azelastine profile

Azelastine is a histamine H1 receptor antagonist that is primarily used as a nasal spray for the treatment of allergic rhinitis. It is also available as an ophthalmic solution for the treatment of allergic conjunctivitis. Azelastine is a synthetic compound that is structurally related to other H1 receptor antagonists, such as cetirizine and loratadine. It is believed to work by blocking the binding of histamine to its receptors, which prevents the release of inflammatory mediators and reduces allergic symptoms. Azelastine is generally well-tolerated, but side effects can include drowsiness, headache, and dry mouth. Research on azelastine has focused on its effectiveness in treating allergic conditions, as well as its potential for treating other conditions, such as migraine headaches and chronic obstructive pulmonary disease (COPD). Azelastine is studied because of its potential to alleviate symptoms of allergic rhinitis and conjunctivitis, providing relief for patients suffering from these conditions. It is also being investigated for its potential to treat other inflammatory conditions.'

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

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. [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]

Related Flora

Flora	Rank	Flora Definition	Family	Family Definition
Boswellia	genus	A plant genus of the family BURSERACEAE used medicinally since ancient times. It is a source of salai guggal (the gum resin), boswellic acid (ursane type TRITERPENES), and FRANKINCENSE.[MeSH]	Burseraceae	A plant family of the order Sapindales, subclass Rosidae, class Magnoliopsida. They are resinous trees and shrubs with alternate leaves composed of many leaflets.[MeSH]

ID Source	ID
PubMed CID	2267
CHEMBL ID	639
CHEBI ID	2950
SCHEMBL ID	4239
MeSH ID	M0075361

Synonym
BRD-A68888262-003-02-9
optilast
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1(2h)-one
azelastine (inn)
D07483
optivar (tn)
BSPBIO_003584
azelastinum [inn-latin]
brn 0900747
1(2h)-phthalazinone, 4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1h-azepin-4-yl)-
4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1h-azepin-4-yl)-1(2h)-phthalazinone hydrochloride
4-(p-chlorobenzyl)-2-(n-methylperhydroazepinyl-(4))-1-(2h)-phthalazinone
azelastina [inn-spanish]
azelastine [inn:ban]
azelastine
58581-89-8
C07768
4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1h-azepin-4-yl)-1-(2h)-phthalazinone
DB00972
KBIO3_002992
SPECTRUM2_000649
SPECTRUM3_001984
SPBIO_000657
NCGC00177979-01
azelastinum
CHEBI:2950 ,
azelastina
4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2h)-one
CHEMBL639 ,
nsc-758971
L001153
FT-0659364
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one
A831938
NCGC00177979-02
hsdb 7991
nsc 758971
zqi909440x ,
unii-zqi909440x
(+-)-azelastine
rac-azelastine
bdbm50341448
758637-88-6
FT-0602900
NCGC00177979-03
S12214
AKOS015894880
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one
gtpl7121
azelastine [who-dd]
azelastine [mi]
azelastine [vandf]
azelastine [inn]
AB00698544-09
HY-B0462A
SCHEMBL4239
AB00698544-11
STL429828
tox21 111469
AB00698544_12
AB00698544_13
DTXSID6022638 ,
4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1h-azepin-4-yl)-1(2h)-phthalazinone
4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1h-azepin-4-yl)-1(2h)-phthalazinone
SBI-0206747.P001
FT-0662382
Q419820
BCP14047
BRD-A68888262-003-07-8
1(2h)-phthalazinone,4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1h-azepin-4-yl)-
BS-32594
EN300-7409356
(+/-)-1-(2h)-phthalazinone, 4-
dtxcid502638
4-(p-chlorobenzyl)-2-(n-methylperhydroazepin-4-yl)-1(2h)-phthalazinone
r06ax19
azelastina (inn-spanish)
r01ac03
azelastinum (inn-latin)
s01gx07

Excerpt	Reference	Relevance
"Azelastine is a selective H1 antagonist that was identified to increase mRNA expression of apolipoprotein A."	( Azelastine a potent antihistamine agent, as hypolipidemic and modulator for aortic calcification in diabetic hyperlipidemic rats model. Elnagar, GM; Elsawy, MM; Elseweidy, MM; Zein, N, 2022)	2.89
"Azelastine hydrochloride is a potent second-generation antihistamine, available in Europe and the USA as a nasal spray formulation for the treatment of allergic rhinitis symptoms. "	( A clinical pharmacokinetic study comparing two azelastine hydrochloride nasal formulations in a single-dose design. Canali, A; Du, D; Stolberg, E; Targett, D, 2014)	2.1
"Azelastine is a second generation histamine H₁-receptor antagonist used as an anti-asthmatic and anti-allergic drug that can induce QT prolongation and torsades de pointes. "	( Effect of azelastine on cardiac repolarization of guinea-pig cardiomyocytes, hERG K⁺ channel, and human L-type and T-type Ca²⁺ channel. Choe, H; Choi, BH; Chu, DH; Jo, SH; Lee, SH; Park, MH; Won, KH, 2013)	2.23
"Azelastine nasal spray is a topical antihistaminic drug for the symptomatic treatment of allergic rhinitis. "	( Effects of azelastine nasal spray on nasal and nasopharyngeal microflora. Aksoy, F; Doğan, R; Gönüllü, N; Ozturan, O; Senturk, E; Veyseller, B; Yilmaz, F, 2016)	2.27
"Azelastine nasal spray is a topical antihistamine with a distinctive taste that may be objectionable to some patients. "	( Double-blind, placebo-controlled trial of reformulated azelastine nasal spray in patients with seasonal allergic rhinitis. Bernstein, JA; Ferguson, BJ; Portnoy, J; Prenner, B; Sacks, HJ; Wheeler, WJ, )	1.82
"Azelastine is a second-generation antihistamine approved for treatment of allergic rhinitis. "	( Efficacy and safety of azelastine 0.15% nasal spray and azelastine 0.10% nasal spray in patients with seasonal allergic rhinitis. Berger, W; La Force, C; Lumry, W; Sacks, H; Shah, S; Wheeler, W, )	1.88
"Azelastine hydrochloride is a histamine receptor-1 (H(1)) antagonist with anti-inflammatory properties that is available in the United States as Astelin Nasal Spray for rhinitis patients who are suffering from sneezing and rhinorrhea. "	( Azelastine nasal spray inhibiting parasympathetic function of tracheal smooth muscle. Chou, YL; Chu, YH; Wang, HW, 2010)	3.25
"Azelastine is a selective antagonist at the human histamine-1 receptor and is used clinically in the treatment of allergic rhinitis. "	( In vitro characterisation of the duration of action of the histamine-1 receptor antagonist azelastine. Begg, M; Clark, KL; Hart, AD; Luttmann, MA; Slack, RJ, 2011)	2.03
"Azelastine hydrochloride is a pharmacologically distinct H1-receptor antagonist with a broad spectrum of antiallergic and anti-inflammatory activity. "	( Azelastine nasal spray: a review of pharmacology and clinical efficacy in allergic and nonallergic rhinitis. Lieberman, PL; Settipane, RA, )	3.02
"Azelastine is a selective H(1)-receptor antagonist that inhibits histamine release and interferes with activation of several other mediators of allergic inflammation. "	( Topical azelastine in perennial allergic conjunctivitis. Canonica, GW; Ciprandi, G; Ellers-Lenz, B; Hermann, R; Kolb, C; Petzold, U, 2003)	2.2
"Azelastine nasal spray is an effective treatment for patients with seasonal allergic rhinitis who do not respond to loratadine and is an alternative to switching to another oral antihistamine or to using multiple antihistamines."	( Efficacy of azelastine nasal spray in patients with an unsatisfactory response to loratadine. Berger, WE; White, MV, 2003)	2.14
"Azelastine is a potent H(1)-antihistamine, which is available as a topical nasal spray and indicated for both seasonal allergic and non-allergic vasomotor rhinitis. "	( Review of azelastine nasal spray in the treatment of allergic and non-allergic rhinitis. Corren, J; Lee, C, 2007)	2.18
"Azelastine is a phthalazinone derivative with H(1)-receptor binding approximately tenfold greater than chlorpheniramine on a milligram-per-milligram basis. "	( Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability. Bernstein, JA, 2007)	3.23
"Azelastine is an effective, rapid-acting, and well-tolerated second-generation antihistamine that improves nasal symptoms associated with SAR and VMR. "	( Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability. Bernstein, JA, 2007)	3.23
"Azelastine is a novel, orally effective, long-acting, antiallergic agent. "	( Inhibition of calcium ionophore (A23187)-stimulated histamine release from rat peritoneal mast cells by azelastine: implications for its mode of action. Chand, N; Diamantis, W; Perhach, JL; Pillar, J; Sofia, RD, 1983)	1.92
"Azelastine is a novel, investigational, antiallergy medication that inhibits the generation, release, and/or end-organ activity of multiple mediators of the inflammatory process in vitro and in vivo. "	( Azelastine nasal spray in the management of seasonal allergic rhinitis. Dockhorn, RJ; Freitag, JJ; Meltzer, EO; Weiler, JM; Widlitz, MD, 1994)	3.17
"Azelastine hydrochloride is an antiallergic drug used in the treatment of rhinitis and asthma."	( Effects of the antiallergic drug azelastine hydrochloride on proliferative responses of lymphocytes to food antigens in patients with food-sensitive atopic dermatitis. Agata, H; Fukutomi, O; Hori, T; Kameyama, T; Kondo, N; Nakashima, Y; Shimozawa, N; Suzuki, Y; Tomatsu, S; Yamagishi, A, )	1.13
"Azelastine solution is a topically (nasal) administered antiallergy drug with a preclinical profile suggestive of efficacy in patients with allergic rhinitis."	( A double-blind, controlled trial to assess the safety and efficacy of azelastine nasal spray in seasonal allergic rhinitis. Findlay, SR; Freitag, JJ; Hampel, F; Ratner, PH; van Bavel, J; Widlitz, MD, 1994)	1.97
"Azelastine is a chemically novel multifunctional antiallergy investigational drug capable of inhibiting mast-cell activation and the synthesis and/or release of chemical mediators of the upper and lower airway inflammatory response. "	( Double-blind assessment of azelastine in the treatment of perennial allergic rhinitis. Freitag, JJ; Grossman, J; Halverson, PC; Hemsworth, GR; Meltzer, EO; Shoenwetter, WF; van Bavel, JH; Woehler, TR, 1994)	2.03
"Azelastine is a novel antiallergy medication currently under investigation for the treatment of allergic rhinitis and asthma. "	( Effectiveness of azelastine nasal solution in seasonal allergic rhinitis. Chervinsky, P; Freitag, JJ; Grossman, J; Halverson, PC; Pearlman, DS; Storms, WW; Widlitz, MD, 1994)	2.07
"Azelastine is a new anti-allergic agent which inhibits leukotriene C4 synthesis and release."	( Protection from hypoxic and N-methyl-D-aspartate injury with azelastine, a leukotriene inhibitor. Panizzon, KL; Wallis, RA, 1993)	1.25
"Azelastine is a chemically novel investigational antiallergy drug with the ability to antagonize the effects of chemical mediators of the early- phase and late phase allergic responses suggesting its usefulness in the treatment of upper and lower airway diseases."	( Safety and efficacy of azelastine nasal spray (Astelin NS) for seasonal allergic rhinitis: a 4-week comparative multicenter trial. Chu, TJ; D'Eletto, TA; Dockhorn, RJ; Freitag, JJ; Kraemer, MJ; LaForce, C; Prenner, BM; Widlitz, MD, 1996)	2.05
"Azelastine is a new antihistamine also available in topical form (i.e., nasal spray)."	( Topical azelastine reduces eosinophil activation and intercellular adhesion molecule-1 expression on nasal epithelial cells: an antiallergic activity. Bagnasco, M; Bertolini, C; Canonica, GW; Ciprandi, G; Grögen, J; Mela, GS; Passalacqua, G; Pronzato, C; Ricca, V; Varese, P, 1996)	1.45
"Azelastine is a topical antihistamine, clinically demonstrated to be effective in allergic rhinitis."	( Seasonal rhinitis and azelastine: long- or short-term treatment? Bagnasco, M; Bertolini, C; Canonica, GW; Ciprandi, G; Fiorino, N; Passalacqua, G; Ricca, V; Riccio, AM; Truffelli, T, 1997)	2.05
"Azelastine is a selective H1-receptor antagonist, which has previously been demonstrated to be effective in the treatment of allergic rhinitis. "	( Azelastine eye drops reduce and prevent allergic conjunctival reaction and exert anti-allergic activity. Bagnasco, M; Buscaglia, S; Canonica, GW; Catrullo, A; Ciprandi, G; Fiorino, N; Montagna, P; Pesce, G, 1997)	3.18
"Azelastine is a powerful topical antihistamine, while budesonide appears to be a potent long-acting anti-inflammatory agent."	( Effect of topical applications of budesonide and azelastine on nasal symptoms, eosinophil count and mediator release in atopic patients after nasal allergen challenge during the pollen season. Clement, P; De Waele, M; Smitz, J; Wang, D, 1997)	1.27
"Azelastine is an oral antiallergic compound but there is no direct evidence of its anti-inflammatory actions in bronchial asthma. "	( The effect of azelastine on the infiltration of inflammatory cells into the bronchial mucosa and clinical changes in patients with bronchial asthma. Hoshino, M; Nakamura, Y, 1997)	2.1
"Azelastine is an oral antiallergic drug. "	( [The effect of azelastine on bronchial mucosa in bronchial asthma--suppression of cytokine mRNA]. Shimojo, J, 1998)	2.1
"Azelastine nasal spray is a topical antihistamine treatment for the symptoms of seasonal allergic rhinitis. "	( Management of allergic rhinitis with a combination antihistamine/anti-inflammatory agent. Lieberman, P, 1999)	1.75
"Azelastine nasal spray is an effective and well-tolerated drug in the treatment of seasonal allergic rhinitis."	( [Clinical assessment of azelastine nasal spray in seasonal allergic rhinitis]. Arcimowicz, M; Samoliński, B; Zawisza, E, 1998)	1.33
"Azelastine hydrochloride is an H1-receptor antagonist with antiinflammatory properties that is available in the US as Astelin Nasal Spray for the treatment of seasonal allergic rhinitis. "	( Double-blind trials of azelastine nasal spray monotherapy versus combination therapy with loratadine tablets and beclomethasone nasal spray in patients with seasonal allergic rhinitis. Rhinitis Study Groups. Berger, WE; Fineman, SM; Lieberman, P; Miles, RM, 1999)	2.06
"Azelastine hydrochloride is a nasally administered antihistamine that is effective and safe for the treatment of perennial and seasonal allergic rhinitis. "	( Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis. Craig, TJ; Golden, SJ, 1999)	2.06
"Azelastine hydrochloride is an antihistamine with anti-inflammatory properties that is available in the United States in a nasal spray formulation for the treatment of seasonal allergic rhinitis. "	( Efficacy of azelastine nasal spray in the treatment of vasomotor (perennial nonallergic) rhinitis. Banov, CH; Lieberman, P, 2001)	2.13
"Azelastine is a newly developed antiallergic drug that is reported to antagonize histamine and leukotrienes in addition to its inhibitory action on release of chemical mediators. "	( Effects of azelastine on vagal neuroeffector transmission in canine and human airway smooth muscle. Aizawa, H; Ikeda, T; Inoue, H; Ito, Y; Miyazaki, N; Shigematsu, N, 1990)	2.11
"Azelastine is a new oral antiasthma agent with bronchodilating and antiallergic properties. "	( Evaluation of the safety and efficacy of multiple doses of azelastine to adult patients with bronchial asthma over time. Bucholtz, GA; Kemp, JP; Koepke, JW; Repsher, LH; Spector, SL; Storms, WW; Tinkelman, DG; Van As, A, 1990)	1.97
"Azelastine is a new investigational drug used to treat rhinitis and asthma. "	( The effect of azelastine on neutrophil and eosinophil generation of superoxide. Busse, W; Randlev, B; Sedgwick, J, 1989)	2.08
"Azelastine is an antiallergic agent which demonstrates histamine H1-receptor antagonist activity and also inhibits histamine release from mast cells following antigen and non-antigen stimuli. "	( Azelastine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. McTavish, D; Sorkin, EM, 1989)	3.16
"Azelastine is a phthalazinone derivative with a wide spectrum of pharmacological activities. "	( Inhibition of cysteinyl-leukotriene production by azelastine and its biological significance. Achterrath-Tuckermann, U; Luck, W; Peskar, BA; Simmet, T; Szelenyi, I, 1988)	1.97
"Azelastine is a novel histamine H1 antagonist with putative antileukotriene activity in guinea pigs. "	( The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin. Aurich, R; Harrison, PJ; Holgate, ST; Rafferty, P, 1988)	1.99
"Azelastine appears to be a safe, efficacious medication for seasonal allergic rhinitis."	( Multicenter, double-blind, multiple-dose, parallel-groups efficacy and safety trial of azelastine, chlorpheniramine, and placebo in the treatment of spring allergic rhinitis. Campbell, BH; Connell, JT; Diamond, L; Donnelly, A; Hamilton, LH; Hemsworth, GR; Perhach, JL; Rosenthal, RR; Weiler, JM, 1988)	1.22
"Azelastine is an orally effective and long-acting inhibitor of in vivo synthesis and/or release of leukotrienes."	( Inhibition of leukotriene (SRS-A)-mediated acute lung anaphylaxis by azelastine in guinea pigs. Chand, N; Diamantis, W; Nolan, K; Perhach, JL; Sofia, RD, 1986)	1.23
"Azelastine is a chemically novel medication that has been demonstrated to be clinically effective for asthma and seasonal allergic rhinitis. "	( Efficacy of azelastine in perennial allergic rhinitis: clinical and rhinomanometric evaluation. Cummins, LH; Hemsworth, GR; Meltzer, EO; Orgel, HA; Perhach, JL; Pierson, WE; Storms, WW, 1988)	2.1
"Azelastine is an orally effective inhibitor of mediator activity in allergic reactions and has also been demonstrated to have bronchodilator activity. "	( A dose-response study of the bronchodilator action of azelastine in asthma. Bucholtz, GA; Kemp, JP; Meltzer, EO; Middleton, E; Newton, JJ; Orgel, HA; Perhach, JL; Spector, SL; Welch, MJ, 1987)	1.96
"Azelastine is a phthalazinone derivative with a wide spectrum of pharmacologically relevant activities. "	( Azelastine, a new antiallergic/antiasthmatic agent, inhibits PAF-acether-induced platelet aggregation, paw edema and bronchoconstriction. Achterrath-Tuckermann, U; Szelenyi, I; Weischer, CH, 1988)	3.16

Excerpt	Reference	Relevance
"Azelastine nasal spray has a rapid (15 minute) onset of action. "	( Onset of action of azelastine nasal spray compared with mometasone nasal spray and placebo in subjects with seasonal allergic rhinitis evaluated in an environmental exposure chamber. D'Andrea, C; Patel, P; Sacks, HJ, )	1.9
"Azelastine has a rapid onset of action with a benefit in about 2 hours and a prolonged duration of activity (12 to 24 hours)."	( Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis. Craig, TJ; Golden, SJ, 1999)	1.34
"Azelastine has a significantly stronger inhibitory effect (IC30 = 4.2 microM) on oxygen free radical generation in AM primed by fetal calf serum than in unprimed AM."	( Inhibition of chemiluminescence in granulocytes and alveolar macrophages by azelastine. Kaufmann, B; Lindstaedt, R; Schmidt, J; Szelenyi, I, 1990)	1.23
"Azelastine has also been found to be clinically effective in the treatment of NAR but its mechanism(s) of action is still poorly elucidated."	( Azelastine desensitization of transient receptor potential vanilloid 1: a potential mechanism explaining its therapeutic effect in nonallergic rhinitis. Bernstein, JA; Haar, L; Jones, WK; Luther, K; Singh, U, )	2.3
"As azelastine has previously been found clinically effective in NAR, additional experiments were performed to determine its ability to desensitize TRPV1 ion channels and its effect on regulating intracellular calcium homeostasis."	( Azelastine desensitization of transient receptor potential vanilloid 1: a potential mechanism explaining its therapeutic effect in nonallergic rhinitis. Bernstein, JA; Haar, L; Jones, WK; Luther, K; Singh, U, )	2.09
"Azelastine has unique effects on dendritic cells and T cell interaction in vitro."	( Unique immunomodulatory effects of azelastine on dendritic cells in vitro. Bäumer, W; Kietzmann, M; Schumacher, S; Stark, H, 2014)	1.4
"Azelastine has established antiallergic and anti-inflammatory effects that are unrelated to H1-receptor antagonism, including inhibitory effects on the synthesis of leukotrienes, kinins, and cytokines; the generation of superoxide free radicals; and the expression of the intercellular adhesion molecule 1."	( Azelastine nasal spray: a review of pharmacology and clinical efficacy in allergic and nonallergic rhinitis. Lieberman, PL; Settipane, RA, )	2.3
"Azelastine nasal spray has been shown to benefit patients who have not responded adequately to loratadine and fexofenadine, and is significantly more efficacious than cetirizine and levocabastine in patients with seasonal allergic rhinitis."	( Review of azelastine nasal spray in the treatment of allergic and non-allergic rhinitis. Corren, J; Lee, C, 2007)	1.46
"Azelastine has demonstrated a wide range of pharmacologic effects on chemical mediators of inflammation including leukotrienes, kinins, and platelet activating factor in vitro and in vivo."	( Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability. Bernstein, JA, 2007)	2.5
"Azelastine nasal spray has a rapid (15 minute) onset of action. "	( Onset of action of azelastine nasal spray compared with mometasone nasal spray and placebo in subjects with seasonal allergic rhinitis evaluated in an environmental exposure chamber. D'Andrea, C; Patel, P; Sacks, HJ, )	1.9
"Azelastine has antiallergic properties and has been proposed as a treatment for asthma."	( The effect of H1-receptor blockade on the development of early- and late-phase bronchoconstriction and increased bronchial responsiveness in allergen-induced asthma. Holgate, ST; Ollier, S; Twentyman, OP, 1993)	1.01
"Azelastine has a rapid onset of action with a benefit in about 2 hours and a prolonged duration of activity (12 to 24 hours)."	( Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis. Craig, TJ; Golden, SJ, 1999)	1.34
"Azelastine has the potential to inhibit the proliferation of haSMCs. "	( Antiproliferative effects of the antiallergic agent azelastine on human aortic smooth-muscle cells: an in vitro study. Betsch, A; Claussen, CD; Duda, SD; Feuls, R; Gebert, R; Johst, U; Kehlbach, R; Rodegerdts, E; Schöber, W; Wiskirchen, J, 2002)	2.01
"Azelastine has a significantly stronger inhibitory effect (IC30 = 4.2 microM) on oxygen free radical generation in AM primed by fetal calf serum than in unprimed AM."	( Inhibition of chemiluminescence in granulocytes and alveolar macrophages by azelastine. Kaufmann, B; Lindstaedt, R; Schmidt, J; Szelenyi, I, 1990)	1.23
"Azelastine has previously been demonstrated to inhibit histamine release, to antagonize histamine-mediated responses, and to be a bronchodilator. "	( The interaction of azelastine with human lung histamine H1, beta, and muscarinic receptor-binding sites. Casale, TB, 1989)	2.05

Excerpt	Reference	Relevance
"Azelastine could inhibit electrical field stimulation-induced spike mucosal contraction."	( Azelastine nasal spray inhibiting sympathetic function on human nasal mucosa in patients with allergy rhinitis. Cheng, LH; Chu, YH; Lee, JC; Lin, YY; Wang, HW; Wu, PC, 2019)	2.68
"Azelastine could inhibit both EFS and methoxamine-induced nasal mucosal contractions in vitro."	( Azelastine nasal spray inhibiting sympathetic function on human nasal mucosa in patients with allergy rhinitis. Cheng, LH; Chu, YH; Lee, JC; Lin, YY; Wang, HW; Wu, PC, 2019)	2.68
"Azelastine could inhibit electrical field stimulation-induced spike contraction."	( Azelastine nasal spray inhibiting parasympathetic function of tracheal smooth muscle. Chou, YL; Chu, YH; Wang, HW, 2010)	2.52
"Azelastine was found to inhibit collagen synthesis without altering cell proliferation during quiescent phases."	( Inhibition of collagen expression by azelastine hydrochloride in cultured skin fibroblasts from normal individuals and scleroderma patients. Tajima, S; Yamada, H, 1996)	1.29
"Azelastine did not inhibit CYP3A4 activity but it did inhibit CYP2D6 and CYP2C19 activity with Ki values exceeding maximum plasma concentration by 120 to 800-fold."	( Lack of effect of azelastine and ketoconazole coadministration on electrocardiographic parameters in healthy volunteers. Harr, JE; Levy, RH; Lyness, WH; Mather, GG; Morganroth, J; Perhach, JL; Rosenberg, A; Trager, WF, 1997)	1.35
"Azelastine did not activate significantly adenylate cyclase unless a cytosolic factor was included within the membrane fraction."	( Azelastine potentiates the prostaglandin-induced increase of cyclic AMP content in human platelets and in guinea-pig alveolar macrophages. Bachelet, M; Hatmi, M; Havet, N; Vargaftig, BB, 1992)	2.45
"Azelastine did not inhibit the effect of inhaled LTC4; the geometric mean PD20FEV1 LTC4 (nmol) after a single dose and 14 days' treatment was 0.60 and 0.59 with placebo compared with 0.65 and 0.75 with azelastine."	( Effect of azelastine on bronchoconstriction induced by histamine and leukotriene C4 in patients with extrinsic asthma. Albazzaz, MK; Patel, KR, 1988)	1.4

Excerpt	Reference	Relevance
"Azelastine pre-treatment resulted in a significant reduction of SP in baseline concentration of SP in BAL and NAL from asthmatics."	( Effect of azelastine on substance P content in bronchoalveolar and nasal lavage fluids of patients with allergic asthma. Baumgarten, C; Furkert, J; Kunkel, G; Laake, E; Müller, S; Nieber, K; Rathsack, R, 1993)	1.41
"Azelastine-treated subjects had significantly fewer nasal symptoms during week 4 (p < 0.05), and BDP-treated subjects had fewer nasal symptoms during week 4 (p < 0.05) and week 5 (p < 0.05) compared with subjects given placebo. "	( Effect of intranasal azelastine and beclomethasone dipropionate on nasal symptoms, nasal cytology, and bronchial responsiveness to methacholine in allergic rhinitis in response to grass pollens. Chiapparino, A; Foresi, A; Hernandez, A; Marazzini, L; Mastropasqua, B; Pelucchi, A, 1995)	2.05
"Azelastine and oxatomide treatment did not improve mucosal PG levels, however, both drugs reduced significantly increases in peptide-LT level, 9.3 +/- 4.6 and 8.6 +/- 4.4, respectively."	( Reduction of adverse effects of indomethacin by anti-allergic drugs in rat stomachs. Goto, H; Hamajima, E; Hoshino, H; Ohara, A; Ozawa, T; Sugiyama, S; Tsukamoto, Y, 1992)	1
"Treatment with azelastine reduced both reflexes."	( Elucidating the mechanism underlying the ocular symptoms associated with allergic rhinitis. Baroody, FM; deTineo, M; Naclerio, RM; Pinto, J, )	0.47
"Treatment with azelastine also resulted in a clinically meaningful improvement in nasal congestion."	( Double-blind assessment of azelastine in the treatment of perennial allergic rhinitis. Freitag, JJ; Grossman, J; Halverson, PC; Hemsworth, GR; Meltzer, EO; Shoenwetter, WF; van Bavel, JH; Woehler, TR, 1994)	0.93
"Pretreatment with azelastine inhibited PAF-induced vascular leakage without affecting neutrophil accumulation."	( Effect of azelastine on platelet-activating factor-induced microvascular leakage in rat airways. Aoshiba, K; Kondo, M; Nagai, A; Nakata, J; Tagaya, E; Tamaoki, J; Yamawaki, I, 1999)	1.03
"Pretreatment with azelastine or cetirizine inhibits the allergen-induced release of mast-cell mediators from the human nasal mucosa. "	( Histamine and tryptase in nasal lavage fluid after allergen challenge: effect of 1 week of pretreatment with intranasal azelastine or systemic cetirizine. Jacobi, HH; Malling, HJ; Mygind, N; Poulsen, LK; Skov, PS, 1999)	0.85
"Treatment with azelastine (4 mg/os once daily) inhibited immediate reactions to allergens by 65% (range 55-74) and to histamine by 68% (range 47-82)."	( Investigation of the anti-allergic activity of azelastine on the immediate and late-phase reactions to allergens and histamine using telethermography. Bähre, M; De Weck, AL; Derer, T, 2000)	0.9
"Treatment with azelastine had no effect on the levels of albumin, interleukin-4, interleukin-5, intercellular adhesion molecule-1, tumor necrosis factor-alpha, and eosinophil cationic protein during the late-phase response."	( Effects of intranasal azelastine on the response to nasal allergen challenge. Assanasen, P; Baroody, FM; deTineo, M; Haney, L; Naclerio, RM; Saengpanich, S, 2002)	0.97
"Pre-treatment with azelastine significantly inhibited both the LTC4 release and the increase in nasal vascular permeability."	( Inhibitory effects of azelastine on nasal allergic responses in sensitized guinea pigs. Asakura, K; Kataura, A; Shirasaki, H; Sohma, S, 1992)	0.92
"Pretreatment with azelastine (3 mg/kg, p.o., 2 hours prior to antigen challenge) tended to normalize microviscosity in the bronchoalveolar lavage fluid obtained from challenged guinea pigs."	( Effect of azelastine on microviscosity of bronchial lavage fluid obtained from actively sensitized and challenged guinea pigs. Achterrath-Tuckermann, U; Motta, C; Szelenyi, I, 1989)	1
"Treatment with azelastine 4.4 mg twice daily for 21 days did not produce any change in salivary antipyrine elimination in 8 normal volunteers."	( The effect of repeated oral doses of azelastine hydrochloride on antipyrine half-life in normal volunteers. Aurich, R; Johnston, A; Turner, P; Warrington, SJ, 1988)	0.9

Excerpt	Reference	Relevance
" The occurrence of these adverse events decreased with time throughout the study."	( Evaluation of the safety and efficacy of multiple doses of azelastine to adult patients with bronchial asthma over time. Bucholtz, GA; Kemp, JP; Koepke, JW; Repsher, LH; Spector, SL; Storms, WW; Tinkelman, DG; Van As, A, 1990)	0.52
" Elicited, volunteered, and observed adverse experiences were recorded for each subject and compared among groups."	( Multicenter, double-blind, multiple-dose, parallel-groups efficacy and safety trial of azelastine, chlorpheniramine, and placebo in the treatment of spring allergic rhinitis. Campbell, BH; Connell, JT; Diamond, L; Donnelly, A; Hamilton, LH; Hemsworth, GR; Perhach, JL; Rosenthal, RR; Weiler, JM, 1988)	0.5
" Diary cards were completed hourly (11:00 AM to 4:00 PM) and at 6:00, 8:00, and 10:00 PM on Saturday and again hourly on Sunday (from 8:00 AM to 4:00 PM) to evaluate rhinitis symptoms and adverse events."	( A dose-ranging study of the efficacy and safety of azelastine nasal spray in the treatment of seasonal allergic rhinitis with an acute model. Benson, PM; Freitag, J; Meltzer, EO; Weiler, JM; Weiler, K; Widlitz, MD, 1994)	0.54
" The groups that received 2 sprays of azelastine per nostril once and twice daily and the chlorpheniramine group had statistically significantly more improvement in total rhinitis symptoms than the placebo group without serious adverse events."	( A dose-ranging study of the efficacy and safety of azelastine nasal spray in the treatment of seasonal allergic rhinitis with an acute model. Benson, PM; Freitag, J; Meltzer, EO; Weiler, JM; Weiler, K; Widlitz, MD, 1994)	0.81
" Adverse experiences in the azelastine groups were minor and infrequent."	( A double-blind, controlled trial to assess the safety and efficacy of azelastine nasal spray in seasonal allergic rhinitis. Findlay, SR; Freitag, JJ; Hampel, F; Ratner, PH; van Bavel, J; Widlitz, MD, 1994)	0.82
" The only notable adverse experiences in the azelastine group were alterations in taste perception and a small mean increase in body weight."	( An evaluation of the efficacy and safety of azelastine in patients with chronic asthma. Azelastine-Asthma Study Group. , 1996)	0.81
"Azelastine hydrochloride is a nasally administered antihistamine that is effective and safe for the treatment of perennial and seasonal allergic rhinitis."	( Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis. Craig, TJ; Golden, SJ, 1999)	2.06
" No serious adverse events were reported, all adverse events were related to nasal symptoms."	( Comparative efficacy and safety of azelastine and levocabastine nasal sprays in patients with seasonal allergic rhinitis. Baehre, M; Falser, N; Rahlfs, VW; Wober, W, 2001)	0.59
" The use of topical azelastine did not cause any adverse event."	( Efficacy and safety of topical azelastine compared with topical mitomycin C in patients with allergic conjunctivitis. Pandey, RM; Ratan, SK; Sodhi, PK, 2003)	0.93
" The use of topical MMC in low doses does not cause any significant adverse effect."	( Efficacy and safety of topical azelastine compared with topical mitomycin C in patients with allergic conjunctivitis. Pandey, RM; Ratan, SK; Sodhi, PK, 2003)	0.6
" The intranasal route of administration delivers drug directly to the target organ, thereby minimising the potential for the systemic adverse effects that may be evident with oral therapy."	( Safety and tolerability profiles of intranasal antihistamines and intranasal corticosteroids in the treatment of allergic rhinitis. Howarth, PH; Salib, RJ, 2003)	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
"When antiallergic agents are used to treat allergic conjunctivitis other than olopatadine, a particularly toxic effect on conjunctival cells associated with azelastine and ketotifen, rather than olopatadine, should be considered clinically."	( Comparison of the conjunctival toxicity of topical ocular antiallergic agents. Kim, N; Lee, JE; Lee, JS; Oum, BS, 2008)	0.54
" In a 1-year safety study, patients with chronic rhinitis were randomized to the new formulation (n = 430) or the original formulation (n = 432) to assess tolerability and the potential for adverse effects on the nasal mucosa."	( Pharmacokinetic characteristics and safety and tolerability of a reformulated azelastine hydrochloride nasal spray in patients with chronic rhinitis. Berger, WE, 2009)	0.58
"The new formulation was safe and well tolerated with long-term use and had a comparable pharmacokinetic profile to the original formulation."	( Pharmacokinetic characteristics and safety and tolerability of a reformulated azelastine hydrochloride nasal spray in patients with chronic rhinitis. Berger, WE, 2009)	0.58
"15% may be effective with once-daily dosing without increasing the incidence of adverse events."	( Efficacy and safety of azelastine 0.15% nasal spray administered once daily in subjects with seasonal allergic rhinitis. Amar, NJ; Howland, WC; Sacks, H; van Bavel, J; Wheeler, W, )	0.44
"15% allowed for once-daily dosing without increasing the incidence of adverse effects."	( Efficacy and safety of azelastine 0.15% nasal spray administered once daily in patients with allergy to Texas mountain cedar pollen. Amar, NJ; Howland, WC; Sacks, H; Wheeler, W, )	0.44
"4%) were the most common adverse events."	( Efficacy and safety of azelastine 0.15% nasal spray administered once daily in patients with allergy to Texas mountain cedar pollen. Amar, NJ; Howland, WC; Sacks, H; Wheeler, W, )	0.44
" Safety was assessed by child- or caregiver-reported adverse events, nasal examinations, vital signs, and laboratory assessments."	( Safety of a novel intranasal formulation of azelastine hydrochloride and fluticasone propionate in children: A randomized clinical trial. Berger, W; Fineman, S; Gawchik, S; Sher, E, 2018)	0.74
"The incidence of treatment-related adverse events (TRAEs) was low in both the AZE/FP (16%) and FP-only (12%) groups after 90 days' continuous use."	( Safety of a novel intranasal formulation of azelastine hydrochloride and fluticasone propionate in children: A randomized clinical trial. Berger, W; Fineman, S; Gawchik, S; Sher, E, 2018)	0.74
"The intranasal formulation of AZE and FP was safe and well tolerated after 3 months' continuous use in children with allergic rhinitis."	( Safety of a novel intranasal formulation of azelastine hydrochloride and fluticasone propionate in children: A randomized clinical trial. Berger, W; Fineman, S; Gawchik, S; Sher, E, 2018)	0.74

Excerpt	Reference	Relevance
" For pharmacokinetic modeling, the mean concentrations of AZ and DAZ in plasma were converted to those in blood."	( Pharmacokinetics of azelastine and its active metabolite, desmethylazelastine, in guinea pigs. Adusumalli, VE; Kucharczyk, N; Sofia, RD; Wong, KK, )	0.45
" When comparing pharmacokinetic parameters from plasma levels (determined with a radioimmunoassay (RIA)) of the elderly with those of young volunteers (26 +/- 5 years), there is a difference in half lives (t1/2 elderly vs young: single dose: 38."	( Tolerability and pharmacokinetics of single and multiple doses of azelastine hydrochloride in elderly volunteers. Borbe, HO; Büker, KM; Peter, G; Riethmüller-Winzen, H; Romeis, P, 1995)	0.53
" The values of AUC0-infinity and Cmax increased linear to the dose (means of AUC0-infinity: 47."	( Tolerability, pharmacokinetics and dose linearity of azelastine hydrochloride in healthy subjects. Borbe, HO; Büker, KM; Peter, G; Riethmüller-Winzen, H; Romeis, P, 1994)	0.54
" The peak concentration (Cmax) of AZ, especially after the first dose, was significantly higher in pediatric dogs than that in adult dogs, whereas following the multiple AZ administrations, the bioavailability parameters for the last dose were similar in the two age groups."	( Pharmacokinetics of the new antiasthma and antiallergy drug, azelastine, in pediatric and adult beagle dogs. Adusumalli, VE; Kucharczyk, N; Sofia, RD; Wichmann, JK; Wong, KK, 1993)	0.53
" Pharmacokinetic investigations have shown the drug to be highly bound to blood proteins, mainly serum albumin, and to have a low brain uptake, explaining its lack of sedative effects."	( Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist. Carrupt, PA; Jolliet, P; Morin, C; Morin, D; Pagliara, A; Rihoux, JP; Testa, B; Tillement, JP; Urien, S, 1998)	0.3
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."	( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004)	0.32
" Since Japanese physicians frequently prescribe this formula combined with azelastine hydrochloride, one of anti-histamine and anti-allergic medicines, we evaluated the pharmacokinetic interactions between SST and azelastine hydrochloride in rats to obtain the drug information for the prevention from disadvantage or adverse effects by their combined therapy."	( Pharmacokinetic interactions between Japanese traditional medicine (kampo) and modern medicine (III). Effect of Sho-seiryu-to on the pharmacokinetics of azelastine hydrochloride in rats. Inagaki, T; Kano, Y; Komatsu, K; Makino, T, 2004)	0.75
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."	( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008)	0.35
"Two studies were conducted to evaluate the safety, tolerability and pharmacokinetic parameters of this new formulation compared with the original azelastine nasal spray."	( Pharmacokinetic characteristics and safety and tolerability of a reformulated azelastine hydrochloride nasal spray in patients with chronic rhinitis. Berger, WE, 2009)	0.78
"In a pharmacokinetic study, 18 healthy volunteers received either a single dose of the new formulation or the original formulation and pharmacokinetic parameters were determined."	( Pharmacokinetic characteristics and safety and tolerability of a reformulated azelastine hydrochloride nasal spray in patients with chronic rhinitis. Berger, WE, 2009)	0.58
"The new formulation was safe and well tolerated with long-term use and had a comparable pharmacokinetic profile to the original formulation."	( Pharmacokinetic characteristics and safety and tolerability of a reformulated azelastine hydrochloride nasal spray in patients with chronic rhinitis. Berger, WE, 2009)	0.58
" The present study was aimed at comparing the clinical pharmacokinetic profiles and assessing the bioequivalence of the new formulation of azelastine hydrochloride with a marketed reference nasal spray product."	( A clinical pharmacokinetic study comparing two azelastine hydrochloride nasal formulations in a single-dose design. Canali, A; Du, D; Stolberg, E; Targett, D, 2014)	0.86

Excerpt	Reference	Relevance
" It is hypothesized that the platelet activating factor receptor antagonist ginkgolide B (GB) and the carotenoid antioxidant astaxanthin (ASX) interact with antihistamines cetirizine dihydrochloride (CTZ) and azelastine (AZE) to potentiate their ability to downregulate potentially pathological immune activation."	( In vitro suppression of lymphocyte activation in patients with seasonal allergic rhinitis and pollen-related asthma by cetirizine or azelastine in combination with ginkgolide B or astaxanthin. Abal, A; Al-Awadhi, R; Al-Sharah, S; Arifhodzic, N; Azeamouzi, C; Haines, D; Mahmoud, FF; Tosaki, A, 2012)	0.77
"A retrospective study was conducted to investigate the efficacy of azelastine nasal spray combined with mussel mucin in the treatment of allergic rhinitis (AR) and the effects of CCL26 and CC chemokine receptor-3 (CCR3)."	( Analysis of the efficacy of azelastine nasal spray combined with mussel mucin in the treatment of allergic rhinitis and the influence of peripheral blood CCL26 and CCR3 levels. Liu, S; Liu, Y; Lu, SF; Zang, GM, 2023)	1.44
"Azelastine nasal spray combined with mussel mucin is effective in the treatment of allergic rhinitis, which can effectively improve patients' clinical symptoms, alleviate nasal ventilation disorders, reduce inflammatory reactions, and improve sleep quality."	( Analysis of the efficacy of azelastine nasal spray combined with mussel mucin in the treatment of allergic rhinitis and the influence of peripheral blood CCL26 and CCR3 levels. Liu, S; Liu, Y; Lu, SF; Zang, GM, 2023)	2.65

Excerpt	Reference	Relevance
" From the analysis according to the Loo-Riegelman method, the absorption rate was revealed to be described by a first-order process."	( Pharmacokinetic and biopharmaceutical studies on azelastine hydrochloride in beagle dogs by quantitative selected-ion monitoring. Fujita, T; Hasegawa, J; Hirose, N; Sugiyama, K; Tanaka, M; Tomono, Y, 1981)	0.52
" After nasal administration, azelastine is systemically absorbed with a bioavailability of about 40%."	( Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis. Craig, TJ; Golden, SJ, 1999)	0.91
" The systemic bioavailability of intranasal corticosteroids varies from <1% to up to 40-50% and influences the risk of systemic adverse effects."	( Safety and tolerability profiles of intranasal antihistamines and intranasal corticosteroids in the treatment of allergic rhinitis. Howarth, PH; Salib, RJ, 2003)	0.32
" • For new combination medicinal products such as MP29-02, the determination of possible pharmacokinetic (PK) drug-drug interactions between both active components and formulation-based bioavailability alterations is essential."	( Bioavailability and disposition of azelastine and fluticasone propionate when delivered by MP29-02, a novel aqueous nasal spray. Bousquet, J; Derendorf, H; Hermann, R; Mascher, H; Maus, J; Munzel, U; Petzold, U, 2012)	0.66
"• This paper provides for the first time information on potential drug-drug interactions, AZE and FP bioavailability and disposition characteristics of each component administered by the novel nasal spray formulation MP29-02."	( Bioavailability and disposition of azelastine and fluticasone propionate when delivered by MP29-02, a novel aqueous nasal spray. Bousquet, J; Derendorf, H; Hermann, R; Mascher, H; Maus, J; Munzel, U; Petzold, U, 2012)	0.66
" Azelastine bioavailability was similar for MP29-02 and Astelin®."	( Bioavailability and disposition of azelastine and fluticasone propionate when delivered by MP29-02, a novel aqueous nasal spray. Bousquet, J; Derendorf, H; Hermann, R; Mascher, H; Maus, J; Munzel, U; Petzold, U, 2012)	1.57
" Pharmacokinetic studies have revealed no drug-drug interactions but a discrete increase in bioavailability of fluticasone propionate which was considered clinically unimportant."	( New patents of fixed combinations of nasal antihistamines and corticosteroids in allergic rhinitis. Wolthers, OD, 2013)	0.39
"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

Excerpt	Relevance	Reference
" No large differences in the quantitative profile between the two dosing routes were observed."	( Metabolism of [14C]azelastine in guinea pigs. Kucharczyk, N; Sofia, RD; Wong, KK; Yang, JT, )	0.46
" A combination of FPL55712 (leukotriene antagonist), diphenhydramine (histamine antagonist), and indomethacin (cyclooxygenase inhibitor) shifted the dose-response curve of ET-1 to the right and suppressed the maximal constriction."	( Multiple mechanisms of bronchoconstrictive responses to endothelin-1. Hasegawa, S; Hirata, F; Ishii, Y; Ninomiya, H; Nomura, A; Ohse, H; Saotome, M; Uchida, Y, 1991)	0.28
" In dose-response experiments with azelastine, 1 to 100 mumol/L, significant inhibition of histamine release was consistently observed in azelastine concentrations greater than or equal to 10 mumol/L."	( Azelastine inhibits IgE-mediated human basophil histamine release. Casale, TB; Little, MM, 1989)	2
" In conclusion, 8 mg/day azelastine, in either a single or twice daily dosage regimen may be regarded as providing effective prophylaxis against bronchial asthma."	( Azelastine in the prophylactic treatment of bronchial asthma: an Italian multicentre comparison with ketotifen. Ambrosi, L; Bariffi, F; Carino, M; Catena, E; Ceccarelli, G; Ciampini, M; Condoluci, M; Crimi, N; Ferretti, G; Gambaro, G, )	1.88
" With three different doses of oral azelastine, we have performed a dose-response study to determine its protective effect on the airways against histamine-induced bronchoconstriction in 12 patients with mild, atopic asthma."	( The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin. Aurich, R; Harrison, PJ; Holgate, ST; Rafferty, P, 1988)	0.82
" Despite azelastine and desmethyl azelastine blood levels that were proportionate to the dosage range, the bronchodilator effect as measured by FEV1 and forced expiratory flow rate between 25% and 75% of FVC was proportionately greater with 4 mg of azelastine during the 8-hour study period than the anticipated bronchodilator response with the 8 and 16 mg doses."	( Pharmacodynamic evaluation of azelastine in subjects with asthma. Katz, RM; Perhach, JL; Rachelefsky, GS; Rohr, AS; Siegel, SC; Spector, SL, 1987)	0.98
" In the isolated guinea pig ileum, the dose-response curve for histamine was shifted to the right by 10(-8) mol/l of diphenhydramine, clemastine or azelastine to the same degree."	( Effects of azelastine hydrochloride, a new antiallergic drug, on the gastrointestinal tract. Igarashi, T; Murakami, M; Shoji, T; Yamanaka, T, 1981)	0.85
"The tolerability and pharmacokinetics of azelastine hydrochloride (CAS 73907-93-0, A-05610) after single and multiple dosing (4."	( Tolerability and pharmacokinetics of single and multiple doses of azelastine hydrochloride in elderly volunteers. Borbe, HO; Büker, KM; Peter, G; Riethmüller-Winzen, H; Romeis, P, 1995)	0.79
"Azelastine nasal spray demonstrated broad clinical antirhinitis activity that for the 2 sprays/nostril bid dosage regimen was consistently clinically and statistically significant."	( Safety and efficacy of azelastine nasal spray (Astelin NS) for seasonal allergic rhinitis: a 4-week comparative multicenter trial. Chu, TJ; D'Eletto, TA; Dockhorn, RJ; Freitag, JJ; Kraemer, MJ; LaForce, C; Prenner, BM; Widlitz, MD, 1996)	2.05
" Results showed that both antihistamines, applied topically of dosed orally, reduced sneezing even when significant increases of histamine concentration in nasal secretions were evidenced immediately after NAC."	( The activity of recent anti-allergic drugs in the treatment of seasonal allergic rhinitis. Clement, P; De Waele, M; Smitz, J; Wang, D, 1996)	0.29
"Thirty patients, sensitized to grass or Parietaria pollen, were allocated to three treatment groups: those receiving the standard dosage (0."	( Seasonal rhinitis and azelastine: long- or short-term treatment? Bagnasco, M; Bertolini, C; Canonica, GW; Ciprandi, G; Fiorino, N; Passalacqua, G; Ricca, V; Riccio, AM; Truffelli, T, 1997)	0.61
" After the treatment with azelastine, capsaicin-induced cough decreased significantly, and the dose-response curve to capsaicin was shifted to a higher concentration in comparison with the the controls."	( Mechanism of the antitussive effect of azelastine in guinea pigs. Ito, N; Miura, M; Sano, M; Sasaki, M; Shioya, T; Watanabe, A, 2002)	0.88
" A small effect on growth has been reported in one study in children receiving a standard dosage over 1 year, however."	( Safety and tolerability profiles of intranasal antihistamines and intranasal corticosteroids in the treatment of allergic rhinitis. Howarth, PH; Salib, RJ, 2003)	0.32
"The objective of the present study was to compare the efficacy and tolerability of azelastine nasal spray administered at the recommended dosage of 2 sprays per nostril twice daily with those of cetirizine in the treatment of moderate to severe SAR."	( Effectiveness of azelastine nasal spray compared with oral cetirizine in patients with seasonal allergic rhinitis. Berger, W; Bernstein, J; Corren, J; Nayak, A; Sacks, H; Storms, W, 2005)	0.89
" Newer topical medications are being used that have multiple actions, such as an antihistaminic effect coupled with mast-cell stabilisation, and which require reduced daily dosing due to their longer duration of action."	( Pharmacotherapy of allergic eye disease. Flynn, TH; Larkin, F; Manzouri, B; Ono, SJ; Wyse, R, 2006)	0.33
" Bitter taste is the most common side effect associated with azelastine nasal spray and this problem can be mitigated by the dosing technique recommended by the manufacturer in the product labeling."	( Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability. Bernstein, JA, 2007)	2.02
"15% may be effective with once-daily dosing without increasing the incidence of adverse events."	( Efficacy and safety of azelastine 0.15% nasal spray administered once daily in subjects with seasonal allergic rhinitis. Amar, NJ; Howland, WC; Sacks, H; van Bavel, J; Wheeler, W, )	0.44
" The primary objectives of this clinical trial were (1) to determine if a reformulated azelastine nasal spray (Astepro) with sucralose as a taste-masking agent provides comparable efficacy to the original formulation (Astelin) and (2) to evaluate dose-response relationships between groups."	( Double-blind, placebo-controlled trial of reformulated azelastine nasal spray in patients with seasonal allergic rhinitis. Bernstein, JA; Ferguson, BJ; Portnoy, J; Prenner, B; Sacks, HJ; Wheeler, WJ, )	0.6
" The percentage changes from baseline in the TNSS in the 2-sprays/nostril dosage groups were 27."	( Double-blind, placebo-controlled trial of reformulated azelastine nasal spray in patients with seasonal allergic rhinitis. Bernstein, JA; Ferguson, BJ; Portnoy, J; Prenner, B; Sacks, HJ; Wheeler, WJ, )	0.38
"The results of this study showed efficacy both with original azelastine nasal spray and with the reformulated nasal spray and a clear dose-response difference between the 1- and 2-spray dosages."	( Double-blind, placebo-controlled trial of reformulated azelastine nasal spray in patients with seasonal allergic rhinitis. Bernstein, JA; Ferguson, BJ; Portnoy, J; Prenner, B; Sacks, HJ; Wheeler, WJ, )	0.62
"10% nasal spray at a dosage of 2 sprays/nostril twice daily in patients with moderate-to-severe seasonal allergic rhinitis (SAR)."	( Efficacy and safety of azelastine 0.15% nasal spray and azelastine 0.10% nasal spray in patients with seasonal allergic rhinitis. Berger, W; La Force, C; Lumry, W; Sacks, H; Shah, S; Wheeler, W, )	0.44
" Compared with products where corticosteroid remains suspended, the new solubilized nasal spray formulation provides added benefit including faster onset of action and superior, convenient dosing of two therapeutics in one convenient product."	( Solubilized nasal steroid (CDX-947) when combined in the same solution nasal spray with an antihistamine (CDX-313) provides improved, fast-acting symptom relief in patients with allergic rhinitis. D'Angelo, P; Lee, J; Liu, J; Patel, D; Pipkin, JD; Salapatek, AM; Zimmerer, RO, )	0.13
"15% allowed for once-daily dosing without increasing the incidence of adverse effects."	( Efficacy and safety of azelastine 0.15% nasal spray administered once daily in patients with allergy to Texas mountain cedar pollen. Amar, NJ; Howland, WC; Sacks, H; Wheeler, W, )	0.44
"15% (n = 251) or placebo (n = 255), both at a dosage of 2 sprays/nostril once daily."	( Efficacy and safety of azelastine 0.15% nasal spray administered once daily in patients with allergy to Texas mountain cedar pollen. Amar, NJ; Howland, WC; Sacks, H; Wheeler, W, )	0.44
" Results demonstrate improved activity of antihistamines by 2 phytochemicals, suggesting dosing strategies for animal trials of ASX- or GB-augmented formulations for seasonal allergic rhinitis and asthma."	( In vitro suppression of lymphocyte activation in patients with seasonal allergic rhinitis and pollen-related asthma by cetirizine or azelastine in combination with ginkgolide B or astaxanthin. Abal, A; Al-Awadhi, R; Al-Sharah, S; Arifhodzic, N; Azeamouzi, C; Haines, D; Mahmoud, FF; Tosaki, A, 2012)	0.58
", approved dosing regimen in the United States), in SAR via a post hoc analysis of data from a previously published direct-comparison study."	( Comparison of intranasal azelastine to intranasal fluticasone propionate for symptom control in moderate-to-severe seasonal allergic rhinitis. Bachert, C; Canonica, GW; Carr, WW; Lieberman, P; Meltzer, E; Mullol, J; Munzel, U; Murray, R; Price, D; Ratner, P; Virchow, JC, )	0.43
"15% spray at a dosage of 2 sprays (137 micrograms/spray) twice daily for 10 days."	( Effect of intranasal azelastine on substance P release in perennial nonallergic rhinitis patients. DuBuske, L; Gawlik, R; Jawor, B; Parzynski, S; Rogala, B, )	0.45
"Fluticasone propionate (FLU) and Azelastine hydrochloride (AZE) are co-formulated with phenylethyl alcohol (PEA) and Benzalkonium chloride (BENZ) (as preservatives) in pharmaceutical dosage form for treatment of seasonal allergies."	( Simultaneous determination of Fluticasone propionate and Azelastine hydrochloride in the presence of pharmaceutical dosage form additives. El-Mosallamy, SS; El-Zeany, BA; Hassan, NY; Merey, HA, 2016)	0.96
"Two simple, sensitive, rapid, validated and cost effective spectroscopic methods were established for quantification of antihistaminic drug azelastine (AZL) in bulk powder as well as in pharmaceutical dosage forms."	( Validated spectroscopic methods for determination of anti-histaminic drug azelastine in pure form: Analytical application for quality control of its pharmaceutical preparations. El-Ashry, SM; El-Masry, AA; El-Wasseef, DR; Hammouda, MEA, 2018)	0.91

Role	Description
H1-receptor antagonist	H1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.
anti-allergic agent	A drug used to treat allergic reactions.
anti-asthmatic drug	A drug used to treat asthma.
bronchodilator agent	An agent that causes an increase in the expansion of a bronchus or bronchial tubes.
platelet aggregation inhibitor	A drug or agent which antagonizes or impairs any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system.
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor	A lipoxygenase inhibitor that interferes with the action of arachidonate 5-lipoxygenase (EC 1.13.11.34).
[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]

Class	Description
phthalazines
tertiary amino compound	A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
monochlorobenzenes	Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
[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]

Pathway	Proteins	Compounds
Azelastine H1-Antihistamine Action	8	7

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Fumarate hydratase	Homo sapiens (human)	Potency	33.1734	0.0030	8.7949	48.0869	AID1347053
EWS/FLI fusion protein	Homo sapiens (human)	Potency	3.9347	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
polyprotein	Zika virus	Potency	33.1734	0.0030	8.7949	48.0869	AID1347053
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
ATP-dependent translocase ABCB1	Homo sapiens (human)	IC50 (µMol)	23.0000	0.0002	2.3185	10.0000	AID679131; AID679132
Cytochrome P450 3A4	Homo sapiens (human)	Ki	0.0200	0.0001	1.4162	9.9000	AID1464994
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	1.0000	0.0000	2.0151	10.0000	AID591568
Cytochrome P450 2D6	Homo sapiens (human)	Ki	0.0501	0.0001	1.1986	8.0000	AID1464996
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	IC50 (µMol)	6.3096	0.0000	1.4039	10.0000	AID1464997
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	Ki	0.5012	0.0001	0.9549	10.0000	AID1464995
Alpha-1A adrenergic receptor	Homo sapiens (human)	Ki	0.0501	0.0000	0.2726	10.0000	AID1331184; AID591514; AID687268
Histamine H1 receptor	Homo sapiens (human)	Ki	0.0012	0.0000	0.5110	10.0000	AID1331182; AID591512; AID687266
Alpha-1B adrenergic receptor	Homo sapiens (human)	Ki	0.0501	0.0000	0.4713	10.0000	AID1331185; AID591515; AID687271
5-hydroxytryptamine receptor 2B	Homo sapiens (human)	Ki	0.0200	0.0003	0.7693	10.0000	AID1464994
Alpha-1A adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.0501	0.0000	0.9650	10.0000	AID1464996
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	0.1000	0.0009	1.9014	10.0000	AID1331187; AID1464938; AID591518; AID687269
Histamine H3 receptor	Homo sapiens (human)	Ki	0.1514	0.0001	0.3399	8.5110	AID1331183; AID591513; AID687267
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Histamine H1 receptor	Homo sapiens (human)	Kd	0.0002	0.0001	0.4021	5.4000	AID1331191; AID1464934; AID591516; AID687274
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
G2/M transition of mitotic cell cycle	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic metabolic process	ATP-dependent translocase ABCB1	Homo sapiens (human)
response to xenobiotic stimulus	ATP-dependent translocase ABCB1	Homo sapiens (human)
phospholipid translocation	ATP-dependent translocase ABCB1	Homo sapiens (human)
terpenoid transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
regulation of response to osmotic stress	ATP-dependent translocase ABCB1	Homo sapiens (human)
transmembrane transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
transepithelial transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
stem cell proliferation	ATP-dependent translocase ABCB1	Homo sapiens (human)
ceramide translocation	ATP-dependent translocase ABCB1	Homo sapiens (human)
export across plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
transport across blood-brain barrier	ATP-dependent translocase ABCB1	Homo sapiens (human)
positive regulation of anion channel activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
carboxylic acid transmembrane transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	ATP-dependent translocase ABCB1	Homo sapiens (human)
regulation of chloride transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
positive regulation of monoatomic ion transport	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
signal transduction	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
neuromuscular synaptic transmission	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
nervous system development	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
regulation of locomotion	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
saliva secretion	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
cognition	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
regulation of postsynaptic membrane potential	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
regulation of glial cell proliferation	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
positive regulation of intracellular protein transport	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmission	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
chemical synaptic transmission	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
behavioral fear response	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
intracellular calcium ion homeostasis	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
locomotory behavior	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
feeding behavior	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
cGMP-mediated signaling	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of nervous system process	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of appetite	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
regulation of corticotropin-releasing hormone secretion	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of fat cell differentiation	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of calcium-mediated signaling	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
release of sequestered calcium ion into cytosol	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
MAPK cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressure	Alpha-1A adrenergic receptor	Homo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressure	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrine	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrine	Alpha-1A adrenergic receptor	Homo sapiens (human)
apoptotic process	Alpha-1A adrenergic receptor	Homo sapiens (human)
smooth muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
signal transduction	Alpha-1A adrenergic receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
activation of phospholipase C activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Alpha-1A adrenergic receptor	Homo sapiens (human)
adult heart development	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Alpha-1A adrenergic receptor	Homo sapiens (human)
response to xenobiotic stimulus	Alpha-1A adrenergic receptor	Homo sapiens (human)
response to hormone	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of autophagy	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cardiac muscle hypertrophy	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Alpha-1A adrenergic receptor	Homo sapiens (human)
intracellular signal transduction	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of action potential	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of smooth muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
calcium ion transport into cytosol	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cardiac muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
cell growth involved in cardiac muscle cell development	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of protein kinase C signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
pilomotor reflex	Alpha-1A adrenergic receptor	Homo sapiens (human)
neuron-glial cell signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
inflammatory response	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
memory	Histamine H1 receptor	Homo sapiens (human)
visual learning	Histamine H1 receptor	Homo sapiens (human)
regulation of vascular permeability	Histamine H1 receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Histamine H1 receptor	Homo sapiens (human)
regulation of synaptic plasticity	Histamine H1 receptor	Homo sapiens (human)
cellular response to histamine	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H1 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
regulation of vasoconstriction	Alpha-1B adrenergic receptor	Homo sapiens (human)
intracellular signal transduction	Alpha-1B adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-1B adrenergic receptor	Homo sapiens (human)
regulation of cardiac muscle contraction	Alpha-1B adrenergic receptor	Homo sapiens (human)
neuron-glial cell signaling	Alpha-1B adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-1B adrenergic receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Alpha-1B adrenergic receptor	Homo sapiens (human)
neural crest cell migration	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cytokine production	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of endothelial cell proliferation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor internalization	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
heart morphogenesis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cardiac muscle hypertrophy	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
intracellular calcium ion homeostasis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
activation of phospholipase C activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cell population proliferation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
response to xenobiotic stimulus	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
neural crest cell differentiation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
intestine smooth muscle contraction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phosphorylation	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
calcium-mediated signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cGMP-mediated signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
vasoconstriction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
negative regulation of apoptotic process	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of MAP kinase activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
embryonic morphogenesis	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
regulation of behavior	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of nitric-oxide synthase activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
release of sequestered calcium ion into cytosol	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of cell division	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein kinase C signaling	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cellular response to temperature stimulus	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
neurotransmitter secretion	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H3 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H3 receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
protein binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATP binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
efflux transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATP hydrolysis activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ubiquitin protein ligase binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
carboxylic acid transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
phosphatidylcholine floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
phosphatidylethanolamine flippase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ceramide floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
phosphatidylinositol phospholipase C activity	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
protein binding	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
Gq/11-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
identical protein binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
alpha1-adrenergic receptor activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
protein binding	Alpha-1A adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
histamine receptor activity	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H1 receptor	Homo sapiens (human)
neurotransmitter receptor activity	Histamine H1 receptor	Homo sapiens (human)
protein binding	Alpha-1B adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Alpha-1B adrenergic receptor	Homo sapiens (human)
alpha1-adrenergic receptor activity	Alpha-1B adrenergic receptor	Homo sapiens (human)
Gq/11-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G-protein alpha-subunit binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
GTPase activator activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
histamine receptor activity	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytoplasm	ATP-dependent translocase ABCB1	Homo sapiens (human)
plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
cell surface	ATP-dependent translocase ABCB1	Homo sapiens (human)
membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
apical plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
extracellular exosome	ATP-dependent translocase ABCB1	Homo sapiens (human)
external side of apical plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
plasma membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
presynaptic membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
axon terminus	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
postsynaptic density membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
glutamatergic synapse	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
cholinergic synapse	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
synapse	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
dendrite	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
plasma membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 2C	Homo sapiens (human)
nucleus	Alpha-1A adrenergic receptor	Homo sapiens (human)
nucleoplasm	Alpha-1A adrenergic receptor	Homo sapiens (human)
cytoplasm	Alpha-1A adrenergic receptor	Homo sapiens (human)
cytosol	Alpha-1A adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
caveola	Alpha-1A adrenergic receptor	Homo sapiens (human)
nuclear membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
intracellular membrane-bounded organelle	Alpha-1A adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
cytosol	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H1 receptor	Homo sapiens (human)
synapse	Histamine H1 receptor	Homo sapiens (human)
dendrite	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H1 receptor	Homo sapiens (human)
nucleus	Alpha-1B adrenergic receptor	Homo sapiens (human)
cytoplasm	Alpha-1B adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
caveola	Alpha-1B adrenergic receptor	Homo sapiens (human)
nuclear membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
nucleoplasm	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
cytoplasm	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
G protein-coupled serotonin receptor complex	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 2B	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Histamine H3 receptor	Homo sapiens (human)
presynapse	Histamine H3 receptor	Homo sapiens (human)
plasma membrane	Histamine H3 receptor	Homo sapiens (human)
synapse	Histamine H3 receptor	Homo sapiens (human)
dendrite	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID28236	Unbound fraction (tissues)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID588219	FDA HLAED, gamma-glutamyl transferase (GGT) increase	2004	Current 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.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID26362	Ionization constant (pKa)	2004	Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5	Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID681468	TP_TRANSPORTER: increase in Doxorubicin intracellular accumulation (Doxorubicin: 17.2 uM, Azelastine: 30 uM) in C6 0.5 cells	1995	Biochemical pharmacology, Jul-17, Volume: 50, Issue:2	Azelastine and flezelastine as reversing agents of multidrug resistance: pharmacological and molecular studies.
AID591576	Antiallergic rhinitis activity in conscious guinea pig assessed as duration of inhibition of histamine-induced nasal congestion at 1 mg/ml administered intranasally	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588217	FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase	2004	Current 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.
AID1331186	Lipophilicity, logD of compound at pH 7.4	2016	Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24	The discovery of quinoline based single-ligand human H
AID588214	FDA HLAED, liver enzyme composite activity	2004	Current 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.
AID1464995	Displacement of [3H]mesulergine from recombinant human 5-ht2C expressed in CHO cells	2017	Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21	Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
AID679131	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cells	2001	European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Feb, Volume: 12, Issue:4	Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport.
AID591532	Volume of distribution at steady state in Beagle dog at 2 mg/kg, po and 1 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID588215	FDA HLAED, alkaline phosphatase increase	2004	Current 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.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588218	FDA HLAED, lactate dehydrogenase (LDH) increase	2004	Current 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.
AID1220556	Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID22246	Pharmacokinetic parameter :volume apparent of distribution was reported	1998	Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6	Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID687274	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	2012	Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20	Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
AID591562	Oral bioavailability in CD rat at 3 mg/kg	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID781328	pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 2005	2014	Pharmaceutical research, Apr, Volume: 31, Issue:4	Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID547621	Cytotoxicity against BESM cells after 88 hrs by HTS assay	2010	Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8	Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID177340	Inhibition of cutaneous histamine reaction in rats.	1995	Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4	Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application i
AID687271	Antagonist activity at human adrenergic alpha1B receptor expressed in rat fibroblasts by by plate-based calcium imaging	2012	Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20	Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
AID540211	Fraction unbound in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID591567	Ratio of drug level in brain to blood in CD rat at 1 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID591533	Half life in CD rat at 3 mg/kg, po and 1 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID1464938	Displacement of [3H]-Dofetilide from recombinant human ERG expressed in CHOK1 cell membranes incubated for 4 hrs under dark condition by luminescence assay	2017	Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21	Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
AID591535	Half life in Beagle dog at 2 mg/kg, po and 1 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID591527	Clearance in CD rat at 3 mg/kg, po and 1 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29423	HPLC capacity factor (k')	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID7783	Unbound fraction (plasma)	2004	Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5	Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588216	FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase	2004	Current 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.
AID1896159	Antiviral activity against HBV infected HepG2 2.2.15 cells assessed as reduction in HBsAg level and measured after 9 days by ELISA	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
AID1464985	Antiallergic activity in ovalbumin-sensitized guinea pig model of histamine-induced allergic rhinitis assessed as reduction in congestion by measuring enhanced pause at 1 mg/ml administered intranasally pretreated for 3 hrs followed by histamine challenge	2017	Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21	Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
AID591530	Volume of distribution at steady state in CD rat at 3 mg/kg, po and 1 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID165615	Test against PAF-induced aggregation of rabbit platelets in vitro	1995	Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4	Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application i
AID687266	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	2012	Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20	Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
AID687267	Antagonist activity at human H3 receptor expressed in CHO cells assessed as inhibition of histamine-induced GTPgamma[S] binding by scintillation proximity assay	2012	Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20	Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
AID591514	Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID591518	Displacement of labeled dofetilide human ERG	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID540210	Clearance in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID591512	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID1207611	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	2012	Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10	Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1220555	Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID28235	Unbound fraction (plasma)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID591516	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID547622	Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay	2010	Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8	Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID24562	Pharmacokinetic parameter :half life in humans was reported	1998	Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6	Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID680873	TP_TRANSPORTER: increase in Doxorubicin intracellular accumulation (Doxorubicin: 17.2 uM, Azelastine: 10 uM) in C6 1V cells	1995	Biochemical pharmacology, Jul-17, Volume: 50, Issue:2	Azelastine and flezelastine as reversing agents of multidrug resistance: pharmacological and molecular studies.
AID1331191	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	2016	Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24	The discovery of quinoline based single-ligand human H
AID1220560	Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID250135	Inhibition of compound against MES-SA/DX5 cell line was determined using P-glycoprotein assay	2005	Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8	A pharmacophore hypothesis for P-glycoprotein substrate recognition using GRIND-based 3D-QSAR.
AID1464997	Displacement of [3H]AF-DX 384 from recombinant human M1 receptor expressed in CHO cells	2017	Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21	Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
AID78852	Ability to inhibit histamine-induced contractions of isolated guinea pig ileum	1995	Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4	Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application i
AID540212	Mean residence time in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID679132	TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells	2001	European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Feb, Volume: 12, Issue:4	Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport.
AID1464996	Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor	2017	Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21	Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
AID1464934	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye ba	2017	Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21	Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
AID1896160	Antiviral activity against HBV infected HepG2 2.2.15 cells assessed as reduction in HBeAg level and measured after 9 days by ELISA	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
AID28233	Fraction ionized (pH 7.4)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID547804	Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells	2010	Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8	Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1678478	Inhibition of recombinant His6-tagged SARS-CoV-2 main protease assessed as residual enzyme activity at 100 uM using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay relative to con	2020	ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12	Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2.
AID1464994	Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells	2017	Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21	Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
AID1220559	Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID591513	Antagonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as inhibition of histamine-induced GTP-gammaS binding	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID591529	Clearance in Beagle dog at 2 mg/kg, po and 1 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID29925	Volume of distribution in man (IV dose)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540209	Volume of distribution at steady state in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1464986	Antiallergic activity in ovalbumin-sensitized guinea pig model of histamine-induced allergic rhinitis assessed as reduction in congestion by measuring enhanced pause at 1 mg/ml administered intranasally pretreated for 24 hrs followed by histamine challeng	2017	Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21	Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID178093	Antiallergic activity in the rat PCA assay following oral administration 1 hour before antigen challenge. Five animals were used in this experiment.	1995	Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4	Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application i
AID687270	Lipophilicity, log D of compound at pH 7.4	2012	Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20	Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
AID1331185	Antagonist activity at adrenergic alpha1B receptor (unknown origin) expressed in Rat1 cells assessed as inhibition of phenylephrine-induced Ca2+ flux preincubated for 30 mins followed by phenylephrine addition by Fluo-4-AM-dye based FLIPR assay	2016	Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24	The discovery of quinoline based single-ligand human H
AID1220557	Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID591568	Inhibition of CYP2D6	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID591515	Binding affinity to human adrenergic Alpha-1B receptor expressed in rat intact fibroblasts	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID1220558	Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID1331183	Antagonist activity at human Histamine H3 receptor expressed in CHO cell membranes assessed as inhibition of histamine-induced [35S]GTPgammaS binding after 2 to 6 hrs by scintillation proximity assay	2016	Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24	The discovery of quinoline based single-ligand human H
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1331182	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	2016	Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24	The discovery of quinoline based single-ligand human H
AID1220554	Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID591564	Oral bioavailability in Beagle dog at 2 mg/kg	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID1331184	Antagonist activity at adrenergic alpha1A receptor (unknown origin) expressed in Rat1 cells assessed as inhibition of phenylephrine-induced Ca2+ flux preincubated for 30 mins followed by phenylephrine addition by Fluo-4-AM-dye based FLIPR assay	2016	Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24	The discovery of quinoline based single-ligand human H
AID29337	Ionisation constant (pKa)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID687268	Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging	2012	Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20	Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
AID8002	Observed volume of distribution	2004	Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5	Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1678479	Inhibition of recombinant His6-tagged SARS-CoV-2 main protease using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay	2020	ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12	Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2.
AID591517	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM incubated for 30 mins measured after washout followed by repeat histamine chal	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID687269	Displacement of [3H]dofetilide from human ERG	2012	Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20	Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
AID591566	Bioavailability in intranasally dosed human	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID540213	Half life in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1331187	Displacement of [3H]-dofetilide from human ERG expressed in CHOK1 cell membranes incubated for 4 hrs in dark by luminescent assay	2016	Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24	The discovery of quinoline based single-ligand human H
AID591536	Liver blood flow in CD rat at 3 mg/kg, po and 1 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
AID425653	Renal clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508627	Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347125	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347124	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347116	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508629	Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508628	Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347121	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal 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.
AID1346037	Human H1 receptor (Histamine receptors)	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	80 (15.78)	18.7374
1990's	213 (42.01)	18.2507
2000's	95 (18.74)	29.6817
2010's	86 (16.96)	24.3611
2020's	33 (6.51)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	160 (28.37%)	5.53%
Reviews	48 (8.51%)	6.00%
Case Studies	5 (0.89%)	4.05%
Observational	2 (0.35%)	0.25%
Other	349 (61.88%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (52)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Randomized Multicenter Phase III Efficacy and Safety Study of AI201901 in Allergic Rhinitis Patients (HILARIA) [NCT04729517]	Phase 3	210 participants (Actual)	Interventional	2021-04-20	Completed
Clinical Trial to Assess Onset of Action of Azelastine Hydrochloride and Fluticasone Propionate Nasal Spray Delivered in a Single Spray (MP-AzeFlu) in the Treatment of Allergen-Induced Allergic Rhinitis Symptoms in Comparison to Placebo and Free Combinati [NCT03004131]	Phase 4	82 participants (Actual)	Interventional	2017-01-07	Completed
Single Dose Pharmacokinetics of Intranasal Fluticasone Delivered by a Fixed Combination With Azelastine (MP29 02) in Comparison to Two Different Fluticasone Nasal Sprays Single-centre, Randomised, Open-label, Three-period, Six-sequence Cross-over Trial (W [NCT01194622]	Phase 1	30 participants (Actual)	Interventional	2010-08-31	Completed
Randomized, Double-Blind, Placebo-Controlled Trial of the Safety and Efficacy of MP03-36 in Patients With Seasonal Allergic Rhinitis [NCT01368445]	Phase 3	617 participants (Actual)	Interventional	2006-08-31	Completed
Clinical Trial to Assess Onset of Action of Azelastine Hydrochloride and Fluticasone Propionate Nasal Spray Delivered in a Single Spray (Dymista) in the Treatment of Allergen-Induced Allergic Rhinitis Symptoms in Comparison to Placebo in an Environmental [NCT04652245]	Phase 4	216 participants (Actual)	Interventional	2020-12-14	Completed
Single Dose Pharmacokinetics of Intranasal Azelastine Delivered by a Fixed Combination With Fluticasone in Comparison to Azelastine Nasal Sprays Single-centre, Randomised, Open-label, Three-period, Six-sequence Cross-over Trial (William's Design) [NCT01190852]	Phase 1	30 participants (Actual)	Interventional	2010-08-31	Completed
[NCT01382654]	Phase 2	131 participants (Actual)	Interventional	2006-09-30	Completed
An Open-label, Single-Dose, Three-way Crossover Study to Compare the Pharmacokinetics of Fixed-Dose Combination of Mometasone + Azelastine Nasal Spray to Mometasone and Azelastine Nasal Sprays in Adolescents (12 to 17 Years of Age) and Young Adults (18 to [NCT05887843]	Phase 1	38 participants (Actual)	Interventional	2023-06-08	Terminated(stopped due to Business decision (no safety concerns).)
A Randomised, Double Blind, 2-way Crossover Trial of 8 Days Repeat Dosing With Intranasal GSK256066 and Azelastine Hydrochloride in the Vienna Challenge Chamber in Subjects With Seasonal Allergic Rhinitis (SAR) [NCT00612118]	Phase 2	70 participants (Actual)	Interventional	2008-02-29	Completed
Active Controlled Trial of the Safety and Tolerability of MP 03-036 (Astepro 0.15%) in Patients With Perennial Allergic Rhinitis [NCT00720382]	Phase 3	703 participants (Actual)	Interventional	2007-03-31	Completed
Randomized, Double-Blind, Placebo-Controlled Trial of the Safety and Efficacy of MP03-36 in Subjects With Seasonal Allergic Rhinitis [NCT00660829]	Phase 3	536 participants (Actual)	Interventional	2007-12-31	Completed
AZE/FLU Nasal Spray on Symptom Control, Nasal Mediators and Nasal Hyperresponsiveness in Allergic Rhinitis (AR) [NCT02238353]	Phase 4	45 participants (Anticipated)	Interventional	2014-10-31	Recruiting
Randomized, Double-blind, Cross-over Clinical Trial to Assess Onset of Action and Efficacy of Azelastine Hydrochloride 0.15% Nasal Spray in the Treatment of Allergen-Induced Allergic Rhinitis Symptoms in an Environmental Exposure Unit in Comparison to Pla [NCT06126952]	Phase 2	84 participants (Anticipated)	Interventional	2023-10-30	Recruiting
Randomized Controlled Trial Evaluating Combination Rupatadine and Fluticasone Propionate Compared to Azelastine Hydrochloride and Fluticasone Propionate in Treating Allergic Rhinitis [NCT04601324]	Phase 4	0 participants (Actual)	Interventional	2020-12-15	Withdrawn(stopped due to PI did not pursue this study)
Prospective, Multicenter, Open-label, Randomized, Parallel, Clinical Study for Assessment of Comparative Efficacy and Safety of Azelastine +Mometasone , Nasal Spray, 140 mcg + 50 mcg, (Sandoz d.d., Slovenia) and Momat Rino Advance, Nasal Spray, 140 mcg + [NCT05590598]	Phase 3	472 participants (Actual)	Interventional	2023-02-13	Completed
An Open Label, Randomized, Three-treatment, Three-period, Crossover, Single Dose Study, to Investigate Drug-drug Interaction and Relative Bioavailability Between the Fixed Dose Combination Azelastine Hydrochloride / Beclomethasone Dipropionate (140/100 μg [NCT04817800]	Phase 1/Phase 2	48 participants (Actual)	Interventional	2021-03-25	Completed
Active-Controlled Trial of the Safety and Tolerability of a MP03-33 in Patients With Chronic Allergic or Nonallergic Rhinitis [NCT00783432]	Phase 3	862 participants (Actual)	Interventional	2006-07-31	Completed
Randomized, Double Blind, Placebo-Controlled Trial of the Safety and Efficacy of MP03-036 in Patients With Seasonal Allergic Rhinitis [NCT00719862]	Phase 3	481 participants (Actual)	Interventional	2007-08-31	Completed
Randomized, Double-Blind Trial of MP29-02 Nasal Spray Compared to Placebo, Azelastine Hydrochloride Nasal Spray, and Fluticasone Propionate Nasal Spray in the Treatment of Patients With Seasonal Allergic Rhinitis. [NCT00740792]	Phase 3	776 participants (Actual)	Interventional	2008-08-31	Completed
Randomized, Double-Blind Trial of MP29-02 Nasal Spray Compared to Placebo, Azelastine Hydrochloride Nasal Spray, and Fluticasone Propionate Nasal Spray in the Treatment of Patients With Seasonal Allergic Rhinitis [NCT00651118]	Phase 3	832 participants (Actual)	Interventional	2008-03-31	Completed
Randomized, Double-Blind, Placebo-Controlled Trial of the Safety and Efficacy of MP03-36 and MP03-33 Compared to Placebo in Patients With Seasonal Allergic Rhinitis [NCT00720278]	Phase 3	526 participants (Actual)	Interventional	2007-08-31	Completed
"Real Life Proof-of-Concept Study to Assess the Effect of Methylcellulose as add-on Seal to the In-season Pharmacologic Rescue Treatment in Subjects With Allergic Rhinitis" [NCT02557269]	Phase 4	60 participants (Actual)	Interventional	2015-05-31	Active, not recruiting
Randomized, Double-Blind, Placebo-Controlled Trial of the Safety and Efficacy of MP03-36 and MP03-33 in Patients With Perennial Allergic Rhinitis [NCT00712920]	Phase 3	581 participants (Actual)	Interventional	2007-01-31	Completed
A Randomized, Double-Blind, Placebo-Controlled, 3-Way Cross-Over Study Comparing Relative Efficacy of CE Budesonide+Azelastine & Rhinocort Aqua+Astelin Nasal Sprays Against Placebo in the Treatment of AR in an EEC Model [NCT00940953]	Phase 2	108 participants (Actual)	Interventional	2008-02-29	Completed
Randomized, Double-Blind, Placebo-Controlled Trial of the Safety and Efficacy of MP03-36 (0.15% Solution) and MP03-33 (0.10% Solution) in Children Ages >6 to <12 With Perennial Allergic Rhinitis [NCT01018862]	Phase 3	489 participants (Actual)	Interventional	2009-11-30	Completed
A Proof of Concept Study to Evaluate Comparative Efficacy of an Azelastine/Fluticasone Combination Nasal Spray vs. Twice the Dose of Fluticasone in Persistent Allergic Rhinitis [NCT00845598]	Phase 4	0 participants (Actual)	Interventional	2010-08-31	Withdrawn(stopped due to Could not get IMP)
A Multicenter, Randomized, Double-blind, Placebo and Active Controlled Parallel-group Trial to Assess the Efficacy and Safety of the Fixed Combination Medicinal Product Mometasone Furoate + Azelastine Hydrochloride Nasal Spray (50 + 140 mcg) in the Treatm [NCT05311475]	Phase 3	669 participants (Actual)	Interventional	2022-04-04	Completed
Efficacy of Azelastine and Mometasone Irrigation in Comparison to Nasal Sprays in Patients With Chronic Rhinitis [NCT05626621]	Phase 4	81 participants (Anticipated)	Interventional	2022-11-23	Recruiting
Investigation of the Efficacy and Safety of Concomitant Administration of Ciclesonide Nasal Spray and Azelastine Nasal Spray in Patients (18 Years or Older) With Perennial Allergic Rhinitis (PAR) Not Adequately Controlled on an Intranasal Corticosteroid o [NCT00806754]	Phase 4	340 participants (Actual)	Interventional	2006-11-30	Completed
Randomized, Double-Blind, Placebo-Controlled Trial of the Safety and Efficacy of MP03-36 in Subjects With Seasonal Allergic Rhinitis [NCT00824473]	Phase 3	506 participants (Actual)	Interventional	2008-12-31	Completed
A Four-Way Double-Blind, Randomized, Placebo Controlled Study to Determine the Efficacy and Speed of Azelastine Nasal Spray and Antihistaminic Agents in Adult Subjects With Allergen Induced Seasonal Allergic Rhinitis [NCT00561717]	Phase 4	70 participants (Actual)	Interventional	2007-10-31	Completed
Single Dose Bioequivalence Study of Azelastine Hydrochloride/Fluticasone Propionate 137microgram/50 Microgram Nasal Spray and DYMISTA Nasal Spray in Healthy Adult Human Subjects [NCT06180083]	Phase 1	56 participants (Actual)	Interventional	2023-03-24	Completed
A Randomized, Open-labeled, Multicenter Clinical Trial to Compare the Efficacy and Safety of On-demand and Continuous Administration of Nasal Spray in the Treatment of Moderate-to-severe Persistent Allergic Rhinitis [NCT05080322]	Phase 4	150 participants (Anticipated)	Interventional	2023-02-10	Recruiting
Proof of Concept Study to Assess Downstream Effects of Using Combined Intranasal Fluticasone Propionate Plus Azelastine Nasal Spray on Asthmatic Inflammation in Patients With Persistent Asthma and Allergic Rhinitis [NCT02953106]	Phase 4	7 participants (Actual)	Interventional	2017-01-20	Terminated(stopped due to The company providing study IMP was unable to supply further batches of IMP.)
A Multicenter, Randomized, Double-blind Phase Ⅲ Study of Mometasone Furoate/Azelastine Hydrochloride Combination Group and Mometasone Furoate and Azelastine Hydrochloride Group 4 Weeks After Treatment, Each Treatment Group Comparisons for Evaluation of Ef [NCT01470053]	Phase 3	347 participants (Actual)	Interventional	2011-03-31	Completed
[NCT00979615]	Phase 4	129 participants (Actual)	Interventional	2009-09-30	Completed
An Open-label, Randomized, Parallel-Group, Multi-Site Study to Evaluate the Efficacy and Safety of Azelastine HCl-Fluticasone Propionate Nasal Spray 137-50 mcg/Spray in Perennial Allergic Rhinitis Patients [NCT06051786]	Phase 2	136 participants (Actual)	Interventional	2020-08-20	Completed
Nasal Ocular Reflexes Contribute to Eye Symptoms in Patients With Allergic Rhinitis [NCT00117832]		20 participants	Interventional	2005-03-31	Completed
Randomized, Double-Blind Trial of MP29-02 Nasal Spray Compared to Placebo, Astelin Nasal Spray, and Fluticasone Propionate Nasal Spray in the Treatment of Patients With Seasonal Allergic Rhinitis [NCT00660517]	Phase 3	607 participants (Actual)	Interventional	2007-12-31	Completed
[NCT00845195]	Phase 4	150 participants (Actual)	Interventional	2009-03-31	Completed
Comparison of Montelukast and Azelastine in Treatment of Moderate to Severe Allergic Rhinitis [NCT04561687]		66 participants (Anticipated)	Interventional	2020-01-16	Recruiting
A Randomized, Double-blind, Placebo-controlled,Parallel-group Study Comparing the Bioequivalence of Azelastine Hydrochloride and Fluticasone Propionate Nasal Spray (Apotex, Inc.) to That of Dymista™ Nasal Spray (Meda Pharmaceuticals, Inc. )in the Treatmen [NCT02279563]	Phase 2	595 participants (Actual)	Interventional	2013-12-31	Enrolling by invitation
A Randomized, Double-Blind, Placebo Controlled, Crossover Study to Evaluate the Onset of Efficacy of Azelastine Hydrochloride 0.15% Nasal Spray in Allergic Rhinitis Sufferers Following Pollen Exposure in an Environmental Exposure Chamber [NCT04264637]	Phase 3	110 participants (Actual)	Interventional	2020-02-03	Completed
A Double-Blind, Randomized, Placebo-Controlled, Parallel-Group, Multi-Site Study to Evaluate the Therapeutic Equivalence of Azelastine Hydrochloride and Fluticasone Propionate, 137/50 mcg Nasal Spray, to Dymista™ Nasal Spray [NCT02249663]	Phase 3	1,535 participants (Anticipated)	Interventional	2014-08-31	Recruiting
Randomized, Double-Blind Trial of the Safety and Efficacy of Dymista Nasal Spray Compared to Placebo Nasal Spray in the Treatment of Children Ages >4 Years to <12 Years With Seasonal Allergic Rhinitis [NCT01915823]	Phase 3	348 participants (Actual)	Interventional	2013-07-31	Completed
Randomized Trial of the Safety of Astepro 0.15% Nasal Spray and Astepro 0.1% Nasal Spray in Children Ages >6 Months to <6 Years With Allergic Rhinitis [NCT01880840]	Phase 4	191 participants (Actual)	Interventional	2013-06-30	Completed
Evaluating Factors Involved in Dymista's Superior Clinical Efficacy to Fluticasone Propionate in the Treatment of Seasonal Allergic Rhinitis [NCT02402465]	Phase 4	20 participants (Anticipated)	Interventional	2015-02-28	Recruiting
Multicentre, Randomized, Double-blind, Parallel Group Phase III Study to Assess Efficacy and Safety of Dymista® Compared to Azep® and Flixonase® Nasal Sprays in the Treatment of Chinese Patients With Allergic Rhinitis/Rhinoconjunctivitis [NCT03599791]	Phase 3	900 participants (Actual)	Interventional	2018-06-29	Completed
Randomized, Double-Blind Trial of MP29-02 Nasal Spray Compared to Placebo, Azelastine Hydrochloride Nasal Spray and Fluticasone Propionate Nasal Spray in the Treatment of Patients With Seasonal Allergic Rhinitis [NCT00883168]	Phase 3	1,791 participants (Actual)	Interventional	2009-04-30	Completed
A Pilot Clinical Evaluation of Astepro® Nasal Spray for Management of Early SARS-CoV-2 Infection [NCT06008860]	Phase 4	280 participants (Anticipated)	Interventional	2023-07-01	Recruiting
[NCT00772304]	Phase 4	102 participants (Actual)	Interventional	2008-10-31	Completed
[NCT02230696]	Phase 3	951 participants (Actual)	Interventional	2014-08-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00651118 (3) [back to overview]	Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (iTNSS)
NCT00651118 (3) [back to overview]	Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (rTNSS)
NCT00651118 (3) [back to overview]	Change From Baseline in Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)at the End of 14 Days
NCT00660517 (3) [back to overview]	Change From Baseline in Adult ( Greater Than 18 Years of Age) Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)at the End of 14 Days
NCT00660517 (3) [back to overview]	Change From Baseline in 12 Hour Reflective Total Nasal Symptom Score (rTNSS)
NCT00660517 (3) [back to overview]	Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (iTNSS)
NCT00660829 (6) [back to overview]	Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (TNSS) (AM and PM Combined)at 14 Days
NCT00660829 (6) [back to overview]	Mean Change From Baseline in Instantaneous Total Nasal Symptom Score (AM) for the Entire 14-day Study Period Compared to Placebo.
NCT00660829 (6) [back to overview]	Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (AM and PM Combined) at 14 Days
NCT00660829 (6) [back to overview]	Change From Baseline in 12-hour Reflective Secondary Symptom Complex Score (SSCS) for the Entire 14-day Study Period Compared to Placebo (AM and PM Combined)
NCT00660829 (6) [back to overview]	Change From Baseline in Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)
NCT00660829 (6) [back to overview]	Change From Baseline on Direct Visual Nasal Exams at 14 Days
NCT00712920 (5) [back to overview]	Change From Baseline in Rinoconjunctivitis Quality of Life Questionnaire and 28 Days
NCT00712920 (5) [back to overview]	Change From Baseline in Instantaneous Total Nasal Symprom scoreS Compared to Placebo (AM and PM Combined)and 28 Days
NCT00712920 (5) [back to overview]	Change From Baseline in 12-hour Reflective Secondary Symptom Complex Score Compared to Placebo (AM and PM Combined)and 28 Days
NCT00712920 (5) [back to overview]	Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (AM and PM Combined) at 28 Days.
NCT00712920 (5) [back to overview]	Change From Baseline on Direct Visual Nasal Exams and 28 Days
NCT00719862 (6) [back to overview]	Change From Baseline in 12-hour Reflective SSCS for the Entire 14-day Study Period Compared to Placebo (Am and PM Combined)
NCT00719862 (6) [back to overview]	Mean Change From Baseline in Instantaneous Total Nasal Symptom Score (tNSS) (AM) for the Entire 14-day Study Period Compared to Placebo
NCT00719862 (6) [back to overview]	Change From Baseline in 12 Hour Instantaneous Total Nasal Sytmptom Score (AM and PM Combined)at 14 Days
NCT00719862 (6) [back to overview]	Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (AM and PM Combined)at 14 Days
NCT00719862 (6) [back to overview]	Change From Baseline in Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)at 14 Days
NCT00719862 (6) [back to overview]	Change From Baseline on Direct Visual Nasal Exams at 14 Days
NCT00720278 (5) [back to overview]	Change From Baseline to Day 14 in the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) Compared to Placebo in Patients 18 Years of Age and Older
NCT00720278 (5) [back to overview]	Change From Baseline in 12-hour Reflective Total Nasal Symptom Score(rTNSS)for the Entire 14-day Study Period Compared to Placebo
NCT00720278 (5) [back to overview]	Change From Baseline in Instantaneous Total Nasal Symptom Score for the Entire 14-day Study Period Compared to Placebo
NCT00720278 (5) [back to overview]	Change From Baseline in the 12-hour Reflective Secondary Symptom Complex Score for the Entire 14-day Study Period Compared to Placebo
NCT00720278 (5) [back to overview]	Change From Baseline on Direct Visual Nasal Exams
NCT00720382 (3) [back to overview]	Change From Baseline on Direct Visual Nasal Exams to 12 Months
NCT00720382 (3) [back to overview]	Change From Baseline on Direct Visual Nasal Exams to 12 Months
NCT00720382 (3) [back to overview]	Change From Baseline to 12 Months in the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) Compared to Placebo in Subjects 18 Years of Age and Older
NCT00740792 (3) [back to overview]	Change From Baseline in Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)
NCT00740792 (3) [back to overview]	Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (iTNSS)
NCT00740792 (3) [back to overview]	Change From Baseline in 12 Hour Reflective Total Nasal Symptom Score (rTNSS)
NCT00772304 (1) [back to overview]	Product Preference Questionnaire for Immediate Taste
NCT00783432 (3) [back to overview]	Number of Participants Reporting Adverse Events
NCT00783432 (3) [back to overview]	Adult Mini-Rhinoconjuctivitis Quality of Life Questionnaire. Change From Baseline in RQLQ Score at Months 1,3,6,9 and 12/or Early Termination.
NCT00783432 (3) [back to overview]	Focused Examination of the Head and Neck With Findings Recorded on a Numeric Scale.
NCT00824473 (6) [back to overview]	Mean Change From Baseline in Instantaneous Total Nasal Symptom Sscore (AM) for the Entire 14-day Study Period Compared to Placebo
NCT00824473 (6) [back to overview]	Change From Baseline in 12-hour Reflective Total Nasal Symptom Score(rTNSS)for the Entire 14-day Study Period Compared to Placebo (AM and PM Combined)at 14 Days
NCT00824473 (6) [back to overview]	Change From Baseline in 12-hour Reflective Total Ocular Symptom Score and Instantaneous Total Ocular Symptom Score for the Entire 14-day Study Period Compared to Placebo (AM and PM Combined)
NCT00824473 (6) [back to overview]	Change From Baseline in Instantaneous Total Nasal Symptom Score for the Entire 14-day Study Period Compared to Placebo (AM and PM Combined)
NCT00824473 (6) [back to overview]	Change From Baseline on Direct Visual Nasal Exams to 14 Days
NCT00824473 (6) [back to overview]	Change From Baseline to Visit 4 in the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) Compared to Placebo in Subjects 18 Years of Age and Older
NCT00845195 (4) [back to overview]	Mean Change in Instantaneous Total Ocular Symptom Scores (iTOSS) From Baseline
NCT00845195 (4) [back to overview]	Mean Change in Instantaneous Total Nasal Symptom Scores (iTNSS) From Baseline
NCT00845195 (4) [back to overview]	Mean Change in Reflective Total Nasal Symptom Score (rTNSS) From Baseline
NCT00845195 (4) [back to overview]	Mean Change in Reflective Total Ocular Symptom Scores (rTOSS) From Baseline
NCT00883168 (3) [back to overview]	Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (iTNSS)
NCT00883168 (3) [back to overview]	Change From Baseline in 12 Hour Reflective Total Nasal Symptom Score (rTNSS)
NCT00883168 (3) [back to overview]	Change From Baseline in Adult Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)
NCT00979615 (5) [back to overview]	Mean Change in Rhinorrhea Reflective Score
NCT00979615 (5) [back to overview]	Mean Change Nasal Congestion Reflective Score
NCT00979615 (5) [back to overview]	Mean Change Postnasal Drip Reflective Score
NCT00979615 (5) [back to overview]	Mean Change in Sneezing Reflective Score
NCT00979615 (5) [back to overview]	Mean Change in 2-week rTNSS From Baseline
NCT01018862 (4) [back to overview]	Change From Baseline in 12-hour Reflective Total Ocular Symptoms Score (TOSS) and Instantaneous Total Ocular Symptoms Score (TOSS) for the Entire 28-day Study Period Compared to Placebo
NCT01018862 (4) [back to overview]	Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (TNSS) for the Entire 28-day Study Period Compared to Placebo
NCT01018862 (4) [back to overview]	Change From Baseline to Visit 4 in the Pediatric Rhinoconjunctivitis Quality of Life Questionnaire (PRQLQ) Compared to Placebo
NCT01018862 (4) [back to overview]	Change From Baseline in the Instantaneous Total Nasal Symptoms Score (TNSS) for the Entire 28-day Study Period Compared to Placebo
NCT01880840 (1) [back to overview]	Safety
NCT01915823 (3) [back to overview]	Pediatric Rhinoconjunctivitis Quality of Life Questionnaire (PRQLQ)
NCT01915823 (3) [back to overview]	Primary Efficacy
NCT01915823 (3) [back to overview]	Safety
NCT02230696 (3) [back to overview]	Mean Change From Baseline in the Mean Instantaneous Total Nasal Symptom Score (iTNSS)
NCT02230696 (3) [back to overview]	Change From Baseline iTNSS Scores on Day 1 Post First Randomized Dose
NCT02230696 (3) [back to overview]	Mean Change From Baseline for Mean Reflective Total Nasal Symptom Score (rTNSS)
NCT04652245 (2) [back to overview]	Change in Patient-assessed Instantaneous Total Nasal Symptom Score (TNSS) From Baseline Compared to Placebo
NCT04652245 (2) [back to overview]	Change in Patient-assessed Instantaneous Total Ocular Symptom Score (TOSS) From Baseline Compared to Placebo

Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (iTNSS)

"change from baseline in 12-hour instantaneous ( how do you feel now) total nasal symptom score (iTNSS)consisting of nasal congestion,runny nose, itchy nose and sneezing scored twice daily (AM and PM) in diary cards for the entire 14 day study period.~The measurement scale is 0 to 24.A reduction in symptom severity score is indicated by a negative value.The more negative the value the better the result." (NCT00651118)
Timeframe: day 1 to day 14

Intervention	units on a scale (Least Squares Mean)
MP29-02	-5.2
Fluticasone Propionate	-4.5
Azelastine HCl	-4.0
Placebo	-2.6

Intervention	units on a scale (Least Squares Mean)
MP29-02	-5.6
Fluticasone Propionate	-4.7
Azelastine HCl	-4.2
Placebo	-2.9

Intervention	units on a scale (Least Squares Mean)
MP29-02	-1.6
Fluticasone Propionate	-1.6
Azelastine HCl	-1.4
Placebo	-0.9

Intervention	units on a scale (Least Squares Mean)
Azelastine HCl 548 Mcg / Fluticasone Propionate 200 Mcg	-1.6
Azelastine Hcl 548 Mcg	-1.2
Fluticasone Propionate 200 Mcg	-1.4
Placebo	-1.0

Intervention	units on a scale (Least Squares Mean)
Azelastine HCl 548 Mcg / Fluticasone Propionate 200 Mcg	-5.3
Azelastine Hcl 548 Mcg	-3.3
Fluticasone Propionate 200 Mcg	-3.8
Placebo	-2.2

Intervention	units on a scale (Least Squares Mean)
Azelastine HCl 548 Mcg / Fluticasone Propionate 200 Mcg	-4.4
Azelastine Hcl 548 Mcg	-3.0
Fluticasone Propionate 200 Mcg	-3.5
Placebo	-1.7

Intervention	Scores on a scale (Least Squares Mean)
	Baseline symptom score	Overall change from baseline
Astepro 0.15%	18.48	-3.53
Placebo	17.98	-1.97

Intervention	Scores on a scale (Least Squares Mean)
	Baseline SSCS	Change in baseline to Day 14
Astepro 0.15%	14.83	-2.81
Placebo	14.40	-1.52

Intervention	Units on a scale (Least Squares Mean)
	Baseline: Overall	Change from Baseline:Overall
Astepro 0.15%	3.81	-1.01
Placebo	3.68	-0.76

Intervention	Participants (Number)
	Epistaxis: screening - None ( n=268, 268)	Epistaxis: screening - Mild ( n=268, 268)	Epistaxis: screening - Moderate ( n=268, 268)	Epistaxis: screening - Severe ( n=268, 268)	Epistaxis: Day 14/ET -None (n=265, 266)	Epistaxis: Day 14/ET -Mild (n=265, 266)	Epistaxis: Day 14/ET -Moderate (n=265, 266)	Epistaxis: Day 14/ET -Severe (n=265, 266)	Nasal Irritation: screening - None ( n=268, 268)	Nasal Irritation: screening -Grade 1A ( n=268, 268	Nasal Irritation: screening Grade 1B ( n=268, 268)	Nasal Irritation: screening -Grade 2 ( n=268, 268)	Nasal Irritation: screening -Grade 3 ( n=268, 268)	Nasal Irritation: screening -Grade 4 ( n=268, 268)	Nasal Irritation: Day 14/ET - none (n=265, 266)	Nasal Irritation: Day 14/ET Grade 1A (n=265, 266)	Nasal Irritation: Day 14/ET Grade 1B (n=265, 266)	Nasal Irritation: Day 14/ET Grade 2 (n=265, 266)	Nasal Irritation: Day 14/ET Grade 3 (n=265, 266)	Nasal Irritation: Day 14/ET Grade 4 (n=265, 266)	Mucosal Edema: screening - none (n= 268, 268)	Mucosal Edema: screening - Mild (n= 268, 268)	Mucosal Edema: screening - Moderate (n= 268, 268)	Mucosal Edema: screening - Severe (n= 268, 268)	Mucosal Edema: Day 14/ET none (n=265, 266)	Mucosal Edema: Day 14/ET Mild (n=265, 266)	Mucosal Edema: Day 14/ET Moderate (n=265, 266)	Mucosal Edema: Day 14/ET Severe (n=265, 266)	Nasal Discharge: screening - none (n= 268, 268)	Nasal Discharge: screening - Mild (n= 268, 268)	Nasal Discharge: screening -Moderate (n= 268, 268)	Nasal Discharge: screening Severe(n= 268, 268)	Nasal Discharge: Day 14/ET none (n=265, 266)	Nasal Discharge: Day 14/ET Mild (n=265, 266)	Nasal Discharge: Day 14/ET Moderate (n=265, 266)	Nasal Discharge: Day 14/ET Severe (n=265, 266)	Mucosal Erythema: screening none (n= 268, 268)	Mucosal Erythema: screening Mild (n= 268, 268)	Mucosal Erythema: screening Moderate (n= 268, 268)	Mucosal Erythema: screening Severe (n= 268, 268)	Mucosal Erythema: Day 14/ET none (n=265, 266)	Mucosal Erythema: Day 14/ET Mild (n=265, 266)	Mucosal Erythema: Day 14/ET Moderate (n=265, 266)	Mucosal Erythema: Day 14/ET Severe (n=265, 266)	Mucosal Bleeding: screening none (n= 268, 268)	Mucosal Bleeding: screening Mild (n= 268, 268)	Mucosal Bleeding: screening Moderate (n= 268, 268)	Mucosal Bleeding: screening Severe (n= 268, 268)	Mucosal Bleeding: Day 14/ET none (n=265, 266)	Mucosal Bleeding: Day 14/ET Mild (n=265, 266)	Mucosal Bleeding: Day 14/ET Moderate(n=265, 266)	Mucosal Bleeding: Day 14/ET Severe (n=265, 266)	Crusting of Mucosa: screening none (n= 268, 268)	Crusting of Mucosa: screening Mild (n= 268, 268)	Crusting of Mucosascreening Moderate (n= 268, 268)	Crusting of Mucosa: screening Severe (n= 268, 268)	Crusting of Mucosa: Day 14/ET - none (n=265, 266)	Crusting of Mucosa: Day 14/ET - Mild (n=265, 266)	Crusting of Mucosa:Day 14/ET Moderate (n=265, 266)	Crusting of Mucosa Day 14/ET Severe( n=265, 266)
Astepro 0.15%	267	1	0	0	265	1	0	0	230	38	0	0	0	0	251	15	0	0	0	0	14	48	177	29	17	77	151	21	58	116	82	12	72	128	62	4	148	69	48	3	157	63	45	1	259	8	0	0	256	10	0	0	245	15	7	1	244	16	6	0
Placebo	267	1	0	0	264	1	0	0	232	36	0	0	0	0	248	15	2	0	0	0	18	55	162	13	6	88	152	19	63	112	79	14	79	122	64	0	145	71	50	2	153	66	45	1	257	11	0	0	257	8	0	0	237	25	6	0	245	14	6	0

Intervention	Units on a Scale (Least Squares Mean)
	Baseline: Overall	Change from Baseline:Overall
Astepro 0.1%	3.18	-1.05
Astepro 0.15%	3.29	-0.94
Placebo	2.98	-0.81

Intervention	Scores on a Scale (Least Squares Mean)
	Baseline SSCS	Change in baseline to Day 28
Astepro 0.1%	11.77	-2.23
Astepro 0.15%	12.39	-2.92
Placebo	11.20	-1.79

Intervention	Scores on a Scale (Number)
	Baseline Least Squares Mean Symptom Score	Change from baseline LS Mean symptom score
Astepro 0.1%	15.5	-3.8
Astepro 0.15%	15.8	-4.0
Placebo	14.7	-3.1

Intervention	Participants (Number)
	Epistaxis: screening - None (n=192,197,192)	Epistaxis: screening - Mild (n=192,197,192)	Epistaxis: screening - Moderate (n=192,197,192)	Epistaxis: screening - Severe (n=192,197,192)	Epistaxis: Day 28/ET - None (n=190,192,192)	Epistaxis: Day 28/ET - Mild (n=190,192,192)	Epistaxis: Day 28/ET - Moderate (n=190,192,192)	Epistaxis: Day 28/ET - Severe (n=190,192,192)	Nasal Irritation: screening - None (n=192,197,192)	Nasal Irritationscreening Grade 1A (n=192,197,192)	Nasal Irritation screening Grade1B (n=192,197,192)	Nasal Irritationscreening Grade 2 (n=192,197,192)	Nasal Irritation screening Grade 3 (n=192,197,192)	Nasal Irritation screening Grade 4 (n=192,197,192)	Nasal Irritation Day 28/ET None (n=190,192,192)	Nasal Irritation Day 28/ETGrade 1A (n=190,192,192)	Nasal Irritation Day 28/ETGrade 1B (n=190,192,192)	Nasal Irritation Day 28/ETGrade 2 (n=190,192,192)	Nasal Irritation Day 28/ETGrade 3 (n=190,192,192)	Nasal Irritation Day 28/ETGrade 4 (n=190,192,192)	Mucosal Edema: screening - None (n=192,197,192)	Mucosal Edema: screening - Mild (n=192,197,192)	Mucosal Edema: screening Moderate (n=192,197,192)	Mucosal Edema: screening - Severe (n=192,197,192)	Mucosal Edema: Day 28/ET None (n=190,192,192)	Mucosal Edema: Day 28/ET Mild (n=190,192,192)	Mucosal Edema: Day 28/ET Moderate (n=190,192,192)	Mucosal Edema: Day 28/ET Severe (n=190,192,192)	Nasal Discharge: screening - None (n=192,197,192)	Nasal Discharge: screening - Mild (n=192,197,192)	Nasal Discharge:screening Moderate (n=192,197,192)	Nasal Discharge: screening Severe (n=192,197,192)	Nasal Discharge:Day 28/ET None (n=190,192,192)	Nasal Discharge:Day 28/ET Mild (n=190,192,192)	Nasal Discharge:Day 28/ET Moderate (n=190,192,192)	Nasal Discharge:Day 28/ET Severe (n=190,192,192)	Mucosal Erythema screening None (n=192,197,192)	Mucosal Erythema screening Mild (n=192,197,192)	Mucosal Erythema screeningModerate (n=192,197,192)	Mucosal Erythema screening Severe (n=192,197,192)	Mucosal Erythema Day 28/ET None (n=190,192,192)	Mucosal Erythema Day 28/ET Mild (n=190,192,192)	Mucosal Erythema Day 28/ET Moderate (n=190,192,192	Mucosal Erythema Day 28/ET Severe (n=190,192,192)	Mucosal Bleeding: screening None (n=192,197,192)	Mucosal Bleeding: screening Mild (n=192,197,192)	Mucosal Bleedingscreening Moderate (n=192,197,192)	Mucosal Bleeding screening Severe (n=192,197,192)	Mucosal Bleeding: Day 28/ET None (n=190,192,192)	Mucosal Bleeding: Day 28/ET Mild (n=190,192,192)	Mucosal Bleeding Day 28/ETModerate (n=190,192,192)	Mucosal Bleeding: Day 28/ET Severe (n=190,192,192)	Crusting of Mucosa: screening None (n=192,197,192)	Crusting of Mucosa: screening Mild (n=192,197,192)	CrustingofMucosa screening Moderate(n=192,197,192)	Crusting of Mucosa screening Severe(n=192,197,192)	Crusting of Mucosa:Day 28/ET None (n=190,192,192)	Crusting of Mucosa:Day 28/ET Mild (n=190,192,192)	CrustingofMucosaDay 28/ET Moderate (n=190,192,192)	Crusting of Mucosa:Day 28/ET Severe(n=190,192,192)	Conjuntival screening None (n=192,197,192)	Conjuntival screening Mild (n=192,197,192)	Conjuntival screening Moderate n=(192,192, 192)	Conjuntival screeningSevere(n=192,197,192)	Conjuntival Day 28/ET None(n=190,192,192)	Conjuntival Day 28/ET Mild(n=190,192,192)	Conjuntival Day 28/ET Moderate(n=190,192)	Conjuntival Day 28/ET Severe (n=190,192, 192)	Erythmatous TM: screening None (n=192,197,192)	Erythmatous TM: screening Mild (n=192,197,192)	Erythmatous TM: screening Moderate(n=192,197,192)	Erythmatous TM:screening Severe (n=192,197,192)	Erythmatous TM: Day 28/ET None (n=190,192, 192)	Erythmatous TM: Day 28/ET Mild (n=190,192, 192)	Erythmatous TM: Day 28/ET Moderate (n=190,192,192)	Erythmatous TM: Day 28/ET Severe (n=190,192, 192)	Lymphadenopathy: screening None (n=192,197,192)	Lymphadenopathy: screening Mild (n=192,197,192)	Lymphadenopathy:screening Moderate (n=192,197,192)	Lymphadenopathy:screening Severe (n=192,197,192)	Lymphadenopathy: Day 28/ET None (n=190,192, 192)	Lymphadenopathy: Day 28/ET Mild (n=190,192, 192)	Lymphadenopathy Day 28/ET Moderate (n=190,192,192)	Lymphadenopathy: Day 28/ET Severe ( n=190,192,192)
Astepro 0.1%	194	3	0	0	189	3	0	0	183	12	2	0	0	0	178	12	1	0	0	1	30	54	84	29	44	71	60	17	51	82	51	13	76	85	24	7	108	58	28	3	124	46	20	2	192	5	0	0	189	3	0	0	178	13	6	0	178	12	2	0	145	43	9	0	145	34	10	3	183	8	6	0	189	1	2	0	189	6	2	0	190	1	1	0
Astepro 0.15%	185	7	0	0	188	4	0	0	170	21	1	0	0	0	175	16	1	0	0	0	23	50	95	24	30	71	72	19	49	83	49	11	81	72	35	4	106	54	30	2	111	51	26	4	183	9	0	0	184	7	1	0	173	13	6	0	175	16	1	0	134	48	10	0	144	36	11	1	185	5	1	1	187	3	1	1	188	3	1	0	188	3	0	1
Placebo	189	3	0	0	188	2	0	0	180	8	3	1	0	0	182	7	1	0	0	0	25	50	98	19	38	69	70	13	55	79	48	10	77	75	31	7	91	61	37	3	101	64	23	2	185	7	0	0	189	1	0	0	173	15	4	0	176	14	0	0	126	56	10	0	125	57	6	2	180	9	2	1	179	8	2	1	186	4	1	1	184	5	1	0

Intervention	Participants (Number)
	Epistaxis: screening - None (n = 242, 239)	Epistaxis: screening - Mild (n = 242, 239)	Epistaxis: screening - Moderate (n = 242, 239)	Epistaxis: screening - Severe (n = 242, 239)	Epistaxis: Day 14/ET - None (n = 241, 237)	Epistaxis: Day 14/ET - Mild (n = 241, 237)	Epistaxis: Day 14/ET - Moderate (n = 241, 237)	Epistaxis: Day 14/ET - Severe (n = 241, 237)	Irritation: screening - None (n = 242, 239)	Irritation: screening - Grade 1A (n = 242, 239)	Irritation: screening - Grade 1B (n = 242, 239)	Irritation: screening - Grade 2 (n = 242, 239)	Irritation: screening - Grade 3 (n = 242, 239)	Irritation: screening - Grade 4 (n = 242, 239)	Irritation: Day 14/ET - None (n = 241, 237)	Irritation: Day 14/ET - Grade 1A (n = 241, 237)	Irritation: Day 14/ET - Grade 1B (n = 241, 237)	Irritation: Day 14/ET - Grade 2 (n = 241, 237)	Irritation: Day 14/ET - Grade 3 (n = 241, 237)	Irritation: Day 14/ET - Grade 4 (n = 241, 237)	Mucosal Edema: screening - None (n =242, 239)	Mucosal Edema: screening - Mild (n =242, 239)	Mucosal Edema: screening - Moderate (n =242, 239)	Mucosal Edema: screening - Severe (n =242, 239)	Mucosal Edema: Day 14/ET - None (n = 241, 236)	Mucosal Edema: Day 14/ET - Mild (n = 241, 236)	Mucosal Edema: Day 14/ET - Moderate (n = 241, 236)	Mucosal Edema: Day 14/ET - Severe (n = 241, 236)	Nasal Discharge: screening - None (n= 242, 239)	Nasal Discharge: screening - Mild (n= 242, 239)	Nasal Discharge: screening - Moderate (n= 242, 239	Nasal Discharge: screening - Severe (n= 242, 239)	Nasal Discharge: Day 14/ET - None (n= 241, 237)	Nasal Discharge: Day 14/ET - Mild (n= 241, 237)	Nasal Discharge: Day 14/ET - Moderate (n= 241, 23	Nasal Discharge: Day 14/ET - Severe (n= 241, 237)	Mucosal Erythema: screening - None (n= 242, 239)	Mucosal Erythema: screening - Mild (n= 242, 239)	Mucosal Erythema: screening - Moderate (n= 242,	Mucosal Erythema: screening - Severe (n= 242, 239	Mucosal Erythema: Day 14/ET - None (n= 241, 237)	Mucosal Erythema: Day 14/ET - Mild (n= 241, 237)	Mucosal Erythema: Day 14/ET - Moderate (n= 241, 23	Mucosal Erythema: Day 14/ET - Severe (n= 241, 237)	Mucosal Bleeding: screening - None (n= 242, 239)	Mucosal Bleeding: screening - Mild (n= 242, 239)	Mucosal Bleeding: screening - Moderate (n= 242, 23	Mucosal Bleeding: screening - Severe (n= 242, 239)	Mucosal Bleeding: Day 14/ET - None (n= 241, 237)	Mucosal Bleeding: Day 14/ET - Mild (n= 241, 237)	Mucosal Bleeding: Day 14/ET - Moderate (n= 241, 23	Mucosal Bleeding: Day 14/ET - Severe (n= 241, 237)	Crusting of Mucosa: screening - None (n= 242, 239)	Crusting of Mucosa: screening - Mild (n= 242, 239)	Crusting of Mucosa:screening Moderate (n= 242,239)	Crusting of Mucosa: screening Severe (n= 242, 239)	Crusting of Mucosa: Day 14/ET - None (n= 241, 237)	Crusting of Mucosa: Day 14/ET - Mild (n= 241, 237)	Crusting of Mucosa: Day14/ETModerate (n= 241,237)	Crusting of Mucosa: Day 14/ET Severe (n= 241, 237)
Astepro 0.15%	234	5	0	0	233	4	0	0	223	16	0	0	0	0	218	17	2	0	0	0	27	67	104	41	31	102	77	26	50	106	71	12	70	121	39	7	113	73	51	2	142	58	33	4	233	6	0	0	233	4	0	0	214	23	2	0	221	12	4	0
Placebo	239	3	0	0	235	6	0	0	230	11	1	0	0	0	227	13	1	0	0	0	27	65	109	41	40	102	76	23	26	120	76	10	81	119	40	1	124	74	39	5	146	64	28	3	237	4	1	0	234	7	0	0	218	22	2	0	231	8	2	0

Intervention	Participants (Number)
	Epistaxis: screening - total	Epistaxis: screening - None	Epistaxis: screening - Mild	Epistaxis: screening - Moderate	Epistaxis: screening - Severe	Epistaxis: Day 14/ET - total	Epistaxis: Day 14/ET - None	Epistaxis: Day 14/ET - Mild	Epistaxis: Day 14/ET - Moderate	Epistaxis: Day 14/ET - Severe	Nasal Irritation: screening - total	Nasal Irritation: screening - None	Nasal Irritation: screening - Grade 1A	Nasal Irritation: screening - Grade 1B	Nasal Irritation: screening - Grade 2	Nasal Irritation: screening - Grade 3	Nasal Irritation: screening - Grade 4	Nasal Irritation: Day 14/ET - Total	Nasal Irritation: Day 14/ET - None	Nasal Irritation: Day 14/ET- Grade 1A	Nasal Irritation: Day 14/ET- Grade 1B	Nasal Irritation: Day 14/ET- Grade 2	Nasal Irritation: Day 14/ET- Grade 3	Nasal Irritation: Day 14/ET- Grade 4	Mucosal Edema: screening - Total	Mucosal Edema: screening - None	Mucosal Edema: screening - Mild	Mucosal Edema: screening - Moderate	Mucosal Edema: screening - Severe	Mucosal Edema: Day 14/ET - total	Mucosal Edema: Day 14/ET - None	Mucosal Edema: Day 14/ET - Mild	Mucosal Edema: Day 14/ET - Moderate	Mucosal Edema: Day 14/ET - Severe	Nasal Discharge: screening - Total	Nasal Discharge: screening - None	Nasal Discharge: screening - Mild	Nasal Discharge: screening - Moderate	Nasal Discharge: screening - Severe	Nasal Discharge: Day 14/ET - Total	Nasal Discharge: Day 14/ET - None	Nasal Discharge: Day 14/ET- Mild	Nasal Discharge: Day 14/ET - Moderate	Nasal Discharge: Day 14/ET - Severe	Mucosal Erythema: screening - Total	Mucosal Erythema: screening - None	Mucosal Erythema: screening - Mild	Mucosal Erythema: screening - Moderate	Mucosal Erythema: screening - Severe	Mucosal Erythema: Day 14/ET - Toal	Mucosal Erythema: Day 14/ET - None	Mucosal Erythema: Day 14/ET - Mild	Mucosal Erythema: Day 14/ET - Moderate	Mucosal Erythema: Day 14/ET - Severe	Mucosal Bleeding: screening - Toal	Mucosal Bleeding: screening - None	Mucosal Bleeding: screening - Mild	Mucosal Bleeding: screening - Moderate	Mucosal Bleeding: screening - Severe	Mucosal Bleeding: Day 14/ET - Total	Mucosal Bleeding: Day 14/ET - None	Mucosal Bleeding: Day 14/ET - Mild	Mucosal Bleeding: Day 14/ET - Moderate	Mucosal Bleeding: Day 14/ET - Severe	Crusting of Mucosa: screening - Total	Crusting of Mucosa: screening - None	Crusting of Mucosa: screening - Mild	Crusting of Mucosa: screening - Moderate	Crusting of Mucosa: screening - Severe	Crusting of Mucosa: Day 14/ET - Total	Crusting of Mucosa: Day 14/ET - None	Crusting of Mucosa: Day 14/ET - Mild	Crusting of Mucosa: Day 14/ET - Moderate	Crusting of Mucosa: Day 14/ET - Severe
Astepro 0.1%	170	169	1	0	0	169	168	1	0	0	0	170	166	4	0	0	0	169	161	8	0	0	0	0	170	3	30	106	31	169	12	60	77	20	170	26	63	67	14	169	46	71	46	6	170	74	56	37	3	167	97	49	18	5	170	167	3	0	0	169	163	6	0	0	170	142	20	7	1	169	148	19	2	0
Astepro 0.15%	178	176	2	0	0	175	166	9	0	0	0	178	169	9	0	0	0	175	165	7	3	0	0	0	178	3	28	114	33	175	15	59	81	20	178	28	67	71	12	175	47	72	45	11	178	92	45	39	2	175	105	42	27	1	178	167	2	0	0	175	163	11	0	1	178	158	18	2	0	175	155	16	3	1
Placebo	178	176	2	0	0	178	174	4	0	0	178	169	0	0	0	0	0	178	168	8	2	0	0	0	178	3	40	108	27	178	14	50	88	26	178	29	72	64	13	178	26	85	47	10	178	81	59	37	1	178	101	51	25	1	178	175	3	0	0	178	171	7	0	0	178	156	17	4	1	178	154	19	4	1

Intervention	Participants (Number)
	Epistaxis - Day 1	Epistaxis - Month 12/ET	Nasal Irritation - Day 1	Nasal Irritation - Month 12/ET	None	Grade 1A	Grade 1B	Grade 2	Grade 3	Grade 4	Conjunctival injection - Day 1	Conjunctival injection - Month 12/ET	Erythematous TM - Day 1	Erythematous TM - Month 12/ET	Mild	Lymphadenophthy-Day 1	Lymphadenopathy - Month 12/ET	Mucosal Edema - Day 1	Severe	Mucosal Edema - Month 12/ET	Nasal Discharge - Day 1	Nasal Discharge - Month 12/ET	Moderate	Mucosal Erythema - Day 1	Mucosal Erythema - Month 12/ET	Mucosal Bleeding - Day 1	Mucosal Bleeding - Month 12/ET	Crusting of Mucosa - Day 1	Crusting of Mucosa - Month 12/ET
Nasonex®	237	229	8	0	0	220	213	7	0	0	237	217	17	3	0	0	0	220	200	17	2	0	0	1	237	164	58	14	1	220	182	31	7	0	236	226	8	1	1	220	206	12	2	0	237	225	12	0	0	220	210	9	1	0	237	42	87	96	12	220	54	94	66	6	237	89	110	33	5	220	90	107	22	1	237	145	67	21	4	220	142	58	20	0	237	224	11	1	1	220	208	11	1	0	237	215	20	1	1	220	197	22	1	0

Intervention	Units on a scale (Least Squares Mean)
	Overall Score Baseline	Month 1	Month 3	Month 6	Month 9	Month 12/ET
Astepro 0.15%	2.78	-0.97	-1.15	-1.13	-1.17	-0.90
Nasonex®	2.75	-0.97	-1.27	-1.29	-1.31	-1.11

Intervention	units on a scale (Least Squares Mean)
MP29-02	-5.5
Azelastine HCL	-4.5
Fluticasone Propionate	-4.6
Placebo	-3.0

Intervention	Percentage of participants (Number)
	Preferred Azelastine Strongly	Preferred Azelastine Somewhat	Preferred Azelastine Slightly	Same	Preferred Olopatadine Slightly	Preferred Olopatadine Somewhat	Preferred Olopatadine Strongly
Olopatadine 0.6% / Azelastine 137 Mcg	26.47	10.78	5.88	15.69	8.82	8.82	23.53

Intervention	Units on a scale (Least Squares Mean)
	Baseline	Month 1	Month 3	Month 6	Month 9	Month 12/Early termination
Astelin Nasal Spray	2.18	-0.83	-1.00	-0.94	-1.16	-0.90
Astepro Nasal Spray	2.25	-0.77	-1.00	-1.04	-1.09	-0.88

azelastine

Description

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Synonyms (80)

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Overview

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Dosage Studied

Roles (6)

Drug Classes (3)

Pathways (1)

Protein Targets (15)

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Biological Processes (159)

Molecular Functions (59)

Ceullar Components (29)

Bioassays (159)

Research

Studies (507)

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Research Demand Index: 65.14

Study Types

Clinical Trials (52)

Trial Overview

Trial Outcomes

Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (iTNSS)

Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (rTNSS)

Change From Baseline in Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)at the End of 14 Days

Change From Baseline in Adult ( Greater Than 18 Years of Age) Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)at the End of 14 Days

Change From Baseline in 12 Hour Reflective Total Nasal Symptom Score (rTNSS)

Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (iTNSS)

Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (TNSS) (AM and PM Combined)at 14 Days

Mean Change From Baseline in Instantaneous Total Nasal Symptom Score (AM) for the Entire 14-day Study Period Compared to Placebo.

Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (AM and PM Combined) at 14 Days

Change From Baseline in 12-hour Reflective Secondary Symptom Complex Score (SSCS) for the Entire 14-day Study Period Compared to Placebo (AM and PM Combined)

Change From Baseline in Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)

Change From Baseline on Direct Visual Nasal Exams at 14 Days

Change From Baseline in Rinoconjunctivitis Quality of Life Questionnaire and 28 Days

Change From Baseline in Instantaneous Total Nasal Symprom scoreS Compared to Placebo (AM and PM Combined)and 28 Days

Change From Baseline in 12-hour Reflective Secondary Symptom Complex Score Compared to Placebo (AM and PM Combined)and 28 Days

Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (AM and PM Combined) at 28 Days.

Change From Baseline on Direct Visual Nasal Exams and 28 Days

Change From Baseline in 12-hour Reflective SSCS for the Entire 14-day Study Period Compared to Placebo (Am and PM Combined)

Mean Change From Baseline in Instantaneous Total Nasal Symptom Score (tNSS) (AM) for the Entire 14-day Study Period Compared to Placebo

Change From Baseline in 12 Hour Instantaneous Total Nasal Sytmptom Score (AM and PM Combined)at 14 Days

Change From Baseline in 12-hour Reflective Total Nasal Symptom Score (AM and PM Combined)at 14 Days

Change From Baseline in Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)at 14 Days

Change From Baseline on Direct Visual Nasal Exams at 14 Days

Change From Baseline to Day 14 in the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) Compared to Placebo in Patients 18 Years of Age and Older

Change From Baseline in 12-hour Reflective Total Nasal Symptom Score(rTNSS)for the Entire 14-day Study Period Compared to Placebo

Change From Baseline in Instantaneous Total Nasal Symptom Score for the Entire 14-day Study Period Compared to Placebo

Change From Baseline in the 12-hour Reflective Secondary Symptom Complex Score for the Entire 14-day Study Period Compared to Placebo

Change From Baseline on Direct Visual Nasal Exams

Change From Baseline on Direct Visual Nasal Exams to 12 Months

Change From Baseline on Direct Visual Nasal Exams to 12 Months

Change From Baseline to 12 Months in the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) Compared to Placebo in Subjects 18 Years of Age and Older

Change From Baseline in Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ)

Change From Baseline in 12 Hour Instantaneous Total Nasal Symptom Score (iTNSS)

Change From Baseline in 12 Hour Reflective Total Nasal Symptom Score (rTNSS)

Product Preference Questionnaire for Immediate Taste

Number of Participants Reporting Adverse Events

Adult Mini-Rhinoconjuctivitis Quality of Life Questionnaire. Change From Baseline in RQLQ Score at Months 1,3,6,9 and 12/or Early Termination.

Focused Examination of the Head and Neck With Findings Recorded on a Numeric Scale.

Mean Change From Baseline in Instantaneous Total Nasal Symptom Sscore (AM) for the Entire 14-day Study Period Compared to Placebo

Change From Baseline in 12-hour Reflective Total Nasal Symptom Score(rTNSS)for the Entire 14-day Study Period Compared to Placebo (AM and PM Combined)at 14 Days

Change From Baseline in 12-hour Reflective Total Ocular Symptom Score and Instantaneous Total Ocular Symptom Score for the Entire 14-day Study Period Compared to Placebo (AM and PM Combined)

Change From Baseline in Instantaneous Total Nasal Symptom Score for the Entire 14-day Study Period Compared to Placebo (AM and PM Combined)

Change From Baseline on Direct Visual Nasal Exams to 14 Days

Change From Baseline to Visit 4 in the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) Compared to Placebo in Subjects 18 Years of Age and Older

Mean Change in Instantaneous Total Ocular Symptom Scores (iTOSS) From Baseline

Mean Change in Instantaneous Total Nasal Symptom Scores (iTNSS) From Baseline

Intervention	Participants (Number)
	Conjunctiva: Total baseline	Conjunctiva: baseline-None	Conjunctiva: baseline-Mild (1+)	Conjunctiva: baseline-Moderate (2+)	Conjunctiva: baseline-Severe (3+)	Conjunctiva: Total M12/ET	Conjunctiva: M12/ET-None	Conjunctiva: M12/ET-Mild (1+)	Conjunctiva: M12/ET-Moderate (2+)	Conjunctiva:M12/ET-Severe (3+)	Tympanic membranes: Total baseline	Tympanic membranes: baseline-None	Tympanic membranes: baseline-Mild (1+)	Tympanic membranes:baselineModerate (2+)	Tympanic membranes: baseline-Severe (3+)	Tympanic membranes: Total M12/ET	Tympanic membranes: M12/ET-None	Tympanic membranes:M12/ET-Mild (1+)	Tympanic membranes: M12/ET-Moderate (2+)	Tympanic membranes:M12/ET Severe (3+)	Lymphadenopathy: Total baseline	Lymphadenopathy: baseline-None	Lymphadenopathy: baseline-Mild (1+)	Lymphadenopathy: baseline-Moderate (2+)	Lymphadenopathy: baseline-Severe (3+)	Lymphadenopathy: Total M12/ET	Lymphadenopathy: M12/ET-None	Lymphadenopathy:M12/ET-Mild (1+)	Lymphadenopathy:M12/ET-Moderate (2+)	Lymphadenopathy: M12/ET-Severe (3+)	Mucosal edema: Total baseline	Mucosal edema: baseline-None	Mucosal edema: baseline-Mild (1+)	Mucosal edema: baseline-Moderate (2+)	Mucosal edema: baseline-Severe (3+)	Mucosal edema: Total M12/ET	Mucosal edema:M12/ET-None	Mucosal edema: M12/ET-Mild (1+)	Mucosal edema: M12/ET-Moderate (2+)	Mucosal edema: M12/ET-Severe (3+)	Nasal discharge: Total baseline	Nasal discharge: baseline-None	Nasal discharge: baseline-Mild (1+)	Nasal discharge: baseline-Moderate (2+)	Nasal discharge: baseline-Severe (3+)	Nasal discharge: Total M12/ET	Nasal discharge:M12/ET-None	Nasal discharge: M12/ET-Mild (1+)	Nasal discharge: M12/ET-Moderate (2+)	Nasal discharge:M12/ET-Severe (3+)	Mucosal erythema: Total baseline	Mucosal erythema: baseline-None	Mucosal erythema: baseline-Mild (1+)	Mucosal erythema: baseline-Monderate (2+)	Mucosal erythema: baseline-Severe (3+)	Mucosal erythema: Total M12/ET	Mucosal erythema: M12/ET-None	Mucosal erythema: M12/ET-Mild (1+)	Mucosal erythema: M12/ET-Moderate (2+)	Mucosal erythema:M12/ET-Severe (3+)	Mucosal bleeding: Total baseline	Mucosal bleeding: baseline-None	Mucosal bleeding: baseline-Mild (1+)	Mucosal bleeding: baseline-Moderate (2+)	Mucosal bleeding: baseline-Severe (3+)	Mucosal bleeding: Total M12/ET	Mucosal bleeding: M12/ET-None	Mucosal bleeding: M12/ET-Mild (1+)	Mucosal bleeding: M12/ET-Moderate (2+)	Mucosal bleeding: M12/ET-Severe (3+)	Mucosal ulcerations: Total baseline	Mucosal ulcerations: baseline-None	Mucosal ulcerations: baseline-Mild (1+)	Mucosal ulcerations: baseline-Moderate (2+)	Mucosal ulcerations: baseline-Severe (3+)	Mucosal ulcerations: Total M12/ET	Mucosal ulcerations: M12/ET-None	Mucosal ulcerations: M12/ET-Mild (1+)	Mucosal ulcerations: M12/ET-Moderate (2+)	Mucosal ulcerations: M12/ET-Severe (3+)	Crusting of mucosa: Total baseline	Crusting of mucosa: baseline-None	Crusting of mucosa: baseline-Mild (1+)	Crusting of mucosa: baseline-Moderate (2+)	Crusting of mucosa: baseline-Severe (3+)	Crusting of mucosa: Total M12/ET	Crusting of mucosa: M12/ET-None	Crusting of mucosa: M12/ET-Mild (1+)	Crusting of mucosa: M12/ET-Moderate (2+)	Crusting of mucosa:M12/ET-Severe (3+)	Epistaxis: Total baseline	Epistaxis: baseline None	Epistaxis: baseline Grade 2	Epistaxis: baseline Grade 3	Epistaxis: baseline Grade 4	Epistaxis:Total M12/ET	Epistaxis: M12/ET None	Epistaxis: M12/ETGrade 2	Epistaxis:M12/ET Grade 3	Epistaxis: M12/ETGrade 4	Ulceration: Total baseline	Ulceration: baseline None	Ulceration: baseline Grade 2	Ulceration: baseline Grade 3	Ulceration: baseline Grade 4	Ulceration: Total M12/ET	Ulceration:M12/ET None	Ulceration: M12/ET Grade 2	Ulceration: M12/ET Grade 3	Ulceration: M12/ET Grade 4	Pain: Total baseline	Pain: baseline None	Pain: baseline Grade 2	Pain: baseline Grade 3	Pain: baseline Grade 4	Pain: Total M12/ET	Pain: M12/ET None	Pain: M12/ET Grade 2	Pain: M12/ET Grade 3	Pain: M12/ET Grade 4
Astelin Nasal Spray	430	254	109	54	13	417	363	43	11	0	430	344	62	17	7	417	408	5	4	0	430	393	27	7	3	417	407	10	0	0	430	30	80	200	120	417	147	182	76	12	430	44	109	183	94	417	173	183	54	7	430	82	112	178	58	417	221	153	35	8	430	376	51	2	1	417	403	10	4	0	430	362	37	25	6	417	404	10	3	0	430	311	75	35	9	417	382	32	3	0	430	416	12	1	1	417	415	2	0	0	430	373	57	0	0	417	411	6	0	0	430	382	28	17	3	417	409	6	2	0
Astepro Nasal Spray	428	264	99	53	12	414	366	44	4	0	428	342	60	21	5	414	405	8	1	0	428	389	32	7	0	414	408	6	0	0	428	32	91	191	114	414	160	176	69	9	428	40	113	179	96	414	178	188	46	2	428	80	120	171	57	414	213	152	45	4	428	362	56	10	0	414	402	11	1	0	428	348	48	26	6	414	401	11	2	0	428	293	86	36	13	414	387	24	3	0	428	402	26	0	0	414	413	1	0	0	428	365	63	0	0	413	404	8	1	0	428	377	38	6	7	413	401	10	2	0

Intervention	Scores on a scale (Least Squares Mean)
	Baseline: Reflective	Change from Baseline: Reflective	Baseline: Instantaneous	Change from Baseline: Instantaneous
Astepro 0.15%	11.52	-2.21	11.08	-2.03
Placebo	11.85	-1.28	11.33	-1.05

Intervention	Participants (Number)
	Epistaxis: screening - None (n=255, 251)	Epistaxis: screening - Mild (n=255, 251)	Epistaxis: screening - Moderate (n=255, 251)	Epistaxis: screening - Severe (n=255, 251)	Epistaxis: Day 14/ET - None (n=255, 249)	Epistaxis: Day 14/ET - Mild (n=255, 249)	Epistaxis: Day 14/ET - Moderate (n=255, 249)	Epistaxis: Day 14/ET - Severe (n=255, 249)	Nasal Irritation: screening - None (n=255, 251)	Nasal Irritation: screening -Grade 1A (n=255, 251	Nasal Irritation: screening -Grade 1B (n=255, 251)	Nasal Irritation: screening - Grade 2 (n=255, 251)	Nasal Irritation: screening - Grade 3 (n=255, 251)	Nasal Irritation: screening - Grade 4 (n=255, 251)	Nasal Irritation: Day 14/ET - None(n=255, 249)	Nasal Irritation: Day 14/ET- Grade 1A (n=255, 249)	Nasal Irritation: Day 14/ET- Grade 1B (n=255, 249)	Nasal Irritation: Day 14/ET- Grade 2 (n=255, 249)	Nasal Irritation: Day 14/ET- Grade 3 (n=255, 249)	Nasal Irritation: Day 14/ET- Grade 4 (n=255, 249)	Mucosal Edema: screening - None (n=255, 251)	Mucosal Edema: screening - Mild (n=255, 251)	Mucosal Edema: screening - Moderate (n=255, 251)	Mucosal Edema: screening - Severe (n=255, 251)	Mucosal Edema: Day 14/ET - None (n=255, 249)	Mucosal Edema: Day 14/ET - Mild (n=255, 249)	Mucosal Edema: Day 14/ET - Moderate (n=255, 249)	Mucosal Edema: Day 14/ET - Severe (n=255, 249)	Nasal Discharge: screening - None (n=255, 251)	Nasal Discharge: screening - Mild (n=255, 251)	Nasal Discharge: screening - Moderate (n=255, 251)	Nasal Discharge: screening - Severe (n=255, 251)	Nasal Discharge: Day 14/ET - None (n=255, 249)	Nasal Discharge: Day 14/ET- Mild (n=255, 249)	Nasal Discharge: Day 14/ET - Moderate (n=255, 249)	Nasal Discharge: Day 14/ET - Severe (n=255, 249)	Mucosal Erythema: screening - None (n=255, 251)	Mucosal Erythema: screening -Mild (n=255, 251)	Mucosal Erythema: screening -Moderate (n=255, 251)	Mucosal Erythema: screening -Severe (n=255, 251)	Mucosal Erythema: Day 14/ET - None (n=255, 249)	Mucosal Erythema: Day 14/ET - Mild (n=255, 249)	Mucosal Erythema: Day 14/ET Moderate (n=255, 249)	Mucosal Erythema: Day 14/ET Severe (n=255, 249)	Mucosal Bleeding: screening - None (n=255, 251)	Mucosal Bleeding: screening - Mild (n=255, 251)	Mucosal Bleeding: screening Moderate (n=255, 251)	Mucosal Bleeding: screening - Severe (n=255, 251)	Mucosal Bleeding: Day 14/ET - None (n=255, 249)	Mucosal Bleeding: Day 14/ET - Mild (n=255, 249)	Mucosal Bleeding: Day 14/ET Moderate (n=255, 249)	Mucosal Bleeding: Day 14/ET - Severe (n=255, 249)	Crusting of Mucosa: screening - None (n=255, 251)	Crusting of Mucosa: screening - Mild (n=255, 251)	Crusting of Mucosascreening Moderate (n=255,251)	Crusting of Mucosa: screening Severe (n=255, 251)	Crusting of Mucosa: Day 14/ET - None (n=255, 249)	Crusting of Mucosa: Day 14/ET - Mild (n=255, 249)	Crusting of Mucosa:Day 14/ET Moderate (n=255, 249)	Crusting of Mucosa:Day 14/ET Severe (n=255, 249)
Astepro 0.15%	249	2	0	0	246	3	0	0	231	20	0	0	0	0	228	19	2	0	0	0	19	58	129	45	24	66	123	36	33	108	89	21	45	120	67	17	139	60	49	3	145	50	36	18	247	3	1	0	243	6	0	0	229	19	3	0	240	8	1	0
Placebo	255	0	0	0	254	1	0	0	236	19	0	0	0	0	246	8	1	0	0	0	18	54	155	28	18	73	131	33	41	102	97	15	38	130	80	7	153	49	47	6	153	49	43	10	251	4	0	0	254	1	0	0	236	17	2	0	248	5	1	1

Intervention	Units on a Scale (Least Squares Mean)
	Baseline:	Change from Baseline:
Astepro 0.15%	4.33	-1.33
Placebo	4.39	-0.98

Intervention	Units on a scale (Mean)
Olopatadine HCl Nasal Spray, 0.6%	2.76
Azelastine HCl Nasal Spray, 0.1%	2.54

Intervention	Units on a scale (Mean)
Olopatadine HCl Nasal Spray, 0.6%	2.64
Azelastine HCl Nasal Spray, 0.1%	2.49

Intervention	Units on a scale (Mean)
Olopatadine HCl Nasal Spray, 0.6%	4.28
Azelastine HCl Nasal Spray, 0.1%	4.15

Intervention	Units on a scale (Mean)
Olopatadine HCl Nasal Spray, 0.6%	4.22
Azelastine HCl Nasal Spray, 0.1%	4.04

Intervention	units on a scale (Least Squares Mean)
MP29-02	-5.0
Azelastine Hcl	-4.3
Fluticasone Propionate	-4.7
Placebo	-3.1

Intervention	units on a scale (Least Squares Mean)
MP03-36 (0.15% Solution)	-1.46
MP03-33 (0.10% Solution)	-1.51
Placebo	-1.28