Page last updated: 2024-12-06

xemilofiban

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

Description

Xemilofiban is a non-peptide, orally active, potent and selective antagonist of the platelet glycoprotein IIb/IIIa receptor. It is an inhibitor of platelet aggregation and has been studied for its potential use in the treatment of acute coronary syndromes, including unstable angina and non-ST-segment elevation myocardial infarction. The mechanism of action of xemilofiban is based on its ability to block the binding of fibrinogen to the glycoprotein IIb/IIIa receptor on platelets, preventing platelet aggregation. Xemilofiban has shown promising results in clinical trials, demonstrating its effectiveness in reducing the risk of ischemic events. However, its use has been limited by the development of bleeding complications. Synthesis of Xemilofiban involves a multi-step process that includes the use of chiral building blocks. Xemilofiban has been studied extensively for its effects on platelet aggregation and its potential therapeutic benefits in the treatment of cardiovascular diseases. The development of xemilofiban as a drug has been driven by the need for effective treatments for acute coronary syndromes and the desire to reduce the incidence of ischemic events. It is a potent inhibitor of platelet aggregation and has the potential to be a valuable tool in the management of cardiovascular diseases.'

xemilofiban: SC-54684A was administered as the hydrochloride salt; inhibits platelet glycoprotein GPIIB IIIA receptor; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60957
CHEMBL ID76098
SCHEMBL ID50663
MeSH IDM0241122

Synonyms (21)

Synonym
CHEMBL76098 ,
sc-54684 ,
cs-551
xemilofiban
ethyl-3s-((4-((4-(aminoiminomethyl)phenyl)amino)-1,4-dioxobutyl)amino)-4-pentynoate
4-pentynoic acid, 3-((4-((4-(aminoiminomethyl)phenyl)amino)-1,4-dioxobutyl)amino)-, ethyl ester, (s)-
xemilofiban [inn]
bdbm50083460
3-[3-(4-carbamimidoyl-phenylcarbamoyl)-propionylamino]-pent-4-ynoic acid ethyl ester (sc-54684a (xemilofiban))
(s)-3-[3-(4-carbamimidoyl-phenylcarbamoyl)-propionylamino]-pent-4-ynoic acid ethyl ester
ethyl (3s)-3-[[4-(4-carbamimidoylanilino)-4-oxobutanoyl]amino]pent-4-ynoate
p614ji3iyk ,
unii-p614ji3iyk
149820-74-6
SCHEMBL50663
xemilofiban [mi]
sc54684
xemilofiban [who-dd]
DTXSID60164410
Q27286268
AKOS040754446

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacodynamic efficacy, clinical safety, and outcomes after prolonged receptor blockade with an orally active GP IIb/IIIa antagonist are not known."( Pharmacodynamic efficacy, clinical safety, and outcomes after prolonged platelet Glycoprotein IIb/IIIa receptor blockade with oral xemilofiban: results of a multicenter, placebo-controlled, randomized trial.
Abbottsmith, CW; Anders, RJ; Anderson, LC; Broderick, TM; Bryzinski, B; Dreiling, RJ; Ferguson, JJ; Hantsbarger, GL; Kereiakes, DJ; Kleiman, NS; Masud, AR; Runyon, JP; Topol, EJ, 1998
)
0.5

Bioavailability

ExcerptReferenceRelevance
"SC-54684A, an orally active antiplatelet drug now in clinical trial, is shown to be a potent, specific fibrinogen binding inhibitor that blocks platelet aggregation to a wide variety of known stimuli and has good bioavailability in animals."( SC-54684A: an orally active inhibitor of platelet aggregation.
Broschat, K; Haas, NF; Keller, BT; King, LW; Nicholson, NS; Panzer-Knodle, SG; Salyers, AK; Szalony, JA; Taite, BB; Zablocki, JA, 1995
)
0.29

Dosage Studied

VDDI Pharmaceuticals plans to develop xemilofiban in cardiovascular disorders. A restructured dosing schedule and narrowed patient selection will be used.

ExcerptRelevanceReference
" Four ester prodrug/acid active metabolite pairs (2a/2e, 60a/60e, 62a/62e, 63a/63e) from the ABAS series which varied in their 3-substituent on the beta-amino ester "aspartate mimetic" were prepared in enantiomerically enriched form (> 95:5), and they were evaluated in canine studies for their ability to block collagen-induced aggregation in platelet-rich plasma, the elimination profile (t1/2 beta-phase), repeated oral dosing studies, and oral systemic availability."( Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
Bovy, PR; Garland, RB; Lindmark, RJ; Rao, SA; Rico, JG; Rogers, TE; Schretzman, LA; Tjoeng, FS; Williams, K; Zablocki, JA, 1995
)
0.29
" A significant dose-response relationship to xemilofiban was observed."( Differential dose-response to oral xemilofiban after antecedent intravenous abciximab. Administration for complex coronary intervention.
Anders, RJ; Anderson, LC; Hantsbarger, G; Higby, NA; Kereiakes, DJ; Kleiman, NS; McDonald, S; Runyon, JP, 1996
)
0.83
" Patients who received abciximab during the coronary intervention and who were randomized to receive xemilofiban were administered a reduced dosage (10 mg TID for 2 weeks) followed by the randomized maintenance dose of 15 or 20 mg BID for 2 more weeks."( Pharmacodynamic efficacy, clinical safety, and outcomes after prolonged platelet Glycoprotein IIb/IIIa receptor blockade with oral xemilofiban: results of a multicenter, placebo-controlled, randomized trial.
Abbottsmith, CW; Anders, RJ; Anderson, LC; Broderick, TM; Bryzinski, B; Dreiling, RJ; Ferguson, JJ; Hantsbarger, GL; Kereiakes, DJ; Kleiman, NS; Masud, AR; Runyon, JP; Topol, EJ, 1998
)
0.72
" In patients treated with xemilofiban, Mab1 binding was unaltered but Mab2 binding decreased from 37 930+/-2061 sites per platelet at baseline to 8318+/-870 sites per platelet 6 hours after dosing (P<0."( Quantifying GPIIb/IIIa receptor binding using 2 monoclonal antibodies: discriminating abciximab and small molecular weight antagonists.
Cox, D; Deering, A; Fitzgerald, D; Foley, B; Quinn, M; Stewart, M, 1999
)
0.6
" Depending on the degree of the precipitation, which was dosage dependent, and the location, which differed somewhat between the two compounds, the lesions varied from acute obstruction with tubule cell necrosis, nephron dilation, and sudden death with no inflammation to severe chronic pyogranulomatous inflammation."( Lesions and identification of crystalline precipitates of glycoprotein IIb-IIIa antagonists in the rat kidney.
Cortez, E; Fouant, M; Friedman, RM; Hribar, J; Khan, N; Levin, S; Nicholas, M; Schlessinger, S,
)
0.13
" However, inhibition of platelet aggregation was low (between 24 and 45%) before dosing on days 60 and 180."( Glycoprotein IIb/IIIa receptor number and occupancy during chronic administration of an oral antagonist.
Cox, D; Fitzgerald, DJ; Foley, JB; Quinn, MJ, 2000
)
0.31
" Oral GP IIb/IIIa inhibitors have been associated with an increased incidence of bleeding, but additional experience may permit the design of dosing regimens that decrease this risk."( Learning from the recently completed oral glycoprotein IIb/IIIa receptor antagonist trials.
Cannon, CP, 2000
)
0.31
" VDDI Pharmaceuticals plans to develop xemilofiban in cardiovascular disorders following on from the phase III studies completed by Pharmacia; a restructured dosing schedule and narrowed patient selection will be used."( Xemilofiban: SC 54684A, xemlofiban.
, 2003
)
2.03
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Integrin beta-3Homo sapiens (human)IC50 (µMol)0.00200.00010.632310.0000AID73015
Integrin alpha-IIbHomo sapiens (human)IC50 (µMol)0.00200.00010.730910.0000AID73015
[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 (16)

Assay IDTitleYearJournalArticle
AID58792Ex vivo duration of inhibition of ADP-induced canine platelet aggregation by 3 mg/kg.1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.
AID10474Area under curve of acid 2a was determined by HPLC at a dosage of 54.5 mg/kg administered intragastrically by gavage method in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID20853Oral systematic bioavailability was determined by the ratio of AUC's of compound administered intragastrically to that ofcompound 2a administered intravenously in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID20851Oral systematic bioavailability was determined by the ratio of AUC's of compound administered intragastrically to that of administered intravenously in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID13552Area under curve of acid 2a was determined by HPLC at a dosage of 5.45 mg/kg administered intragastrically by capsule method in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID13551Area under curve of acid 2a was determined by HPLC at a dosage of 2.27 mg/kg administered intravenously by bolus method in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID640615Clearance in human liver microsomes at 1 uM measured after 60 mins by HPLC analysis2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Capture hydrolysis signals in the microsomal stability assay: molecular mechanisms of the alkyl ester drug and prodrug metabolism.
AID20852Oral systematic bioavailability was determined by the ratio of AUC's of compound administered intragastrically to that of compound 2a administered intravenously in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID24275Beta-phase half-life was reported, after administration of 2.5 mg/kg intravenously in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID24274Beta-phase half-life was reported, after administration of 2.27 mg/kg intravenously in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID58965Duration of action to obtain >20% ex vivo collagen induced platelet aggregation was reported, after 10 mg/kg (post-ig) into dogs.1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID92991In vitro inhibitory potency against human gel filtered platelet (GFP) aggregation1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.
AID73015In vitro inhibition of biotinylated fibrinogen binding to immobilized fibrinogen receptor.1999Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.
AID13553Area under curve of acid 2a was determined by HPLC at a dosage of 5.45 mg/kg administered intragastrically by gavage method in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
AID18185Oral bioavailability in dog2000Journal 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.
AID13554Area under curve of acid 2a was determined by HPLC at a dosage of 54.5 mg/kg administered intragastrically by capsule method in dog1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (39)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's20 (51.28)18.2507
2000's18 (46.15)29.6817
2010's1 (2.56)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.76

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 Index17.76 (24.57)
Research Supply Index3.97 (2.92)
Research Growth Index4.10 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (23.81%)5.53%
Reviews18 (42.86%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (33.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]