Half-Life of Ticagrelor and Its Active Metabolite
The elimination half-life of ticagrelor ranges from approximately 7 to 14.9 hours, while its active metabolite AR-C124910XX has a half-life of approximately 9 to 12 hours.
Pharmacokinetic Parameters
Based on research evidence in healthy subjects, ticagrelor demonstrates the following half-life characteristics:
- Ticagrelor parent compound: Mean elimination half-life of 10.9-14.9 hours after both single and multiple doses 1
- AR-C124910XX (active metabolite): Mean elimination half-life of 9.1-11.9 hours 1
A drug interaction study showed slightly shorter values, with ticagrelor half-life of 6.7 hours under control conditions, which was minimally prolonged to 7.2 hours with grapefruit juice co-administration 2.
Clinical Implications
Steady-State Achievement
Both ticagrelor and its active metabolite reach steady-state concentrations rapidly with twice-daily dosing, typically within the first few days of treatment 1. This relatively short half-life supports the twice-daily dosing regimen used clinically.
Time to Peak Concentration
- Ticagrelor is rapidly absorbed with median time to maximum concentration (Tmax) of 2 hours 1
- The active metabolite AR-C124910XX is rapidly formed with median Tmax of 2.0-3.0 hours 1
Important Caveats
Special populations may exhibit altered pharmacokinetics:
- Patients on VA-ECMO show reduced ticagrelor clearance and increased volume of distribution 3
- Female subjects demonstrate shorter half-life compared to males 4
- Food intake prolongs half-life and reduces clearance 4
The predictable and linear pharmacokinetics across the therapeutic dose range (90-180 mg) make ticagrelor's elimination profile consistent and reliable for clinical use 1.