Drug General Information
Drug ID
D0PU8T
Former ID
DNCL001872
Drug Name
E5555
Synonyms
Atopaxar
Drug Type
Small molecular drug
Indication Acute coronary syndrome [ICD9: 444; ICD10:I74] Phase 2 [522232], [540648]
Company
Eisai
Structure
Download
2D MOL

3D MOL

Formula
C29H38FN3O5
InChI
InChI=1S/C29H38FN3O5/c1-7-37-23-15-19-16-33(28(31)24(19)25(30)27(23)38-8-2)17-22(34)18-13-20(29(3,4)5)26(35-6)21(14-18)32-9-11-36-12-10-32/h13-15,31H,7-12,16-17H2,1-6H3
InChIKey
QWKAUGRRIXBIPO-UHFFFAOYSA-N
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) Thrombin receptor Target Info Antagonist [531439], [531931]
KEGG Pathway Rap1 signaling pathway
Calcium signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Endocytosis
PI3K-Akt signaling pathway
Complement and coagulation cascades
Platelet activation
Regulation of actin cytoskeleton
Pathways in cancer
NetPath Pathway TGF_beta_Receptor Signaling Pathway
TCR Signaling Pathway
PANTHER Pathway Angiogenesis
Blood coagulation
Pathway Interaction Database PAR1-mediated thrombin signaling events
Reactome Common Pathway of Fibrin Clot Formation
Peptide ligand-binding receptors
G alpha (q) signalling events
Thrombin signalling through proteinase activated receptors (PARs)
WikiPathways Complement and Coagulation Cascades
Regulation of Actin Cytoskeleton
GPCRs, Class A Rhodopsin-like
IL1 and megakaryotyces in obesity
Apoptosis-related network due to altered Notch3 in ovarian cancer
Hematopoietic Stem Cell Differentiation
Gastrin-CREB signalling pathway via PKC and MAPK
Thrombin signalling through proteinase activated receptors (PARs)
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 522232ClinicalTrials.gov (NCT00619164) A Double-Blind Study of E5555 in Japanese Patients With Acute Coronary Syndrome. U.S. National Institutes of Health.
Ref 540648(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4048).
Ref 531439Safety and tolerability of atopaxar in the treatment of patients with acute coronary syndromes: the lessons from antagonizing the cellular effects of Thrombin-Acute Coronary Syndromes Trial. Circulation. 2011 May 3;123(17):1843-53.
Ref 531931Atopaxar and its effects on markers of platelet activation and inflammation: results from the LANCELOT CAD program. J Thromb Thrombolysis. 2012 Jul;34(1):36-43.

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