438 and references

Transport proteins mediating the uptake and ef-flux of small molecules across hepatocellular mem-brane domains are key determinants of hepatobiliary elimination, and thus of the half-life of many drugs and endogenous substances in blood plasma. Uptake transporters with overlapping substrate specificity and localized to the basolateral (sinusoidal) membra-ne of human hepatocytes include the organic anion transporters OATP1B3 (OATP8), OATP1B1 (OATP-C), and OATP2B1 (OATP-B). Subsequent to the uptake of drugs and possible phase I and pha-se II reactions, the necessary and final step in elimi-nation and detoxification is predominantly mediated by members of the multidrug resistance protein sub-family of ABC transporters (MRPs or ABCCs), par