The Impact of ABCB1 and CES1 Polymorphisms on Dabigatran Pharmacokinetics in Healthy Chinese Subjects

• DOI: 10.2147/pgpm.s291723
• Publication Date: 2021-04-22T22:48:05Z
• Authors: Yue Liu; Chenguang Yang; Wenyuan Qi; Zuowei Pei; Wei Xue; Huolan Zhu; Min Dong; Ying Guo; Duanduan Cong; Fang Wang
• Keywords: Crossover study; Oral anticoagulant

Abstract: Dabigatran is a novel direct oral anticoagulant agent, whose plasma concentration closely related to bleeding risk. Genetic polymorphisms can affect the level of dabigatran. The purpose this study was understand relationship between dabigatran-related genes and dabigatran in healthy Chinese subjects after taking single dose. This performed with single-center, single-dose, randomized, open-label, four-period crossover trial design under both fasting fed conditions. A total 106 eligible were enrolled 104 genotyped. One-way analysis variance (ANOVA) used compare pharmacokinetic parameters among different genotypes linear regression applied explore multiplicative interaction variables. In study, we found that genotype frequencies CES1 rs2244613 rs8192935 significantly Caucasians, but ABCB1 rs1045642 rs4148738 similar populations. associated peak There no significant gender difference exposure Furthermore, food delayed absorption had little effect on C max AUC 0-∞ . Keywords: anticoagulants, dabigatran, genetics, pharmacogenetics, CES1,