Ticagrelor
Brand: Brilinta (US/EU) / Ticawell (IN) / Ticaflo (IN) / Ticadro (BD)
Antiplatelet
P2Y12 inhibitor (reversible, not a prodrug)
Pharmacokinetics
| Half-life | 7 hours |
| Tmax | 1.5 h |
| Bioavailability | 36 % (approx) |
| Protein Binding | 99 % |
| Volume of Distribution | 0.08 L/kg (approx) |
| Clearance Route | hepatic |
| Active Metabolites | yes |
| Notes | Not a prodrug; CYP3A4 substrate; twice-daily dosing; avoids clopidogrel resistance due to CYP2C19 polymorphism. | Updated 2025: Recent guideline analysis supports monotherapy option post-ACS for reduced bleeding; meta-analysis (AHA 2025) notes higher bleeding risk vs older P2Y₁₂ inhibitors; BMJ 2024 investigation raised concerns about PLATO trial data integrity. | Updated 2025: Guideline analysis supports monotherapy option post-ACS for reduced bleeding; meta-analysis confirms higher bleeding risk vs clopidogrel; BMJ investigation raised questions about PLATO trial data. References: https://www.jacc.org/doi/10.1016/j.jacc.2025.04.046 , https://www.bmj.com/content/384/bmj.q107 |