Page last updated: 2024-11-04

carteolol

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

Description

Carteolol is a non-selective beta-blocker used primarily to treat high blood pressure (hypertension) and glaucoma. It works by blocking the effects of adrenaline (epinephrine) on the heart and blood vessels, leading to a slower heart rate and lower blood pressure. Carteolol is also effective in reducing the pressure inside the eye, which is beneficial for treating glaucoma. The synthesis of carteolol involves several steps, starting with the reaction of 2-chloro-5-nitroaniline with formaldehyde and then proceeding through a series of reactions to form the final compound. It is studied to understand its therapeutic potential in various conditions, including heart disease and glaucoma, as well as to explore its potential for new drug development.'

Carteolol: A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2583
CHEMBL ID839
CHEBI ID3437
SCHEMBL ID24810
SCHEMBL ID23721779
MeSH IDM0003563

Synonyms (61)

Synonym
carteolol [inn:ban]
carteololum [inn-latin]
2(1h)-quinolinone, 5-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)-3,4-dihydro-
5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2(1h)-one
carteololum
CHEBI:3437 ,
bdbm50040065
BRD-A42167015-003-03-7
PRESTWICK2_000446
5-({3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl}oxy)-3,4-dihydroquinolin-2(1h)-one
BSPBIO_000492
NCGC00179541-01
carteolol (inn)
D07624
BPBIO1_000542
AB00514682
carteolol
C06874
51781-06-7
DB00521
PRESTWICK0_000446
SPBIO_002431
PRESTWICK1_000446
OPREA1_672850
PRESTWICK3_000446
CHEMBL839 ,
L000777
5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1h-quinolin-2-one
(s)-5-(3-(tert-butylamino)-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1h)-one
A828767
AKOS015918236
unii-8nf31401xg
8nf31401xg ,
5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2-ol
gtpl7142
5-(3-(tert-butylamino)-2-hydroxypropoxy)-3,4-dihydrocarbostyril
carteolol [vandf]
carteolol [jan]
carteolol [who-dd]
carteolol [inn]
carteolol [mi]
SCHEMBL24810
5-(3-(tert-butylamino)-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1h)-one
5-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl]-3,4-dihydro-2(1h)-quinolinone
5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-2(1h)-quinolinone #
LWAFSWPYPHEXKX-UHFFFAOYSA-N
2(h)-quinolinone, 5-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-3,4-dihydro-
AB00514682_06
DTXSID3022746 ,
5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydroquinolin-2-one
Q546434
BCP13007
EN300-18563029
SCHEMBL23721779
HY-17495
CS-0009237
dtxcid202746
carteololum (inn-latin)
c07aa15
carteololo
s01ed05

Research Excerpts

Overview

Carteolol is a commonly-used topical medication for primary open-angle glaucoma. It is a beta adrenoceptor antagonist used topically to reduce intraocular pressure, typically twice daily.

ExcerptReferenceRelevance
"Carteolol is a commonly-used topical medication for primary open-angle glaucoma. "( Carteolol triggers senescence via activation of β-arrestin-ERK-NOX4-ROS pathway in human corneal endothelial cells in vitro.
Fan, TJ; Jiang, GJ; You, XG, 2023
)
3.8
"Carteolol is an effective, safe topical treatment for superficial IHs. "( A prospective study of topical carteolol therapy in Chinese infants with superficial infantile hemangioma.
Gan, LQ; Ni, SL; Tan, CH; Wang, H, 2018
)
2.21
"Carteolol is a frequently used nonselective β-adrenoceptor antagonist for glaucoma and ocular hypertension treatment, and its repeated/prolonged usage might be cytotoxic to the cornea, especially the outmost human corneal epithelium (HCEP). "( Cytotoxicity of carteolol to human corneal epithelial cells by inducing apoptosis via triggering the Bcl-2 family protein-mediated mitochondrial pro-apoptotic pathway.
Fan, TJ; Shan, M, 2016
)
2.22
"Carteolol is a beta-adrenoceptor antagonist with intrinsic sympathomimetic activity. "( [Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study].
Allaire, C; Nordmann, JP; Romanet, JP; Trinquand, C, 2003
)
2.04
"Carteolol is an effective antihypertensive."( Time-dependent antihypertensive effect of carteolol--a beta-adrenoceptor antagonist with partial agonist activity.
Giles, TD; Kaneish, A; Quiroz, AC; Sander, GE, 1984
)
1.25
"Carteolol is a nonselective beta-adrenergic blocking agent with intrinsic sympathomimetic activity. "( Beta-blocking effect of single oral doses of carteolol.
Cavanaugh, JH; MacLeod, CM; Stoll, RW, 1981
)
1.97
"Carteolol is a topical beta-blocker used in ophthalmology to decrease the intraocular pressure. "( Vasorelaxing properties of carteolol in isolated porcine ciliary arteries.
Champion, C; Flammer, J; Haefliger, IO; Kasper, J, 2000
)
2.05
"Carteolol is a beta adrenoceptor antagonist used topically to reduce intraocular pressure, typically twice daily. "( Ocular hypotensive efficacy and safety of once daily carteolol alginate.
Allaire, C; Demailly, P; Trinquand, C, 2001
)
2
"Carteolol is a nonselective adrenergic blocking agent. "( Color Doppler imaging of retrobulbar hemodynamics after topical carteolol in normal tension glaucoma.
Chen, MJ; Ching, J; Chiou, HJ; Chou, K; Hsu, WM, 2001
)
1.99
"Carteolol is a nonselective beta-blocker with intrinsic sympathomimetic activity (I.S.A.). "( A long term clinical trial of carteolol in the management of glaucoma. Belgian Carteolol Study Participants.
Goethals, M; Missotten, L; Vandeputte, O; Vercruysse, K, 1992
)
2.01
"Carteolol is a relatively potent nonselective beta-adrenoceptor antagonist with partial agonist activity. "( Ocular carteolol. A review of its pharmacological properties, and therapeutic use in glaucoma and ocular hypertension.
Chrisp, P; Sorkin, EM,
)
2.03
"Carteolol is a beta-adrenergic partial agonist with higher intrinsic activity, to which the response results from interaction with low affinity sites."( Interactions of befunolol, a beta-adrenergic partial agonist, and its derivatives with high and low affinity sites in beta-adrenoceptors.
Koike, K; Takayanagi, I, 1987
)
0.99

Effects

Carteolol has little adrenergic beta-receptor stimulating effect in doses which block prominent positive chronotropic and inotropic effects of norepinephrine. Carteolol is a useful tool for clarifying whether or not presynaptic beta-adrenoceptors tonically function.

ExcerptReferenceRelevance
"Carteolol has been determined by high-performance liquid chromatography but with less satisfactory sensitivity."( Determination of the beta-blocker carteolol in human plasma by a sensitive gas chromatographic-negative-ion chemical ionization high-resolution mass spectrometric method.
Kashimoto, M; Kimura, Y; Nagasawa, M; Sugawara, M, 1995
)
1.29
"Carteolol has neither stimulative nor inhibitory effects on CYP1A2, 2C9, 2C19, 2E1, and 3A4 activities."( Metabolism of carteolol by cDNA-expressed human cytochrome P450.
Kudo, S; Odomi, M; Uchida, M, 1997
)
1.38
"Carteolol has little adrenergic beta-receptor stimulating effect in doses which block prominent positive chronotropic and inotropic effects of norepinephrine."( The inotropic and chronotropic responses of isolated canine atrium to 5-(3-tert.-butylamino-2-hydroxy)propoxy-3,4-dihydrocarbostyril hydrochloride (carteolol).
Chiba, S, 1979
)
1.18
"Carteolol has interaction with retinal beta-adrenergic receptors related to the origin of the ERG b-wave."( [Effects of carteolol on electroretinograms in isolated perfused cat eye].
Miyamura, N; Uji, Y, 1992
)
1.38
"Carteolol has the highest pA2 and is a useful tool for clarifying whether or not presynaptic beta-adrenoceptors tonically function."( A trial for kinetic evaluation of the antagonistic potency of several beta-antagonists on presynaptic beta-adrenoceptors.
Amano, H; Kubo, T; Kuwahara, M; Misu, Y, 1987
)
0.99

Actions

Carteolol reduced the increase in the arterial blood pressure under stress and lowered the raised pressure-rate product. Carteolol did not generate relaxation at concentrations up to 1 mM.

ExcerptReferenceRelevance
"Carteolol reduced the increase in the arterial blood pressure under stress and lowered the raised pressure-rate product."( [Clinical experiences in patients with coronary heart disease and angina pectoris].
Sölter, H, 1983
)
0.99
"Carteolol did not generate relaxation at concentrations up to 1 mM."( Effects of beta antagonists on mechanical properties in rabbit ciliary artery.
Hayashi, E; Hayashi-Morimoto, R; Ishikawa, H; Sato, Y; Yoshitomi, T, 1999
)
1.02
"Carteolol did not cause any significant changes in the three parameters."( Comparative study of five beta-adrenoceptor blocking agents on sinoatrial conduction time in isolated blood-perfused canine atria.
Chiba, S; Kobayashi, M; Shimotori, M, 1985
)
0.99
"Carteolol did not cause endothelium-dependent relaxations of femoral or coronary arteries."( Endothelium-dependent effects of carteolol.
Boulanger, C; Iqbal, A; Janczewski, P; Vanhoutte, PM, 1988
)
1.28

Treatment

Carteolol treatment decreased high-density lipoprotein cholesterol levels by 3.3% (-0.04 mmol/l) and raised the ratio of total to high- density lipop protein levels by 4.0%. The high carteolol dose restored SR Ca2+-ATPase and myofibrillar ATPase activities, along with creatine kinase, lactate dehydrogenase, aspartate transaminase, and ATP synthase activities.

ExcerptReferenceRelevance
"Carteolol treatment decreased high-density lipoprotein cholesterol levels by 3.3% (-0.04 mmol/l) and raised the ratio of total to high-density lipoprotein cholesterol levels by 4.0% (0.15 unit); timolol treatment decreased high-density lipoprotein cholesterol levels by 8.0% (-0.10 mmol/l) and raised the ratio of total to high-density lipoprotein cholesterol levels by 10.0% (0.37 unit)."( Effects of ocular carteolol and timolol on plasma high-density lipoprotein cholesterol level.
Freedman, NJ; Freedman, SF; Keates, EU; Lobaugh, B; Ollie, A; Samsa, GP; Shields, MB, 1993
)
1.34
"Carteolol treatment increased beta-adrenergic receptor density, and the high carteolol dose restored SR Ca2+-ATPase and myofibrillar ATPase activities, along with creatine kinase, lactate dehydrogenase, aspartate transaminase, and ATP synthase activities, to normal."( Cellular and molecular remodeling in a heart failure model treated with the beta-blocker carteolol.
Bristow, MR; DiSalvo, TG; Gwathmey, JK; Hajjar, RJ; Khan, F; Kim, CS; Matsumori, A, 1999
)
1.25
"Pretreatment with carteolol unmasked the contractile responses to NA in preparations at 17-19 days of incubation."( Developmental disappearance of excitatory alpha 1-adrenoceptor function in the oesophagus of chick embryo.
Miyazaki, H; Ohga, A; Taneike, T, 1989
)
0.6

Toxicity

Carteolol was orally administered to mice once a day at doses of 3, 30 and 150 mg/kg/day during the perinatal and lactation periods. It was evaluated on its adverse effects on pregnant animals and their offspring.

ExcerptReferenceRelevance
"Carteolol was orally administered to mice once a day at doses of 3, 30 and 150 mg/kg/day during the perinatal and lactation periods and evaluated on its adverse effects on pregnant animals and their offspring."( Reproduction study of carteolol hydrochloride in mice. Part 2. Peri -and postnatal toxicity.
Nishino, H; Numoto, T; Tamagawa, M; Tanaka, N, 1979
)
2.02
" Carteolol was shown to be safe and well tolerated by most patients."( Carteolol treatment of essential hypertension: a long-term study of safety and efficacy.
Klepper, MJ; Luther, RR; Maurath, CJ; Peckinpaugh, RO; Ringham, GL, 1986
)
2.62
" The most common side effect was transient stinging on instillation of drops, which did not differ significantly between groups."( Ocular hypotensive efficacy and safety of once daily carteolol alginate.
Allaire, C; Demailly, P; Trinquand, C, 2001
)
0.56
" Among the 17 reported adverse events, three were assessed as drug-related: one vertigo, one superficial punctate keratitis in the alginate group and one decrease in blood pressure in the standard group."( [Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study].
Allaire, C; Nordmann, JP; Romanet, JP; Trinquand, C, 2003
)
0.59
"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
" Adverse reactions and dropouts were recorded."( Short-term Efficacy and Safety of a Latanoprost/Carteolol Fixed Combination Switched From Concomitant Therapy to in Patients With Primary Open-angle Glaucoma or Ocular Hypertension.
Inoue, K; Ishida, K; Iwasa, M; Shiokawa, M; Tomita, G, 2018
)
0.74
", tafluprost/timolol (TAF/TIM) and latanoprost/carteolol (LAT/CAR), by determining their effects on intraocular pressure (IOP) in ocular normotensive monkeys and examining their toxic effects on ocular surface using human corneal epithelial cells."( Efficacy and safety of the fixed combinations of tafluprost/timolol and latanoprost/carteolol.
Akaishi, T; Fuwa, M; Kato, M; Mieda, M; Shimazaki, A; Taniguchi, T; Yamashita, N, 2019
)
1
"Case/non-case analyses were performed in the FDA Adverse Events Reporting System (FAERS) using data from 2010-2020 to examine the reporting odds ratio (ROR) signal for OPP for all classes of antiglaucoma medications under multiple conditions: (i) comparison to all other drugs in FAERs, (ii) comparison to other antiglaucoma medications, (iii) comparison to vehicle/hydrating eye drops with cases of OPP and (iv) comparison to vehicle/hydrating eyedrops with and without cases of OPP to control for topical irritant and preservative effects."( Topical ophthalmic beta-blockers are associated with ocular pseudopemphigoid: A pharmacovigilance study of antiglaucoma medications utilising the FDA adverse event reporting system.
Jedlowski, MF; Jedlowski, PM, 2022
)
0.72

Pharmacokinetics

The aim of this study was to investigate possible pharmacokinetic interactions of neuroleptic haloperidol with the beta-blocker carteolol and the anticholinergic biperiden. The authors compared the differences between ocular and nasal instillation relating to the pharmacokinetics and pharmacodynamic effects of a carteOLol-ophthalmic solution.

ExcerptReferenceRelevance
" The Cmax of carteolol (4."( Pharmacokinetics of topical beta-adrenergic antagonists in rabbit aqueous humor evaluated with the microdialysis method.
Fukuda, S; Kanda, Y; Kiuchi, Y; Koide, R; Oguchi, K; Ohtori, R; Sato, H; Ueda, T, 1998
)
0.67
" The aim of this study was to investigate possible pharmacokinetic interactions of neuroleptic haloperidol with the beta-blocker carteolol and the anticholinergic biperiden."( Pharmacokinetic and pharmacodynamic interactions among haloperidol, carteolol hydrochloride and biperiden hydrochloride.
Aoki, S; Hisazumi, H; Isawa, S; Kudo, S; Kumagai, Y; Miura, S; Murasaki, M; Uchiumi, M; Yoshioka, M, 1999
)
0.74
" The authors compared the differences between ocular and nasal instillation relating to the pharmacokinetic and pharmacodynamic effects of a carteolol-ophthalmic solution on IOP and heart rate (HR) in a randomized, double-blind, crossover, placebo-controlled design in 11 healthyyoung extensive metabolizers for CYP2D6."( Pharmacokinetic and pharmacodynamic differences between ocular and nasal instillation of carteolol on intraocular pressure and heart rate in Japanese men with high CYP2D6 activity.
Ishii, Y; Matsuki, S; Muraguchi, R; Nakagawa, M; Nakamura, K; Nakano, S; Nakatsuka, K; Uemura, N, 2002
)
0.74

Compound-Compound Interactions

ExcerptReferenceRelevance
"We prepared magnesium hydroxide (MH) nanoparticles, and investigated their effect when combined with dissolved carteolol on the bioavailability and intraocular pressure (IOP)-reducing effect of carteolol."( Enhancement in Corneal Permeability of Dissolved Carteolol by Its Combination with Magnesium Hydroxide Nanoparticles.
Fukuoka, Y; Ishii, M; Kanai, K; Nagai, N; Okamoto, N; Otake, H; Shimomura, Y; Yamaoka, S, 2018
)
0.95

Bioavailability

The increased ocular bioavailability of 1% carteolol in the presence of alginic acid led to an equivalent concentration in the target tissue although administration was only once a day.

ExcerptReferenceRelevance
"The pharmacokinetics and absolute bioavailability of a new nonselective beta-adrenoreceptor blocking agent, carteolol, were investigated after administration of single intravenous and oral doses to eight normal volunteers."( Pharmacokinetics and absolute bioavailability of carteolol, a new beta-adrenergic receptor blocking agent.
Chiba, K; Horai, Y; Ishizaki, T; Kushida, K; Ohnishi, A; Sasaki, T; Suganuma, T, 1983
)
0.73
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" The increased ocular bioavailability of 1% carteolol in the presence of alginic acid led to an equivalent concentration in the target tissue although administration was only once a day compared with twice a day for 1% carteolol alone."( A new long acting ophthalmic formulation of carteolol containing alginic acid.
Driot, JY; Maurin, F; Sébastian, C; Séchoy, O; Tissié, G; Trinquand, C, 2000
)
0.83
" During single dose studies, an increase in bioavailability ranging from 40% to 60% was observed in the aqueous humor and in the iris-ciliary body."( Alginic acid effect on carteolol ocular pharmacokinetics in the pigmented rabbit.
Driot, JY; Elena, PP; Sébastian, C; Tissié, G; Trinquand, C, 2002
)
0.63
"Environmentally responsive gel formulation for ocular controlled delivery of carteolol hydrochloride (HCl) was developed in an attempt to improve ocular bioavailability and hence decrease its systemic absorption and side effects."( Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride.
Al-Dosari, H; Al-Jenoobi, F; El-Kamel, A,
)
0.61
"Ocular bioavailability after instillation of carteolol was investigated by ion pair formation, taking into consideration a balance between lipophilicity and water solubility."( Improvement of the ocular bioavailability of carteolol by ion pair.
Higashiyama, M; Inada, K; Ohtori, A; Tajika, T, 2006
)
0.85
"We prepared magnesium hydroxide (MH) nanoparticles, and investigated their effect when combined with dissolved carteolol on the bioavailability and intraocular pressure (IOP)-reducing effect of carteolol."( Enhancement in Corneal Permeability of Dissolved Carteolol by Its Combination with Magnesium Hydroxide Nanoparticles.
Fukuoka, Y; Ishii, M; Kanai, K; Nagai, N; Okamoto, N; Otake, H; Shimomura, Y; Yamaoka, S, 2018
)
0.95

Dosage Studied

Carteolol was formulated with 1% alginic acid. During repeated dose studies, this increased ocular bioavailability of carteolol. The beta-blocking potency, estimated from the area under the dose-response curve (beta-blocking action) was also 300 times greater than that of propranolol.

ExcerptRelevanceReference
" In view of the clinical dosage levels, it is sugg ested that the antiarrhythmic effects of OPC-1085 depend predominantly on its beta blocking action."( Cardiac electrophysiologic action of carteolol hydrochloride (OPC-1085), a new beta-adrenergic blocking agent.
Ozawa, M; Toda, H; Watanabe, Y, 1978
)
0.53
" beta 1-PAA was demonstrated with carteolol by dose-related increases in resting heart rate and systolic blood pressure, and a plateau in the dose-response curve for attenuation of exercise tachycardia."( Evaluation of in vivo partial beta 1/beta 2-agonist activity: a dose-ranging study with carteolol.
Lipworth, BJ; McDevitt, DG; Wheeldon, NM, 1992
)
0.78
"In order to determine the appropriate dosage of carteolol in renal dysfunction, the pharmacokinetics of carteolol has been examined in appropriate patients."( Pharmacokinetics of carteolol in patients with impaired renal function.
Amemiya, M; Asano, Y; Furuya, H; Sakairi, Y; Tabei, K, 1992
)
0.86
" The most commonly chosen dosage levels were 20 mg of carteolol and 80 mg of nadolol."( A comparison of carteolol and nadolol in the treatment of stable angina pectoris.
Glassman, HN; Jordan, DC; Luther, RR, 1988
)
0.87
" To avoid an increase in side-effects due to drug accumulation, the dosage of carteolol should be adjusted in relation to the reduction in creatinine clearance."( Pharmacokinetics of carteolol in relation to renal function.
Hasenfuss, G; Just, H; Knauf, H; Mutschler, E; Schäfer-Korting, M, 1985
)
0.82
" Photoinactivation of beta-adrenoceptors caused a considerable parallel shift in the dose-response curve of isoprenaline."( Relationship between intrinsic activity of beta-adrenoceptor agonist and amount of spare receptors in guinea pig taenia caecum.
Koike, K; Takayanagi, I, 1983
)
0.27
" The beta-blocking potency, estimated from the area under the dose-response curve (beta-blocking action) of carteolol, was also 300 times greater than that of propranolol and correlated well with the extent of the structural changes in the heart."( Dose-related inhibitory effects of the beta-adrenoceptor blocking drugs carteolol and propranolol on cardiac hypertrophy in spontaneously hypertensive rats.
Igawa, T; Ikezono, K; Kimura, Y; Watanabe, K, 1984
)
0.71
" In a long-term study in dogs there was no evidence of cumulation except at the very high dosage of 200 mg/kg."( [Animal experimental studies on the pharmacokinetics of carteolol].
Lang, W, 1983
)
0.51
" The dose-response relation and duration of action of the beta-blocking agent 5-(3-tert-butylamino-2-hydroxy-propoxy)-3,4-dihydro-2(1H)-quinolinone hydrochloride (carteolol hydrochloride, Endak, Endak mite) were investigated by means of exercise testing under randomized, double-blind conditions in two groups of healthy probands (n = 9 and n = 9, respectively)."( [Heart rate behavior and the ischemic ST-segment under carteolol hydrochloride. Dose-response relationship and duration of effect].
Kaltenbach, M; Kober, G; Mikludy, R; Veidt, J, 1983
)
0.71
" The dosage forms were tested on intraocular hypertensive-induced rabbits."( Poly(epsilon-caprolactone) nanocapsules in carteolol ophthalmic delivery.
Hoffman, M; Maincent, P; Marchal-Heussler, L; Sirbat, D, 1993
)
0.55
" The intracerebral and serum concentrations of carteolol were determined in male rats receiving repetitive oral dosing of the compound once daily for 7 days."( Intracerebral penetration of carteolol hydrochloride in rats.
Abe, Y; Furukawa, M; Kudo, S; Odomi, M; Umehara, K, 1997
)
0.85
"5% are highly effective in lowering intraocular pressure when measured at the end of the dosing interval."( Efficacy of carteolol hydrochloride 1% vs timolol maleate 0.5% in patients with increased intraocular pressure. Nocturnal Investigation of Glaucoma Hemodynamics Trial Study Group.
Cohen, JS; Netland, PA; Nussbaum, LL; Stewart, WC; Weiss, H, 1997
)
0.68
"Phenylephrine dose-dependently contracted ciliary artery smooth muscle, and bunazosin (1 microM) shifted this dose-response curve to the right."( Effects of beta antagonists on mechanical properties in rabbit ciliary artery.
Hayashi, E; Hayashi-Morimoto, R; Ishikawa, H; Sato, Y; Yoshitomi, T, 1999
)
0.3
" In an effort to provide a once daily dosing regimen, carteolol was formulated with 1% alginic acid."( Ocular hypotensive efficacy and safety of once daily carteolol alginate.
Allaire, C; Demailly, P; Trinquand, C, 2001
)
0.81
" During repeated dose studies, this increased ocular bioavailability of carteolol in the presence of alginic acid led to an equivalent concentration in the target tissue, although the dosage was only once a day compared with twice a day for the usual carteolol eyedrops."( Alginic acid effect on carteolol ocular pharmacokinetics in the pigmented rabbit.
Driot, JY; Elena, PP; Sébastian, C; Tissié, G; Trinquand, C, 2002
)
0.86
" In an effort to provide a once-daily dosing regimen, carteolol was formulated with 1% alginic acid."( [Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study].
Allaire, C; Nordmann, JP; Romanet, JP; Trinquand, C, 2003
)
0.84
"Both topical β blockers with a once-daily dosing regimen temporarily deteriorate optical quality of the eye by increasing higher-order aberrations, and the increases are much larger after instillation of timolol gel than long-acting carteolol."( Time course of changes in ocular aberrations after instillation of carteolol long-acting solution and timolol gel-forming solution.
Daito, M; Hiraoka, T; Kiuchi, T; Okamoto, F; Oshika, T, 2011
)
0.79
" In conclusion, carteolol above 1/64 of its clinical therapeutic dosage has a time- and dose-dependent cytotoxicity to HCEP cells, which is achieved by inducing apoptosis via triggering Bcl-2 family protein-mediated mitochondrial pro-apoptotic pathway."( Cytotoxicity of carteolol to human corneal epithelial cells by inducing apoptosis via triggering the Bcl-2 family protein-mediated mitochondrial pro-apoptotic pathway.
Fan, TJ; Shan, M, 2016
)
1.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
beta-adrenergic antagonistAn agent that binds to but does not activate beta-adrenergic receptors thereby blocking the actions of endogenous or exogenous beta-adrenergic agonists. beta-Adrenergic antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches and anxiety.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
antiglaucoma drugAny drug which can be used to prevent or alleviate glaucoma, a disease in which the optic nerve is damaged, resulting in progressive, irreversible loss of vision. It is often, though not always, associated with increased pressure of the fluid in the eye.
anti-arrhythmia drugA drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres.
sympatholytic agentAny compound which inhibits the postganglionic functioning of the sympathetic nervous system (SNS).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
quinolone
secondary alcoholA secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
Carteolol Action Pathway478

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.00190.00011.33919.9840AID218718
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (36)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID218533beta-adrenoceptor blocking activity of the perorally administered compound was evaluated by inhibition of isiprenaline-induced tachycardia in rats1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID40539Selectivity for beta-1 receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID41891Tested for intrinsic sympathomimetic activity (ISA); antagonist with partial agonistic properties1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID41488Selectivity for beta-2 adrenergic receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID220928Beta-adrenoceptor blocking activity after intravenous dose as inhibition of isiprenaline-induced tachycardia in rats1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID218718Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (321)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990117 (36.45)18.7374
1990's103 (32.09)18.2507
2000's53 (16.51)29.6817
2010's32 (9.97)24.3611
2020's16 (4.98)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 50.11

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

MetricThis Compound (vs All)
Research Demand Index50.11 (24.57)
Research Supply Index6.11 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index82.35 (26.88)
Search Engine Supply Index2.03 (0.95)

This Compound (50.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials93 (26.20%)5.53%
Reviews12 (3.38%)6.00%
Case Studies22 (6.20%)4.05%
Observational1 (0.28%)0.25%
Other227 (63.94%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (5)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Parallel, Open-label Study to Evaluate Efficacy and Safety Effects Using Mikelan® LA Ophthalmic Solution (OS) 2% Versus Timoptol® XE Ophthalmic Solution (OS) 0.5% in Ocular Hypertension Patients [NCT00972426]Phase 432 participants (Anticipated)Interventional2009-10-31Completed
[NCT02108288]Phase 130 participants (Actual)Interventional2014-04-30Completed
A Phase III, Multi-center, Randomized, Single-blind (to Evaluator), Parallel, and Positive-controlled Clinical Trial Evaluating the Efficacy and Safety of OPC-1085EL Ophthalmic Solution in the Treatment of Primary Open Angle Glaucoma or Ocular Hypertensio [NCT05583474]Phase 3240 participants (Anticipated)Interventional2022-09-27Recruiting
[NCT02105272]Phase 3237 participants (Actual)Interventional2014-04-30Completed
[NCT02105285]Phase 3193 participants (Actual)Interventional2014-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02105272 (6) [back to overview]Decrease From Baseline in Intraocular Pressure
NCT02105272 (6) [back to overview]Decrease From Baseline in Intraocular Pressure at Week 8 at 2 Hours After IMP Administration
NCT02105272 (6) [back to overview]Decrease From Baseline in Intraocular Pressure at Week 8 at 8 Hours After IMP Administration
NCT02105272 (6) [back to overview]Intraocular Pressure at Week 8 at 2 Hours After IMP Administration
NCT02105272 (6) [back to overview]Intraocular Pressure at Week 8 at 8 Hours After IMP Administration
NCT02105272 (6) [back to overview]Intraocular Pressure at Week 8 Predose
NCT02105285 (6) [back to overview]Change From Baseline in Intraocular Pressure at Week 8 at 8 Hours After IMP Administration
NCT02105285 (6) [back to overview]Decrease From Baseline in Intraocular Pressure at Week 8 at 2 Hours After IMP Administration
NCT02105285 (6) [back to overview]Decrease From Baseline in Intraocular Pressure at Week 8 Predose
NCT02105285 (6) [back to overview]Intraocular Pressure at Week 8 at 2 Hours After IMP Administration
NCT02105285 (6) [back to overview]Intraocular Pressure at Week 8 at 8 Hours After IMP Administration
NCT02105285 (6) [back to overview]Intraocular Pressure at Week 8 Predose
NCT02108288 (4) [back to overview]Cmax of Carteolol
NCT02108288 (4) [back to overview]Cmax of Latanoprost Acid
NCT02108288 (4) [back to overview]Tmax of Carteolol
NCT02108288 (4) [back to overview]Tmax of Latanoprost Acid

Decrease From Baseline in Intraocular Pressure

(NCT02105272)
Timeframe: Baseline, week 8 predose

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution2.9
Latanoprost Ophthalmic Solution1.6

[back to top]

Decrease From Baseline in Intraocular Pressure at Week 8 at 2 Hours After IMP Administration

"Comparison of each group in change from baseline in intraocular pressure at Week 8 at 2 hours after IMP administration.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105272)
Timeframe: Baseline, Week 8 at 2 hours after IMP administration

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution2.1
Latanoprost Ophthalmic Solution1.0

[back to top]

Decrease From Baseline in Intraocular Pressure at Week 8 at 8 Hours After IMP Administration

"Comparison of each group in change from baseline in intraocular pressure at 8 at 8 hours after IMP administration.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105272)
Timeframe: Baseline, Week 8 at 8 hours after IMP administration

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution1.7
Latanoprost Ophthalmic Solution1.0

[back to top]

Intraocular Pressure at Week 8 at 2 Hours After IMP Administration

"Comparison of each group in intraocular pressure at Week 8 at 2 hours after IMP administration.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105272)
Timeframe: Week 8 at 2 hours after IMP administration

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution17.2
Latanoprost Ophthalmic Solution18.2

[back to top]

Intraocular Pressure at Week 8 at 8 Hours After IMP Administration

"Comparison of each group in intraocular pressure at Week 8 at 8hours after IMP administration.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105272)
Timeframe: Week 8 at 8 hours after IMP administration

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution16.7
Latanoprost Ophthalmic Solution17.4

[back to top]

Intraocular Pressure at Week 8 Predose

Comparison of each group in intraocular pressure at Week 8 Predose. The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome. (NCT02105272)
Timeframe: Week 8 Predose

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution17.1
Latanoprost Ophthalmic Solution18.4

[back to top]

Change From Baseline in Intraocular Pressure at Week 8 at 8 Hours After IMP Administration

"Comparison of each group in change from baseline in intraocular pressure at Week 8 at 8 hours after IMP administration.~Arm of a treatment group coming together with latanoprost / carteolol is a reference group. As for Primary Outcome and Secondary Outcome analysis , the OPC-1085EL group was compared only to the carteolol group, not to the latanoprost/carteolol concomitant group.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105285)
Timeframe: Baseline, Week 8 at 8 hours after IMP administration

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution3.0
Carteolol Long-acting Ophthalmic Solution0.3

[back to top]

Decrease From Baseline in Intraocular Pressure at Week 8 at 2 Hours After IMP Administration

"Comparison of each group in change from baseline in intraocular pressure at Week 8 at 2 hours after IMP administration.~Arm of a treatment group coming together with latanoprost / carteolol is a reference group. As for Primary Outcome and Secondary Outcome analysis , the OPC-1085EL group was compared only to the carteolol group, not to the latanoprost/carteolol concomitant group.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105285)
Timeframe: Baseline, Week 8 at 2 hours after IMP administration

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution2.9
Carteolol Long-acting Ophthalmic Solution0.8

[back to top]

Decrease From Baseline in Intraocular Pressure at Week 8 Predose

"Comparison of each group in change from baseline in intraocular pressure. Arm of a treatment group coming together with latanoprost / carteolol is a reference group. As for Primary Outcome and Secondary Outcome analysis , the OPC-1085EL group was compared only to the carteolol group, not to the latanoprost/carteolol concomitant group." (NCT02105285)
Timeframe: Baseline, Week 8 Predose

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution3.5
Carteolol Long-acting Ophthalmic Solution1.6

[back to top]

Intraocular Pressure at Week 8 at 2 Hours After IMP Administration

"Comparison of each group in intraocular pressure at Week 8 at 2 hours after IMP administration.~Arm of a treatment group coming together with latanoprost / carteolol is a reference group. As for Primary Outcome and Secondary Outcome analysis , the OPC-1085EL group was compared only to the carteolol group, not to the latanoprost/carteolol concomitant group.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105285)
Timeframe: Week 8 at 2 hours after IMP administration

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution15.7
Carteolol Long-acting Ophthalmic Solution17.8

[back to top]

Intraocular Pressure at Week 8 at 8 Hours After IMP Administration

"Comparison of each group in intraocular pressure at Week 8 at 8 hours after IMP administration.~Arm of a treatment group coming together with latanoprost / carteolol is a reference group. As for Primary Outcome and Secondary Outcome analysis , the OPC-1085EL group was compared only to the carteolol group, not to the latanoprost/carteolol concomitant group.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105285)
Timeframe: Week 8 at 8 hours after IMP administration

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution15.2
Carteolol Long-acting Ophthalmic Solution17.9

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Intraocular Pressure at Week 8 Predose

"Comparison of each group in intraocular pressure at Week 8 Predose. Arm of a treatment group coming together with latanoprost / carteolol is a reference group. As for Primary Outcome and Secondary Outcome analysis , the OPC-1085EL group was compared only to the carteolol group, not to the latanoprost/carteolol concomitant group.~The number of subjects showed in the Participant Flow comes from all the subjects administered IMP. For efficacy analysis, on the other hand, several subjects were excluded from the analysis according to the statistical analysis plan. For example, subjects without IOP after administration were excluded. In addition, IOP measurement at 8 hours was not mandatory. That is why there are differences between the number in the Participant Flow and Outcome." (NCT02105285)
Timeframe: Week 8 Predose

InterventionmmHg (Mean)
OPC-1085EL Ophthalmic Solution16.3
Carteolol Long-acting Ophthalmic Solution18.2

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Cmax of Carteolol

(NCT02108288)
Timeframe: Day 1 and Day 7

,
Interventionng/mL (Mean)
Day 1Day 7
Carteolol Long-acting Ophthalmic Solution0.99841.627
OPC-1085EL Ophthalmic Solution0.85581.174

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Cmax of Latanoprost Acid

(NCT02108288)
Timeframe: Day 1 and Day 7

,
Interventionpg/mL (Mean)
Day 1Day 7
Latanoprost Ophthalmic Solution21.2217.48
OPC-1085EL Ophthalmic Solution19.7718.47

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Tmax of Carteolol

(NCT02108288)
Timeframe: Day 1 and Day 7

,
Interventionh (Median)
Day 1Day 7
Carteolol Long-acting Ophthalmic Solution0.250.38
OPC-1085EL Ophthalmic Solution0.250.25

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Tmax of Latanoprost Acid

(NCT02108288)
Timeframe: Day 1 and Day 7

,
Interventionmin (Median)
Day 1Day 7
Latanoprost Ophthalmic Solution1010
OPC-1085EL Ophthalmic Solution105

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