Abstract

Effects of Renal Impairment and Chronic Hemodialysis on the Pharmacokinetics, Pharmacodynamics and Safety of Rivaroxaban

Rivaroxaban is a potent, direct oral Factor Xa inhibitor with high oral bioavailability, predictable pharmacokinetics (PK), and a rapid onset and offset of action. Inhibiting Factor Xa blocks thrombin generation and subsequently thrombin-mediated activation of coagulation. Rivaroxaban has a dual mode of elimination, in which approximately two-thirds of the absorbed dose is hepatically metabolized through oxidative and hydrolytic pathways then excreted as inactive metabolites in both the urine and the feces. The remaining third of the absorbed dose is eliminated as unchanged drug in the urine via P-gp-mediated and ABCG2 (also abbreviated as Bcrp for breast cancer resistance protein)-mediated secretion. Considering the percentage of the administered dose renally eliminated by direct renal excretion as unchanged drug in the urine, the pharmacokinetic (PK) and pharmacodynamic (PD) changes that may occur in a renally impaired population were assessed. This assessment consisted of two Clinical Pharmacology studies that were conducted in subjects with various degrees of renal impairment. This review highlights the findings of these two studies.


Author(s): Maria Langas and Kenneth Todd Moore*

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