General
Preferred name
TICAGRELOR
Synonyms
AR-C 126532XX ()
AZD6140 ()
Ticagrelor (AZD6140) ()
Brilinta ()
AZD 6140, AR-C 126532XX ()
Ticagrelor-d7 ()
AR-C126532XX ()
POSSIA ()
AZD-6140 ()
Brilique ()
P&D ID
PD009197
CAS
274693-27-5
1265911-55-4
Tags
available
drug
Approved by
FDA
First approval
2011
2010
Drug indication
Thrombosis
Myocardial infarction
Acute coronary syndrome
Arterial thrombosis
Drug Status
approved
withdrawn
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS Plasma concentrations of ticagrelor are higher in the elderly, women, patients of Asian ethnicity, and those with hepatic impairment. Plasma concentrations are decreased in patients with darker skin and those with severe renal impairment. Japenese patients have 40% higher plasma concentrations than Caucasian patients. This difference decreases to 20% when corrections for body weight are made. Ticagrelor has not been tested in severe hepatic impairment.
MOA Ticagrelor is a reversible allosteric antagonist of P2Y12. This prevents ADP binding to the P2Y12 receptor. Because it is not a prodrug, it may be of use to patients who are poor metabolizers as they may not receive as much benefit from a prodrug.
INDICATION Ticagrelor is indicated for the prevention of thrombotic events like stroke or heart attack in patients with acute coronary syndrome or myocardial infarction with ST elevation.
METABOLISM Ticagrelor is de-hydroxyethylated at the 5th position of the cyclopentane ring by CYP3A4 to AR-C124910XX. 30-40% of the drug is metabolised this way.
DESCRIPTION Ticagrelor is a selective P2Y12 receptor antagonist . (GtoPdb)
DESCRIPTION Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.
PRICE 40
DESCRIPTION Positive allosteric modulator of M1 receptors (Tocris Bioactive Compound Library)
DESCRIPTION Ticagrelor is a P2Y12 platelet inhibitor used in patients with a history of myocardial infarction or with acute coronary syndrome (ACS) to prevent future myocardial infarction, stroke and cardiovascular death. (Enamine Bioactive Compounds)
DESCRIPTION Ticagrelor (AR-C 126532XX), produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU). (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
29
AdooQ Bioactive Compound Library
A11238
Axon Medchem Screening Library
3111
Cayman Chemical Bioactives
15425
25027
ChEMBL Approved Drugs
CHEMBL398435
ChEMBL Drugs
CHEMBL398435
Concise Guide to Pharmacology 2017/18
1765
Concise Guide to Pharmacology 2019/20
1765
Concise Guide to Pharmacology 2021/22
1765
Concise Guide to Pharmacology 2023/24
1765
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB08816
DrugBank Approved Drugs
DB08816
DrugCentral
4184
DrugCentral Approved Drugs
4184
DrugMAP
DMBR01X
DrugMAP Approved Drugs
DMBR01X
Enamine Bioactive Compounds
EBC-12279
EU-OPENSCREEN Bioactive Compound Library
EOS100638
EUbOPEN Chemogenomics Library
EUB0000463
Guide to Pharmacology
1765
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL398435
MedChem Express Bioactive Compound Library
HY-10064
NCATS Inxight Approved Drugs
GLH0314RVC
ReFrame library
Selleckchem Bioactive Compound Library
ticagrelor
TargetMol Bioactive Compound Library
T0179
Tocris Bioactive Compound Library
6864
Withdrawn 2.0
EMA44
External IDs
44
Properties
(calculated by RDKit )
Molecular Weight
522.19
Hydrogen Bond Acceptors
11
Hydrogen Bond Donors
4
Rotatable Bonds
10
Ring Count
5
Aromatic Ring Count
3
cLogP
2.01
TPSA
138.44
Fraction CSP3
0.57
Chiral centers
6.0
Largest ring
6.0
QED
0.23
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
CYP2C9
P2Y
P2Y12
P2RY12
P2Y12 antagonist
P2 Receptor
P2Y Receptor
Primary Target
Purinergic (P2Y) Receptors
MOA
Antagonist
purinergic receptor antagonist
Indication
acute coronary syndrome (ACS), myocardial infarction
ATC
B01AC24
Pathway
GPCR/G protein
Metabolism
Neuroscience
Recommended Cell Concentration
None
Source data