Repositioning Candidate Details

Candidate ID: R1157
Source ID: DB08816
Source Type: approved
Compound Type: small molecule
Compound Name: Ticagrelor
Synonyms: (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; Ticagrelor
Molecular Formula: C23H28F2N6O4S
SMILES: CCCSC1=NC2=C(N=NN2[C@@H]2C[C@H](OCCO)[C@@H](O)[C@H]2O)C(N[C@@H]2C[C@H]2C2=CC(F)=C(F)C=C2)=N1
Structure:
DrugBank Description: Ticagrelor, or AZD6140, was first described in the literature in 2003. Ticagrelor is an ADP derivative developed for its P2Y<sub>12</sub> receptor antagonism. Unlike , ticagrelor is not a prodrug. It is marketed by Astra Zeneca as Brilinta in the US and Brilique or Possia in the EU,. Ticagrelor was granted EMA approval on 3 December 2010. Ticagrelor was granted FDA approval on 20 July 2011.
CAS Number: 274693-27-5
Molecular Weight: 522.568
DrugBank Indication: Ticagrelor is indicated to reduce the risk of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome or a history of myocardial infarction. Ticagrelor is also indicated to reduce the risk of a first myocardial infarction or stroke in high risk patients with coronary artery disease.
DrugBank Pharmacology: Ticagrelor is a P2Y<sub>12</sub> receptor antagonist that inhibits the formation of thromboses to reduce the risk of myocardial infarction and ischemic stroke. It has a moderate duration of action as it is given twice daily, and a wide therapeutic index as high single doses are well tolerated. Patients should be counselled regarding the risk of bleeding, dyspnea, and bradyarrhythmias.
DrugBank MoA: Ticagrelor is a P2Y<sub>12</sub> receptor antagonist. The P2Y<sub>12</sub> receptor couples with Gα<sub>i2</sub> and other G<sub>i</sub> proteins which inhibit adenylyl cyclase. G<sub>i</sub> mediated signalling also activates PI3K, Akt, Rap1b, and potassium channels. The downstream effects of these activities mediate hemostasis and lead to platelet aggregation. Antagonism of the P2Y<sub>12</sub> receptor reduces development of occlusive thromboses, which can reduce the risk of myocardial infarction and ischemic stroke.
Targets: P2Y purinoceptor 12 inhibitor
Inclusion Criteria: Therapeutic strategy associated