Page last updated: 2024-12-06

nedocromil

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

Description

Nedocromil sodium is a mast cell stabilizer. It prevents the release of histamine and other inflammatory mediators from mast cells, which are involved in allergic reactions. Nedocromil sodium is used to treat allergic rhinitis (hay fever) and asthma. It is available as a nasal spray, eye drops, and an inhaler. Nedocromil sodium is effective in treating allergic reactions, but it does not cure the underlying allergy. It is important to note that nedocromil sodium may cause side effects, such as headache, nausea, and cough. If you are experiencing any of these side effects, it is important to talk to your doctor. Nedocromil sodium is an important medication for people with allergies, but it should only be used as directed by your doctor.'

Nedocromil: A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with ASTHMA, including EOSINOPHILS; NEUTROPHILS; MACROPHAGES; MAST CELLS; MONOCYTES; AND PLATELETS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

3,4-dihydroxybenzoate: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

3,4-dihydroxybenzoate : A dihydroxybenzoate having the two hydroxy groups located at the 3- and 4-positions. [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 CID50294
CHEMBL ID746
CHEBI ID7492
SCHEMBL ID4611
MeSH IDM0026945
PubMed CID54675866
CHEBI ID36241
MeSH IDM0026945

Synonyms (85)

Synonym
BIDD:GT0716
fpl-59002
9-ethyl-4,6-dioxo-10-propyl-6,9-dihydro-4h-pyrano[3,2-g]quinoline-2,8-dicarboxylic acid
fpl59002
nedocromil (usan/inn)
D05129
nedocromilum
CHEBI:7492 ,
nedocromilo
69049-73-6
C07255
nedocromil
DB00716
9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4h-pyrano(3,2-g)quinoline-2,8-dicarboxylic acid
nedocromilo [spanish]
nedocromilum [latin]
4h-pyrano(3,2-g)quinoline-2,8-dicarboxylic acid, 9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-
c19h17no7
fpl 59002
9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4h-pyrano(3,2-g)chinolin-2,8-dicarbonsaeure
CHEMBL746
L001326
9-ethyl-4,6-dioxo-10-propylpyrano[3,2-g]quinoline-2,8-dicarboxylic acid
NCGC00182073-02
dtxsid7023356 ,
cas-69049-73-6
dtxcid803356
tox21_113148
nedocromil [usan:inn:ban]
unii-0b535e0bn0
0b535e0bn0 ,
AKOS016014051
FT-0630782
nedocromil [mi]
9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4h-pyrano[3,2-g]quinoline-2,8-dicarboxylic acid
nedocromil [vandf]
nedocromil [usan]
nedocromil [inn]
nedocromil [who-dd]
HY-13448
9-ethyl-4,6-dioxo-10-propylpyrano[5,6-g]quinoline-2,8-dicarboxylic acid
gtpl7607
SCHEMBL4611
tox21_113148_1
NCGC00182073-03
AC-30178
9-ethyl-4,6-dioxo-10-propyl-4h,6h,9h-chromeno[7,6-b]pyridine-2,8-dicarboxylic acid
EX-A098
sr-01000944506
SR-01000944506-1
nedocromil, >=98% (hplc)
mfcd00864606
BCP22724
Q416706
NCGC00182073-07
AS-56153
EN300-19765926
r01ac07
r03bc03
9-ethyl-4,6-dioxo-10-propyl-6,9-dihydro-4h-pyrano(3,2-g)quinoline-2,8-dicarboxylic acid
nedocromil calicum
s01gx04
9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4h-pyrano(3,2-g)chinolin-2,8-dicarbonsaure
nedocromilum (latin)
CHEBI:36241
4,5-dihydroxybenzoate
benzoic acid, 3,4-dihydroxy- (9ci)
1ykp ,
db03946 ,
aids-002961
37580_fluka
aids002961
aids082396
aids-082396
smr000528167
d-3487 ,
C0120
4-10-00-01459 (beilstein handbook reference)
tulip017459
nsc16631
C00230 ,
3,4-dihydroxybenzoate
3,4-dhba
2BUV
Q27104346

Research Excerpts

Overview

Nedocromil sodium is a novel anti-inflammatory agent that has been demonstrated to significantly improve pulmonary function and decrease bronchial hyperreactivity in asthmatic patients. It is a mast-cell stabilizer that prevents or ablates both the acute and late phases of the allergic response.

ExcerptReferenceRelevance
"Nedocromil sodium is a non-steroidal prophylactic agent for the management of asthma. "( [Effect of nedocromil sodium on clinical course and histamine airway responsiveness in patients with pollen induced bronchial asthma].
Grabski, W; Grzelewska-Rzymowska, I; Kroczyńska-Bednarek, J; Rozniecki, J; Zieba, M, 1995
)
2.12
"Nedocromil sodium is a novel anti-inflammatory agent that has been demonstrated to significantly improve pulmonary function and decrease bronchial hyperreactivity in asthmatic patients. "( Clinical overview of nedocromil sodium.
König, P,
)
1.89
"Nedocromil sodium is a non steroidal agent with anti-inflammatory properties."( [Inhaled corticotherapy sparing effect by sodium nedocromil in moderate to severe asthma].
Braunstein, G; Montagut, A; Murciano, D; Pariente, R, 1994
)
1.26
"Nedocromil sodium is a well-tolerated antiasthmatic agent for initial therapy in patients with mild or moderate asthma not well controlled with inhaled beta-2 agonists and/or where methylxanthines are indicated. "( Nedocromil sodium (Tilade).
Bartels, LA; Farrington, E,
)
3.02
"Nedocromil sodium is a recently approved anti-inflammatory medication for the treatment of mild to moderate asthma. "( Nedocromil: a new agent for the treatment of asthma.
Keenan, JM, 1994
)
3.17
"Nedocromil sodium is a mast-cell stabilizer that prevents or ablates both the acute and late phases of the allergic response. "( Topical pharmacotherapy for allergic rhinitis: nedocromil.
Mabry, RL,
)
1.83
"Nedocromil sodium is a non-steroidal prophylactic agent developed for the management of asthma. "( Steroid sparing effect of nedocromil sodium in asthmatic patients on high doses of inhaled steroids.
Britton, JR; Cooper, S; Tattersfield, AE; Wong, CS, 1993
)
2.03
"Nedocromil sodium (NS) is a new drug for the treatment of bronchial asthma. "( Effect of nedocromil sodium and cromoline sodium on atopic basophil function.
Agami, O; Fireman, E; Kivity, S; Topilsky, M, 1996
)
2.14
"Nedocromil sodium is an anti-inflammatory drug, and we questioned whether it also affects the leakage of plasma proteins."( Nedocromil sodium in obstructive airways disease: effect on symptoms and plasma protein leakage in sputum.
Habets, FJ; Hart, AA; Jansen, HM; Out, TA; Roos, CM; Schoonbrood, DF, 1997
)
2.46
"Nedocromil proved to be a good pharmacological tool to inhibit stress-induced release of mediators from mast cells."( Histamine release induced by immobilization, gentle handling and decapitation from mast cells and its inhibition by nedocromil in rats.
Huang, ZL; Maeyama, K; Mochizuki, T; Watanabe, H, 1999
)
1.23
"Nedocromil sodium is a nonsteroidal anti-inflammatory drug used to control asthmatic attacks. "( Nedocromil sodium inhibits canine adenovirus bronchiolitis in beagle puppies.
Anderson, KA; Bice, DE; Bowers, MC; Chen, H; Lantz, RC; Lemen, RJ; Muggenburg, BA; Weger, NS; Witten, ML,
)
3.02
"Nedocromil sodium 2% is an effective treatment for perennial allergic conjunctivitis."( Efficacy and acceptability of nedocromil sodium 2% and olopatadine hydrochloride 0.1% in perennial allergic conjunctivitis.
Alexander, M; Allegro, S; Hicks, A,
)
1.14
"Nedocromil sodium is a new chemical entity. "( [Basic research on nedocromil sodium].
Joseph, M; Rainey, DK, 1992
)
2.05
"Nedocromil sodium is a new prophylactic antiasthmatic medication. "( [Review of North American studies on nedocromil sodium].
Boulet, LP, 1992
)
2
"Nedocromil sodium is a pyranoquinoline dicarboxylic acid derivative, formulated in a metered-dose inhaler. "( A 3-month evaluation of the efficacy of nedocromil sodium in asthma: a randomized, double-blind, placebo-controlled trial of nedocromil sodium conducted by a Canadian multicenter study group.
Boulet, LP; Cartier, A; Cockcroft, D; Gruber, J; Keshmiri, M; Kesten, S; Laberge, F; Lee-Chuy, E; MacDonald, GF; Rebuck, AS, 1990
)
1.99
"Nedocromil is a potent agent for the suppression of bronchial hyperresponsiveness."( [Study of the protective action of nedocromil sodium with bronchial cold-air provocation in children with bronchial asthma].
Ahrens, P; Hofmann, D; Mönkhoff, M; Wönne, R, 1990
)
1.28
"Nedocromil sodium is a new chemical entity which shows similar properties to sodium cromoglycate (SCG) and in addition exhibits a preferential activity in stabilizing mucosal mast cells. "( Nedocromil sodium is more potent than sodium cromoglycate against AMP-induced bronchoconstriction in atopic asthmatic subjects.
Holgate, ST; Phillips, GD; Richards, R, 1989
)
3.16
"Nedocromil is a new non-bronchodilator substance with mast cell stabilizing properties. "( [Protective effect of nedocromil on hypo- and hypertonic solution-induced airway obstruction in exogenous allergic bronchial asthma].
Overlack, A; Rudnik, T; Scheid, ML, 1989
)
2.03
"Nedocromil sodium is a new compound for the long-term treatment of bronchial asthma. "( Nedocromil sodium: a review of clinical studies.
Patalano, F; Ruggieri, F, 1989
)
3.16
"Nedocromil sodium proved to be an effective, safe and well-tolerated drug in the antiinflammatory long-term treatment of reversible obstructive airways disease."( [Nedocromil sodium therapy in asthma patients. Therapeutic effect in addition to treatment with oral theophylline and inhaled bronchodilator agents].
Beck, W; Boos, R; van Kampen, C; Weede, W, 1989
)
1.91
"Nedocromil sodium is a pyranoquinoline derivative that has been developed for the treatment of asthma. "( Effect of nedocromil sodium on sulphur dioxide induced bronchoconstriction.
Barnes, PJ; Dixon, CM; Fuller, RW, 1987
)
2.12
"Nedocromil sodium is a sodium cromoglycate-like drug which inhibits activation and mediator release from inflammatory cells such as eosinophils, neutrophils, macrophages, monocytes, mast cells and platelets. "( Nedocromil sodium. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of reversible obstructive airways disease.
Brogden, RN; Gonzalez, JP, 1987
)
3.16
"Nedocromil sodium is a new antiasthmatic drug with properties similar to sodium cromoglycate. "( The efficacy of nedocromil sodium (Tilade) in asthma.
Alpers, JH; Bowes, G; Czarny, D; Pain, MC; Rubinfeld, AR; Ruffin, RE, 1987
)
2.06

Effects

Nedocromil sodium has been shown to modulate production of a number of powerful cytokines, such as GM-CSF and TNF alpha. It has been used as a replacement for sustained-release theophylline therapy.

ExcerptReferenceRelevance
"Nedocromil sodium has a good safety profile."( Nedocromil sodium for chronic asthma in children.
McKean, M; Sridhar, AV, 2006
)
2.5
"Nedocromil sodium has a good safety profile."( Nedocromil sodium for chronic asthma in children.
McKean, M; Sridhar, AV, 2006
)
2.5
"Nedocromil sodium has also been shown to improve symptoms when added to existing treatment with methylxanthines and corticosteroids."( Nedocromil sodium. An updated review of its pharmacological properties and therapeutic efficacy in asthma.
Brogden, RN; Sorkin, EM, 1993
)
2.45
"Nedocromil sodium has been demonstrated to significantly affect both early-phase and late-phase inflammatory events including effects on mast cell activation and effects on eosinophil function."( Mediator assays and modulation of inflammation in asthma: introduction.
DuBuske, LM,
)
0.85
"Nedocromil sodium has been used as a replacement for sustained-release theophylline therapy; the overall efficacy of nedocromil sodium is at least equivalent to that of theophylline, with less adverse effects occurring in those patients treated with nedocromil sodium rather than with theophylline."( Clinical overview of nedocromil sodium.
König, P,
)
1.17
"Nedocromil sodium has been directly compared with all of the antiasthmatic medications currently used in the United States including theophylline, beta-adrenergic agents, inhaled corticosteroids, and cromolyn sodium."( A review of some recent clinical studies with nedocromil sodium.
Wasserman, SI, 1993
)
1.27
"Nedocromil sodium has good clinical effect, and it may serve as a first-line choice for antiinflammatory therapy in asthma."( Nedocromil sodium versus albuterol in the management of allergic asthma.
de Jong, JW; de Monchy, JG; Koëter, GH; Postma, DS; Teengs, JP; van der Mark, TW, 1994
)
2.45
"Nedocromil sodium has proven to be efficacious in prophylactic and long-term therapy for the treatment of seasonal allergic rhinitis. "( Nedocromil sodium is rapidly effective in the therapy of seasonal allergic rhinitis.
Casale, TB; Donnelly, A, 1993
)
3.17
"Nedocromil sodium has very rapid plasma clearance and is confined to the extravascular space."( General pharmacology, pharmacokinetics, and toxicology of nedocromil sodium.
Clark, B, 1993
)
1.25
"Nedocromil sodium has been shown to modulate production of a number of powerful cytokines, such as GM-CSF and TNF alpha, which are produced by the human nasal epithelium, as well as by involved inflammatory cells and lymphocytes, and which orchestrate the inflammatory response to allergen or to pollutant provocation."( Clinical implications of the pharmacological profile of Tilarin.
Davies, RJ, 1996
)
1.02
"Nedocromil sodium has recently been introduced as a potential substitute for the mast cell stabilizer cromolyn sodium."( Efficacy of nedocromil sodium and cromolyn sodium in an experimental model of ocular allergy.
Calonge, M; Herreras, JM; Montero, JA; Pastor, JC; Ramón, JJ, 1996
)
1.39
"Nedocromil sodium has been shown to be capable of inhibiting chloride ion flux in mast cells, epithelial cells, and neurons. "( Chloride transport and the actions of nedocromil sodium and cromolyn sodium in asthma.
Alton, EW; Norris, AA, 1996
)
2.01
"Nedocromil sodium has prevented the edema in human skin induced by substance P and neurokinin A, and, in the isolated rabbit trachea, has prevented substance P-induced potentiation of cholinergic neural responses at preganglionic (but not postganglionic) sites."( Effects of nedocromil sodium on airway neurogenic mechanisms.
Chung, KF, 1996
)
1.41
"Nedocromil sodium has also been shown to prevent the subsequent development of bronchial hyperresponsiveness."( Clinical effects of nedocromil sodium on allergen-related mechanisms.
Bleecker, ER; Mason, PL; Moore, WC, 1996
)
1.34
"Nedocromil sodium (NS) has been shown to inhibit the late asthma response to inhaled antigen and to control symptoms in chronic asthma; in both processes the eosinophil is thought to be an important contributor. "( Inhibition of eosinophil density change and leukotriene C4 generation by nedocromil sodium.
Bjornsdottir, U; Busse, WW; Geiger, KM; Sedgwick, JB, 1992
)
1.96
"Nedocromil sodium has therefore been profiled in a number of systems ranging from simple in vitro tests and in vivo models of passive anaphylaxis to complex models of anaphylactic bronchoconstriction in actively sensitized primates."( The pharmacology of nedocromil sodium.
Eady, RP, 1986
)
1.32
"Nedocromil sodium has been shown to inhibit adenosine- and neurokinin A-induced bronchoconstriction both in the rat and in man."( Effect of nedocromil sodium on bronchoconstriction induced by adenosine and tachykinins.
Joos, G; Pauwels, R; Van der Straeten, M, 1989
)
1.4
"Nedocromil sodium has been observed to stimulate bronchial C fibers, and it is suggested that this activity may relate to the antitussive effect of the compound."( Effect of nedocromil sodium on SO2-induced airway hyperresponsiveness and citric acid-induced cough in dogs.
Eady, RP; Jackson, DM, 1989
)
1.4

Actions

Nedocromil sodium can inhibit the activity of a range of inflammatory cells including mast cells. It inhibited increase in plasma histamine level induced by stress in a dose-dependent manner.

ExcerptReferenceRelevance
"Nedocromil sodium can inhibit the activity of a range of inflammatory cells including mast cells, as has been demonstrated in several studies."( Effect of nedocromil sodium on mediator release from mast cells.
Pearce, FL, 1993
)
1.41
"Nedocromil inhibited the increase in plasma histamine level induced by stress in a dose-dependent manner."( Histamine release induced by immobilization, gentle handling and decapitation from mast cells and its inhibition by nedocromil in rats.
Huang, ZL; Maeyama, K; Mochizuki, T; Watanabe, H, 1999
)
1.23

Treatment

Nedocromil sodium treatment had no effect on airway responsiveness to histamine, methacholine, and adenosine-5'-monophosphate, pulmonary function, and symptom scores. Nedocromill pretreatment significantly (P < 0.05) decreased PAF-induced hyperreactivity in AKR/J mice but not in W/Wv mice.

ExcerptReferenceRelevance
"Nedocromil treatment halted contractile dysfunction in diabetic mice and reduced cardiac mast cell density, which correlated with reduced bioactive enzyme secretions, reduced expression of extracellular matrix remodeling factors and collagen synthesis, and normalized cytokine levels."( Myocardial remodeling in diabetic cardiomyopathy associated with cardiac mast cell activation.
Cong, XL; Fan, M; Gao, H; Han, SF; Huang, ZG; Jin, Q; Shan, Y, 2013
)
1.11
"Nedocromil-treated eyes showed no statistical or clinical differences from placebo at any time point."( A placebo-controlled comparison of ketotifen fumarate and nedocromil sodium ophthalmic solutions for the prevention of ocular itching with the conjunctival allergen challenge model.
Greiner, JV; Minno, G, 2003
)
1.28
"Nedocromil sodium treatment had no effect on airway responsiveness to histamine, methacholine, and adenosine-5'-monophosphate, pulmonary function, and symptom scores. "( Effects of nedocromil sodium in the treatment of non-allergic subjects with chronic obstructive pulmonary disease.
de Jong, JW; Koëter, GH; Postma, DS; van der Mark, TW, 1994
)
2.12
"Only nedocromil-treated patients demonstrated a statistically significant improvement in morning peak expiratory flow rate (PEFR) as compared with placebo."( Nedocromil sodium is more effective than cromolyn sodium for the treatment of chronic reversible obstructive airway disease.
Chatterjee, SS; Dorow, PD; Lal, S; Venho, KK, 1993
)
2.18
"Nedocromil pretreatment significantly (P < 0.05) decreased PAF-induced hyperreactivity in AKR/J mice but not in W/Wv mice (P > 0.05)."( PAF-induced airways hyperreactivity is modulated by mast cells in mice.
Kleeberger, SR; Longphre, M; Paquette, N; Zhang, LY, 1996
)
1.02
"Nedocromil-treated dogs had significantly (p < 0.05) less mucosal inflammation (mean +/- SEM, 39% +/- 5%), epithelial denudation (36% +/- 5%), and BAL neutrophilia (11 +/- 3) than did Sal/CAV2 dogs (51% +/- 6%, 57% +/- 4%, and 33% +/- 8%, respectively)."( Nedocromil sodium inhibits canine adenovirus bronchiolitis in beagle puppies.
Anderson, KA; Bice, DE; Bowers, MC; Chen, H; Lantz, RC; Lemen, RJ; Muggenburg, BA; Weger, NS; Witten, ML,
)
2.3
"Nedocromil sodium treatment reduced tear concentrations of histamine (by 77%) and PGD(2) (by 70%) at 30 minutes after challenge (both P <.05)."( Nedocromil sodium and levocabastine reduce the symptoms of conjunctival allergen challenge by different mechanisms.
Ahluwalia, P; Anderson, DF; Church, MK; McGill, JI; Wilson, SJ, 2001
)
2.47
"3. Nedocromil sodium pretreatment (10 mg ml-1 by nebulization) 10 min prior to OA completely inhibited the acute bronchoconstrictor response to OA."( Nedocromil sodium inhibits airway hyperresponsiveness and eosinophilic infiltration induced by repeated antigen challenge in guinea-pigs.
Ishida, K; Schellenberg, RR; Thomson, RJ, 1991
)
2.24
"Two nedocromil sodium treated patients were withdrawn owing to treatment taste and vomiting."( Inhaled nedocromil sodium as additional treatment to high dose inhaled corticosteroids in the management of bronchial asthma.
Jørgensen, H; Svendsen, UG, 1991
)
1.2
"Both nedocromil sodium treatments blocked (P less than 0.05) this antigen-induced airway hyperresponsiveness.(ABSTRACT TRUNCATED AT 250 WORDS)"( Nedocromil sodium in allergen-induced bronchial responses and airway hyperresponsiveness in allergic sheep.
Abraham, WM; Eldridge, M; Garrido, R; Nieves, L; Stevenson, JS, 1988
)
2.17
"All nedocromil sodium treatments gave significantly smaller falls in PEFR than placebo."( A comparative study of the effect of three doses of nedocromil sodium and placebo given by pressurized aerosol to asthmatics with exercise-induced bronchoconstriction.
Schaanning, J; Vilsvik, J, 1988
)
1.01
"Treatment with nedocromil sodium significantly (p less than 0.02) inhibited the accumulation of mast cells but not eosinophils."( Allergen-induced changes in the nasal mucous membrane in seasonal allergic rhinitis: effect of nedocromil sodium.
Clague, J; Davies, RJ; Gatland, D; Gomez, E; Lozewicz, S, 1990
)
0.84
"Treatment with nedocromil sodium (100-150 mg/kg), 3 times daily, starting on day 7 post-inoculation, significantly decreases the incidence and the severity of the disease."( Treatment of experimental allergic neuritis with nedocromil sodium.
Johnson, D; Seeldrayers, PA; Weiner, HL; Yasui, D, 1989
)
0.87
"Treatment with nedocromil sodium led to significant (P less than 0.05) improvements in clinic assessment of FEV1 and PEFR both before and after an inhaled bronchodilator from at least the eighth week onwards."( Effects of adding nedocromil sodium (Tilade) to the routine therapy of patients with bronchial asthma.
Chatterjee, PC; Chatterjee, SS; Fyans, PG, 1989
)
0.95
"Treatment with nedocromil sodium significantly reduced the early response to antigen and blocked the late response."( The effect of nedocromil sodium and cromolyn sodium on antigen-induced responses in allergic sheep in vivo and in vitro.
Abraham, WM; Chapman, GA; Jackowski, J; Stevenson, JS; Tallent, MW, 1987
)
0.97
"Treatment with nedocromil sodium (4 mg q.i.d.) for up to 52 weeks demonstrated a progressive reduction in bronchodilator usage throughout the whole treatment period."( Clinical evaluation of nedocromil sodium in asthma.
Holgate, ST, 1986
)
0.92

Toxicity

Prophylactic administration of mometasone furoate before the pollen season is safe and may lead to improved control of SAR compared with nedocromil sodium.

ExcerptReferenceRelevance
" Adverse events were minor and transient."( Efficacy and safety of nedocromil sodium ophthalmic solution in the treatment of seasonal allergic conjunctivitis.
Blumenthal, M; Casale, T; Dockhorn, R; Jarmoszuk, I; Kaiser, H; Smith, R; Zeitz, HJ, 1992
)
0.59
" Extensive laboratory monitoring of renal, hepatic and haematological functions before, during and at the end of the study failed to provide any evidence of drug-induced toxic effects."( The acceptability, safety and efficacy of nedocromil sodium in long-term clinical use in patients with perennial asthma.
Carrasco, E; Sepulveda, R,
)
0.4
" It can be concluded from this study that nedocromil sodium is a safe and effective drug in the management of asthma."( A group comparative study of the safety and efficacy of nedocromil sodium (Tilade) in reversible airways disease: a preliminary report.
Bewtra, AK; Bodman, SF; Chick, TW; Koepke, JW; Nair, N; Nathan, RA; Selner, JC; Storms, WW; Townley, RG; van As, A, 1986
)
0.78
" Test treatments were well-accepted by both adults and children, and there were no major adverse events."( Clinical experience with Tilavist: an overview of efficacy and safety.
Kjellman, NI; Stevens, MT, 1995
)
0.29
" Safety was assessed by reports of adverse events."( Efficacy and safety of nedocromil sodium 2% ophthalmic solution b.i.d. in the treatment of ragweed seasonal allergic conjunctivitis.
Blumenthal, MN; Melamed, J; Schwartz, RH; Zeitz, HJ,
)
0.44
"Sputum induction is a relatively noninvasive and safe procedure that can provide information on eosinophilic inflammation and treatment response and is also associated with several measures of asthma control."( Safety and application of induced sputum analysis in childhood asthma.
Covar, RA; Martin, RJ; Murphy, J; Silkoff, PE; Spahn, JD; Sundstrom, DA; Szefler, SJ, 2004
)
0.32
"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
" Diary cards recording symptoms, use of medication, and adverse events were kept by the patients."( Efficacy and safety of mometasone furoate vs nedocromil sodium as prophylactic treatment for moderate/severe seasonal allergic rhinitis.
Baibas, N; Garris, V; Kompoti, E; Kontou-Fili, K; Manoussakis, E; Papadopoulos, D; Papadopoulos, NG; Petalas, K; Pitsios, C; Saxoni-Papageorgiou, P; Tassios, I, 2006
)
0.59
" No serious adverse event was recorded, and there was no difference between the treatments in any adverse event."( Efficacy and safety of mometasone furoate vs nedocromil sodium as prophylactic treatment for moderate/severe seasonal allergic rhinitis.
Baibas, N; Garris, V; Kompoti, E; Kontou-Fili, K; Manoussakis, E; Papadopoulos, D; Papadopoulos, NG; Petalas, K; Pitsios, C; Saxoni-Papageorgiou, P; Tassios, I, 2006
)
0.59
"Prophylactic administration of mometasone furoate before the pollen season is safe and may lead to improved control of SAR compared with the use of nedocromil sodium."( Efficacy and safety of mometasone furoate vs nedocromil sodium as prophylactic treatment for moderate/severe seasonal allergic rhinitis.
Baibas, N; Garris, V; Kompoti, E; Kontou-Fili, K; Manoussakis, E; Papadopoulos, D; Papadopoulos, NG; Petalas, K; Pitsios, C; Saxoni-Papageorgiou, P; Tassios, I, 2006
)
0.79

Pharmacokinetics

The plasma pharmacokinetic profiles of nedocromil sodium and the pharmacodynamic effect (bronchodilation) of salbutamol were evaluated.

ExcerptReferenceRelevance
"The pharmacokinetic properties of nedocromil sodium give this agent a high safety margin in the treatment of asthma."( General pharmacology, pharmacokinetics, and toxicology of nedocromil sodium.
Clark, B, 1993
)
0.81
" The plasma pharmacokinetic profiles of nedocromil sodium and the pharmacodynamic effect (bronchodilation) of salbutamol were evaluated."( Equivalence of pharmacokinetic characteristics and bronchodilating effect between two combined formulations of nedocromil sodium and salbutamol: MDI and nebulizer solution.
Bustacchini, S; Pistelli, R; Reggio, S; Valente, S, 1996
)
0.77

Compound-Compound Interactions

ExcerptReferenceRelevance
" 12 patients received during a month salbutamol combined with nedocromil (Tilade 8 mg per day)."( [Bronchial hyperreactivity in patients with bronchial asthma treated with salbutamol and salbutamol combined with beclocort or nedocromil].
Krasnowska, M; Liebhart, E; Małolepszy, J, 1994
)
0.73

Bioavailability

ExcerptReferenceRelevance
" This compound is very hydrophilic and is well absorbed by tissues such as the lung but not by tissues with tight junctions such as the gut."( [Basic research on nedocromil sodium].
Joseph, M; Rainey, DK, 1992
)
0.61
" Sodium cromoglycate and nedocromil sodium, which are poorly absorbed from the gastrointestinal tract, were tested by intraperitoneal administration."( LCB 2183 inhibits the inflammation associated with oxazolone-induced contact sensitivity.
Bonhomme, Y; Brown, T; Murray, N; Zoerkler, N, 1994
)
0.59
" This method could be used to compare the relative bioavailability to the lungs following inhalation, and hence the performance of different inhaled products and inhalation techniques."( Determination of the relative bioavailability of nedocromil sodium to the lung following inhalation using urinary excretion.
Aswania, OA; Chrystyn, H; Corlett, SA, 1998
)
0.55
" The degree of this improvement is similar to that observed with long-term inhaled corticosteroid treatment, suggesting that IPO13 variation may improve nuclear bioavailability of endogenous glucocorticoids."( Importin-13 genetic variation is associated with improved airway responsiveness in childhood asthma.
Kaplan, F; Lasky-Su, J; Raby, BA; Tantisira, K; Van Steen, K; Weiss, ST, 2009
)
0.35
"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

Nedocromil significantly relieved preexisting seasonal allergic rhinitis symptoms during peak pollen exposures within 2 hours of the first dose. The therapeutic benefits were maintained on a dosing regimen of four times a day. Addition to an ongoing regimen of beclomethasone may also allow for reduction in the dosage.

ExcerptRelevanceReference
" The results suggest that nedocromil sodium may permit a reduction in theophylline dosage and possibly substitute for theophylline in previously dependent patients."( Effects of the addition of nedocromil sodium to maintenance bronchodilator therapy in the management of chronic asthma.
Callaghan, B; Clancy, L; Teo, NC, 1992
)
0.88
" At 110 min after dosing, subjects took a slow, full inspiration with a 30 s breath-hold, and at 150 min after dosing the subjects performed one single forced expiration."( The effect of respiratory manoeuvres and pharmacological agents on the pharmacokinetics of nedocromil sodium after inhalation.
Holgate, ST; Honeywell, RG; Renwick, AG; Singh, S; Summers, QA, 1992
)
0.5
" Twenty-seven atopic asthmatic adults (21-39 years), with a measurable maximal-response plateau on the dose-response curve (20-55% fall in FEV1), were randomly allocated into two parallel treatment groups."( The long-term effect of nedocromil sodium on the maximal degree of airway narrowing to methacholine in atopic asthmatic subjects.
Bel, EH; Dijkman, JH; Sont, JK; Sterk, PJ, 1992
)
0.59
" dosage but without statistical significance."( Comparison of nedocromil sodium at two dosage frequencies with placebo in the management of chronic asthma.
Drennan, C; Holst, P; Jones, D; Rea, H; Thornley, P; Wells, A, 1992
)
0.64
" Specific lung resistance (SRL) was measured to assess bronchial responses to PAF, and airway responsiveness was determined by deriving a provocative dose of carbachol in breath units causing an increase in SRL to 4 L times centimeters of H2O per liters per second (PD4) from carbachol dose-response curves."( PAF-induced airway responses in sheep: effects of a PAF antagonist and nedocromil sodium.
Abraham, WM; Ahmed, T; D'Brot, J; Fernandez, A; Mansour, E; Soler, M, 1990
)
0.51
"1 X 10(-6) M) and matched placebo were administered by identical metered dose inhalers 30 min before a dose-response to sodium metabisulphite (5-100 mg ml-1) was performed."( Inhaled sodium metabisulphite induced bronchoconstriction: inhibition by nedocromil sodium and sodium cromoglycate.
Dixon, CM; Ind, PW, 1990
)
0.51
" Airway response was measured as FEV1 and the dose of substance P (using a dose range of 23-736 nmol) producing a 20% decrease in FEV1 (PD20) was calculated from the individual semilogarithmic dose-response curves."( Effect of nedocromil on bronchospasm induced by inhalation of substance P in asthmatic subjects.
Crimi, N; Mistretta, A; Oliveri, R; Palermo, B; Palermo, F; Polosa, R; Vancheri, C, 1988
)
0.68
" The dose-response curves for NKA after nedocromil sodium treatment were significantly shifted to the right compared to the curve after placebo-treatment."( The effect of nedocromil sodium on the bronchoconstrictor effect of neurokinin A in subjects with asthma.
Joos, GF; Pauwels, RA; Van der Straeten, ME, 1989
)
0.91
" In guinea-pig airway, microvascular leakage induced by allergen was significantly inhibited by prior treatment with nedocromil sodium (100 micrograms/kg IV), but this had no effect on histamine-induced leakage and reduced PAF-induced leakage only at a dosage of 5 mg/kg."( Effects of nedocromil sodium on airway microvascular leakage and neural reflexes.
Barnes, PJ, 1989
)
0.88
" These results suggest that asthmatic patients who require inhaled steroids show better control of their asthma with the addition of nedocromil sodium than of placebo over a four week period after reduction of the dosage of their inhaled steroids."( Nedocromil sodium in adults with asthma dependent on inhaled corticosteroids: a double blind, placebo controlled study.
Allan, GW; Bone, MF; Burge, PS; Connolly, CK; Dent, RG; Keaney, NP; Kubik, MM; Summers, GD, 1989
)
1.92
" The plasma concentrations and urinary excretion of nedocromil sodium have been determined following single dose administration in six healthy volunteers dosed orally (1 mg kg-1) and intravenously (0."( The pharmacokinetics of nedocromil sodium, a new drug for the treatment of reversible obstructive airways disease, in human volunteers and patients with reversible obstructive airways disease.
Brown, K; Foulds, RA; Lal, S; Morris, DA; Neale, MG; Thomas, D, 1987
)
0.83
" However, preliminary clinical data suggest that although nedocromil sodium cannot substitute completely for bronchodilators or inhaled corticosteroids, with its additive and dose-sparing effects and the convenience of a twice daily dosage it is a promising prophylactic adjunctive agent for the management of reversible obstructive airways disease."( Nedocromil sodium. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of reversible obstructive airways disease.
Brogden, RN; Gonzalez, JP, 1987
)
1.96
" The dose of adenosine producing a 20% change in FEV1(PD20) was calculated from the individual semi-logarithmic dose-response curves."( Comparative study of the effects of nedocromil sodium (4 mg) and sodium cromoglycate (10 mg) on adenosine-induced bronchoconstriction in asthmatic subjects.
Crimi, N; Maccarrone, C; Mistretta, A; Oliveri, R; Palermo, B; Palermo, F; Polosa, R; Vancheri, C, 1988
)
0.55
" Airway responsiveness was assessed by determining from dose-response curves the carbachol concentration (in % wt/vol) that increased sRL to 5 cmH2O/s."( Nedocromil sodium in allergen-induced bronchial responses and airway hyperresponsiveness in allergic sheep.
Abraham, WM; Eldridge, M; Garrido, R; Nieves, L; Stevenson, JS, 1988
)
1.72
"The safety, acceptability and efficacy of nedocromil sodium, given by metered dose inhaler at a dosage of 4 mg four times daily, were investigated in a 52-week open assessment study of 79 perennial bronchial asthmatic patients maintained on oral bronchodilator therapy."( The acceptability, safety and efficacy of nedocromil sodium in long-term clinical use in patients with perennial asthma.
Carrasco, E; Sepulveda, R,
)
0.66
" Nedocromil sodium, at the dosage used in this study, was well tolerated and provided a useful addition to asthma therapy."( A double-blind comparative trial of nedocromil sodium and placebo in the management of bronchial asthma in patients routinely using oral bronchodilators.
Agbayani, BF; Cua-Lim, F; Lachica, D, 1986
)
1.46
" Percentage of dosage of beta 2 adrenergics inhaled as against the total of beta 2 (oral and inhaled)."( [Evaluation of the impact of a care program for asthmatic children on the quality of anti-asthma drug prescriptions].
Alba, F; Gimeno, J; González, M; Madridejos, R, 1995
)
0.29
" Addition of nedocromil sodium to an ongoing regimen of beclomethasone may also allow for reduction in the dosage of inhaled corticosteroid."( Clinical overview of nedocromil sodium.
König, P,
)
0.82
" Each patient was dosed on six occasions, separated by at least 3 days."( The effect of physiological manoeuvres on the absorption of inhaled nedocromil sodium.
Ghosh, SK; Neale, MG; Patel, KR, 1994
)
0.52
" Early asthmatic response was analyzed using three indices: dose producing a 20% decrease in FEV1 (PD20), the slope of and area under the dose-response curve."( Protective effect of nedocromil sodium on the dual asthmatic response to bronchial antigen challenge.
Bessot, JC; Bigot, H; Hutt, N; Kopferschmitt-Kubler, MC; Pauli, G, 1993
)
0.6
"Nedocromil significantly relieved preexisting seasonal allergic rhinitis symptoms during peak pollen exposures within 2 hours of the first dose, and the therapeutic benefits were maintained on a dosing regimen of four times a day."( Nedocromil sodium is rapidly effective in the therapy of seasonal allergic rhinitis.
Casale, TB; Donnelly, A, 1993
)
3.17
" On the first of 5 days, each subject had a history taken and physical examination, SO2 baseline test, laboratory testing, and a methacoline dose-response test."( Effects of nedocromil sodium on the bronchomotor response to sulfur dioxide in asthmatic patients.
Bigby, B; Boushey, H, 1993
)
0.68
" As compared with baseline control (regular dose of inhaled steroids), patients treated with nedocromil plus the 50 percent reduced dosage of inhaled corticosteroid consistently demonstrated comparable or better symptom control."( Nedocromil sodium is more effective than cromolyn sodium for the treatment of chronic reversible obstructive airway disease.
Chatterjee, SS; Dorow, PD; Lal, S; Venho, KK, 1993
)
1.95
"Changes in time course of blood partial pressures of oxygen (PtcO2) and carbon dioxide (PtcCO2) before, during and after challenge with ultrasonically nebulized distilled water (UNDW) were evaluated in 22 children with mild asthma in basal conditions, and after 8 weeks of therapy with inhaled nedocromil sodium at a daily dosage of 8 or 16 mg."( Effect of inhaled nedocromil sodium therapy on blood gas changes in children challenged with ultrasonically nebulized distilled water. A comparison of 8 mg versus 16 mg daily dose.
Bruni, S; Cutrona, FM; De Cristofaro, L; Fabbrizi, E; Giorgi, PL; Kantar, A; Lanfranchi, E; Oggiano, N; Piccinini, R, 1995
)
0.8
" Neither heparin nor nedocromil sodium affected the dose-response curve or the maximum response to Ach."( Protective effect of heparin on immunologically induced tracheal smooth muscle contraction in vitro.
Abraham, MK; Abraham, WM; Ahmed, T, 1996
)
0.61
" Nedocromil sodium was given for 4 weeks in May, at the dosage of 4 mg, 4 times a day in each nostril."( [Nedocromil sodium nasal spray in the treatment of seasonal allergic rhinitis].
Biasi, D; Carletto, A; Lunardi, C; Maleknia, T; Pacor, ML, 1996
)
2.11
" Nedocromil sodium 2% ophthalmic solution was given at the dosage of 1 drop four times a day for four weeks during the month of June."( [Nedocromil sodium as a topical treatment of allergic conjunctivitis due to grasses].
Biasi, D; Carletto, A; Lunardi, C; Maleknia, T; Pacor, ML, 1996
)
2.11
" We wanted to assess whether the combination of a beta 2-bronchodilator with an anti-inflammatory treatment in the same metered-dose inhaler (MDI) with a regular dosing schedule might improve compliance."( Compliance with nedocromil sodium and a nedocromil sodium/salbutamol combination. Compliance Working Group.
Braunstein, GL; Harper, AE; Trinquet, G, 1996
)
0.64
" Ten patients with aspirin-induced asthma underwent three bronchial challenges with a single dose of lysine acetylsalicylate (LASA) that caused a decrease in FEV1 of 25% or more in a preliminary dose-response test 30 min after inhalation of 4 mg nedocromil sodium, 10 mg sodium cromoglycate, or placebo."( Attenuation of aspirin-induced bronchoconstriction by sodium cromoglycate and nedocromil sodium.
Bianco, S; Gambaro, G; Pieroni, MG; Refini, RM; Robuschi, M; Sestini, P; Vaghi, A, 1997
)
0.71
" The authors conclude that studies with NED in nonatopic asthmatics should be continued, but the dosage of the drug ought to be bigger and the time of treatment ought to be longer."( [The effect of nedocromil sodium on the clinical course, ventilatory parameters and nonspecific bronchial hyperreactivity in patients with nonatopic bronchial asthma treated with beclomethasone dipropionate].
Grabski, W; Grzelewska-Rzymowska, I; Kroczyńska-Bednarek, J; Tymińska, K, 1997
)
0.65
" Nedocromil sodium was given twice a day at the dosage of 4 mg each time for two months."( [Nedocromil sodium is effective in the treatment of mild and moderate allergic asthma caused by Dermatophagoides pteronyssinus].
Biasi, D; Carletto, A; Lunardi, C; Maleknia, T; Pacor, ML, 1998
)
2.12
" in nonatopic asthma should be continued, but the dosage of the drug ought to be bigger and the time of treatment should to be longer."( [The effect of nedocromil sodium on spontaneous production of histamine releasing factor (HRF) by mononuclear blood cells in patients with nonatopic bronchial asthma].
Grabski, W; Grzegorczyk, J; Grzelewska-Rzymowska, I; Kroczyńska-Bednarek, J; Kuźmińska, B; Rozniecki, J, 1997
)
0.65
"0 h after dosing is representative of the amount of drug delivered to the lungs."( Determination of the relative bioavailability of nedocromil sodium to the lung following inhalation using urinary excretion.
Aswania, OA; Chrystyn, H; Corlett, SA, 1998
)
0.55
" In 10 healthy volunteers a significantly greater amount of NCS was excreted in the urine following inhalation than after oral dosing (p<0."( Validation of a high-performance liquid chromatography assay for urinary nedocromil sodium following oral and inhaled administration.
Aswania, OA; Chrystyn, H; Corlett, SA, 1998
)
0.53
" The newer mast-cell stabilizing agent nedocromil sodium has a similar safety profile to sodium cromoglycate, but is more potent and has a more convenient twice-daily dosing regimen."( Treating severe eye allergy.
Verin, P, 1998
)
0.57
" Subgroup analyses based on age, dosage of medications and timing of exercise post-inhalation were consistent with the overall pooled analyses."( Nedocromil sodium vs. sodium cromoglycate for preventing exercise-induced bronchoconstriction in asthmatics.
Kelly, K; Rowe, BH; Spooner, CH, 2000
)
1.75
"In this 8-week open-label, prospective study, 30 patients with grass pollen allergy and ocular itching instilled nedocromil sodium 2% ophthalmic solution twice daily for a 5-day baseline period, followed by once-daily dosing thereafter."( Twice-daily and once-daily nedocromil sodium 2% ophthalmic solution for the treatment of seasonal allergic conjunctivitis.
Alexander, M; Allegro, S; Hicks, A,
)
0.64
") to be more effective overall than the regimen containing the highest fexo-fenadine dosage (with nedocromil as rescue only)."( Supplementation of fexofenadine therapy with nedocromil sodium 2% ophthalmic solution to treat ocular symptoms of seasonal allergic conjunctivitis.
Alexander, M; Allegro, S; Hicks, A; Patel, P, 2003
)
0.8
"Supplementation of oral fexofenadine therapy with nedocromil sodium 2% ophthalmic solution relieves ocular symptoms of seasonal allergic rhinoconjunctivitis, allowing control of rhinal symptoms with half the recommended dosage of fexofenadine."( Supplementation of fexofenadine therapy with nedocromil sodium 2% ophthalmic solution to treat ocular symptoms of seasonal allergic conjunctivitis.
Alexander, M; Allegro, S; Hicks, A; Patel, P, 2003
)
0.83
" In this single-center, 7-day, prospective, double-blind, single-dose, crossover, parallel-group study, subjects were randomized to be bilaterally dosed with pemirolast, cromolyn, or ketorolac at each of 3 visits."( A combined analysis of two studies assessing the ocular comfort of antiallergy ophthalmic agents.
Amdahl, L; Graves, A; Shulman, DG; Washington, C, 2003
)
0.32
" They do not induce tolerance, the aerosol dosage can be easily titrated for the individual, and the protective effect is immediate."( Single-dose agents in the prevention of exercise-induced asthma: a descriptive review.
Anderson, SD, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
anti-asthmatic drugA drug used to treat asthma.
anti-allergic agentA drug used to treat allergic reactions.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
dicarboxylic acidAny carboxylic acid containing two carboxy groups.
organic heterotricyclic compoundAn organic tricyclic compound in which at least one of the rings of the tricyclic skeleton contains one or more heteroatoms.
dihydroxybenzoateA hydroxybenzoate that is the conjugate base of dihydroxybenzoic acid.
[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]

Pathways (35)

PathwayProteinsCompounds
vanillin and vanillate degradation II39
vanillin and vanillate degradation I28
trans-caffeate degradation (aerobic)311
4-coumarate degradation (aerobic)517
4-nitrobenzoate degradation26
L-glutamate degradation IX (via 4-aminobutanoate)234
3-chlorobenzoate degradation II (via protocatechuate)512
4-chlorobenzoate degradation416
phthalate degradation (aerobic)19
4-hydroxymandelate degradation638
terephthalate degradation410
superpathway of aromatic compound degradation via 2-hydroxypentadienoate5095
superpathway of aromatic compound degradation via 3-oxoadipate3681
m-cresol degradation116
polybrominated dihydroxylated diphenyl ethers biosynthesis317
spongiadioxin C biosynthesis318
protocatechuate degradation I (meta-cleavage pathway)1529
protocatechuate degradation II (ortho-cleavage pathway)518
protocatechuate degradation III (para-cleavage pathway)515
bisphenol A degradation114
aromatic compounds degradation via u03B2-ketoadipate1127
2,4-xylenol degradation to protocatechuate317
superpathway of vanillin and vanillate degradation827
toluene degradation III (aerobic) (via p-cresol)924
4-methylphenol degradation to protocatechuate311
ubiquinol-6 bypass biosynthesis (eukaryotic)526
quinate degradation II69
quinate degradation I46
superpathway of aerobic toluene degradation3847
shikimate degradation I25
rutin degradation230
shikimate degradation II27
4-toluenesulfonate degradation I614
ubiquinol-6 bypass biosynthesis426
superpathway of aromatic compound degradation3349

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLI family zinc finger 3Homo sapiens (human)Potency33.49150.000714.592883.7951AID1259392
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency30.04740.003041.611522,387.1992AID1159552; AID1159553
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
[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)
Chain A, PROTOCATECHUATE 3,4-DIOXYGENASE ALPHA CHAINAcinetobacter baylyi ADP1Kd100.0000100.0000100.0000100.0000AID977611
Chain B, PROTOCATECHUATE 3,4-DIOXYGENASE BETA CHAINAcinetobacter baylyi ADP1Kd100.0000100.0000100.0000100.0000AID977611
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (76)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
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.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID179612Antiallergic activity against rat passive cutaneous anaphylaxis (PCA) reaction induced by 25 mg/kg of ovalbumin given iv (bolus).1992Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
Antiallergic and cytoprotective activity of new N-phenylbenzamido acid derivatives.
AID1774076Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID89756Inhibition of anti-IgE antibody stimulated histamine release in human lung, at 75 uM compound concentration; Inactive1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Novel indolecarboxamidotetrazoles as potential antiallergy agents.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
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.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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]
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]
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.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID89991Percent inhibition of histamine release from human basophils at a concentration of 10 uM.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel thiophene-, pyrrole-, furan-, and benzenecarboxamidotetrazoles as potential antiallergy agents.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
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]
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
AID1774078Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
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.
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]
AID182636Cytoprotective activity against ethanol-induced gastric lesions in male conscious rats; Inactive.1992Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
Antiallergic and cytoprotective activity of new N-phenylbenzamido acid derivatives.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID88612Evaluated for the inhibition of human basophil histamine release stimulated by anti-Immunoglobulin E (IgE) at a concentration of 10 uM; inactive1992Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5
Novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles as potential antiallergy agents.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID89980Inhibition of anti-IgE antibody-stimulated histamine release in human basophills at 33 uM1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Novel indolecarboxamidotetrazoles as potential antiallergy agents.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID89992Percent inhibition of histamine release from human basophils at a concentration of 33 uM.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel thiophene-, pyrrole-, furan-, and benzenecarboxamidotetrazoles as potential antiallergy agents.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1774075Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
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]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID76552Inhibition of ovalbumin-stimulated histamine release in guinea pig lung, at 75 uM compound concentration; Inactive1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Novel indolecarboxamidotetrazoles as potential antiallergy agents.
AID88614Compound was evaluated for the inhibition of human basophil histamine release stimulated by anti-Immunoglobulin E (IgE) at a concentration of 33 uM; inactive1992Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5
Novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles as potential antiallergy agents.
AID1774079Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
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.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2004Annual review of microbiology, , Volume: 58Biophysical analyses of designed and selected mutants of protocatechuate 3,4-dioxygenase1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (673)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990134 (19.91)18.7374
1990's357 (53.05)18.2507
2000's118 (17.53)29.6817
2010's52 (7.73)24.3611
2020's12 (1.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 52.43

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

MetricThis Compound (vs All)
Research Demand Index52.43 (24.57)
Research Supply Index6.86 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index87.36 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (52.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials254 (36.18%)5.53%
Trials0 (0.00%)5.53%
Reviews110 (15.67%)6.00%
Reviews1 (4.55%)6.00%
Case Studies5 (0.71%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other333 (47.44%)84.16%
Other21 (95.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Two-Part, Randomized, Placebo-Controlled, Crossover Trial to Evaluate the Differential Effects of Inhaled Nedocromil, Oral Montelukast, and Inhaled Mometasone on Markers of the Early Airway Response to Allergen in Asthmatics [NCT01061333]Phase 116 participants (Actual)Interventional2010-06-30Completed
[NCT00135681]0 participants Interventional1996-12-31Completed
Childhood Asthma Management Program [NCT00000575]Phase 31,041 participants (Actual)Interventional1991-09-30Completed
The Effects of Nedocromil Sodium and Cetirizine HCl on Exercise-induced Arterial Hypoxemia in Highly-trained Swimmers [NCT05095311]Phase 44 participants (Actual)Interventional2021-05-19Terminated(stopped due to The recruited population was no longer made available to participate in the study.)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00000575 (7) [back to overview]Bronchial Responsiveness to Serial Methacholine Concentrations Inhaled Into the Lungs
NCT00000575 (7) [back to overview]Change From Baseline in the Rate of Asthma Free Days
NCT00000575 (7) [back to overview]Change in Height From Baseline to End of Treatment, 4-6 Years Later
NCT00000575 (7) [back to overview]Mortality
NCT00000575 (7) [back to overview]Need for Urgent Care for Asthma
NCT00000575 (7) [back to overview]Pulmonary Function as Measured by Normalized FEV1 Over a 4-6 Year Period
NCT00000575 (7) [back to overview]Standardized Depression Scale -- Children's Depression Inventory
NCT01061333 (8) [back to overview]Allergen-induced Changes in Urinary 9P
NCT01061333 (8) [back to overview]Allergen-induced Changes in Urinary Leukotriene (LT) E4
NCT01061333 (8) [back to overview]Allergen-induced Concentrations of Sputum LTC4
NCT01061333 (8) [back to overview]Allergen-induced Concentrations of Sputum LTD4
NCT01061333 (8) [back to overview]Allergen-induced Concentrations of Sputum LTE4
NCT01061333 (8) [back to overview]Change in Forced Expiratory Volume in 1 Second (FEV1)
NCT01061333 (8) [back to overview]Change in Plasma 9P at 20 Minutes
NCT01061333 (8) [back to overview]Change in Plasma 9α-11β-PGF2 (9P) at 5 Minutes

Bronchial Responsiveness to Serial Methacholine Concentrations Inhaled Into the Lungs

Bronchial responsiveness to serial concentrations of inhaled methacholine solution (mg/ml) as measured by serial ratios of follow-up to baseline FEV1 (forced volume of air expired from the lungs in one second). A dose-response curve is calculated from the serial ratios in relation to the serial concentrations to determine PC20, the concentration associated with a 20% drop from baseline in FEV1; this PC20 is the outcome measure with units mg/ml of methacholine. (NCT00000575)
Timeframe: 4-6 years from baseline

Interventionmg/ml of methacholine (Geometric Mean)
1 Budesonide3.0
2 Nedocromil1.8
3 Placebo1.9

[back to top]

Change From Baseline in the Rate of Asthma Free Days

Change from baseline proportion of days without asthma symptoms or other asthma related events to proportion of days during the 4-6 years of follow-up. Asthma free days were determined from daily asthma diaries kept from baseline to the end of treatment, 4-6 years later. (NCT00000575)
Timeframe: 4-6 years from baseline

Interventiondays per month (Mean)
1 Budesonide11.3
2 Nedocromil9.3
3 Placebo9.3

[back to top]

Change in Height From Baseline to End of Treatment, 4-6 Years Later

Change in standing height from baseline to end of treatment. Standing height is measured three times without shoes using a calibrated Harpenden stadiometer; the average of the three repeated heights to the nearest 0.1 cm is the height measure at either baseline or end of treatment. (NCT00000575)
Timeframe: 4-6 years from baseline

Interventioncm (Mean)
1 Budesonide22.7
2 Nedocromil23.7
3 Placebo23.8

[back to top]

Mortality

Counts of deaths from asthma. (NCT00000575)
Timeframe: 4-6 years from baseline

Interventionparticipants (Number)
1 Budesonide0
2 Nedocromil1
3 Placebo0

[back to top]

Need for Urgent Care for Asthma

Counts during the period of treatment (4-6 years) of visits to emergency rooms or equivalent urgent care settings for asthma treatment. (NCT00000575)
Timeframe: 4-6 years from baseline

Interventionrate per 100 person years (Number)
1 Budesonide12
2 Nedocromil16
3 Placebo22

[back to top]

Pulmonary Function as Measured by Normalized FEV1 Over a 4-6 Year Period

Change in FEV1 % of predicted, post-bronchodilator use, from baseline to the end of treatment (4-6 years after randomization). Percent predicted determined from three separate published sets of reference equations for white, black, and Hispanic children - see NEJM 343: 1054-1062, 2000 for more details and references. (NCT00000575)
Timeframe: At the end of treatment, 4-6 years from baseline assessment

Interventionpercentage of predicted value (Mean)
1 Budesonide0.6
2 Nedocromil-0.5
3 Placebo-0.1

[back to top]

Standardized Depression Scale -- Children's Depression Inventory

Change in total score on the Children's Depression Inventory from baseline to the end of treatment, 4-6 years later. The total score ranges from 0-54 with higher scores indicating greater levels of depression. (NCT00000575)
Timeframe: 4-6 years from baseline

Interventionunits on a scale (Mean)
1 Budesonide-3.2
2 Nedocromil-1.8
3 Placebo-2.2

[back to top]

Allergen-induced Changes in Urinary 9P

Fold change over baseline in Urinary 9P at 2 hours post allergen challenge (NCT01061333)
Timeframe: Baseline and 2 hours post allergen challenge

InterventionFold change over baseline (Geometric Mean)
Placebo1.54
Nedocromil1.39
Montelukast1.45
Mometasone1.40

[back to top]

Allergen-induced Changes in Urinary Leukotriene (LT) E4

Fold change over baseline in urinary LTE4 at 2 hours post-allergen challenge (NCT01061333)
Timeframe: Baseline and 2 hours post allergen challenge

InterventionFold change over baseline (Geometric Mean)
Placebo1.77
Nedocromil1.19
Montelukast1.40
Mometasone1.62

[back to top]

Allergen-induced Concentrations of Sputum LTC4

Concentrations of LTC4 in sputum at 2 hours post-allergen challenge (NCT01061333)
Timeframe: 2 hours post allergen challenge

Interventionpg/mL (Geometric Mean)
Placebo13.63
Nedocromil14.02
Montelukast13.76
Mometasone12.14

[back to top]

Allergen-induced Concentrations of Sputum LTD4

Concentrations of LTD4 in sputum at 2 hours post-allergen challenge (NCT01061333)
Timeframe: 2 hours post allergen challenge

Interventionpg/mL (Geometric Mean)
Placebo17.48
Nedocromil18.04
Montelukast18.52
Mometasone17.37

[back to top]

Allergen-induced Concentrations of Sputum LTE4

Concentrations of LTE4 in sputum at 2 hours post-allergen challenge (NCT01061333)
Timeframe: 2 hours post allergen challenge

Interventionpg/mL (Geometric Mean)
Placebo115.5
Nedocromil149.8
Montelukast181.3
Mometasone140.3

[back to top]

Change in Forced Expiratory Volume in 1 Second (FEV1)

Maximal percent drop in FEV1 at 20 minutes post allergen challenge (NCT01061333)
Timeframe: Pre-allergen challenge and 20 minutes after allergen challenge

InterventionPercentage drop in FEV1 (Least Squares Mean)
Placebo-24.66
Nedocromil-8.44
Montelukast-9.15
Mometasone-16.17

[back to top]

Change in Plasma 9P at 20 Minutes

Fold change over baseline of plasma 9P at 20 minutes post-allergen challenge (NCT01061333)
Timeframe: Pre-allergen challenge and 20 minutes post allergen challenge

InterventionFold change over baseline (Geometric Mean)
Placebo1.22
Nedocromil0.72
Montelukast0.72
Mometasone1.06

[back to top]

Change in Plasma 9α-11β-PGF2 (9P) at 5 Minutes

Fold change over baseline of plasma 9P at 5 minutes post-allergen challenge (NCT01061333)
Timeframe: Pre-allergen challenge and 5 minutes post allergen challenge

InterventionFold change over baseline (Geometric Mean)
Placebo0.77
Nedocromil0.97
Montelukast1.08
Mometasone1.00

[back to top]