Ticagrelor

Ticagrelor, sold under the brand name Brilinta among others, is a medication used for the prevention of stroke, heart attack and other events in people with acute coronary syndrome, meaning problems with blood supply in the coronary arteries. It acts as a platelet aggregation inhibitor by antagonising the P2Y12 receptor. The drug is produced by AstraZeneca.

Ticagrelor
Clinical data
Trade namesBrilinta, Brilique, others
Other namesAZD-6140
AHFS/Drugs.comMonograph
MedlinePlusa611050
License data
Pregnancy
category
  • AU: B1
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • US: WARNINGRx-only
  • EU: Rx-only
Pharmacokinetic data
Bioavailability36%
Protein binding>99.7%
MetabolismLiver (CYP3A4)
Elimination half-life7 hrs (ticagrelor), 8.5 hrs (active metabolite AR-C124910XX)
ExcretionBile duct
Identifiers
  • (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
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.114.746
Chemical and physical data
FormulaC23H28F2N6O4S
Molar mass522.57 g·mol−1
3D model (JSmol)
  • CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(F)c(F)c2)c2nnn([C@@H]3C[C@H](OCCO)[C@@H](O)[C@H]3O)c2n1
  • InChI=1S/C23H28F2N6O4S/c1-2-7-36-23-27-21(26-15-9-12(15)11-3-4-13(24)14(25)8-11)18-22(28-23)31(30-29-18)16-10-17(35-6-5-32)20(34)19(16)33/h3-4,8,12,15-17,19-20,32-34H,2,5-7,9-10H2,1H3,(H,26,27,28)/t12-,15+,16+,17-,19-,20+/m0/s1 N
  • Key:OEKWJQXRCDYSHL-FNOIDJSQSA-N N
 NY (what is this?)  (verify)

The most common side effects include dyspnea (difficulty breathing), bleeding and raised uric acid level in the blood.

It was approved for medical use in the European Union in December 2010, and in the United States in July 2011. In 2020, it was the 247th most commonly prescribed medication in the United States, with more than 1 million prescriptions.

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