Page last updated: 2024-11-12

elinogrel

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

Description

elinogrel: a P2Y12 inhibitor and platelet aggregation inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16066663
CHEMBL ID2103828
SCHEMBL ID160663
MeSH IDM0546630

Synonyms (29)

Synonym
prt-060128
936500-94-6
D09607
elinogrel (usan/inn)
prt060128
prt 060128
915y8e749j ,
unii-915y8e749j
elinogrel [usan:inn]
elinogrel
CHEMBL2103828
bdbm50397204
SCHEMBL160663
elinogrel [usan]
elinogrel [who-dd]
2-thiophenesulfonamide, 5-chloro-n-(((4-(6-fluoro-1,4-dihydro-7-(methylamino)-2,4-dioxo-3(2h)-quinazolinyl)phenyl)amino)carbonyl)-
elinogrel [mi]
5-chloro-n-((4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,4-dihydroquinazolin-3(2h)-yl)phenyl)carbamoyl)thiophene-2-sulfonamide ,
elinogrel [inn]
AKOS025142086
NCGC00387478-01
1-(5-chlorothiophen-2-yl)sulfonyl-3-[4-[6-fluoro-7-(methylamino)-2,4-dioxo-1h-quinazolin-3-yl]phenyl]urea
DTXSID50918262
FT-0724857
DB06350
Q15408411
HY-11021
CS-0002993
MS-29701

Research Excerpts

Overview

Elinogrel (PRT060128) is a reversible, potent and competitive inhibitor of the P2Y(12) receptor. It can be administered by both oral and intravenous routes and rapidly achieves near complete platelet inhibition.

ExcerptReferenceRelevance
"Elinogrel is a potent, direct-acting (ie, non-prodrug), selective, competitive, and reversible P2Y(12) inhibitor available in both intravenous and oral formulations."( Rationale and design of the randomized, double-blind trial testing INtraveNous and Oral administration of elinogrel, a selective and reversible P2Y(12)-receptor inhibitor, versus clopidogrel to eVAluate Tolerability and Efficacy in nonurgent Percutaneous
Bhatt, DL; Gibson, CM; Gretler, DD; Harrington, RA; Huber, K; Kochman, J; Leonardi, S; Madan, M; McClure, MW; Paynter, GE; Rao, SV; Roe, MT; Thompson, V; Welsh, RC; Zeymer, U, 2010
)
1.3
"Elinogrel (PRT060128) is a reversible, potent and competitive inhibitor of the P2Y(12) receptor with a fast onset and offset of action that can be administered by both oral and intravenous routes and rapidly achieves near complete platelet inhibition."( Elinogrel: pharmacological principles, preclinical and early phase clinical testing.
Angiolillo, DJ; Rao, SV; Ueno, M, 2010
)
2.52
"Elinogrel is a novel competitive, reversible ADP-receptor antagonist available in oral and intravenous formulation."( Elinogrel, an orally and intravenously available ADP-receptor antagonist. How does elinogrel affect a personalized antiplatelet therapy?
Gawaz, M; Geisler, T; Müller, KA, 2012
)
2.54

Pharmacokinetics

ExcerptReferenceRelevance
"This substudy of the Intravenous and Oral Administration of Elinogrel to Evaluate Tolerability and Efficacy in Nonurgent Percutaneous Coronary Intervention patients (INNOVATE-PCI) trial evaluated the pharmacokinetic and pharmacodynamic effects of two dosing regimens of IV followed by oral elinogrel (120 mg IV plus 100 mg oral twice daily; 120 mg IV plus 150 mg oral twice daily) versus standard clopidogrel therapy (300-600 mg oral loading dose plus 75 mg oral maintenance dose) in 56 patients undergoing nonurgent PCI."( Pharmacokinetic and pharmacodynamic effects of elinogrel: results of the platelet function substudy from the intravenous and oral administration of elinogrel to evaluate tolerability and efficacy in nonurgent percutaneous coronary intervention patients (I
Angiolillo, DJ; Broderick, S; Buerke, M; Conley, PB; Dabrowski, M; Gurbel, PA; Harrington, RA; Jennings, LK; Kochman, J; McClure, MW; Neumann, FJ; Rao, SV; Saucedo, JF; Stephens, G; Stumpf, J; Trenk, D; Welsh, RC; Wójcik, J, 2012
)
0.88

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

IV and oral elinogrel achieves more rapid and enhanced antiplatelet effects. These were not significant during chronic dosing in this pilot investigation.

ExcerptRelevanceReference
"This substudy of the Intravenous and Oral Administration of Elinogrel to Evaluate Tolerability and Efficacy in Nonurgent Percutaneous Coronary Intervention patients (INNOVATE-PCI) trial evaluated the pharmacokinetic and pharmacodynamic effects of two dosing regimens of IV followed by oral elinogrel (120 mg IV plus 100 mg oral twice daily; 120 mg IV plus 150 mg oral twice daily) versus standard clopidogrel therapy (300-600 mg oral loading dose plus 75 mg oral maintenance dose) in 56 patients undergoing nonurgent PCI."( Pharmacokinetic and pharmacodynamic effects of elinogrel: results of the platelet function substudy from the intravenous and oral administration of elinogrel to evaluate tolerability and efficacy in nonurgent percutaneous coronary intervention patients (I
Angiolillo, DJ; Broderick, S; Buerke, M; Conley, PB; Dabrowski, M; Gurbel, PA; Harrington, RA; Jennings, LK; Kochman, J; McClure, MW; Neumann, FJ; Rao, SV; Saucedo, JF; Stephens, G; Stumpf, J; Trenk, D; Welsh, RC; Wójcik, J, 2012
)
0.88
"Compared with clopidogrel, the combination of IV and oral elinogrel achieves more rapid and enhanced antiplatelet effects that were sustained through the transition to oral elinogrel in the peri-PCI period, but these were not significant during chronic dosing in this pilot investigation."( Pharmacokinetic and pharmacodynamic effects of elinogrel: results of the platelet function substudy from the intravenous and oral administration of elinogrel to evaluate tolerability and efficacy in nonurgent percutaneous coronary intervention patients (I
Angiolillo, DJ; Broderick, S; Buerke, M; Conley, PB; Dabrowski, M; Gurbel, PA; Harrington, RA; Jennings, LK; Kochman, J; McClure, MW; Neumann, FJ; Rao, SV; Saucedo, JF; Stephens, G; Stumpf, J; Trenk, D; Welsh, RC; Wójcik, J, 2012
)
0.88
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency18.99910.01237.983543.2770AID1645841
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
P2Y purinoceptor 12Homo sapiens (human)IC50 (µMol)3.35330.00041.048910.0000AID1298774; AID1298779; AID1871501
P2Y purinoceptor 12Homo sapiens (human)Ki0.02300.00202.82209.8300AID1850680; AID703441
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (27)

Processvia Protein(s)Taxonomy
G protein-coupled adenosine receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
monoatomic ion transportP2Y purinoceptor 12Homo sapiens (human)
substrate-dependent cell migration, cell extensionP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
hemostasisP2Y purinoceptor 12Homo sapiens (human)
calcium-mediated signalingP2Y purinoceptor 12Homo sapiens (human)
cerebral cortex radial glia-guided migrationP2Y purinoceptor 12Homo sapiens (human)
cell projection organizationP2Y purinoceptor 12Homo sapiens (human)
lamellipodium assemblyP2Y purinoceptor 12Homo sapiens (human)
platelet activationP2Y purinoceptor 12Homo sapiens (human)
positive regulation of integrin activation by cell surface receptor linked signal transductionP2Y purinoceptor 12Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
positive regulation of monoatomic ion transportP2Y purinoceptor 12Homo sapiens (human)
response to axon injuryP2Y purinoceptor 12Homo sapiens (human)
regulation of chemotaxisP2Y purinoceptor 12Homo sapiens (human)
positive regulation of chemotaxisP2Y purinoceptor 12Homo sapiens (human)
establishment of localization in cellP2Y purinoceptor 12Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionP2Y purinoceptor 12Homo sapiens (human)
platelet aggregationP2Y purinoceptor 12Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 12Homo sapiens (human)
visual system developmentP2Y purinoceptor 12Homo sapiens (human)
positive regulation of ruffle assemblyP2Y purinoceptor 12Homo sapiens (human)
regulation of microglial cell migrationP2Y purinoceptor 12Homo sapiens (human)
positive regulation of microglial cell migrationP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
G protein-coupled adenosine receptor activityP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled ADP receptor activityP2Y purinoceptor 12Homo sapiens (human)
guanyl-nucleotide exchange factor activityP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membraneP2Y purinoceptor 12Homo sapiens (human)
cell surfaceP2Y purinoceptor 12Homo sapiens (human)
membraneP2Y purinoceptor 12Homo sapiens (human)
cell projection membraneP2Y purinoceptor 12Homo sapiens (human)
cell body membraneP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1871503Antiplatelet activity in human assessed as inhibition of ADP-induced platelet aggregation at 100 mg, po after 4 hrs
AID1871502Half life in human plasma
AID1298779Displacement of [3H]-2-Mes-ADP from human P2Y12 receptor in platelets by scintillation counter2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
State of affairs: Design and structure-activity relationships of reversible P2Y12 receptor antagonists.
AID1298774Antagonist activity at P2Y12 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation by microplate reader analysis2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
State of affairs: Design and structure-activity relationships of reversible P2Y12 receptor antagonists.
AID1850680Binding affinity to P2Y12 (unknown origin) assessed as inhibition constant2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Strategies for targeting the P2Y
AID703442Inhibition of ADP-stimulated platelet aggregation in human platelet rich plasma by 96-well format based turbidimetric method2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.
AID1871500Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation
AID703441Displacement of [33P]2-MeS-ADP from human recombinant P2Y12 receptor expressed in CHO cell membranes by scintillation counting method2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.
AID1871501Displacement of [3H]2MeSADP from human P2Y12 preincubated for 5 mins followed by [3H]2MeSADP addition and measured after 15 mins by scintillation counting method
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's30 (88.24)24.3611
2020's4 (11.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.23

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 Index27.23 (24.57)
Research Supply Index3.69 (2.92)
Research Growth Index5.13 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (11.43%)5.53%
Reviews18 (51.43%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (37.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]