Dabigatran acylglucuronide, an active metabolite of dabigatran, exhibits higher plasma concentrations and distinct anticoagulant effects compared to dabigatran, suggesting that it may play a more significant role in overall anticoagulant activity than previously assumed. Idarucizumab, a monoclonal antibody fragment, binds to both free and thrombin-bound dabigatran, neutralizing its anticoagulant effects. However, its efficacy in reversing anticoagulation induced by dabigatran acylglucuronide remains unclear.
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January 2025
Background: Dabigatran etexilate (DABE), a prodrug of dabigatran (DAB), is a direct thrombin inhibitor used to prevent ischemic stroke and thromboembolism during atrial fibrillation. The effect of genetic polymorphisms on its metabolism, particularly , has not been extensively explored in humans. This study aimed to investigate the effects of , , and polymorphisms on the pharmacokinetics of DAB and its acylglucuronide metabolites in healthy subjects.
View Article and Find Full Text PDFPharmaceutics
April 2022