TABLE 2

Hepatic transporters involved in parent drug and metabolite pairs

Drugs and MetabolitesBasolateral Uptake TransportersBasolateral Efflux TransportersCanalicular Efflux TransportersReferences
BilirubinOATP1B1, OATP1B3NANALengyel et al. (2005); van de Steeg et al. (2012;, Chang et al. (2013)
Bilirubin mono/diglucuronideOATP1B1Mrp1, MRP3BCRP, MRP2/Mrp2
DiclofenacNot substrate of either OATP1B1, OATP1B3, or OATP2B1Not substrate of MRP3Not substrate of either BCRP or MRP2Zhang et al. (2016)
Diclofenac acyl glucuronideOATP1B1, OATP2B1MRP3BCRP, MRP2
EnalaprilOATP1B1, OATP1B3Not substrate of either MRP3 or MRP4MRP2/Mrp2Liu et al. (2006); Ferslew et al. (2014)
EnalaprilatNAMRP4MRP2/Mrp2
EzetimibeNot substrate of either OATP1B1, OATP1B3 or OATP2B1NANot substrate of MRP2Oswald et al. (2008); Fahrmayr et al. (2012)
Ezetimibe glucuronideOATP1B1, OATP2B1NAMRP2
IrinotecanNot substrate of OATP1B1NAP-gp, MRP2Nozawa et al. (2005); Di Martino et al. (2011)
SN-38OATP1B1NABCRP, P-gp, MRP2
SN-38 glucuronideNot substrate of OATP1B1NAMRP2
MorphineOCT1Not substrate of MRP3P-gpTzvetkov et al. (2013); Venkatasubramanian et al. (2014)
Morphine 6-glucuronideNAMRP3P-gp, MRP2
ParoxetineNANANAMatsunaga et al. (2013)
M1-glucuronideNANAMRP2/Mrp2
M1-sulfateNANANot substrate of either MRP2/Mrp2, BCRP/Bcrp, or BSEP/Bsep
Mycophenolate mofetilNANANAPicard et al. (2010); Matsunaga et al. (2014); Tetsuka et al. (2014b)
Mycophenolic acid (MPA)Not substrate of OATPsNANA
MPA phenyl-glucuronide (MPAG)OATP1B1, OATP1B3MRP3, MRP4MRP2/Mrp2
TroglitazoneNANANAEnokizono et al. (2007); Lee et al. (2010)
Troglitazone sulfateOATP1B1Mrp3, Mrp4BCRP, MRP2
  • NA, not applicable; SN-38, 7-ethyl-10-hydroxycamptothecin.