Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H15ClFN5O5S2 |
Molecular Weight | 523.945 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC1=CC2=C(C=C1F)C(=O)N(C(=O)N2)C3=CC=C(NC(=O)NS(=O)(=O)C4=CC=C(Cl)S4)C=C3
InChI
InChIKey=LGSDFTPAICUONK-UHFFFAOYSA-N
InChI=1S/C20H15ClFN5O5S2/c1-23-15-9-14-12(8-13(15)22)18(28)27(20(30)25-14)11-4-2-10(3-5-11)24-19(29)26-34(31,32)17-7-6-16(21)33-17/h2-9,23H,1H3,(H,25,30)(H2,24,26,29)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/20608816Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800022611 | http://www.wikidoc.org/index.php/Elinogrel
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20608816
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800022611 | http://www.wikidoc.org/index.php/Elinogrel
Elinogrel, previously known as PRT060128 or PRT128, is a direct-acting, reversible P2Y12 inhibitor for both intravenous and oral administration. Elinogrel has been tested in 2 phase II studies for the treatment of acute coronary syndrome, myocardial infarction and prevention of secondary thrombotic events. Elinogrel therapy was associated with an increased incidence of dyspnea and incidence of elevated liver transaminases. The development of the drug was terminated in January 2012 by Novartis.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2001 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20608816 |
23.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Preventing | Unknown Approved UseUnknown |
Doses
Dose | Population | Adverse events |
---|---|---|
150 mg 2 times / day multiple, oral (max) Highest studied dose Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.339, 340 |
unhealthy, ADULT n = 408 Health Status: unhealthy Condition: coronary artery disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 408 Sources: Page: p.339, 340 |
Disc. AE: Dyspnea... AEs leading to discontinuation/dose reduction: Dyspnea (grade 1-2, 1%) Sources: Page: p.339, 340 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dyspnea | grade 1-2, 1% Disc. AE |
150 mg 2 times / day multiple, oral (max) Highest studied dose Dose: 150 mg, 2 times / day Route: oral Route: multiple Dose: 150 mg, 2 times / day Sources: Page: p.339, 340 |
unhealthy, ADULT n = 408 Health Status: unhealthy Condition: coronary artery disease Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 408 Sources: Page: p.339, 340 |
PubMed
Title | Date | PubMed |
---|---|---|
Emerging antiplatelet agents, differential pharmacology, and clinical utility. | 2010 |
|
Pharmacokinetic, pharmacodynamic and clinical profile of novel antiplatelet drugs targeting vascular diseases. | 2010 Feb 1 |
|
New P2Y12 inhibitors versus clopidogrel in percutaneous coronary intervention: a meta-analysis. | 2010 Nov 2 |
|
Newer antithrombotic drugs. | 2010 Oct |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22647518
80-mg intravenous bolus of elinogrel was given immediately before percutaneous coronary intervention, followed by twice-daily oral elinogrel administration of 50, 100, or 150 mg for 60 days
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20608816
When two concentrations of elinogrel (2.5 or 5.0 mmol/l) were added in vitro to the blood of diabetic patients, an anti-thrombotic effect was observed, supporting evidence that elinogrel may overcome the limitation of poor clopidogrel response.
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C80483
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C549473
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16066663
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CHEMBL2103828
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C96896
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UU-95
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m4870
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Elinogrel
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100000144446
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DTXSID50918262
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)