Ticagrelor Steady-State Trough Concentration in Chinese Patients Undergoing Percutaneous Coronary Intervention

Eur J Drug Metab Pharmacokinet. 2024 Jan;49(1):33-42. doi: 10.1007/s13318-023-00867-z. Epub 2023 Nov 24.

Abstract

BACKGROUND AND OBJECTIVE: Platelets play a pivotal role in thrombotic events associated with acute coronary syndrome (ACS), making oral antiplatelet therapy a cornerstone in antithrombotic strategies. The dosing regimen for the oral antiplatelet drug ticagrelor warrants evaluation to ensure its appropriateness in clinical practice. Therefore, this study aimed to investigate the real-world clinical application of ticagrelor by determining the optimal therapeutic concentration of ticagrelor in Chinese patients undergoing percutaneous coronary intervention (PCI).

Methods: We enrolled a cohort of 912 patients who underwent PCI with drug-eluting stent implantation for the treatment of ACS. We measured steady-state plasma drug concentrations using high-performance liquid chromatography-tandem mass spectrometry. The therapeutic drug concentration range at steady state was established on the basis of clinical pharmacodynamic indices, with verification of reliability through concentration-effect analysis and receiver operating characteristic curve assessment.

Results: Analysis of plasma samples from the 912 patients revealed significant variations in the steady-state trough concentration of ticagrelor associated with factors such as gender, age, hypertension, and hyperlipidemia. On the basis of this analysis, the optimal therapeutic range for steady-state trough concentration was determined to be 240.65-335.83 ng/mL. Furthermore, the upper limit values for steady-state concentration were established at 439.97 ng/mL for male patients and 347.06 ng/mL for female patients.

Conclusions: This study provides robust and reliable insights into the optimal therapeutic steady-state trough concentrations of ticagrelor in Chinese patients with post-percutaneous coronary intervention. These findings have significant implications for guiding the rational use of antiplatelet drugs and facilitating precise drug administration in Chinese patients undergoing percutaneous coronary intervention.

MeSH terms

  • Acute Coronary Syndrome* / drug therapy
  • Acute Coronary Syndrome* / etiology
  • Acute Coronary Syndrome* / surgery
  • China
  • Drug-Eluting Stents*
  • Female
  • Humans
  • Male
  • Percutaneous Coronary Intervention* / adverse effects
  • Percutaneous Coronary Intervention* / methods
  • Platelet Aggregation Inhibitors / therapeutic use
  • Reproducibility of Results
  • Ticagrelor / adverse effects
  • Treatment Outcome

Substances

  • Ticagrelor
  • Platelet Aggregation Inhibitors