Characterizing Apixaban Pharmacokinetics Through Physiologically-Based Pharmacokinetic Modeling: Critical Role of Biliary Secretion and Enterohepatic Circulation in Humans.

ABSTRACT: Apixaban, a factor Xa inhibitor, is a direct oral anticoagulant with a well-balanced elimination; it is eliminated evenly via feces, urine (with no active secretion), and as metabolites after oral administration. The common understanding is that biliary secretion and enterohepatic circulation (EHC) of apixaban are limited in humans, and that fecal excretion may be attributable to intestinal secretion. However, a decrease in apixaban blood concentration with activated charcoal coadministration in humans suggests possible involvement of EHC. This study aimed to evaluate the contribution of biliary excretion, EHC, and intestinal secretion to apixaban pharmacokinetics (PK) using a physiologically-based pharmacokinetic (PBPK) model. A top-down analysis was performed using blood concentration an

SUBMITTER: Tsuchitani T 

PROVIDER: S-EPMC12823302 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature