Pharmacokinetic and pharmacodynamic analysis of oral direct inhibitors of activated coagulation factor X for application to individualized pharmacotherapy

2016 Fiscal Year Final Research Report

• Project/Area Number: 15K18938
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: Ritsumeikan University
• Principal Investigator: Ueshima Satoshi 立命館大学, 薬学部, 助教 (70734771)
• Research Collaborator: Katsura Toshiya 立命館大学, 薬学部, 教授 (10283615) ; Terada Tomohiro 滋賀医科大学, 医学部, 教授 (10324641) ; Horie Minoru 滋賀医科大学, 医学部, 教授 (90183938) ; Hira Daiki 滋賀医科大学, 医学部, 特任助教 (50636959)
• Project Period (FY): 2015-04-01 – 2017-03-31
• Keywords: 第Xa因子阻害薬 / 母集団薬物速度論 / PK/PD解析 / 薬理ゲノム解析 / 個別化投与設計

Outline of Final Research Achievements

Apixaban, an oral direct inhibitor of activated coagulation factor X (FXa), is used to prevent stroke or systemic embolism in patients. This study aimed to evaluate the influences of characteristics of patients and genetic variants in drug transporters (ABCB1 and ABCG2) and enzyme (CYP3A5) on pharmacokinetics and pharmacodynamics of apixaban. The population pharmacokinetic and pharmacodynamic analysis using clinical data from patients showed that genetic variants of ABCG2 and CYP3A5　as well as renal function and body weight and were intrinsic factors of apixaban pharmacokinetics. This analysis also indicated that pharmacological activities of apixaban were stronger in patients with a history of cancer than those without a history of cancer.

Free Research Field

医療薬学