To improve the present bioartificial liver systems by adding the capacity for selective and active transport, recombinant hepatic GS-HepG2 and renal proximal convoluted tubular cell line-multidrug resistant (PCTL-MDR) cell lines were cocultured on opposite sides of a expanded polytetrafluoroethylene (ePTFE) membrane, and active transport and drug metabolism were examined. PCTL-MDR formed a tight monolayer on the ePTFE membrane to block nonspecific leakage of polysaccharide, while the cells transported anionic digoxin from the membrane side to the medium side. GS-HepG2 cells showed a capacity for testosterone metabolism, and the metabolite, probably androstenedione, as well as testosterone, was transported by PCTL-MDR. The combination of hepatic and renal cell lines in the appropriate bioreactor vessel will enable bioartificial hemofiltration, which has not been achieved with the present bioartificial liver assist systems.