Strategies for the prediction of in vivo drug clearance from in vitro drug metabolite kinetic
data are well established for the rat. In this animal species, metabolism rate-substrate …

Bilirubin, a breakdown product of heme, is normally glucuronidated and excreted by the
liver into bile. Failure of this system can lead to a buildup of conjugated bilirubin in the blood, …

Organic anion transporting polypeptides (OATPs) are uptake transporters for a broad range
of endogenous compounds and xenobiotics. To investigate the physiologic and …

Purpose To apply physiologically-based pharmacokinetic (PBPK) modeling to investigate
the consequences of reduction in activity of hepatic and intestinal uptake and efflux …

Some substrates of cytochrome P450 (CYP) 3A4, the most abundant CYP in the human liver
responsible for the metabolism of many structurally diverse therapeutic agents, do not obey …

Purpose: Organic anion-transporting polypeptide (OATP) drug uptake transporters are
thought to play an important role in drug pharmacokinetics and toxicokinetics. We aimed to …

Interindividual variability in activity of uptake transporters is evident in vivo, yet limited data
exist in vitro, confounding in vitro-in vivo extrapolation. The uptake kinetics of seven organic …

Human organic anion-transporting polypeptide 1B1 (OATP1B1) is an important hepatic
uptake transporter that can transport a wide variety of drugs. In the present study, we have …

Kinetic parameters describing hepatic uptake in hepatocytes are frequently estimated
without appropriate incorporation of bidirectional passive diffusion, intracellular binding, and …

Purpose: Organic anion-transporting polypeptides (OATP) mediate the cellular uptake of a
broad range of drugs. The hydrophobic anticancer drug, paclitaxel (PTX), was recently …