Page last updated: 2024-11-06

levocabastine

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Description

Levocabastine is a potent and selective histamine H1 receptor antagonist. It is a chiral molecule, with the levo enantiomer being the active form. Levocabastine is primarily used in the treatment of allergic rhinitis, a condition characterized by inflammation of the nasal passages. It works by blocking the action of histamine, a chemical that is released by the body in response to allergens. Levocabastine is available as a nasal spray and eye drops. It is generally well-tolerated, but common side effects include drowsiness, headache, and dry mouth. Levocabastine is a synthetic compound, and its synthesis is relatively straightforward. It is typically synthesized by reacting a chiral amine with an appropriate aromatic aldehyde. Levocabastine is a valuable tool for studying the role of histamine in allergic reactions. It is also being investigated as a potential treatment for other inflammatory conditions, such as asthma and eczema. Because of its effectiveness in blocking histamine, levocabastine is widely studied as a potential treatment for allergies. Researchers are exploring its effectiveness and potential benefits in different allergy-related conditions, including allergic conjunctivitis, allergic rhinitis, and urticaria. Moreover, the potential application of levocabastine in treating other inflammatory conditions, like asthma, eczema, and even neurological disorders, is being investigated. This ongoing research aims to broaden the therapeutic applications of levocabastine beyond its current use in treating allergic rhinitis.'

levocabastine: for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID54385
CHEMBL ID1615438
CHEBI ID135679
CHEBI ID92584
SCHEMBL ID152978
SCHEMBL ID4577
MeSH IDM0136782

Synonyms (65)

Synonym
AB00514704-06
BRD-K33453211-003-03-2
levocobastine
gtpl1586
PRESTWICK2_001039
PRESTWICK3_001039
BSPBIO_001257
NCGC00179240-01
AB00514704
levocabastine
DB01106
BPBIO1_001382
c26h29fn2o2
levocabastina [spanish]
4-piperidinecarboxylic acid, 1-(4-cyano-4-(4-fluorophenyl)cyclohexyl)-3-methyl-4-phenyl-, (3s-(1(cis),3alpha,4beta))-
levocabastinum [latin]
levocabastine [inn:ban]
PRESTWICK0_001039
PRESTWICK1_001039
SPBIO_003108
CHEBI:135679
levocabastine (inn)
D08117
79516-68-0
79449-98-2
(3s,4r)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid
NCGC00179240-02
r 50547
unii-h68bp06s81
levocabastina
h68bp06s81 ,
levocabastinum
AKOS016013998
levocabastin
(+-)-trans-1-(cis-4-cyano-4-(p-fluorophenyl)cyclohexyl)-3-methyl-4-phenylisonipecotic acid
cabastine [inn]
unii-cou3rrh769
cou3rrh769 ,
cabastinum
cabastine
(+-)-trans-1-(cis-4-cyano-4-(p-fluorophenyl)cyclohexyl)-3-methyl-4-phenylisonipecotic acid.
r50547
levocabastine [mi]
levocabastine [who-dd]
4-piperidinecarboxylic acid, 1-(4-cyano-4-(4-fluorophenyl)cyclohexyl)-3-methyl-4-phenyl-, (-)-(1(cis),3.alpha.,4.beta.)-
levocabastine [inn]
levocabastine [vandf]
CHEMBL1615438
SCHEMBL152978
SCHEMBL4577
(+/-)-trans-1-(cis-4-cyano-4-(p-fluorophenyl)cyclohexyl)-3-methyl-4-phenylisonipecotic acid
DTXSID1048548
bdbm50019405
(3s,4r)-1-(4-cyano-4-(4-fluorophenyl)cyclohexyl)-3-methyl-4-phenylpiperidine-4-carboxylic acid
CHEBI:92584
(3s,4r)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid
Q27164305
Q2240116
rel-(3r,4s)-1-[cis-4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid
DTXSID001024637
CS-0002969
HY-14277
EN300-6481353
(3s,4r)-3-methyl-4-phenyl-1-[(1s,4s)-4-cyano-4-(4-fluorophenyl)cyclohexyl]piperidine-4-carboxylic acid
AKOS040752530

Research Excerpts

Overview

Levocabastine is an antiallergic drug acting as a histamine H1-receptor antagonist. It is currently a target drug for drug repurposing to treat other diseases like vernal keratoconjuctivitis.

ExcerptReferenceRelevance
"Levocabastine is an important drug in treatment of allergy and currently a target drug for drug repurposing to treat other diseases like vernal keratoconjuctivitis."( Biophysical insight into the interaction of levocabastine with human serum albumin: spectroscopy and molecular docking approach.
Abdelhameed, AS; Ajmal, MR; Al-Alawy, AIA; Almutairi, FM; Khan, RH; Majid, N; Siddiqi, MK, 2021
)
1.6
"Levocabastine is an antiallergic drug acting as a histamine H1-receptor antagonist. "( Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine.
Baiula, M; Bedini, A; Bucolo, C; Fascì, D; Govoni, P; Qasem, AR; Spampinato, S; Spartà, A, 2008
)
2.02
"Levocabastine is a very potent histamine H1 antagonist, available for ocular use as eye drops containing 0.5 mg/ml of levocabastine with benzalkonium chloride as a preservative. "( Tolerability of levocabastine eye drops.
Blockhuys, S; Janssens, M, 1993
)
2.07
"Levocabastine is a potent histamine H1 receptor antagonist used topically in the treatment of patients with allergic rhinitis. "( Selective effect of levocabastine on histamine receptor and histamine release from human leukocytes and guinea pig isolated tissue.
Boegheim, JP; de Graaf-in't Veld, T; Garrelds, IM; Saxena, PR; van Toorenenbergen, AW; van Wijk, RG; Zijlstra, FJ, 1996
)
2.06
"Levocabastine is a potent and selective histamine H1-receptor antagonist which has been evaluated as a topical treatment (nasal spray and/or eyedrops) for allergic rhinitis and/or conjunctivitis. "( Levocabastine. An update of its pharmacology, clinical efficacy and tolerability in the topical treatment of allergic rhinitis and conjunctivitis.
McTavish, D; Noble, S, 1995
)
3.18
"Levocabastine is a selective topical H1 antagonist, effective in the treatment of seasonal allergic rhinitis and conjunctivitis."( Topical ocular levocabastine reduces ICAM-1 expression on epithelial cells both in vivo and in vitro.
Bagnasco, M; Buscaglia, S; Canonica, GW; Catrullo, A; Ciprandi, G; Fiorino, N; Montagna, P; Paolieri, F; Pesce, G; Riccio, AM, 1996
)
2.09
"Levocabastine is a potent and highly selective H1-receptor antagonist specifically developed for the topical treatment of allergic conjunctivitis. "( Levocabastine eye drops do not affect accommodative capacity in volunteers and intraocular pressure in glaucoma patients.
Remky, A; Wohlrab, TM; Wolf, S,
)
3.02
"Levocabastine is an antihistaminic agent for topical application. "( [Clinical efficacy and safety of levocarbastine++ in the therapy in children suffering from seasonal allergic rhinitis and conjunctivitis who are less than 12 year of age].
Bukowczan, Z; Doniec, Z; Kossek, M; Kurzawa, R; Mazurek, H; Radliński, J; Sak-Kopytyńska, I; Urbanek, E, 1998
)
1.74
"Levocabastine is a recently developed, potent H1-receptor blocker intended for topical application. "( Rapid onset of action of levocabastine eye-drops in histamine-induced conjunctivitis.
Feinberg, G; Stokes, TC, 1993
)
2.03
"Levocabastine is a selective histamine H1-receptor antagonist exerting inhibitory effects on the release of chemical mediators from mast cells and on the chemotaxis of polymorphonuclear leukocytes and eosinophils. "( [Pharmacological and clinical properties of levocabastine hydrochloride (eye drop and nasal spray), a selective H1 antagonist].
Akiyoshi, M; Enomoto, S; Hirano, F; Maki, E; Shigeoka, T; Takahashi, H; Torii, S, 2002
)
2.02
"Levocabastine is a novel H1-receptor antagonist for topical use, which is being investigated in allergic rhinitis (nasal spray) and conjunctivitis (eye drops). "( Levocabastine: a new topical approach for the treatment of paediatric allergic rhinoconjunctivitis.
Janssens, MM, 1992
)
3.17
"Levocabastine is a new topical histamine H1 antagonist. "( Efficacy of levocabastine in conjunctival provocation studies.
Janssens, M, 1992
)
2.11
"Levocabastine is a newly synthesized histamine H1 antagonist which has been formulated as both eye drops and nasal spray."( New trends in the treatment of allergic conjunctivitis.
Blockhuys, S; Janssens, M; Parys, W, 1992
)
1
"Levocabastine is a long acting, highly potent and selective histamine H1-receptor antagonist, which has been developed for nasal and ocular administration. "( Levocabastine. A review of its pharmacological properties and therapeutic potential as a topical antihistamine in allergic rhinitis and conjunctivitis.
Dechant, KL; Goa, KL, 1991
)
3.17
"Levocabastine is a new H1 receptor blocking antihistamine which is intended for topical use in the treatment of allergic conjunctivitis. "( Topical levocabastine protects better than sodium cromoglycate and placebo in conjunctival provocation tests.
Björkstén, B; Blychert, LO; Kjellman, NI; Rimås, M, 1990
)
2.16
"Levocabastine is a potent competitor against histamine for conjunctival H1 receptors and should prove a useful, possibly long-acting drug for the reversal of inflammatory conjunctivitis and inhibition of its recurrence."( Application of histamine-induced conjunctivitis to the assessment of a topical antihistamine, levocabastine.
Feinberg, G; Stokes, TC, 1987
)
1.21
"Levocabastine is a new selective H1 receptor antagonist. "( Effect of a new selective H1 receptor antagonist (levocabastine) in a nasal and conjunctival provocation test.
Kolly, M; Pécoud, A; Zuber, P, 1987
)
1.97
"Levocabastine is a new, highly potent, and specific H1 antagonist. "( Effect of levocabastine, a new H1 antagonist, in a conjunctival provocation test with allergens.
Pécoud, A; Zuber, P, 1988
)
2.12
"Levocabastine is a potent antihistamine drug, structurally unrelated to neurotensin. "( Evidence for a displaceable non-specific [3H]neurotensin binding site in rat brain.
Laduron, PM; Leysen, JE; Schotte, A, 1986
)
1.71

Effects

Levocabastine has a fast onset of action, with 94% of patients experiencing symptom relief within 15 min after the first instillation.

Levocabastine eye drops have been found to be well tolerated with an adverse-effect profile comparable to placebo and sodium cromoglycate. The topical application of the drug does not irritate the mucosa of conjunctivas and nasal cavities. Levocabstine has a fast onset of action, with 94% of patients experiencing symptom relief within 15 min after the first instillation.

ExcerptReferenceRelevance
"Levocabastine has a fast onset of action."( New trends in the treatment of allergic conjunctivitis.
Blockhuys, S; Janssens, M; Parys, W, 1992
)
1
"Levocabastine has a fast onset of action, with 94% of patients experiencing symptom relief within 15 min after the first instillation of levocabastine eye drops."( Levocabastine: an effective topical treatment of allergic rhinoconjunctivitis.
Janssens, MM; Vanden Bussche, G, 1991
)
2.45
"Levocabastine has no influence on the order parameter tested with liposomes, suggesting that the drug provides no significant effect on the membrane fluidity of lipid bilayer."( Antiallergic profile of the novel H1-antihistaminic compound levocabastine.
Akagi, M; Chokki, M; Kamei, C; Mio, M; Shirasaka, T; Tasaka, K, 1993
)
1.25
"Levocabastine eye drops have been found to be well tolerated with an adverse-effect profile comparable to placebo and sodium cromoglycate."( Levocabastine eye drops: a new approach for the treatment of acute allergic conjunctivitis.
Abelson, MB; Weintraub, D,
)
2.3
"Levocabastine has been demonstrated to have rapid onset of action in children with SAR and the topical application of the drug does not irritate the mucosa of conjunctivas and nasal cavities."( [Clinical efficacy and safety of levocarbastine++ in the therapy in children suffering from seasonal allergic rhinitis and conjunctivitis who are less than 12 year of age].
Bukowczan, Z; Doniec, Z; Kossek, M; Kurzawa, R; Mazurek, H; Radliński, J; Sak-Kopytyńska, I; Urbanek, E, 1998
)
1.02
"Levocabastine, which has affinity for the NT2 receptor, did not inhibit specific binding of (125)I-NT in membrane competition or autoradiographic studies."( Characterization and autoradiographic localization of neurotensin binding sites in human sigmoid colon.
Azriel, Y; Burcher, E, 2001
)
1.03
"Levocabastine has a fast onset of action."( New trends in the treatment of allergic conjunctivitis.
Blockhuys, S; Janssens, M; Parys, W, 1992
)
1
"Levocabastine has a fast onset of action, with 94% of patients experiencing symptom relief within 15 min after the first instillation of levocabastine eye drops."( Levocabastine: an effective topical treatment of allergic rhinoconjunctivitis.
Janssens, MM; Vanden Bussche, G, 1991
)
2.45

Actions

ExcerptReferenceRelevance
"Levocabastine prevented an increase in the vascular permeability of nasal mucosa elicited by instillation of these three inducers."( [Pharmacological and clinical properties of levocabastine hydrochloride (eye drop and nasal spray), a selective H1 antagonist].
Akiyoshi, M; Enomoto, S; Hirano, F; Maki, E; Shigeoka, T; Takahashi, H; Torii, S, 2002
)
1.3

Treatment

Pretreatment with levocabastine resulted in a median ATD of 32,000 BU, compared with 10,000 after cromoglycate (P less than 0.001) or placebo.

ExcerptReferenceRelevance
"Pretreatment with levocabastine dose-dependently decreased the contractile response to histamine, showing an irreversible competitive mechanism."( Selective effect of levocabastine on histamine receptor and histamine release from human leukocytes and guinea pig isolated tissue.
Boegheim, JP; de Graaf-in't Veld, T; Garrelds, IM; Saxena, PR; van Toorenenbergen, AW; van Wijk, RG; Zijlstra, FJ, 1996
)
0.94
"Pretreatment with levocabastine resulted in a median ATD of 32,000 BU, compared with 10,000 after cromoglycate (P less than 0.001) or placebo (P less than 0.01)."( Topical levocabastine protects better than sodium cromoglycate and placebo in conjunctival provocation tests.
Björkstén, B; Blychert, LO; Kjellman, NI; Rimås, M, 1990
)
1.04

Toxicity

ExcerptReferenceRelevance
" Overall, the incidence of adverse events was similar for both treatment groups."( Efficacy and safety of levocabastine nasal spray for seasonal allergic rhinitis.
Dolen, J; Hampel, FC; Holton, D; Karcher, K; Martin, BG; Travers, S,
)
0.44
"5% ophthalmic solution instilled four times daily is effective and safe in reducing the signs and symptoms of seasonal allergic conjunctivitis."( Efficacy and safety of ketorolac tromethamine 0.5% and levocabastine 0.05%: a multicenter comparison in patients with seasonal allergic conjunctivitis.
Donshik, PC; Pearlman, D; Pinnas, J; Raizman, MB; Tauber, J; Tinkelman, D; Walters, TR,
)
0.38
" 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
)
0.56
" The type and frequency of adverse events were similar across treatment groups."( Efficacy and safety of ketotifen eye drops in the treatment of seasonal allergic conjunctivitis.
Cooper, C; Kidd, M; Lanz, R; McKenzie, SH; Steven, I, 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
" The safety evaluation included adverse events, visual acuity, intra-ocular pressure and study drug drop sensation."( [Safety and efficacy of a new preservative-free levocabastine ophthalmic solution (Levofree®) using the conjunctival provocation test].
Allaire, C; Bassols, A; Siou-Mermet, R, 2012
)
0.63
" The incidence of adverse events was lower with the preservative-free solution than with the preserved suspension."( [Safety and efficacy of a new preservative-free levocabastine ophthalmic solution (Levofree®) using the conjunctival provocation test].
Allaire, C; Bassols, A; Siou-Mermet, R, 2012
)
0.63
" All treatments were well tolerated, and adverse event incidence was similar across the treatment groups."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.65

Pharmacokinetics

The linear and predictable pharmacokinetic properties of the histamine H1-receptor antagonist levocabastine make it particularly suitable for intranasal or ocular treatment of allergic rhinoconjunctivitis.

ExcerptReferenceRelevance
" The decreased urinary excretion most likely contributed to the prolonged half-life (from 36 hours to 95 hours) and increased area under the plasma concentration-time curve (+56%) in the patients with renal insufficiency as compared with the healthy volunteers."( Pharmacokinetics of orally administered levocabastine in patients with renal insufficiency.
Heykants, J; Huang, ML; Stephen, A; Van Peer, A; Woestenborghs, R; Zazgornik, J, 1993
)
0.55
"The linear and predictable pharmacokinetic properties of the histamine H1-receptor antagonist levocabastine make it particularly suitable for intranasal or ocular treatment of allergic rhinoconjunctivitis."( The pharmacokinetic properties of topical levocabastine. A review.
Heykants, J; Meuldermans, W; Snoeck, E; Van de Velde, V; Van Peer, A; Woestenborghs, R, 1995
)
0.77
" The mean terminal half-life was approximately 45 and 44 hours, respectively."( Lack of effect of erythromycin and ketoconazole on the pharmacokinetics and pharmacodynamics of steady-state intranasal levocabastine.
Grover, M; Hall, N; Hassell, A; Hunt, T; Lee, P; Mechlinski, W; Pesco-Koplowitz, L; Smith, R; Travers, S; Wiesinger, B; Zhou, H, 1999
)
0.51
"The purpose of this study was to investigate potential systemic pharmacokinetic interactions between intranasal fluticasone furoate (FF) and levocabastine (LEVO) when delivered simultaneously via a metered atomizing spray pump."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.86
"These results suggest that in healthy subjects, for LEVO, there is no pharmacokinetic interaction with FF when delivered as FF/LEVO FDC."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.65

Bioavailability

ExcerptReferenceRelevance
" As the majority of data were below the assay sensitivity for FF, any potential differences in the bioavailability of FF when delivered alone or as FF/LEVO FDC could not be established."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.65

Dosage Studied

Oxotremorine-induced tremor and salivation in mice were delayed after extremely high dosage of levocabastine. These were much less effective than those seen after diphenhydramine and ketotifen.

ExcerptRelevanceReference
" Oxotremorine-induced tremor and salivation in mice were delayed after extremely high dosage of levocabastine; however, these were much less effective than those seen after diphenhydramine and ketotifen."( Central effect of the potent long-acting H1-antihistamine levocabastine.
Aoki, I; Kamei, C; Tasaka, K; Tsujimoto, S; Yoshida, T, 1990
)
0.74
" Although the 6-hour hemodialysis procedure starting 4 hours after dosing eliminated 10% of the oral dose, the terminal half-life and the total area under the plasma concentration-time curve did not differ significantly between the hemodialysis and the nonhemodialysis patients."( Pharmacokinetics of orally administered levocabastine in patients with renal insufficiency.
Heykants, J; Huang, ML; Stephen, A; Van Peer, A; Woestenborghs, R; Zazgornik, J, 1993
)
0.55
" The newer mast-cell stabilizing agent nedocromil sodium has a similar safety profile to sodium cromoglycate, but is more potent and has a more convenient twice-daily dosing regimen."( Treating severe eye allergy.
Verin, P, 1998
)
0.3
"To test the hypothesis that intranasal levocabastine (LEVO) may provide benefits as a oncedaily treatment in allergic rhinitis (AR), this non-inferiority study compared the effect at steady state of once- and twice-daily dosing with LEVO on allergen-induced nasal symptoms in AR patients."( Once-daily dosing of levocabastine has comparable efficacy to twice-daily dosing in the treatment of allergic rhinitis assessed in an allergen challenge chamber.
Bareille, P; Gupta, A; Ignar, D; Mark, S; Miller, SR; Murdoch, RD; Patel, P; Salapatek, AM, 2015
)
1.01
"82), demonstrating noninferiority between the two LEVO dosing regimens by meeting the pre-specified criterion of an upper limit of 95% CI<1."( Once-daily dosing of levocabastine has comparable efficacy to twice-daily dosing in the treatment of allergic rhinitis assessed in an allergen challenge chamber.
Bareille, P; Gupta, A; Ignar, D; Mark, S; Miller, SR; Murdoch, RD; Patel, P; Salapatek, AM, 2015
)
0.74
"The results of this study support the hypothesis that at steady state LEVO 200 µg taken once-daily provides similar benefit to LEVO 200 µg dosed twice-daily."( Once-daily dosing of levocabastine has comparable efficacy to twice-daily dosing in the treatment of allergic rhinitis assessed in an allergen challenge chamber.
Bareille, P; Gupta, A; Ignar, D; Mark, S; Miller, SR; Murdoch, RD; Patel, P; Salapatek, AM, 2015
)
0.74
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperidines
[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
Levocabastine H1-Antihistamine Action87

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neurotensin receptor type 2Rattus norvegicus (Norway rat)Ki0.03300.00580.09170.6440AID1154142
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neurotensin receptor type 2Rattus norvegicus (Norway rat)EC50 (µMol)0.02800.01800.07080.2170AID1154139
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (31)

Assay IDTitleYearJournalArticle
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.
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.
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.
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).
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).
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID1154139Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID419514Volume of distribution at steady state in human at 0.2 mg, iv2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
In silico prediction of volume of distribution in human using linear and nonlinear models on a 669 compound data set.
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).
AID1154136Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1154138Antagonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as inhibition of NT-induced calcium release by FLIPR assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
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).
AID1154140Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay relative to SR142948a2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
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.
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).
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).
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).
AID1154142Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
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).
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).
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).
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).
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).
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).
AID1346325Human NTS2 receptor (Neurotensin receptors)2001Molecular pharmacology, Dec, Volume: 60, Issue:6
Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2.
AID1346315Rat NTS2 receptor (Neurotensin receptors)1996FEBS letters, May-20, Volume: 386, Issue:2-3
Molecular cloning of a levocabastine-sensitive neurotensin binding site.
AID1346374Mouse NTS2 receptor (Neurotensin receptors)1998Biochemical and biophysical research communications, Feb-13, Volume: 243, Issue:2
Stable expression of the mouse levocabastine-sensitive neurotensin receptor in HEK 293 cell line: binding properties, photoaffinity labeling, and internalization mechanism.
AID1346325Human NTS2 receptor (Neurotensin receptors)1996The Journal of neuroscience : the official journal of the Society for Neuroscience, Sep-15, Volume: 16, Issue:18
Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain.
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 (190)

TimeframeStudies, This Drug (%)All Drugs %
pre-199019 (10.00)18.7374
1990's92 (48.42)18.2507
2000's53 (27.89)29.6817
2010's23 (12.11)24.3611
2020's3 (1.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 47.59

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

MetricThis Compound (vs All)
Research Demand Index47.59 (24.57)
Research Supply Index5.68 (2.92)
Research Growth Index4.93 (4.65)
Search Engine Demand Index90.40 (26.88)
Search Engine Supply Index2.41 (0.95)

This Compound (47.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials89 (43.63%)5.53%
Reviews21 (10.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other94 (46.08%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Study of Medication for Nonallergic Rhinitis (NAR) Based on Cluster Analysis [NCT04002349]80 participants (Anticipated)Interventional2019-07-01Recruiting
A Randomized, Double-blind, Placebo Controlled, 3 Way Cross Over Study in Subjects With Allergic Rhinitis to Assess the Effect of Intranasal Repeat Doses of Levocabastine When Administered Once Daily or Twice Daily on the Symptoms of Rhinitis in an Allerg [NCT01949051]Phase 278 participants (Actual)Interventional2013-10-01Completed
A Randomised, Double-blind, Placebo-controlled, 3 Way, Incomplete Block Cross Over Study in Subjects With Allergic Rhinitis to Assess the Effect of Once Daily Single and Repeat Doses of Intranasal Fluticasone Furoate/Levocabastine Fixed Dose Combination ( [NCT01957202]Phase 271 participants (Actual)Interventional2013-10-31Completed
A Randomized, Double-blind, Active-controlled, Multicenter Phase 3 Clinical Trial to Evaluate the Efficacy and Safety of Concomitant Mometasone Furoate and Levocabastine HCl in Perennial Allergic Rhinitis Patients [NCT02498509]Phase 3459 participants (Anticipated)Interventional2015-05-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01949051 (2) [back to overview]Weighted Mean of the Total Nasal Symptom Score (TNSS) (0-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 8
NCT01949051 (2) [back to overview]Weighted Mean of the Symptom Scores for the Four Individual Components of the Total Nasal Symptom Score (TNSS) (Nasal Congestion, Rhinorrhea, Nasal Itching and Sneezing) (0-4) Hours Post Start of the Allergen Chamber Challenge on Day 8
NCT01957202 (4) [back to overview]Weighted Mean of the Magnitude of Symptom Relief on Total Nasal Symptom Score (TNSS) (2-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 1 of Each Treatment Period
NCT01957202 (4) [back to overview]Weighted Mean of the Magnitude of Symptom Relief on Total Ocular Symptom Score (TOSS) (2-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 1 of Each Treatment Period
NCT01957202 (4) [back to overview]Weighted Mean of the Total Nasal Symptom Score (TNSS) (0-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 8 of Each Treatment Period
NCT01957202 (4) [back to overview]Weighted Mean of the Total Ocular Symptom Score (TOSS) (0-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 8 of Each Treatment Period

Weighted Mean of the Total Nasal Symptom Score (TNSS) (0-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 8

The TNSS (score of 0-12) is defined as the sum of the symptom scores for the four individual components (nasal congestion, rhinorrhea, nasal itch, and sneezing, each scored on 0-3 scale [0=none, 1=mild, 2=moderate, 3=severe]). TNSS was measured at the pre-allergen chamber challenge, and then every 15 minutes from 0 to 4 hours post start of the allergen chamber challenge. In the Environmental Exposure Chamber (EEC), aerosolized allergen was administered in a sealed chamber to evaluate the efficacy of antihistamines/other treatments. Weighted mean TNSS was calculated by dividing the value of the area under the response time curve over the 0-4 hours (calculated by trapezoidal rule) by the time interval of available data. (NCT01949051)
Timeframe: Day 8 of each treatment period (up to 13 Weeks)

InterventionScores on a scale (Least Squares Mean)
Placebo5.190
Levocabastine 200µg OD4.071
Levocabastine 400µg BID3.840

[back to top]

Weighted Mean of the Symptom Scores for the Four Individual Components of the Total Nasal Symptom Score (TNSS) (Nasal Congestion, Rhinorrhea, Nasal Itching and Sneezing) (0-4) Hours Post Start of the Allergen Chamber Challenge on Day 8

TNSS contains symtom scores for the four individual components (nasal congestion [NACG], rhinorrhea [RHSCR], nasal itching [NAITS] and sneezing [SNZS]), each scored on a 0 - 3 scale [0=none, 1=mild, 2=moderate, 3=severe]). TNSS was measured at the pre-allergen chamber challenge, and then every 15 minutes from 0 to 4 hours post start of the allergen chamber challenge. In the Environmental Exposure Chamber (EEC), aerosolized allergen is administered in a sealed chamber to evaluate the efficacy of antihistamines/other treatments. The participants recorded their symptom scores on an e-diary. The mean score for each participant was calculated using the available diary data from the assessment periods, taking the average of non-missing data during the period. Weighted mean of the individual symptoms of theTNSS were calculated by dividing the value of the area under the response time curve over the 0-4 hours (calculated by trapezoidal rule) by the time interval of available data. (NCT01949051)
Timeframe: Day 8 of each treatment period (up to 13 Weeks)

,,
InterventionScores on a scale (Least Squares Mean)
NACGRHSCRNAITSSNZS
Levocabastine 200µg OD1.2171.0351.0990.647
Levocabastine 400µg BID1.2261.0041.0400.529
Placebo1.4831.4031.2571.018

[back to top]

Weighted Mean of the Magnitude of Symptom Relief on Total Nasal Symptom Score (TNSS) (2-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 1 of Each Treatment Period

Magnitude of symptom relief was assessed by calculating change from pre-dose weighted mean TNSS (2-4h) post start of the allergen chamber challenge at Day 1. The pre-dose value was the maximum of the three pre-dose measurements (1h 15 minutes (min), 1h 30 min and 1h 45 min post start of the allergen chamber challenge). The TNSS (score of 0-12) is defined as the sum of the symptom scores for the four individual components (nasal congestion, rhinorrhea, nasal itch and sneezing, each scored on 0-3 scale [0=none, 1=mild, 2=moderate, 3=severe]). (NCT01957202)
Timeframe: Day 1 of each treatment period (up to 80 days)

InterventionScores on a scale (Least Squares Mean)
Placebo-1.335
FF 100 μg-0.904
Levo 200 μg-2.588
FF 100 μg/Levo 200 μg-2.267

[back to top]

Weighted Mean of the Magnitude of Symptom Relief on Total Ocular Symptom Score (TOSS) (2-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 1 of Each Treatment Period

Magnitude of symptom relief was assessed by calculating change from pre-dose weighted mean TOSS (2-4h) post start of the allergen chamber challenge at Day 1. The pre-dose value was the maximum of the three pre-dose measurements (1h 15 minutes (min), 1h 30 min and 1h 45 min post start of the allergen chamber challenge). The TOSS (score of 0-9) is defined as the sum of the symptom scores for the three individual components (red, itchy, and tearing eyes, each scored on 0-3 scale [0=none, 1=mild, 2=moderate, 3=severe], average of two eyes). (NCT01957202)
Timeframe: Day 1 of each treatment period (up to 80 days)

InterventionScores on a scale (Least Squares Mean)
Placebo-0.097
FF 100 μg-0.272
Levo 200 μg-0.633
FF 100 μg/Levo 200 μg-0.446

[back to top]

Weighted Mean of the Total Nasal Symptom Score (TNSS) (0-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 8 of Each Treatment Period

The TNSS (score of 0-12) is defined as the sum of the symptom scores for the four individual components (nasal congestion, rhinorrhea, nasal itch, and sneezing, each scored on 0-3 scale [0=none, 1=mild, 2=moderate, 3=severe]). TNSS was measured at the pre-allergen chamber challenge, and then every 15 minutes from 0 to 4 hours post start of the allergen chamber challenge. In the Environmental Exposure Chamber (EEC), aerosolized allergen was administered in a sealed chamber to evaluate the efficacy of antihistamines/other treatments. Weighted mean TNSS was calculated by dividing the value of the area under the response time curve over the 0-4 hours (calculated by trapezoidal rule) by the time interval of available data. (NCT01957202)
Timeframe: Day 8 of each treatment period (up to 80 days)

InterventionScores on a scale (Least Squares Mean)
Placebo6.030
FF 100 μg4.189
Levo 200 μg4.500
FF 100 μg/Levo 200 μg1.933

[back to top]

Weighted Mean of the Total Ocular Symptom Score (TOSS) (0-4) Hours (h) Post Start of Allergen Chamber Challenge on Day 8 of Each Treatment Period

The TOSS (score of 0-9) is defined as the sum of the symptom scores for the three individual components (red, itchy, and tearing eyes , each scored on 0-3 scale [0=none, 1=mild, 2=moderate, 3=severe], average of two eyes). TOSS was measured at the pre-allergen chamber challenge, and then every 15 minutes from 0 to 4 hours post start of the allergen chamber challenge. In the Environmental Exposure Chamber (EEC), aerosolized allergen was administered in a sealed chamber to evaluate the efficacy of antihistamines/other treatments. Weighted mean TOSS was calculated by dividing the value of the area under the response time curve over the 0-4 hours (calculated by trapezoidal rule) by the time interval of available data. (NCT01957202)
Timeframe: Day 8 of each treatment period (up to 80 days)

InterventionScores on a scale (Least Squares Mean)
Placebo1.321
FF 100 μg0.761
Levo 200 μg0.621
FF 100 μg/Levo 200 μg0.546

[back to top]