Hepatic drug transport studies

Rapid hepatic uptake and extensive biliary clearance affect the therapeutic potential of many drug candidates. In particular, hepatic transport is important to drug delivery (targeting the hepatic system), drug metabolism (liver uptake and metabolic enzyme accessibility), biliary clearance (systemic bioavailability effects), inter-individual differences (pharmacogenetic concerns) and inhibition of transporters (drug-drug interaction and safety concerns). In this white paper, Qualyst Inc. offers a mini-review of hepatic drug transport studies.

Until recently, investigations of hepatic disposition were limited to in vivo or complex ex vivo studies. Now, however, several means can be used to assess drug transporter specificity and hepatobiliary disposition of drug candidates and metabolites. These include the use of recombinant expression techniques and sandwich-cultured hepatocytes.

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