TABLE 5

Drug transporter inhibition

TransporterTest SystemCRV431 IC50 (µM)CsA IC50 (µM)CRV431 Inhibitory Potency vs. CsA
P-gpCaco-2>501>50× less
BCRPMDCKII-BCRP2337.7× less
BSEPVesicles1.420.423.4× less
MRP2Vesicles20.7102.1× less
OATP1B1HEK2930.30.047.5× less
OATP1B3HEK2930.60.087.5× less
OAT1HEK293>50>50Same (no inhibition)
OCT2HEK293>50>50Same (no inhibition)
OAT3HEK2930.473>10>21× more
NTCPHEK29345.31>45× less
MATE-1HEK293>100>100Same (no inhibition)
MATE-2HEK293>100>100Same (no inhibition)
  • BCRP, breast cancer resistance protein; HEK, human embryonic kidney; MATE, multidrug and toxin extrusion; MDCK, Madin–Darby canine kidney; OCT, organic cation transporter; P-gp, permeability-glycoprotein.