Ticagrelor

Ticagrelor
Clinical data
Trade namesBrilinta, Brilique, others
Other namesAZD-6140
AHFS/Drugs.comMonograph
MedlinePlusa611050
License data
Pregnancy
category
Routes of
administration		By mouth
ATC code
Legal status
Legal status
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 Edit this at Wikidata
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
 ☒NcheckY (what is this?)  (verify)

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.[7] The drug is produced by AstraZeneca.

90 mg tablet of Brilinta

The most common side effects include dyspnea (difficulty breathing), bleeding and raised uric acid level in the blood.[6]

It was approved for medical use in the European Union in December 2010,[6][8][9] and in the United States in July 2011.[5][10][11] In 2020, it was the 247th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[12][13]

  1. ^ "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 12 May 2022. Retrieved 13 May 2022.
  2. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  3. ^ "Ticalor; Blooms The Chemist Ticagrelor; Apo-Ticagrelor; Ticagrelor Arx (Accelagen Pty Ltd)". Therapeutic Goods Administration (TGA). 11 November 2022. Retrieved 9 April 2023.
  4. ^ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  5. ^ a b "Brilinta- ticagrelor tablet". DailyMed. 10 August 2021. Retrieved 19 May 2022.
  6. ^ a b c "Brilique EPAR". European Medicines Agency. 17 September 2018. Retrieved 18 May 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  7. ^ Jacobson KA, Boeynaems JM (July 2010). "P2Y nucleotide receptors: promise of therapeutic applications". Drug Discovery Today. 15 (13–14): 570–578. doi:10.1016/j.drudis.2010.05.011. PMC 2920619. PMID 20594935.
  8. ^ "Assessment Report for Brilique" (PDF). European Medicines Agency. January 2011. Archived from the original (PDF) on 17 May 2018. Retrieved 3 February 2011.
  9. ^ "European Public Assessment Report Possia". Archived from the original on 12 June 2018. Retrieved 24 January 2011.
  10. ^ "FDA approves blood-thinning drug Brilinta to treat acute coronary syndromes" (Press release). U.S. Food and Drug Administration (FDA). 20 July 2011. Archived from the original on 12 January 2017.
  11. ^ "Drug Approval Package: Brilinta (ticagrelor) NDA #022433". U.S. Food and Drug Administration (FDA). 22 August 2011. Retrieved 22 May 2021.
  12. ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  13. ^ "Ticagrelor - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.