School of Biotechnology and Pharmaceutical Engineering, West Anhui University, Moon Island, West of Yunlu Bridge, Lu'an, 237012, People's Republic of China.
Anhui Engineering Laboratory for Conservation and Sustainable Utilization of Traditional Chinese Medicine Resource, Lu'an, 237012, Anhui, People's Republic of China.
Eur J Drug Metab Pharmacokinet. 2024 Jan;49(1):33-42. doi: 10.1007/s13318-023-00867-z. Epub 2023 Nov 24.
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).
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.
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.
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.
血小板在与急性冠脉综合征（ACS）相关的血栓事件中起着关键作用，使口服抗血小板治疗成为抗血栓策略的基石。需要评估口服抗血小板药物替格瑞洛的剂量方案，以确保其在临床实践中的适当性。因此，本研究旨在通过确定接受经皮冠状动脉介入治疗（PCI）的中国患者替格瑞洛的最佳治疗浓度来研究替格瑞洛在真实世界中的临床应用。
我们纳入了 912 例接受药物洗脱支架置入术治疗 ACS 的 PCI 患者的队列。我们使用高效液相色谱-串联质谱法测定稳态血浆药物浓度。基于临床药效学指标确定稳态时替格瑞洛的治疗药物浓度范围，并通过浓度-效应分析和受试者工作特征曲线评估来验证可靠性。
分析 912 例患者的血浆样本显示，替格瑞洛的稳态谷浓度与性别、年龄、高血压和高脂血症等因素显著相关。基于此分析，确定了稳态谷浓度的最佳治疗范围为 240.65-335.83ng/ml。此外，稳态浓度的上限值分别为男性 439.97ng/ml 和女性 347.06ng/ml。
本研究为中国经皮冠状动脉介入治疗后患者替格瑞洛的最佳治疗稳态谷浓度提供了有力且可靠的见解。这些发现对指导抗血小板药物的合理使用以及促进中国经皮冠状动脉介入治疗患者的精确药物管理具有重要意义。
