Page last updated: 2024-11-08

roxifiban

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

Description

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

Cross-References

ID SourceID
PubMed CID177230
CHEMBL ID18301
SCHEMBL ID344302
MeSH IDM0303115

Synonyms (20)

Synonym
bdbm50075579
(s)-2-butoxycarbonylamino-3-{2-[(r)-3-(4-carbamimidoyl-phenyl)-4,5-dihydro-isoxazol-5-yl]-acetylamino}-propionic acid methyl ester
2-butoxycarbonylamino-3-{2-[3-(4-carbamimidoyl-phenyl)-4,5-dihydro-isoxazol-5-yl]-acetylamino}-propionic acid methyl ester(dmp 754(roxifiban))
roxifiban
CHEMBL18301 ,
methyl (2s)-2-(butoxycarbonylamino)-3-[[2-[(5r)-3-(4-carbamimidoylphenyl)-4,5-dihydro-1,2-oxazol-5-yl]acetyl]amino]propanoate
dmp754
unii-q476fmz72g
l-alanine, 3-(((3-(4-(aminoiminomethyl)phenyl)-4,5-dihydro-5-isoxazolyl)acetyl)amino)-n-(butoxycarbonyl)-, methyl ester, (r)-
l-alanine, 3-((((5r)-3-(4-(aminoiminomethyl)phenyl)-4,5-dihydro-5-isoxazolyl)acetyl)amino)-n-(butoxycarbonyl)-, methyl ester
roxifiban [inn]
170902-47-3
q476fmz72g ,
roxifiban [who-dd]
(2s)-3-(2-((5r)-3-(p-amidinophenyl)-2-isoxazolin-5-yl)acetamido)-2-(carboxyamino)propionic acid, 2-butyl methyl ester
SCHEMBL344302
DTXSID70168969
methyl (s)-2-((butoxycarbonyl)amino)-3-(2-((r)-3-(4-carbamimidoylphenyl)-4,5-dihydroisoxazol-5-yl)acetamido)propanoate
Q27286984
AKOS040746301

Research Excerpts

Overview

Roxifiban (DMP 754) is a glycoprotein (GP) IIb/IIIa antagonist. Roxifiban is an esterprodrug that is hydrolyzed, after oral administration, to XV459.

ExcerptReferenceRelevance
"Roxifiban is an oral prodrug of XV459, a potent and specific inhibitor of the glycoprotein (GP) IIb/IIIa receptor previously under investigation for the treatment of peripheral arterial disease and acute coronary care syndrome. "( Integrated pharmacokinetic/pharmacodynamic model of XV459, a potent and specific GPIIb/IIIa inhibitor, in healthy male volunteers.
Barrett, JS; Ebling, WF; Fossler, MJ; Garner, D; Kornhauser, D; Ma, S; Mondick, J; Pieniaszek, HJ; Quon, CY, 2002
)
1.76
"Roxifiban (DMP 754) is a glycoprotein (GP) IIb/IIIa antagonist. "( Simultaneous quantification of seven active metabolites of roxifiban in human plasma by LC/MS/MS in the presence of an interfering displacer at millimolar concentrations.
Emm, TA; Jiao, Q; Lloyd, TL; Mutlib, A; Pieniaszek, HJ; Shi, G; Sy, SK; Unger, SE; Wernicki, A, 2003
)
2
"Roxifiban is an esterprodrug that is hydrolyzed, after oral administration, to the active glycoprotein (GP) IIb/IIIa antagonist, XV459. "( Safety, tolerability, pharmacokinetics, and time course of pharmacologic response of the active metabolite of roxifiban, XV459, a glycoprotein IIb/IIIa antagonist, following oral administration in healthy volunteers.
Cain, VA; Ebling, W; Fossler, MJ; Kornhauser, DM; Ma, S; Mondick, JT; Pieniaszek, HJ; Sy, SK, 2002
)
1.97

Effects

ExcerptReferenceRelevance
"Roxifiban has pharmacokinetic and pharmacodynamic properties believed to be more favorable than the earlier oral agents."( Effects of glycoprotein IIb/IIIa antagonists on platelet activation: development of a transfer method to mimic peak to trough receptor occupancy.
Billheimer, JT; He, B; Seiffert, D; Spitz, SM; Stern, AM, 2002
)
1.04

Toxicity

ExcerptReferenceRelevance
" This serious adverse event was observed with a frequency of approximately 2% in early clinical trials with the potent, orally bioavailable glycoprotein (GP) IIb/IIIa receptor antagonist roxifiban."( Validation and implementation of drug-dependent antibody assays in clinical trials for safety monitoring of patients dosed with roxifiban, an orally bioavailable glycoprotein IIb/IIIa antagonist.
Barrett, YC; Billheimer, J; Ebling, W; Pieniaszek, H; Seiffert, D, 2007
)
0.74

Pharmacokinetics

ExcerptReferenceRelevance
" Roxifiban has pharmacokinetic and pharmacodynamic properties believed to be more favorable than the earlier oral agents."( Effects of glycoprotein IIb/IIIa antagonists on platelet activation: development of a transfer method to mimic peak to trough receptor occupancy.
Billheimer, JT; He, B; Seiffert, D; Spitz, SM; Stern, AM, 2002
)
1.22

Compound-Compound Interactions

ExcerptReferenceRelevance
" Subtherapeutic doses of tinzaparin combined with abciximab or roxifiban resulted in a distinct synergy that improved anticoagulant and antiplatelet efficacy mediated by TF, fXa, or thrombin."( Comparative efficacy of different low-molecular-weight heparins (LMWHs) and drug interactions with LMWH: implications for management of vascular disorders.
Mousa, SA, 2000
)
0.55

Bioavailability

ExcerptReferenceRelevance
" DMP754 demonstrated oral bioavailability of 20."( Intravenous and oral antithrombotic efficacy of the novel platelet GPIIb/IIIa antagonist roxifiban (DMP754) and its free acid form, XV459.
Kapil, R; Mousa, SA; Mu, DX, 1999
)
0.53
" Because of their predictable pharmacokinetics and bioavailability after subcutaneous administration, LMWHs can be more convenient for outpatient use than UFH."( Comparative efficacy of different low-molecular-weight heparins (LMWHs) and drug interactions with LMWH: implications for management of vascular disorders.
Mousa, SA, 2000
)
0.31
" This serious adverse event was observed with a frequency of approximately 2% in early clinical trials with the potent, orally bioavailable glycoprotein (GP) IIb/IIIa receptor antagonist roxifiban."( Validation and implementation of drug-dependent antibody assays in clinical trials for safety monitoring of patients dosed with roxifiban, an orally bioavailable glycoprotein IIb/IIIa antagonist.
Barrett, YC; Billheimer, J; Ebling, W; Pieniaszek, H; Seiffert, D, 2007
)
0.74

Dosage Studied

Roxifiban (DMP754) is a novel oral platelet GP IIb/IIIa receptor inhibitor. The clinical qualifications of the two assays were conducted in two phase II clinical trials in coronary arterial disease (CAD) patients dosed with roxifiban.

ExcerptRelevanceReference
" Isoxazolylsulfonamide 34b (DMP 802), a highly selective GPIIb/IIIa antagonist, demonstrated a prolonged duration of action after iv and po dosing and high affinity for resting and activated platelets."( Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
Anderson, PS; Batt, DG; Di Meo, SV; Frietze, WE; Hausner, EA; Houghton, GC; Kapil, RP; Lalka, GK; Liu, J; Mousa, SA; Olson, RE; Orwat, MJ; Pinto, DJ; Rabel, SR; Racanelli, AL; Reilly, TM; Sielecki, TM; Thoolen, MJ; Tobin, AE; Wexler, RR; Wityak, J, 1999
)
0.3
" The method involved weighing of the sample, disintegration of the dosage form by homogenization, extraction of the analyte in the homogenate solution, filtration of the homogenate, dilution of the filtrate and transfer to autosampler vials."( Automated sample preparation of Roxifiban tablets: transfer of a manual method to an automated workstation.
Lloyd, DK; Reilly, K; Shamrock, WF, 2000
)
0.59
" Initial LC/MS identification of metabolites was achieved by dosing the rat with an equimolar mixture of d0:d4 roxifiban and detecting isotopic clusters of pseudomolecular ions."( Mass spectrometric and NMR characterization of metabolites of roxifiban, a potent and selective antagonist of the platelet glycoprotein IIb/IIIa receptor.
Christ, DD; Diamond, S; Gan, L; Mutlib, AE; Nemeth, G; Shockcor, J; Way, R, 2000
)
0.76
" Measurable plasma concentrations of XV459 appeared rapidly and were sustained throughout the dosing interval of 24 hours."( Safety, tolerability, pharmacokinetics, and time course of pharmacologic response of the active metabolite of roxifiban, XV459, a glycoprotein IIb/IIIa antagonist, following oral administration in healthy volunteers.
Cain, VA; Ebling, W; Fossler, MJ; Kornhauser, DM; Ma, S; Mondick, JT; Pieniaszek, HJ; Sy, SK, 2002
)
0.53
" Form II is the thermodynamically stable crystal form over the practical range of drug substance storage and handling and dosage form processing and storage."( Polymorphism of roxifiban.
Campbell, GC; Everlof, JG; Foris, CM; Maurin, MB; Nemeth, GA; Rabel, SR; Rowe, SM; Vickery, RD, 2002
)
0.66
" Nevertheless, none of these fibans was able to effectively block shear-induced platelet adhesion at targeted clinical dosing regimens except for abciximab."( Comparative analysis of various platelet glycoprotein IIb/IIIa antagonists on shear-induced platelet activation and adhesion.
Barbera, FA; Dorsam, RT; Feuerstein, GZ; Friedman, SM; Gibbs, S; Lauver, A; Savion, N; Varon, D; Wang, H; Wang, X, 2002
)
0.31
" Site occupancy studies combined with clot retraction experiments addressed whether high affinity and slow off-rate compounds can alter clot retraction during the dosing interval."( Regulation of clot retraction by glycoprotein IIb/IIIa antagonists.
Billheimer, JT; He, B; Kieras, CJ; Pedicord, DL; Seiffert, D; Stern, AM, 2002
)
0.31
" Whole blood was collected at pre-dose and during the dosing interval directly into citrate fixative so that circulating levels of platelet activation could be assessed."( Effects of the glycoprotein IIb/IIIa antagonist Roxifiban on P-selectin expression, fibrinogen binding, and microaggregate formation in a phase I dose-finding study: no evidence for platelet activation during treatment with a glycoprotein IIb/IIIa antagon
Bradley, JD; Cain, VA; Feuerstein, GZ; Hua, TA; Kornhauser, DM; Martin, DE; Munzer, DA; Seiffert, D; Stern, AM; Tchinnes, MA; Thomas, BE, 2003
)
0.57
" This study examined the dose-response effect on inhibition of platelet aggregation by roxifiban (DMP754), a novel oral platelet GP IIb/IIIa receptor inhibitor, and its safety and tolerability in patients with a history of chronic stable angina pectoris."( The use of roxifiban (DMP754), a novel oral platelet glycoprotein IIb/IIIa receptor inhibitor, in patients with stable coronary artery disease.
Cain, VA; Daly, RN; Ebling, W; Gussak, I; Kopecky, SL; Murphy, J; Pieniaszek, HJ; Simonson, K; Sy, SK; Wilcox, RA; Williams, B; Wright, RS, 2003
)
0.93
" In the present investigation, the effect of roxifiban (class I) on ex vivo clot dynamics using recalcified blood was tested in normal, healthy volunteers (n = 7) dosed with 1 mg BID roxifiban for 9 days."( Using thrombelastography to determine the efficacy of the platelet glycoprotein IIb/IIIa antagonist, roxifiban, on platelet/fibrin-mediated clot dynamics in humans.
Bozarth, JM; Feuerstein, GZ; Mousa, SA; Seiffert, D, 2005
)
0.8
" The clinical qualifications of the two assays were conducted in two phase II clinical trials in coronary arterial disease (CAD) patients dosed with roxifiban."( Validation and implementation of drug-dependent antibody assays in clinical trials for safety monitoring of patients dosed with roxifiban, an orally bioavailable glycoprotein IIb/IIIa antagonist.
Barrett, YC; Billheimer, J; Ebling, W; Pieniaszek, H; Seiffert, D, 2007
)
0.74
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Integrin beta-3Homo sapiens (human)IC50 (µMol)0.06000.00010.632310.0000AID222642
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)0.06000.00052.773925.1700AID222642
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)0.06000.00052.891925.1700AID222642
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)0.06000.00052.747825.1700AID222642
Integrin alpha-IIbHomo sapiens (human)IC50 (µMol)0.06000.00010.730910.0000AID222642
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)0.06000.00052.780225.1700AID222642
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)0.06000.00053.314249.5000AID222642
[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)
Integrin beta-3Homo sapiens (human)Kd0.00260.00010.11780.6500AID72995; AID72997
Integrin alpha-IIbHomo sapiens (human)Kd0.00260.00010.12430.6500AID72995; AID72997
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (70)

Processvia Protein(s)Taxonomy
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID160951Concentration required for maximal in vitro inhibition of aggregation of human platelet rich plasma (hPRP)2001Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16
Synthesis and pharmacology of modified amidine isoxazoline glycoprotein IIb/IIIa receptor antagonists.
AID222642Inhibition of human platelet aggregation2000Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19
Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
AID72995Dissociation constant for activated Fibrinogen Receptor1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
AID60399Inhibition ex vivo platelet aggregation by the compound in dogs after 1 hr of administration of iv bolus dose of 0.3 mg/kg1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
AID60400Inhibition ex vivo platelet aggregation by the compound in dogs after 24 hr of administration of iv bolus dose of 0.3 mg/kg1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
AID60401Inhibition ex vivo platelet aggregation by the compound in dogs after 5 hr of administration of iv bolus dose of 0.025 mg/kg1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
AID60531Inhibition of ex vivo platelet aggregation by the compound in dogs after 1 hr of administration of iv bolus dose of 0.025 mg/kg1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
AID72997Dissociation constant for unactivated Fibrinogen Receptor1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
AID158068The compounds were tested for their ability to inhibit ADP-stimulated platelet aggregation in dog platelet rich plasma1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
AID158251The compound was tested against free acid of DMP 754 to inhibit ADP-stimulated platelet aggregation in human platelet rich plasma1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
AID60526Inhibition ex vivo platelet aggregation by the compound in dogs after 6 hr of administration of iv bolus dose of 0.3 mg/kg1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (40)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (12.50)18.2507
2000's34 (85.00)29.6817
2010's0 (0.00)24.3611
2020's1 (2.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.21

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 Index21.21 (24.57)
Research Supply Index3.87 (2.92)
Research Growth Index4.50 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (17.50%)5.53%
Reviews1 (2.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other32 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]