Ticagrelor

Ticagrelor
Clinical data


Trade names	Brilinta, Brilique, Possia
AHFS/Drugs.com	Monograph
MedlinePlus	a611050
License data	EU EMA: Brilique US FDA: Ticagrelor
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	by mouth
ATC code	B01AC24 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	36%
Protein binding	>99.7%
Metabolism	Hepatic (CYP3A4)
Biological half-life	7 hrs (ticagrelor), 8.5 hrs (active metabolite AR-C124910XX)
Excretion	Biliary
Identifiers
IUPAC name (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
Synonyms	AZD-6140
CAS Number	274693-27-5^Y
PubChem CID	9871419
IUPHAR/BPS	1765
ChemSpider	8047109^N
UNII	GLH0314RVC
KEGG	D09017^Y
ChEMBL	CHEMBL398435^N
ECHA InfoCard	100.114.746
Chemical and physical data
Formula	C₂₃H₂₈F₂N₆O₄S
Molar mass	522.567 g/mol
3D model (Jmol)	Interactive image
SMILES CCCSC1=NC(=C2C(=N1)N(N=N2)[C@@H]3C[C@@H]([C@H]([C@H]3O)O)OCCO)N[C@@H]4C[C@H]4C5=CC(=C(C=C5)F)F
InChI 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?)

Ticagrelor (trade name Brilinta, Brilique, and Possia) is a platelet aggregation inhibitor produced by AstraZeneca.

Ticagrelor is an antagonist of the P2Y₁₂ receptor.

The drug was approved for use in the European Union by the European Commission on December 3, 2010. The drug was approved by the US Food and Drug Administration on July 20, 2011.

Ticagrelor is used for the prevention of thrombotic events (for example stroke or heart attack) in people with acute coronary syndrome or myocardial infarction with ST elevation. The drug is combined with acetylsalicylic acid unless the latter is contraindicated. There is no high quality evidence for the use of ticagrelor in non-ST elevation acute coronary syndrome.

The FDA indication for ticagrelor is reduction of the rate of cardiovascular death, myocardial infarction (MI), and stroke in people with acute coronary syndrome or history of myocardial infarction.

AHA/ACC Guidelines (09/2014) state: "It is reasonable to choose ticagrelor over clopidogrel for P2Y12 inhibition treatment in patients with NSTE-ACS treated with early invasive strategy and/or coronary stenting".

Ticagrelor was found to be comparable to acetylsalicylic acid in people with acute ischemic stroke or transient ischemic attack.

Contraindications for ticagrelor are: active pathological bleeding and a history of intracranial bleeding, as well as reduced liver function and combination with drugs that strongly influence activity of the liver enzyme CYP3A4, because the drug is metabolized via CYP3A4 and excreted via the liver.

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