Phase<scp>I</scp>and<scp>II</scp>metabolism and<scp>MRP</scp>2‐mediated export of bosentan in a<scp>MDCKII</scp>‐<scp>OATP1B1‐CYP3A4‐UGT1A1‐MRP2</scp>quadruple‐transfected cell line

Abstract

These in vitro data indicate that bosentan is a substrate of UGT1A1. Moreover, the efflux transporter MRP2 mediates export of bosentan and most likely also of bosentan glucuronide in the cell system. Taken together, cell lines simultaneously expressing transport proteins and metabolizing enzymes represent additional useful tools for the investigation of the interplay of transport and metabolism of drugs.