TABLE 5

Hepatic OATP inhibition interactions, in vitro to in vivo translation

PerpetratorOATPIn Vitro SubstrateIC50Cmax/IC50AUC RatioCmax RatioIn Vivo VictimReference
µM
Brexpiprazole1B1Estradiol 17-β-glucuronide8.390.05N/TFDA (2015v)
Brexpiprazole metabolite DM-34111B1Estradiol 17-β-glucuronide9.130.01N/T
Cobimetinib1B1Estrone-3-sulfate118<0.1N/TFDA (2015h)
1B3Fluo-385<0.1N/T
Daclatasvir1B1BMS-7915532.31.02a,b1.471.84RosuvastatinFDA (2015j)
1B3Cholecystokinin octapeptide5.70.41a,b
Deoxycholic acid1B1N/PN/P0.14bN/T, R < 1.25FDA (2015p)
1B3N/PN/P0.11bN/T, R < 1.25
Edoxaban1B1N/P62.70.01aN/TFDA (2015w)
1B3N/P50.80.01aN/T
Eluxadoline1B1Estradiol 17-β-glucuronide32.6% at 400 ng/mlN/A1.411.18RosuvastatinFDA (2015zc)
Isavuconazonium sulfate1B1N/P11.21.53a,b1.401.05AtorvastatinFDA (2015i)
Lenvatinib1B1Estradiol 17-β-glucuronide7.290.21a,bN/TFDA (2015q)
Lesinurad1B1N/P9.31.8b1.011.17AtorvastatinFDA (2015zg)
1B3N/P43.10.4b
Osimertinib1B1N/P220.05N/TFDA (2015x)
1B3N/P52.50.02N/T
Panobinostat1B1N/PN/PN/T, R = 1FDA (2015l)
Sacubitril1B1N/P1.93.11b1.301.75AtorvastatinFDA (2015k)
1B3N/P3.81.55a,b
Sacubitril metabolite LBQ6571B1N/P126N/A
Selexipag1B1Atorvastatin2.40.01aN/TFDA (2015z)
1B3Taurocholic acid1.70.02aN/T
Selexipag metabolite ACT-3336791B1Atorvastatin3.5N/AN/T
1B3Taurocholic acid4.1N/AN/T
Tenofovir alafenamide fumarate1B1Fluo-329.8% at 100 µMN/AFDA (2015m)
1B3Fluo-325.5% at 100 µMN/A
  • N/A, not applicable; N/P, not provided; N/T, not tested.

  • a Ratio was calculated by the University of Washington Drug Interaction Database editorial team.

  • b Values exceed the FDA cut-off value of 0.1.