geroprotector;
serotonergic antagonist
mrs 1523
2,3-diethyl-4,5-dipropyl-6-phenylpyridine-3-thiocarboxylate-5-carboxylate: adenosine A3 receptor antagonist		2.0310
or486
OR486: structure given in first source		2.0310
fg 9041
FG 9041: structure given in first source		2.0310quinoxaline derivative
iik7
IIK7: structure in first source		2.0310
sb 415286
3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione: a glycogen synthase kinase-3 inhibitor; structure in first source		2.0310C-nitro compound;
maleimides;
monochlorobenzenes;
phenols;
secondary amino compound;
substituted aniline		antioxidant;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent
dm 235
DM 235: structure in first source		2.0310
jhw 015
[no description available]		2.0310indolecarboxamide
bw 723c86
[no description available]		2.0310tryptamines
sc 560
SC560 : A member of the class of pyrazoles that is 1H-pyrazole which is substituted at positions 1, 3 and 5 by 4-methoxyphenyl, trifluoromethyl and 4-chlorophenyl groups, respectively. Unlike many members of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors, SC-560 is selective for COX-1.		2.0310aromatic ether;
monochlorobenzenes;
organofluorine compound;
pyrazoles		angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 1 inhibitor;
non-steroidal anti-inflammatory drug
sc-19220
[no description available]		2.0310aromatic ether
le 300
[no description available]		2.0310indoles
flosequinan
[no description available]		2.0210quinolines
ly 367265
LY 367265: a 5-hydroxytryptamine transporter inhibitor; a 5-HT(2A) receptor antagonist; structure in first source. LY-367,265 : A fluoroindole that is 1H-indole in which the hydrogens at positions 3 and 6 are replaced by 1-[2-(2,2-dioxo-5,6-dihydro-4H-2lambda(6)-[1,2,5]thiadiazolo[4,3,2-ij]quinolin-1(2H)-yl)ethyl]-1,2,3,6-tetrahydropyridin-4-yl and fluoro groups, respectively. It is an inhibitor of the 5-hydroxytryptamine transporter (Ki = 2.3 nM) and an antagonist of 5-hydroxytryptamine(2A) receptor (Ki = 0.81 nM).		2.0310dihydropyridine;
fluoroindole;
tertiary amino compound;
thiadiazoloquinoline		antidepressant;
geroprotector;
serotonergic antagonist;
serotonin uptake inhibitor
tolcapone
Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase.		3.31102-nitrophenols;
benzophenones;
catechols		antiparkinson drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
diclofenac sodium
Diclofenac Sodium: The sodium form of DICLOFENAC. It is used for its analgesic and anti-inflammatory properties.. diclofenac sodium : The sodium salt of diclofenac.		2.0310organic sodium salt
cgp 7930
2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)phenol: structure in first source		2.0310alkylbenzene
1,3,5-tris(4-hydroxyphenyl)-4-propyl-1h-pyrazole
4,4',4''-(4-propylpyrazole-1,3,5-triyl)trisphenol : A pyrazole that is 1H-pyrazole bearing three 4-hydroxyphenyl substituents at positions 1, 3 and 5 as well as a propyl substituent at position 4. Potent, subtype-selective estrogen receptor agonist (EC50 ~ 200 pM); displays 410-fold selectivity for ERalpha over ERbeta. Prevents ovariectomy-induced weight gain and loss of bone mineral density, and induces gene expression in the hypothalamus following systemic administration in vivo.		2.0310phenols;
pyrazoles		estrogen receptor agonist
sib 1757
SIB 1757: a selective mGluR5 antagonist; structure in first source		2.0310
sphingosine
sphing-4-enine : A sphingenine in which the C=C double bond is located at the 4-position.. sphingenine : A 2-aminooctadecene-1,3-diol having (2S,3R)-configuration.. sphingoid : Sphinganine, its homologs and stereoisomers, and the hydroxy and unsaturated derivatives of these compounds.. 2-aminooctadec-4-ene-1,3-diol : A 2-aminooctadecene-1,3-diol having its double bond at position 4.		2.0310sphing-4-eninehuman metabolite;
mouse metabolite
quercetin
[no description available]		3.31107-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
apigenin
Chamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.		2.0310trihydroxyflavoneantineoplastic agent;
metabolite
luteolin
[no description available]		2.03103'-hydroxyflavonoid;
tetrahydroxyflavone		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
c-Jun N-terminal kinase inhibitor;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
immunomodulator;
nephroprotective agent;
plant metabolite;
radical scavenger;
vascular endothelial growth factor receptor antagonist
calcitriol
dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes		2.0210D3 vitamins;
hydroxycalciol;
triol		antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical
quercitrin
[no description available]		3.3110alpha-L-rhamnoside;
monosaccharide derivative;
quercetin O-glycoside;
tetrahydroxyflavone		antileishmanial agent;
antioxidant;
EC 1.1.1.184 [carbonyl reductase (NADPH)] inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.14.18.1 (tyrosinase) inhibitor;
plant metabolite
daphnetin
[no description available]		2.0310hydroxycoumarin
alprostadil
[no description available]		2.0210prostaglandins Eanticoagulant;
human metabolite;
platelet aggregation inhibitor;
vasodilator agent
genistein
[no description available]		2.03107-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
amphotericin b
Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.		2.0210antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic		antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
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.		2.432011beta-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
timolol maleate
(S)-timolol maleate : The maleic acid salt of the active (S)-enantiomer of timolol, comprising equimolar amounts of (S)-timolol and maleic acid.		2.0310maleate saltanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
brompheniramine maleate
brompheniramine maleate : The maleic acid salt of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.0310maleate saltanti-allergic agent
chlorpheniramine maleate
[no description available]		2.0310organic molecular entity
clemastine fumarate
clemastine fumarate : The fumaric acid salt of clemastine. An antihistamine with antimuscarinic and moderate sedative properties, it is used for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.		2.0310fumarate saltanti-allergic agent;
antipruritic drug;
H1-receptor antagonist;
muscarinic antagonist
olopatadine
[no description available]		2.0210
methylergonovine maleate
[no description available]		2.0310ergoline alkaloidgeroprotector
bw b1090u
[no description available]		2.0210isoquinolines
astaxanthine
astaxanthine: a keto form of carotene; pigment in flesh of Scottish salmon (Salmo salar) crustacoa-lobster (Homarus gammarus, flamingo feathers; structure; a carotenoid without vitamin A activity, has shown anti-oxidant and anti-inflammatory activities. astaxanthin : A carotenone that consists of beta,beta-carotene-4,4'-dione bearing two hydroxy substituents at positions 3 and 3' (the 3S,3'S diastereomer). A carotenoid pigment found mainly in animals (crustaceans, echinoderms) but also occurring in plants. It can occur free (as a red pigment), as an ester, or as a blue, brown or green chromoprotein.		2.0310carotenol;
carotenone		animal metabolite;
anticoagulant;
antioxidant;
food colouring;
plant metabolite
harman
harman: a beta-carboline; RN given refers to parent cpd; structure. harman : An indole alkaloid fundamental parent with a structure of 9H-beta-carboline carrying a methyl substituent at C-1. It has been isolated from the bark of Sickingia rubra, Symplocus racemosa, Passiflora incarnata, Peganum harmala, Banisteriopsis caapi and Tribulus terrestris, as well as from tobacco smoke. It is a specific, reversible inhibitor of monoamine oxidase A.		2.0310harmala alkaloid;
indole alkaloid fundamental parent;
indole alkaloid		anti-HIV agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
plant metabolite
caryophyllene
(-)-beta-caryophyllene : A beta-caryophyllene in which the stereocentre adjacent to the exocyclic double bond has S configuration while the remaining stereocentre has R configuration. It is the most commonly occurring form of beta-caryophyllene, occurring in many essential oils, particularly oil of cloves.. beta-caryophyllene : A sesquiterpene with a [7.2.0]-bicyclic structure comprising fused 9- and 4-membered rings, with a trans-ring junction, a trans-double bond between the 4- and 5-positions of the 9-membered ring, a methylidene group at position 9, and methyl groups at positions 3, 11, and 11. The most commonly occurring form is the (1R,9S)-(-)-enantiomer, which is found in many essential oils, particularly clove oil.. cannabinoid : A diverse group of pharmacologically active secondary metabolite characteristic to Cannabis plant as well as produced naturally in the body by humans and animals. Cannabinoids contain oxygen as a part of the heterocyclic ring or in the form of various functional groups. They are subdivided on the basis of their origin.		3.3110beta-caryophyllenefragrance;
insect attractant;
metabolite;
non-steroidal anti-inflammatory drug
mangostin
mangostin: xanthone from rind of Garcinia mangostana Linn. fruit. alpha-mangostin : A member of the class of xanthones that is 9H-xanthene substituted by hydroxy group at positions 1, 3 and 6, a methoxy group at position 7, an oxo group at position 9 and prenyl groups at positions 2 and 8. Isolated from the stems of Cratoxylum cochinchinense, it exhibits antioxidant, antimicrobial and antitumour activities.		3.3110aromatic ether;
phenols;
xanthones		antimicrobial agent;
antineoplastic agent;
antioxidant;
plant metabolite
morin
morin: a light yellowish pigment found in the wood of old fustic (Chlorophora tinctoria). morin : A pentahydroxyflavone that is 7-hydroxyflavonol bearing three additional hydroxy substituents at positions 2' 4' and 5.		2.03107-hydroxyflavonol;
pentahydroxyflavone		angiogenesis modulating agent;
anti-inflammatory agent;
antibacterial agent;
antihypertensive agent;
antineoplastic agent;
antioxidant;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
hepatoprotective agent;
metabolite;
neuroprotective agent
myricetin
[no description available]		2.03107-hydroxyflavonol;
hexahydroxyflavone		antineoplastic agent;
antioxidant;
cyclooxygenase 1 inhibitor;
food component;
geroprotector;
hypoglycemic agent;
plant metabolite
daidzein
[no description available]		2.03107-hydroxyisoflavonesantineoplastic agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
phytoestrogen;
plant metabolite
caffeic acid phenethyl ester
phenethyl caffeate : An alkyl caffeate ester in which 2-phenylethyl is the alkyl component.		2.0310alkyl caffeate esteranti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
antioxidant;
antiviral agent;
immunomodulator;
metabolite;
neuroprotective agent
rottlerin
rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1);. rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis.		2.0310aromatic ketone;
benzenetriol;
chromenol;
enone;
methyl ketone		anti-allergic agent;
antihypertensive agent;
antineoplastic agent;
apoptosis inducer;
K-ATP channel agonist;
metabolite
flupenthixol
cis-flupenthixol : A flupenthixol in which the double bond adopts a cis-configuration.		2.0310flupenthixoldopaminergic antagonist
n-oleoyldopamine
N-oleoyldopamine: putative capsaicin receptor ligand; produces hyperalgesia; isolated from the brain. N-oleoyldopamine : A fatty amide resulting from the formal condensation of the carboxy group of oleic acid with the amino group of dopamine. Synthesised in catecholaminergic neurons, it crosses the blood-brain barrier and might be considered as a carrier of dopamine into the brain. It is a transient receptor potential vanilloid type 1 (TRPV1) receptor agonist.		2.0310catechols;
fatty amide;
N-(fatty acyl)-dopamine;
secondary carboxamide		TRPV1 agonist
pheniramine maleate
Naphcon A: tradename; contains above compounds; ophthalmic solution		2.0310organic molecular entity
travoprost
Travoprost: A cloprostenol derivative that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.. travoprost : The isopropyl ester of prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophthalmic solutions of travoprost are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. It is a pro-drug; the isopropyl ester group is hydrolysed by esterases in the cornea to the biologically active free acid, fluprostenol.		2.0510(trifluoromethyl)benzenes;
isopropyl ester;
prostaglandins Falpha		antiglaucoma drug;
antihypertensive agent;
ophthalmology drug;
prodrug;
prostaglandin receptor agonist
tranilast
tranilast: antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis. tranilast : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.		2.0310amidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide		anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent
7432 s
Ceftibuten: A cephalosporin antibacterial agent that is used in the treatment of infections, including urinary-tract and respiratory-tract infections.. ceftibuten : A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to treat urinary-tract and respiratory-tract infections.		2.0210cephalosporin;
dicarboxylic acid		antibacterial drug
trimipramine maleate
[no description available]		2.0310maleate saltantidepressant
etretinate
retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof.		2.0210enoate ester;
ethyl ester;
retinoid		keratolytic drug
isotretinoin
Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases.		2.4320retinoic acidantineoplastic agent;
keratolytic drug;
teratogenic agent
misoprostol
Misoprostol: A synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion, and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties.. misoprostol : A diastereoisomeric mixture composed of approximately equal amounts of a double racemate of four of the sixteen possible diastereoisomers of methyl (13E)-11,16-dihydroxy-16-methyl-9-oxoprost-13-en-1-oate that is racemic prostaglandin E1 which is lacking the hydroxy group at position 15, but which has an additional hydroxy group at position 16. It is a synthetic prostaglandin E1 analogue, used in the treatment of gastric and duodenal ulcers. A weak abortifacient, it is also used for cervical ripening prior to surgical termination of pregnancy. The (11R,16S)-diastereoisomer is the pharmacologically active form.		2.0210
xylometazoline hydrochloride
[no description available]		2.0310
flunarizine hydrochloride
[no description available]		2.0310diarylmethane
ketotifen fumarate
ketotifen fumarate : An organoammonium salt consisting of equimolar amounts of ketotifen(1+) and fumarate(1-) ions. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is a non-bronchodilator anti-asthmatic drug.		2.0310organoammonium saltanti-asthmatic drug;
H1-receptor antagonist
epoprostenol
[no description available]		2.0210prostaglandins Imouse metabolite
cis-flupenthixol dihydrochloride
cis-flupenthixol dihydrochloride : The dihydrochloride salt of cis-flupenthixol.		2.0310hydrochloridegeroprotector
betamethasone benzoate
[no description available]		2.021021-hydroxy steroid
n-arachidonylglycine
N-arachidonylglycine: structure in first source. N-arachidonoylglycine : Biologically active derivative of anandamide		2.0310fatty amide;
N-acylglycine
n-oleoylethanolamine
N-oleoylethanolamine: ceramidase inhibitor. oleoyl ethanolamide : An N-(long-chain-acyl)ethanolamine that is the ethanolamide of oleic acid. The monounsaturated analogue of the endocannabinoid anandamide.		2.0310endocannabinoid;
N-(long-chain-acyl)ethanolamine;
N-acylethanolamine 18:1		EC 3.5.1.23 (ceramidase) inhibitor;
geroprotector;
PPARalpha agonist
cyclosporine
ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF		2.0310homodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
phenoxybenzamine hydrochloride
[no description available]		2.0310organic molecular entity
phenylephrine hydrochloride
Nose: A part of the upper respiratory tract. It contains the organ of SMELL. The term includes the external nose, the nasal cavity, and the PARANASAL SINUSES.. phenylephrine hydrochloride : A hydrochloride that is the monohydrochloride salt of phenylephrine.		2.0310hydrochloride
mepyramine maleate
histosol: proprietary mixture of synthetic aromatic hydrocarbons forming an extremely nonpolar organic solvent		2.0310
dorzolamide
dorzolamide: topically effective ocular hypotensive carbonic anhydrase inhibitor; RN refers to mono-HCl (4S-trans)-isomer. dorzolamide : 5,6-Dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide in which hydrogens at the 4 and 6 positions are substituted by ethylamino and methyl groups, respectively (4S, trans-configuration). A carbonic anhydrase inhibitor, it is used as the hydrochloride in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension.		2.0210sulfonamide;
thiophenes		antiglaucoma drug;
antihypertensive agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
hydromorphone
Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class.		2.0210morphinane alkaloid;
organic heteropentacyclic compound		mu-opioid receptor agonist;
opioid analgesic
ly 163892
loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria.		2.0210carbacephem;
zwitterion		antibacterial drug;
antimicrobial agent
meprednisone
[no description available]		2.021021-hydroxy steroid
nalmefene
nalmefene: RN given refers to 5-alpha isomer		2.0210morphinane alkaloid
topiramate
Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine.		2.0210cyclic ketal;
ketohexose derivative;
sulfamate ester		anticonvulsant;
sodium channel blocker
brefeldin a
[no description available]		3.5920macrolide antibioticPenicillium metabolite
fenretinide
Fenretinide: A synthetic retinoid that is used orally as a chemopreventive against prostate cancer and in women at risk of developing contralateral breast cancer. It is also effective as an antineoplastic agent.. 4-hydroxyphenyl retinamide : A retinoid obtained by formal condensation of the carboxy group of all-trans retinoic acid and the anilino group of 4-hydroxyaniline. Synthetic retinoid agonist. Antiproliferative, antioxidant and anticancer agent with a long half-life in vivo. Apoptotic effects appear to be mediated by a mechanism distinct from that of 'classical' retinoids.		2.0310monocarboxylic acid amide;
retinoid		antineoplastic agent;
antioxidant
calcipotriene
[no description available]		2.0210cyclopropanes;
hydroxy seco-steroid;
seco-cholestane;
secondary alcohol;
triol		antipsoriatic;
drug allergen
peridinin
peridinin: structure		3.3110
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid: RN refers to (E)-isomer; structure given in first source. arotinoid acid : A retinoid that consists of benzoic acid substituted at position 4 by a 2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl group. It is a synthetic retinoid that acts as a selective agonist for the retinoic acid receptors (RAR).		2.0310benzoic acids;
naphthalenes;
retinoid		antineoplastic agent;
retinoic acid receptor agonist;
teratogenic agent
l-2-(carboxypropyl)glycine
[no description available]		2.0310
4-aminocrotonic acid
[no description available]		2.0310
clobetasol
Clobetasol: A derivative of PREDNISOLONE with high glucocorticoid activity and low mineralocorticoid activity. Absorbed through the skin faster than FLUOCINONIDE, it is used topically in treatment of PSORIASIS but may cause marked adrenocortical suppression.. clobetasol : A 3-oxo-Delta(1),Delta(4)-steroid that is 16beta-methylpregna-1,4-diene-3,20-dione bearing hydroxy groups at the 11beta and 17alpha positions, fluorine at position 9, and a chlorine substituent at position 21. It is used as its 17alpha-propionate ester to treat various skin disorders, including exzema and psoriasis.		2.021011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
chlorinated steroid;
fluorinated steroid;
glucocorticoid;
tertiary alpha-hydroxy ketone		anti-inflammatory drug;
SMO receptor agonist
denopamine
denopamine: structure given in first source		2.0310dimethoxybenzene
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.		2.021011beta-hydroxy steroid;
17alpha-hydroxy steroid;
3-oxo-Delta(4) steroid;
corticosteroid;
fluorinated steroid;
thioester		anti-allergic agent;
anti-asthmatic drug
halobetasol
halobetasol: used in ointment to treat psoriasis; Ulobetasol cream contains 0.05% 6-fluoroclobetasol 17-propionate		2.0210corticosteroid hormone
l 655,708
[no description available]		2.0310
latanoprost
Latanoprost: A prostaglandin F analog used to treat OCULAR HYPERTENSION in patients with GLAUCOMA.. latanoprost : A prostaglandin Falpha that is the isopropyl ester prodrug of latanoprost free acid. Used in the treatment of open-angle glaucoma and ocular hypertension.		2.4420isopropyl ester;
prostaglandins Falpha;
triol		antiglaucoma drug;
antihypertensive agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
prodrug
nalbuphine
Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS.		2.0210organic heteropentacyclic compoundmu-opioid receptor antagonist;
opioid analgesic
ro 41-1049
Ro 41-1049: structure given in first source		2.0310
rimexolone
[no description available]		2.021020-oxo steroid
sb 200646a
[no description available]		2.0310
seglitide
seglitide: more potent than somatostatin for inhibition of insulin, glucagon & growth hormone release; used experimentally in treatment of Alzheimer's disease; somatostatin receptor antagonist		2.0310
sib 1893
SIB 1893: a selective mGluR5 antagonist; structure in first source		2.0310
vinorelbine
[no description available]		2.0210acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
ring assembly;
vinca alkaloid		antineoplastic agent;
photosensitizing agent
su 6656
SU 6656: a c-Src kinase inhibitor; used to probe growth signaling; structure in first source. SU6656 : A member of the class of oxindoles that is 3-methyleneoxindole in which the hydrogeh at position 5 has been replaced by a dimethylaminosulfonyl group and in which one of the hydrogens of the methylene group has been replaced by a 4,5,6,7-tetrahydro-indol-2-yl group. It is a specific inhibitor of Src family kinase.		2.0310
andrographolide
[no description available]		3.3110carbobicyclic compound;
gamma-lactone;
labdane diterpenoid;
primary alcohol;
secondary alcohol		anti-HIV agent;
anti-inflammatory drug;
antineoplastic agent;
metabolite
fluvoxamine
Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder.		2.0210(trifluoromethyl)benzenes;
5-methoxyvalerophenone O-(2-aminoethyl)oxime		antidepressant;
anxiolytic drug;
serotonin uptake inhibitor
tyrphostin ag 555
[no description available]		2.0310
tyrphostin ag-494
AG 494: tyrphostin that blocks Cdk2 activation; structure in first source		2.0310
tyrphostin b44
tyrphostin B44: inhibits protein kinases; an analog of tyrphostin B46; B44(+) is B50, and is the stereoisomer of B44(-)		2.0310
ag-490
[no description available]		2.0310catechols;
enamide;
monocarboxylic acid amide;
nitrile;
secondary carboxamide		anti-inflammatory agent;
antioxidant;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector;
STAT3 inhibitor
ag 112
[no description available]		2.0310
ag 183
AG 183: structure given in first source		2.0310
semaxinib
semaxanib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is replaced by a 3,5-dimethylpyrrol-2-yl group.		2.0310olefinic compound;
oxindoles;
pyrroles		angiogenesis modulating agent;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist
su 11248
[no description available]		3.3110monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
8-(3-chlorostyryl)caffeine
8-(3-chlorostyryl)caffeine: adenosine antagonist. 8-(3-chlorostyryl)caffeine : Caffeine substituted at its 8-position by an (E)-3-chlorostyryl group.		2.0310monochlorobenzenes;
trimethylxanthine		adenosine A2A receptor antagonist;
EC 1.4.3.4 (monoamine oxidase) inhibitor
bay 11-7085
BAY11-7085 : A sulfone that is benzene substituted by [(E)-2-cyanoethenyl]sulfonyl and tert-butyl groups at position 1 and 4, respectively. It is an irreversible inhibitor of IkappaB-alpha phosphorylation in cells (IC50 = 10 muM) and prevents the activation of NF-kappaB.		2.0310benzenes;
nitrile;
sulfone		anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
ferroptosis inducer;
NF-kappaB inhibitor
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers.		2.0210dihydroxy monocarboxylic acid;
indoles;
organofluorine compound
molsidomine
[no description available]		2.0310ethyl ester;
morpholines;
oxadiazole;
zwitterion		antioxidant;
apoptosis inhibitor;
cardioprotective agent;
nitric oxide donor;
vasodilator agent
diamide
Diamide: A sulfhydryl reagent which oxidizes sulfhydryl groups to the disulfide form. It is a radiation-sensitizing agent of anoxic bacterial and mammalian cells.		2.03101,1'-azobis(N,N-dimethylformamide)
oxiconazole
oxiconazole: RN given refers to parent cpd(Z)-isomer; structure given in first source. oxiconazole : An oxime O-ether that is the 2,4-dichlorobenzyl ether of the oxime obtained by formal condensation of hydroxylamine with the carbonyl group of acetopnenone in which the phenyl group is substituted by chlorines at positions 2 and 4, and in which one of the hydrogens of the methyl group is replaced by a 1H-imidazol-1-yl group. An antifungal agent, it is used (generally as the nitrate salt) in creams and powders for the topical treatment of fungal skin infections.		2.0210conazole antifungal drug;
dichlorobenzene;
imidazole antifungal drug;
imidazoles;
oxime O-ether		antiinfective agent
nomifensine maleate
[no description available]		2.0310
naltrexone
Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.		2.0210cyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound		antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
nalbuphine hydrochloride
[no description available]		2.0310hydrochloride
butorphanol
Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain.		2.0210morphinane alkaloidantitussive;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
cefixime
[no description available]		2.0210cephalosporinantibacterial drug;
drug allergen
lisinopril
Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.		2.0210dipeptideEC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
benazepril
benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure.		2.0210benzazepine;
dicarboxylic acid monoester;
ethyl ester;
lactam		EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
ramipril
Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles.		2.0210azabicycloalkane;
cyclopentapyrrole;
dicarboxylic acid monoester;
dipeptide;
ethyl ester		bradykinin receptor B2 agonist;
cardioprotective agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
matrix metalloproteinase inhibitor;
prodrug
indinavir sulfate
Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.		2.0210dicarboxylic acid diamide;
N-(2-hydroxyethyl)piperazine;
piperazinecarboxamide		HIV protease inhibitor
isoalloxazine
isoalloxazine: structure		2.0310benzo[g]pteridine-2,4-dione
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		2.0210dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
vinblastine sulfate
[no description available]		2.0310
n-methylscopolamine bromide
scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide.		2.0310
dextromethorphan hydrobromide
dextromethorphan hydrobromide : The hydrobromide and monohydrate of the antitussive drug dextromethorphan.		2.0310hydrate;
hydrobromide
naloxone hydrochloride
naloxone hydrochloride : A hydrochloride resulting from the formal reaction of equimolar amounts of naloxone and hydrogen chloride. A specific opioid antagonist, it is used to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		2.0310hydrochlorideantidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
s-trans,trans-farnesylthiosalicylic acid
farnesylthiosalicylic acid: structure in first source		2.0310sesquiterpenoid
sulindac sulfone
sulindac sulfone: inhibits K-ras-dependent cyclooxygenase-2; sulfated analog of indomethacin;; CP248 is an antineoplastic agent that fosters microtubule depolymerization; structure in first source. sulindac sulfone : A sulfone metabolite of sulindac that inhibits cell growth by inducing apoptosis independently of cyclooxygenase inhibition. It inhibits the development and induces regression of premalignant adenomatous polyps. Lipoxygenase and Cox-2 inhibitor.		2.0310monocarboxylic acid;
organofluorine compound;
sulfone		apoptosis inducer;
cyclooxygenase 2 inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor
cefuroxime
[no description available]		2.02103-(carbamoyloxymethyl)cephalosporin;
furans;
oxime O-ether		drug allergen
ceftriaxone
[no description available]		2.02101,2,4-triazines;
1,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 3.5.2.6 (beta-lactamase) inhibitor
cefepime
Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		2.0210cephalosporin;
oxime O-ether		antibacterial drug
ceftazidime
[no description available]		2.0210cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
trandolapril
trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension.		2.0210dicarboxylic acid monoester;
dipeptide;
ethyl ester;
organic heterobicyclic compound;
secondary amino compound;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
naltrexone hydrochloride
naltrexone hydrochloride : A hydrochloride obtained by reaction of oxycodone with one molar equivalent of hydrochloric acid. it is a mu-opioid receptor antagonist that is used to treat alcohol dependence.		2.0310hydrochlorideantidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
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.		2.1110
guanabenz acetate
[no description available]		2.0310dichlorobenzenegeroprotector
guanabenz
Guanabenz: An alpha-2 selective adrenergic agonist used as an antihypertensive agent.		2.0210dichlorobenzene
nylidrin hydrochloride
[no description available]		2.0310alkylbenzene
triprolidine hydrochloride anhydrous
triprolidine hydrochloride (anh.) : A hydrochloride resulting from the formal reaction of equimolar amounts of triprolidine and hydrogen chloride. Its monohydrate is used for the symptomatic relief of uticaria, rhinitis, and various pruritic skin disorders.		2.0310hydrochlorideH1-receptor antagonist
famotidine
[no description available]		2.43201,3-thiazoles;
guanidines;
sulfonamide		anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
fenoterol
fenoterol hydrobromide : The hydrobromide salt of fenoterol. A beta2-adrenergic agonist, it is used as a bronchodilator in the management of reversible airway obstruction.		2.0310hydrobromidebeta-adrenergic agonist;
bronchodilator agent;
sympathomimetic agent
tiapridex
Tiapride Hydrochloride: A benzamide derivative that is used as a dopamine antagonist.		2.0310benzamides
quipazine maleate
[no description available]		2.0310
n-(2-aminoethyl)-4-chlorobenzamide hydrochloride
Ro 16-6491: structure given in first source		2.0310
tulobuterol hydrochloride
[no description available]		2.0310organic molecular entity
hp 029
[no description available]		2.0310
cefotaxime
Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups.		2.02101,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen
aztreonam
[no description available]		2.0210beta-lactam antibiotic allergen;
monobactam		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
n,n,n-trimethyl-1-(4-stilbenoxy)-2-propylammonium iodide
[no description available]		2.0310
6-(bromomethylene)tetrahydro-3-(1-naphthaleneyl)-2h-pyran-2-one
6-(bromomethylene)tetrahydro-3-(1-naphthaleneyl)-2H-pyran-2-one: structure given in first source; potent irreversible, mechanism-based inhibitor of myocardial calcium-independent phospholipase A2		2.0310naphthalenes
nf023
[no description available]		2.0310
nf 449
[no description available]		2.0310
7-chloro-4-hydroxy-2-phenyl-1,8-naphthyridine
[no description available]		2.0310
gr 46611
GR 46611: known to lower body temperature in guinea pigs		2.0310
cci 15641
[no description available]		2.0210cephalosporin
cefpodoxime
[no description available]		2.0210carboxylic acid;
cephalosporin		antibacterial drug
diacetylmonoxime
diacetylmonoxime: used diagnostically for determining urea in blood; structure; myosin ATPase antagonist. diacetylmonoxime : A ketoxime obtained via formal condensation of butane-2,3-dione with hydroxylamine. It is a reversible myosin ATPase inhibitor.		2.0310
homatropine hydrobromide, (endo-(+-)-isomer)
[no description available]		2.0310
vancomycin hydrochloride
[no description available]		2.0310
moxisylyte hydrochloride
[no description available]		2.0310monoterpenoid
dizocilpine maleate
Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.		2.0310maleate salt;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
beta-aminopropionitrile fumarate
beta-aminopropionitrile fumarate: RN given refers to unspecified fumarate		2.0310
flupirtine
[no description available]		2.0310
zimelidine hydrochloride
[no description available]		2.0310
pregna-4,17-diene-3,16-dione, (17z)-isomer
[no description available]		2.0310
su 4312
SU4312 : A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group. SU 4312 is a vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 and platelet derived growth factor (PDGF) receptor inhibitor. It also inhibits the neuronal nitric oxide synthase (NOS) and exhibits neuroprotection against NO-mediated neurotoxicity.		2.0310
dirithromycin
[no description available]		2.0210macrolide antibioticprodrug
gw 1929
GW 1929: activates peroxisome proliferator-activated receptor-gamma; structure in first source		2.0310benzophenones
cefpodoxime proxetil
cefpodoxime proxetil: structure given in first source; prodrug for cefpodoxime. cefpodoxime proxetil : The 1-[(isopropoxycarbonyl)oxy]ethyl (proxetil) ester prodrug of cefpodoxime. After swallowing, hydrolysis of the ester group occurs in the intestinal epithelium, to release active cefpodoxime in the bloodstream. It is used to treat acute otitis media, pharyngitis, and sinusitis.		2.0210carboxylic acid;
carboxylic ester;
cephalosporin		antibacterial drug;
prodrug
ceftizoxime
[no description available]		2.0210cephalosporinantibacterial drug
protriptyline hydrochloride
[no description available]		2.0310hydrochlorideantidepressant
n(4)-chloroacetylcytosine arabinoside
[no description available]		2.0310
n-(3-(cyclohexylidene-(1h-imidazol-4-ylmethyl))phenyl)ethanesulfonamide
[no description available]		2.0310
n-(4-amino-2-chlorophenyl)phthalimide
N-(4-amino-2-chlorophenyl)phthalimide: has anticonvulsant activity; structure in first source		2.0310
cgp 12177a
[no description available]		2.0210
cb 34
CB 34: ligand for peripheral benzodiazepine receptors; structure in first source		2.0310
b 43
RK-24466 : A member of the class of pyrrolopyrimidines that is 7H-pyrrolo[2,3-d]pyrimidine substituted by amino, 4-phenoxyphenyl, and cyclopentyl groups at positions 4, 5 and 7, respectively. It is a potent inhibitor of Lck that inhibits Lck (64-509) and LckCD isoforms (IC50 of less than 1 and 2 nM, respectively).		2.0310aromatic amine;
aromatic ether;
cyclopentanes;
primary amino compound;
pyrrolopyrimidine		EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
(8R)-7-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,13,14-triol
[no description available]		2.0310aporphine alkaloid
(8R)-7-propyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,13,14-triol
[no description available]		2.0310aporphine alkaloid
3-(6-chloro-3-pyridazinyl)-3,8-diazabicyclo(3.2.1)octane
3-(6-chloro-3-pyridazinyl)-3,8-diazabicyclo(3.2.1)octane: structure in first source		2.0310
2-(3,3-diphenylpropylamino)acetamide
[no description available]		2.0310diarylmethane
4-(2-(phenylsulfonylamino)ethylthio)-2,6-difluorophenoxyacetamide
4-(2-(phenylsulfonylamino)ethylthio)-2,6-difluorophenoxyacetamide: structure given in first source		2.0310
gw2974
GW2974: quinazoline derivative, which is able to block the activation of both the EGFR and erbB2		2.0310pyridopyrimidine
7-hydroxy-2-n,n-dipropylaminotetralin, (r)-isomer
[no description available]		2.1310
l 162313
L 162313: a biphenylimidazole derivative; a non-peptide angiotensin agonist; no further information available 2/95		2.0310
l-165041
4-(3-(2-propyl-3-hydroxy-4-acetyl)phenoxy)propyloxyphenoxy acetic acid: a PPAR-delta agonist has regulatory effects on a variety of adipokines, and these effects might explain some of their metabolic function.		2.0310aromatic ketone
mrs 1754
[no description available]		2.0310oxopurine
s-nitroso-n-acetylpenicillamine
S-Nitroso-N-Acetylpenicillamine: A sulfur-containing alkyl thionitrite that is one of the NITRIC OXIDE DONORS.		2.0310nitroso compound;
nitrosothio compound		nitric oxide donor;
vasodilator agent
pd 404182
[no description available]		2.0310
sb 222200
[no description available]		2.0310quinolines
dantrolene sodium
dantrolene sodium (anhydrous) : The anhydrous sodium salt of dantrolene.		2.0310
cr 2945
CR 2945: a member of non-peptide CCKB receptor antagonist		2.0310
nitrofurantoin
Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA.		2.0210imidazolidine-2,4-dione;
nitrofuran antibiotic;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic		antibacterial drug;
antiinfective agent;
hepatotoxic agent
ici 215001
ICI 215001: active metabolite of ICI D7114; no other info avail 9/92		2.0210monocarboxylic acid
sb 218795
SB 218795: structure in first source		2.0310quinolines
dihydroceramide
N-acetylsphinganine : A dihydroceramide in which the ceramide acyl group is specified as acetyl.		2.0310N-acylsphinganine
epinephrine bitartrate
[no description available]		2.0310
bicuculline methobromide
[no description available]		2.0310
butylscopolammonium bromide
Butylscopolammonium Bromide: Antimuscarinic quaternary ammonium derivative of scopolamine used to treat cramps in gastrointestinal, urinary, uterine, and biliary tracts, and to facilitate radiologic visualization of the gastrointestinal tract.		2.0310
butaclamol hydrochloride
[no description available]		2.0310
dantrolene
[no description available]		2.0210
a 38503
[no description available]		2.0310
8-hydroxy-2-(di-n-propylamino)tetralin hydrobromide
[no description available]		2.0310
sk&f 89976-a
[no description available]		2.0310
cv 1808
2-phenylaminoadenosine: has coronary & cardiohemodynamic effects		2.0310purine nucleoside
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.		4.5870indanes;
monohydroxyquinoline;
quinolone;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent
cyclo(leucyl-prolyl)
cyclo(leucyl-prolyl): structure in first source. cyclo(L-Leu-L-Pro) : A homodetic cyclic peptide composed from leucyl and prolyl residues.		3.3110dipeptide;
homodetic cyclic peptide;
pyrrolopyrazine		bacterial metabolite;
marine metabolite
fluvoxamine maleate
[no description available]		2.0310(trifluoromethyl)benzenes
naloxone benzoylhydrazone
[no description available]		2.0310
fosinopril
[no description available]		2.0210
2-methyl-6-(phenylethynyl)pyridine hydrochloride
2-methyl-6-(phenylethynyl)pyridine hydrochloride : A hydrochloride salt obtained by reaction of 2-methyl-6-(phenylethynyl)pyridine with one equivalent of hydrochloric acid. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.		2.0310hydrochlorideanxiolytic drug;
metabotropic glutamate receptor antagonist
amiprilose
[no description available]		2.0310
(R)-fluoxetine hydrochloride
(R)-fluoxetine hydrochloride : A hydrochloride obtained by reaction of (R)-fluoxetine with one equivalent of hydrochloric acid.		2.0310hydrochlorideantidepressant;
serotonin uptake inhibitor
sc 795
[no description available]		2.0510
3-((3-(4-chloro-3-ethylphenoxy)phenyl)(3-(1,1,2,2-tetrafluoroethoxy)benzyl)amino)-1,1,1-trifluoropropan-2-ol
3-((3-(4-chloro-3-ethylphenoxy)phenyl)(3-(1,1,2,2-tetrafluoroethoxy)benzyl)amino)-1,1,1-trifluoropropan-2-ol: inhibits cholesteryl ester transfer protein; structure in first source		2.0510
l 755507
L 755507: a benzenesulfonamide derivative; structure in first source		2.9710
desmethylselegiline hydrochloride
[no description available]		2.0310
3-morpholino-sydnonimine monohydrochloride
[no description available]		2.0310
t 1032
T 1032: a cyclic GMP phosphodiesterase-5 inhibitor; structure in first source		2.0310
qx-314 bromide
[no description available]		2.0310
(S)-fluoxetine hydrochloride
(S)-fluoxetine hydrochloride : A hydrochloride obtained by reaction of (S)-fluoxetine with one equivalent of hydrochloric acid.		2.0310hydrochlorideantidepressant;
serotonin uptake inhibitor
sr 59230a
3-(2-ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate: structure given in first source		2.0310
u 74389g
[no description available]		2.0310
1-(2-methoxyphenyl)piperazine hydrochloride
[no description available]		2.0310
y 27632, dihydrochloride, (4(r)-trans)-isomer
[no description available]		2.0310
noscapine hydrochloride
[no description available]		2.0310
a 77636
(1R,3S)-3-(adamantan-1-yl)-1-(aminomethyl)-3,4-dihydroisochromene-5,6-diol hydrochloride : A hydrochloride salt obtained by mixing equimolar amounts of (1R,3S)-3-(adamantan-1-yl)-1-(aminomethyl)-3,4-dihydroisochromene-5,6-diol with hydrochloric acid. Potent and selective dopamine D1-like receptor agonist (pEC50 values are 8.97 and < 5 for D1-like and D2-like receptors respectively). Displays anti-Parkinsonian activity following oral administration in vivo.		2.0310hydrochlorideantiparkinson drug;
dopamine agonist
cgp 20712a
CGP 20712A: structure given in first source; CGP 26505, a beta1-selective beta-adrenoceptor antagonist, is the (S)-isomer of CGP 20712A		2.0310
osu 03012
OSU 03012: a PDK-1 inhibitor; structure in first source		3.3110antibiotic antifungal drug;
aromatic amide;
glycine derivative;
organofluorine compound;
phenanthrenes;
pyrazoles		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
levodopa methyl ester hydrochloride
[no description available]		2.0310
vilanterol
[no description available]		3.6120benzyl alcohols;
dichlorobenzene;
ether;
phenols;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent
benalfocin hydrochloride
[no description available]		2.0310
lu 19005
[no description available]		2.0310
benoxathian hydrochloride
[no description available]		2.0310
((2-n-butyl-6,7-dichloro-2-cyclopentyl-2,3-dihydro-1-oxo-1h-inden-5-yl)oxy)acetic acid, (+)-isomer
[no description available]		2.0310
n-cyclopropyl adenosine-5'-carboxamide
[no description available]		2.0310
cefotaxime sodium
[no description available]		2.0310organic sodium salt
calpain inhibitor iii
calpain inhibitor III: potential anticataract drug		2.0310
nystatin a1
Nystatin: Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.. nystatin : A heterogeneous mixture of polyene compounds produced by cultures of Streptomyces noursei. It mainly consists of three biologically active components designated nystatin A1, nystatin A2, and nystatin A3. It is used to treat oral and dermal fungal infections.. nystatin A1 : A polyene macrolide antibiotic; part of the nystatin complex produced by several Streptomyces species. It is an antifungal antibiotic used for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species.		2.0210nystatins
5-hydroxy-2-n,n-dipropylaminotetralin, (s)-isomer
[no description available]		2.1310
tiotropium bromide
tiotropium bromide hydrate : A hydrate that is the monohydrate form of tiotropium bromide. Used for maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease.		2.0610
GR 127935 hydrochloride
GR 127935 hydrochloride : A hydrochloride obtained by reaction of GR 127935 with one equivalent of hydrochloric acid. Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.		2.0310hydrochlorideserotonergic antagonist
olodaterol
[no description available]		3.7820aromatic ether;
benzoxazine;
phenols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent
mrs 1845
[no description available]		2.0310
lactimidomycin
lactimidomycin: a glutarimide antibiotic isolated from Streptomyces amphibiosporus		3.3110macrolide
1-aminocyclopropane-1-carboxylic acid hydrochloride
[no description available]		2.0310
alaproclate hydrochloride
[no description available]		2.0310
ubenimex
[no description available]		2.0310peptide
3-chloroalanine hydrochloride, (l-ala)-isomer
[no description available]		2.0310
dsp 4 hydrochloride
[no description available]		2.0310
calcimycin
Calcimycin: An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.		2.0310benzoxazole
(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzodioxan hydrochloride
N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine hydrochloride : A hydrochloride salt that is obtained by reaction of N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine with one equivalent of hydrogen chloride. An alpha1A-adrenergic selective antagonist.		2.0310hydrochloridealpha-adrenergic antagonist
2-cyclooctyl-2-hydroxyethylamine hydrochloride
[no description available]		2.0310
cirazoline monohydrochloride
[no description available]		2.0310
adtn
[no description available]		2.0310
apocodeine hydrochloride, (r)-isomer
[no description available]		2.0310
Dihydro-beta-erythroidine hydrobromide
[no description available]		2.0310indoles
lilly 78335
[no description available]		2.0310
efaroxan hydrochloride
[no description available]		2.0310
fenoldopam hydrobromide
[no description available]		2.0310
1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride : A hydrochloride salt that is obtained by reaction of 1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine with two equivalents of hydrogen chloride. Potent and selective inhibitor of dopamine uptake (KD = 5.5 nM in rat striatal membranes).		2.0310hydrochloridedopamine uptake inhibitor
guvacine hydrochloride
[no description available]		2.0310
7-hydroxy-2-n,n-dipropylaminotetralin hydrobromide
[no description available]		2.0310
8-hydroxy-2-(di-n-propylamino)tetralin hydrobromide, (r)-isomer,
[no description available]		2.0310organic molecular entity
1-(2-(4-(4-fluoro-benzoyl)-piperidin-1-yl)-ethyl)-3,3-dimethyl-1,2-dihydro-indol-2-one
LY-310762 hydrochloride : A hydrochloride resulting from the formal reation of equimolar amount of LY-310762 with hydrogen chloride. A potent and selective antagonist for the 5-hydroxytryptamine 1D (5-HT1D) receptor.		2.0310hydrochloridereceptor modulator;
serotonergic antagonist
4-iodoclonidine
[no description available]		2.0310
4-methylpyrazole monohydrochloride
[no description available]		2.0310
tele-methylhistamine
[no description available]		2.0310
alpha-methyltyrosine methyl ester, monohydrochloride
[no description available]		2.0310
octoclothepine maleate
[no description available]		2.0310
2-(n-phenethyl-n-propyl)amino-5-hydroxytetralin hydrochloride
[no description available]		2.0310
du 24565
[no description available]		2.0310
2-methoxyidazoxan hydrochloride
[no description available]		2.0310
ro 25-6981
[no description available]		2.0310
sk&f 77434
N-allyl-1-phenyl-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol hydrobromide : A hydrobromide salt prepared from N-allyl-1-phenyl-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol and one equivalent of hydrogen bromide. Selective dopamine D1-like receptor partial agonist (IC50 values are 19.7 and 2425 nM for binding to D1-like and D2-like receptors respectively). Centrally active following systemic administration in vivo.		2.0310hydrobromidedopamine agonist;
prodrug
3-[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline-9-yl]-1,1-diethylurea
[no description available]		2.0310organic heterotetracyclic compound;
organonitrogen heterocyclic compound
demethylcantharidin
demethylcantharidin: has antineoplastic activity; structure in first source		2.0310
atropine sulfate
[no description available]		2.0310
1-deoxynojirimycin hydrochloride
[no description available]		2.0310
win 62577
[no description available]		2.0310
amodiaquine hydrochloride
[no description available]		2.0510
quinine sulfate
[no description available]		2.0310hydrate
quercetin
[no description available]		2.0310
rv 538, (r-(r*,r*))-isomer
[no description available]		2.0310
3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (1s-cis)-isomer
[no description available]		2.0310
valproate sodium
Epilim: oral sodium valproate used as antidepressive agent. sodium valproate : The sodium salt of valproic acid.. valproate : A branched-chain saturated fatty acid anion that is the conjugate base of valproic acid.		2.0310organic sodium saltgeroprotector
mesna
Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE.		2.0210organosulfonic acid
u 63557a
[no description available]		2.0310
cefamandole nafate
[no description available]		2.0210organic sodium saltantibacterial drug;
prodrug
taurocholic acid, monosodium salt
[no description available]		2.0310bile salt
cefmetazole sodium
cefmetazole sodium : An organic sodium salt that is the sodium salt of cefmetazole.		2.0310organic sodium saltantimicrobial agent
fusidate sodium
[no description available]		2.0310
cephapirin sodium
cephapirin sodium : The sodium salt of cephapirin. A first-generation cephalosporin antibiotic, it is effective against gram-negative and gram-positive organisms. Being more resistant to beta-lactamases than penicillins, it is effective agains most staphylococci, though not methicillin-resistant staphylococci.		2.0310cephalosporin;
organic sodium salt		antibacterial drug
sodium cephalothin
[no description available]		2.0310organic sodium salt
cefazolin sodium
cefazolin sodium : A cephalosporin organic sodium salt having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups.		2.0310organic sodium salt
5-hydroxydecanoic acid, monosodium salt
[no description available]		2.0310
ro13-9904
Ceftriaxone: A broad-spectrum cephalosporin antibiotic and cefotaxime derivative with a very long half-life and high penetrability to meninges, eyes and inner ears.. ceftriaxone : A third-generation cephalosporin compound having 2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetylamino and [(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)sulfanyl]methyl side-groups.		2.0310
phenytoin sodium
[no description available]		2.0310
cr 1409
lorglumide sodium : A racemate comprising equal amounts of (R)- and (S)-lorglumide sodium.		2.0310
cortisol succinate, sodium salt
hydrocortisone hemisuccinate: RN given refers to (11beta)-isomer; Synonyms Solu-Cortef & sopolcort H refer to Na salt		2.0310organic molecular entity
sofosbuvir
Sofosbuvir: A uridine monophosphate analog inhibitor of HEPATITIS C VIRUS (HCV) polymerase NS5B that is used as an ANTIVIRAL AGENT in the treatment of CHRONIC HEPATITIS C.. sofosbuvir : A nucleotide conjugate that is used in combination with ledipasvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection.		3.3110isopropyl ester;
L-alanyl ester;
nucleotide conjugate;
organofluorine compound;
phosphoramidate ester		antiviral drug;
hepatitis C protease inhibitor;
prodrug
tatanan a
tatanan A: from the rhizomes of Acorus tatarinowii Schott; structure in first source		3.3110
tetracycline
Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.		2.0210
minocycline
Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.		2.0210
piroxicam
[no description available]		2.4320benzothiazine;
monocarboxylic acid amide;
pyridines		analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
meclocycline
[no description available]		2.0210
lfm a13
LFM-A13 : An enamide obtained by formal condensation of the carboxy group of (2Z)-2-cyano-3-hydroxybut-2-enoic acid with the amino group of 2,5-dibromoaniline. It is a dual-function inhibitor of Bruton's tyrosine kinase (BTK) and Polo-like kinases (PLK) that exhibits anticancer properties.		2.0310aromatic amide;
dibromobenzene;
enamide;
enol;
nitrile;
secondary carboxamide		antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 2.7.11.21 (polo kinase) inhibitor;
geroprotector;
platelet aggregation inhibitor
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		2.0210benzenes;
hydroxycoumarin;
methyl ketone
bromadiolone
[no description available]		2.0510diarylheptanoid
l 701324
L 701324: a glycine/NMDA receptor antagonist		2.0310quinolines
hispidin
hispidin: metabolite of Basidiomycete Polyporus hispidus. hispidin : Fungal metabolite first found in basidiomycete Inonotus hispidus (formerly Polyporus hispidus).		2.03102-pyranones;
catechols		antioxidant;
EC 2.7.11.13 (protein kinase C) inhibitor;
fungal metabolite
minocycline hydrochloride
[no description available]		2.0310
demeclocycline hydrochloride
demeclocycline hydrochloride : The hydrochloride salt of demeclocycline. A tetracycline antibiotic, it is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective.		2.0310
acyclovir
Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections.		2.43202-aminopurines;
oxopurine		antimetabolite;
antiviral drug
sepiapterin
sepiapterin: A substrate of sepiapterin reductase		2.0310sepiapterin
isoxanthopterin
[no description available]		2.0310dihydroxypteridine
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.0210cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
clozapine
Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.		2.4320benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
didanosine
Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS.		2.0210purine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor;
geroprotector;
HIV-1 reverse transcriptase inhibitor
ganciclovir
[no description available]		2.43202-aminopurines;
oxopurine		antiinfective agent;
antiviral drug
valacyclovir
Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES.		2.0210L-valyl esterantiviral drug
olanzapine
Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.		2.0210benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
penciclovir
penciclovir : A member of the class of 2-aminopurines that is guanine in which the hydrogen at position 9 is substituted by a 4-hydroxy-3-(hydroxymethyl)but-1-yl group. An antiviral drug, it is administered topically for treatment of herpes labialis. A prodrug, famciclovir, is used for oral administration.		2.02102-aminopurines;
propane-1,3-diols		antiviral drug
zaprinast
zaprinast: anaphylaxis inhibitor; structure		2.0310triazolopyrimidines
allopurinol
Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.		2.4320nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger
thiolactomycin
thiolactomycin: from actinomycetes; structure given in first source		2.0310
2,4-diaminohypoxanthine
2,4-diaminohypoxanthine: do not confuse abbreviation DAHP with various dehydro-deoxy-arabino-heptulosonic acid phosphates which also use DAHP; RN given refers to parent cpd; structure		2.0310hydroxypyrimidine
rifabutin
[no description available]		2.0210
quazinone
[no description available]		2.0310
8-bromocyclic gmp, sodium salt
sodium 8-bromo-3',5'-cyclic GMP : An organic sodium salt having 8-bromoguanosine 3',5'-cyclic phosphate as the counterion. A membrane permeable cGMP analogue that activates protein kinase G (PKG). It is 4.3-fold more potent than cGMP in activating PKG1alpha and promotes relaxation of tracheal and vascular smooth muscle tissue in vitro.		2.0310organic sodium saltmuscle relaxant;
protein kinase G agonist
ag-879
AG-879: structure given in first source		2.0310
ConditionIndicatedRelationship StrengthStudiesTrials
Parasite Infections
[description not available]		02.0510
Innate Inflammatory Response
[description not available]		014.384220
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		014.384220
Acute Liver Injury, Drug-Induced
[description not available]		05.2841
Adverse Drug Event
[description not available]		08.99132
Chemical and Drug Induced Liver Injury
A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.		05.2841
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		08.99132
Contact Dermatitis
[description not available]		02.2110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		010.88289
Itching
[description not available]		02.4320
Dermatitis, Contact
A type of acute or chronic skin reaction in which sensitivity is manifested by reactivity to materials or substances coming in contact with the skin. It may involve allergic or non-allergic mechanisms.		02.2110
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		02.4320
Congenital Zika Syndrome
[description not available]		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Airflow Obstruction, Chronic
[description not available]		025.25554345
Pulmonary Disease, Chronic Obstructive
A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.		127.25554345
Asthma, Bronchial
[description not available]		026.341,014469
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).		128.341,014469
Breathlessness
[description not available]		015.575030
Dyspnea
Difficult or labored breathing.		015.575030
Cough
A sudden, audible expulsion of air from the lungs through a partially closed glottis, preceded by inhalation. It is a protective response that serves to clear the trachea, bronchi, and/or lungs of irritants and secretions, or to prevent aspiration of foreign materials into the lungs.		06.8583
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		015.374330
Pneumonia
Infection of the lung often accompanied by inflammation.		015.374330
Blood Pressure, High
[description not available]		02.5120
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		02.5120
Candida Infection
[description not available]		03.5720
Cancer of Larynx
[description not available]		03.420
Laryngeal Diseases
Pathological processes involving any part of the LARYNX which coordinates many functions such as voice production, breathing, swallowing, and coughing.		03.420
Candidiasis
Infection with a fungus of the genus CANDIDA. It is usually a superficial infection of the moist areas of the body and is generally caused by CANDIDA ALBICANS. (Dorland, 27th ed)		03.5720
Laryngeal Neoplasms
Cancers or tumors of the LARYNX or any of its parts: the GLOTTIS; EPIGLOTTIS; LARYNGEAL CARTILAGES; LARYNGEAL MUSCLES; and VOCAL CORDS.		03.420
47,XX,+21
[description not available]		02.2510
Down Syndrome
A chromosome disorder associated either with an extra chromosome 21 or an effective trisomy for chromosome 21. Clinical manifestations include hypotonia, short stature, brachycephaly, upslanting palpebral fissures, epicanthus, Brushfield spots on the iris, protruding tongue, small ears, short, broad hands, fifth finger clinodactyly, Simian crease, and moderate to severe INTELLECTUAL DISABILITY. Cardiac and gastrointestinal malformations, a marked increase in the incidence of LEUKEMIA, and the early onset of ALZHEIMER DISEASE are also associated with this condition. Pathologic features include the development of NEUROFIBRILLARY TANGLES in neurons and the deposition of AMYLOID BETA-PROTEIN, similar to the pathology of ALZHEIMER DISEASE. (Menkes, Textbook of Child Neurology, 5th ed, p213)		02.2510
Disease Exacerbation
[description not available]		017.326140
Genetic Predisposition
[description not available]		09.75131
Chronic Illness
[description not available]		011.393311
Attachment Loss, Periodontal
[description not available]		04.6211
Infections, Coronavirus
[description not available]		04.6211
Chemical Dependence
[description not available]		04.6211
Cerebral Infarction, Middle Cerebral Artery
[description not available]		04.6211
Osteoarthritis of Knee
[description not available]		04.6211
Deafness, Transitory
[description not available]		04.6211
Liver Abscess, Pyogenic
Single or multiple areas of PUS due to bacterial infection within the hepatic parenchyma. It can be caused by a variety of BACTERIA, local or disseminated from infections elsewhere such as in APPENDICITIS; CHOLECYSTITIS; PERITONITIS; and after LIVER TRANSPLANTATION.		04.6211
Complications of Diabetes Mellitus
[description not available]		07.7444
Acute Kidney Failure
[description not available]		07.7444
Carcinogenesis
The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.		07.7444
Fatty Liver, Nonalcoholic
[description not available]		04.6211
Esophageal Squamous Cell Carcinoma
A carcinoma that originates usually from cells on the surface of the middle and lower third of the ESOPHAGUS. Tumor cells exhibit typical squamous morphology and form large polypoid lesions. Mutations in RNF6, LZTS1, TGFBR2, DEC1, and WWOX1 genes are associated with this cancer.		04.6211
2019 Novel Coronavirus Disease
[description not available]		07.9254
Ancylostomiasis
Infection of humans or animals with hookworms of the genus ANCYLOSTOMA. Characteristics include anemia, dyspepsia, eosinophilia, and abdominal swelling.		04.6211
Auricular Fibrillation
[description not available]		05.6332
Bladder Cancer
[description not available]		04.6211
Bladder Disorder, Neurogenic
[description not available]		04.6211
Acute Brain Injuries
[description not available]		04.6211
Benign Neoplasms, Brain
[description not available]		07.7444
Breast Cancer
[description not available]		07.8964
Carcinoma, Non-Small Cell Lung
[description not available]		04.6211
Carcinoma, Epidermoid
[description not available]		04.6211
Cerebral Ischemia
[description not available]		04.6211
Caries, Dental
[description not available]		04.6211
Alloxan Diabetes
[description not available]		04.6211
Diabetes Mellitus, Adult-Onset
[description not available]		04.6211
Canine Diseases
[description not available]		04.6211
Cancer of Esophagus
[description not available]		04.6211
Fistula
Abnormal communication most commonly seen between two internal organs, or between an internal organ and the surface of the body.		04.6211
Cancer of Gastrointestinal Tract
[description not available]		04.6211
Astrocytoma, Grade IV
[description not available]		04.6211
Glial Cell Tumors
[description not available]		04.7521
Focal Segmental Glomerulosclerosis
[description not available]		04.6211
Cardiac Failure
[description not available]		08.85105
Bleeding
[description not available]		05.0731
Hepatocellular Carcinoma
[description not available]		04.6211
Infections, Klebsiella
[description not available]		04.6211
Cirrhosis, Liver
[description not available]		04.6211
Liver Dysfunction
[description not available]		04.6211
Cancer of Liver
[description not available]		04.6211
Cancer of Lung
[description not available]		04.7821
Malignant Melanoma
[description not available]		04.6211
Mitral Incompetence
[description not available]		04.6211
Kahler Disease
[description not available]		04.6211
Cardiomyopathies, Primary
[description not available]		04.6211
Benign Neoplasms
[description not available]		04.821
Angiogenesis, Pathologic
[description not available]		08.0864
Morbid Obesity
[description not available]		04.6211
Arthritis, Degenerative
[description not available]		04.6211
Pocket, Periodontal
[description not available]		04.6211
Pericementitis
[description not available]		04.6211
Complication, Postoperative
[description not available]		05.6932
Condition, Preneoplastic
[description not available]		04.7921
Cancer of Prostate
[description not available]		07.7444
Embolism, Pulmonary
[description not available]		04.6211
Acute Respiratory Distress Syndrome
[description not available]		05.0531
Sarcoma, Epithelioid
[description not available]		04.6211
Linear Skull Fracture
[description not available]		04.6211
Cancer of Stomach
[description not available]		09.9399
Nicotine Addiction
[description not available]		04.6211
Zoonoses
Diseases of non-human animals that may be transmitted to HUMANS or may be transmitted from humans to non-human animals.		04.6211
Coxarthrosis
[description not available]		04.6211
Injury, Ischemia-Reperfusion
[description not available]		07.7854
MPTP Neurotoxicity Syndrome
[description not available]		04.6211
Shoulder Injuries
Injuries involving the SHOULDERS and SHOULDER JOINT.		04.6211
Hemorrhage, Gingival
[description not available]		04.6211
Local Neoplasm Recurrence
[description not available]		04.6211
Acute Disease
Disease having a short and relatively severe course.		011.43208
Atrial Fibrillation
Abnormal cardiac rhythm that is characterized by rapid, uncoordinated firing of electrical impulses in the upper chambers of the heart (HEART ATRIA). In such case, blood cannot be effectively pumped into the lower chambers of the heart (HEART VENTRICLES). It is caused by abnormal impulse generation.		05.6332
Biliary Tract Diseases
Diseases in any part of the BILIARY TRACT including the BILE DUCTS and the GALLBLADDER.		04.6211
Urinary Bladder Neoplasms
Tumors or cancer of the URINARY BLADDER.		04.6211
Urinary Bladder, Neurogenic
Dysfunction of the URINARY BLADDER due to disease of the central or peripheral nervous system pathways involved in the control of URINATION. This is often associated with SPINAL CORD DISEASES, but may also be caused by BRAIN DISEASES or PERIPHERAL NERVE DISEASES.		04.6211
Brain Injuries
Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.		04.6211
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		07.7444
Breast Neoplasms
Tumors or cancer of the human BREAST.		07.8964
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		04.6211
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		04.6211
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		012.5216
Brain Ischemia
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.		04.6211
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		011.393311
Dental Caries
Localized destruction of the tooth surface initiated by decalcification of the enamel followed by enzymatic lysis of organic structures and leading to cavity formation. If left unchecked, the cavity may penetrate the enamel and dentin and reach the pulp.		04.6211
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		05.0631
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		04.6211
Esophageal Neoplasms
Tumors or cancer of the ESOPHAGUS.		04.6211
Gingival Hemorrhage
The flowing of blood from the marginal gingival area, particularly the sulcus, seen in such conditions as GINGIVITIS, marginal PERIODONTITIS, injury, and ASCORBIC ACID DEFICIENCY.		04.6211
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		04.6211
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		04.7521
Glomerulosclerosis, Focal Segmental
A clinicopathological syndrome or diagnostic term for a type of glomerular injury that has multiple causes, primary or secondary. Clinical features include PROTEINURIA, reduced GLOMERULAR FILTRATION RATE, and EDEMA. Kidney biopsy initially indicates focal segmental glomerular consolidation (hyalinosis) or scarring which can progress to globally sclerotic glomeruli leading to eventual KIDNEY FAILURE.		04.6211
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		08.85105
Hemorrhage
Bleeding or escape of blood from a vessel.		05.0731
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		04.6211
Ischemia
A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.		04.6211
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		04.6211
Klebsiella Infections
Infections with bacteria of the genus KLEBSIELLA.		04.6211
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		04.6211
Liver Diseases
Pathological processes of the LIVER.		04.6211
Liver Neoplasms
Tumors or cancer of the LIVER.		04.6211
Lung Neoplasms
Tumors or cancer of the LUNG.		04.7821
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		04.6211
Mitral Valve Insufficiency
Backflow of blood from the LEFT VENTRICLE into the LEFT ATRIUM due to imperfect closure of the MITRAL VALVE. This can lead to mitral valve regurgitation.		04.6211
Multiple Myeloma
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.		04.6211
Cardiomyopathies
A group of diseases in which the dominant feature is the involvement of the CARDIAC MUSCLE itself. Cardiomyopathies are classified according to their predominant pathophysiological features (DILATED CARDIOMYOPATHY; HYPERTROPHIC CARDIOMYOPATHY; RESTRICTIVE CARDIOMYOPATHY) or their etiological/pathological factors (CARDIOMYOPATHY, ALCOHOLIC; ENDOCARDIAL FIBROELASTOSIS).		04.6211
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		04.821
Obesity, Morbid
The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2.		04.6211
Osteoarthritis
A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.		04.6211
Periodontal Pocket
An abnormal extension of a gingival sulcus accompanied by the apical migration of the epithelial attachment and bone resorption.		04.6211
Periodontitis
Inflammation and loss of connective tissues supporting or surrounding the teeth. This may involve any part of the PERIODONTIUM. Periodontitis is currently classified by disease progression (CHRONIC PERIODONTITIS; AGGRESSIVE PERIODONTITIS) instead of age of onset. (From 1999 International Workshop for a Classification of Periodontal Diseases and Conditions, American Academy of Periodontology)		04.6211
Pneumonia, Viral
Inflammation of the lung parenchyma that is caused by a viral infection.		04.6211
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		05.6932
Precancerous Conditions
Pathological conditions that tend eventually to become malignant.		04.7921
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		08.89164
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		07.7444
Pulmonary Embolism
Blocking of the PULMONARY ARTERY or one of its branches by an EMBOLUS.		04.6211
Respiratory Distress Syndrome
A syndrome characterized by progressive life-threatening RESPIRATORY INSUFFICIENCY in the absence of known LUNG DISEASES, usually following a systemic insult such as surgery or major TRAUMA.		05.0531
Sarcoma
A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.		04.6211
Stomach Neoplasms
Tumors or cancer of the STOMACH.		09.9399
Tobacco Use Disorder
Tobacco used to the detriment of a person's health or social functioning. Tobacco dependence is included.		04.6211
Vitiligo
A disorder consisting of areas of macular depigmentation, commonly on extensor aspects of extremities, on the face or neck, and in skin folds. Age of onset is often in young adulthood and the condition tends to progress gradually with lesions enlarging and extending until a quiescent state is reached.		04.6211
Osteoarthritis, Hip
Noninflammatory degenerative disease of the hip joint which usually appears in late middle or old age. It is characterized by growth or maturational disturbances in the femoral neck and head, as well as acetabular dysplasia. A dominant symptom is pain on weight-bearing or motion.		04.6211
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		07.7854
Coronavirus Infections
Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).		04.6211
Substance-Related Disorders
Disorders related to substance use or abuse.		04.6211
Infarction, Middle Cerebral Artery
NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.		04.6211
Osteoarthritis, Knee
Noninflammatory degenerative disease of the knee joint consisting of three large categories: conditions that block normal synchronous movement, conditions that produce abnormal pathways of motion, and conditions that cause stress concentration resulting in changes to articular cartilage. (Crenshaw, Campbell's Operative Orthopaedics, 8th ed, p2019)		04.6211
Hearing Loss
A general term for the complete or partial loss of the ability to hear from one or both ears.		04.6211
Lipid Metabolism Disorders
Pathological conditions resulting from abnormal anabolism or catabolism of lipids in the body.		04.6211
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		07.7444
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		04.6211
Allergic Rhinitis
[description not available]		02.3110
Rhinitis, Allergic
An inflammation of the NASAL MUCOSA triggered by ALLERGENS.		02.3110
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		05.76112
Airway Remodeling
The structural changes in the number, mass, size and/or composition of the airway tissues.		02.1510
Metaplasia
A condition in which there is a change of one adult cell type to another similar adult cell type.		02.1510
Acute Edematous Pancreatitis
[description not available]		02.1710
Colicky Pain
[description not available]		02.1710
Pancreatitis
INFLAMMATION of the PANCREAS. Pancreatitis is classified as acute unless there are computed tomographic or endoscopic retrograde cholangiopancreatographic findings of CHRONIC PANCREATITIS (International Symposium on Acute Pancreatitis, Atlanta, 1992). The two most common forms of acute pancreatitis are ALCOHOLIC PANCREATITIS and gallstone pancreatitis.		02.1710
Abdominal Pain
Sensation of discomfort, distress, or agony in the abdominal region.		02.1710
Infections, Respiratory
[description not available]		06.9352
Adverse Effects, Long Term
[description not available]		04.4511
Respiratory Tract Infections
Invasion of the host RESPIRATORY SYSTEM by microorganisms, usually leading to pathological processes or diseases.		06.9352
Allergic Reaction
[description not available]		06.7372
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		06.7372
Dermatitis Medicamentosa
[description not available]		02.9540
Keratoderma Blennorrhagicum
[description not available]		02.1710
Leg Dermatoses
A nonspecific term used to denote any cutaneous lesion or group of lesions, or eruptions of any type on the leg. (From Stedman, 25th ed)		02.1710
Keratosis
Any horny growth such as a wart or callus.		02.1710
Nasal Catarrh
[description not available]		02.4820
Rhinitis
Inflammation of the NASAL MUCOSA, the mucous membrane lining the NASAL CAVITIES.		02.4820
Insulin Sensitivity
[description not available]		02.1710
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		02.1710
Recrudescence
[description not available]		08.01104
Acid Alpha-Glucosidase Deficiency
[description not available]		02.5720
Glycogen Storage Disease Type II
An autosomal recessively inherited glycogen storage disease caused by GLUCAN 1,4-ALPHA-GLUCOSIDASE deficiency. Large amounts of GLYCOGEN accumulate in the LYSOSOMES of skeletal muscle (MUSCLE, SKELETAL); HEART; LIVER; SPINAL CORD; and BRAIN. Three forms have been described: infantile, childhood, and adult. The infantile form is fatal in infancy and presents with hypotonia and a hypertrophic cardiomyopathy (CARDIOMYOPATHY, HYPERTROPHIC). The childhood form usually presents in the second year of life with proximal weakness and respiratory symptoms. The adult form consists of a slowly progressive proximal myopathy. (From Muscle Nerve 1995;3:S61-9; Menkes, Textbook of Child Neurology, 5th ed, pp73-4)		02.5720
MS (Multiple Sclerosis)
[description not available]		02.4920
Multiple Sclerosis
An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)		02.4920
Bronchial Pneumonia
[description not available]		02.2110
Bronchial Hyperreactivity
Tendency of the smooth muscle of the tracheobronchial tree to contract more intensely in response to a given stimulus than it does in the response seen in normal individuals. This condition is present in virtually all symptomatic patients with asthma. The most prominent manifestation of this smooth muscle contraction is a decrease in airway caliber that can be readily measured in the pulmonary function laboratory.		014.333721
Breathing Sounds
[description not available]		05.5444
Respiratory Sounds
Noises, normal and abnormal, heard on auscultation over any part of the RESPIRATORY TRACT.		05.5444
Bronchospasm, Exercise-Induced
[description not available]		013.994623
Asthma, Exercise-Induced
Asthma attacks following a period of exercise. Usually the induced attack is short-lived and regresses spontaneously. The magnitude of postexertional airway obstruction is strongly influenced by the environment in which exercise is performed (i.e. inhalation of cold air during physical exertion markedly augments the severity of the airway obstruction; conversely, warm humid air blunts or abolishes it).		115.994623
Infections, Picornaviridae
[description not available]		02.7430
Airway Hyper-Responsiveness
[description not available]		06.7283
Lung Injury, Acute
[description not available]		04.7232
Acute Lung Injury
A condition of lung damage that is characterized by bilateral pulmonary infiltrates (PULMONARY EDEMA) rich in NEUTROPHILS, and in the absence of clinical HEART FAILURE. This can represent a spectrum of pulmonary lesions, endothelial and epithelial, due to numerous factors (physical, chemical, or biological).		04.7232
Preterm Birth
[description not available]		02.4820
Complications, Pregnancy
[description not available]		04.1860
Premature Birth
CHILDBIRTH before 37 weeks of PREGNANCY (259 days from the first day of the mother's last menstrual period, or 245 days after FERTILIZATION).		02.4820
Aura
[description not available]		02.110
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.110
Muscle Relaxation
That phase of a muscle twitch during which a muscle returns to a resting position.		06.55181
Cytomegalovirus
A genus of the family HERPESVIRIDAE, subfamily BETAHERPESVIRINAE, infecting the salivary glands, liver, spleen, lungs, eyes, and other organs, in which they produce characteristically enlarged cells with intranuclear inclusions. Infection with Cytomegalovirus is also seen as an opportunistic infection in AIDS.		02.1110
Allergic Bronchopulmonary Aspergilloses
[description not available]		02.1110
Aspergillosis, Allergic Bronchopulmonary
Hypersensitivity reaction (ALLERGIC REACTION) to fungus ASPERGILLUS in an individual with long-standing BRONCHIAL ASTHMA. It is characterized by pulmonary infiltrates, EOSINOPHILIA, elevated serum IMMUNOGLOBULIN E, and skin reactivity to Aspergillus antigen.		02.1110
Apoplexy
[description not available]		02.4820
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		02.4820
Altitude Hypoxia
Low ambient oxygen tension associated with ALTITUDE.		06.4191
Brain Swelling
[description not available]		03.420
Pulmonary Hypertension
[description not available]		04.7521
Altitude Sickness
Multiple symptoms associated with reduced oxygen at high ALTITUDE.		06.4191
Brain Edema
Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6)		03.420
Hypertension, Pulmonary
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.		04.7521
Cystic Fibrosis of Pancreas
[description not available]		07.4884
Cystic Fibrosis
An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION.		07.4884
Bronchiolitis, Exudative
[description not available]		02.1310
Graft-Versus-Host Disease
[description not available]		02.1310
Bronchiolitis Obliterans
Inflammation of the BRONCHIOLES leading to an obstructive lung disease. Bronchioles are characterized by fibrous granulation tissue with bronchial exudates in the lumens. Clinical features include a nonproductive cough and DYSPNEA.		14.1310
Graft vs Host Disease
The clinical entity characterized by anorexia, diarrhea, loss of hair, leukopenia, thrombocytopenia, growth retardation, and eventual death brought about by the GRAFT VS HOST REACTION.		02.1310
Cushing's Syndrome
[description not available]		02.9840
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted
[description not available]		02.1310
Cushing Syndrome
A condition caused by prolonged exposure to excess levels of cortisol (HYDROCORTISONE) or other GLUCOCORTICOIDS from endogenous or exogenous sources. It is characterized by upper body OBESITY; OSTEOPOROSIS; HYPERTENSION; DIABETES MELLITUS; HIRSUTISM; AMENORRHEA; and excess body fluid. Endogenous Cushing syndrome or spontaneous hypercortisolism is divided into two groups, those due to an excess of ADRENOCORTICOTROPIN and those that are ACTH-independent.		02.9840
Hepatitis C
INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown.		02.1310
HIV Coinfection
[description not available]		02.7430
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		02.7430
Allergy, Egg
[description not available]		02.1310
Cirrhosis
[description not available]		02.1310
Chronic Esophagitis, Eosinophilic
[description not available]		02.1310
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		02.1310
Eosinophilic Esophagitis
Chronic ESOPHAGITIS characterized by esophageal mucosal EOSINOPHILIA. It is diagnosed when an increase in EOSINOPHILS are present over the entire esophagus. The reflux symptoms fail to respond to PROTON PUMP INHIBITORS treatment, unlike in GASTROESOPHAGEAL REFLUX DISEASE. The symptoms are associated with IgE-mediated hypersensitivity to food or inhalant allergens.		02.1310
Haemophilus Infections
Infections with bacteria of the genus HAEMOPHILUS.		02.4420
Infections, Staphylococcal
[description not available]		02.1510
Moraxella Infections
[description not available]		02.1510
Staphylococcal Infections
Infections with bacteria of the genus STAPHYLOCOCCUS.		02.1510
Edema, Pulmonary
[description not available]		06.66121
Pulmonary Edema
Excessive accumulation of extravascular fluid in the lung, an indication of a serious underlying disease or disorder. Pulmonary edema prevents efficient PULMONARY GAS EXCHANGE in the PULMONARY ALVEOLI, and can be life-threatening.		06.66121
Obstructive Lung Diseases
[description not available]		014.055835
Lung Diseases, Obstructive
Any disorder marked by obstruction of conducting airways of the lung. AIRWAY OBSTRUCTION may be acute, chronic, intermittent, or persistent.		116.055835
Arrhythmia
[description not available]		06.9565
Tachyarrhythmia
[description not available]		06.2772
Arrhythmias, Cardiac
Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.		06.9565
Tachycardia
Abnormally rapid heartbeat, usually with a HEART RATE above 100 beats per minute for adults. Tachycardia accompanied by disturbance in the cardiac depolarization (cardiac arrhythmia) is called tachyarrhythmia.		06.2772
Cardiomyopathy, Congestive
[description not available]		02.4220
Cardiomyopathy, Dilated
A form of CARDIAC MUSCLE disease that is characterized by ventricular dilation, VENTRICULAR DYSFUNCTION, and HEART FAILURE. Risk factors include SMOKING; ALCOHOL DRINKING; HYPERTENSION; INFECTION; PREGNANCY; and mutations in the LMNA gene encoding LAMIN TYPE A, a NUCLEAR LAMINA protein.		02.4220
Action Tremor
[description not available]		08.1676
Heart Disease, Ischemic
[description not available]		03.821
Bronchitis
Inflammation of the large airways in the lung including any part of the BRONCHI, from the PRIMARY BRONCHI to the TERTIARY BRONCHI.		09.02164
Tremor
Cyclical movement of a body part that can represent either a physiologic process or a manifestation of disease. Intention or action tremor, a common manifestation of CEREBELLAR DISEASES, is aggravated by movement. In contrast, resting tremor is maximal when there is no attempt at voluntary movement, and occurs as a relatively frequent manifestation of PARKINSON DISEASE.		08.1676
Myocardial Ischemia
A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).		03.821
Cardiac Death
[description not available]		02.0510
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.		08.34152
Bone Fractures
[description not available]		012.632625
Low Bone Density
[description not available]		012.592525
Age-Related Osteoporosis
[description not available]		012.672626
Bone Diseases, Metabolic
Diseases that affect the METABOLIC PROCESSES of BONE TISSUE.		012.592525
Osteoporosis
Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.		012.672626
Fractures, Bone
Breaks in bones.		012.632625
Lung, Hyperlucent
A lung with reduced markings on its chest radiograph and increased areas of transradiancy (hyperlucency). A hyperlucent lung is usually associated with pulmonary emphysema or PNEUMOTHORAX.		02.0510
Allergy, Food
[description not available]		02.4420
Food Hypersensitivity
Gastrointestinal disturbances, skin eruptions, or shock due to allergic reactions to allergens in food.		02.4420
Dermatitis, Eczematous
[description not available]		09.6799
Eczema
A pruritic papulovesicular dermatitis occurring as a reaction to many endogenous and exogenous agents (Dorland, 27th ed).		09.6799
Smoking Cessation
Discontinuing the habit of SMOKING.		05.3770
Hypertrophy
General increase in bulk of a part or organ due to CELL ENLARGEMENT and accumulation of FLUIDS AND SECRETIONS, not due to tumor formation, nor to an increase in the number of cells (HYPERPLASIA).		02.0510
Airway Obstruction
Any hindrance to the passage of air into and out of the lungs.		012.5187
Cancer of Cervix
[description not available]		02.0510
Uterine Cervical Neoplasms
Tumors or cancer of the UTERINE CERVIX.		02.0510
Dermatitis, Periocular
[description not available]		02.4520
Dermatitis, Perioral
A papular eruption of unknown etiology that progresses to residual papular erythema and scaling usually confined to the area of the mouth, and almost exclusively occurring in young women. It may also be localized or extend to involve the eyelids and adjacent glabella area of the forehead (periocular dermatitis). (Dorland, 28th ed)		02.4520
Emergencies
Situations or conditions requiring immediate intervention to avoid serious adverse results.		04.131
Cardiovascular Stroke
[description not available]		03.6530
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		03.6530
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		03.3520
Allergy, Drug
[description not available]		02.9340
Atopic Hypersensitivity
[description not available]		05.2243
Drug Hypersensitivity
Immunologically mediated adverse reactions to medicinal substances used legally or illegally.		02.9340
Cognition Disorders
Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.		02.0510
Brain Vascular Disorders
[description not available]		06.3590
Cerebrovascular Disorders
A spectrum of pathological conditions of impaired blood flow in the brain. They can involve vessels (ARTERIES or VEINS) in the CEREBRUM, the CEREBELLUM, and the BRAIN STEM. Major categories include INTRACRANIAL ARTERIOVENOUS MALFORMATIONS; BRAIN ISCHEMIA; CEREBRAL HEMORRHAGE; and others.		06.3590
Weight Reduction
[description not available]		02.9710
Weight Loss
Decrease in existing BODY WEIGHT.		02.9710
Emphysema
A pathological accumulation of air in tissues or organs.		14.4520
Hematuria
Presence of blood in the urine.		02.0610
Cystitis
Inflammation of the URINARY BLADDER, either from bacterial or non-bacterial causes. Cystitis is usually associated with painful urination (dysuria), increased frequency, urgency, and suprapubic pain.		02.0610
Centriacinar Emphysema
[description not available]		03.6230
Bronchial Diseases
Diseases involving the BRONCHI.		06.952
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		15.3720
Asthenia
Clinical sign or symptom manifested as debility, or lack or loss of strength and energy.		02.4720
Hyperglycemia, Postprandial
Abnormally high BLOOD GLUCOSE level after a meal.		02.0610
Hyperglycemia
Abnormally high BLOOD GLUCOSE level.		02.0610
Bronchospasm
[description not available]		07.89123
Cat Diseases
Diseases of the domestic cat (Felis catus or F. domesticus). This term does not include diseases of the so-called big cats such as CHEETAHS; LIONS; tigers, cougars, panthers, leopards, and other Felidae for which the heading CARNIVORA is used.		03.4611
Bronchial Spasm
Spasmodic contraction of the smooth muscle of the bronchi.		19.89123
Rhinitis, Allergic, Nonseasonal
[description not available]		04.7521
Rhinitis, Allergic, Perennial
Inflammation of the mucous membrane of the nose similar to that found in hay fever except that symptoms persist throughout the year. The causes are usually air-borne allergens, particularly dusts, feathers, molds, animal fur, etc.		04.7521
Apical Ballooning Syndrome
[description not available]		02.0710
Takotsubo Cardiomyopathy
A transient left ventricular apical dysfunction or ballooning accompanied by electrocardiographic (ECG) T wave inversions. This abnormality is associated with high levels of CATECHOLAMINES, either administered or endogenously secreted from a tumor or during extreme stress.		02.0710
Anoxemia
[description not available]		06.4863
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		06.4863
Eosinophilia, Tropical
[description not available]		06.1262
Eosinophilia
Abnormal increase of EOSINOPHILS in the blood, tissues or organs.		06.1262
Respiration Disorders
Diseases of the respiratory system in general or unspecified or for a specific respiratory disease not available.		02.9910
Diseases, Occupational
[description not available]		03.6430
Lactic Acidosis
[description not available]		02.0710
Acidosis, Lactic
Acidosis caused by accumulation of lactic acid more rapidly than it can be metabolized. It may occur spontaneously or in association with diseases such as DIABETES MELLITUS; LEUKEMIA; or LIVER FAILURE.		02.0710
Drug Overdose
Accidental or deliberate use of a medication or street drug in excess of normal dosage.		02.0710
Bilateral Headache
[description not available]		05.5732
Nasopharyngitis
Inflammation of the NASOPHARYNX, usually including its mucosa, related lymphoid structure, and glands.		0310
Muscle Spasm
[description not available]		0310
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		05.5732
Spasm
An involuntary contraction of a muscle or group of muscles. Spasms may involve SKELETAL MUSCLE or SMOOTH MUSCLE.		0310
Hay Fever
[description not available]		05.8755
Rhinitis, Allergic, Seasonal
Allergic rhinitis that occurs at the same time every year. It is characterized by acute CONJUNCTIVITIS with lacrimation and ITCHING, and regarded as an allergic condition triggered by specific ALLERGENS.		05.8755
Adenocarcinoma, Basal Cell
[description not available]		02.0110
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.0110
Bruise
[description not available]		07.8355
Drug Withdrawal Symptoms
[description not available]		09.5299
Contusions
Injuries resulting in hemorrhage, usually manifested in the skin.		07.8355
Substance Withdrawal Syndrome
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.		09.5299
Apnea, Obstructive Sleep
[description not available]		02.0110
Sleep Apnea, Obstructive
A disorder characterized by recurrent apneas during sleep despite persistent respiratory efforts. It is due to upper airway obstruction. The respiratory pauses may induce HYPERCAPNIA or HYPOXIA. Cardiac arrhythmias and elevation of systemic and pulmonary arterial pressures may occur. Frequent partial arousals occur throughout sleep, resulting in relative SLEEP DEPRIVATION and daytime tiredness. Associated conditions include OBESITY; ACROMEGALY; MYXEDEMA; micrognathia; MYOTONIC DYSTROPHY; adenotonsilar dystrophy; and NEUROMUSCULAR DISEASES. (From Adams et al., Principles of Neurology, 6th ed, p395)		02.0110
Disease, Pulmonary
[description not available]		03.8121
Lung Diseases
Pathological processes involving any part of the LUNG.		03.8121
Bacterial Disease
[description not available]		03.3120
Bacterial Infections
Infections by bacteria, general or unspecified.		03.3120
Hyperventilation
A pulmonary ventilation rate faster than is metabolically necessary for the exchange of gases. It is the result of an increased frequency of breathing, an increased tidal volume, or a combination of both. It causes an excess intake of oxygen and the blowing off of carbon dioxide.		05.6554
Bagassosis
A diffuse parenchymal lung disease caused by inhaled dust from processing SUGARCANE (bagasse), usually in the manufacturing of wallboard.		03.411
Pneumoconiosis
A diffuse parenchymal lung disease caused by inhalation of dust and by tissue reaction to their presence. These inorganic, organic, particulate, or vaporized matters usually are inhaled by workers in their occupational environment, leading to the various forms (ASBESTOSIS; BYSSINOSIS; and others). Similar air pollution can also have deleterious effects on the general population.		03.411
Constriction, Pathological
[description not available]		06.7142
Constriction, Pathologic
The condition of an anatomical structure's being constricted beyond normal dimensions.		06.7142
Dilatation, Pathologic
The condition of an anatomical structure's being dilated beyond normal dimensions.		02.0210
Edema, Laryngeal
[description not available]		02.0210
Laryngitis
Inflammation of the LARYNGEAL MUCOSA, including the VOCAL CORDS. Laryngitis is characterized by irritation, edema, and reduced pliability of the mucosa leading to VOICE DISORDERS such as APHONIA and HOARSENESS.		02.0210
Leukokeratosis
Leukoplakic lesions related to abnormal keratin fiber formation.		02.0210
Neurologic Voice Disorder
[description not available]		02.0210
Laryngeal Edema
Abnormal accumulation of fluid in tissues of any part of the LARYNX, commonly associated with laryngeal injuries and allergic reactions.		02.0210
Leukoplakia
A white patch lesion found on a MUCOUS MEMBRANE that cannot be scraped off. Leukoplakia is generally considered a precancerous condition, however its appearance may also result from a variety of HEREDITARY DISEASES.		02.0210
Voice Disorders
Pathological processes that affect voice production, usually involving VOCAL CORDS and the LARYNGEAL MUCOSA. Voice disorders can be caused by organic (anatomical), or functional (emotional or psychological) factors leading to DYSPHONIA; APHONIA; and defects in VOICE QUALITY, loudness, and pitch.		02.0210
Community Acquired Infection
[description not available]		02.0210
Eczema, Atopic
[description not available]		03.7921
Dermatitis, Atopic
A chronic inflammatory genetically determined disease of the skin marked by increased ability to form reagin (IgE), with increased susceptibility to allergic rhinitis and asthma, and hereditary disposition to a lowered threshold for pruritus. It is manifested by lichenification, excoriation, and crusting, mainly on the flexural surfaces of the elbow and knee. In infants it is known as infantile eczema.		03.7921
Dysphagia
[description not available]		02.0210
Deglutition Disorders
Difficulty in SWALLOWING which may result from neuromuscular disorder or mechanical obstruction. Dysphagia is classified into two distinct types: oropharyngeal dysphagia due to malfunction of the PHARYNX and UPPER ESOPHAGEAL SPHINCTER; and esophageal dysphagia due to malfunction of the ESOPHAGUS.		02.0210
Diseases of Immune System
[description not available]		03.3420
Immune System Diseases
Disorders caused by abnormal or absent immunologic mechanisms, whether humoral, cell-mediated, or both.		03.3420
Chronic Bronchitis
[description not available]		03.8221
Bronchitis, Chronic
A subcategory of CHRONIC OBSTRUCTIVE PULMONARY DISEASE. The disease is characterized by hypersecretion of mucus accompanied by a chronic (more than 3 months in 2 consecutive years) productive cough. Infectious agents are a major cause of chronic bronchitis.		15.8221
Fasting Hypoglycemia
HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.		02.0210
Hypoglycemia
A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.		02.0210
Birth Weight
The mass or quantity of heaviness of an individual at BIRTH. It is expressed by units of pounds or kilograms.		02.0210
Edema-Proteinuria-Hypertension Gestosis
[description not available]		02.0210
Pre-Eclampsia
A complication of PREGNANCY, characterized by a complex of symptoms including maternal HYPERTENSION and PROTEINURIA with or without pathological EDEMA. Symptoms may range between mild and severe. Pre-eclampsia usually occurs after the 20th week of gestation, but may develop before this time in the presence of trophoblastic disease.		02.0210
Metabolic Acidosis
[description not available]		02.0310
Hypercapnia
A clinical manifestation of abnormal increase in the amount of carbon dioxide in arterial blood.		02.0310
Acidosis
A pathologic condition of acid accumulation or depletion of base in the body. The two main types are RESPIRATORY ACIDOSIS and metabolic acidosis, due to metabolic acid build up.		02.0310
Cardiac Hypertrophy
Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.		02.0310
Cardiomegaly
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.		02.0310
Tricuspid Incompetence
[description not available]		03.4211
Adrenal Gland Hypofunction
[description not available]		02.4420
Adrenal Insufficiency
Conditions in which the production of adrenal CORTICOSTEROIDS falls below the requirement of the body. Adrenal insufficiency can be caused by defects in the ADRENAL GLANDS, the PITUITARY GLAND, or the HYPOTHALAMUS.		02.4420
Bilateral Nasal Obstruction
[description not available]		03.4111
Nasal Obstruction
Any hindrance to the passage of air into and out of the nose. The obstruction may be unilateral or bilateral, and may involve any part of the NASAL CAVITY.		03.4111
Infections, Respiratory Syncytial Virus
[description not available]		02.0310
Respiratory Syncytial Virus Infections
Pneumovirus infections caused by the RESPIRATORY SYNCYTIAL VIRUSES. Humans and cattle are most affected but infections in goats and sheep have been reported.		02.0310
Bone Loss, Osteoclastic
[description not available]		03.4111
Polyarthritis
[description not available]		02.0310
Absence Seizure
[description not available]		02.0310
Drop Attack
[description not available]		02.0310
Arthritis
Acute or chronic inflammation of JOINTS.		02.0310
Depression
Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.		02.0310
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		02.0310
Syncope
A transient loss of consciousness and postural tone caused by diminished blood flow to the brain (i.e., BRAIN ISCHEMIA). Presyncope refers to the sensation of lightheadedness and loss of strength that precedes a syncopal event or accompanies an incomplete syncope. (From Adams et al., Principles of Neurology, 6th ed, pp367-9)		02.0310
Electrocardiogram QT Prolonged
[description not available]		02.0310
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.		02.0310
Dysesthesia
[description not available]		02.0310
Allergy, Latex
[description not available]		02.0310
Endothelioma, Vascular
[description not available]		02.0310
Cancer of Skin
[description not available]		02.0310
Hemangioendothelioma
A neoplasm derived from blood vessels, characterized by numerous prominent endothelial cells that occur singly, in aggregates, and as the lining of congeries of vascular tubes or channels. Hemangioendotheliomas are relatively rare and are of intermediate malignancy (between benign hemangiomas and conventional angiosarcomas). They affect men and women about equally and rarely develop in childhood. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1866)		02.0310
Skin Neoplasms
Tumors or cancer of the SKIN.		02.0310
Lymphocytopenia
[description not available]		04.3522
Lymphopenia
Reduction in the number of lymphocytes.		04.3522
Palsy
[description not available]		02.0410
Allergic Angiitis
[description not available]		02.0410
Mononeuritis
[description not available]		02.0410
Paralysis
A general term most often used to describe severe or complete loss of muscle strength due to motor system disease from the level of the cerebral cortex to the muscle fiber. This term may also occasionally refer to a loss of sensory function. (From Adams et al., Principles of Neurology, 6th ed, p45)		02.0410
Churg-Strauss Syndrome
Widespread necrotizing angiitis with granulomas. Pulmonary involvement is frequent. Asthma or other respiratory infection may precede evidence of vasculitis. Eosinophilia and lung involvement differentiate this disease from POLYARTERITIS NODOSA.		02.0410
Mononeuropathies
Disease or trauma involving a single peripheral nerve in isolation, or out of proportion to evidence of diffuse peripheral nerve dysfunction. Mononeuropathy multiplex refers to a condition characterized by multiple isolated nerve injuries. Mononeuropathies may result from a wide variety of causes, including ISCHEMIA; traumatic injury; compression; CONNECTIVE TISSUE DISEASES; CUMULATIVE TRAUMA DISORDERS; and other conditions.		02.0410
Bleb
[description not available]		03.821
Moniliasis, Oral
[description not available]		03.4311
Candidiasis, Oral
Infection of the mucous membranes of the mouth by a fungus of the genus CANDIDA. (Dorland, 27th ed)		03.4311
Agricultural Worker Disease
[description not available]		03.4311
Labor, Premature
[description not available]		02.0410
alpha 1-Antitrypsin Deficiency
Deficiency of the protease inhibitor ALPHA 1-ANTITRYPSIN that manifests primarily as PULMONARY EMPHYSEMA and LIVER CIRRHOSIS.		03.4311
Left Ventricular Dysfunction
[description not available]		02.0410
Bacterial Endocarditides
[description not available]		02.0410
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		02.0410
Endocarditis, Bacterial
Inflammation of the ENDOCARDIUM caused by BACTERIA that entered the bloodstream. The strains of bacteria vary with predisposing factors, such as CONGENITAL HEART DEFECTS; HEART VALVE DISEASES; HEART VALVE PROSTHESIS IMPLANTATION; or intravenous drug use.		02.0410
Thromboembolism
Obstruction of a blood vessel (embolism) by a blood clot (THROMBUS) in the blood stream.		02.0410
Ventricular Dysfunction, Left
A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall.		02.0410
Anaphylactic Reaction
[description not available]		01.9810
Anaphylaxis
An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death.		01.9810
Electrolytes
Substances that dissociate into two or more ions, to some extent, in water. Solutions of electrolytes thus conduct an electric current and can be decomposed by it (ELECTROLYSIS). (Grant & Hackh's Chemical Dictionary, 5th ed)		01.9810
Acute Hypercapnic Respiratory Failure
[description not available]		02.940
Symptom Cluster
[description not available]		01.9810
Respiratory Insufficiency
Failure to adequately provide oxygen to cells of the body and to remove excess carbon dioxide from them. (Stedman, 25th ed)		02.940
Syndrome
A characteristic symptom complex.		01.9810
Central Nervous System Origin Vertigo
[description not available]		01.9810
Vertigo
An illusion of movement, either of the external world revolving around the individual or of the individual revolving in space. Vertigo may be associated with disorders of the inner ear (EAR, INNER); VESTIBULAR NERVE; BRAINSTEM; or CEREBRAL CORTEX. Lesions in the TEMPORAL LOBE and PARIETAL LOBE may be associated with FOCAL SEIZURES that may feature vertigo as an ictal manifestation. (From Adams et al., Principles of Neurology, 6th ed, pp300-1)		01.9810
Endotoxin Shock
[description not available]		01.9810
Shock, Septic
Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.		01.9810
Central Nervous System Neoplasm
[description not available]		01.9810
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		01.9810
Central Nervous System Neoplasms
Benign and malignant neoplastic processes that arise from or secondarily involve the brain, spinal cord, or meninges.		01.9810
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.3920
Enuresis
Involuntary discharge of URINE after expected age of completed development of urinary control. This can happen during the daytime (DIURNAL ENURESIS) while one is awake or during sleep (NOCTURNAL ENURESIS). Enuresis can be in children or in adults (as persistent primary enuresis and secondary adult-onset enuresis).		01.9910
Gastric Ulcer
[description not available]		01.9910
Stomach Ulcer
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		01.9910
Hives
[description not available]		03.7721
Urticaria
A vascular reaction of the skin characterized by erythema and wheal formation due to localized increase of vascular permeability. The causative mechanism may be allergy, infection, or stress.		03.7721
Infections, Pseudomonas
[description not available]		02.420
Pseudomonas Infections
Infections with bacteria of the genus PSEUDOMONAS.		02.420
Experimental Hepatoma
[description not available]		01.9910
Atrophy, Muscle
[description not available]		01.9910
Cachexia
General ill health, malnutrition, and weight loss, usually associated with chronic disease.		01.9910
Muscular Atrophy
Derangement in size and number of muscle fibers occurring with aging, reduction in blood supply, or following immobilization, prolonged weightlessness, malnutrition, and particularly in denervation.		01.9910
Long Sleeper Syndrome
[description not available]		05.4744
Sleep Wake Disorders
Abnormal sleep-wake schedule or pattern associated with the CIRCADIAN RHYTHM which affect the length, timing, and/or rigidity of the sleep-wake cycle relative to the day-night cycle.		05.4744
Apnea, Sleep
[description not available]		03.3811
Sleep Apnea Syndromes
Disorders characterized by multiple cessations of respirations during sleep that induce partial arousals and interfere with the maintenance of sleep. Sleep apnea syndromes are divided into central (see SLEEP APNEA, CENTRAL), obstructive (see SLEEP APNEA, OBSTRUCTIVE), and mixed central-obstructive types.		03.3811
Esophageal Reflux
[description not available]		02.9110
Gastroesophageal Reflux
Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.		02.9110
Food Poisoning
[description not available]		0210
Human Trichinellosis
[description not available]		0210
Trichinellosis
An infection with TRICHINELLA. It is caused by eating raw or undercooked meat that is infected with larvae of nematode worms TRICHINELLA genus. All members of the TRICHINELLA genus can infect human in addition to TRICHINELLA SPIRALIS, the traditional etiological agent. It is distributed throughout much of the world and is re-emerging in some parts as a public health hazard and a food safety problem.		0210
Postpartum Amenorrhea
[description not available]		03.3811
Amenorrhea
Absence of menstruation.		03.3811
Anesthesia
A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.		0210
Allergic Contact Dermatitis
[description not available]		0210
Dermatitis, Allergic Contact
A contact dermatitis due to allergic sensitization to various substances. These substances subsequently produce inflammatory reactions in the skin of those who have acquired hypersensitivity to them as a result of prior exposure.		0210
Asthmatic Crisis
[description not available]		02.9210
Status Asthmaticus
A sudden intense and continuous aggravation of a state of asthma, marked by dyspnea to the point of exhaustion and collapse and not responding to the usual therapeutic efforts.		02.9210
Stunted Growth
[description not available]		0210
Growth Disorders
Deviations from the average values for a specific age and sex in any or all of the following: height, weight, skeletal proportions, osseous development, or maturation of features. Included here are both acceleration and retardation of growth.		0210
Abnormalities, Drug-Induced
Congenital abnormalities caused by medicinal substances or drugs of abuse given to or taken by the mother, or to which she is inadvertently exposed during the manufacture of such substances. The concept excludes abnormalities resulting from exposure to non-medicinal chemicals in the environment.		0210
Eperythrozoonosis
[description not available]		0210
Extravasation of Contrast Media
[description not available]		0210
Hoarseness
An unnaturally deep or rough quality of voice.		0210
Atrial Ectopic Beats
[description not available]		0210
Adjustment Sleep Disorder
[description not available]		0210
Equine Diseases
[description not available]		03.3911
Mouth Diseases
Diseases involving the MOUTH.		03.3911
Mycoplasma dispar Infection
[description not available]		0210
Breast Diseases
Pathological processes of the BREAST.		01.9710
Delayed Postpartum Hemorrhage
[description not available]		01.9710
Ache
[description not available]		01.9710
Postpartum Hemorrhage
Excess blood loss from uterine bleeding associated with OBSTETRIC LABOR or CHILDBIRTH. It is defined as blood loss greater than 500 ml or of the amount that adversely affects the maternal physiology, such as BLOOD PRESSURE and HEMATOCRIT. Postpartum hemorrhage is divided into two categories, immediate (within first 24 hours after birth) or delayed (after 24 hours postpartum).		01.9710
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		01.9710
Anemia, Fanconi
[description not available]		02.1310
Fanconi Anemia
Congenital disorder affecting all bone marrow elements, resulting in ANEMIA; LEUKOPENIA; and THROMBOPENIA, and associated with cardiac, renal, and limb malformations as well as dermal pigmentary changes. Spontaneous CHROMOSOME BREAKAGE is a feature of this disease along with predisposition to LEUKEMIA. There are at least 7 complementation groups in Fanconi anemia: FANCA, FANCB, FANCC, FANCD1, FANCD2, FANCE, FANCF, FANCG, and FANCL. (from Online Mendelian Inheritance in Man, http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227650, August 20, 2004)		02.1310
Idiopathic Parkinson Disease
[description not available]		02.1310
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		02.1310