Metabolism and excretion of rivaroxaban, an oral, direct factor Xa inhibitor, in rats, dogs, and humans.

Title page Metabolism and excretion of rivaroxaban – an oral, direct Factor Xa inhibitor – in rats, dogs and humans

Running title: Metabolism of rivaroxaban in vivo (33/60 characters) Abbreviations: AUC, area under the concentration–time curve; AUC norm , AUC normalized to rivaroxaban dose and body weight ; AUC 0–tn , AUC from 0 to the terminal time point; This article has not been copyedited and formatted. The final version may differ from this version. Abstract Rivaroxaban is a novel, oral, direct Factor X...

In vitro metabolism of rivaroxaban, an oral, direct factor Xa inhibitor, in liver microsomes and hepatocytes of rats, dogs, and humans.

The in vitro metabolism of rivaroxaban, a novel, oral, direct factor Xa inhibitor for the prevention and treatment of thromboembolic disorders, was investigated in several species, including humans. The objective of this study was to elucidate metabolite structures and identify the metabolic pathways to provide support for in vivo safety and clinical studies. [(14)C]Rivaroxaban was incubated wi...

Comparative metabolism of 14C-labeled apixaban in mice, rats, rabbits, dogs, and humans.

The metabolism and disposition of [(14)C]apixaban, a potent, reversible, and direct inhibitor of coagulation factor Xa, were investigated in mice, rats, rabbits, dogs, and humans after a single oral administration and in incubations with hepatocytes. In plasma, the parent compound was the major circulating component in mice, rats, dogs, and humans. O-Demethyl apixaban sulfate (M1) represented a...

Title page In vitro metabolism of rivaroxaban – an oral, direct Factor Xa inhibitor – in liver microsomes and hepatocytes of rat, dog and man

The discovery of rivaroxaban: translating preclinical assessments into clinical practice

Direct oral anticoagulants that target a single coagulation factor (such as factor Xa or thrombin) have been developed in recent years in an attempt to address some of the limitations of traditional anticoagulants. Rivaroxaban is an oral, direct factor Xa inhibitor that inhibits free and clot-bound factor Xa and factor Xa in the prothrombinase complex. Preclinical studies demonstrated a potent ...