DGIdb - TICAGRELOR Drug Record

TICAGRELOR chembl:CHEMBL398435 Approved

Alternate Names:

AR-C126532XX
TICAGRELOR
BRILINTA
AZD-6140
BRILIQUE
BRILIQUE®
AZD 6140
AZD6140
(1S,2S,3R,5S)-3-(7-((1R,2S)-2-(3,4-DIFLUOROPHENYL)CYCLOPROPYLAMINO)-5-(PROPYLTHIO)-3H-(1,2,3)TRIAZOLO(4,5-D)PYRIMIDIN-3-YL)-5-(2-HYDROXYETHOXY)CYCLOPENTANE-1,2-DIOL
BRILINTA®
chemidplus:274693-27-5
drugbank:08816
rxcui:1116632
pubchem.compound:9871419
chembl:CHEMBL398435

Drug Info:

FDA Approval	approved
Drug Class	small molecule
Drug Indications	antithrombotic

(2 More Sources)

Publications:

Varenhorst C et al., 2015, Effect of genetic variations on ticagrelor plasma levels and clinical outcomes., Eur Heart J
Storey et al., 2007, Inhibition of platelet aggregation by AZD6140, a reversible oral P2Y12 receptor antagonist, compared with clopidogrel in patients with acute coronary syndromes., J. Am. Coll. Cardiol.
Springthorpe et al., 2007, From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis., Bioorg. Med. Chem. Lett.
Chan NC et al., 2014, Role of phenotypic and genetic testing in managing clopidogrel therapy., Blood
Teng R, 2015, Ticagrelor: Pharmacokinetic, Pharmacodynamic and Pharmacogenetic Profile: An Update., Clin Pharmacokinet
Malhotra N et al., 2015, A pharmacodynamic comparison of a personalized strategy for anti-platelet therapy versus ticagrelor in achieving a therapeutic window., Int J Cardiol
Li M et al., 2017, Association of PEAR1 rs12041331 polymorphism and pharmacodynamics of ticagrelor in healthy Chinese volunteers., Xenobiotica

TICAGRELOR PEAR1

Interaction Score: 3.99

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27937053

Sources:
PharmGKB

TICAGRELOR P2RY12

Interaction Score: 3.54

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Binding data obtained using washed platelets in 96-well plates, with [<sup>125</sup>I]-P2Y<sub>12</sub> antagonist as radioligand.

Direct Interaction? True

Endogenous Drug? False

PMIDs:
17980251 17827008 24951432 26063049

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

TICAGRELOR CYP3A43

Interaction Score: 2.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25935875

Sources:
PharmGKB
TICAGRELOR UGT2B7

Interaction Score: 0.76

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25935875

Sources:
PharmGKB
TICAGRELOR SLC29A1

Interaction Score: 0.57

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
TICAGRELOR SLCO1B1

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25935875

Sources:
PharmGKB
TICAGRELOR CYP2C19

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26151596

Sources:
PharmGKB FDA
TICAGRELOR CYP3A4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25935875

Sources:
PharmGKB

TdgClinicalTrial: TICAGRELOR
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antithrombotic

Drug Class small molecule

FDA Approval approved

Publications:

PharmGKB: ticagrelor

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Varenhorst C et al., 2015, Effect of genetic variations on ticagrelor plasma levels and clinical outcomes., Eur Heart J

Chan NC et al., 2014, Role of phenotypic and genetic testing in managing clopidogrel therapy., Blood

Malhotra N et al., 2015, A pharmacodynamic comparison of a personalized strategy for anti-platelet therapy versus ticagrelor in achieving a therapeutic window., Int J Cardiol

GuideToPharmacology: 135649975
- Version: 29-September-2020
Alternate Names:

TICAGRELOR GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL398435
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL398435
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
FDA: Ticagrelor
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Details of the Assay for Interaction	Binding data obtained using washed platelets in 96-well plates, with [<sup>125</sup>I]-P2Y<sub>12</sub> antagonist as radioligand.
Direct Interaction?	True
Endogenous Drug?	False

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

TICAGRELOR Drug Record

TICAGRELOR chembl:CHEMBL398435 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27937053

Sources: PharmGKB

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Binding data obtained using washed platelets in 96-well plates, with [<sup>125</sup>I]-P2Y<sub>12</sub> antagonist as radioligand. Direct Interaction? True Endogenous Drug? False

PMIDs: 17980251 17827008 24951432 26063049

Sources: TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25935875

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25935875

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25935875

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26151596

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25935875

Sources: PharmGKB

TdgClinicalTrial: TICAGRELOR

Alternate Names:

Drug Info: Drug Indications antithrombotic Drug Class small molecule FDA Approval approved

Publications:

PharmGKB: ticagrelor

Alternate Names:

Drug Info:

GuideToPharmacology: 135649975

Alternate Names: TICAGRELOR GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL398435

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL398435

Alternate Names:

Drug Info:

Publications:

FDA: Ticagrelor

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
27937053

Sources:
PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Binding data obtained using washed platelets in 96-well plates, with [<sup>125</sup>I]-P2Y<sub>12</sub> antagonist as radioligand.

Direct Interaction? True

Endogenous Drug? False

PMIDs:
17980251 17827008 24951432 26063049

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
25935875

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
25935875

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
25935875

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
26151596

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
25935875

Sources:
PharmGKB

Drug Info:

Drug Indications antithrombotic

Drug Class small molecule

FDA Approval approved

Alternate Names:

TICAGRELOR GuideToPharmacology Ligand Name