Incubation Time Influences Organic Anion Transporter 1 Kinetics and Renal Clearance Predictions.

ABSTRACT: Accurate predictions of drug uptake transporter involvement in renal excretion of xenobiotics require determination of in vitro transport kinetic parameters under initial-rate conditions. The purpose of the present study was to determine how changing the incubation time from initial rate to steady state influences ligand interactions with the renal organic anion transporter 1 (OAT1), and the impact of the different experimental conditions on pharmacokinetic predictions. Transport studies were performed with Chinese hamster ovary cells expressing OAT1 (CHO-OAT1) and the Simcyp Simulator was used for physiological-based pharmacokinetic predictions. Maximal transport rate and intrinsic uptake clearance (CL_int) for PAH decreased with increasing incubation time. The CL_int

SUBMITTER: Buaben AO 

PROVIDER: S-EPMC10204490 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature