Page last updated: 2024-11-12

sar 1118

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

Description

lifitegrast: An LFA-1 (LYMPHOCYTE FUNCTION-ASSOCIATED ANTIGEN-1) antagonist that is used in the treatment of DRY EYE SYNDROMES. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

lifitegrast : An N-acyl-L-alpha-amino acid obtained by formal condensation of the carboxy group of N-[2-(1-benzofuran-6-carbonyl)]-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxylic acid with the amino group of 3-(methanesulfonyl)-L-phenylalanine. Used for treatment of keratoconjunctivitis sicca (dry eye syndrome). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID11965427
CHEMBL ID2048028
CHEBI ID133023
SCHEMBL ID2632068
MeSH IDM0577395

Synonyms (57)

Synonym
1025967-78-5
xiidra
sar1118
n-[2-(1-benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carbonyl]-3-(methanesulfonyl)-l-phenylalanine
lifitegrast
CHEBI:133023 ,
sar-1118
sar 1118
bdbm50386331
S3714
lifitegrast (usan/inn)
xiidra (tn)
D10374
unii-038e5l962w
lifitegrast [usan:inn]
l-phenylalanine, n-((2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl)carbonyl)-3-(methylsulfonyl)-
(2s)-2-(((2-(benzofuran-6-ylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinolin-6- yl)carbonyl)amino)-3-(3-(methylsulfonyl)phenyl)propanoic acid
038e5l962w ,
shp606
CHEMBL2048028 ,
shp-606
lifitegrast [usan]
lifitegrast [orange book]
lifitegrast [who-dd]
lifitegrast [inn]
lifitegrast [mi]
compound 1g [pmid: 24900456]
gtpl7533
(2s)-2-[[2-(1-benzofuran-6-carbonyl)-5,7-dichloro3,4-dihydro-1h-isoquinoline-6-carbonyl]amino]-3-(3-methylsulfonylphenyl)propanoic acid
SCHEMBL2632068
AC-32534
(s)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid
DTXSID60145345 ,
mfcd28502439
AKOS030628489
CS-6264
(s)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid;(s)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)
HY-19344
DB11611
(2s)-2-[[2-(1-benzofuran-6-carbonyl)-5,7-dichloro-3,4-dihydro-1h-isoquinoline-6-carbonyl]amino]-3-(3-methylsulfonylphenyl)propanoic acid
lifitegrast; sar 1118
EX-A2582
DS-20052
Q23044263
AMY4450
CCG-270245
l-phenylalanine, n-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-
n-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-l-phenylalanine
A900838
lifitegrastum
(2s)-2-(((2-(benzofuran-6-ylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinolin-6-yl)carbonyl)amino)-3-(3-(methylsulfonyl)phenyl)propanoic acid
n-(2-(1-benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carbonyl)-3-(methanesulfonyl)-l-phenylalanine
compound 1g (pmid: 24900456)
dtxcid6067836
s01xa25
(2s)-2-{[2-(1-benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinolin-6-yl]formamido}-3-(3-methanesulfonylphenyl)propanoic acid
EN300-20605731

Research Excerpts

Overview

SAR 1118 is an investigational small molecule lymphocyte function-associated antigen-1 (LFA-1; CD11a/CD18; αLβ2) antagonist that inhibits LFA- 1 binding to intercellular adhesion molecule-1. SAR 1118 targeting T-cell-mediated inflammation.

ExcerptReferenceRelevance
"SAR 1118 is an investigational small molecule lymphocyte function-associated antigen-1 (LFA-1; CD11a/CD18; αLβ2) antagonist that inhibits LFA-1 binding to intercellular adhesion molecule-1 (ICAM-1; CD54) targeting T-cell-mediated inflammation."( Safety and pharmacokinetics of a novel lymphocyte function-associated antigen-1 antagonist ophthalmic solution (SAR 1118) in healthy adults.
Burnier, JP; Gadek, TR; Haughey, DB; Newman, MS; O'Neill, CA; Semba, CP; Smith, VL; Swearingen, D, 2011
)
1.3

Toxicity

SAR 1118 Ophthalmic Solution appears safe and well-tolerated up to 5. dose-dependent levels of drug were detected in aqueous.

ExcerptReferenceRelevance
" No serious ocular or nonocular adverse events (AEs) occurred over 1,148 subject study days (41 days/subject) and no significant abnormalities were identified on ocular exam."( Safety and pharmacokinetics of a novel lymphocyte function-associated antigen-1 antagonist ophthalmic solution (SAR 1118) in healthy adults.
Burnier, JP; Gadek, TR; Haughey, DB; Newman, MS; O'Neill, CA; Semba, CP; Smith, VL; Swearingen, D, 2011
)
0.58
" The only adverse events reported were instillation site irritation (4/13, 31%) and dysgeusia (3/13, 23%)."( Safety, tolerability, and bioavailability of topical SAR 1118, a novel antagonist of lymphocyte function-associated antigen-1: a phase 1b study.
Do, DV; Gadek, TR; Gehlbach, P; Handa, JT; Nguyen, QD; Paskowitz, DM; Semba, C; Shaikh, O; Solomon, S; Stark, W, 2012
)
0.63
"Topical SAR 1118 was safe and well tolerated, and dose-dependent levels of drug were detected in aqueous."( Safety, tolerability, and bioavailability of topical SAR 1118, a novel antagonist of lymphocyte function-associated antigen-1: a phase 1b study.
Do, DV; Gadek, TR; Gehlbach, P; Handa, JT; Nguyen, QD; Paskowitz, DM; Semba, C; Shaikh, O; Solomon, S; Stark, W, 2012
)
1.06
" The primary objective was percentage and severity of treatment-emergent adverse events (TEAEs)."( Safety of Lifitegrast Ophthalmic Solution 5.0% in Patients With Dry Eye Disease: A 1-Year, Multicenter, Randomized, Placebo-Controlled Study.
Donnenfeld, ED; Karpecki, PM; Majmudar, PA; Nichols, KK; Raychaudhuri, A; Roy, M; Semba, CP, 2016
)
0.43
"0% seemed safe and well tolerated in this study, with no unexpected adverse events."( Safety of Lifitegrast Ophthalmic Solution 5.0% in Patients With Dry Eye Disease: A 1-Year, Multicenter, Randomized, Placebo-Controlled Study.
Donnenfeld, ED; Karpecki, PM; Majmudar, PA; Nichols, KK; Raychaudhuri, A; Roy, M; Semba, CP, 2016
)
0.43
" Treatment-emergent adverse events and drop comfort scores were assessed."( Safety and tolerability of lifitegrast ophthalmic solution 5.0%: Pooled analysis of five randomized controlled trials in dry eye disease.
Donnenfeld, ED; Hovanesian, JA; Karpecki, PM; Nichols, KK; Raychaudhuri, A; Shojaei, A; Zhang, S, 2019
)
0.51
" Ocular treatment-emergent adverse events occurring in >5% in either group were instillation site irritation (lifitegrast, 15."( Safety and tolerability of lifitegrast ophthalmic solution 5.0%: Pooled analysis of five randomized controlled trials in dry eye disease.
Donnenfeld, ED; Hovanesian, JA; Karpecki, PM; Nichols, KK; Raychaudhuri, A; Shojaei, A; Zhang, S, 2019
)
0.51
"0% appeared to be safe and well tolerated for the treatment of dry eye disease."( Safety and tolerability of lifitegrast ophthalmic solution 5.0%: Pooled analysis of five randomized controlled trials in dry eye disease.
Donnenfeld, ED; Hovanesian, JA; Karpecki, PM; Nichols, KK; Raychaudhuri, A; Shojaei, A; Zhang, S, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Dosing was divided into 3 periods each separated by a 72-h treatment-free observation: once-daily (QD) × 1, twice-daily (BID) × 10, and thrice-daily (TID) × 10 days."( Safety and pharmacokinetics of a novel lymphocyte function-associated antigen-1 antagonist ophthalmic solution (SAR 1118) in healthy adults.
Burnier, JP; Gadek, TR; Haughey, DB; Newman, MS; O'Neill, CA; Semba, CP; Smith, VL; Swearingen, D, 2011
)
0.58
" Tear PK profiles support a QD/BID dosing schedule."( Safety and pharmacokinetics of a novel lymphocyte function-associated antigen-1 antagonist ophthalmic solution (SAR 1118) in healthy adults.
Burnier, JP; Gadek, TR; Haughey, DB; Newman, MS; O'Neill, CA; Semba, CP; Smith, VL; Swearingen, D, 2011
)
0.58
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
anti-inflammatory drugA substance that reduces or suppresses inflammation.
lymphocyte function-associated antigen-1 antagonistAny antagonist of lymphocyte function-associated antigen-1
[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 (5)

ClassDescription
L-phenylalanine derivativeA proteinogenic amino acid derivative resulting from reaction of L-phenylalanine at the amino group or the carboxy group, or from the replacement of any hydrogen of L-phenylalanine by a heteroatom.
sulfoneAn organosulfur compound having the structure RS(=O)2R (R =/= H).
N-acyl-L-alpha-amino acidAny L-alpha-amino acid carrying an N-acyl substituent.
isoquinolinesA class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives.
1-benzofuransA member of the class of benzofurans consisting of a 1-benzofuran skeleton and its substituted derivatives thereof.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Integrin beta-2Homo sapiens (human)IC50 (µMol)0.04150.00080.59053.7800AID669545; AID669546
Intercellular adhesion molecule 1Homo sapiens (human)IC50 (µMol)0.02870.00301.212210.0000AID669545; AID669546; AID669552
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)20.00000.00011.753610.0000AID669554
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)3.00000.00002.800510.0000AID669555
Integrin alpha-LHomo sapiens (human)IC50 (µMol)0.04150.00080.60203.7800AID669545; AID669546
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)20.00000.00091.901410.0000AID669556
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (98)

Processvia Protein(s)Taxonomy
microglial cell activationIntegrin beta-2Homo sapiens (human)
receptor-mediated endocytosisIntegrin beta-2Homo sapiens (human)
phagocytosis, engulfmentIntegrin beta-2Homo sapiens (human)
apoptotic processIntegrin beta-2Homo sapiens (human)
inflammatory responseIntegrin beta-2Homo sapiens (human)
cell adhesionIntegrin beta-2Homo sapiens (human)
leukocyte cell-cell adhesionIntegrin beta-2Homo sapiens (human)
cell-matrix adhesionIntegrin beta-2Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-2Homo sapiens (human)
cell-cell signalingIntegrin beta-2Homo sapiens (human)
regulation of cell shapeIntegrin beta-2Homo sapiens (human)
neutrophil chemotaxisIntegrin beta-2Homo sapiens (human)
receptor internalizationIntegrin beta-2Homo sapiens (human)
positive regulation of superoxide anion generationIntegrin beta-2Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-2Homo sapiens (human)
endodermal cell differentiationIntegrin beta-2Homo sapiens (human)
receptor clusteringIntegrin beta-2Homo sapiens (human)
positive regulation of neutrophil degranulationIntegrin beta-2Homo sapiens (human)
negative regulation of dopamine metabolic processIntegrin beta-2Homo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationIntegrin beta-2Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusIntegrin beta-2Homo sapiens (human)
positive regulation of protein targeting to membraneIntegrin beta-2Homo sapiens (human)
amyloid-beta clearanceIntegrin beta-2Homo sapiens (human)
cell-cell adhesionIntegrin beta-2Homo sapiens (human)
cell-cell adhesion via plasma-membrane adhesion moleculesIntegrin beta-2Homo sapiens (human)
positive regulation of leukocyte adhesion to vascular endothelial cellIntegrin beta-2Homo sapiens (human)
neutrophil migrationIntegrin beta-2Homo sapiens (human)
positive regulation of prostaglandin-E synthase activityIntegrin beta-2Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-2Homo sapiens (human)
regulation of leukocyte mediated cytotoxicityIntercellular adhesion molecule 1Homo sapiens (human)
T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cellIntercellular adhesion molecule 1Homo sapiens (human)
T cell antigen processing and presentationIntercellular adhesion molecule 1Homo sapiens (human)
positive regulation of cellular extravasationIntercellular adhesion molecule 1Homo sapiens (human)
cell adhesionIntercellular adhesion molecule 1Homo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion moleculesIntercellular adhesion molecule 1Homo sapiens (human)
leukocyte cell-cell adhesionIntercellular adhesion molecule 1Homo sapiens (human)
membrane to membrane dockingIntercellular adhesion molecule 1Homo sapiens (human)
cell adhesion mediated by integrinIntercellular adhesion molecule 1Homo sapiens (human)
adhesion of symbiont to hostIntercellular adhesion molecule 1Homo sapiens (human)
symbiont entry into host cellIntercellular adhesion molecule 1Homo sapiens (human)
receptor-mediated virion attachment to host cellIntercellular adhesion molecule 1Homo sapiens (human)
leukocyte migrationIntercellular adhesion molecule 1Homo sapiens (human)
establishment of endothelial barrierIntercellular adhesion molecule 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to glucose stimulusIntercellular adhesion molecule 1Homo sapiens (human)
T cell extravasationIntercellular adhesion molecule 1Homo sapiens (human)
regulation of ruffle assemblyIntercellular adhesion molecule 1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to amyloid-betaIntercellular adhesion molecule 1Homo sapiens (human)
cellular response to leukemia inhibitory factorIntercellular adhesion molecule 1Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntercellular adhesion molecule 1Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
T cell activation via T cell receptor contact with antigen bound to MHC molecule on antigen presenting cellIntegrin alpha-LHomo sapiens (human)
phagocytosisIntegrin alpha-LHomo sapiens (human)
inflammatory responseIntegrin alpha-LHomo sapiens (human)
cell adhesionIntegrin alpha-LHomo sapiens (human)
heterophilic cell-cell adhesion via plasma membrane cell adhesion moleculesIntegrin alpha-LHomo sapiens (human)
leukocyte cell-cell adhesionIntegrin alpha-LHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-LHomo sapiens (human)
signal transductionIntegrin alpha-LHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-LHomo sapiens (human)
memory T cell extravasationIntegrin alpha-LHomo sapiens (human)
receptor clusteringIntegrin alpha-LHomo sapiens (human)
cell-cell adhesionIntegrin alpha-LHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-LHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (53)

Processvia Protein(s)Taxonomy
cargo receptor activityIntegrin beta-2Homo sapiens (human)
amyloid-beta bindingIntegrin beta-2Homo sapiens (human)
complement component C3b bindingIntegrin beta-2Homo sapiens (human)
integrin bindingIntegrin beta-2Homo sapiens (human)
protein bindingIntegrin beta-2Homo sapiens (human)
protein kinase bindingIntegrin beta-2Homo sapiens (human)
ICAM-3 receptor activityIntegrin beta-2Homo sapiens (human)
heat shock protein bindingIntegrin beta-2Homo sapiens (human)
metal ion bindingIntegrin beta-2Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-2Homo sapiens (human)
virus receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
transmembrane signaling receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
integrin bindingIntercellular adhesion molecule 1Homo sapiens (human)
protein bindingIntercellular adhesion molecule 1Homo sapiens (human)
signaling receptor activityIntercellular adhesion molecule 1Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
protein bindingIntegrin alpha-LHomo sapiens (human)
ICAM-3 receptor activityIntegrin alpha-LHomo sapiens (human)
metal ion bindingIntegrin alpha-LHomo sapiens (human)
cell adhesion molecule bindingIntegrin alpha-LHomo sapiens (human)
integrin bindingIntegrin alpha-LHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
plasma membraneIntegrin beta-2Homo sapiens (human)
external side of plasma membraneIntegrin beta-2Homo sapiens (human)
cell surfaceIntegrin beta-2Homo sapiens (human)
membraneIntegrin beta-2Homo sapiens (human)
integrin alphaL-beta2 complexIntegrin beta-2Homo sapiens (human)
integrin alphaM-beta2 complexIntegrin beta-2Homo sapiens (human)
integrin alphaX-beta2 complexIntegrin beta-2Homo sapiens (human)
specific granule membraneIntegrin beta-2Homo sapiens (human)
plasma membrane raftIntegrin beta-2Homo sapiens (human)
extracellular exosomeIntegrin beta-2Homo sapiens (human)
tertiary granule membraneIntegrin beta-2Homo sapiens (human)
ficolin-1-rich granule membraneIntegrin beta-2Homo sapiens (human)
extracellular vesicleIntegrin beta-2Homo sapiens (human)
integrin complexIntegrin beta-2Homo sapiens (human)
receptor complexIntegrin beta-2Homo sapiens (human)
focal adhesionIntegrin beta-2Homo sapiens (human)
cell surfaceIntegrin beta-2Homo sapiens (human)
immunological synapseIntercellular adhesion molecule 1Homo sapiens (human)
extracellular spaceIntercellular adhesion molecule 1Homo sapiens (human)
plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
focal adhesionIntercellular adhesion molecule 1Homo sapiens (human)
external side of plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
cell surfaceIntercellular adhesion molecule 1Homo sapiens (human)
membraneIntercellular adhesion molecule 1Homo sapiens (human)
membrane raftIntercellular adhesion molecule 1Homo sapiens (human)
collagen-containing extracellular matrixIntercellular adhesion molecule 1Homo sapiens (human)
extracellular exosomeIntercellular adhesion molecule 1Homo sapiens (human)
plasma membraneIntercellular adhesion molecule 1Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
plasma membraneIntegrin alpha-LHomo sapiens (human)
cell surfaceIntegrin alpha-LHomo sapiens (human)
membraneIntegrin alpha-LHomo sapiens (human)
integrin alphaL-beta2 complexIntegrin alpha-LHomo sapiens (human)
specific granule membraneIntegrin alpha-LHomo sapiens (human)
extracellular exosomeIntegrin alpha-LHomo sapiens (human)
integrin complexIntegrin alpha-LHomo sapiens (human)
external side of plasma membraneIntegrin alpha-LHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID669567Inhibition of ICAM-1-mediated MIP-1alpha release2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669569Inhibition of ICAM-1-mediated IL-1beta release2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669571Inhibition of ICAM-1-mediated IL-10 release2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669564Toxicity in dog administered topically with 1% PBS solution tid for 12 weeks2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669549Half life in Sprague-Dawley rat at 5 mg/kg, iv2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669552Inhibition of human recombinant ICAM-1 adhesion into human Jurkat cells after 1 hr2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669553Genotoxicity in Salmonella typhimurium by Ames test2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669547Metabolic stability in human liver microsomes assessed as compound remaining after 30 mins2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669548Metabolic stability in rat liver microsomes assessed as compound remaining after 30 mins2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669546Antagonist activity at LFA-1/ICAM-1 in human HuT-78 T-cells assessed as inhibition of cell adhesion after 1 hr by p-nitrophenyl n-acetyl-beta-D-glucosaminide method in presence of 10% human serum2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669545Antagonist activity at LFA-1/ICAM-1 in human HuT-78 T-cells assessed as inhibition of cell adhesion after 1 hr by p-nitrophenyl n-acetyl-beta-D-glucosaminide method2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669565Increase of mean schirmer's tear test in dog administered topically with 1% PBS solution tid for 12 weeks measured after 1 to 12 weeks2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669566Inhibition of ICAM-1-mediated IFNgamma release2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669556Inhibition of human ERG2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669570Inhibition of ICAM-1-mediated IL-6 release2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669568Inhibition of ICAM-1-mediated IL-1alpha release2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669554Inhibition of CYP3A42012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669555Inhibition of CYP2C92012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669551AUC in Sprague-Dawley rat at 5 mg/kg, iv2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
AID669550Clearance in Sprague-Dawley rat at 5 mg/kg, iv2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (42)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's24 (57.14)24.3611
2020's18 (42.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 15.86

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

MetricThis Compound (vs All)
Research Demand Index15.86 (24.57)
Research Supply Index3.99 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (15.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (23.26%)5.53%
Reviews10 (23.26%)6.00%
Case Studies1 (2.33%)4.05%
Observational0 (0.00%)0.25%
Other22 (51.16%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]